Abstract
(24R)-pseudo-ginsenoside HQ (R-PHQ) and (24S)-pseudo-ginsenoside HQ (S-PHQ) are the main metabolites of (20S)-ginsenoside Rh2 (Rh2) in vivo. In this study, we found that Rh2, R-PHQ, and S-PHQ upregulated the innate and adaptive immune response in cyclophosphamide (CTX) induced-immunocompromised mice as evidenced by the number of leukocytes, cellular immunity, and phagocytosis of macrophages. Spleen T-lymphocyte subpopulations and the serum cytokines level were also balanced in these immunosuppressed mice. Furthermore, co-administration with R-PHQ or S-PHQ did not compromise the antitumor activity of CTX in the hepatoma H22-bearing mice. Treatment with R-PHQ and S-PHQ clearly induced the apoptosis of tumor cells, significantly increased the expression of Bax, and remarkably inhibited the expression of Bcl-2 and vascular endothelial growth factor (VEGF) in H22 tumor tissues. The anti-tumor activity of R-PHQ and S-PHQ could be related to the promotion of tumor apoptosis and inhibition of angiogenesis and may involve the caspase and VEGF signaling pathways. This study provides a theoretical basis for further study on R-PHQ and S-PHQ.
Highlights
Cyclophosphamide (CTX) is one of the most widely used antitumor agents in clinical chemotherapy, the application of which often results in leukopenia, immunosuppression, and myelosuppression [1]
Two in vivo metabolites of Rh2—R-pseudo-ginsenoside HQ (PHQ) and S-PHQ—were semi-synthesized and their immunomodulatory effects were investigated in a CTX-induced immunosuppression mouse model
[29] Here, we demonstrated that R-PHQ and S-PHQ significantly suppressed the growth of H22 tumor in a dose-dependent manner
Summary
Cyclophosphamide (CTX) is one of the most widely used antitumor agents in clinical chemotherapy, the application of which often results in leukopenia, immunosuppression, and myelosuppression [1]. Numerous studies have demonstrated that ginsenosides are the major active compounds of antioxidant, anti-obesity, anti-inflammation, neuroprotective, anti-tumor, anti-coagulant, and immunoregulatory effects in P. ginseng [5,6]. Some ginsenosides, such as 20(R)-ginsenoside Rg3 (Shen Yi Capsule, Jilin YATAI Group Pharmaceutical Investment Co., Ltd.), have been clinically applied as tumor neovascularization inhibitors in China [7,8]. Oral administration of ginsenosides has shown poor absorption and low bioavailability, which has limited their clinical application [9]. To improve the bioavailability and enhance their pharmacologic activities, numerous scientists have pursued chemical structure modifications of ginsenosides [10]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
