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丹参重要活性成分隐丹参酮的生物活性与药理学综述。

A review of the biological activity and pharmacology of cryptotanshinone, an important active constituent in Danshen.

作者信息

Li Huayao, Gao Chundi, Liu Cun, Liu Lijuan, Zhuang Jing, Yang Jing, Zhou Chao, Feng Fubin, Sun Changgang, Wu Jibiao

机构信息

College of Chinese Medicine, Shandong University of Traditional Chinese Medicine, Jinan, 250014, Shandong, PR China.

College of First Clinical Medicine, Shandong University of Traditional Chinese Medicine, Jinan, 250014, Shandong, PR China.

出版信息

Biomed Pharmacother. 2021 May;137:111332. doi: 10.1016/j.biopha.2021.111332. Epub 2021 Feb 4.

DOI:10.1016/j.biopha.2021.111332
PMID:33548911
Abstract

Cryptotanshinone (IUPAC name: (R)-1,2,6,7,8,9-hexahydro-1,6,6-trimethyl-phenanthro(1,2-b)furan-10,11-dione), a biologically active constituent extracted from the roots and rhizomes of the plant Salvia miltiorrhiza, has been studied in depth as a medicinally active compound and shown to have efficacy in the treatment of numerous diseases and disorders. In this review, we describe in detail the current status of cryptotanshinone research, including findings relating to the structure, pharmacokinetics, pharmacological activity, and derivatives of this compound. Cryptotanshinoneh as a diverse range of pharmacological effects, including anti-cancer, anti-inflammatory, immune regulatory, neuroprotective, and anti-fibrosis activities. Studies on the molecular mechanisms underlying the activities of cryptotanshinone have established that the JAK2/STAT3, PI3K/AKT, NF-κB, AMPK, and cell cycle pathways are involved in the inhibitory and pro-apoptotic effects of cryptotanshinone on different tumor cell lines, these molecular pathways interact in a coordinated manner to inhibit cell proliferation, migration and invasion,and induce transformation, autophagy, necrosis, and cellular immunity. The anti-inflammatory mechanisms of cryptotanshinone have been found to be associated with the TLR4-MyD88/PI3K/Nrf2 and TLR4-MyD88/NF-κB/MAPK pathways, whereasthe Hedgehog, NF-κB, and Nrf-2/HO-1 pathways are regulated by cryptotanshinone to reduce organ fibrosis, and its inhibitory effects on the PI3K/AKT-eNOS pathway have been linked to neuroprotective effects. Given the potential medicinal utility of cryptotanshinone, further research is needed to verify the efficacy and safety of this compound in clinical use, evaluate its pharmacological activity, and identify molecular targets.

摘要

隐丹参酮(IUPAC名称:(R)-1,2,6,7,8,9-六氢-1,6,6-三甲基-菲并(1,2-b)呋喃-10,11-二酮)是从植物丹参的根和根茎中提取的一种生物活性成分,作为一种具有药用活性的化合物已得到深入研究,并显示出对多种疾病和病症具有治疗功效。在本综述中,我们详细描述了隐丹参酮的研究现状,包括与该化合物的结构、药代动力学、药理活性和衍生物相关的研究结果。隐丹参酮具有多种药理作用,包括抗癌、抗炎、免疫调节、神经保护和抗纤维化活性。对隐丹参酮活性的分子机制研究表明,JAK2/STAT3、PI3K/AKT、NF-κB、AMPK和细胞周期途径参与了隐丹参酮对不同肿瘤细胞系的抑制和促凋亡作用,这些分子途径以协调的方式相互作用,以抑制细胞增殖、迁移和侵袭,并诱导细胞转化、自噬、坏死和细胞免疫。已发现隐丹参酮的抗炎机制与TLR4-MyD88/PI3K/Nrf2和TLR4-MyD88/NF-κB/MAPK途径有关,而刺猬信号通路、NF-κB和Nrf-2/HO-1途径受隐丹参酮调节以减轻器官纤维化,其对PI3K/AKT-eNOS途径的抑制作用与神经保护作用有关。鉴于隐丹参酮潜在的药用价值,需要进一步研究以验证该化合物在临床应用中的疗效和安全性,评估其药理活性,并确定分子靶点。

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