摘要
目的 研究P-糖蛋白(P-gp)调控下,石菖蒲挥发油、α及β-细辛醚对远志活性成分3,4,5-三甲氧基肉桂酸(TMCA)在大鼠空肠、回肠的吸收特性的影响。方法 MTT实验研究P-gp抑制剂维拉帕米(Ver)、石菖蒲挥发油、α-及β-细辛醚对远志细胞毒作用的影响;外翻肠囊法研究TMCA在空肠、回肠中的吸收速率常数(Ka)及累积吸收量(Q),考察以上药物对其肠吸收特性的影响。结果 石菖蒲挥发油、α-及β-细辛醚、Ver可增加远志细胞毒作用。TMCA在空肠、回肠中为线性吸收(r>0.95),回肠段Q及Ka值高于空肠段;石菖蒲挥发油、α-及β-细辛醚、Ver可显著提高TMCA在空肠、回肠中的Q及Ka值(P<0.05或P<0.01)。结论 TMCA为P-gp底物;石菖蒲挥发油所含α-及β-细辛醚可能通过抑制肠段P-gp功能,提高TMCA肠道吸收。
Objective To investigated the influence of the volatile oil of Acori tatarinowii rhizome,α-asarone and β-asarone on adsorption characteristics of 3,4,5-trimethoxycinnamic acid (TMCA), the active constituents of Polygalae radix in rats’ jejunum and ileum by P-Glycoprotein (P-gp) modulation. Methods MTT assay is applied in investigating the impact of the verpamail (Ver), an P-gp inhibitor, volatile oil,α- and β-asarone on the cytotoxicity of Polygalae radix. The everted intestine sac model is employed to research the accumulative absorbed doses (Q) and absorption rate constants (Ka) of TMCA in jejunum and ileum. To investigate the influence of Ver, volatile oil,α- and β-asarone on the intestinal absorption characteristics of TMCA. Results The volatile oil of Acori tatarinowii rhizome,α-asarone,β-asarone and Ver significantly reduced the IC50 of Polygalae radix in Caco- 2 cells. The absorption model of TMCA is linearity with r > 0.95. Q and Ka of TMCA in jejunum is aelatively higher than that in ileum. The volatile oil of Acori tatarinowii rhizome,α-asarone,β-asarone and Ver significantly inhance the constant of Q and Ka of TMCA in jejunum and ileum (P < 0.05 or P < 0.01). Conclusion TMCA may the potential P-gp substrate. The volatile oil of Acori tatarinowii rhizome,α-asarone and β-asarone could increase the intestinal absorbtion of TMCA. Because they could inhibit the function of P-gp.
作者
孟雪
贾璞
张毅
王世祥
郑晓晖
陈志永
骆晶
MENG Xue;JIA Pu;ZHANG Yi;WANG Shi-xiang;ZHENG Xiao-hui;CHEN Zhi-yong;LUO Jing(Shaanxi Academy of Traditional Chinese Medicine, Xi'an 710003, China;College of Life Sciences,Northwest University, Xi'an 710069, China;Xianyang Central Hospital, Xianyang 712000, China)
出处
《现代中药研究与实践》
CAS
2019年第5期19-23,共5页
Research and Practice on Chinese Medicines
基金
陕西省中医药管理局中医药课题（15-ZY014）
陕西省教育厅科研计划项目（09JS086）
陕西省重点研发计划一般项目（2019SF-280）
作者简介
孟雪(1986-),女,博士,助理研究员,研究方向:中药创新药物研究。E-mail:mengxuenir@163.com;通讯作者:骆晶(1981-),男,硕士,主治医师,研究方向:中医药临床研究。E-mail:luojing28@163.com.
