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基于网络药理学剖析黄芪-黄连药对抗胰岛素抵抗的活性成分及保护机制

Network Pharmacology-Based Dissection of the Active Ingredients and Protective Mechanism of the and Herb Pair against Insulin Resistance.

作者信息

Yang Xin-Yu, Wang Wen-Xiao, Huang Yu-Xi, Yue Shi-Jun, Zhang Bai-Yang, Gao Huan, Zhang Lei, Yan Dan, Tang Yu-Ping

机构信息

Department of Pharmacy, Beijing Key Laboratory of Bio-characteristic Profiling for Evaluation of Rational Drug Use, Beijing Shijitan Hospital, Capital Medical University, Beijing 100038, China.

Key Laboratory of Shaanxi Administration of Traditional Chinese Medicine for TCM Compatibility, Shaanxi University of Chinese Medicine, Xi'an 712046, China.

出版信息

ACS Omega. 2021 Jun 30;6(27):17276-17288. doi: 10.1021/acsomega.1c01209. eCollection 2021 Jul 13.

DOI:10.1021/acsomega.1c01209
PMID:34278114
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8280704/
Abstract

The and herb pair (DQ) has been widely utilized in traditional Chinese medicine for the longevity and for preventing and treating cardio-cerebrovascular diseases. Often associated with cardio-cerebrovascular diseases are comorbidities such as insulin resistance. However, the protective mechanisms of DQ against insulin resistance remain not well understood. Through network pharmacology analysis, a total of 94 candidate active compounds selected from DQ (61 from Bunge and 33 from (Burk.) F. H. Chen) interacted with 52 corresponding insulin resistance-related targets, which mainly involved insulin resistance and the AMPK signaling pathway. Furthermore, the contribution index calculation results indicated 25 compounds as the principal components of this herb pair against insulin resistance. Among them, ginsenoside F2, protocatechuic acid, and salvianolic acid B were selected and validated to promote glucose consumption through activating AMPK phosphorylation and upregulating GLUT4 in insulin-resistant cell model (HepG2/IR) cells. These findings indicated that DQ has the potential for repositioning in the treatment of insulin resistance mainly through the AMPK signaling pathway.

摘要

大黄和人参药对（DQ）在传统中药中已被广泛用于延年益寿以及预防和治疗心脑血管疾病。与心脑血管疾病常伴发的合并症如胰岛素抵抗。然而，DQ对胰岛素抵抗的保护机制仍未完全清楚。通过网络药理学分析，从DQ中筛选出的94种候选活性化合物（61种来自人参，33种来自大黄）与52个相应的胰岛素抵抗相关靶点相互作用，这些靶点主要涉及胰岛素抵抗和AMPK信号通路。此外，贡献指数计算结果表明25种化合物是该药对抵抗胰岛素抵抗的主要成分。其中，人参皂苷F2、原儿茶酸和丹酚酸B经筛选和验证，可通过激活AMPK磷酸化和上调胰岛素抵抗细胞模型（HepG2/IR）细胞中的GLUT4来促进葡萄糖消耗。这些发现表明，DQ主要通过AMPK信号通路在治疗胰岛素抵抗方面具有重新定位的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0b9/8280704/45a1c4fd06db/ao1c01209_0007.jpg
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