Piperine enhances the bioavailability of the tea polyphenol (-)-epigallocatechin-3-gallate in mice
Piperine enhances the bioavailability of the tea polyphenol (-)-epigallocatechin-3-gallate in mice
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DOI：
10.1093/jn/134.8.1948
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发表时间：
2004-08-01
影响因子：
4.2
通讯作者：
Yang, CS
中科院分区：
文献类型：
--
作者：
Lambert, JD;Hong, JG;Yang, CS
从绿色茶（Camellia sinensis）中提取的（-）-表没食子儿茶素-3-没食子酸酯（EGCG）已在致癌动物模型中显示出化学预防活性。此前，我们报道了大鼠（1.6%）和小鼠（26.5%）中EGCG的生物利用度。在这里，我们报告说，与第二种饮食成分，胡椒碱（从黑胡椒），增强了小鼠的生物利用度的表没食子儿茶素没食子酸酯。对雄性CF-1小鼠同时灌胃给予163.8 mumol/kg的EGCG和70.2 mumol/kg的胡椒碱使血浆C，a和曲线下面积（AUC）增加了1.3倍。甜菜碱似乎通过抑制葡萄糖醛酸化和胃肠道转运来增加EGCG的生物利用度。在小鼠小肠中，100 mumol/L的野牡丹碱抑制EGCG葡萄糖醛酸化（40%），但在肝微粒体中不抑制。20 μ mol/L的苦参碱也能抑制人HT-29结肠腺癌细胞中EGCG-3”-葡萄糖醛酸苷的生成。在单独用EGCG处理后，CF-1小鼠的小肠EGCG水平在60分钟时具有C-max = 37.50 +/- 22.50 nmol/g，然后在90分钟时降低至5.14 +/- 1.65 nmol/g;然而，与胡椒碱共处理导致在90分钟时C-max = 31.60 +/- 15.08 nmol/g，并且水平维持在20 nmol/g以上直到180 min。这导致小肠EGCG AUC显著增加（4621.80 +/- 1958.72 vs. 1686.50 +/- 757.07（nmol/g（.）min））。EGCG在胡椒碱共处理小鼠的结肠和粪便中的出现比单独用EGCG处理的小鼠慢。本研究证明了第二种膳食成分对EGCG生物利用度的调节，并说明了膳食化学品之间相互作用的机制。
(-)-Epigallocatechin-3-gallate (EGCG), from green tea (Camellia sinensis), has demonstrated chemopreventive activity in animal models of carcinogenesis. Previously, we reported the bioavailability of EGCG in rats (1.6%) and mice (26.5%). Here, we report that cotreatment with a second dietary component, piperine (from black pepper), enhanced the bioavailability of EGCG in mice. Intragastric coadministration of 163.8 mumol/kg EGCG and 70.2 mumol/kg piperine to male CF-1 mice increased the plasma C,a and area under the curve (AUC) by 1.3-fold compared to mice treated with EGCG only. Piperine appeared to increase EGCG bioavailability by inhibiting glucuronidation and gastrointestinal transit. Piperine (100 mumol/L) inhibited EGCG glucuronidation in mouse small intestine (by 40%) but not in hepatic microsomes. Piperine (20 mumol/L) also inhibited production of EGCG-3"-glucuronide in human HT-29 colon adenocarcinoma cells. Small intestinal EGCG levels in CF-1 mice following treatment with EGCG alone had a C-max = 37.50 +/- 22.50 nmol/g at 60 min that then decreased to 5.14 +/- 1.65 nmol/g at 90 min; however, cotreatment with piperine resulted in a C-max = 31.60 +/- 15.08 nmol/g at 90 min, and levels were maintained above 20 nmol/g until 180 min. This resulted in a significant increase in the small intestine EGCG AUC (4621.80 +/- 1958.72 vs. 1686.50 +/- 757.07 (nmol/g(.)min)). EGCG appearance in the colon and the feces of piperine-cotreated mice was slower than in mice treated with EGCG alone. The present study demonstrates the modulation of the EGCG bioavailablity by a second dietary component and illustrates a mechanism for interactions between dietary chemicals.