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Novel ginsenosides show stronger antiplatelet activity

Ginseng is one of the best treasures in ancient Chinese medicine and was regarded as the best tonic for improving body strength. It is generally safe without reported toxicity and side effects, and people have used to treat minor diseases and to prolong longevity for thousands of years.One of the most valued benefits of ginseng advocated in ancient times is to promote cardiovascular health and to help modulate blood glucose levels.

In modern science, researchers did found ginseng have potentially unique cardiovascular health. Ginsenosides are pharmacologically active compounds in ginseng that are responsible for cardiovascular benefits.

Antiplatelet activity of ginsenosides

Thrombosis is one of the most serious events for cardiovascular diseases, and naturally,platelet-forming inhibition is one of the effective ways to reduce the incidence of thrombotic events.

Ginsenosides have been shown to modulate platelet function and are considered as a potential antiplatelet agent, with many studies indicating their role in inhibiting platelet aggregation.

In addition, ginsenosides have less toxicity and side effects, which is why they are so attractive in medical research.

A recent study published in the Journal of Ginseng Research conducted detailed research on the antiplatelet activity of novel ginsenosides as well as their synergistic effects.

The study authors confirmed the modulatory functions of non-saponin and total saponin fraction and reviewed the antiplatelet effects of ginsenosides like Rg1, Rg2, Rh1, Rh2, Rg5, Rs1, Rs2, etc, and their potential mechanisms of action.

Novel ginsenosides with stronger antiplatelet activity

Ginsenosides are unstable and can be converted into novel ginsenosides with high bioavailability.

In the study, ginsenoside Rg3 was converted into novel Ginsenoside 2H-Rg3 under acidic and high-temperature conditions and showed stronger antiplatelet activity than its parent compounds.

Ginsenoside Rp1 was also prepared from other ginsenosides by reducing hydrogenation(Rg3, 2h-Rg3, Rg5, and Rk1). Excitedly, it has been shown to have 10 times more potent anticancer effects than its parent ginsenosides Rg3 and Rg5. The rat and mouse model results confirmed the antiplatelet effects of Rp1.

Ginsenoside Rp3 was obtained using the same preparation method with Rp1. The antiplatelet activity of Rp3was examined in human experiments. The scanning electron microscopy observation showed that ginsenoside Rg3 could suppress platelet activation in a dose-dependent relationship.

Synergistic effects of ginsenosides on platelet function

Since combination therapy usually shows synergistic effects, the researchers of the study were curious about the synergistic effects of ginsenosides on antiplatelet properties. The researchers did tests with a group pf ginsenosides Rg3, 2H-Rg3, Rp1, Rp3, and Rp4 in 10-20% inhibitory concentrations.

A combination of Rp3 and Rp1 or 2H-Rg3 achieved synergistic effects against platelet aggregation, and the cotreatment of Rp3 and Rp4 showed augmented effects, compared with using alone.

The study is of great significance, in which preclinically confirmed the antiplatelet activity of ginsenosides in cardiovascular diseases. Also, the findings that novel ginsenosides converted from already identified ginsenosides exhibit stronger antiplatelet activity and show synergistic effects are of great practical value, providing innovative insight for drug design.

Reference:

Irfan M, Kim M, Rhee MH. Anti-platelet role of Korean ginseng and ginsenosides in cardiovascular diseases. J Ginseng Res. 2020;44(1):24-32. doi:10.1016/j.jgr.2019.05.005