Studies on the synthesis and anti-fatigue activity of the salidroside derivatives

ZHENG Wei; CAO Xufang; ZHANG Kaixia; SUN Liang; JIN Yongsheng; GUO Liangjun

doi:10.3969/j.issn.1006-0111.2018.01.012

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Objective A series of 4 substituted salidroside derivatives were designed and synthesized. Their anti-fatigue effects were investigated. Methods With five-acetyl glucose and different 4-substituted benzyl tyrosols as the starting materials,salidroside derivatives were synthesized through glycosidation and deacetylation reactions. The exercise exhaustive mice model was used to study the anti-fatigue effects of those synthesized derivatives by comparing the loading swimming time of mice. Results 10 novel salidroside derivatives were synthesized. The loading swimming tests showed that the swimming time of the mice in the positive group (salidroside) and 3a -1 group (phenethyl-β-D-glucoside) was longer than that in the control group with statistically significant difference(P<0.05). The swimming times for other groups were similar to control group with no statistically significant difference. Conclusion This synthetic method for salidroside derivatives was convenient and feasible for large production. The 4-hydroxyl groups on the benzene ring of salidroside and its derivatives may be the active site responsible for their anti-fatigue activity.

Studies on the synthesis and anti-fatigue activity of the salidroside derivatives

1. Department of Drug and Equipment, No. 98 Hospital of PLA, Huzhou 313000, China

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

Received Date: 2017-06-14

Rev Recd Date: 2017-07-17

Key words:

salidroside /
derivatives /
anti-fatigue

Abstract: Objective A series of 4 substituted salidroside derivatives were designed and synthesized. Their anti-fatigue effects were investigated. Methods With five-acetyl glucose and different 4-substituted benzyl tyrosols as the starting materials,salidroside derivatives were synthesized through glycosidation and deacetylation reactions. The exercise exhaustive mice model was used to study the anti-fatigue effects of those synthesized derivatives by comparing the loading swimming time of mice. Results 10 novel salidroside derivatives were synthesized. The loading swimming tests showed that the swimming time of the mice in the positive group (salidroside) and 3a -1 group (phenethyl-β-D-glucoside) was longer than that in the control group with statistically significant difference(P<0.05). The swimming times for other groups were similar to control group with no statistically significant difference. Conclusion This synthetic method for salidroside derivatives was convenient and feasible for large production. The 4-hydroxyl groups on the benzene ring of salidroside and its derivatives may be the active site responsible for their anti-fatigue activity.

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Studies on the synthesis and anti-fatigue activity of the salidroside derivatives

doi: 10.3969/j.issn.1006-0111.2018.01.012

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