Abstract
Red ginseng (RG) and black ginseng (BG, CJ EnerG) were prepared from fresh ginseng using one and nine cycles of steaming and drying, respectively. This process reduces the molecular weight (MW) of ginsenoside-active compounds in ginseng by removing sugar moieties from their dammaranes. We compared the pharmacokinetic characteristics of ginsenosides between BG comprising mainly low-MW ginsenosides (Rg3, Rg5, Rk1, and Rh1) and RG that predominantly contains high-MW ginsenosides (Rb1, Rb2, Rc, Rd, Re, and Rg1). The safety profiles and tolerability were also studied using a randomized, double-blind, single-dose, crossover clinical trial. A combination of Rb1, Rg1, and Rg3, well-known representative and functional RG components, exhibited a 1 h faster absorption rate (Tmax) and 58% higher exposure (24 h area under the concentration–time curve, AUC24) in BG than in RG. Furthermore, the combination of Rg3, Rg5, and Rk1, the major and most efficient components in BG, displayed 824% higher absorption (AUC24) in BG than in RG. The total ginsenoside showed a 5 h rapid intestinal absorption (Tmax) and 79% greater systemic exposure (AUC24) in BG than in RG. No clinically significant findings were observed in terms of safety or tolerability. Thus, BG extract was more effective than RG extract.
Highlights
The PK characteristics of the 14 ginsenosides were analyzed by administering a single dose of red ginseng (RG) and black ginseng (BG)
The PK results suggested that the systemic exposures (AUC24 ) and
to reach Cmax (Tmax) of total ginsenosides were 79% higher and 5 h earlier in the BG extract than in the RG
Summary
A. Meyer) is a widely used traditional medicinal plant in Asian countries, such as Korea, China, and Japan, and in the United States and Europe. Ginseng possesses several pharmacological activities, including anti-inflammatory, anti-diabetic, anti-tumor, immune-regulatory, anti-oxidation, and anti-fatigue properties. These activities are attributed to the pharmacological action of dammarane-type saponins, known as ginsenosides, which are the active components of ginseng [1,2,3,4]. Gin senosides are classified as protopanaxadiol (PPD) and protopanaxatriol (PPT) types. Examples of PPD-type ginsenosides are Rb1, Rb2, Rc, Rd, Rg3, Rk1, Rg5, Rh2, compound K (CK), and PPD, whereas PPT-type ginsenosides include Re, Rg1, Rh1, and PPT (Figure 1)
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