PT - JOURNAL ARTICLE AU - Jamie R. Friedman AU - Nicholas A. Nolan AU - Kathleen C. Brown AU - Sarah L. Miles AU - Austin T. Akers AU - Kate W. Colclough AU - Jessica M. Seidler AU - John M. Rimoldi AU - Monica A. Valentovic AU - Piyali Dasgupta TI - Anticancer Activity of Natural and Synthetic Capsaicin Analogs AID - 10.1124/jpet.117.243691 DP - 2018 Mar 01 TA - Journal of Pharmacology and Experimental Therapeutics PG - 462--473 VI - 364 IP - 3 4099 - http://jpet.aspetjournals.org/content/364/3/462.short 4100 - http://jpet.aspetjournals.org/content/364/3/462.full SO - J Pharmacol Exp Ther2018 Mar 01; 364 AB - The nutritional compound capsaicin is the major spicy ingredient of chili peppers. Although traditionally associated with analgesic activity, recent studies have shown that capsaicin has profound antineoplastic effects in several types of human cancers. However, the applications of capsaicin as a clinically viable drug are limited by its unpleasant side effects, such as gastric irritation, stomach cramps, and burning sensation. This has led to extensive research focused on the identification and rational design of second-generation capsaicin analogs, which possess greater bioactivity than capsaicin. A majority of these natural capsaicinoids and synthetic capsaicin analogs have been studied for their pain-relieving activity. Only a few of these capsaicin analogs have been investigated for their anticancer activity in cell culture and animal models. The present review summarizes the current knowledge of the growth-inhibitory activity of natural capsaicinoids and synthetic capsaicin analogs. Future studies that examine the anticancer activity of a greater number of capsaicin analogs represent novel strategies in the treatment of human cancers.