羟基红花黄色素A的Caco-2细胞摄取转运研究

被引：4

作者：

王刚 ^{[1
]}

李晴宇 ^{[1
]}

方秋黎 ^{[2
]}

韩旻 ^{[2
]}

高建青 ^{[2
]}

机构：

[1] 杭州市第一人民医院药剂科

[2] 浙江大学药学院药物制剂研究所

来源：

中国药学杂志 | 2009年 / 44卷 / 05期

关键词：

羟基红花黄色素A; 稳定性; 排泄; 摄取; 转运; Caco-2细胞;

D O I：

暂无

中图分类号：

R285 [中药药理学];

学科分类号：

1008 ;

摘要：

目的研究羟基红花黄色素A(HSYA)的胃肠吸收转运机制。方法采用Caco-2细胞模型考察孵育时间、介质pH、药物浓度及抑制剂(环孢菌素A和叠氮钠)对羟基红花黄色素A摄取转运的影响,并分析HSYA灌胃给药后在大鼠尿及粪中的累积排泄。结果HSYA的摄取符合被动扩散过程,pH7.8环境下药物的细胞摄取量[(1.05±0.045)mg·g-1]低于pH5.4[(1.24±0.09)mg·g-1](P<0.05),其在Caco-2单细胞层的表观透过系数(Papp)为(2.16±1.21)×10-8cm·s-1,加入环孢菌素A和叠氮钠后其Papp显著提高(P<0.05),分别为(47.92±17.8)×10-8和(12.53±4.55)×10-8cm·s-1。HSYA大鼠灌胃给药(5.6mg·kg-1)后31h,其尿和粪中的累积排泄量分别为给药剂量的0.74%和28.57%。结论HSYA的吸收基本符合被动扩散过程并有P-gp的参与,其黏膜透过性较差,碱性环境相对不利于药物的吸收。HSYA口服后的胃肠吸收较差,大量的药物被排出体外或在胃肠道内被代谢转化。

引用

页码：353 / 357

页数：5

共 15 条

[1]

Therapeutic effects of hydroxysafflor yellow A on focal cerebral ischemic injury in rats and its primary mechanisms. Zhu HB,Zhang L,Wang ZH,et al. Journal of Asian Natural Products Research . 2005

[2]

Mechanisms of transportand structure-permeability relationship of sulfasalazine and its analogsin Caco-2cell monolayer. Liang E,,Proudfoot J,Yazdanian M. Pharmacological Research . 2000

[3]

Oral absorption of Ginsenoside Rb1using in vitro and in vivo models. Han M,Sha X,Wu Y,et al. Planta Medica . 2006

[4]

Pharmacokineticsand excretion of hydroxyl safflor yellow A,a potentneuroprotective agent from safflower,in rats and dogs. Chu DF,Liu WH,Huang Z,et al. Planta Medica . 2006

[5]

l Neuroprotective effects of hydroxysafflor yellow A; In vivo and in vitro studies. Zhu HB,Wang ZH,et a. Planta Medica . 2003

[6]

Hydroxysafflor yellow A protects rat brains against ischemia-reperfusion injury by antioxidant action. Wei,X,Liu,H,Sun,X,Fu,F,Zhang,X,Wang,J,An,J,Ding,H. Neuroscience Letters . 2005

[7]

Evidence that hydroxysaffloryellow A protects the heart against ischaemia-reperfusioninjury by inhibiting mitochondrial permeability transitionpore opening. Liu YN,Zhou ZM,Chen P. Clinical and Experimental Pharmacology and Physiology . 2008

[8]

Two new quinochalcone yellow pigments from carthamus tinctorius and Ca2+ antagonistic activity of tinctormine. Meselhy R. Meselhy,Shigetoshi Kadota,Yasunori Momose,et al. Chemical and Pharmaceutical Bulletin . 1993

[9]

Protective effects of hydroxysafflor yellow A on acute and chronic congestive cardiac failure mediated by reducing ET-1,NOS and oxidative stress in rats. HE H,YANG X,SHI M,et al. Journal of Pharmacokinetics and Pharmacodynamics . 2008

[10]

Cardioprotective effects of hydroxysafflor yellow A on diabetic cardiac insufficiency attributed to up-regulation of the expression of intracellular calcium handling proteins of sarcoplasmic reticulum in rats. HE H,LIU Q,SHI M,et al. Phytotherapy Research . 2008

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