Ng Siu Pong, Wong Ka Yin, Zhang Li, Zuo Zhong, Lin Ge
Faculty of Medicine, The Chinese University of Hong Kong, School of Pharmacy, Shatin, New Territories, Hong Kong.
J Pharm Pharm Sci. 2004 Dec 20;8(1):1-9.
Four flavones, namely Apigenin, Baicalein, Chrysin and Luteolin, were selected for study and comparison of their absorption and metabolism in gut using the in vitro Caco-2 monolayer model.
Transport of the four flavones in the Caco-2 monolayer model was studied in both Apical-to-Basolateral and Basolateral-to-Apical directions.
All of the selected flavones were able to pass through the Caco-2 cell monolayer with no significant efflux. The permeability coefficients of the four compounds were all greater than 10(-6) cm/sec and those of Apigenin and Baicalein were even greater than 10(-5) cm/sec. Glucuronides of the tested flavones were all formed in the Caco-2 cell monolayer model and a structure-activity relationship has been proposed for this glucuronidation. In addition, Apical-to-Basolateral transport studies were performed in Caco-2 models pre-treated with Chrysin, an UGT inducer. Quantities of the corresponding glucuronides formed were all significantly higher in Chrysin-treated groups than the controls.
It demonstrated that all selected flavones were substrates of the UGT isoforms that are inducible by Chrysin.
选用芹菜素、黄芩素、白杨素和木犀草素这四种黄酮类化合物，利用体外Caco-2单层细胞模型研究并比较它们在肠道中的吸收和代谢情况。
在Caco-2单层细胞模型中，研究了这四种黄酮类化合物在顶侧到基底侧以及基底侧到顶侧两个方向上的转运情况。
所有选定的黄酮类化合物均能穿过Caco-2细胞单层，且无明显外排现象。这四种化合物的渗透系数均大于10^(-6) cm/秒，其中芹菜素和黄芩素的渗透系数甚至大于10^(-5) cm/秒。受试黄酮类化合物的葡萄糖醛酸苷均在Caco-2细胞单层模型中形成，并针对这种葡萄糖醛酸化提出了构效关系。此外，在用白杨素（一种UGT诱导剂）预处理的Caco-2模型中进行了顶侧到基底侧的转运研究。白杨素处理组中形成的相应葡萄糖醛酸苷的量均显著高于对照组。
结果表明，所有选定的黄酮类化合物都是可被白杨素诱导的UGT同工酶的底物。
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