Rollyson William D, Stover Cody A, Brown Kathleen C, Perry Haley E, Stevenson Cathryn D, McNees Christopher A, Ball John G, Valentovic Monica A, Dasgupta Piyali
Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA.
Department of Pharmacology, Physiology and Toxicology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, USA.
J Control Release. 2014 Dec 28;196:96-105. doi: 10.1016/j.jconrel.2014.09.027. Epub 2014 Oct 12.
The dietary compound capsaicin is responsible for the "hot and spicy" taste of chili peppers and pepper extracts. It is a valuable pharmacological agent with several therapeutic applications in controlling pain and inflammation. Emerging studies show that it displays potent anti-tumor activity in several human cancers. On a more basic research level, capsaicin has been used as a ligand to activate several types of ion-channel receptors. The pharmacological activity of capsaicin-like compounds is dependent on several factors like the dose, the route of administration and most importantly on its concentration at target tissues. The present review describes the current knowledge involving the metabolism and bioavailability of capsaicinoids in rodents and humans. Novel drug delivery strategies used to improve the bioavailability and therapeutic index of capsaicin are discussed in detail. The generation of novel capsaicin-mimetics and improved drug delivery methods will foster the hope of innovative applications of capsaicin in human disease.
膳食化合物辣椒素是辣椒和辣椒提取物“辛辣”味道的来源。它是一种有价值的药理剂，在控制疼痛和炎症方面有多种治疗应用。新出现的研究表明，它在几种人类癌症中显示出强大的抗肿瘤活性。在更基础的研究层面，辣椒素已被用作激活几种类型离子通道受体的配体。辣椒素类化合物的药理活性取决于几个因素，如剂量、给药途径，最重要的是其在靶组织中的浓度。本综述描述了目前关于辣椒素类化合物在啮齿动物和人类体内代谢及生物利用度的知识。详细讨论了用于提高辣椒素生物利用度和治疗指数的新型药物递送策略。新型辣椒素模拟物的产生和改进的药物递送方法将为辣椒素在人类疾病中的创新应用带来希望。
