川芎挥发油对雷公藤甲素体外透皮性能及细胞毒性的影响  

Effect of volatile oil of Ligusticum chuanxiong on transdermal properties and cytotoxicity of triptolide in vitro

作　　者：蒋成 臧振中 陈丽华 朱海婷 傅世华 朱卫丰 吴文婷 施韡 管咏梅 JIANG Cheng;ZANG Zhenzhong;CHEN Lihua;ZHU Haiting;FU Shihua;ZHU Weifeng;WU Wenting;SHI Wei;GUAN Yongmei(Key Laboratory of Modern Preparation of Traditional Chinese Medicine,Ministry of Education,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,Jiangxi;School of Pharmacy,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,Jiangxi;Dept.of Pharmacy,Rehabilitation Hospital Affiliated to Fujian University of Traditional Chinese Medicine,Fuzhou 350003)

机构地区：[1]江西中医药大学现代中药制剂教育部重点实验室,南昌330004 [2]江西中医药大学药学院,南昌330004 [3]福建中医药大学附属康复医院药学部,福州350003

出　　处：《中国药房》2024年第4期413-418,共6页China Pharmacy

基　　金：国家自然科学基金地区科学基金项目(No.82060722);江西中医药大学校级研究生创新专项(No.JZYC22S69);福建中医药大学校管课题临床专项(No.XB2021049)。

摘　　要：目的探究川芎挥发油对雷公藤甲素体外透皮性能和细胞毒性的影响。方法采用气相色谱-质谱联用法对川芎挥发油的化学成分进行分析。分离KM小鼠下腹皮肤,分为雷公藤甲素、雷公藤甲素配伍川芎挥发油1∶10、1∶50、1∶100组(以下简称“配伍1∶10“”配伍1∶50”“配伍1∶100”组),将各组小鼠皮肤与相应乳膏各0.2 g充分接触24 h后,采用高效液相色谱法测定各组接收液中雷公藤甲素的累计透皮量(Q_(n)),并计算透皮吸收速率(J_(ss));再以人永生化角质形成细胞(HaCat)为模型,采用CCK-8法检测不同浓度川芎挥发油和雷公藤甲素配伍前后的细胞存活率。结果共鉴定出62个川芎挥发油化学成分,包括Z-藁本内酯、洋川芎内酯、β-瑟林烯等。与雷公藤甲素组比较,配伍1∶10组和配伍1∶50组24 h内雷公藤甲素的Q_(n)(P<0.01)和J_(ss)有所升高,而配伍1∶100组的Q_(n)(P<0.05)和J_(ss)有所下降。与雷公藤甲素组比较,雷公藤甲素浓度在36、72、144 ng/mL时,配伍1∶10组和配伍1∶50组可以显著提高HaCat细胞的存活率(P<0.05或P<0.01),而配伍1∶100组细胞的存活率反而降低,但差异无统计学意义(P>0.05)。结论雷公藤甲素与川芎挥发油在配伍比例为1∶10和1∶50时可以促进雷公藤甲素的透皮吸收,且可降低雷公藤甲素对HaCat细胞的毒性。OBJECTIVE To explore the effect of volatile oil of Ligusticum chuanxiong on the transdermal properties and cytotoxicity of triptolide in vitro.METHODS The chemical constituents of the volatile oil of L.chuanxiong were analyzed by gas chromatography-mass spectrometry.The lower abdominal skin of KM mice was separated and divided into triptolide group,triptolide in compatibility with volatile oil of L.chuanxiong groups at 1∶10,1∶50,1∶100(hereinafter referred to as“compatibility 1∶10”“compatibility 1∶50”“compatibility 1∶100”groups).After the skin of mice in each group was fully exposed to 0.2 g of the corresponding cream for 24 h,the cumulative transdermal dose(Q_(n))of triptolide in the receiving solution of each group was determined by high-performance liquid chromatography,and the transdermal absorption rate(J_(ss))was calculated.Human immortalized keratinocytes(HaCat)were used as a model,the CCK-8 method was used to detect the cell survival rate of different concentrations of the volatile oil of L.chuanxiong and triptolide before and after compatibility.RESULTS A total of 62 chemical constituents of the volatile oil of L.chuanxiong were identified,including Z-ligustilide,senkyunolide,andβ-selinene.The Q_(n)(P<0.01)and J_(ss)of triptolide increased within 24 h in the compatibility 1∶10 and 1∶50 groups,while the Q_(n)(P<0.05)and J_(ss)decreased in the compatibility 1∶100 group as compared with the triptolide group.Compared with the triptolide group,the cell survival rate of HaCat was significantly increased in the compatibility 1∶10 and 1∶50 groups when the triptolide concentrations were 36,72 and 144 ng/mL(P<0.05 or P<0.01);while the cell survival rate of HaCat was decreased in the compatibility 1∶100 group,but the difference was not statistically significant(P>0.05).CONCLUSIONS When the compatibility ratio of triptolide and volatile oil of L.chuanxiong was 1∶10 or 1∶50,it can promote the transdermal absorption of triptolide and reduce the cytotoxicity of triptolide to HaCa

关 键 词：川芎挥发油 雷公藤甲素 透皮吸收 配伍 增效减毒 细胞毒性 

分 类 号：R965[医药卫生—药理学]