具有抗炎活性的克罗丹二萜类化合物王魏。

IF 4.4 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Frontiers in Pharmacology Pub Date : 2025-03-20 eCollection Date: 2025-01-01 DOI:10.3389/fphar.2025.1561954
Hailin Li, Jing Liu, Chuhong Fang, Shanglei Ning
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引用次数: 0

摘要

摘要从矢状拟菜(Paratinospora sagittata, Oliv)的块根中分离到7个新的氯烷二萜,命名为tinotanoids I-O(1-7)。王伟[同]:Tinospora sagittata var. yunnanensis (S.Y.Hu) H.S.Lo;防己科)。通过质谱(MS)、核磁共振(NMR)、电子圆二色性(ECD)和x射线晶体学等先进的光谱方法,对这些新代谢物的结构进行了解析,包括它们的绝对构型。抗炎活性评价表明,代谢物3和4对脂多糖(LPS)激活的RAW264.7巨噬细胞一氧化氮(NO)产生有明显抑制作用,IC50值分别为12.5±0.5 μM和16.4±0.7 μM,优于阳性对照槲皮素和地塞米松。此外,代谢物3和4以剂量依赖性的方式有效抑制促炎细胞因子TNF-α和IL-6。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Clerodane diterpenoids with anti-inflammatory activity from the tuberous root of Paratinospora sagittata (Oliv.) Wei Wang.

Seven novel clerodane diterpenoids, designated tinotanoids I-O (1-7), were isolated from the tuberous roots of Paratinospora sagittata (Oliv.) Wei Wang [syn.: Tinospora sagittata var. yunnanensis (S.Y.Hu) H.S.Lo; Menispermaceae]. The structural elucidation of these new metabolites, including their absolute configurations, was achieved through advanced spectroscopic methods such as mass spectrometry (MS), nuclear magnetic resonance (NMR), electronic circular dichroism (ECD), and X-ray crystallography. Evaluation of their anti-inflammatory activity revealed that metabolites 3 and 4 exhibited potent inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-activated RAW264.7 macrophages, with IC50 values of 12.5 ± 0.5 and 16.4 ± 0.7 μM, respectively, which are better than those of the positive controls, quercetin and dexamethasone. Additionally, metabolites 3 and 4 effectively inhibited the pro-inflammatory cytokines TNF-α and IL-6 in a dose-dependent manner.

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来源期刊
Frontiers in Pharmacology
Frontiers in Pharmacology PHARMACOLOGY & PHARMACY-
CiteScore
7.80
自引率
8.90%
发文量
5163
审稿时长
14 weeks
期刊介绍: Frontiers in Pharmacology is a leading journal in its field, publishing rigorously peer-reviewed research across disciplines, including basic and clinical pharmacology, medicinal chemistry, pharmacy and toxicology. Field Chief Editor Heike Wulff at UC Davis is supported by an outstanding Editorial Board of international researchers. This multidisciplinary open-access journal is at the forefront of disseminating and communicating scientific knowledge and impactful discoveries to researchers, academics, clinicians and the public worldwide.
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