从紫萁科植物中提取的山奈酚衍生物的体外α-葡萄糖苷酶抑制作用及计算研究。
In Vitro α-glucosidase Inhibition and Computational Studies of Kaempferol Derivatives from Dryopteris cycanida.
机构信息
Department of Botany, Islamia College University Peshawar, Peshawar, Pakistan.
Department of Chemistry, University of Malakand, Upper Dir, Pakistan.
出版信息
Curr Top Med Chem. 2020;20(9):731-737. doi: 10.2174/1568026620666200130161033.
BACKGROUND
Dryopteris cycadina has diverse traditional uses in the treatment of various human disorders which are supported by pharmacological studies. Similarly, the phytochemical studies of this plant led to the isolation of numerous compounds.
METHODOLOGY
The present study deals with α-glucosidase inhibition of various kaempferol derivates including kaempferol-3, 4/-di-O-α- L-rhamnopyranoside 1, kaempferol-3, 5-di-O-α-L-rhamnoside 2 and kaempferol-3,7-di-O-α- L-rhamnopyranoside 3.
RESULTS
The results showed marked concentration-dependent inhibition of the enzyme when assayed at different concentrations and the IC50 values of compounds 1-3 were 137±9.01, 110±7.33, and 136±1.10 mM, respectively far better than standard compound, acarbose 290±0.54 mM. The computational studies revealed strong docking scores of these compounds and augmented the in vitro assay.
CONCLUSION
In conclusion, the isolated kaempferol derivatives 1-3 from D. cycadina exhibited potent α- glucosidase inhibition.
背景
鳞毛蕨属植物在治疗各种人类疾病方面具有多种传统用途，这些用途得到了药理学研究的支持。同样，对这种植物的植物化学研究导致了许多化合物的分离。
方法
本研究涉及各种山柰酚衍生物对α-葡萄糖苷酶的抑制作用，包括山柰酚-3,4/-二-O-α-L-鼠李吡喃糖苷 1、山柰酚-3,5-二-O-α-L-鼠李糖苷 2 和山柰酚-3,7-二-O-α-L-鼠李吡喃糖苷 3。
结果
结果表明，当在不同浓度下进行测定时，这些化合物在浓度依赖性上对酶表现出显著的抑制作用，化合物 1-3 的 IC50 值分别为 137±9.01、110±7.33 和 136±1.10mM，明显优于标准化合物阿卡波糖 290±0.54mM。计算研究显示这些化合物具有很强的对接评分，并增强了体外测定。
结论
总之，从鳞毛蕨属植物中分离出的山柰酚衍生物 1-3 对α-葡萄糖苷酶表现出很强的抑制作用。
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