ABSTRACT
Hepatocellular carcinoma(HCC)is the third leading cause of cancer death worldwide.Ginsenoside Rk3,an important and rare saponin in heat-treated ginseng,is generated from Rg1 and has a smaller mo-lecular weight.However,the anti-HCC efficacy and mechanisms of ginsenoside Rk3 have not yet been characterized.Here,we investigated the mechanism by which ginsenoside Rk3,a tetracyclic triterpenoid rare ginsenoside,inhibits the growth of HCC.We first explored the possible potential targets of Rk3 through network pharmacology.Both in vitro(HepG2 and HCC-LM3 cells)and in vivo(primary liver cancer mice and HCC-LM3 subcutaneous tumor-bearing mice)studies revealed that Rk3 significantly inhibits the proliferation of HCC.Meanwhile,Rk3 blocked the cell cycle in HCC at the G1 phase and induced autophagy and apoptosis in HCC.Further proteomics and siRNA experiments showed that Rk3 regulates the phosphatidylinositol 3-kinase(PI3K)/protein kinase B(AKT)pathway to inhibit HCC growth,which was validated by molecular docking and surface plasmon resonance.In conclusion,we report the discovery that ginsenoside Rk3 binds to PI3K/AKT and promotes autophagy and apoptosis in HCC.Our data strongly support the translation of ginsenoside Rk3 into novel PI3K/AKT-targeting ther-apeutics for HCC treatment with low toxic side effects.
ABSTRACT
Objective: To study the minor triterpenoid saponins from the roots of Panax notoginseng, which provided basis for the systematic research, quality control and safety evaluation of P. notoginseng. Methods The compounds were isolated and purified by MCI resin, ODS, along with Preparative-HPLC, and the structures were identified by spectroscopic analysis, and comparing with the pubished literature values. Results: Twelve monomeric compounds isolated from the roots of P. notoginseng, were identified as notoginsenoside P1 (1), notoginsenoside T5 (2), ginsenoside Rk3 (3), ginsenoside Rh4 (4), notoginsenoside T3 (5), 20(S)-protopanaxatriol (6), dammar 20 (21),24-diene-3β,6α,12β-triol (7), ginsenoside Rg3 (8), gypenoside XIII (9), ginsenoside Rk1 (10), ginsenoside Rg5 (11), and 20 (S)-ginsenoside Rh2 (12). Conclusion: Compound 1 is a new dammarane-type triterpenoid saponin
ABSTRACT
Objective: To employ the response surface methodology (RSM) to optimize the preparation conditions for ginsenoside Rh4 (GRh4) and Rk3 (GRk3) using the yields as index. Methods: High temperature hydrolysis combined with RSM was used to prepare GRk3 and GRh4 from ginsenoside Rg1 (GRg1), and the reaction conditions were optimized at the same time. Results: The optimal preparation conditions of GRk3 and GRh4 were confirmed using Design Expert 7.1.6 software as followss: acid concentration of 0.02%, reaction temperature of 116.4℃, and reaction time of 2.22 h, respectively. Under the above conditions, the yields of GRk3 and GRh4 were 123.56 mg with conversion rate of 61.78%. Conclusion: The preparation conditions obtained from RSM optimization are suitable for large scale preparation of GRk3 and GRh4.
ABSTRACT
Objective: A new, environment-friendly and efficient method for the preparation of rare ginsenoside Rg6, F4, Rk3, and Rh4 was established, which provides a theoretical basis for preparing rare ginsenosides. Methods: Rare ginsenoside was prepared by hydrolyzing ginsenoside Re using aspartic acid as the catalyst, through semi preparative HPLC, the target compounds Rg6, F4, Rk3, and Rh4 were rapidly separated from the degradation products, quantitative analysis, and structure identification by HPLC and NMR. Results: Ginsenoside Re was hydrolyzed by aspartic acid according to the ratio 10∶1 at 120℃ for 1 h, the conversion rate of ginsenoside Re was 100%, the yields of rare ginsenoside Rg6, F4, Rk3, and Rh4 were 11.2%, 13.1%, 20.6%, and 24.3%, respectively, and the purity of the four compounds were all above 99%. Conclusion: The method is simple, low-cost, and non-pollution for environment, the research has important application value for the development of green environmental protection of rare ginsenosides drugs and health food.