Li Hui-Fang, Zhang Dong, Qu Wen-Jun, Wang Hai-Lin, Liu Yang, Borjigdai Almaz, Cui Jian, Dong Zheng-Qi
Institute of Medicinal Plant, Chinese Academy of Medical Sciences, Beijing 100193, China.
Minzu University of China, Beijing 100081, China.
Zhongguo Zhong Yao Za Zhi. 2016 Apr;41(7):1198-1203. doi: 10.4268/cjcmm20160707.
The solubility and permeability on four kinds of flavonoids (kaempferol, hesperidin, apigenin, genistein) were test according to the theory of biopharmaceutics classification system (BCS), and their absorption mechanism. The solubility was investigated by the method in determination of solubility of "Chinese Pharmacopoeia 2010". To detect appearance permeability of compounds mentioned above, the appropriate concentrations were selected by the MTT method in cell transfer experiments in Caco-2 cell model, which established by in vitro cell culture method. Therefore, these compounds were classified with BCS according to solubility and permeability. In addition, to explore absorption mechanisms, the experiments in three different concentrations of compounds in high, medium and low in bidirectional transformation methods in Caco-2 cell model contacted. The study indicated that all of kaempferol, hesperidin, apigenin, genistein have the characteristics in low solubility and high permeability, which belong to BCSⅡ, and the absorption mechanism of kaempferol was active transportation. Whereas, hesperidin, apigenin, genistein were passive transportation. In this study, it carried out initial explorations on establishment of determination for solubility and permeability in flavonoids, and provided theoretical reference for further research on BCS in traditional Chinese medicine.
根据生物药剂学分类系统(BCS)理论,对四种黄酮类化合物(山奈酚、橙皮苷、芹菜素、染料木黄酮)的溶解度和渗透性及其吸收机制进行了研究。采用《中国药典2010年版》中溶解度测定方法考察其溶解度。为检测上述化合物的表观渗透性,通过体外细胞培养法建立Caco-2细胞模型,采用MTT法在细胞转运实验中选择合适浓度。因此,根据溶解度和渗透性对这些化合物进行BCS分类。此外,为探究吸收机制,在Caco-2细胞模型中采用双向转运法,对三种不同浓度(高、中、低)的化合物进行实验。研究表明,山奈酚、橙皮苷、芹菜素、染料木黄酮均具有低溶解度和高渗透性的特点,属于BCSⅡ类,山奈酚的吸收机制为主动转运,而橙皮苷、芹菜素、染料木黄酮为被动转运。本研究对黄酮类化合物溶解度和渗透性测定方法的建立进行了初步探索,为中药BCS的进一步研究提供了理论参考。