激光扫描共聚焦显微镜观测大黄素β-环糊精包合物在鼻咽癌细胞的跨膜转运及分布

Observation of Emodin-β-CD Inclusion Complex′s Transmembrane Transport in Nasopharyngeal Carcinoma Cells and Its Distribution by the Laser Scanning Confocal Microscope

利用激光扫描共聚焦显微镜动态研究大黄素β-环糊精包合物在鼻咽癌CNE-1细胞的跨膜转运及分布。结果显示,大黄素β-环糊精包合物以颗粒的形式主要分布于胞浆中,在其浓度为5~40mg·L-1时细胞对其摄取量随浓度的增加呈非线性增加;NaN3、甘露醇可抑制CNE-1细胞对大黄素β-环糊精包合物的摄入量,环孢菌素A(CsA)在药物浓度低(小于5mg·L-1)时可显著增加细胞对大黄素β-环糊精包合物的摄入量,而在药物浓度大时,反而抑制细胞的摄取量。相对大黄素而言,大黄素β-环糊精包合物在细胞内持续时间较长。大黄素β环糊精包合物在鼻咽癌CNE-1细胞的跨膜转运主要遵循能量依赖的内吞模式且受P-gp蛋白的调控,这一特性可为药物剂型研究提供参考。

The transmembrane transport and distribution characteristics of emodin-^-CD inclusion complex in the nasopharyngeal carcinoma CNE-1 cells are observed using laser scanning confocal microscope. The results show that both emodin and emodin-β3-CD inclusion complex are mainly distributed in the cytoplasm in granules. In the concentration range of 5-4.0 mg~ L -1, the intake of emodin-β-CD inclusion complex nonlinearly increases with the increase of concentrations. Compared with the control group, emodin-β-CD inclusion complex uptake in cells is significantly lower than that of treatment with NaNs and mannitol, After treatment with P-glycoprotein inhibitors cyclosporin A （CsA）, intake of emodin-β-CD inclusion complex at low concentrations （smaller than 5 mg L 1） significantly increases, but at high concentrations, intake of emodin-β-CD inclusion complex significantly decreases. Emodin-β-CD inclusion complex has long time of maintaining high concentration in cell relative to emodin. The mechanism of emodin-β-CD inclusion complex uptake in cells may involve energy-dependent endocytosis and P-glycoproteins participates in the conveying process of emodin-β-CD inclusion complex in CNE-1 cells. It provides a reference to improving emodin formulations.