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具有蛋白酪氨酸磷酸酶 1B 抑制活性的总皂苷水解产物中的新达玛烷型三萜皂苷。

New dammarane-type triterpenoids from hydrolyzate of total saponins with protein tyrosine phosphatase 1B inhibitory activity.

机构信息

Guizhou Engineering Research Center of Industrial Key-technology for Dendrobium Nobile, Zunyi Medical University, Zunyi, Guizhou, China.

Joint International Research Laboratory of Ethnomedicine of Ministry of Education, Zunyi Medical University, Zunyi, Guizhou, China.

出版信息

J Enzyme Inhib Med Chem. 2023 Dec;38(1):2281263. doi: 10.1080/14756366.2023.2281263. Epub 2023 Nov 15.

DOI:10.1080/14756366.2023.2281263
PMID:37965892
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10653776/
Abstract

Protein tyrosine phosphatase 1B (PTP1B) is a key factor and regulator of glucose, lipid metabolism throughout the body, and a promising target for treatment of type 2 diabetes mellitus (T2DM). is a famous oriental traditional medicinal herbal plant and functional food, which has shown many beneficial effects on glucose and lipid metabolism. The aim of the present study is to assess the inhibitory activity of five new and four known dammarane triterpenoids isolated from the hydrolysate product of total saponins. The bioassay data showed that all the compounds exhibited significant inhibitory activity against PTP1B. The structure-activity relationship showed that the strength of PTP1B inhibitory activity was mainly related to the electron-donating group on its side chain. Molecular docking analysis suggested that its mechanism may be due to the formation of competitive hydrogen bonding between the electron-donating moiety and the Asp48 amino acid residues on the PTP1B protein.

摘要

蛋白酪氨酸磷酸酶 1B（PTP1B）是调节全身葡萄糖、脂质代谢的关键因子，也是治疗 2 型糖尿病（T2DM）的有希望的靶点。黄芪是一种著名的东方传统药用草本植物和功能性食品，对葡萄糖和脂质代谢有许多有益的作用。本研究的目的是评估从总皂苷水解产物中分离得到的 5 种新的和 4 种已知的达玛烷三萜的抑制活性。生物测定数据表明，所有化合物对 PTP1B 均表现出显著的抑制活性。构效关系表明，PTP1B 抑制活性的强弱主要与其侧链上的供电子基团有关。分子对接分析表明，其作用机制可能是由于供电子部分与 PTP1B 蛋白上的 Asp48 氨基酸残基形成竞争性氢键。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/eaa069739854/IENZ_A_2281263_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/680701837ec0/IENZ_A_2281263_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/fc95cf64172f/IENZ_A_2281263_F0002_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/8ba5a46ab8e8/IENZ_A_2281263_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/6635694d68a4/IENZ_A_2281263_SCH0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/a51bda7fa4a6/IENZ_A_2281263_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/eaa069739854/IENZ_A_2281263_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/680701837ec0/IENZ_A_2281263_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/fc95cf64172f/IENZ_A_2281263_F0002_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/8ba5a46ab8e8/IENZ_A_2281263_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/6635694d68a4/IENZ_A_2281263_SCH0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/a51bda7fa4a6/IENZ_A_2281263_F0004_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1a/10653776/eaa069739854/IENZ_A_2281263_F0005_C.jpg

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