title: Harnessing the Therapeutic Potential of Capsaicin and Its Analogues in Pain and Other Diseases.
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.
authors.affiliation: National Leading Research Laboratory (NLRL) of Molecular Modeling &amp; Drug Design, College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 03760, Korea. shaherinb@gmail.com.
authors.forename: Shaherin
authors.initials: S
authors.lastname: Basith
authors.affiliation: National Leading Research Laboratory (NLRL) of Molecular Modeling &amp; Drug Design, College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 03760, Korea. babana1987@naver.com.
authors.forename: Minghua
authors.initials: M
authors.lastname: Cui
authors.affiliation: National Leading Research Laboratory (NLRL) of Molecular Modeling &amp; Drug Design, College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 03760, Korea. sunhye_15@naver.com.
authors.forename: Sunhye
authors.initials: S
authors.lastname: Hong
authors.affiliation: National Leading Research Laboratory (NLRL) of Molecular Modeling &amp; Drug Design, College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 03760, Korea. sunchoi@ewha.ac.kr.
authors.forename: Sun
authors.initials: S
authors.lastname: Choi
mesh_terms: D002211:Capsaicin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D002212:Capsicum / Q000737:chemistry / Q000145:classification; D002986:Clinical Trials as Topic; D006801:Humans; D015394:Molecular Structure; D010146:Pain / Q000188:drug therapy* / Q000209:etiology / Q000378:metabolism; D018689:Sensory System Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship; D050916:TRPV Cation Channels / Q000378:metabolism
chemical_list: D018689:Sensory System Agents; D050916:TRPV Cation Channels; C494482:TRPV1 protein, human; D002211:Capsaicin
keywords: analogues; capsaicin; desensitization; neuropathic pain; therapeutic