摘要
目的:研究萜烯类经皮促透剂桉树醇(1,8-Cineole)对HaCaT细胞膜流动性及细胞内Ca2+浓度的影响,探究其促透作用机制。方法:采用CCK-8试剂盒测定并计算桉树醇对HaCaT细胞的半数抑制率(IC50);利用荧光漂白恢复技术(FRAP)测定不同浓度桉树醇对HaCaT细胞膜流动性的影响;采用流式细胞仪测定桉树醇对HaCaT细胞内Ca2+浓度的改变。结果:桉树醇药物IC50为9.077 mmol·L-1;不同浓度桉树醇均可显著增加细胞膜流动性,且随着药物浓度的增大而增加,呈剂量依赖性关系。同时,桉树醇可降低HaCaT细胞内Ca2+浓度。结论:桉树醇的经皮促透作用机制可能与影响角质细胞内Ca2+浓度进而改变细胞膜流动性有关。
Objective： To investigate the effects of 1,8-cineole on intracellular Ca2＋ concentration and membrane fluidity of HaCaT cells and study its possible mechanism of penetration enhancement action. Methods： The well-established and standard penetratration enhancer azone was employed as a positive control in this study. The cytotoxicities of 1,8-cineole and azone on HaCaT cells were measured by CCK-8 assay, and their half maximal inhibitory concentrations （IC50） were calculated with reference to the literature method. Fluorescence recovery after photobleaching （FRAP） was employed to investigate the effect of 1,8-cineole and azone on membrane fluidity, and flow cytometer was used to monitor the change of intracellular Ca2＋ concentration of HaCaT cells after being treated with these penetration enhancers. Results： The IC50 values of 1 , 8-cineole and azone were 9. 077 and 0. 172 mmol. L-1, respectively. Similar to azone, 1,8-cineole could significantly improve the membrane fluidity in a concentration-dependent manner, and effectively decrease the intracellular Ca2＋ concentration of HaCaT cells. Conclusion： The penetration enhancement mechanism of 1,8-cineole is associated with the changes of the membrane fluidity and intracellular Ca2. concentration of HaCaT cells.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2014年第21期2568-2571,2580,共5页
Chinese Journal of New Drugs
