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蜈蚣中具有抗肾纤维化活性的结构多样的生物碱。

Structurally Diverse Alkaloids with Anti-Renal-Fibrosis Activity from the Centipede .

机构信息

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

Guangdong Key Laboratory for Biomedical Measurements and Ultrasound Imaging, National-Regional Key Technology Engineering Laboratory for Medical Ultrasound, School of Biomedical Engineering, Shenzhen University Medical School, Shenzhen 518060, China.

出版信息

J Nat Prod. 2024 Apr 26;87(4):1103-1115. doi: 10.1021/acs.jnatprod.4c00044. Epub 2024 Apr 10.

DOI:10.1021/acs.jnatprod.4c00044
PMID:38600744
Abstract

Twelve new alkaloids, scolopenolines A-L (-, -, , ), along with six known analogues, were isolated from , identified by analysis of spectroscopic data and quantum chemical and computational methods. Scolopenoline A (), a unique guanidyl-containing C quinoline alkaloid, features a 6/6/5 ring backbone. Scolopenoline B () is a novel sulfonyl-containing heterodimer comprising quinoline and tyramine moieties. Scolopenoline G () presents a rare C quinoline skeleton with a 6/6/5 ring system. Alkaloids , , , and - display anti-inflammatory activity, while and - also exhibit anti-renal-fibrosis activity. Drug affinity responsive target stability and RNA-interference assays show that Lamp2 might be a potentially important target protein of for anti-renal-fibrosis activity.

摘要

从 中分离得到 12 种新的生物碱,即 scolopenolines A-L(-,-,-,),以及 6 种已知类似物,通过光谱数据分析以及量子化学和计算方法进行鉴定。Scolopenoline A()是一种独特的胍基含 C 喹啉生物碱,具有 6/6/5 环骨架。Scolopenoline B()是一种新型的含磺酰基的杂二聚体,由喹啉和酪胺部分组成。Scolopenoline G()呈现出罕见的 C 喹啉骨架,具有 6/6/5 环系统。生物碱 、 、 、 和 - 具有抗炎活性,而 和 - 也表现出抗肾纤维化活性。药物亲和反应靶标稳定性和 RNA 干扰试验表明,Lamp2 可能是 用于抗肾纤维化活性的一个潜在重要靶标蛋白。

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