以酒石酸泰乐菌素为底药,探讨α-菠菜甾醇对小鼠小肠段药物转运体P-gp和PEPT1表达的影响。48只小鼠分为4组:α-菠菜甾醇组,酒石酸泰乐菌素组,α-菠菜甾醇和酒石酸泰乐菌素混合组,生理盐水对照组。每组按0.2 m L·10 g^(-1)体质量的...以酒石酸泰乐菌素为底药,探讨α-菠菜甾醇对小鼠小肠段药物转运体P-gp和PEPT1表达的影响。48只小鼠分为4组:α-菠菜甾醇组,酒石酸泰乐菌素组,α-菠菜甾醇和酒石酸泰乐菌素混合组,生理盐水对照组。每组按0.2 m L·10 g^(-1)体质量的剂量每天灌胃一次,共灌胃5 d,分别在1,3,5 d后处死1批采样。采用免疫组化的方法测定1,3,5 d的小鼠肠道上P-gp和PEPT1的表达。试验结果表明,α-菠菜甾醇组和混合组相对于对照组外排性药物转运体P-gp表达减少,而摄取性药物转运体PEPT1表达增多;酒石酸泰乐菌素组的外排性药物转运体P-gp表达增多,摄取性药物转运体PEPT1表达减少;且都随着用药时间的延长差异增大。表明α-菠菜甾醇具有抑制药物转运体P-gp表达和促进药物转运体PEPT1表达的作用。展开更多
寡肽转运蛋白1(oligopeptide transporter 1,PepT1;solute carrier family 15 member 1,SLC15A1)是一种主要存在于小肠上皮细胞的质子依赖型转运蛋白质,转运底物主要为蛋白质水解产物中的二肽、三肽以及与二肽、三肽结构类似的一些化合...寡肽转运蛋白1(oligopeptide transporter 1,PepT1;solute carrier family 15 member 1,SLC15A1)是一种主要存在于小肠上皮细胞的质子依赖型转运蛋白质,转运底物主要为蛋白质水解产物中的二肽、三肽以及与二肽、三肽结构类似的一些化合物。PepT1的研究有助于促进药物生物利用度的提高,对于肿瘤的治疗也具有十分重要的意义。现主要从PepT1的晶体结构、靶向前药、转运底物、相互作用的蛋白质及PepT1的疾病应答机制等几方面展开综述。展开更多
为研究温氏土鸡和白洛克鸡胚小肠寡肽转运载体PepT1(solute carrier family 15 member 1)以及Na+/H+交换载体NHE2(solute carrier family 9 member 2)和NHE3(solute carrier family 9member 3)mRNA的表达规律,选取产蛋日龄相近的温氏土...为研究温氏土鸡和白洛克鸡胚小肠寡肽转运载体PepT1(solute carrier family 15 member 1)以及Na+/H+交换载体NHE2(solute carrier family 9 member 2)和NHE3(solute carrier family 9member 3)mRNA的表达规律,选取产蛋日龄相近的温氏土鸡和白洛克鸡所产种蛋各96枚,每个品种随机分为6组,每组16枚,在相同的条件下进行孵化。分别在9(E9)、12(E12)。展开更多
To overcome the main barrier of intestinal epithelium for the oral absorption of poorly water-soluble drugs and further improve their oral absorption, Gly-Sar, the substrate of the oligopeptide transporter PepT1 widel...To overcome the main barrier of intestinal epithelium for the oral absorption of poorly water-soluble drugs and further improve their oral absorption, Gly-Sar, the substrate of the oligopeptide transporter PepT1 widely distributed in the small intestine,conjugated poly(ethylene glycol)-block-poly(D,L-lactide)(Gly-Sar-PEG-b-PLA) was designed and synthesized, and Pep T1-targeted polymeric micelles were prepared and characterized. The structure of the synthesized Gly-Sar-PEG-b-PLA was confirmed by use of TLC and 1 H-NMR. The average molecular weight measured by GPC was 5954 g/mol with PDI of 1.34. The DiI-loaded polymeric micelles from Gly-Sar-PEG-b-PLA with drug loading content of 0.076% were characterized to exhibit 40.36 nm in diameter with PDI of 0.294, and well-defined spherical shape observed by TEM. Furthermore, the PepT1-targeted polymeric micelles profoundly enhanced intestinal absorption of poorly water-soluble drug. Therefore, the designed PepT1-targeted polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs.展开更多
文摘寡肽转运蛋白1(oligopeptide transporter 1,PepT1;solute carrier family 15 member 1,SLC15A1)是一种主要存在于小肠上皮细胞的质子依赖型转运蛋白质,转运底物主要为蛋白质水解产物中的二肽、三肽以及与二肽、三肽结构类似的一些化合物。PepT1的研究有助于促进药物生物利用度的提高,对于肿瘤的治疗也具有十分重要的意义。现主要从PepT1的晶体结构、靶向前药、转运底物、相互作用的蛋白质及PepT1的疾病应答机制等几方面展开综述。
文摘为研究温氏土鸡和白洛克鸡胚小肠寡肽转运载体PepT1(solute carrier family 15 member 1)以及Na+/H+交换载体NHE2(solute carrier family 9 member 2)和NHE3(solute carrier family 9member 3)mRNA的表达规律,选取产蛋日龄相近的温氏土鸡和白洛克鸡所产种蛋各96枚,每个品种随机分为6组,每组16枚,在相同的条件下进行孵化。分别在9(E9)、12(E12)。
基金National Natural Science Foundation of China(Grant No.81673366)the National Key Science Research Program of China(973 Program,Grant No.2015CB932100)
文摘To overcome the main barrier of intestinal epithelium for the oral absorption of poorly water-soluble drugs and further improve their oral absorption, Gly-Sar, the substrate of the oligopeptide transporter PepT1 widely distributed in the small intestine,conjugated poly(ethylene glycol)-block-poly(D,L-lactide)(Gly-Sar-PEG-b-PLA) was designed and synthesized, and Pep T1-targeted polymeric micelles were prepared and characterized. The structure of the synthesized Gly-Sar-PEG-b-PLA was confirmed by use of TLC and 1 H-NMR. The average molecular weight measured by GPC was 5954 g/mol with PDI of 1.34. The DiI-loaded polymeric micelles from Gly-Sar-PEG-b-PLA with drug loading content of 0.076% were characterized to exhibit 40.36 nm in diameter with PDI of 0.294, and well-defined spherical shape observed by TEM. Furthermore, the PepT1-targeted polymeric micelles profoundly enhanced intestinal absorption of poorly water-soluble drug. Therefore, the designed PepT1-targeted polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs.
