Advanced progress on pharmacokinetics of Astragali Radix and pharmacological activities of its in vivo constituents

Astragali Radix (Huangqi in Chinese, AR), from the dried roots of Astragalus membranaceus var. mongholicus or A. membranaceus , has been widely utilized for centuries in China, Russia, Kazakhstan, and Mongolia. This review comprehensively summarizes the research progress on the pharmacokinetics of AR extract and its constituents, together with the pharmacological activities of ingredients in vivo , which aims to provide scientific evidence for the rational application and future research of AR. To date, the pharmacokinetics of AR ingredients has predominantly focused on flavonoids and saponins which are also the primary constituents of AR. The pharmacokinetics research indicated that the metabolites of AR exhibited high exposure in vivo . The metabolism of AR also demonstrated that only ten prototypes including eight flavonoids and two saponins were directly absorbed, most constituents were converted to their metabolites. Flavonoids are mainly biotransformed by intestinal microbiota and various enzymes, while saponins are primarily metabolized in the intestine and excreted via feces. The constituents in vivo containing absorbed prototypes along with their metabolites demonstrate a variety of pharmacological effects, such as antitumor, anti-inflammatory, anti-viral, antioxidant, neuroprotective, cardioprotective, and hepatic protective effects. AR has been extensively used in medicine and food realm, however its therapeutic substances and pharmacological actions are still to be fully elucidated. Further pharmacokinetic, metabolic and pharmacological studies are crucial for solving this issue, which will provide valuable guidance for its clinical application and development.