20(R)-Ginsenoside Rh2, a minor stereoisomer of ginsenoside Rh2, possesses matrix metalloproteinase inhibitory. 20(R)-Ginsenoside Rh2 has anticancer, anti- proliferation, anti-inflammatory and antioxidative activities, it also shows selective osteoclastgenesis inhibitory activity. 20(R)-Ginsenoside Rh2 reduce apoptotic rate significantly, enhance the activity of caspase-3 and induces apoptosis in human lung adenocarcinoma A549 cells.
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Effects of 20 (S) -ginsenoside Rh2 and 20 (R) -ginsenoside Rh2 on proliferation and apoptosis of human lung adenocarcinoma A549 cells.[Pubmed: 22007558
To evaluate and explore the effects of 20(S)-ginsenoside Rh2 and 20(R)-Ginsenoside Rh2 on the cytotoxicity, proliferation and the apoptosis of human lung adenocarcinoma A549 cells, and to illustrate the structure-activity relationship and possible mechanisms of anti-tumor active ingredients of ginseng.
METHODS AND RESULTS:
A549 cells were treated with different concentration gradient of 20(R)-Ginsenoside Rh2 (S and R structure) and incubated for different time.MTT test indicated that 20(R)-Ginsenoside Rh2 had a strong cytotoxicity activity to A549 cells. Ginsenoside Rh2 could obviously inhibit the cell proliferation in human lung adenocarcinoma cell line A549 at the effective doses of 25 mg x L(-1) treated with 48 h.
20(R)-Ginsenoside Rh2 and 20(S)-ginsenoside Rh2 had a significant inhibitory effect on the proliferation. Compared with 20(S)-ginsenoside Rh2, 20 (S)-ginsenoside Rh2 has been shown to have significant anticancer effects and to be capable of blocking cell proliferation and causing G1 phase arrest in human lung adenocarcinoma A549 cells. 20(R)-Ginsenoside Rh2 and 20(S)-ginsenoside Rh2 have been shown to have anticancer effects and to be capable of increasing inchoate apoptotic rate, reducing apoptotic rate significantly, enhancing the activity of Caspase-3 and inducing apoptosis in human lung adenocarcinoma A549 cells.
Bioorg Med Chem Lett. 2009 Jun 15;19(12):3320-3.
20(R)-ginsenoside Rh2, not 20(S), is a selective osteoclastgenesis inhibitor without any cytotoxicity.[Pubmed: 19428246
Increased osteoclastic bone resorption plays a central role in the pathogenesis of many bone diseases, and osteoclast inhibitors are the most widely used treatments for these diseases. Ginsenosides, the main component of ginseng, have been known for their medicinal effects such as anti-inflammatory and anti-proliferative activities.
METHODS AND RESULTS:
In this study, we investigated the inhibitory effects of ginsenosides (20(R)-Ginsenoside Rh2 and ginsenoside 20(S)-Rh2) on osteoclastgenesis using RAW264 cells in vitro. Only 20(R)-Ginsenoside Rh2 showed selective osteoclastgenesis inhibitory activity without any cytotoxicity up to 100 microM.
These results implied that the stereochemistry of the hydroxyl group at C-20 may play an important role in selective osteoclastgenesis inhibitory activity.
J Pharm Pharmacol. 2013 Feb;65(2):310-6.
Anti-inflammatory, antioxidative and matrix metalloproteinase inhibitory properties of 20(R)-ginsenoside Rh2 in cultured macrophages and keratinocytes.[Pubmed: 23278699
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 AND RESULTS:
In-vitro anti-inflammatory activity of 20(R)-Ginsenoside 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. 20(R)-Ginsenoside 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)-Ginsenoside Rh2 could suppress the gelatinolytic activity of MMP-9 enhanced by tumour necrosis factor-α in the keratinocytes.
20(R)-Ginsenoside Rh2, a minor stereoisomer of ginsenoside Rh2, possesses matrix metalloproteinase inhibitory, anti-inflammatory and antioxidative activity.