The chemical structure, pharmacological activity, and clinical progress of Gentianae Radix et Rhizoma.
Hongfang Liu, Xiao Liu, Sheng Liu, Feng Zhao
Abstract
Open AccessAs pivotal medicinal resources in the Gentiana genus (Gentianaceae), Gentianae Radix et Rhizoma exhibit remarkable chemical diversity and multi-target pharmacological activities. This review highlights G. scabra Bunge., Gentiana rhodantha Franch., Gentiana manshurica Kitag., Gentiana veitchiorum Hemsl., and other species, compiling 172 constituents from literature (2004-2024) and traditional sources: terpenoids (66 iridoids, 47 triterpenoids, and others), flavonoids, lignans, and alkaloids. Iridoids (e.g., gentiopicroside, swertiamarin) and triterpenoids are key bioactive agents. Pharmaco-logically, Gentiana extracts target NF-κB and MAPK pathways to suppress in-flammation and oxidative liver injury via Nrf2 activation, while inducing tumor cell apoptosis (Bax/Bcl-2) and S/G2-M phase arrest to inhibit lung/liver cancer proliferation. They enhance gastrointestinal repair, regulate motility, and mitigate chronic pain through central-peripheral analgesic synergy. Clinically, gentiopicroside demonstrates hepatoprotective, antiviral, and neuroprotective effects, with applications in herpes zoster, non-alcoholic fatty liver disease, and metabolic disorders. This review represents the first comprehensive integration of multidimensional chemi-cal-pharmacological-clinical data on Gentianae Radix et Rhizoma constituents, aiming to promote the expanded application of Gentianae Radix et Rhizoma in the pharma-ceutical field, provide a scientific basis for further development and utilization, and lay a foundation for subsequent research and industrial development.