期刊
TRANSLATIONAL ONCOLOGY
卷 15, 期 1, 页码 -出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.tranon.2021.101280
关键词
Curcumin derivative; Ovarian cancer; ST03; Apoptosis; Bioavailability
类别
资金
- Department of IT, BT and ST, Govt. [SR/FST/LSI-536/2012]
- DST [2121330491]
- UGC
- University Grants commission, Govt. of India
In this study, a curcumin derivative called ST03 exhibited better bioavailability and stability compared to curcumin. ST03 demonstrated anticancer effects by inducing reactive oxygen species (ROS) and activating the intrinsic apoptotic pathway in ovarian cancer cells. ST03 also inhibited the migration of ovarian cancer cells. These findings suggest that ST03 has potential as a promising drug candidate for anticancer therapies.
Curcumin is known for its anticancer properties, but its clinical application is limited due to its poor bioavail-ability and chemical stability. In this study we report the curcumin derivative, ST03 (1,2-bis[(3E,5E)-3,5-bis[(2-chlorophenyl)methylene]-4-oxo-1-piperidyl]ethane-1,2-dione) exhibits similar to 14 fold better bioavailability compared to curcumin and is detectable in plasma up to 12 h. ST03 induces ROS, activates the intrinsic apoptotic pathway as evident by disruption of mitochondrial membrane potential, and induction of proapoptotic proteins in ovarian cancer lines PA1 and A2780. ST03 also blocked the migration of ovarian cancer cells. ST03 exerted its antitumor effect in-vivo in the EAC mouse model by activating the intrinsic apoptotic pathway. Our findings demonstrate ST03, a curcumin derivative, with better bioavailability and stability with no discernable toxicity in vivo to be a promising drug candidate for anticancer therapies.
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