辣椒素的摄取、代谢与生物学效应

The consumption, metabolism and biological effects of capsaicin

辣椒是经常食用的食物之一,辣椒中含量最丰富且生物活性最活跃的是辣椒素,辣椒素是一种天然的生物碱,来源于辣椒属植物,又名反-8-甲基-N-香草基-6-壬烯基酰胺。是具有高度挥发性、亲脂疏水性的白色结晶粉末。皮肤角质层吸收非常快,85%～95%的辣椒素都可以经过胃肠道迅速吸收,吸收后的辣椒素主要经过肝脏细胞色素酶P450代谢,还有一小部分在小肠中水解。代谢产物主要经过肾脏排出,少部分以原型的形式经粪便和尿液排出。全身给药后,脑、脊髓和肝脏中的辣椒素浓度较高。临床试验表明,辣椒素可能具有减重、抗癌、缓解疼痛、保护心血管和胃肠道等多种生物活性,并依靠TRPV1受体发挥多种病理生理功能。然而,作为辣椒提取物中最活跃的成分,辣椒素的确切功能仍然存在争议,辣椒素可能随着其摄入的剂量变化而产生不同的效能,并且辣椒素在体内的代谢途径和方式也较为独特。因此,本文旨在系统性综述辣椒素的摄取、代谢与生物学效应,为辣椒素在药用前景提供了新的实验依据和思路,并为辣椒素潜在临床价值的发掘奠定了理论基础。

Chili is a widely used flavoring food.The major active compounds of chili are Capsaicin.Capsaicin(trans-8-methyl-N-vanillyl-6-nonenamide)is a naturally occurring alkaloid derived from plants of the genus Capsicum.It is a highly volatile,pungent,hydrophobic,colorless and odorless white crystalline powder.Topical capsaicin in humans is rapidly and well absorbed through the skin.85%~95%of capsaicin can be absorbed by a nonactive process from the stomach and whole intestine.Cytochrome P450 enzymes participate in the metabolism of capsaicin in liver,and a small part of capsaicin is hydrolyzed in the small intestine.Capsaicin is eliminated mainly by the kidneys,with a small untransformed proportion excreted in the feces and urine.Systemic administration of capsaicin involves both intravenous and subcutaneous methods.Capsaicin in the liver,brain and spinal cord was very high compared with the blood.Clinical trials have shown that capsaicin may have various biological activities,such as weight loss,anti-cancer,pain relief,protection of cardiovascular and gastrointestinal tract,and rely on TRPV1 receptor to exert various pathophysiological functions.However,as the most active ingredient in capsicum extract,the exact function of capsaicin is still controversial.Capsaicin may have different effects depending on the dosage of intake,and its metabolism in the body is unique.Our article aims to systematically review the consumption,metabolism and biological effects of capsaicin,which provides new experimental ideas for medicinal prospects of capsaicin in the future,and a theoretical foundation for the potential clinical value of capsaicin.