• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Harmful Algae >Permeability of dihydro- and cysteine-brevetoxin metabolites across a Caco-2 cell monolayer
【24h】

Permeability of dihydro- and cysteine-brevetoxin metabolites across a Caco-2 cell monolayer

机译：跨Caco-2细胞单层的二氢和半胱氨酸短毒素毒素代谢物的渗透性

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

Brevetoxin B is a highly reactive molecule, due in part to an α,β-unsaturated aldehyde group at the terminal side chain, leading to metabolism by reduction, oxidation and conjugation. These reactions have little effect to reduce intrinsic activity at the voltage-gated sodium channel or during toxicity testing by either enzyme-linked immunosorbent assay or mouse bioassay. Here we investigate the potential for intestinal absorption of the two most abundant brevetoxins present in Gulf of Mexico oysters using human Caco-2 cell monolayers, a widely utilized in vitro test to predict oral bioavailability of drugs and their metabolites. We found that both dihydrobrevetoxin B and cysteine brevetoxin B were rapidly taken up by the Caco-2 monolayer. However, only dihydrobrevetoxin B passes through the monolayer to reach the basal compartment. Dihydrobrevetoxin B has a moderate apparent permeability coefficient of 1.6× 10~(-6) cm/s at 500 ng/mL and nearly 50% of the toxin passes from the apical to basal compartment in 24 h. The inability of the cysteine brevetoxin B to pass through an intestinal epithelial barrier suggests that this bioactive brevetoxin metabolite that persists in shellfish may not contribute to neurotoxic shellfish poisoning.
机译：短毒素B是一种高反应性分子，部分归因于末端侧链上的α，β-不饱和醛基，可通过还原，氧化和结合而导致新陈代谢。这些反应对通过电压连锁的钠通道或通过酶联免疫吸附测定或小鼠生物测定进行的毒性测试在降低内在活性方面几乎没有影响。在这里，我们使用人Caco-2细胞单层膜调查了存在于墨西哥湾牡蛎中的两种最丰富的短肠毒素在肠道上的吸收潜力，这种单层膜被广泛用于体外测试以预测药物及其代谢产物的口服生物利用度。我们发现Caco-2单层迅速吸收了二氢短肌毒素B和半胱氨酸短毒素B。但是，只有二氢小肠毒素B穿过单层到达基底腔室。二氢短杆菌毒素B在500 ng / mL时具有中等的表观渗透系数，为1.6×10〜（-6）cm / s，并且在24小时内近50％的毒素从根尖传递到基底腔。半胱氨酸短毒素B无法通过肠道上皮屏障，这表明这种在贝类中持续存在的生物活性短毒素毒素代谢产物可能不会导致神经毒性贝类中毒。

著录项

  • 来源
    《Harmful Algae》 |2014年第2期|22-26|共5页
  • 作者

    Jerome Henri; Tod A. Leighfleld; Rachelle Lanceleur; Antoine Huguet; John S. Ramsdell; Valerie Fessard;

  • 作者单位

    ANSES - French Agency for Food, Environmental and Occupational Health & Safety, Fougeres Laboratory, 8 rue Claude Bourgelat BP 90203,35302 Fougeres cedex, France,ANSES - Fougeres Laboratory, 10B rue Claude Bourgelat BP 90203, 35302 Fougeres cedex, France;

    Marine Biotoxins Program, Center for Coastal Environmental Health and Biomolecular Research, NOAA National Ocean Service, 219 Fort Johnson Road, Charleston, SC 29412, USA;

    ANSES - French Agency for Food, Environmental and Occupational Health & Safety, Fougeres Laboratory, 8 rue Claude Bourgelat BP 90203,35302 Fougeres cedex, France;

    ANSES - French Agency for Food, Environmental and Occupational Health & Safety, Fougeres Laboratory, 8 rue Claude Bourgelat BP 90203,35302 Fougeres cedex, France;

    Marine Biotoxins Program, Center for Coastal Environmental Health and Biomolecular Research, NOAA National Ocean Service, 219 Fort Johnson Road, Charleston, SC 29412, USA;

    ANSES - French Agency for Food, Environmental and Occupational Health & Safety, Fougeres Laboratory, 8 rue Claude Bourgelat BP 90203,35302 Fougeres cedex, France;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

    Brevetoxin; Metabolites; Caco-2; Intestinal permeability;

    机译：短毒素;代谢物Caco-2;肠通透性;

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