Anticancer Activity of Natural and Synthetic Capsaicin Analogs

Abstract

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.

Open‐tubular capillary electrochromatographic application of a sol‐gel matrix with chilli peppers, garlic, or synthetic additives

“…Among the mineral constituents, Fe, Ca, K, Mg, P, S, Na, and Se can be found. Capsaicin or the extract of chilli fruits was reported to have antidiabetic, anticancer, antiulcer, anticoagulant, analgesic, antiarthritic activities, as well as immunomodulatory, cardiovascular, pain-relief effects and memory enhancing, respiratory, hepatoprotective, anthelmintic, antifungal and antiviral activity [15][16][17].…”

Long INterspersed element‐1 mobility as a sensor of environmental stresses

“…Capsaicin (trans‐8‐methyl‐ N ‐vanillyl‐6‐noneamide) is the main neurologically active component of chili peppers in the plant genus Capsicum (Friedman et al ., ). It is used as analgesic to treat pain and inflammation, and its analgesic activity is mediated by transient receptor potential subfamily vanilloid member 1 receptor (TRPV1), indeed it functions as an agonist of the TRPV1 receptor (Julius et al ., ).…”

Inhibition of LINE-1 Retrotransposition by Capsaicin

“…Emerging evidence indicates that capsaicin exhibits an anti-cancer and/or growth-inhibitory effect in various cancers [ 16 , 24 ]. Although the mechanisms of how capsaicin exhibits these inhibitory effects against various cancer cell types still remain unclear, the proposed mechanisms are related to cell cycle arrest and induction of apoptosis [ 25 ].…”

“…Capsaicin is a major chemical constituent of Asiasari Radix and Capsicum annuum [ 16 ] and also a constituent of a Chinese traditional herbal medicine, Sho-seiryu-to . The compound is a homovanillic acid derivative and is known as a potent analgesic that is used for treating pain and inflammation [ 17 ].…”