Yoo Saebyul, Park Bom-I, Kim Do-Hyun, Lee Sooyoung, Lee Seung-Hoon, Shim Wang-Seob, Seo Yong Ki, Kang Kimoon, Lee Kyung-Tae, Yim Sung-Vin, Soung Do Yu, Kim Bo-Hyung
Department of Biomedical Science and Technology, Graduate School, Kyung Hee University, Seoul 02447, Korea.
Food Research Institutes, CJ CheilJedang, Suwon 16495, Korea.
Pharmaceutics. 2021 Apr 2;13(4):487. doi: 10.3390/pharmaceutics13040487.
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 (T) and 58% higher exposure (24 h area under the concentration-time curve, AUC) 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 (AUC) in BG than in RG. The total ginsenoside showed a 5 h rapid intestinal absorption (T) and 79% greater systemic exposure (AUC) 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.
红参(RG)和黑参(BG,CJ EnerG)分别由鲜参经1次和9次蒸制与干燥制备而成。该过程通过去除达玛烷型人参皂苷活性成分上的糖基,降低了其分子量(MW)。我们比较了主要包含低分子量人参皂苷(Rg3、Rg5、Rk1和Rh1)的BG与人参皂苷主要为高分子量(Rb1、Rb2、Rc、Rd、Re和Rg1)的RG之间人参皂苷的药代动力学特征。还采用随机、双盲、单剂量、交叉临床试验研究了安全性和耐受性。Rb1、Rg1和Rg3(著名的代表性和功能性RG成分)的组合在BG中的吸收速率(T)比RG快1小时,暴露量(浓度-时间曲线下24小时面积,AUC)高58%。此外,BG中的主要且最有效的成分Rg3、Rg5和Rk1的组合在BG中的吸收(AUC)比RG高824%。总人参皂苷在BG中的肠道快速吸收时间(T)为5小时,全身暴露量(AUC)比RG高79%。在安全性或耐受性方面未观察到具有临床意义的结果。因此,BG提取物比RG提取物更有效。