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来自白木香沉香的四种新愈创木烷倍半萜及其对肾纤维化的生物活性。

Four new guaiane sesquiterpenes from Agarwood of Aquilaria sinensis and their biological activity toward renal fibrosis.

作者信息

Cheng Li-Zhi, Li Xu-Yang, Li Yi-Fei, Zhou Hong, Chen Xie-Hui, Chang Junlei

机构信息

Department of Geriatrics, Shenzhen Longhua District Central Hospital, Shenzhen 518110, Guangdong, PR China; Shenzhen Key Laboratory of Biomimetic Materials and Cellular Immunomodulation, Institute of Biomedicine and Biotechnology, Shenzhen Institute of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, Guangdong, PR China.

Guangdong Provincial Key Laboratory of Chinese Medicine Ingredients and Gut Microbiomics, Institute for Inheritance-Based Innovation of Chinese Medicine, School of Pharmacy, Shenzhen University Medical School, Shenzhen University, Shenzhen 518055, PR China.

出版信息

Fitoterapia. 2024 Oct;178:106143. doi: 10.1016/j.fitote.2024.106143. Epub 2024 Jul 23.

DOI:10.1016/j.fitote.2024.106143
PMID:39053740
Abstract

Four undescribed guaiane sesquiterpenes, aquisinenoids I-L (2-5) and five known compounds were isolated from the resins of Aquilaria sinensis. Their structures were deduced based on spectroscopic data analysis, X-ray crystallography and ECD calculations. Biologically, compounds 1, 5, 6 and 9 showed anti-renal fibrosis activity, significantly reducing the levels of fibronectin, collagen I, and α-SMA. Compounds 2-4, 7 and 8 could reduce one or two of these proteins at non-toxic concentrations in TGF-β1 induced NRK-52E cells.

摘要

从白木香树脂中分离得到了4个未描述的愈创木烷型倍半萜——沉香新素I-L(2-5)以及5个已知化合物。通过光谱数据分析、X射线晶体学和电子圆二色光谱(ECD)计算推导了它们的结构。生物学实验表明,化合物1、5、6和9具有抗肾纤维化活性,可显著降低纤连蛋白、I型胶原蛋白和α-平滑肌肌动蛋白(α-SMA)的水平。在转化生长因子-β1(TGF-β1)诱导的NRK-52E细胞中,化合物2-4、7和8在无毒浓度下可降低其中一种或两种蛋白质的水平。

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