Nonivamide?is?a?capsaicin?analog.?Capsaicin?is?an?anti-proliferation?agent?with?IC50?value?of?100?μM?in?A172?cells.
Capsaicin?is an anti-proliferation agent with IC50 value of 100 μM in A172 cells.
Capsaicin?is an active component of chili peppers. It selectively binds to TRPV1 which is a heat-activated calcium channel. Capsaicin?causes the channel to open below 37 °C. This is why capsaicin?is linked to the sensation of heat. [1] Capsaicin?has been reported to possess anti-carcinogenic and anti-mutagenic activities. In human glioma A172 cells, capsaicin?reduced cell viability with IC50 of ～100 μM treated for 1 day. Capsaicin?inhibited cell growth and induced apoptosis through down-regulation of Bcl-2 and activation of caspase-3. Capsaicin?also induced terminal differentiation, which contribute to A172 cell growth inhibition.[2] On the other hand, capsaicin?reduced the basal generation of ROS, which may played a role in the induction of apoptosis by capsaicin.[3] In MCF-7 cells, capsaicin?induced cell apoptosis through the mitochondrial pathway, and subsequently caused PARP-1 cleaved by activation of caspase-7.[4] In human SCLC cell line, capsaicin?displayed robust anti-proliferative activity with MTT assay. Furthermore, capsaicin (10 mg/kg body weight) significantly reduced the growth rate of established (800 mm3) H69 tumors xenotransplanted in nude mice. [5]
References:
1.?M. J. Caterina, M. A. Schumacher, M. Tominaga, T. A. Rosen, J. D. Levine and D. Julius, Nature 1997, 389, 816-824.
2.?Y. G. Gil and M. K. Kang, Life Sci 2008, 82, 997-1003.
3.?Y. S. Lee, D. H. Nam and J. A. Kim, Cancer Lett 2000, 161, 121-130.
4.?H. C. Chang, S. T. Chen, S. Y. Chien, S. J. Kuo, H. T. Tsai and D. R. Chen, Hum Exp Toxicol 2011, 30, 1657-1665.
5.?K. C. Brown, T. R. Witte, W. E. Hardman, H. Luo, Y. C. Chen, A. B. Carpenter, J. K. Lau and P. Dasgupta, PLoS One 2010, 5, e10243.>
