Capsaicin-like anti-obese activities of evodiamine from fruits of Evodia rutaecarpa, a vanilloid receptor agonist
Capsaicin-like anti-obese activities of evodiamine from fruits of Evodia rutaecarpa, a vanilloid receptor agonist
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DOI：
10.1055/s-2001-17353
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发表时间：
2001-10-01
期刊：
影响因子：
2.7
通讯作者：
Kamiya, T
中科院分区：
文献类型：
--
作者：
Kobayashi, Y;Nakano, Y;Kamiya, T
吴茱萸碱是吴茱萸属植物吴茱萸果实的主要生物碱成分，具有与辣椒素相当的类香草素受体激动活性。中国文献将吴茱萸果实称为“热性”草药。尽管吴茱萸碱和辣椒素在体外的作用相似，但吴茱萸碱没有可感知的味道，包括辛辣的味道。因此，检测了吴茱萸碱和吴茱萸果实提取物在预防雄性C3 H小鼠或雄性SD大鼠肥胖中的有效性。当以饲料的0.03%补充吴茱萸碱并喂给小鼠12天时，肾周脂肪重量变得显著低于对照组。吴茱萸碱饮食组的附睾脂肪量也减少。当以吴茱萸果实的乙醇提取物的形式以0.02%的剂量添加到高脂饮食中并喂养大鼠21天时，与对照饮食组相比，体重、肾周脂肪重量、附睾脂肪重量、血清游离脂肪酸水平、肝脏中的总脂质、肝脏中的甘油三酯和肝脏中的胆固醇水平显著降低。此外，无论是在肾周脂肪组织中的脂肪分解活性和棕色脂肪组织线粒体中的特定GDP结合，作为增强产热的生物学指标，在吴茱萸喂养大鼠显着增加。禁食小鼠皮下注射1-3 mg/kg吴茱萸碱，显示核心体温降低1-2 ℃。这种低温效应可通过腹腔注射辣椒素受体拮抗剂（capsazepine）（10 mg/kg）进行预处理来预防。另一方面，皮下注射1-3 mg/kg吴茱萸碱的食物饱足小鼠显示核心体温不变，尾部皮肤温度增加超过5 ℃，表明通过增强散热增加能量消耗。总之，我们已经证明，一种新的非辛辣的香草素受体激动剂，吴茱萸碱，模仿辣椒素诱导的特征性抗肥胖作用。吴茱萸碱可同时诱导热损失和产热，耗散食物能量，防止内脏周围脂肪堆积和体重增加。
Evodiamine, a major alkaloidal principle of Evodia fruits (Evodia rutaecarpa, Rutaceae), showed vanilloid receptor agonistic activities comparable to capsaicin. The Chinese literature refers to Evodia fruits as a "hot nature" herb. In spite of the similarities in the actions of evodiamine and capsaicin in vitro, evodiamine has no perceptible taste, including a peppery hot taste. Therefore, the effectiveness of evodiamine and the extract of Evodia fruits in preventing obesity on male C3H mice, or male SD rats were examined. When evodiamine was supplemented at 0.03% of the diet and fed to mice for 12 days, the perirenal fat weight became significantly lower than in the control group. The epididymal fat mass was also decreased in the evodiamine diet group. When evodiamine was supplemented at 0.02% in the form of ethanol extract of Evodia fruits to the high-fat diet and fed to rats for 21 days, the body weight, the perirenal fat weight, epididymal fat weight, the levels of serum free fatty acid, total lipids in the liver, triglyceride in the liver, and cholesterol level in the liver were significantly reduced as compared with the control diet group. Furthermore, both lipolytic activity in the perirenal fat tissue and specific GDP binding in brown adipose tissue mitochondria, as the biological index of enhanced heat production, were significantly increased in the evodiamine fed rats. Fasting mice subcutaneously administered 1-3 mg/kg evodiamine showed decreased core body temperature by 1-2 degreesC. This hypothermic effect was prevented by the pretreatment of intraperitoneally administered 10 mg/kg capsazepine, a vanilloid receptor antagonist. on the other hand, food-sated mice subcutaneously administered 1-3 mg/kg evodiamine showed unchanged core body temperature and increased tail skin temperature by more than 5 degreesC, suggesting the increased energy expenditure by enhanced heat dissipation. In conclusion, we have demonstrated that a novel non-pungent vanilloid receptor agonist, evodiamine, mimics the characteristic anti-obese effects induced by capsaicin. Evodiamine would induce heat loss and heat production at the same time and dissipate food energy, preventing the accumulation of perivisceral fat and the body weight increase.