7种常见理气药挥发油对川芎嗪的促透作用及机制

Enhancing effect and mechanism of volatile oil of 7 common qi regulating medicine on penetration of ligustrazine

目的:比较7种理气药挥发油对川芎嗪的促透作用并探究作用机制。方法:提取陈皮、枳实、佛手、香附、乌药、蜘蛛香、云木香挥发油,通过GC-MS测定成分含量。体外渗透实验考察挥发油对川芎嗪的体外促透活性,并检测皮肤刺激性。通过分子对接技术研究不同种类单体成分的作用情况。结果:与空白组比较,各理气药挥发油对川芎嗪均具有促透效果,5%佛手挥发油的促透效果最好(P<0.05),对皮肤无刺激性。7种挥发油的主要成分可分为单萜、含氧单萜、倍半萜和含氧倍半萜4类,其中含氧单萜类成分与神经酰胺复合物的结合能力最强。结论:含氧单萜可能是萜类发挥促透作用的主要成分,为经皮给药系统中促透剂的筛选提供思路。

Objective:Compare the effect of 7 kinds of volatile oil of qi regulating medicine on the promotion of ligustrazine and explore the mechanism of action.Methods:GC-MS was used to determine the content of the volatile oils of tangerine peel,Fructus Aurantii Immaturus,bergamot,Cyperus rotundus,Radix Linderae,spider incense,and Radix Aucklandiae.The penetration promoting activity of the volatile oils on ligustrazine were investigated by in vitro permeation experiments,and its penetration mechanism was studied using molecular docking technology.Results:All the enhancers had significantly higher enhancing effects on the permeation of Ligustrazine than the control group.Among them,5%of the bergamot oil had the best penetration promotion effect(P<0.05).GC-MS analysis found that the main components of the seven volatile oils can be divided into four categories:monoterpenes,oxygen-containing monoterpenes,sesquiterpenes and oxygen-containing sesquiterpenes.Molecular docking shows that the oxygen-containing monoterpenoids have a strong binding ability with the ceramide complex.Conclusion:Oxygenated monoterpenes may be the main components of terpenoids that play a permeation-enhancing effect,which provided ideas for the screening of permeation enhancers in transdermal drug delivery systems.