中文摘要：

目的研究丹红注射液中主要成分羟基红花黄色素A（HSYA）在Caco-2细胞单层模型的转运特征。方法MTT法确定HSYA对Caco-2细胞单层模型作用的安全浓度范围；采用Caco-2细胞单层模型考察转运时间、药物质量浓度、温度、pH值以及P-糖蛋白（P-gP）抑制剂维拉帕米和能量代谢抑制剂叠氮化钠对HSYA转运的影响；RT-PCR法检测HSYA及维拉帕米对多药耐药基因（MDR1）表达的影响。结果从顶侧（AP）到底侧（BL）（AP→BL），HSYA的表观渗透系数（Papp）在2×10-6-5×10-6cm／s，表明其吸收性中等；HSYA的转运与其质量浓度和时间呈正相关，37℃下HSYA的Papp与4、25℃下的Papp有显著差异（P〈0．01），pH值为9．0时的Papp与pH值为5．0、7．4时的Papp值也有明显差异（P〈0．01）。维拉帕米能明显下调MDR1基因的表达，但HSYA的转运不受维拉帕米的影响；叠氮化钠影响细胞能量代谢，但HSYA的转运不受能量代谢异常的影响，且Papp（BL→AP）/app（AP→BL）在1-1．5，HSYA的吸收过程基本符合被动扩散。结论HSYA在Caco-2细胞模型的转运方式为被动扩散，且不受P-gP和能量代谢的影响，低温和碱性环境下不利于HSYA的吸收。

英文摘要：

Objective To investigate the transport characteristics of hydroxysaffior yellow A （HSYA） in Danhong Injection across Caco-2 cell monolayer. Methods Safe concentration range of HSYA against Caco-2 cell monolayer model was selected by MTT method; The effects of time, drug concentration, temperature, pH, P-gp inhibitor （Verapamil）, and energy metabolism inhibitor （sodium azide） on the absorption of HSYA were observed by Caco-2 cell monolayer model; The multidrug resistance （MDRI） gene expression in Caco-2 cells was analyzed by the RT-PCR method. Results The Papp of HSYA transport from apical （AP） side to basolateral （BL） side was in 2 ×10-6 -5 × 10-6 cm/s, which showed a medium absorption. The transport of HSYAwas positively correlated with time and concentration. The Papp of HSYA transport at 37 ℃ has significant differences with those at 4 and 25 ℃ （P 〈 0.01）. The Papp of HSYA transport under pH 9.0 has significant differences with those under pH 5.0 and 7.4 （P 〈 0.01）. The gene expression of MDR1 was significantly reduced by Verapamil, but the transport of HSYA was not influenced by Verapamil and sodium azide, the number of Papp（BL→AP）/Papp（AP→BL） was between 1 and 1.5, so the absorption of HSYA was basically in line with the passive diffusion. Conclusion The transport of HSYA across Caco-2 cell monolayer model is passive diffusion, and is not influenced by the change of P-gp and energy metabolism. Low temperature and alkaline environment are not conducive to the absorption of HSYA.