In vivo metabolism, pharmacokinetics, and pharmacological activities of ginsenosides from ginseng

Ginseng, a traditional herb with a history spanning thousands of years in Asian culture, has gained widespread recognition for its valuable pharmacological properties. The primary active constituents of ginseng, ginsenosides, are renowned for their diverse biological activities, including cardioprotective, anti-tumor, anti-inflammatory, and neuroprotective effects. However, the therapeutic potential of ginsenosides is often constrained by their low bioavailability in their native forms. During metabolism, ginsenosides undergo biotransformation by intestinal microbiota and enzymes, yielding metabolites with significantly enhanced bioavailability. Thus, to enhance the utility of ginsenosides as pharmaceutical agents and health products, it is essential to deepen our understanding of their metabolic processes and bioavailability in vivo. This review provides a comprehensive analysis of the ginsenoside content in ginseng and the modifications that occur during in vivo metabolism. Particular emphasis is placed on the plasma concentrations of ginsenoside metabolites, as well as the pivotal roles of specific microorganisms and enzymes in the metabolic process. Additionally, the pharmacokinetics of ginsenosides in the bloodstream following metabolism and their associated pharmacological activities are thoroughly examined. By offering a detailed exploration of ginsenosides' metabolism and pharmacodynamics, this review aims to advance our understanding of their therapeutic potential and support future research and drug development initiatives.