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芒果苷衍生物的合成及其PTP1B酶抑制活性研究

周宇,  胡丽娜,  罗剑飞,  俞世冲,  吴秋业

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周宇, 胡丽娜, 罗剑飞, 俞世冲, 吴秋业. 芒果苷衍生物的合成及其PTP1B酶抑制活性研究[J]. 药学实践与服务, 2011, 29(3): 193-196.
引用本文: 周宇, 胡丽娜, 罗剑飞, 俞世冲, 吴秋业. 芒果苷衍生物的合成及其PTP1B酶抑制活性研究[J]. 药学实践与服务, 2011, 29(3): 193-196.
shu
ZHOU Yu, HU Li-na, LUO Jian-fei, YU Shi-chong, WU Qiu-ye. Synthesis and PTP1B activity of enzyme inhibition of mangiferin derivates[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(3): 193-196.
Citation: ZHOU Yu, HU Li-na, LUO Jian-fei, YU Shi-chong, WU Qiu-ye. Synthesis and PTP1B activity of enzyme inhibition of mangiferin derivates[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(3): 193-196.
shu

芒果苷衍生物的合成及其PTP1B酶抑制活性研究

  • 1.

    解放军第82医院,江苏 淮安 223001

  • 2.

    第二军医大学有机化学教研室,上海 200433

基金项目: 上海市科委基础重点项目 ( 08JC1405500).

Synthesis and PTP1B activity of enzyme inhibition of mangiferin derivates

  • 1.

    NO. 82 Hospital of PLA, Huaian 223001,China

  • 2.

    Department of Organic Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China

  • 摘要: 目的 设计合成一系列芒果苷衍生物并进行体外蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性实验。 方法 利用亲核取代反应在芒果苷上引入疏水苄基,设计合成8个新化合物4~11,采用比色法对化合物进行PTP1B抑制活性研究。 结果 设计合成的8个化合物对PTP1B酶都有一定的抑制作用。 结论 芒果苷衍生物的活性明显好于芒果苷本身的活性,苄基的对位取代活性要优于邻位和间位取代,且苄基上氯原子取代的衍生物要高于其它原子取代的化合物活性。
    Abstract: Objective To synthetize and conduct PTP1B inhibitory activity experiment of series of novel mangiferin derivates. Methods Different benzyl groups were introduced to mangiferin framework by nucleophilic substitution reaction. All the compounds were screened against protein tyrosine phosphatase 1B(PTP1B)with the colorimetrie assay. Results Eight compounds were synthesized and all the compounds exhibited PTP1B inhibitory activity to some extent. Conclusions Derivates of mangiferin remarkably enhanced the activity compared with mangiferin itself. In addition, the benzylated derivates with chloro atom had better inhibitory activity than other substitution groups. Furthermore,the para position of the benzyl was a better place for introducing substituent than meta and ortho position.
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    [2] 彭志刚,罗 军,赖永熔,等.芒果苷对K562胞端粒酶活性和细胞周期的影响[J].中药药理与临床,2007, 23(1): 13.
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    [7] Miura T, Ichiki H, Hashimoto I, et al. Antidiabetic activity of a xanthone compound, mangiferin[J]. Phytomedicine, 2001, 8(2): 85.
    [8] Pei Z, Liu G, Lubben TH, et al. Inhibition of protein tyrosine phosphatase 1B as a potential treatment of diabetes and obesity[J]. Curr Pharm Des, 2004, 10(28): 3481.
    [9] Dadke S, Chernoff J. Protein-tyrosine phosphatase 1B as a potential drug target for obesity[J]. Curr Drug Targets Immune Endocr Metabol Disord, 2003, 3(4): 299.
    [10] Kim HO, Blaskovich MA. Recent discovery and development of protein tyrosine phosphatase inhibitors[J]. Expert Opin Ther Patents, 2002, 12(6): 871.
    [11] Elchebly M, Payette P, Michaliszyn E, et al. Increased insulin sensitivity and obesity resistance in mice lacking the protein tyrosine phosphatase-1B gene[J]. Science, 1999, 283(5407): 1544.
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    [13] 廖洪利,陈 军,杨 倩.芒果苷衍生物的制备[J].药学实践杂志,2010, 27(5): 49.
    [14] Goldstein BJ, Bittner-Kowalezyk A, White MF, et al. Tyrosine dephosphorylation and deactivation of insulin receptor substrate-1 by protein-tyrosine phosphatase 1B: Possible facilitation by the formation of a ternary complex with the GRB2 adaptor protein[J]. J Biol Chem, 2000, 275: 4283.
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  • 收稿日期:  2011-01-06
  • 修回日期:  2011-03-10

芒果苷衍生物的合成及其PTP1B酶抑制活性研究

  • 1. 解放军第82医院,江苏 淮安 223001
  • 2. 第二军医大学有机化学教研室,上海 200433
    • 基金项目:  上海市科委基础重点项目 ( 08JC1405500).
  • 收稿日期: 2011-01-06
  • 修回日期: 2011-03-10

摘要: 目的 设计合成一系列芒果苷衍生物并进行体外蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性实验。 方法 利用亲核取代反应在芒果苷上引入疏水苄基,设计合成8个新化合物4~11,采用比色法对化合物进行PTP1B抑制活性研究。 结果 设计合成的8个化合物对PTP1B酶都有一定的抑制作用。 结论 芒果苷衍生物的活性明显好于芒果苷本身的活性,苄基的对位取代活性要优于邻位和间位取代,且苄基上氯原子取代的衍生物要高于其它原子取代的化合物活性。

English Abstract

周宇, 胡丽娜, 罗剑飞, 俞世冲, 吴秋业. 芒果苷衍生物的合成及其PTP1B酶抑制活性研究[J]. 药学实践与服务, 2011, 29(3): 193-196.
引用本文: 周宇, 胡丽娜, 罗剑飞, 俞世冲, 吴秋业. 芒果苷衍生物的合成及其PTP1B酶抑制活性研究[J]. 药学实践与服务, 2011, 29(3): 193-196.
shu
ZHOU Yu, HU Li-na, LUO Jian-fei, YU Shi-chong, WU Qiu-ye. Synthesis and PTP1B activity of enzyme inhibition of mangiferin derivates[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(3): 193-196.
Citation: ZHOU Yu, HU Li-na, LUO Jian-fei, YU Shi-chong, WU Qiu-ye. Synthesis and PTP1B activity of enzyme inhibition of mangiferin derivates[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(3): 193-196.
shu

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