• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>The Veterinary Journal >Effects of triclabendazole on secretion of danofloxacin and moxidectin into the milk of sheep: role of triclabendazole metabolites as inhibitors of the ruminant ABCG2 transporter.
【24h】

Effects of triclabendazole on secretion of danofloxacin and moxidectin into the milk of sheep: role of triclabendazole metabolites as inhibitors of the ruminant ABCG2 transporter.

机译：三氯苯达唑对绵羊乳中达氟沙星和莫昔克丁分泌的影响：三氯苯达唑代谢物作为反刍动物ABCG2转运蛋白抑制剂的作用。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

ATP-binding cassette transporter G2/breast cancer resistance protein (ABCG2/BCRP) mediates drug-drug interactions that affect the secretion of drugs into milk. The aims of this study were: (1) to determine whether the major plasma metabolites of the flukicide triclabendazole (TCBZ), triclabendazole sulfoxide (TCBZSO) and triclabendazole sulfone (TCBZSO2), inhibit ovine and bovine ABCG2 and its Y581S variant in vitro, and (2) to examine whether coadministration of TCBZ with the ABCG2 substrates danofloxacin (a fluoroquinolone) and moxidectin (a milbemycin) affects the secretion of these drugs into the milk of sheep. TCBZSO and TCBZSO2 inhibited ruminant ABCG2 in vitro by reversing the reduced mitoxantrone accumulation and reducing basal to apical transport of nitrofurantoin in cells transduced with bovine variants (S581 and Y581) and the ovine variant of ABCG2. Coadministration of TCBZ with moxidectin or danofloxacin to sheep resulted in significantly reduced levels of moxidectin, but not danofloxacin, in the milk of TCBZ-treated sheep compared to sheep administered moxidectin or danofloxacin alone. The milk area under concentration time curve (AUC 0-48 h) was 2.99+or-1.41 micro g h/mL in the group treated with TCBZ and moxidectin, and 7.75+or-3.58 micro g h/mL in the group treated with moxidectin alone. The AUC (0-48 h) milk/plasma ratio was 37% lower in the group treated with TCBZ and moxidectin (7.34+or-1.51) than in the group treated with moxidectin alone (11.68+or-3.61). TCBZ metabolites appear to inhibit ruminant ABCG2 and affect the secretion of ABCG2 substrates into milk of sheep.
机译：ATP结合盒转运蛋白G2 /乳腺癌抗性蛋白（ABCG2 / BCRP）介导影响药物向牛奶分泌的药物相互作用。这项研究的目的是：（1）确定杀菌剂三氯苯达唑（TCBZ），三氯苯达唑亚砜（TCBZSO）和三氯苯达唑砜（TCBZSO 2 ）的主要血浆代谢物是否抑制绵羊和牛ABCG2 （2）检查TCBZ与ABCG2底物达氟沙星（一种氟喹诺酮）和莫昔克丁（一种米尔贝霉素）的共同给药是否影响这些药物向羊奶中的分泌。 TCBZSO和TCBZSO 2 在体外抑制反刍动物ABCG2，其方法是逆转减少的米托蒽醌积累，并减少转导牛变体（S581和Y581）和ABCG2的绵羊变体的细胞中呋喃妥因的基础至顶端转运。与单独施用莫昔克丁或单氧氟沙星的绵羊相比，将TCBZ与莫昔克丁或达氧氟沙星共同施用给绵羊可导致经TCBZ处理的绵羊的牛奶中的莫昔菌素（而非达氟沙星）水平显着降低。浓缩时间曲线下的牛奶面积（AUC 0-48 h）在TCBZ和莫昔克丁治疗组中为2.99+或-1.41 micro gh / mL，单独莫昔克丁治疗组为7.75+或-3.58 micro gh / mL 。 TCBZ和莫昔克丁治疗组（7.34+或-1.51）的AUC（0-48 h）牛奶/血浆比率比单独莫昔克丁治疗组（11.68+或-3.61）低37％。 TCBZ代谢物似乎抑制反刍动物ABCG2，并影响ABCG2底物向绵羊乳中的分泌。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号