IJSRP, Volume 5, Issue 2, February 2015 Edition [ISSN 2250-3153]
Debasmita Dutta, Ankita Sarkar, Biswajit Chakraborty, Chinmay Chowdhury, Padma Das
Traditional medicines or herbal formulations can serve as the source of potential new chemotherapeutic drugs. Nowadays novel plant derived natural products have been designed to determine biological structure-activity relationships. A new family of betulinic acid derivatives were synthesized and the structure-activity relationship of the compounds was initially evaluated by comparing their in vitro cytotoxicity against 4 human cancer cell lines U937, HepG2, HT29, MCF-7 and non cancerous human PBMC. Betulinic Acid derivative, BC-SM-05 was the most potent inducer of apoptosis and the most effective inhibitor of cell growth and proliferation with IC50 value 19.6 µM for colon carcinoma cell line HT-29. In addition, BC-SM-05 at IC50 concentration was also found to generate increased ROS production and caspases activation. Moreover, HT-29 cells treated with BC-SM-05 and stained with Hoechst 33258 showed formation of apoptotic bodies and DNA degradation whereas untreated cells had intact nuclei. All together our data indicates that BC-SM-05 induces apoptosis in HT-29 cells via mitochondrial dependent pathway may prove itself to be a potential therapeutic agent for colon cancer, providing a basis for the development of the compound as a novel anticancer agent.