马钱苷作为典型的环烯醚萜苷类天然化合物，是传统中药山茱萸Corni Fructus的代表性活性成分，近年来因其显著的神经保护、抗肿瘤、代谢调节及骨关节保护等多靶点生物活性而备受关注。当前研究普遍聚焦于其药效验证与单一信号通路的探讨，但仍存在体内机制复杂、生物利用度低及代谢产物作用未明等关键科学问题。通过系统综述马钱苷在体内的吸收、分布、代谢与排泄特征，揭示其药动学过程受多药耐药蛋白、肠道菌群及病理状态协同调控的规律；并深入总结其在神经系统、肿瘤、代谢性疾病及骨关节疾病等中的药理作用机制，阐明其通过多条关键信号通路实现抗炎、抗凋亡及代谢稳态重建等多层调控效应，从系统药理学角度为中药活性成分机制研究提供新思路。

Loganin, a representative iridoid glycoside derived from Shanzhuyu (Corni Fructus), has attracted increasing attention due to its significant multi-target biological activities, including neuroprotective, antitumor, metabolic regulatory, and osteoarticular protective effects. Despite substantial progress in pharmacodynamic validation and the exploration of individual signaling pathways, critical scientific issues remain unresolved, particularly regarding its complex in vivo mechanisms, limited bioavailability, and unclear effects of its metabolites. By systematically reviewing the absorption, distribution, metabolism, and excretion characteristics of loganin in vivo, this review elucidates the coordinated regulation of its pharmacokinetic behavior by multidrug resistance transporters, gut microbiota, and pathological states. Furthermore, we comprehensively summarize its pharmacological mechanisms in neurological disorders, cancer, metabolic diseases, and osteoarticular conditions, highlighting its multi-layered regulatory effects mediated through key signaling networks involved in anti-inflammation, anti-apoptosis, and reconstruction of metabolic homeostasis via multiple key signaling pathways. From a systems pharmacology perspective, this work provides an integrated framework for understanding the mechanistic basis of bioactive constituents derived from traditional Chinese medicine.

R285

河南省重大科技专项（231100310200）