01 Jan
Investigating the Great Possibility of Rare Ginsenosides as Drugs and Nutraceuticals
1. Introduction
Rare ginsenosides, a group of dammarane triterpenoids that exist in low natural abundance, fuels a high concern from scholars recently, showing great potential as shining components in drugs and nutraceuticals.
2. The difference between primary ginsenosides and rare ginsenosides
Ginsenosides are chiefly extracted from the plants of Araliaceae such as Panax ginseng, Panax notoginseng, and Panax quinquefolius. In light of their natural abundance, ginsenosides are usually divided into macro (primary) saponins (ginsenosides Rb1, Rg1, Re, Rd, etc.) and rare (secondary) ginsenosides (Rg5, Rk1, Rg3, etc). Relative to primary ginsenosides, rare ginsenosides are easy to be absorbed by human body, with much higher biological activity, membrane permeability and bioavailability.
3. The stereochemistry properties of rare ginsenosides
The stereochemistry-driven difference in bioactivities is mostly focused on the 20(S/R)-Rg3 and 20(S/R)-Rh2 epimers. The stereochemistry properties confer rare ginsenosides with diverse bioactivities. Typically, the crucial factors that contribute to the efficacy of rare ginsenosises encompass the number of sugar molecules, sugar linkage and double bonds within C-17 side chain. For instance, the anti-tumor effect increased as the number of sugar moieties in a ginsenoside decreased.
4. Pharmacological activities of rare ginsenosides
Rare ginsenosides serve as natural ligands for some specific receptors such as bile acid (FXR/TGR5), steroid hormone, estrogen, glucocorticoid, androgen, platelet adenosine diphosphate, which are determined to exert immunoregulatory and adaptogen-like effect, anti-aging effect, anti-tumor effect, as well as their effects on cardiovascular and cerebrovascular system, central nervous system, obesity and diabetes.
5. The impact of rare ginsenosides upon gut microbiota
In addition to above-mentioned pharmacological activities, rare ginsenosides are also contributive to maintaining the homeostasis of gut microbiota. Under normal physiological condition, there is a dynamic balance in gut microbiota, which would be disrupted in the onset and development of certain disease. Rare ginenosides can restore the decreased abundance of certain affected microbiota, regulating the intestinal microecology to influence the physiological function of the host.
6. Conclusion
By leverage of the stereochemistry properties, rare ginsenosides exhibit superior bioactivity, opening up new opportunities for the discovery and development of drugs and nutraceuticals.
Reference
Szot JO, Cuny H, Martin EM, et al. A metabolic signature for NADSYN1-dependent congenital NAD deficiency disorder. J Clin Invest. 2024;134(4):e174824. Published 2024 Feb 15. doi:10.1172/JCI174824
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