Potential of ginsenoside Rh₂ and its derivatives as anti-cancer agents

As a steroid skeleton-based saponin, ginsenoside Rh₂ (G-Rh₂) is one of the major bioactive ginsenosides from the plants of genus Panax L. Many studies have reported the notable pharmacological activities of G-Rh₂ such as anticancer, antiinflammatory, antiviral, antiallergic, antidiabetic, and anti-Alzheimer’s activities. Numerous preclinical studies have demonstrated the great potential of G-Rh₂ in the treatment of a wide range of carcinomatous diseases in vitro and in vivo. G-Rh₂ is able to inhibit proliferation, induce apoptosis and cell cycle arrest, retard metastasis, promote differentiation, enhance chemotherapy and reverse multi-drug resistance against multiple tumor cells. The present review mainly summarizes the anticancer effects and related mechanisms of G-Rh₂ in various models as well as the recent advances in G-Rh₂ delivery systems and structural modification to ameliorate its anticancer activity and pharmacokinetics characteristics.