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从生长于埃及的沙漠植物叶片中分离出的内生菌sp. 的酚类化合物的抗糖尿病活性。

Anti-diabetic activities of phenolic compounds of sp., an endophyte isolated from the leaves of desert plants growing in Egypt.

作者信息

Elbermawi Ahmed, Ali Ahmed R, Amen Yhiya, Ashour Ahmed, Ahmad Kadria F, Mansour El-Sayed S, Halim Ahmed F

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University Mansoura 35516 Egypt

Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University Mansoura 35516 Egypt

出版信息

RSC Adv. 2022 Sep 1;12(38):24935-24945. doi: 10.1039/d2ra02532a. eCollection 2022 Aug 30.

DOI:10.1039/d2ra02532a
PMID:36199870
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9434606/
Abstract

Six phenolic compounds (talaroflavone (1), alternarienoic acid (2), altenuene (3), altenusin (4), alternariol (5), and alternariol-5--methyl ether (6)) were isolated from the solid rice culture media of sp., an endophyte isolated from the fresh leaves of three desert plants, Dammer (Solanaceae), L. (Amaryllidaceae) and L. (Apocynaceae). Compounds 2, 3, and 4 exhibited potent α-glucosidase and lipase inhibitory activities suggesting that they might act as naturally occurring anti-diabetic candidates. The same compounds showed potent binding in the active site for both enzymes with desirable pharmacokinetic properties. The isolated bioactive compounds were not exclusive to a certain host plant which reveals the dominant ecological standpoints for consequent optimization. This could lead to a cost-effective and reproducible yield applicable to commercial scale-up.

摘要

从三种沙漠植物新鲜叶片中分离得到的内生真菌的固体水稻培养基中，分离出六种酚类化合物（塔拉罗黄酮（1）、链格孢菌烯酸（2）、链格孢菌素（3）、链格孢菌素（4）、链格孢酚（5）和链格孢酚 - 5 - 甲基醚（6）），这三种沙漠植物分别为茄科的、石蒜科的 和夹竹桃科的 。化合物2、3和4表现出强大的α - 葡萄糖苷酶和脂肪酶抑制活性，表明它们可能作为天然的抗糖尿病候选物。相同的化合物在两种酶的活性位点均表现出强大的结合能力，并具有理想的药代动力学性质。分离得到的生物活性化合物并非特定宿主植物所独有，这揭示了后续优化的主要生态观点。这可能会带来适用于商业扩大规模的具有成本效益且可重复的产量。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/e59fd618345f/d2ra02532a-f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/67c73f186048/d2ra02532a-f1.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/31157407ad66/d2ra02532a-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/cbc126127bed/d2ra02532a-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/37856664bf5e/d2ra02532a-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/2e7889a315d7/d2ra02532a-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/e59fd618345f/d2ra02532a-f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/67c73f186048/d2ra02532a-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/3ff832ae9859/d2ra02532a-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/31157407ad66/d2ra02532a-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/cbc126127bed/d2ra02532a-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/37856664bf5e/d2ra02532a-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/2e7889a315d7/d2ra02532a-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ecc/9434606/e59fd618345f/d2ra02532a-f7.jpg

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