Nonivamide (Capsaicin Analog)

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Background

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]

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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.>