Anti-Angiogenic Properties of Ginsenoside Rg3

Abstract

Ginsenoside Rg3 (Rg3) is a member of the ginsenoside family of chemicals extracted from Panax ginseng. Like other ginsenosides, Rg3 has two epimers: 20(S)-ginsenoside Rg3 (SRg3) and 20(R)-ginsenoside Rg3 (RRg3). Rg3 is an intriguing molecule due to its anti-cancer properties. One facet of the anti-cancer properties of Rg3 is the anti-angiogenic action. This review describes the controversies on the effects and effective dose range of Rg3, summarizes the evidence on the efficacy of Rg3 on angiogenesis, and raises the possibility that Rg3 is a prodrug.

Keywords: 20(R)-ginsenoside Rg3; 20(S)-ginsenoside Rg3; angiogenesis; epimer; ginsenoside Rg3.

Figure 1

Structure of ginsenoside Rg3 as 2D (a) and 3D, generated in UCSF Chimera program (b), showing the chiral center at carbon 20, aglycone steroid-like backbone with hydrophobic properties and glycoside hydrophilic moiety, responsible for the water solubility of ginsenoside Rg3 (Rg3).

Figure 2

Signaling molecules and pathways that are affected by Rg3 in an endothelial cell. (a) VEGF–VEGFR2 interaction and inhibition of the related signaling pathways and molecules, (b) decreased expression of TGF-β1 and the related signaling molecules, (c) blocking the water transport function of AQP1 and decreased expression of AQP1. Red arrows ↓ and ↑ show the effect of Rg3 on decreased and increased expression of molecules, respectively.