Gypsogenin is a well-known natural saponin which has marked anticancer effects towards various types of cancer cell lines [1]. Gypsogenin can inhibit the growth and metastasis of Lewis lung cancer and triggers apoptosis by increasing Bax levels and possesses anticancer activities against L1210, CCER-CEM and Ls174T cancer cells [2]. Gypsogenin derivatives possess great potential as important pharmacophores.
Gypsogenin (0.1, 1, 10 and 100μM; 72h) displayed good cytotoxicity in the low concentration for several cancer cells (MCF-7, HeLa, Jurkat and K562), the values of IC50 ranged from 3.25 to 13.68μM [1]. Gypsogenin (5, 10, 20 and 40μM; 72h) showed a strong antiproliferative effect, with an IC50 between 5 and 10μM on HL-60 cells [3].
Gypsogenin (5.0, 7.5, 10.0mg/kg; 8d; i.p.) reduced the tumor weight and showed a preliminary anti-metastatic role on Lewis lung cancer in C57BL/6J mice [2].
References:
[1] Emirdağ S, Ulusoy N G, Aksel M. Design, synthesis and biological evaluation of novel gypsogenin derivatives as potential anticancer and antimicrobial agents [J]. Chemistry & biodiversity, 2024, 21(6): e202400471.
[2] Tian G, Zhou L, Zhong Y, et al. Experimental studies of the therapeutic effect of Gypsophila oldhamiana gypsogenin on Lewis lung cancer in mice [J]. Chinese Journal of Clinical Oncology, 2008, 5(3): 206-210.
[3] Ozturk S E, Babahan I, Ozmen A. Synthesis, characterization and in vitro anti-neoplastic activity of gypsogenin derivatives [J]. Bioorganic chemistry, 2014, 52/54: 15-23.