Anti-inflammatory, antioxidative and matrix metalloproteinase inhibitory properties of 20(R)-ginsenoside Rh2 in cultured macrophages and keratinocytes

Objectives: This work aimed to assess the matrix metalloproteinase inhibitory and related pharmacological actions of 20(R)-ginsenoside Rh2 (20(R)-Rh2) in cultured macrophages and keratinocytes.

Methods: In-vitro anti-inflammatory activity of 20(R)-Rh2 was evaluated by analysing nitric oxide (NO) and prostaglandin E2 (PGE2) contents in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells. Its antioxidant activity was determined by measuring the level of Reactive Oxygen Species (ROS) in the macrophage and keratinocyte cells. Matrix metalloproteinase-9 (MMP-9) and -2 (MMP-2) activity in the culture medium was detected using zymography.

Key findings: 20(R)-Rh2 was able to suppress NO, PGE2, ROS and pro-matrix metalloproteinase-9 (pro-MMP-9) levels that were enhanced in the LPS-stimulated murine RAW264.7 macrophage cells. 20(R)-Rh2 also exhibited inhibitory effects on the level of ROS and the activity of MMP-9 and -2 in human HaCat keratinocyte cells without stimulant exposure. 20(R)-Rh2 could suppress the gelatinolytic activity of MMP-9 enhanced by tumour necrosis factor-α in the keratinocytes.

Conclusions: 20(R)-Rh2, a minor stereoisomer of ginsenoside Rh2, possesses matrix metalloproteinase inhibitory, anti-inflammatory and antioxidative activity.