Curcumin derivative 1, 2-bis [(3E, 5E)-3, 5-bis [(2-chlorophenyl) methylene]-4-oxo-1-piperidyl] ethane-1, 2-dione (ST03) induces mitochondria mediated apoptosis in ovarian cancer cells and inhibits tumor progression in EAC mouse model

Translational Oncology

Raghunandan Mahadeva¹  Bibha Choudhary²  Vinay Teja³  Jinsha Koroth³  Febina Ravindran³  Tanvi R Parashar³  Subhas S Karki³ 

[1]Manipal Academy of Higher Education, Manipal 576104, India

[2]Department of Pharmaceutical Chemistry, KLE Academy of Higher Education and Research, KLE College of Pharmacy, Rajajinagar, Bangalore, KN, India

[3]Institute of Bioinformatics and Applied Biotechnology, Electronic city phase 1, Bangalore 560100, Karnataka, India

关键词: Curcumin derivative;    Ovarian cancer;    ST03;    Apoptosis;    Bioavailability;   

DOI  :  

来源: DOAJ

【 摘 要 】

Curcumin is known for its anticancer properties, but its clinical application is limited due to its poor bioavailability 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 ∼ 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.

【 授权许可】

Unknown