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牛蒡苷通过激活 Nrf2 通路拮抗雷公藤内酯醇诱导的肝毒性。

Arctiin Antagonizes Triptolide-Induced Hepatotoxicity via Activation of Nrf2 Pathway.

机构信息

School of Pharmacy, Drug Research & Development Center, Wannan Medical College, Wuhu, Anhui 241002, China.

Anhui Provincial Engineering Research Center for Polysaccharide Drugs, Wuhu, Anhui 241002, China.

出版信息

Biomed Res Int. 2020 Oct 16;2020:2508952. doi: 10.1155/2020/2508952. eCollection 2020.

DOI:10.1155/2020/2508952
PMID:33123566
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7586171/
Abstract

Triptolide (TP) is the most effective ingredient found in the traditional Chinese herbal Hook F, and it is widely used in therapies of autoimmune and inflammatory disorders. However, the hepatotoxicity induced by TP has restricted its use in clinical trials. Arctiin is known as a protective agent against oxidative stress, and it exerts liver-protecting effect. This study was aimed at investigating the protective role of arctiin against TP-induced hepatotoxicity using and models. The results indicated that TP not only obviously induced liver injury in mice but also significantly inhibited the growth of HepG2 cells and increased the level of intracellular reactive oxygen. Furthermore, TP obviously decreased the expressions of proteins of Nrf2 pathway including HO-1, NQO1, and Nrf2 associated with oxidative stress pathway. However, the above experimental indexes were reversed by the treatment of arctiin. Our results suggested that arctiin could alleviate TP-induced hepatotoxicity, and the molecular mechanism is likely related to its capacity against oxidative stress.

摘要

雷公藤红素(TP)是从传统中药虎杖中发现的最有效的成分,它被广泛应用于治疗自身免疫和炎症性疾病。然而,TP 的肝毒性限制了其在临床试验中的应用。牛蒡子苷是一种已知的抗氧化应激保护剂,具有护肝作用。本研究旨在探讨牛蒡子苷对雷公藤红素诱导的肝毒性的保护作用,采用 和 模型进行研究。结果表明,雷公藤红素不仅明显诱导了小鼠的肝损伤,还显著抑制了 HepG2 细胞的生长,增加了细胞内活性氧的水平。此外,雷公藤红素明显降低了与氧化应激途径相关的 Nrf2 途径蛋白 HO-1、NQO1 和 Nrf2 的表达。然而,牛蒡子苷的处理逆转了上述实验指标。我们的结果表明,牛蒡子苷可以减轻雷公藤红素诱导的肝毒性,其分子机制可能与其抗氧化应激能力有关。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5bca/7586171/ef668fab600e/BMRI2020-2508952.007.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5bca/7586171/e1cef6553bf7/BMRI2020-2508952.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5bca/7586171/26b54214c660/BMRI2020-2508952.002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5bca/7586171/ef668fab600e/BMRI2020-2508952.007.jpg

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