Surh Y J, Lee S S
Department of Epidemiology & Public Health, Yale University School of Medicine, New Haven, CT 06520-8034, USA.
Life Sci. 1995;56(22):1845-55. doi: 10.1016/0024-3205(95)00159-4.
Capsaicin (8-methyl-N-vanillyl-6-nonenamide) is a primary pungent and irritating principle present in chilies and red peppers which are widely used as spices. Because of its selective effects on the functions of a defined subpopulation of sensory neurons, capsaicin is currently used as a versatile tool for the study of pain mechanisms and also for pharmacotherapy to treat several pain disorders. Considering the frequent consumption of capsaicin as a food additive and its current medicinal use, correct assessment of hazardous effects of this compound is important. Mutagenic and carcinogenic activities of capsaicin and chili extracts have been studied, but results are conflicting. Mammalian metabolism of capsaicin has been also reported. Capsaicin appears to interact with xenobiotic metabolizing enzymes, particularly microsomal cytochrome P450-dependent monooxygenases which are involved in activation as well as detoxification of various chemical carcinogens and mutagens. Recent studies have shown that hepatic cytochrome P450 2E1 catalyzes the conversion of capsaicin to reactive species such as the phenoxy radical intermediate capable of covalently binding to the active site of the enzyme as well as tissue macromolecules. While covalent modification of protein and nucleic acids leads to toxicity including necrosis, mutagenesis, and carcinogenesis, suicidal inhibition of microsomal cytochrome P450 may prohibit further activation of capsaicin and also of other toxic xenobiotics. Results from recent studies indicate that capsaicin possesses the chemoprotective activity against some chemical carcinogens and mutagens.
辣椒素（8-甲基-N-香草基-6-壬酰胺）是辣椒和红辣椒中存在的主要辛辣和刺激性成分，辣椒和红辣椒被广泛用作香料。由于其对特定亚群感觉神经元功能的选择性作用，辣椒素目前被用作研究疼痛机制以及治疗多种疼痛疾病的药物治疗的通用工具。考虑到辣椒素作为食品添加剂的频繁消费及其当前的药用用途，正确评估该化合物的有害影响很重要。已经研究了辣椒素和辣椒提取物的致突变和致癌活性，但结果相互矛盾。也有关于辣椒素在哺乳动物体内代谢的报道。辣椒素似乎与外源性代谢酶相互作用，特别是微粒体细胞色素P450依赖性单加氧酶家族，这些酶参与各种化学致癌物和诱变剂的激活以及解毒过程。最近的研究表明，肝细胞色素P450 2E1催化辣椒素转化为活性物质，如苯氧基自由基中间体，该中间体能够与酶的活性位点以及组织大分子共价结合。虽然蛋白质和核酸的共价修饰会导致包括坏死、诱变和致癌在内的毒性，但微粒体细胞色素P450的自杀性抑制可能会阻止辣椒素以及其他有毒外源性物质的进一步激活。最近的研究结果表明，辣椒素对某些化学致癌物和诱变剂具有化学保护活性。
