薄荷醇通过调节角质形成细胞内钙离子浓度而产生促透作用  

Menthol promotes percutaneous absorption by regulating calcium concentration in keratinocytes

作　　者：刘文彬 黄钊 王晖 LIU Wen-bin;HUANG Zhao;WANG hui(Guangdong Provincial Key Laboratory of Pharmaceutical Bioactive Substances,School of Life Sciences and Biopharmaceutics;School of Traditional Chinese Medicine,Guangdong Pharmaceutical University,Guangzhou 510006,China)

机构地区：[1]广东药科大学生命科学与生物制药学院,广东省生物活性药物研究重点实验室,广东广州510006 [2]广东药科大学中药学院,广东广州510006

出　　处：《中国药理学通报》2023年第1期23-28,共6页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No81072591)。

摘　　要：目的研究薄荷醇促透作用的可能机制。方法原代培养人角质形成细胞,考察薄荷醇对KC细胞连接紧密性的影响,流式细胞术测定对KC细胞内Ca^(2+)浓度的影响,试剂盒法测定对KC细胞内Ca^(2+)-ATP酶活性、PLC活性、PKC活性和ATP含量的影响,考马斯蓝染色测定对KC微丝骨架结构的影响。结果与空白对照组相比,薄荷醇能明显降低KC间连接紧密性、Ca^(2+)-ATP酶活性和ATP含量,增加细胞内Ca^(2+)浓度、PLC活性和PKC活性,KC细胞间隙明显增加。与200μmol·L^(-1)薄荷醇组相比,联合使用PLC阻滞剂U73122和钙离子通道阻滞剂硝苯地平后,均能增加KC间连接紧密性,降低胞内Ca^(2+)浓度。结论薄荷醇通过增加KC胞内Ca^(2+)浓度发挥促透作用,这与其增强PLC活性、促进外源性Ca^(2+)内流有关。Aim To study the possible mechanism of menthol promotes percutaneous absorption.Methods Primary cultured human keratinocytes were used to investigate the effect of menthol on the junction tightness of KC.The effect of menthol on the concentration of Ca^(2+)in KC was measured by flow cytometry,the effects on Ca^(2+)-ATPase activity,PLC activity,PKC activity and ATP content in KC were measured by kit method,and the effect of on the microfilaments skeleton structure of KC was determined by Coomassie blue staining.Results Compared with the blank control group,menthol could significantly reduce the junction tightness between KCs,Ca^(2+)-ATPase activity and ATP content,increase the intracellular Ca^(2+)concentration,PLC activity and PKC activity,and reduce the cell volume and widen the cell gap.Compared with 200μmol·L-1 menthol group,the combination of PLC blocker u73122 and calcium channel blocker nifedipine could increase the junction tightness and reduce the concentration of intracellular Ca^(2+).Conclusions Menthol can promote percutaneous absorption by increasing the intracellular Ca^(2+)concentration of KC,which is related to enhancing PLC activity and promoting exogenous Ca^(2+)influx.

关 键 词：薄荷醇 促透机制 经皮吸收 钙离子 磷脂酶C 蛋白激酶C 

分 类 号：R322.99[医药卫生—人体解剖和组织胚胎学] R329.24[医药卫生—基础医学] R348.1R977.3