论文部分内容阅读
研究辛芍提取物在Caco-2细胞中的吸收特性。该文建立人源结肠腺癌细胞系Caco-2细胞模型,采用UPLC-MS测定辛芍提取物中芍药内酯苷、没食子酸、咖啡酸、灯盏乙素、灯盏甲素5个活性成分在细胞裂解液中的含量。并用此模型分别研究p H,时间,温度以及药物浓度对辛芍提取物中芍药内酯苷等5种成分的吸收影响,并且考察在P-糖蛋白抑制剂存在与否时5种成分的转运情况,预测这5种成分在Caco-2细胞中的吸收机制。实验结果表明,在37℃下,辛芍组方提取物中5种成分的摄取具有一定的时间依赖性;在0.5~12.5 g·L~(-1),摄取呈浓度依赖性,符合被动扩散过程;在pH 4.0~7.4,咖啡酸、灯盏乙素、灯盏甲素3个成分的细胞吸收量随p H增加而显著降低(P<0.05);在4~37℃,咖啡酸的细胞吸收量随温度升高而降低,而其余4个成分随着温度升高而增加;加入P-糖蛋白抑制剂维拉帕米和环孢菌素A,咖啡酸与灯盏乙素的细胞摄取量显著增加(P<0.05)。说明辛芍提取物中芍药内酯苷等5种成分的吸收机制可能为被动扩散,且灯盏乙素和咖啡酸可能是P-糖蛋的底物。
To study the absorption characteristics of extract of Sinopotaxus in Caco-2 cells. In this study, Caco-2 cell model of human colon adenocarcinoma cell line was established. UPLC-MS was used to determine the content of aldehydes, gallic acid, caffeic acid, scutellarin, Lysate content. The model was used to study the effects of p H, time, temperature and drug concentration on the absorption of 5 components, such as albiflorin from Radix Paeoniae Alba, and the transport of 5 components in the presence of P-glycoprotein inhibitor Situation, predict the absorption mechanism of these five components in Caco-2 cells. The experimental results showed that at 37 ℃, the uptake of five components in the extract of Xin Shao recipe was time-dependent. At the concentration of 0.5 ~ 12.5 g · L -1, uptake was in a concentration-dependent manner and was consistent with passive diffusion (P <0.05); at 4 ~ 37 ℃, the cell uptake of caffeic acid, scutellarin, and scutellarin were significantly decreased with the increase of p H (P <0.05) Decreased with increasing temperature, while the other four components increased with the increase of temperature. The addition of p-glycoprotein inhibitor verapamil and cyclosporine A significantly increased the cellular uptake of caffeic acid and scutellarin (P <0.05). These results indicated that the absorption mechanism of 5 components such as albiflorin in Radix Paeoniae Alba was probably passive diffusion, and scutellarin and caffeic acid might be substrates of P-glycoprotein.