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开发并验证了一种新的 HPTLC-HRMS 方法,用于定量测定从 中提取的强效胰腺脂肪酶抑制剂先导化合物 Echitamine。

Development and validation of a new HPTLC-HRMS method for the quantification of a potent pancreatic lipase inhibitory lead Echitamine from .

机构信息

Laboratory of Natural Product Chemistry, Department of Pharmacy, Birla Institute of Technology and Science, Pilani-333031 (BITS Pilani), Pilani, Rajasthan, India.

出版信息

Nat Prod Res. 2021 Nov;35(22):4680-4684. doi: 10.1080/14786419.2019.1705817. Epub 2019 Dec 24.

Abstract

is an important indole alkaloid rich medicinal plant with diverse pharmacological activity. To understand the effect of extraction techniques, the stem bark sample of was subjected to continuous hot percolation, ultrasonic extraction, and cold maceration techniques. Continuous hot percolation technique extractive exhibited a potential pancreatic lipase (PL) inhibitory activity and further bio-assay guided fractionation resulted in the isolation of echitamine with a PL inhibitory activity (IC = 10.92 µM). A new validated HPTLC-HRMS method was developed for the quantification of echitamine by using a mobile phase of chloroform: methanol (80:20, v/v) with 0.04% formic acid. Echitamine content in the individual extractives were in direct correlation with the PL inhibitory activity (Pearson's r = -0.9409). The molecular docking studies further confirmed the PL inhibitory potential of echitamine. These results clearly highlight the role of echitamine as a natural product-based lead for potent PL inhibitory activity.

摘要

是一种富含吲哚生物碱的重要药用植物,具有多种药理学活性。为了了解提取技术的效果,对 的茎皮样品进行了连续热渗滤、超声提取和冷浸技术处理。连续热渗滤技术提取物表现出潜在的胰腺脂肪酶 (PL) 抑制活性,进一步的生物测定指导分离得到具有 PL 抑制活性的麦角新碱(IC = 10.92 μM)。建立了一种新的经验证的 HPTLC-HRMS 方法,用于通过使用氯仿:甲醇(80:20,v/v)与 0.04%甲酸的流动相定量测定麦角新碱。各提取物中的麦角新碱含量与 PL 抑制活性呈直接相关(Pearson's r = -0.9409)。分子对接研究进一步证实了麦角新碱的 PL 抑制潜力。这些结果清楚地强调了麦角新碱作为基于天然产物的潜在强效 PL 抑制活性的先导化合物的作用。

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