Li Hailin, Liu Jing, Fang Chuhong, Ning Shanglei
Department of Hepatobiliary Surgery, General Surgery, Qilu Hospital of Shandong University, Jinan, Shandong, China.
Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai, Shandong, China.
Front Pharmacol. 2025 Mar 20;16:1561954. doi: 10.3389/fphar.2025.1561954. eCollection 2025.
Seven novel clerodane diterpenoids, designated tinotanoids I-O (1-7), were isolated from the tuberous roots of (Oliv.) Wei Wang [syn.: 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 IC values of 12.5 ± 0.5 and 16.4 ± 0.7 M, 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.
从中华青牛胆（Oliv.）Wang [同义词：云南青牛胆（S.Y.Hu）H.S.Lo；防己科]的块根中分离出七种新的克罗烷二萜类化合物，命名为青牛胆素I - O（1 - 7）。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，实现了对这些新代谢产物的结构解析，包括它们的绝对构型。对它们的抗炎活性评估表明，代谢产物3和4在脂多糖（LPS）激活的RAW264.7巨噬细胞中对一氧化氮（NO）的产生表现出强效抑制作用，IC值分别为12.5±0.5和16.4±0.7 μM，优于阳性对照槲皮素和地塞米松。此外，代谢产物3和4以剂量依赖的方式有效抑制促炎细胞因子TNF-α和IL-6。
