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首页> 外文期刊>Chemistry: A European journal >Structure-Activity Relationships in Cholapod Anion Carriers: Enhanced Transmembrane Chloride Transport through Substituent Tuning
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Structure-Activity Relationships in Cholapod Anion Carriers: Enhanced Transmembrane Chloride Transport through Substituent Tuning

机译：藻类阴离子载体中的结构-活性关系：通过取代基调节增强跨膜氯化物运输。

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摘要

Chloride transport by a series of steroid-based "cholapod" receptors/carriers was studied in vesicles. The principal method involved preincorporation of the cholapods in the vesicle membranes. and the use of lucigenin fluorescence quenching to detect inward-transported Cl-. The results showed a partial correlation between anion affinity and transport activity, in that changes at the steroidal 7 and 12 positions affected both properties in concert. However. changes at the steroidal 3-position yielded irregular effects. Among the new steroids investigated the bis-p-nitrophenylthiourea 3 showed unprecedented activity, giving measurable transport through membranes with a transporter/lipid ratio of 1:250000 (an average of <2 transporter molecules per vesicle). Increasing transporter lipophilicity had no effect, and positively charged steroids had low activity. The p-nitrophenyl monourea 25 showed modest but significant activity. Measurements using a second method, requiring the addition of transporters to preformed vesicle suspensions, implied that transporter delivery was problematic in some cases. A series of measurements employing membranes of different thicknesses provided further evidence that the cholapods act as mobile anion carriers.
机译：在囊泡中研究了一系列基于类固醇的“胆足动物”受体/载体的氯化物转运。主要方法包括将胆囊细胞预先掺入囊泡膜中。以及使用光泽精蛋白荧光猝灭检测向内运输的Cl-。结果显示，阴离子亲和力和转运活性之间存在部分相关性，因为甾体7位和12位的变化会同时影响两个特性。然而。甾体3位的变化产生不规则的影响。在研究的新类固醇中，双-对硝基苯基硫脲3表现出空前的活性，可通过转运蛋白/脂质比率为1：250000的膜进行可测量的转运（每个囊泡平均<2个转运蛋白分子）。转运蛋白亲脂性的增加没有作用，带正电荷的类固醇的活性较低。对硝基苯基单脲25显示适度但显着的活性。使用第二种方法进行的测量需要在预先形成的囊泡悬浮液中添加转运蛋白，这暗示着在某些情况下转运蛋白的运送存在问题。使用不同厚度的膜进行的一系列测量提供了进一步的证据，表明该脉足动物充当了可移动的阴离子载体。

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