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[黄芩苷和黄芩素作为纤维化疾病潜在治疗药物的研究进展]

[Research advances on baicalin and baicalein as potential therapeutic agents for fibrotic disease].

作者信息

Zhu Qing-Jun

机构信息

School of Traditional Chinese Medicine, Shandong University of Traditional Chinese Medicine, Ji'nan 250355, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2017 Apr;42(7):1271-1276. doi: 10.19540/j.cnki.cjcmm.20170224.018.

DOI:10.19540/j.cnki.cjcmm.20170224.018
PMID:29052385
Abstract

Tissue and organ fibrosis is the major cause for disability and death related to a variety of diseases worldwide. As specific therapies to halt, or even to reverse the existing tissue fibrosis are not yet available, it is of great significance to find new anti-fibrosis therapeutic agents. Tissue and organ fibrosis is a nonphysiological scarring process, associated with excessive deposition of extracellular matrix, and leads to impairment of organ function. Fibrotic lesions of all organs show similar histological abnormalities. In recent years, plenty of studies showed that Baicalin and baicalein had anti-fibrosis effects in different tissues or organs. In this paper, the effects and mechanisms of baicalin and baicalein on different organ fibrosis were reviewed. Baicalin and its aglycone baicalein had similarity in structural and pharmacological characteristics, with broad biotransformation effect within the body. The research suggested that baicalin and baicalein can suppress different tissue and organ fibrosis occurrence and development via various mechanisms, including down-regulating expression of promote-fibrosis cytokines, inhibiting pro-fibrogenic signaling pathways, anti-inflammatory and anti-oxidant effects. Though baicalin and baicalein are promising anti-fibrosis agents, there is still a long way to go before being approved as specific anti-fibrotic drugs.

摘要

组织和器官纤维化是全球范围内与多种疾病相关的致残和死亡的主要原因。由于目前尚无阻止甚至逆转现有组织纤维化的特异性疗法,因此寻找新的抗纤维化治疗药物具有重要意义。组织和器官纤维化是一种非生理性瘢痕形成过程,与细胞外基质的过度沉积有关,并导致器官功能受损。所有器官的纤维化病变都表现出相似的组织学异常。近年来,大量研究表明黄芩苷和黄芩素在不同组织或器官中具有抗纤维化作用。本文综述了黄芩苷和黄芩素对不同器官纤维化的作用及机制。黄芩苷及其苷元黄芩素在结构和药理特性上具有相似性,在体内具有广泛的生物转化作用。研究表明,黄芩苷和黄芩素可通过多种机制抑制不同组织和器官纤维化的发生和发展,包括下调促纤维化细胞因子的表达、抑制促纤维化信号通路、抗炎和抗氧化作用。尽管黄芩苷和黄芩素是很有前景的抗纤维化药物,但在被批准为特异性抗纤维化药物之前仍有很长的路要走。

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[Research advances on baicalin and baicalein as potential therapeutic agents for fibrotic disease].[黄芩苷和黄芩素作为纤维化疾病潜在治疗药物的研究进展]
Zhongguo Zhong Yao Za Zhi. 2017 Apr;42(7):1271-1276. doi: 10.19540/j.cnki.cjcmm.20170224.018.
2
Network pharmacology and molecular docking analysis on molecular targets: Mechanisms of baicalin and baicalein against hyperuricemic nephropathy.基于分子靶点的网络药理学与分子对接分析:黄芩苷和黄芩素抗高尿酸血症肾病的作用机制
Toxicol Appl Pharmacol. 2021 Aug 1;424:115594. doi: 10.1016/j.taap.2021.115594. Epub 2021 May 24.
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Exploring the chemopreventive properties and perspectives of baicalin and its aglycone baicalein in solid tumors.探索黄芩苷及其苷元黄芩素在实体瘤中的化学预防特性及前景。
Eur J Med Chem. 2017 Jan 27;126:844-852. doi: 10.1016/j.ejmech.2016.11.058. Epub 2016 Dec 1.
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In vitro potential modulation of baicalin and baicalein on P-glycoprotein activity and expression in Caco-2 cells and rat gut sacs.黄芩苷和黄芩素对Caco-2细胞及大鼠肠囊模型中P-糖蛋白活性和表达的体外潜在调节作用
Pharm Biol. 2016 Sep;54(9):1548-56. doi: 10.3109/13880209.2015.1107744. Epub 2016 Jan 25.
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Baicalin protects mice against Salmonella typhimurium infection via the modulation of both bacterial virulence and host response.黄芩苷通过调节细菌毒力和宿主反应来保护小鼠免受鼠伤寒沙门氏菌感染。
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Role of Intestinal Microbiota in Baicalin-Induced Drug Interaction and Its Pharmacokinetics.肠道微生物群在黄芩苷诱导的药物相互作用及其药代动力学中的作用。
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Differential inhibitory effects of baicalein and baicalin on LPS-induced cyclooxygenase-2 expression through inhibition of C/EBPbeta DNA-binding activity.黄芩素和黄芩苷通过抑制C/EBPβ DNA结合活性对脂多糖诱导的环氧化酶-2表达的差异抑制作用。
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Baicalein and baicalin promote antitumor immunity by suppressing PD-L1 expression in hepatocellular carcinoma cells.黄芩素和黄芩苷通过抑制肝癌细胞 PD-L1 表达促进抗肿瘤免疫。
Int Immunopharmacol. 2019 Oct;75:105824. doi: 10.1016/j.intimp.2019.105824. Epub 2019 Aug 19.
9
Exploring therapeutic potentials of baicalin and its aglycone baicalein for hematological malignancies.探索黄芩苷及其苷元黄芩素对血液系统恶性肿瘤的治疗潜力。
Cancer Lett. 2014 Nov 1;354(1):5-11. doi: 10.1016/j.canlet.2014.08.003. Epub 2014 Aug 13.
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Mechanistic and therapeutic perspectives of baicalin and baicalein on pulmonary hypertension: A comprehensive review.基于黄芩素和黄芩苷的肺动脉高压发病机制和治疗学研究进展:一篇综述。
Biomed Pharmacother. 2022 Jul;151:113191. doi: 10.1016/j.biopha.2022.113191. Epub 2022 May 25.

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Baicalin inhibits PDGF-BB-induced hepatic stellate cell proliferation, apoptosis, invasion, migration and activation via the miR-3595/ACSL4 axis.黄芩素通过 miR-3595/ACSL4 轴抑制 PDGF-BB 诱导的肝星状细胞增殖、凋亡、侵袭、迁移和激活。
Int J Mol Med. 2018 Apr;41(4):1992-2002. doi: 10.3892/ijmm.2018.3427. Epub 2018 Jan 25.