药学实践与服务

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Synthesis of paclitaxel palmitate and the formulation optimization of its liposomes 紫杉醇棕榈酸酯的合成及其脂质体的制备与处方研究

CHEN Bingchen, WANG Sizhen, GUO Beibei, YANG Feng

2024, 42(9): 379-384, 410. doi: 10.12206/j.issn.2097-2024.202404062

Objective To improve the cellular uptake efficiency and the therapeutic effect through the structural modification of paclitaxel （PTX） and the preparation of corresponding liposomes. Methods The prodrug of paclitaxel, PTX-PA, was prepared by esterification reaction, and the quantitative detection method of PTX-PA was established. Next,the optimal formulation and preparation of PTX-PA/Lip was obtained through single factor screening based on their appearance, particle size, and encapsulation efficiency. Results The PTX-PA was successfully synthesized, and the established HPLC quantitative analysis method for PTX-PA met the methodological requirements. After the optimal preparation and formulation research through single factor screening, the particle size of optimized PTX-PA/Lip was （62.75±1.81） nm with a PDI of （0.076±0.02）, while the drug encapsulation rate reached more than 90%. Conclusion This research successfully prepared palmitic acid modified paclitaxel liposomes based on nanotechnology, enhancing the drug delivery efficiency of paclitaxel and laying the foundation for the pharmacodynamics research of PTX-PA. More>>

Establishment of mouse model of hand-foot syndrome induced by capecitabine 卡培他滨致小鼠手足综合征模型的建立及评价

WANG Peng, CHEN Shun, ZHAO Yi, GAO Shouhong, et al

2024, 42(9): 385-388, 398. doi: 10.12206/j.issn.2097-2024.202308045

Objective Hand-foot syndrome is a dose-limiting toxicity of capecitabine. At present, there is no unified gold standard for the establishment of hand-foot syndrome model. To induce hand-foot syndrome and provide a reference for the establishment of hand-foot syndrome model by administering capecitabine in ICR mice. Methods 42 male ICR mice were randomly divided into control group (6 mice) and experimental group (36 mice). The experimental group was given capecitabine (275 mg/kg, twice/d) by intragastric administration for two weeks, and the control group was given 0.5% CMC-Na (4 ml/kg, twice/d), to evaluate whether the animal model of hand-foot syndrome was successfully constructed through H&E staining of mouse foot skin samples and observe morphological changes and the characteristic appearance of mouse foot skin. After the experiment, the mice were sacrificed, and plasma was collected to quantify the concentrations of capecitabine and metabolites. Results Control mice did not showed symptoms of hand-foot syndrome. The skin of the feet of 19 mice in the experimental group showed symptoms such as erythema and swelling, and H&E staining results showed that the plantar skin angular epidermis was thickened, and part of the keratin was exfoliated and damaged, which was considered to be hand-foot syndrome. There were no significant differences in the concentrations of capecitabine and its metabolites between mice with and without hand-foot syndrome. Conclusion The model of hand-foot syndrome induced by capecitabine in mice was successfully established. Differences in exposure levels of capecitabine and metabolites may not be the cause of hand-foot syndrome. More>>

Pharmacodynamic effects of Qiwei Zhigan prescription on non-alcoholic steatohepatitis in animal model 七味脂肝方对非酒精性脂肪性肝炎动物模型的药效学评价

YANG Jianing, ZHAO Yiying, XIAO Wei

2024, 42(9): 389-398. doi: 10.12206/j.issn.2097-2024.202404096

Objective To investigate the therapeutic effect of Qiwei Zhigan prescription on two classic animal models of non-alcoholic steatohepatitis（NASH）. Methods Methionine-choline-deficient（MCD）rat model and choline-deficient, L-amino acid-defined, high-fat and high cholesterol diet（CDAHFHC）mouse model were used. 48 rats and 96 mice were randomly divided into 6 groups: control group, model group, Qiwei Zhigan prescription group（low, medium and high dose group）, positive drug group. After 2 weeks of modeling, the drugs were administrated continuously for 28 days. The efficacy of Qiwei Zhigan prescription in the treatment of non-alcoholic steatohepatitis was evaluated by detecting the serum liver function, blood lipid biochemical index and liver tissue lipid levels of each group of animals, as well as by evaluating the liver histopathological changes. Results The gross anatomical morphology of the liver was improved by Qiwei Zhigan after oral administration of clinical equivalent dose or higher doses in two experimental animal models. The liver weight and liver index of NASH mice were reduced by the prescription. The levels of ALT, ALP and LDH in serum of NASH rats were decreased, and the level of HDL was increased. The levels of ALT, AST, TBIL, ALP, LDH and TG in serum of NASH mice were decreased, and the content of TG in liver was also decreased. The pathological damage of liver tissue was ameliorated, the inflammation of liver tissue was reduced, as well as the degree of ballooning of liver cells and the NAS score of the liver, and there was a certain dose-effect relationship between the groups; the proliferation of collagen fibers in the hepatic lobules and around the portal area of NASH mice was significantly reduced; the density of positive cells labeled by F4/80 was decreased, and the activation of Kupffer cells was alleviated. Conclusion Qiwei Zhigan prescription could effectively ameliorate the progression of two classic NASH models, and decrease the development trend from liver inflammation to liver fibrosis in NASH. More>>

Determination of phosphorus content in calcium hydrogen phosphate tablets by ³¹P-qNMR 核磁共振磷谱法测定磷酸氢钙咀嚼片中药物含量

XIA Zhewei, ZENG Yuanye, ZHU Haifei, LI Yu, et al

2024, 42(9): 399-401, 406. doi: 10.12206/j.issn.2097-2024.202404063

Objective To establish a high-precision and high-specificity quantitative nuclear magnetic resonance phosphorus spectrometry method（³¹P-qNMR）for detecting the phosphorus content in calcium hydrogen phosphate chewable tablets. Methods Hexamethyl phosphoramide was used as an internal standard, phosphorus spectrum data of calcium hydrogen phosphate chewable tablets solution was collected. The linear relationship of calcium hydrogen phosphate within the concentration range of 1.0 to 9.0 mg/ml was studied, and sample recovery rate and repeatability experiments were conducted. Results Calcium hydrogen phosphate and the internal standard demonstrated a good linear relationship within the concentration range of 1.0 to 9.0 mg/ml, with a regression equation A = 0.0043 + 0.1836C. The recovery rates for low, medium, and high concentrations were 98.0%, 98.1%, and 98.4%, respectively, with relative standard deviations（RSD）of 0.31%, 0.68%, and 0.62%, respectively（n= 9）. The average content of calcium hydrogen phosphate in the chewable tablets was determined to be 98.1%. Conclusion This study successfully established a high-precision and highly specific method for quantifying the content of calcium hydrogen phosphate in chewable tablets, which did not require a self-reference substance, was simple in sample preparation, and had a fast detection speed. The method could provide a new technical support for the quality control of phosphorus-containing drugs. More>>

Simultaneous determination of five flavonoids in Ganmao’an granules by HPLC-MS/MS HPLC-MS/MS同时测定感冒安颗粒中5种黄酮成分的含量

CHEN Fangjian, LUO Jinqian, WANG Zhijun, HU Yeshuai, et al

2024, 42(9): 402-406. doi: 10.12206/j.issn.2097-2024.202403030

Objective To develop a high performance liquid chromatography-tandem mass spectrometry （HPLC-MS/MS） method for simultaneous determination of five flavonoids in Ganmao’an granules （GMA）. Methods Chromatographic separation was achieved on a Kromasil C₁₈ Column （150 mm× 4.6 mm,5 μm,100 Å）, which was eluted with methanol （A）-0.1 % formic acid （B） at the flow rate of 1.0 ml/min. The gradient condition was as follows: 0-20 min, 35% A, and 20-40 min, 45% A. The column temperature was 25 °C. Analytes were detected using a triple quadrupole tandem mass spectrometer equipped with an electrospray ionization source in the negative ion scanning. The multiple reaction monitoring mode was used for qualitative analysis. For each flavonoid, two precursor ion/product ion transitions were chosen: lutin m/z 609.1→300.1, hyperin and isoquercitrin m/z 463.0→300.1, quercetin m/z 301.0→151.0, luteolin m/z 285.0→132.9. Results Five flavonoids showed the good relationships within their own concentration ranges （correlation coefficient r>0.999 1）, whose average recoveries were in the range of 100.63 %-102.81 % with RSDs of 0.67 %-2.07 %. The content results of rutin, hyperoside, isoquercetin, quercetin, and luteolin in 10 batches of GMA were 32.23-479.83, 0.291-1.825, 11.44-20.54, 6.32-18.41, 3.46-6.51 μg/g, respectively. Conclusion The results indicated that the developed method was sensitive, accurate and could provide excellent specificity for simultaneous determination of five flavonoids in GMA. More>>

Advances in chiral analysis and stereoselective pharmacokinetics of dihydropyridine calcium antagonists 二氢吡啶类钙离子拮抗药物手性分析及其立体选择性药动学研究进展

ZHANG Yixin, GUAN Xinyi, WANG Boning, WEN Jun, et al

2024, 42(8): 319-324. doi: 10.12206/j.issn.2097-2024.202308062

Chiral drugs are closely related to the safety and effectiveness of drug use. Most dihydropyridine drugs have chiral carbon atoms, which are used as racemes and produce stereoselective disposal characteristics after entering the body, and may affect the safety and effectiveness of drugs. Therefore, based on the chiral resolution and pharmacokinetic characteristics of this class of drugs, the selection rules of chiral HPLC and CE methods and in vivo analysis applications of this class of drugs in recent years were reviewed. The stereoselective pharmacokinetics of this class of drugs were listed and compared. It was found that some of these drugs had obvious differences in stereoselective pharmacokinetics, and the pharmacokinetics and toxicity in vivo were also different. More>>

Exploration of the antidepressant mechanism of Baihe Zhimu decoction based on NLRP1 inflammasome 基于NLRP1炎症小体探讨百合知母汤抗抑郁的作用机制

YUE Chunhua, BEN Yongguang, WANG Haiqiao

2024, 42(8): 325-333. doi: 10.12206/j.issn.2097-2024.202401033

Objective To study the mechanism of antidepressant effect of Baihe Zhimu decoction based on NLRP1 inflammasome. Methods A chronic unpredictable mild stress（CUMS）induced depression mouse model was constructed. C57BL/6J mice were randomly divided into a control group, CUMS group, low-dose Baihe Zhimu decoction group, high-dose Baihe Zhimu decoction group, and MDP group（NLRP1 activator）. After continuous administration for 4 weeks, the behavioral characteristic of mice was investigated. The levels of mice hippocampal inflammatory factors IL-1β、IL-6,TNF-α, and neurotransmitters 5-HT, NE, and DA were detected by ELISA. The expression of inflammasome related proteins NLRP1, ASC, and caspase-1, as well as related proteins in BDNF/TrkB and ERK/AKT/mTOR signaling pathway were detected by Western blot. Immunofluorescence was used to detect changes in BDNF expression in the hippocampus of mice. Results Baihe Zhimu decoction inhibited the activation of NLRP1 inflammasomes in the hippocampus of CUMS mice, improved their behavioral characteristics, increased the level of neurotransmitters in the hippocampus, and reduced the inflammatory response. The NLRP1 activator MDP reversed the above effects of Baihe Zhimu decoction. Baihe Zhimu decoction increased BDNF, TrkB expression, and phosphorylation levels of ERK, AKT, and mTOR proteins, which could be reversed by MDP. Conclusion Baihe Zhimu decoction improved depression like behavior in CUMS mice by inhibiting NLRP1 inflammasome activation and hippocampal neuroinflammatory response, and thereby activating BDNF/TrkB and ERK/AKT/mTOR signaling pathway. More>>

Pharmacoeconomic evaluation of pembrolizumab versus platinum chemotherapy as first-line treatment in advanced non-small cell lung cancer 帕博利珠单抗与铂类化疗方案在晚期非小细胞肺癌一线治疗中的药物经济学评价

SONG Yutong, XIA Derun, GU Heng, TANG Shaowen, et al

2024, 42(8): 334-340. doi: 10.12206/j.issn.2097-2024.202303023

Objective To make the cost-effectiveness analysis of pembrolizumab and platinum chemotherapy as the first-line treatment for advanced non-small cell lung cancer （NSCLC） in the population with tumor proportion score （TPS） ≥ 1% of PD-L1, and provide some reference for the clinical use and future price negotiation of pembrolizumab. Methods Based on Pubmed database, the published RCT literatures of pembrolizumab were analyzed, and the survival data were extracted, combined with the treatment plan of a tertiary hospital, the Markov model were established to simulate the cost and health effectiveness of patients for twenty years, and the stability of the model was tested by one-way sensitivity analysis and probability sensitivity analysis. Results Twenty years later, the cost-effectiveness ratio of pembrolizumab group and chemotherapy group was ￥58 517.60/quality adjusted life month (QALM) and ￥41 213.08/QALM. Compared with the chemotherapy group, the incremental cost effective ratio (ICER) was ￥104 485.36/QALM. Conclusion When the willingness to pay （WTP） value was ￥30 902/QALM, the pembrolizumab therapy was not more cost-effective advantages than platinum chemotherapy, and the sensitivity analysis showed that the results of the model were relatively stable. More>>

Determination and pharmacokinetics investigation of prodrugs of paclitaxel fatty acid esters in mouse plasma by UPLC-MS/MS UPLC-MS/MS法测定小鼠血浆中紫杉醇脂肪酸酯前药及其药代动力学研究

CHEN Bingchen, TONG Dafeng, WAN Miao, YAN Feihu, et al

2024, 42(8): 341-345. doi: 10.12206/j.issn.2097-2024.202404082

Objective To establish an UPLC-MS/MS method for determinating content of three paclitaxel fatty acid esters such as paclitaxel myristate （PTX-MA）, paclitaxel palmitate （PTX-PA） and paclitaxel myristate （PTX-SA） in mouse plasma, and preliminarily investigate the pharmacokinetic characteristics of their liposomes in mice. Methods Eclipse Plus C8 chromatography column （2.1 mm×50 mm, 1.8 μm） was used with different proportions of 0.2% formic acid aqueous solution （A） and methanol （B） mixture as mobile phase for gradient elution at a flow rate of 0.3 ml/min. The collum temperature was 30℃. The sample injection volume was 10 μl. The triple quadrupole mass series spectrometer was used as multi-reaction monitoring （MRM）. Results PTX-MA, PTX-PA and PTX-SA all exhibited a good linear relationship in the range of 5.0~500.0 ng/ml （r>0.9950）. Their RSD of precision, stability, extraction recovery rate and matrix effect test results was all less than 10%. The half-lives （t_1/2） for liposomes of three paclitaxel fatty acid esters PTX-MA-L、PTX-PA-L and PTX-SA-L in mice were 14.78 h, 44.49 h and 69.32 h individually, and their clearance rates （CL） were 29.06 L·kg/h, 24.94 L·kg/h and 13.74 L·kg/h, respectively. Conclusion This method had high specificity, sensitivity, easy operation and good stability, which could be used for the determination of paclitaxel fatty acid esters in mouse plasma. The results of pharmacokinetic studies in mice showed that t_1/2 for paclitaxel fatty acid esters were significantly prolonged, and the clearance rate were significantly reduced with the length of fatty acid carbon chains increasement, which indicated that esterification of paclitaxel with different chain length saturated fatty acids could obviously alter its in vivo pharmacokinetic properties, which provided scientific basis for the research and development of nano formulations of paclitaxel fatty acid ester prodrug. More>>

Prediction of characteristic chromatogram for Abri Herba based on network pharmacology and molecular docking 基于网络药理学与分子对接预测鸡骨草特征图谱研究

ZHANG Chengzhong, ZHU Xueyan, BU Qitao, WANG Hongrui, et al

2024, 42(8): 350-358. doi: 10.12206/j.issn.2097-2024.202303048

Objective To predict the potential Q-markers of Abri Herba based on network pharmacology and molecular docking and establish a quality control characteristic. Methods The network relationship of “Abri Herba - component - target - pathway” was constructed by using a variety of databases and the method of network pharmacology. The potential Q-markers of Abri Herba were predicted and then the characteristic Chromatogram of Abri Herba was established by high performance liquid chromatography Results Through the network pharmacological prediction, it was found that the components of abrine hypaphorine, schaftoside in Abri Herba were closely associated with the main targets, such as AKT1, STAT3, HIF1A, GRB2, MMP9, which could act on HIF-1, PI3K-Akt, JAK-STAT and other signaling pathways and have good pharmacological activities to be potential Q-markers of Abri Herba. Then HPLC was used to establish the characteristic according to retention time. Conclusion Through network pharmacology and molecular dock-prediction combined with HPLC detection, the characteristic chromatogram was established with the components of abrine hypaphorine, schaftoside as Q-markers, which could control the quality of Abri Herba by combining the components and pharmacological activities. More>>

The roles of Bajitianwan formula on Aβ-injured osteoblasts and the mechanism based on network pharmacology 巴戟天丸组方对Aβ损伤成骨细胞的作用及基于网络药理学的机制研究

JIANG Tao, XU Weifan, JIANG Yiping, XIA Tianshuang, et al

2024, 42(7): 285-290, 296. doi: 10.12206/j.issn.2097-2024.202305011

Objective To explore the effect of Bajitianwan（BJTW）formula on bone formation of Aβ-injured osteoblasts and its mechanism. Methods Osteoblasts isolated from neonatal 24-hour Wistar rats were used for the study, and osteoblasts were subjected to damage with Aβ1-42 oligomers, and pharmacological intervention was performed with the aqueous extract of BJTW formula. The MTT assay, alkaline phosphatase（ALP）activity assay, catalase（CAT）activity assay, superoxide dismutase（SOD）activity assay, glutathione（GSH）activity assay and malondialdehyde（MDA）activity assay were carried out respectively. The expression levels of bone morphogenetic protein 2（BMP2）, osteogenic specific transcription factor（RUNX-2）and osteoprotective protein（OPG）were detected by Western blotting. After confirming the effect of BJTW formula on Aβ-injured osteoblasts, the network pharmacology method was used to predict the potential pathways. Results The BJTW formula significantly promoted the proliferation of Aβ-injured osteoblasts, increased ALP, SOD and GSH activity, inhibited MDA activity, and promoted the expression of bone formation-related proteins BMP2, RUNX-2 and OPG. Network pharmacological analysis showed that the effect of ameliorating of Aβ-injured osteoblasts by BJTW formula was mainly mediated by AGE-RAGE, PI3K-Akt, MAPK and neuroactive ligand-receptor interaction signaling pathways. Conclusion In this study, the effect of BJTW formula on improving the osteoblasts damaged by Aβ was confirmed for the first time, and its related mechanism was explored based on network pharmacology method. The results lay a strong foundation for the clinical application of traditional formula BJTW against osteoporosis. More>>

Exploration of the role and mechanism of all-trans retinoic acid on activation and oxidative stress of hepatic stellate cell 全反式维甲酸对肝星状细胞活化及氧化应激的作用和机制探索

XIU Jianping, YANG Chaoai, LIU Xi’ao, PAN Qianyu, et al

2024, 42(7): 291-296. doi: 10.12206/j.issn.2097-2024.202312054

Objective To explore the role and potential mechanisms of all-trans retinoic acid （ATRA） on activation and oxidative stress of hepatic stellate cell （HSC）. Methods Platelet-derived growth factor （PDGF-bb, 10 ng/ml） was applied to induce the activation of HSCs, which was then treated with ATRA at a dosage of 5 μmol/L for 48 h. The effects of ATRA on HSC activation were evaluated by detecting changes in cell growth viability and phenotypic marker expression. The effects of ATRA on HSC oxidative stress were evaluated by detecting changes in intracellular reactive oxygen species （ROS）, reduced glutathione （GSH） and malondialdehyde （MDA）, and the expression of antioxidant genes. The effects of ATRA on HSC autophagic activity were evaluated by detecting changes in autophagy marker expression and autophagic flow. Results Compared with the PDGF-bb group, the cell viability was significantly reduced in ATRA-treated HSCs （P<0.01）, as well as the expression of α-SMA and Collagen I. The intracellular levels of ROS and MDA were significantly reduced in ATRA-treated HSCs （P<0.01）, whereas the GSH level was significantly increased （P<0.01）. The expression levels of antioxidant genes （NRF2, HO-1, and ATF4）, were significantly higher in ATRA-treated HSCs than those in the normal ones under PDGF-bb condition （P<0.01）. Meanwhile, the expression of autophagy markers Beclin 1 and LC3 Ⅱ/I, and signal of autophagy flow in ATRA-treated HSCs were found to be significantly reduced （P<0.01）. Conclusion ATRA significantly inhibited PDGF-bb-induced HSC activation and reduced the level of oxidative stress and autophagic activity of HSCs, which had potential applications in the prevention and treatment of liver fibrosis. More>>

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Comparative study of pharmacodynamic experiments on compound Heishen drop pills and compound Heishen pills

HE Jing, AN Ye, ZHANG Chaoshen

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202404009

Abstract(1283) HTML(533) PDF (879KB)(1)

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Objection: To study and compare the pharmacodynamics in the treatment of chronic pharyngitis between Compound Heishen pills and Compound Heishen Drop pills. Methods Sixty healthy Wistar rats were randomly divided into blank group, positive control group and treatment group. The foot swelling thickness of each rat was measured at 1.0, 2.0, 3.0, 4.0, 5.0 and 6.0 h after inflammation, and the foot swelling rate of each rat was calculated. Through the experimental model of rat toe swelling, the inhibition of foot swelling induced by carrageenan was observed by two dosage forms: drop pill and pill. Sixty healthy Kunming mice were randomly divided into the blank group, positive control group and treatment group. After 4 days of continuous intragastric administration, the mice were intraperitoneally injected with 0.5% phenol red solution. After 30min, the mice were sacrificed, their trachea was dissected and washed with 0.5%NaHCO₃ solution. The washing solution was put into ultraviolet spectrophotometer, and the absorbance was measured at 546 nm to calculate the corresponding concentration of phenolic red. Through the expectorant experiment of phenol red in mice, the effects of dropping pill and pill on the secretion of phenol red in experimental mice respiratory tract were compared. Results The experimental results of toes swelling in rats showed that compared with the blank experimental group, the five groups all had significant inhibition effect on acute foot swelling induced by carrageenan in rats. Compared with traditional form group, improved form had significant difference. The results of phenol red sputum removing experiment in mice showed that compared with the blank group the amount of phenol red secretion in mice was increased in 5 test groups could . There was no significant difference between improved form and traditional form on the amount of phenol red secretion in mice. Conclusion Both preparations had the function of anti-inflammatory and eliminating phlegm. There were no remarkable differences between the two preparations on pharmacologic actions.

Study on the effect of berberine combined with fluconazole on Candida albcians tolerant strains

SONG Zecheng, MA Shanshan, HU Qiaoling, ZHONG Hua, WANG Yan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202409047

Abstract(61) HTML(54) PDF (2143KB)(1)

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Objective To investigate the combined effect of berberine （BBR） and fluconazole （FLC） on FLC-tolerant Candida albicans in vitro. Methods The sensitivity of 8 strains of Candida albicans to FLC was assessed by determining their minimal inhibitory concentration （MIC） using broth microdilution method. FLC-tolerant strains were screened from FLC-sensitive strains by disk diffusion assay. The effect of BBR combined with FLC on FLC-tolerant Candida albicans was investigated by disk diffusion assay. Results All eight strains of Candida albicans exhibited sensitivity to FLC, with minimal inhibitory concentration （MIC₅₀） values below 0.5 μg/ml. Strains Y0109, 9821, 7879, 7654, and 9296 displayed colony growth in the inhibition zone after 48 hours of constant temperature incubation, indicating FLC tolerance. When strains Y0109 and 9821 were subjected to a combination of BBR and FLC, the number of colonies within the inhibition zone decreased progressively with the increase of BBR concentration following a 48-hour constant temperature culture. The inhibition zone became clear with the increasing of BBR concentration and increased with the increase of FLC loading, which showed a dose-dependent relationship. Conclusion The interaction between BBR and FLC demonstrated efficacy against FLC-tolerant strains.

Study on the Pharmacological Effects and Mechanism of Gegen-Zhimu Herb Pair in Preventing and Treating Alzheimer's Disease by UHPLC-Q/TOF-MS Metabolomics Strategy

CHAO Liang, WANG Hui, SHEN Shuqi, YOU Piaoxue, JI Kaihong, HONG Zhanying

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202409035

Abstract(87) HTML(58) PDF (1859KB)(0)

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Objective To evaluate the efficacy of Puerariae lobatae radix （PLR） and Anemarrhenae Rhizoma （AR） in preventing and treating Alzheimer’s disease （AD） and explore its potential mechanism of action by LC-MS serum metabolomics strategy. Methods The AD rat model was established by administering aluminum chloride （AlCl₃） and D-galactose （D-gal） for 20 weeks. The traditional Chinese medicine intervention group was given the PLR, AR, and PLR-AR extracts for 8 weeks by gavage. The model effect and efficacy were evaluated by Morri’s water maze test and biochemical indicators including SOD, NO, and MDA; Metabolomics research based on the UHPLC-Q/TOF-MS method was conducted, and relevant metabolic pathways were analyzed through the MetaboAnalyst online website. Results The learning and memory abilities of AD model rats were significantly decreased compared with the control group, and the levels of oxidative stress and lipid peroxides were significantly increased （P<0.05）, while the SOD content was decreased considerably （P<0.01）. the learning and memory abilities of AD model rats were improved, oxidative stress and lipid peroxidation levels were reversed, and serum SOD content was increased significantly after the intervention of PLR-AR, with better effects than single drugs. Through metabolomics, 70 differential metabolites were identified between the AD model group and the control group, mainly involving 10 pathways, including phenylalanine, tyrosine, and tryptophan biosynthesis, phenylalanine metabolism, and unsaturated fatty acid biosynthesis, et.al. The intervention of PLR-AR could adjust 47 metabolites, with 20 metabolites showing significant differences （P<0.05）. The significantly adjusted metabolites involve 6 pathways, including phenylalanine, tyrosine, and tryptophan biosynthesis, et.al. Conclusion The combination of PLR and AR could significantly improve the learning and memory abilities of AD rat models. The mechanism may be related to the improvement of oxidative stress and lipid peroxidation levels, the increase of serum SOD content, and the regulation of phenylalanine, tyrosine, and tryptophan biosynthesis pathways.

Study on Anti-constipation Effect of Black Garlic Polysaccharide

GUAN Mengyao, XIA Tianshuang, HE Xuhui, JIANG Yiping, XIN Hailiang

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202403059

Abstract(51) HTML(48) PDF (475KB)(0)

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Objective To establish the functional constipated mouse model by compound diphenoxylate, and explore the anti-constipation effect of black garlic polysaccharide. Methods Mouse small intestine ink propulsion experiment and mouse defecation experiment were carried out respectively. Each experiment was randomly divided into blank group, model group, positive group and black garlic polysaccharide （0.25, 0.5, 1 g/kg） groups. Mice in blank group and model group were given distilled water, and in positive group were given lactulose oral solution. Compound diphenoxylate （5 mg/kg） was intragastric administrated after 1 week of administration, and small intestine propulsion experiment and defecation experiment were conducted respectively. Results Compared with model group, intestinal propulsion rate of black garlic polysaccharide groups was significantly increased and first dejection time was significantly shorten, and the number, weight and fecal water content increased significantly at 6 h in middle and high dose groups. Conclusion Black garlic polysaccharide could promote intestinal propelling, shorten defecation time and increase fecal water content.

Optimization of purification process and component analysis of alkaloids from Zanthoxylum bungeanum Maxim

YANG Heying, LUO Caiping, PENG Ting, LIANG Wenyi, SHEN Songzhang, SU Juan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202404066

Abstract(70) HTML(60) PDF (1291KB)(1)

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Objective To optimize the process conditions and analyze the components of alkaloids from Zanthoxylum bungeanum Maxim（Z. bungeanum）using macroporous resin. Methods Combining single factor tests and orthogonal tests, the content of hydroxy-α-sanshool（HAS）and hydroxy-β-sanshool（HBS）were considered as indexes to determine the best process parameters. Ultra-performance liquid chromatography-quadrupole tandem time-of-flight mass spectrometry（UPLC-Q-TOF-MS^E）was used to identify the structures of alkaloids. Results The optimal conditions were Mitsubishi HP-20 macroporous resin, the loading solution concentration was 0.2 g crude drug/ml, the ratio of crude drug to resin volume was 1 g:2.5 ml, the diameter/height ratio of resin column was 1:7, the dynamic adsorption flow rate was 4 times of bed volume（BV）per hour, and the adsorption time was 1 h. Impurities were removed by using 2 BV of 20% ethanol, 5 BV of 80% ethanol was used to elution, and the content of HAS and HBS was 4.71% and 1.02%, respectively. A total of 20 alkaloids were identified from Z. bungeanum. Conclusion This method was stable and feasible, obtaining high purity and various kinds of alkaloids, which could be used for the enrichment and purification of alkaloids from Z. bungeanum.

Research progress on the treatment of vascular dementia by promoting blood circulation and removing blood stasis

DUAN Yu, LIU Aijun

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202408045

Abstract(85) HTML(58) PDF (921KB)(0)

Abstract:
The method of promoting blood circulation and removing blood stasis refers to the use of traditional Chinese medicine with a dispersing effect that can eliminate blood stasis in the body to treat the syndrome of blood stasis; It has the effects of unblocking blood vessels, dissipating stasis, regulating menstruation and relieving pain; Widely used for conditions such as chest tightness, heartache, dementia, menstrual disorders caused by blood stasis. Common medicines include Salvia miltiorrhiza Bunge; Panax notoginseng （Burkill）; Ligusticum chuanxiong Hort; Radix Curcumae, etc. Blood activating and stasis removing drugs generally have the effects of improving microcirculation, relaxing blood vessels, inhibiting thromboxane formation, and inhibiting platelet aggregation. They have good therapeutic effects on blood stasis syndrome in diseases such as coronary heart disease, angina pectoris, and vascular dementia. The research progress on traditional Chinese medicine and modern medicine on the treatment of vascular dementia with blood activating and stasis removing drugs were reviewed, in order to provide reference for the clinical application of blood activating and stasis removing methods in the treatment of vascular dementia.

Research progress on ANXA3 gene and protein

FENG Tingting, ZHANG Jingxiang, WANG Yan, XU Weiheng, ZHANG Junping

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202309023

Abstract(390) HTML(236) PDF (851KB)(1)

Abstract:
Annexin A3（ANXA3）is a member of the membrane associated protein family. It has two subtypes of 36 kDa and 33 kDa. Its gene is located on the fourth chromosome of human. ANXA3, widely expressed in human bone marrow, lung, placenta, prostate and thyroid, is closely related to several biological processes such as exoplasmosis, vascular production, fat cell maturity, and white blood cell migration. Studies have found that ANXA3 is abnormally expressed in various diseases including cancer, cardiovascular disease and inflammation. It can regulate multiple signaling pathways such as JNK, NF-κB, PI3K/AKT, and may become a potential drug target for treatment of related diseases. The structure, functions, the link with diseases and related mechanisms of ANXA3 were summarized in this paper, which could provide reference for ANXA3 related research.

Study on leaf epidermal microstructure of medicinal blue herbs

BAI Yunjun, ZHAO Yuyang, JIN Yan, FU Lu, YUAN Yuan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202404069

Abstract(360) HTML(274) PDF (3195KB)(5)

Abstract:
Objective The complex evolutionary history of the origin of medicinal blue herbs results in the presence of adulterants, affecting the accuracy and safety of clinical medication. To provide a reference basis for the identification of medicinal blue herbs with leaves as the medicinal part based on leaf epidermis microstructure. Methods The species belonging to medicinal blue herbs and their close relatives （10 species from 4 genera） were systematically investigated. The leaf epidermis microstructure of these species were observed and analyzed by optical microscopy and scanning electron microscopy. A species retrieval table were established based on the microstructure. Results Combining the distribution of stomata, types of subsidiary cells, stomatal index, stomatal density, characteristics of the periclinal walls of epidermal cells, and epidermal appendages could accurately distinguish species among the Clerodendrum cyrtophyllum, Polygonum tinctorium, Isatis indigotica, I. violascens, I. costata, I. minima, Strobilanthes wallichii, S. dalzielii, S. pentstemonoides, and S. cusia. Conclusion Microscopic characteristics of leaf epidermis can provide reference data for accurately differentiating the botanical origins of medicinal blue herbs.

Network pharmacological mechanism of Danshen Baizhu prescription on the treatment of coronary heart disease, vascular dementia and idiopathic membranous nephropathy

XU Lulu, LIU Aijun

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202312027

Abstract(1136) HTML(523) PDF (6479KB)(8)

Abstract:
Objective To investigate the material basis and mechanism of Danshen Baizhu prescription in coronary heart disease, vascular dementia and idiopathic membranous nephropathy based on network pharmacology. Methods TCMSP, PubChem, UniProt, GeneCards, OMIM, and DrugBank databases were used to obtain drug and disease targets, and the TCM-compound-drug target network, compound-common target-disease network, and protein-protein interaction map were drawn by STRING database and Cytoscape software, and gene enrichment analysis was performed by Metascape database. Results A total of 164 active compounds, 509 potential targets, and 141 common targets were screened out. The main active ingredients are Tanshinone II A, Isorhamnetin, Quercetin, Luteolin, Kampferol, β-sitosterol, Stigmasterol, etc. The key targets are albumin, interleukin 6, Tumor necrosis factor , serine/threonine kinase 1, vascular endothelial growth factor A , mainly enriching in the positive regulation of cell migration, cell viability, protein phosphorylation, response to growth factors, oxidative stress and other biological processes and lipid and atherosclerosis, MAPK, atherosclerosis and fluid shear force, AGE-RAGE, IL-17, PI3K-Akt and other signaling pathways. Conclusion The mechanism of action of Danshen Baizhu prescription for coronary heart disease, vascular dementia and idiopathic membranous nephropathy may mainly play a role in multiple targets and pathways such as inhibition of inflammation, inhibition of oxidative stress, and vasodilation.

Analysis on the use of medicines in treatment of benign prostatic hyperplasia in sample hospitals under the national volume-based procurement policy

LI Rui¹, ZHANG Qianqian², WANG Ruidong³, GAO Xiaofeng¹

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202408031

Abstract(837) HTML(465) PDF (1249KB)(6)

Abstract:
Objective To explore the impact of national volume-based procurement policies on the use of medicines in treatment of benign prostatic hyperplasia （BPH） and provide data support for the rational clinical use of medicines in BPH treatment. Methods Data on the usage of BPH treatment medications from 2019 to 2023 were extracted from the Chinese Medicine Economic Information Network （CMEI）, covering 892 hospitals （including 645 tertiary hospitals and 247 secondary hospitals）. The changes in various indicators, including the consumption sum, Defined daily doses （DDDs）, Defined daily dose cost （DDDc）, and the ranking ratio （B/A） of these drugs were analyzed and compared. Results From 2019 to 2023, due to the influence of relevant policies, the overall consumption sums of medicines used in the sample hospitals in BPH treatment showed a trend of decreasing first and then rising steadily. The DDDs showed an overall upward trend, while the DDDc demonstrated a gradual decline. Tamsulosin and finasteride consistently ranked first and second in DDDs. The B/A value for tamsulosin was significantly higher than that of other BPH treatment medications. Conclusion The implementation of national centralized drug volume-based procurement policies and other policies from 2019 to 2023 had effectively reduced the economic burden of patients with benign prostatic hyperplasia. Tamsulosin and finasteride, which had the highest B/A in the two categories of α-blockers and 5α-reductase inhibitors, dominated the market for BPH treatment. The clinical use of BPH treatment medications was relatively rational.

Adverse reaction analysis of drug-induced liver injury

ZHANG Yan, LI Yanjun, LIU Jiahui, DENG Jiao, YUAN Yuan, ZHANG Jingyi

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202404034

Abstract(1249) HTML(612) PDF (846KB)(6)

Abstract:
Objective To analyze the adverse reaction reports of drug-induced liver injury in recent ten years, explore the characteristics and related rules of drug-induced liver injury, and provide reference for clinical safe drug use. Methods ADRs in our hospital from 2011 to 2021 which belonged to drug-induced liver injuries were collected, and Pareto analysis was carried on. Results In 259 ADR reports, the most common type of drug-induced liver injury was hepatocellular injury （37.84%）. The age of drug-induced liver injury was mainly over 46 years, totaling 195 （75.28%）. Drugs were mainly distributed in cardiovascular system medicine （44.02%）, anti-infective medicine （23.94%）and anti-tumor medicine （11.58%）. Among the cardiovascular drugs, atorvastatin calcium 40mg and over 40mg were the highest proportion, with 53 cases （46.49%）. The main anti-infectious drugs were cephalosporins （29.03%）, carbapenem （19.35%）, antifungal （17.74%）and quinolones （11.29%）. Adverse reactions occurred within 6 days （69.88%）, the duration of adverse reactions was 1-2 weeks（31.66%）, and most patients improved （47.88%） or cured （37.07%）. Conclusion For middle-aged and elderly patients, when the application of cardiovascular system drugs, anti-infective drugs or anti-tumor drugs, it is necessary to monitor the liver function changes of patients for at least 6 days. If there are abnormalities, the drugs should be stopped or given treatment in time, to avoid the progress of drug-induced liver injury.

The practice of rational drug use management in hospitals under the reform of DRGs payment methods

YANG Bin, WANG Zuojun, CHEN Han, ZHANG Jingyi

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202404030

Abstract(1415) HTML(682) PDF (1007KB)(12)

Abstract:
Objective To establish an effective management mode, give full play to the role of DRGs in rational drug use, formulate the pharmaceutical clinical path, and intervene the prescription behavior of doctors, which could improve the level of rational drug use in the hospital through the management practice of rational drug use under the payment method of DRGs in a third-grade hospital. Methods A drug introduction mechanism, a rational drug use supervision mechanism and an active and rational drug use data drying mechanism based on DRGs were established, and the rational drug use indicators such as drug consumption index, average drug cost, and auxiliary drug use were accurately positioned based on the information platform, and the accurate and refined management of rational drug use was realized through the daily supervision of the office of the Pharmaceutical Affairs Committee. Results and conclusions Under the multi-dimensional and multi-level rational drug use management based on DRGs, the effect of rational drug use was evaluated after the reform of DRGs payment method, and all the indexes of rational drug use in our hospital were continuously improved.

Hydrogel scaffolds loaded with bone marrow mesenchymal stem cells/resveratrol liposomes for traumatic brain injury treatment

CHI Wenya, YUAN Yan, LI Weilin, WU Tongyu, YU Yuan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202406034

Abstract(2145) HTML(685) PDF (2074KB)(9)

Abstract:
Objective To prepare a thermosensitive hydrogel scaffold loaded with bone marrow mesenchymal stem cells（BMSCs）and resveratrol liposomes （RSV-LIP） to form a therapeutic unit and evaluate its treatment efficacy for traumatic brain injury （TBI）. Methods BMSCs were extracted from rats, and RSV-LIP was prepared and characterized. Cell models were constructed to investigate the pharmacological effects of BMSCs combined with RSV-LIP. BMSCs and RSV-LIP were then loaded into the hydrogel, and a TBI mouse model was established to evaluate the therapeutic effects of the hydrogel. Results The RSV-LIP had a particle size of 127.8 nm, a Zeta potential of −4.9 mV, an encapsulation efficiency of 78.50%, and a drug loading content of 2.37%. Live-dead staining indicated good biocompatibility of the hydrogel. The combination of BMSCs and RSV-LIP significantly inhibited TNF-α and reduced ROS levels, promoting cell migration in scratch assays. Compared to the control group, the hydrogel group showed significantly lower mNSS scores （P<0.01）, higher hanging scores （P<0.001）, and reduced stepping errors （P<0.001）. Conclusion The combination of BMSCs and RSV-LIP exhibited antioxidative stress, anti-inflammatory, and neurogenic cell migration-promoting effects. When loaded into a hydrogel scaffold and locally implanted, it could improve the motor and sensory functions in TBI mice.

Reasonable management and control practice of prophylactic use of antibiotics for urinary system lithotripsy

CHEN Yijun, WANG Zhuo, HE Miao, ZHANG Yu, TIAN Jing

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202402034

Abstract(2171) HTML(750) PDF (993KB)(4)

Abstract:
Objective To analyze the effectiveness of reasonable control measures for prophylactic use of antibiotics for urinary system lithotripsy. Methods By antimicrobial stewardship, strengthening special comments on antibiotics and information notification on rational use of antibiotics, adding and improving the pre-review rules for antibiotics prescriptions, conducting in-depth clinical training and consultation by clinical pharmacists, strengthening innovation in rational use of drugs, and taking various measures to actively improve rational use of prophylactic antibiotics of lithotripsy in urology department, the changes of indexes related to antibiotics in urology department from 2019 to 2022 were analyzed. Results After active and reasonable control, Antibiotics Use Density in urology department decreased year by year. The utilization rate of antibiotics in inpatients decreased from 94.27% in 2019 to 77.47% in 2022. Various rate of microbial inspection reached the standard in 2022; The imipenem and cilastatin sodium for injection ranking of prophylactic use of antibiotics consumption DDDs for urinary system lithotripsy decreased from the 4th place in 2019 to the 8th place in 2022. The ranking of the urology department on carbapenem consumption DDDs in the whole hospital decreased from the 8th place in 2019 to the 12th place in 2022. At the same time, the incidence of urinary tract lithotripsy postoperative infection showed a decreasing trend year by year, from 0.84% in 2019 to 0.49% in 2022. Conclusion Positive control measures can promote the rational use of prophylactic antibiotics for urinary system lithotripsy.

Correlation between plasma concentration of voriconazole and polymorphisms in CYP2C19, CYP2C9 and CYP3A5 genes in children

GUI Mingzhu, LI Jing, LI Zhiling

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202402020

Abstract(1490) HTML(1517) PDF (842KB)(6)

Abstract:
Objective To explore the effects of CYP2C19, CYP2C9 and CYP3A5 genotypes on the plasma concentration of voriconazole in children. Methods Collected blood samples from 50 hospitalized children with invasive fungal infections who received intravenous voriconazole from January 2020 to December 2020. High performance liquid chromatography was used to detect the blood trough concentration of voriconazole, and the time-of-flight mass spectrometry detection system was used to detect the genotypes of CYP2C19, CYP2C9 and CYP3A5, and the effects of children’s genotyping on the plasma concentration, efficacy and adverse reactions of voriconazole were analyzed. Results The total effective rate of 50 children with IFI was 84% （42/50） after voriconazole treatment. The incidence of adverse reactions was 20% （10/50 cases）. The measured plasma concentration of voriconazole ranged from 0.56~7.62 μg/ml. Combined with the different mutation types of CYP2C19 gene loci, three metabolic activities were produced: fast, medium and slow, and the test results showed that there were 16 cases of fast metabolism, 27 cases of intermediate metabolism and 7 cases of slow metabolism. There was a significant difference in plasma concentrations between the three groups （F=15.359, P< 0.001）, and the drug concentrations in the fast metabolic group were significantly lower than those in the intermediate metabolic and slow metabolic groups. The mutations of CYP2C9 and CYP3A5 had no significant effect on the plasma concentrations of the drugs, which were （F=2.213, P=0.086）and （F=0.757, P=0.475）. Conclusion Voriconazole had significant efficacy in the treatment of invasive fungal infections in children, and the adverse reactions were mild. CYP2C19 genotype was significantly related to the rate of drug metabolism and was an important factor affecting blood drug concentration, the detection of drug concentration and genotype of voriconazole was helpful to adjust the effective drug dose clinically and achieve more scientific and individualized treatment.

Study on the efficacy and mechanism of Tongbianling capsule in the treatment of constipation

CHEN Ying, XU Zihua, HU Bei, CUI Yaling, GAO Huan, WU Qiong

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202404008

Abstract(3839) HTML(1700) PDF (4039KB)(15)

Abstract:
Object To study the efficacy and potential mechanism of Tongbianling capsule in constipation. Methods To observe the effects of Tongbianling capsule on intestinal motility in normal mice and carbon powder propulsion rate in small intestine of constipation model mice after administration. The potential targets and key pathways of Tongbianling capsule in treating constipation were identified through network pharmacology. To verify the mechanism, the expression of p-PI3K/PI3K, p-AKT/AKT and CASP3 proteins in mouse colon tissue was detected by the western blot. Results The time for mice to excrete the first black stool was shortened and the number of fecal particles was increased in Tongbianling capsule administration group, and the carbon powder propulsion rate of mice in each Tongbianling capsule administration group was increased. The results of network pharmacology showed that treatment of constipation by Tongbianling capsule may be related to signaling pathways such as PI3K-Akt signaling pathway and 5-HT. The protein expression of p-PI3K/PI3K, p-AKT/AKT, and CASP3 in mouse colon tissue could be significantly downregulated in administration group. Conclusion Tongbianling capsule could effectively promote intestinal peristalsis in mice, increase the frequency of defecation, and effectively treat constipation. The mechanism of its action may be related to the direct or indirect regulation of intestinal motility by the PI3K-Akt signaling pathway.

Skin pharmacokinetics of inositol nicotinate in heparin sodium inositol nicotinate cream

CUI Yaling, WU Qiong, MA Liangyu, HU Bei, YAO Dong, XU Zihua

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202404006

Abstract(2790) HTML(745) PDF (965KB)(9)

Abstract:
Objective To establish an HPLC method to determine the concentration of inositol nicotinate（IN） in rat skin, and study the pharmacokinetic characteristics of IN after transdermal administration of heparin sodium inositol nicotinate cream（GJR） in rats. Methods HPLC method was used to establish a simple and rapid analytical method for the determination of IN concentration in the skin of rats at different time points after administration. The established method was used to study the pharmacokinetics of IN after transdermal administration of GJR in rats, and the pharmacokinetic parameters were fitted with DAS software. Results The linearity of the analytical method was good in the concentration range of 0.25~20 μg/ml, the quantitative limit was 0.25 μg/ml, and the average recovery rate was 96.18%. The pharmacokinetic parameters of IN after transdermal administration of GJR in rats were as follows: t_1/2 was （4.555±2.054） h, T_max was （6±0）h, C_max was （16.929±2.153）mg/L, AUC_0−t was （150.665±16.568） mg·h /L ,AUC_0−∞ was （161.074±23.917） mg·h /L, MRT_（0−t） was （9.044±0.618）h, MRT_{（0−∞）} was （10.444±1.91） h, CLz/F was （0.19±0.03） L/（h·kg）, and Vz/F was （1.19±0.437） L/（h·kg）. Conclusion IN could quickly penetrate the skin and accumulate in the skin for a long time, which was beneficial to the pharmacological action of drugs on the lesion site for a long time. The method was simple, rapid, specific and reproducible, which could be successfully applied to the pharmacokinetic study of IN after transdermal administration in rats.

Anti-frostbite effect of miglitol on cold-exposed mice through UCP1-mediated thermogenic activation

LI Xiang, LU Hongyuan, ZHANG Mingyu, GAO Huan, YAO Dong, XU Zihua

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202404005

Abstract(2630) HTML(963) PDF (1670KB)(19)

Abstract:
Objective To investigate the effect and mechanism of miglitol on regulating the energy metabolism of brown adipocytes by activating UCP1 and improving cold injury in mice after cold exposure. Methods Primary brown adipocytes were induced into mature adipocytes, the effect of miglitol on the viability of brown adipocytes was investigated by MTT method, the lipid droplet consumption level of cells after drug administration was investigated by Oil Red O staining technology, and the level of UCP1, a key protein of thermogenesis in brown adipocytes, was detected by Western blotting. The activity of anti-frostbite was investigated in cold exposure at 4 ℃ and −20 ℃. KM mice, which were randomly divided into control group, cold exposure group, miglitol group and all-trans retinoic acid group, and after 7 days of repeated administration, the body surface temperature of mice was detected by infrared thermal imaging system, the anal temperature change was detected by anal thermometer, and the expression levels of UCP1 and PGC1-α in adipose tissue were detected by immunoblotting. Results Compared with the control group, the lipid droplet consumption and UCP1 expression levels in brown adipocytes in the miglitol group were significantly increased. The levels of body surface temperature and rectal temperature increased significantly after cold exposure, and the levels of UCP1 and PGC1α in the brown adipose tissue of mice increased significantly, which indicated that the miglitol could activate the critical proteins UCP1 and PGC1α of the thermogenesis pathway, increase the thermogenesis of mice after cold exposure, and thus improve the effect of cold injury for toe swelling. Conclusion Miglitol could play a role in improving cold injury and body temperature in mice by increasing the level of UCP1 and PGC1α, which are key targets of the thermogenesis pathway to promote the thermogenesis of brown fat.

Study on the synergistic antifungal effects of Caspofungin Acetate loaded glyceryl monostearate nanoparticle on Candida albicans

GUO Lingyi, LIU Yanchao, GAO LU, LIU Ruiyao, LV Quanzhen, YU Yuan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202310043

Abstract(3599) HTML(910) PDF (0KB)(5)

Abstract:
Objective To prepare and characterize caspofungin acetate-loaded solid lipid nanoparticles using glycerol monostearate （CAS-SLNs）, and investigate the antifungal effect of potentiation on Candida albicans in vitro and in vivo. Methods A high performance liquid chromatography method was established for the determination of caspofungin acetate （CAS）. CAS-SLNs were prepared by the melt-emulsification method and characterized. The minimum inhibitory concentration （MIC）and the inhibitory effect on Candida albicans biofilm were determined. A systemic infection model of Candida albicans was established in mice, and the growth curve models for body weight and fungal load of kidneys of the animals were investigated after intravenous infection. Results The retention time of CAS was 6.8 min. The calibration curve showed good linearity, and the precision and stability met the requirements of the assay. Transmission electron microscopy revealed that CAS-SLNs were spherical, with a particle size of 135.97±1.73 nm. The Zeta potential was 19.33±0.37 mV, drug loading was 7.55±0.68%, and encapsulation efficiency was 67.71±1.74%. CAS-SLNs showed significant in vitro antifungal inhibition with a MIC of 9.78×10⁻⁴ g/ml, which was significantly better than CAS group and the physical mixture group of CAS and GMS, as well as the same biofilm inhibition was observed（P<0.001, P<0.001）. Pharmacodynamic studies demonstrated that CAS-SLNs maintained stable body weight gain compared to the control（P<0.01）and CAS groups in Candida albicans invasive infection model, and that CAS-SLNs significantly reduced renal fungal burden load relative to the CAS group （P<0.05）. In vivo study revealed that a stable body weight was maintained in CAS-SLNs group compared to the control group （P<0.01）in Candida albicans invasive infection model. CAS-SLNs also significantly reduced renal fungal load compared to the CAS group（P<0.05）. Conclusion CAS-SLNs significantly enhanced the antifungal effects of CAS in vitro and in vivo, which provided a valuable insight for the research of new formulation of CAS.

Rapid determination of tramadol in urine by surface-enhanced Raman spectroscopy

YAO Xiaojing, JI Peiying, LU Feng, SHI Guorong, FU Xiang

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202401072

Abstract(5832) HTML(1466) PDF (1577KB)(13)

Abstract:
Objective To establish a method for rapid detection of tramadol in urine by liquid-liquid extraction（LLE）-surface-enhanced Raman spectroscopy （SERS）. Methods Tramadol was extracted from urine with chloroform: isopropyl alcohol （9∶1）extractant and detected in urine samples by enhanced Raman spectroscopy （wavelength 785 nm）. Results The quantitative curve of tramadol was Y=204.35X−465.62, r=0.9952, and the linear range was 1-100 μg/ml. The detection limit of tramadol by this method （S/N=3）was 0.53 μg/ml. The sensitivity of SERS was higher than that of conventional methods, and it had reasonable reproducibility. Conclusion This method is simple, efficient and economical, and can be used for qualitative and quantitative analysis of tramadol personalized medicine.

Comprehensive evaluation of powder-liquid double-chamber bag products : a systematic review

SHU Fei, SUN Rui, SONG Kai, ZHANG Yuanlin, YAN Jiaming, SHU Lixin

In Press doi: 10.12206/j.issn.2097-2024.202312009

Abstract(6071) HTML(2108) PDF (998KB)(56)

Abstract:
Objective Compared with traditional powder injection, the advantages of powder-liquid double-chamber bag products were comprehensively evaluated. Methods The systematic review method was used to collect the literature on powder-liquid double-chamber bag, extract common evaluation indicators, evaluate the use value of powder-liquid double-chamber bag products, and conduct a comprehensive comparison with traditional powder injection products. Results A total of 23 articles were included in the literature. The effectiveness indicators used for evaluation were the stability of the liquid medicine, the accuracy of the preparation concentration, and the residual amount of the liquid medicine; the safety indicators were the incidence of insoluble particles and the incidence of punctures and scratches. The economic indicators were preparation cost, occupied volume of preparation supplies, waste weight, hospitalization cost and incidence of blood infection. The applicability indicators were preparation time, average occupation of medical staff, packaging weight and storage and transportation volume, environmental adaptability, and ease of waste disposal. Accessibility indicators are the number of manufacturers, raw material supply capacity, and patient affordability. Through the rapid evaluation of literature evidence, it was found that the stability and concentration accuracy of the powder-liquid double-chamber bag were higher than those of the traditional powder injection, and the domestic supply had been achieved. The double-chamber bag method can reduce the infusion reaction and shorten the preparation time of the liquid medicine. Conclusion Compared with traditional powder injectabler products, powder-liquid double-chamber bags have advantages in the dimensions of effectiveness, safety, economy, suitability and innovation, and the accessibility dimension meets the requirements.

Analysis of characteristics of adverse drug reactions in our hospital from 2021 to 2023

SONG Hongwei, WANG Yan, FANG Ming, MA Yunpeng, ZHONG Chao, XU Yixin, XU Feng, ZHOU Ting

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202404041

Abstract(4826) HTML(1455) PDF (885KB)(22)

Abstract:
Objective To analyze the characteristics of adverse drug reactions （ADR） reported in our hospital from 2021-2023, to provide reference for promoting rational clinical drug use. Methods ADR data reported in our hospital were collected retrospectively, including patients' basic information, drugs causing adverse reactions, types of adverse reactions and outcomes. Descriptive analysis methods were used to summarize and analyze the data. Results A total of 979 cases of ADR were reported in our hospital from 2021 to 2023. The highest proportion of patients with ADR occurred in the age range of 31 to 50, and more male patients （63.5%）. The top five drugs involved with adverse reactions were antibiotics （48.8%）, Chinese medicine injections, vitamins, Chinese patent medicine, equine tetanus immunoglobulin. Among antibiotics, cefuroxime, ceftazidime and cefotiam were the majority. The organs/systems involved in all ADR were mainly skin and accessories damage （55.4%）. The clinical manifestations were rash, itching, and maculopapular rash. Conclusion From 2021 to 2023, the most common drugs causing adverse drug reactions in our hospital are still mainly antibacterial drugs, and the rational clinical use of antibacterial drugs still needs to be paid attention to.

Research and Application Progress on Recognition Components for Surface Plasmon Resonance Sensors in the Pharmaceutical Field

WANG Xiaofei, ZHANG Ying, GU Jiayu, HU Xiner, ZHANG Hai, CAO Yan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202309014

Abstract(7064) HTML(2469) PDF (1525KB)(13)

Abstract:
Surface plasmonresonance （SPR） sensoris anoptical detection technique enables real-time and dynamic monitoring of biological samples. SPR-based biosensors have remarkable characteristics such as label-free detection and high sensitivity, making them important tools for studying molecular interactions. The recognition element, which plays a critical role in SPR sensors, allows for specific identification and capture of target analytes, closely influencing the selectivity performance of the sensor. The progress on SPR sensors in pharmaceutical research were reviewed, which focused on the application of recognition elements such as antibodies, aptamers, molecularly imprinted polymers, and metal nanoparticles.

Determination of Lamotrigine in Human Plasma by Central cutting two-dimensional liquid Chromatography

LIN Junrong, ZHANG Minxin, ZHAO Xuemei, HUANG Aiwen

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202306020

Abstract(4212) HTML(1080) PDF (1115KB)(4)

Abstract:
Objective To establish a central cutting two-dimensional liquid chromatography for the determination of lamotrigine in human plasma. Methods External standard method was used. The first dimensional chromatographic column: SNCB（T）-1A（silica gel, 4.6 mm×50 mm, 5 μm）, mobile phase A:VCV-1D mobile phase, flow rate: 0.4 ml/min; mobile phase B: water, flow rate: 1.0 ml/min; second dimensional chromatographic column: Symmetry C₁₈ （4.6 mm×250 mm, 5 μm）, mobile phase: acetonitrile-10 mmol/L ammonium acetate solution（V/V=25∶75）, flow rate: 1.0 ml/min; Intermediate column: SBX 4-MA（resin, 3.0 mm×10 mm, 5µm）. The UV detection wavelength: 306 nm, the column temperature: 45 ℃, and the injection volume: 200 μl. Results The linear range of lamotrigine was 1.24-39.50 μg/ml, the lower limit of quantification was 1.24 μg/ml, the detection limit was 0.02 μg/ml, the intra-day precision RSD was less than 5%, the day-to-day precision RSD was less than 10%, the variation of intra-day accuracy ranged from 102.17% to 111.17%, and the daytime accuracy variation ranged from 99.80% to 107.31% the recovery RSD was less than 5%, and the variation range was 89.95% -96.16%. After 24 hours storage at room temperature, repeated freezing and thawing for 3 times and storage at-40 ℃ for 2 weeks, the ratio of the measured value / labeled value ranged from 87.01% to 115.88%. Conclusion In this study, a method with simple operation, good stability, high sensitivity and good reproducibility was established, which could be suitable for clinical monitoring of blood concentration of lamotrigine and provides reliable monitoring data support for clinical individualized medication guidance.

Study on quality standard of Andrographis paniculata standard decoction based on UPLC characteristic chromatogram and quantitative analysis of multi-components by single marker

MA Zhiling, WANG Xiaoya, DU Weibo, ZHANG Zhiqiang, SHEN Jianmei, LIU Yan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202310021

Abstract(4047) HTML(1057) PDF (1585KB)(9)

Abstract:
Objective To establish quality evaluation method of Andrographis paniculata standard decoction by UPLC. Methods 21 batches of Andrographis paniculata standard decoctions were prepared according to the standardization method of TCM decoction pieces. The UPLC characteristic chromatograms analysis method was established. With andrographolide as a reference, quantitative analysis of multi-components by single marker（QAMS）was established for new neoandrographolide, 14 deoxyandrographolide and dehydrated andrographolide and the results were compared with the external standard method（ESM）to determine the accuracy of the method. Results Similarity Evaluation System for Chromatographic Fingerprint of TCM（2012 edition）was used to analyze and compare the characteristic chromatograms, and seven common peaks were determined and five were identified including luteolin-7-O-β-D-glucuronide, andrographolide, neoandrographolide, 14-deoxyandrographolide and dehydroandrographolide. The RSDs of content results of each component by QAMS and ESM were all within 3%. Conclusion The determination method is reliable and accurate, which can be used to reflect the intrinsic quality of Andrographis paniculata standard decoction more comprehensively and provide the basis for the quality evaluation of Andrographis paniculata formula granules and other preparations.

Clinical research progress on RRx-001

GONG Yangyang, LOU Chunyang, ZHANG Huojun, MIAO Zhenyuan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202402028

Abstract(4721) HTML(1880) PDF (1796KB)(18)

Abstract:
It is difficult to treat malignant tumors, neurodegenerative diseases, and vascular diseases. For pathogenesis complexity of these diseases, researchers have focused on finding more drugs with high efficacy and low side effects. As a potential first-in-class drug, RRx-001 is expected to be an important first-line drug in tumor immunology, radiosensitizer and radio protecter. Currently, RRx-001 entered phase III clinical trials. The data of the phase II clinical trials demonstrated its safety and effectivity as a single agent and in combination with first-line clinical drugs. The novel mechanisms of RRx-001 and the result of main clinical trials were summarized, which could be valuable to further optimization and clinical application.

Research on the chemical compositions and their biological activities of Piper nigrum L.

GAO Xing, ZHAO Fengping, WANG Wentao, TIAN Wei, ZHENG Canhui, CHEN Xin

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202308065

Abstract(6584) HTML(4304) PDF (1638KB)(53)

Abstract:
Piper nigrum L. is an evergreen climbing vine, which belongs to the genus Piperia in the Piperaceae family. Piper nigrum L., which known as the “king of spices”, is used as both food and medicine. The main active substances in Piper nigrum L. are alkaloids mainly composed of amides, and essential oil, as well as phenolic compounds. In this paper, the chemical compositions, especially amide alkaloids, and their biological activities of Piper nigrum L. were summarized. These studies showed that Piper nigrum L., as a medicinal and food plant, had a wide range of biological activities and was deserved further research and in-depth utilization.

Effects and mechanism of Triptolide on cerebral ischemia-reperfusion injury in rats

ZHU Dongjie, HE Xinzheng, ZOU Jie, YU Shidan, LI Hongxia

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202311021

Abstract(4984) HTML(1837) PDF (1393KB)(24)

Abstract:
Objective To investigate the effect of Triptolide on cerebral ischemia- reperfusion injury (CIRI) and explore its molecular mechanism. Methods One hundred and forty-four Wistar rats were randomly divided into sham operation group, model group, low, medium, high dose of triptolide group and butylphthalide group, with 24 rats in each group. The CIRI rat model was established by blocking the middle cerebral artery for 2 hours. 3 days before modeling, the rats in each group were ip administration once a day. 24 hours after reperfusion, the neurological deficit score was detected, the rate of cerebral infarction was measured by TTC staining, the blood brain barrier (BBB) permeability was detected by EB penetration test. The pathological changes neurons in the ischemic penumbra cortex were observed by HE and TUNEL staining. The content of inflammatory factors in ischemic cerebral cortex were detected by ELISA method. The expression of TLR4/NF-κB pathway related proteins were detected by Western blot. Results Compared with the model group, the neurological deficit score, cerebral infarction rate and EB content in the Triptolide middle, high dose groups and the Butylphthalide group were significantly decreased (P<0.05). The pathological changes of cortical neurons in the ischemic penumbra were significantly improved, and the apoptosis rate of neurons was significantly decreased (P<0.05). The content of TNF-α, IL-1β and the expression of TLR4, p-NF-κB, cleaved Caspase-3, Bax were significantly decreased, the expression of Bcl-2 was significantly increased, the ratio of p-NF-κB/NF-κB and Bax/Bcl-2 were significantly decreased (P<0.05). The regulatory effect of the high dose triptolide group on various detection indexes were better than that of the Butylphthalide group (P<0.05). Conclusion Triptolide could protect the permeability of BBB, improve the neurological deficit and neuropathy in CIRI rats, and reduce the rate of cerebral infarction, its mechanism may be related to the inhibition of TLR4/NF-κB pathway and which mediated inflammatory response and neuronal apoptosis.

Flavonoids from Corn Silk (Zea mays L.) and its pharmacological effects

ZHOU Licheng, OU Yiming

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202309037

Abstract(6655) HTML(2378) PDF (1084KB)(26)

Abstract:
Corn silk, a Traditional Chinese Medicine, has the effect of calming liver, cholagogue, detumescence and diuresis. Corn silk is also widely used as tea and functional food. Natural flavonoids have multiple biological activities, which are also the main bioactive components of corn silk. In the past decade, many new advances have been made in the chemistry, analysis, pharmacology, pharmacokinetics, and safety evaluation of corn silk flavonoids. The chemical composition research of flavonoids has enriched the quantity of flavonoids in corn silk. Pharmacological studies have confirmed and expanded the efficacy of corn silk flavonoids. And safety evaluation has provided a theoretical basis for the safe application of corn silk flavonoids. Through literature search, the extraction, separation, compositional analysis, content determination, pharmacological effect, pharmacokinetics, and safety research progress of corn silk flavonoids in the past ten years were reviewed in this paper.

Effect of Hypoproteinemia on Cefoperazone Plasma Concentration

ZHAN Ji-hua, YAN Ying

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202309040

Abstract(3997) HTML(1019) PDF (833KB)(8)

Abstract:
Objective To analyze the effect of hypoproteinemia on the use of cefoperazone in patients, and provide references for the rational use of cefoperazone in clinical practice. Methods Clinical data of patients with cefoperazone blood concentration monitoring in our hospital from July 2021 to March 2022 were collected, and divided into low albumin group and normal albumin group according to different albumin concentration. Statistical analysis were conducted based on gender, age, laboratory examination, cefoperazone valley concentration and clinical efficacy of the two groups. Results Age, gender, inflammation and liver function of two groups had not shown statistical difference (P>0.05). Low protein group had significantly higher levels of creatinine than those in group with normal albumin (P<0.05). The trough concentration of cefoperazone in the low protein group was 46.29±36.94 mg/L, and that in the normal albumin group was 38.18±33.79 mg/L. Among the low protein patient group, the plasma concentration of cefoperazone in those treated with human albumin was significantly higher than that in the patients without human albumin treatment (P<0.05). Comparison of the clinical efficacy of the two groups revealed that the low protein group had a lower clinical response rate (P<0.05). Conclusion Supplementation of human serum albumin in patients with hypoproteinemia could increase the plasma concentration of cefoperazone, and correcting hypoproteinemia could be helpful for anti-infection treatment.

Effect of Huoxin Pill (concentrated pill) combined with Baduanjin on prognosis after interventional operation of acute myocardial infarction complicated with heart failure

WANG Peng, WU Zonggui, ZHANG Zhengyan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202308034

Abstract(4057) HTML(1356) PDF (890KB)(15)

Abstract:
Objective To observe the effect of Huoxin Pill (concentrated pill) combined with Baduanjin on the prognosis of patients with acute myocardial infarction complicated by Percutaneous Coronary Intervention (PCI). Methods 120 Patients with acute myocardial infarction complicated with heart failure who received emergency interventional treatment in our hospital from January 2022 to January 2023 were randomly divided into Western medicine treatment group and Traditional Chinese Medicine （TCM）comprehensive treatment group. Western medicine treatment: standard Western medicine treatment + five prescriptions for cardiac rehabilitation; Based on Western medicine treatment, Huaxin pill (concentrated pill) combined with Baduanjin therapy was added to the TCM comprehensive treatment group, and the follow-up was 6 months. The observed indexes were exertion angina pectoris scale, Chinese Medicine Syndrome Scale, Chinese medicine syndrome treatment effect evaluation, 6-minute walking test (6MWT), left ventricular ejection fraction (LVEF), and brain natriuretic peptide precursor (pro-BNP). Results Sixty patients were enrolled in the two groups respectively. During the treatment, 2 cases fell off in the Western medicine treatment group and 8 cases fell off in the TCM comprehensive treatment group, and a total of 110 cases were enrolled in the group. Compared with the western treatment group, TCM combined therapy significantly improved angina pectoris scale score, TCM Syndrome Scale score, pro-BNP, LVEF and 6MWT (P < 0.001). There were no significant differences in blood routine, liver and kidney function, potassium, blood glucose, blood lipids and cardiac Troponin I (cTnI) between the two groups (P > 0.05). No adverse cardiovascular events occurred during the entire treatment period in both groups. Conclusion Huaxin Pill (concentrated pill) combined with Baduanjin was more effective than Western therapy in improving LVEF, 6MWT distance, exercise tolerance and cardiac function in patients with acute myocardial infarction complicated with heart failure.

Study of the treatment compliance and influencing factors of inhalation therapy in patients with stable chronic obstructive pulmonary disease

DUAN Hu, ZHOU Yanqing, QIAN Yulin, ZHAO Liang

In Press doi: 10.12206/j.issn.2097-2024.202204094

Abstract(5307) HTML(2919) PDF (839KB)(44)

Abstract:
Objective To study the compliance and influencing factors of inhalation therapy in patients with stable chronic obstructive pulmonary disease (COPD),and carry out patient education and management accordingly. Methods COPD patients were selected from Respiratory Clinic of Luodian Hospital of Baoshan District of Shanghai from June to December of 2021. Compliance and inhalation techniques were assessed with the Morisky Medication Adherence Scale and the ten-step inhalation technique, and the factors influencing compliance were analyzed. Results A total of 58 outpatients with COPD were included, in which 25 cases (43.1%) with moderate or above compliance. Univariate analysis showed that the patients with course of disease ≥5 years, CAT(COPD assessment test)≥10 points, used 2 inhalation devices and inhalation technique score ≥8 points had better compliance when compared with other patients (P<0.05). Conclusion Patient education and management should be carried out actively. The patients with course of disease<5 years, CAT<10 points should be highly concerned. The patients' ability to use inhalation devices and personal preference should be fully considered. Training on the use of devices should be strengthened and regularly follow-up evaluation should be carried out.

Analysis of the chemical constituents of Maxing Shigan decoction by UPLC-Q-TOF/MS

ZHAO Xue, GU Yanqiu, CHU Haowen, WU Caisheng, LI Gao, CHEN Xiaofei

In Press doi: 10.12206/j.issn.2097-2024.202306028

Abstract(5614) HTML(1729) PDF (1510KB)(21)

Abstract:
Objective To analyze chemical constituents of compound Maxing Shigan decoction by ultra-high perfor-mance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS). Methods The separation was performed on a UPLC BEH C₁₈ column (2.1 mm×100 mm, 2.5 µm), with a gradient elution applying 0.1% aqueous formic acid solution and 0.1% formic acid acetonitrile as a mobile phase. The column temperature was 40 °C. The flow rate was 0.4 ml/min and the analysis time was 15 min. Mass spectrometry (MS) data were collected in both positive and negative ESI ion modes. Results Through UPLC-QTOF/MS analysis and reference validation, a total of 59 chemical components in Maxing Shigan decoction were identified. Conclusion In this study, an ultra-high performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS) method was established to identify the chemical components of Maxing Shigan decoction. This method is simple, efficient, sensitive and accurate, and provides a basis for the elucidation of the pharmacodynamic material basis and mechanism of Maxing Shigan decoction. It can provide data reference for the optimization of the compatibility of traditional Chinese medicine in the treatment of COVID-19.

Molecular mechanism of Shenling Baizhu powder in treatment of cancer cachexia based on network pharmacology

KE Gang, DONG Qingke, XIAO Shirong, GONG Qian, LI Rong, WANG Daijie

In Press doi: 10.12206/j.issn.2097-2024.202208115

Abstract(7106) HTML(2000) PDF (3143KB)(37)

Abstract:
Objective To analyze the pharmacological mechanism of Shenling Baizhu powder in the treatment of cancer cachexia based on the network pharmacological method and provide a reference for the clinical application of classical traditional Chinese medicine(TCM) prescriptions. Methods Through TCMSP and BATMAN-TCM databases, the main chemical components and their targets of the TCM prescription of Shenling Baizhu powder were obtained, and the active components of the TCM were screened according to ADME. The main targets of cancer cachexia were obtained through OMIM, Genecards, Disgenet and DRUGBANK databases, and protein interaction analysis was conducted using String platform to build a PPI network. The “drug active ingredient target” network of Shenling Baizhu powder was constructed by Cytoscape 3.7.2 software, and then the biological processes and pathways involved were analyzed by using Metascape platform. Finally, molecular docking verification was conducted by Discovery Studio. Results The core active ingredients of Shenling Baizhu powder in the treatment of cancer cachexia are quercetin, kaempferol, pyrolignous acid, stigmasterol, luteolin, β-sitosterol, etc. The core targets are AKT1, TP53, TNF, IL-6, MAPK3, CASP3, JUN, CTNNB1, HIF1A, EGFR, etc. The molecular docking test also showed that the top 10 active ingredients, such as pyrolignous acid, stigmasterol and β-sitosterol, had good binding activities with most of the target sites. The biological pathway of Shenling Baizhu powder in treating cancer cachexia is mainly to regulate tumor related pathway, metabolism related pathway, inflammatory factors and appetite related pathway. Conclusion This study preliminarily revealed the mechanism of action of Shenling Baizhu powder in treating cancer cachexia with multi components, multi targets and multi pathways, which provided a basis for the clinical development and utilization of Shenling Baizhu powder.

The mechanism of nicotinamide combined with amphotericin B against Candida albicans based on metabolomics technology

WAN Lizhi, WANG Jinghan, WU Chunrong, LI Ling

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202307034

Abstract(5166) HTML(1401) PDF (1598KB)(28)

Abstract:
Objective To investigate the potential mechanism of nicotinamide combined with amphotericin B against Candida albicans based on metabolomics. Methods The intracellular metabolites of C. albicans intervened by different drugs including NAM, AmB, and their combination with a proper concentration were analyzed by gas chromatography-mass spectrometry. The differential metabolites were screened by multivariate statistical analysis and identified by searching the NIST database. Results Compared with the control group, the NAM intervention group was hardly separated from it, while the AmB group and NAM+AmB group showed a clear trend separation. Under the intervention of AmB, 23 metabolites significantly changed compared with the control group, and 28 metabolites remarkably changed after NAM+AmB intervention, including amino acids, organic acids, sugars and other components. Conclusion NAM, as an endogenous metabolite of C. albicans, combined with AmB could enhance the effects of AmB in the original metabolic pathway and changed it to a certain extent. It is speculated that AmB combined with NAM may pose more antifungal effect on Candida albicans by regulating the tricarboxylic acid cycle, interfering with amino acid metabolism and influencing polyamine synthesis.

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Abstract(5844) HTML(1410) PDF (699KB)(92)

Abstract:

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.

Abstract(3052) HTML(1006) PDF (0KB)(326)

Abstract:

Lactic acid bacteria as recombinant protein drug delivery carrier

WANG Xufang, WANG Yanting, YAO Chunmeng, LU Bin

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202309021

Abstract(7140) HTML(2429) PDF (863KB)(71)

Abstract:
Lactic acid bacteria is a good candidate in living drug delivery system for its safety, beneficial nature, and intestinal colonizability. At present, most studies use it as a protein drug delivery carrier for disease treatment. As a model organism, a variety of gene modification schemes enable it to be applied to various diseases and can play a significant therapeutic effect. Lactic acid bacteria drug carrier has many advantages, including non-invasive drug delivery, gene editing, large-scale production Therefore, the use of lactic acid bacteria as recombinant protein expression vector has attracted global attention. In this review, the application basis, bioavailability improvement, gene editing strategy and research and application status of lactobacillus drug delivery system were summarized.

Study on the effect of Lishukang capsule on learning and memory impairment in mice with high altitude hypoxia based on Keap1/Nrf2/HO-1 signal pathway

MENG Panpan, SONG Muge, YANG Shichao, CHEN Keming, YANG Zhongduo, MA Huiping

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202303006

Abstract(6427) HTML(1551) PDF (2083KB)(25)

Abstract:
Objective Study on the effect of Lishukang capsule on learning and memory impairment in mice with high altitude hypoxia based on Keap1/Nrf2/HO-1 signal pathway. Methods Sixty male Balb/C mice were randomly divided into normal control group, hypoxia model group, Rhodiola capsule group: 400 mg/kg, low, medium and high dose groups of Lishukang capsule: 400 mg/kg, 600 mg/kg, 800 mg/kg, with 10 mice in each group. The normal control group was fed at the local altitude (1500m) after 7 days of intragastric administration in each group, and the rest groups were fed at the low pressure and hypoxia animal experimental cabin to simulate the altitude of 7500 m for hypoxia for 3 days. During this period, the normal control group and the hypoxia model group were given normal saline once a day, and 1 hour after the last administration, the eight arm maze was used to test the spatial memory ability of mice under simulated high altitude hypoxia; HE staining was used to observe the morphological changes of hippocampus in mice; Western blot was used to detect the changes of protein content of Keap1/Nrf2/HO-1 signal pathway and apoptosis related protein in hippocampus of mice. Results Compared with the normal control group, the spatial memory ability of mice in the hypoxia model group was significantly impaired (P<0.01); HE staining showed that hippocampal neurons in mice were seriously injured; the content of brain tissue Keap1 protein and apoptosis related protein Bax and Caspase-3 increased (P<0.01); the content of Nrf2, HO-1 and apoptosis related protein Bcl-2 decreased (P<0.01). Compared with the hypoxia model group, the error rate of mice in the high dose group of Lishukang capsule in the eight arm maze behavior experiment was significantly reduced (P<0.05, P<0.01); HE staining showed that the neurons were arranged orderly and the cell morphology was good; the content of Keap1 protein and apoptosis related protein Bax and Caspase-3 decreased (P<0.01); the content of Nrf2, HO-1 and apoptosis related protein Bcl-2 increased (P<0.01). Conclusion High altitude hypoxia can lead to oxidative stress injury in mice and induce the expression of apoptosis related genes, thus aggravating the cognitive dysfunction of mice; Lishukang capsule can effectively improve the learning and memory impairment in mice caused by hypoxia, and its mechanism may be related to regulating the Keap1/Nrf2/HO-1 signal pathway and reducing apoptosis.

Determination and effect of five alkaloids from extracts of Piper longum on rats with experimental myocardial ischemia induced by injection of pituitrin

YI Bowen, LIU Huining, ZHENG Rui, REN Jiawei, LIU Yang

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202112011

Abstract(5946) HTML(1703) PDF (999KB)(22)

Abstract:
Objective To determine the content of five alkaloids from extracts of piper longum and test the pharmacodynamic effect of them on rats with experimental myocardial ischemia induced by injection of pituitrin. Methods The content of five alkaloids was determined simultaneously by HPLC. The experimental myocardial ischemia in rats was induced by injection of pituitrin, and the absolute value of T wave change and change of heart rate before and after model establishment were chosen to be the observation index. The effects of large, medium and small dose groups were evaluated. Results Three batches of samples were analyzed, with the contents of piperine for 56.1%, 49.7%, 51.6%; N-isobutyl-(2E,4E)octadecatrienamide for 4.5%, 4.2%, 4.3%; guineensine for 0.46%, 0.38%, 0.40%; piplartine for 1.73%, 1.67%, 1.70% and piperamide for 0.55%, 0.46%, 0.49%, respectively. All dose groups from extracts of piper longum had significantly reduced the absolute value of T wave and almost have no effect on the change of heart rate, except the high dose group showed the effect of reducing heart rate at some time . Conclusion The HPLC method was suitable for the simultaneous determination of five alkaloids from extracts of piper longum. It was shown that extracts of piper longum had good bioactivity in anti-myocardial ischemia.

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Chief Editor: LI Jie Wei

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ISSN 2097-2024 CN 31-2185/R

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