Abstract
Capsaicin is the most predominant and naturally occurring alkamide found in Capsicum fruits. Since its discovery in the 19th century, the therapeutic roles of capsaicin have been well characterized. The potential applications of capsaicin range from food flavorings to therapeutics. Indeed, capsaicin and few of its analogues have featured in clinical research covered by more than a thousand patents. Previous records suggest pleiotropic pharmacological activities of capsaicin such as an analgesic, anti-obesity, anti-pruritic, anti-inflammatory, anti-apoptotic, anti-cancer, anti-oxidant, and neuro-protective functions. Moreover, emerging data indicate its clinical significance in treating vascular-related diseases, metabolic syndrome, and gastro-protective effects. The dearth of potent drugs for management of such disorders necessitates the urge for further research into the pharmacological aspects of capsaicin. This review summarizes the historical background, source, structure and analogues of capsaicin, and capsaicin-triggered TRPV1 signaling and desensitization processes. In particular, we will focus on the therapeutic roles of capsaicin and its analogues in both normal and pathophysiological conditions.
Highlights
Introduction and Historical ViewpointThe transfer of foods between the New and Old Worlds during the Columbian Exchange introduced the chili pepper to the world [1]
The aim of this review is to provide a comprehensive overview of the capsaicin compound, and more importantly delve into its therapeutic potential in various human ailments
Another study demonstrated the effect of capsaicin in endothelium-dependent and -independent relaxation on rat mesenteric-artery which may be mediated by endothelial nitric oxide synthase-NO pathway and calcitonin gene-related peptide (CGRP), respectively [199]
Summary
The transfer of foods between the New and Old Worlds during the Columbian Exchange introduced the chili pepper to the world [1]. Several compounds related to capsaicin grouped as capsaicinoids have been isolated from Capsicum species [9]. EU supported the application of Qutenza for post-herpetic neuralgia (PHN), peripheral neuropathic pain (PNP), and HIV-associated distal sensory polyneuropathy (HIV-DSP) related pain conditions [24,25], in the USA, the FDA approved its use for PHN only [26,27] These reports and several other studies clearly depicted capsaicin as an exciting pharmacological agent and its application in different clinical conditions are still being investigated [28,29]. Peppers) show in similar effects like capsaicinoids, but differ slightly in the structure capsinoids Thegeneral generalchemical chemicalstructure structure capsaicinoid capsinoid related analogues differ in theinR-group are summarized. Moiety and in thelinkage central (shown linkage (shown in red) and R-group
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