Capsaicin and Its Analogues: Structure-Activity Relationship Study

X.-F.      Huang; J.-Y.      Xue; A.-Q.      Jiang; H.-L.      Zhu

doi:10.2174/0929867311320210004

Abstract

Capsaicin, the main ingredient responsible for the hot pungent taste of chilli peppers, is an alkaloid found in the Capsicum family. Capsaicin was traditionally used for muscular pain, headaches, to improve circulation and for its gastrointestinal protective effects. It was also commonly added to herbal formulations because it acts as a catalyst for other herbs and aids in their absorption. In addition, capsaicin and other capsaicinoid compounds showed strong evidence of having promising potential in the fight against many types of cancer. The mechanism of action of capsaicin has been extensively studied over the past decade. It has been established that capsaicin binds to the transient receptor potential vanilloid 1 receptor which was expressed predominantly by sensory neurons. And many analogues of capsaicin have been synthesized and evaluated for diverse bioactivities. In this review, we will attempt to summarize the biology and structureactivity relationship of capsaicinoids.

Keywords: Capsaicin, analgesic, anti-cancer, vasorelaxation, gastroprotection, structure and activity relationship.

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