Lin Ziyang, Liang Mingjie, Zhang Xianlong, Cen Zhuo, Kang Fengxin, Liang Baien, Lai Ying, Li Minyi, Duan Tingting, Yang Junzheng, Liu Bo
The Second Clinical Medical College, Guangzhou University of Chinese Medicine, Guangzhou, People's Republic of China.
Guangdong Nephrotic Drug Engineering Technology Research Center, Guangdong Consun Pharmaceutical Group, Guangzhou, People's Republic of China.
Drug Des Devel Ther. 2025 May 8;19:3763-3777. doi: 10.2147/DDDT.S518508. eCollection 2025.
Methylnissolin (also known as Astrapterocarpan) is an isoflavonoid compound featuring a pterocarpan core structure. To date, leguminous plants of the genus remain the exclusive natural source of Methylnissolin and its glycoside derivative, Methylnissolin-3-O-glucoside. Upon oral administration, Methylnissolin and its glycosides enter systemic circulation and modulate signaling pathways such as RIPK2/ASK1, PI3K/AKT, IκB/NF-κB, MAPK, and Nrf2/HO-1. Their pharmacological activities span anti-inflammatory, antioxidant, glucose-lipid metabolism regulation, and antitumor effects, underscoring their broad potential for drug development. This review comprehensively evaluates the physicochemical properties, pharmacological activities, mechanisms of action, pharmacokinetic characteristics, and toxicological profile of Methylnissolin and its glycoside derivatives. Notably, we systematically elucidate the metabolic fate of methylnissolin, identifying hydroxylation, demethylation, dimerization, hydration, and dehydrogenation as predominant biotransformation pathways. Furthermore, the influence of factors such as plant variety, geographical origin, and processing methods on Methylnissolin and its glycoside content in is analyzed, providing crucial insights for drug development and resource utilization.
甲基尼索林（也称为阿斯屈普托卡潘）是一种具有紫檀素核心结构的异黄酮类化合物。迄今为止，该属豆科植物仍然是甲基尼索林及其糖苷衍生物甲基尼索林-3-O-葡萄糖苷的唯一天然来源。口服后，甲基尼索林及其糖苷进入体循环并调节RIPK2/ASK1、PI3K/AKT、IκB/NF-κB、MAPK和Nrf2/HO-1等信号通路。它们的药理活性包括抗炎、抗氧化、调节糖脂代谢和抗肿瘤作用，凸显了其在药物开发方面的广阔潜力。本综述全面评估了甲基尼索林及其糖苷衍生物的理化性质、药理活性、作用机制、药代动力学特征和毒理学概况。值得注意的是，我们系统地阐明了甲基尼索林的代谢命运，确定羟基化、去甲基化、二聚化、水合和脱氢为主要的生物转化途径。此外，还分析了植物品种、地理来源和加工方法等因素对该属植物中甲基尼索林及其糖苷含量的影响，为药物开发和资源利用提供了关键见解。
