A Natural Compound Methylnissolin: Physicochemical Properties, Pharmacological Activities, Pharmacokinetics and Resource Development.

IF 4.7 2区医学 Q1 CHEMISTRY, MEDICINAL

Drug Design, Development and Therapy Pub Date : 2025-05-08 eCollection Date: 2025-01-01 DOI:10.2147/DDDT.S518508

Ziyang Lin, Mingjie Liang, Xianlong Zhang, Zhuo Cen, Fengxin Kang, Baien Liang, Ying Lai, Minyi Li, Tingting Duan, Junzheng Yang, Bo Liu

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引用次数: 0

Abstract

Methylnissolin (also known as Astrapterocarpan) is an isoflavonoid compound featuring a pterocarpan core structure. To date, leguminous plants of the genus Astragalus 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 Astragalus membranaceus is analyzed, providing crucial insights for drug development and resource utilization.

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天然化合物甲基尼索林：理化性质、药理活性、药代动力学及资源开发。

甲基尼索林（Methylnissolin，又称Astrapterocarpan）是一种具有翼龙ocarpan核心结构的异黄酮类化合物。迄今为止，豆科植物黄芪属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，甲基尼索林及其苷类进入体循环，调节信号通路，如RIPK2/ASK1、PI3K/AKT、i -κB /NF-κB、MAPK和Nrf2/HO-1。其药理活性跨越抗炎、抗氧化、调节糖脂代谢和抗肿瘤作用，强调了其广泛的药物开发潜力。本文综述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特征。值得注意的是，我们系统地阐明了甲基尼索林的代谢命运，确定了羟基化、去甲基化、二聚化、水合作用和脱氢作用是主要的生物转化途径。进一步分析了植物品种、产地、加工方法等因素对黄芪中甲基尼索林及其苷含量的影响，为药物开发和资源利用提供重要依据。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Drug Design, Development and Therapy CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY

CiteScore

9.00

自引率

0.00%

发文量

382

审稿时长

>12 weeks

期刊介绍： Drug Design, Development and Therapy is an international, peer-reviewed, open access journal that spans the spectrum of drug design, discovery and development through to clinical applications. The journal is characterized by the rapid reporting of high-quality original research, reviews, expert opinions, commentary and clinical studies in all therapeutic areas. Specific topics covered by the journal include: Drug target identification and validation Phenotypic screening and target deconvolution Biochemical analyses of drug targets and their pathways New methods or relevant applications in molecular/drug design and computer-aided drug discovery* Design, synthesis, and biological evaluation of novel biologically active compounds (including diagnostics or chemical probes) Structural or molecular biological studies elucidating molecular recognition processes Fragment-based drug discovery Pharmaceutical/red biotechnology Isolation, structural characterization, (bio)synthesis, bioengineering and pharmacological evaluation of natural products** Distribution, pharmacokinetics and metabolic transformations of drugs or biologically active compounds in drug development Drug delivery and formulation (design and characterization of dosage forms, release mechanisms and in vivo testing) Preclinical development studies Translational animal models Mechanisms of action and signalling pathways Toxicology Gene therapy, cell therapy and immunotherapy Personalized medicine and pharmacogenomics Clinical drug evaluation Patient safety and sustained use of medicines.