本文通过模拟胃肠消化法评价柑橘类水果（宽皮柑、脐橙和金桔）的多酚生物有效性和抗肿瘤细胞增殖的活性。柑橘水果经过模拟胃肠消化后，采用高效液相色谱法测定主要多酚单体的释放量，亚甲基蓝法测定柑橘水果提取物抗HepG2细胞增殖的活性。结果表明，释放量较大（>20 mg/kg FW）的柑橘多酚是新橙皮甙、根皮苷、柚皮素、香草酸和原儿茶酸等。模拟胃消化过程可以促进根皮苷、香草酸和原儿茶酸的释放，而所检测的大部分多酚在肠消化过程显著降解（p<0.05）。宽皮柑、脐橙和金桔模拟胃肠消化后其产生细胞毒性的浓度显著降低（p<0.05），模拟胃消化及模拟肠消化后的提取物（浓度分别为84.56、93.74、32.26 mg/mL和121.23、107.14、40.03 mg/mL）作用于HepG2细胞72 h后，细胞的存活率分别为65.46%、37.20%、24.19%和21.32%、43.52%、12.31%，表明模拟胃肠消化过程可以促进抗HepG2细胞增殖的活性物质释放。

The bioaccessibility and anti-tumor cell proliferation activity of Citrus fruits (Citrus reticulata, Navel orange and Kumquat) polyphenol were evaluated by simulated gastrointestinal digestion. After the Citrus fruits were simulated for gastrointestinal digestion, the release of major polyphenols was determined by high performance liquid chromatography, and the activity of Citrus fruit extracts against HepG2 cells was determined by methylene blue method. The results showed that Citrus polyphenols with a large release amount (>20 mg/kg FW) were neohesperidin, phlorizin, naringenin, vanillic acid, protocatechuic acid, and the like. Simulated gastric digestion promoted the release of phlorizin, vanillic acid, and protocatechuic acid, and most of the polyphenols detected significantly degraded during intestinal digestion. After simulating gastrointestinal digestion, the Citrus fruits concentrations that produced cytotoxicity were significantly reduced. The cells survival rates were 65.46%, 37.20%, 24.19% and 21.32%, 43.52%, 12.31%, respectively, after HepG2 cells were treated with simulated gastric digestion and simulated intestine digestion of the Citrus reticulata, Navel orange and Kumquat extracts (Concentrations of 84.56, 93.74, 32.26 mg/mL and 121.23, 107.14, 40.03 mg/mL, respectively) for 72 hours. This suggests that the simulated gastric digestion promotes the release of active substances against HepG2 cell proliferation.

广东省国际合作项目（2012B050600031）；深圳市科技计划项目（JCYJ20130331151512026）