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基于生物测定的方法从 Buch-Ham ex D Don. 的果实中分离得到具有强α-葡萄糖苷酶抑制活性的化合物及其筛选

Bioassay-guided isolation of potent α-glucosidase inhibitory compounds from the fruit of Buch-Ham ex D Don. and their screening.

机构信息

Natural Product Chemistry section, CSIR-North East Institute of Science and Technology, Branch Itanagar, Naharlagun, Arunachal Pradesh-791110, India.

Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.

出版信息

Nat Prod Res. 2022 Aug;36(16):4243-4248. doi: 10.1080/14786419.2021.1973464. Epub 2021 Sep 14.

Abstract

Two bioactive compounds caffeic and sinapic acid were isolated from the fruit of the Buch-Ham ex D Don using bioassay guided approach. These compounds were isolated from water fraction using column chromatography followed by semi preparative HPLC. These compounds showed very potent anti-diabetic and antioxidant activities. The molecular docking was carried out to predict the mode of interaction of the isolated compounds with α-glucosidase. The α-glucosidase inhibitory activity of caffeic and sinapic acid was determined, and their IC values were found 0.67 and 0.82 µg/ml, respectively. A QSAR equation was generated with an value of 84.81%, which is suitable enough for predicting the IC values of test molecules. The aforementioned finding confirms the isolated compounds show very significant anti-diabetic potential which is supported by the molecular docking and QSAR study. So, it has ample scope for drug development with further and clinical study.

摘要

采用生物活性导向方法,从 Buch-Ham ex D Don 的果实中分离出两种生物活性化合物咖啡酸和芥子酸。这些化合物是用水部分通过柱色谱分离,然后通过半制备 HPLC 进一步分离得到的。这些化合物表现出很强的抗糖尿病和抗氧化活性。进行了分子对接,以预测分离化合物与 α-葡萄糖苷酶的相互作用模式。测定了咖啡酸和芥子酸的 α-葡萄糖苷酶抑制活性,它们的 IC 值分别为 0.67 和 0.82 μg/ml。生成了一个 QSAR 方程, 值为 84.81%,足以用于预测测试分子的 IC 值。上述发现证实,分离出的化合物表现出非常显著的抗糖尿病潜力,这得到了分子对接和 QSAR 研究的支持。因此,它具有进一步和临床研究的药物开发的广阔前景。

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