Identification and characterization of nucleoside transporters that participate in placental permeation of drugs
参与药物胎盘渗透的核苷转运蛋白的鉴定和表征
基本信息
- 批准号:16590104
- 负责人:
- 金额:$ 2.3万
- 依托单位:
- 依托单位国家:日本
- 项目类别:Grant-in-Aid for Scientific Research (C)
- 财政年份:2004
- 资助国家:日本
- 起止时间:2004 至 2005
- 项目状态:已结题
- 来源:
- 关键词:
项目摘要
Ribavirin, an antivirus agent, was shown to be transported via CNT3 and ENT1 in human choriocarcinoma (Bewo) cells. Then we investigated characteristics of each subtype of the nucleoside transporters. Using Xenopus laevis oocytes expressing human nucleoside transporters, it was suggested that ribavirin has relatively higher affinity (〜20 μM) to sodium-dependent transporters (CNT) and lower affinity (〜mM) to sodium-independent transporters (ENT). Since it is reported that both CNT and ENT express in the brush border membrane of the placental epithelial cells, we measured the uptake of rebavirin by the oocytes expressing both hCNT3 and hENT1 (co-expressing oocyte). The uptake of ribavirin by co-expressing oocytes was lower than that by the oocytes that expressing only hCNT3. These results suggest that the concentration of ribavirin in the cells is maintained by the uptake via CNT and efflux via ENT and permeation of ribavirin through the placenta is not concentrative toward fetal side.On the other hand, it was suggested that in the intestine, in which CNT and ENT express in brush border membrane and basolateral membrane, respectively, these transporters also contribute to the absorption of ribavirin. In the intestine, rebavirin was suggested to be taken up by concentrative manner through the brush border membrane, and then fluxed into blood flow by facilitated diffusion through the basolateral membrane.
利巴韦林是一种抗病毒药物,可通过CNT3和ENT1在人绒毛膜癌细胞(Bewo)中转运。然后,我们研究了核苷转运蛋白的每一亚型的特征。利用表达人核苷转运蛋白的非洲爪哇卵母细胞,发现利巴韦林对钠依赖转运蛋白具有较高的亲和力(~20μM),而对钠非依赖性转运蛋白的亲和力较低(~mM)。由于有报道称CNT和ENT都在胎盘上皮细胞的刷状缘膜上表达,我们测量了同时表达hCNT3和hENT1的卵母细胞(共表达卵母细胞)对瑞巴韦林的摄取。共表达的卵母细胞对利巴韦林的摄取低于单独表达hCNT3的卵母细胞。这些结果表明,利巴韦林在细胞内的浓度是通过CNT摄取和通过ENT排出维持的,利巴韦林通过胎盘的渗透不是向胎盘集中的。另一方面,在肠道中,CNT和ENT分别在刷状缘膜和基侧膜上表达,这些转运体也有助于利巴韦林的吸收。在肠道中,瑞巴韦林可通过刷状缘膜浓集吸收,然后通过基侧膜促进扩散进入血流。
项目成果
期刊论文数量(0)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
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SUGAWARA Mitsuru其他文献
SUGAWARA Mitsuru的其他文献
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{{ truncateString('SUGAWARA Mitsuru', 18)}}的其他基金
Optimization of drug administration order in anti-cancer drug combination therapy in hematopoietic stem cell transplantation
造血干细胞移植抗癌药物联合治疗给药顺序的优化
- 批准号:
25460203 - 财政年份:2013
- 资助金额:
$ 2.3万 - 项目类别:
Grant-in-Aid for Scientific Research (C)
Relation between the efficacy and the activity of transporters ofnucleoside analogue
核苷类似物转运蛋白功效与活性的关系
- 批准号:
19590135 - 财政年份:2007
- 资助金额:
$ 2.3万 - 项目类别:
Grant-in-Aid for Scientific Research (C)