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.

loganin  /  pharmacokinetics  /  preparation development  /  bioavailability  /  neuroprotection  /  antitumor  /  metabolic regulation  /  bone and joint protection