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hmily601木虫 (正式写手)
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[求助]
帮忙翻译下啊（有机化学）
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| Amphotericin B is the archetype for small molecules that form transmembrane ion channels. However, despite extensive study for more than five decades, even the most basic features of this channel structure and its contributions to the antifungal activities of this natural product have remained unclear. We herein report that a powerful series of functional group-deficient probes have revealed many key underpinnings of the ion channel and antifungal activities of amphotericin B. Specifically, in stark contrast to two leading models, polar interactions between mycosamine and carboxylic acid appendages on neighboring amphotericin B molecules are not required for ion channel formation, nor are these functional groups required for binding to phospholipid bilayers. Alternatively, consistent with a previously unconfirmed third hypothesis, the mycosamine sugar is strictly required for promoting a direct binding interaction between amphotericin B and ergosterol. The same is true for cholesterol. Synthetically deleting this appendage also completely abolishes ion channel and antifungal activities. All of these results are consistent with the conclusion that a mycosamine-mediated direct binding interaction between amphotericin B and ergosterol is required for both forming ion channels and killing yeast cells. The enhanced understanding of amphotericin B function derived from these synthesis-enabled studies has helped set the stage for the more effective harnessing of the remarkable ion channel-forming capacity of this prototypical small molecule natural product. |
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【答案】应助回帖
★ ★
Mally89(金币+2): 感谢应助！~欢迎常来！~O(∩_∩)O~ 2011-06-17 20:25:06
hmily601(金币+30, 翻译EPI+1): 辛苦了啊！！ 2011-06-17 20:50:22
Mally89(金币+2): 感谢应助！~欢迎常来！~O(∩_∩)O~ 2011-06-17 20:25:06
hmily601(金币+30, 翻译EPI+1): 辛苦了啊！！ 2011-06-17 20:50:22
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两性霉素B是那些形成跨膜离子通道的小分子的原型，然而，尽管广泛的研究了五十多年，但是这种通道结构的最基本特征以及该天然产物的对抑菌活性的贡献仍不是很清楚。在此我们报道了一个强大官能团缺失的探测器系列，该系列揭示了两性霉素B抑菌活性和离子通道的许多关键基础。特别的是附属于邻近两性霉素B分子上的mycosamine（胺）和羧酸之间的极性相互作用不需要离子通道的形成，这与两个领 先模型是完全相反的，这些官能团也不需要绑定到磷脂双分子层上。或者与早先未证明的第三个假设是一致的，mycosamine（胺）糖在促进麦角甾醇和两性霉素B直接结合互动中是必须的，同样对胆固醇也是这样的。以合成方法拆除这种附属物也能彻底地丧失其离子通道和抑菌活性，所有的这些与得到的结论是一致的，结论是在麦角甾醇和两性霉素B以mycosamine（胺）为媒介的直接结合互动中需要形成离子通道并杀死酵母细胞。关于两性霉素B官能化的进一步理解来自于这些合成功能研究，合成功能研究为这些典型的天然产物小分子更有效地利用异常离子通道形成能力提供了平台。 |
2楼2011-06-17 16:42:19