State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China; Department of Pharmacy, Fifth Medical Center of PLA General Hospital, Beijing, 100039, China.
Pharmacol Res. 2021 Mar;165:105444. doi: 10.1016/j.phrs.2021.105444. Epub 2021 Jan 22.
With the development of high-throughput screening and bioinformatics technology, natural products with a range of pharmacological targets in multiple diseases have become important sources of new drug discovery. These compounds are derived from various plants, including the dried root of Scutellaria baicalensis Georgi, which is often used as a traditional Chinese herb named Huangqin, a popular medication used for thousands of years in China. Many studies have shown that baicalin, an extract from Scutellaria baicalensis Georgi, exerts various protective effects on liver and gut diseases. Baicalin plays a therapeutic role mainly by mediating downstream apoptosis and immune response pathways induced by upstream oxidative stress and inflammation. During oxidative stress regulation, PI3K/Akt/NRF2, Keap-1, NF-κB and HO-1 are key factors associated with the healing effects of baicalin on NAFLD/NASH, ulcerative colitis and cholestasis. In the inflammatory response, IL-6, IL-1β, TNF-α, MIP-2 and MIP-1α are involved in the alleviation of NAFLD/NASH, cholestasis and liver fibrosis by baicalin, as are TGF-β1/Smads, STAT3 and NF-κB. Regarding the apoptosis pathway, Bax, Bcl-2, Caspase-3 and Caspase-9 are key factors related to the suppression of hepatocellular carcinoma and attenuation of liver injury and colorectal cancer. In addition to immune regulation, PD-1/PDL-1 and TLR4-NF-κB are correlated with the alleviation of hepatocellular carcinoma, ulcerative colitis and colorectal cancer by baicalin. Moreover, baicalin regulates intestinal flora by promoting the production of SCFAs. Furthermore, BA is involved in the interactions of the liver-gut axis by regulating TGR5, FXR, bile acids and the microbiota. In general, a comprehensive analysis of this natural compound was conducted to determine the mechanism by which it regulates bile acid metabolism, the intestinal flora and related signaling pathways, providing new insights into the pharmacological effects of baicalin. The mechanism linking the liver and gut systems needs to be elucidated to draw attention to its great clinical importance.
随着高通量筛选和生物信息学技术的发展，具有多种疾病多种药理靶点的天然产物已成为新药发现的重要来源。这些化合物来源于各种植物，包括黄芩的干燥根，黄芩是一种常用的中国传统草药，在中国已使用了数千年。许多研究表明，黄芩中的一种提取物黄芩苷对肝脏和肠道疾病具有多种保护作用。黄芩苷主要通过调节上游氧化应激和炎症诱导的下游凋亡和免疫反应途径发挥治疗作用。在氧化应激调节中，PI3K/Akt/NRF2、Keap-1、NF-κB 和 HO-1 是与黄芩苷对非酒精性脂肪性肝病/非酒精性脂肪性肝炎、溃疡性结肠炎和胆汁淤积的治疗作用相关的关键因素。在炎症反应中，IL-6、IL-1β、TNF-α、MIP-2 和 MIP-1α 参与了黄芩苷对非酒精性脂肪性肝病/非酒精性脂肪性肝炎、胆汁淤积和肝纤维化的缓解，TGF-β1/Smads、STAT3 和 NF-κB 也是如此。关于凋亡途径，Bax、Bcl-2、Caspase-3 和 Caspase-9 是与黄芩苷抑制肝癌和减轻肝损伤和结直肠癌相关的关键因素。除了免疫调节，PD-1/PDL-1 和 TLR4-NF-κB 与黄芩苷对肝癌、溃疡性结肠炎和结直肠癌的缓解有关。此外，黄芩苷通过促进 SCFAs 的产生来调节肠道菌群。此外，BA 通过调节 TGR5、FXR、胆汁酸和微生物群来参与肝肠轴的相互作用。总之，对这种天然化合物进行了综合分析，以确定其调节胆汁酸代谢、肠道菌群和相关信号通路的机制，为黄芩苷的药理作用提供了新的见解。需要阐明连接肝脏和肠道系统的机制，以引起对其重要临床意义的关注。
