MECHANISM OF BREFELDIN A ACTION

Brefeldin A(BFA)是一种真菌代谢物，具有广泛的 生物活性，包括抗真菌和抗肿瘤 活动。在过去的几年里，人们对此产生了巨大的兴趣 在它对细胞的影响上，因为它被发现具有独特的 干扰囊泡运输的能力。在它的影响中， 它有能力驱散高尔基情结，至少返回 它的一些成分进入内质网(ER)。博鳌亚洲论坛还 阻止新合成的蛋白质进入细胞表面 离开急诊室。为了更好地理解博鳌亚洲论坛的作用机制，我们 将其与两种荧光染料偶联，并研究其胞内情况 本地化。这两种结合物都保持了它们的生物活性， 两者都专门定位于活体或 乙醛固定细胞。与细胞内膜的相互作用是 可能是由于与脂类的相互作用，因为它被洗涤剂消除了 提取脂类。这些偶联物是第一批结合在一起的染料 内质网和高尔基复合体不结合其他突出的膜结合 作为这些细胞器的探针，应该是有用的 在活细胞中。它们对固定细胞内质网染色的能力将是 在细胞化学研究中作为ER的标记物有很大用处。最后， BFA与ER和GC膜的相互作用可能是至关重要的 它的生物活性。

Brefeldin A (BFA) is a fungal metabolite with a broad range of biological activities, including the anti-fungal and anti-tumor activities. In the past few years there has been tremendous interest in its effect on cells, since it has been found to have the unique ability to interfere with vesicular trafficking. Among its effects, it has the ability to disperse the Golgi complex, returning at least some of its components to the endoplasmic reticulum (ER). BFA also prevents newly synthesized proteins destined for the cell surface from leaving the ER. To better understand the mechanism of BFA action we conjugated it to two fluorescent dyes and studied its intracellular localization. Both conjugates maintained their biological activity, and both specifically localized to the ER and Golgi complex in live or aldehyde-fixed cells. The interaction with intracellular membranes is probably due to interaction with lipids as it is abolished by detergent extraction of lipids. These conjugates are the first dyes that bind the ER and Golgi complex without binding other prominent membrane bound compartments and should prove useful as probes for the these organelles in living cells. Their ability to stain the ER of fixed cells will be of great use as markers of the ER in cytochemical studies. Finally, the interaction of BFA with the ER and GC membranes might be critical to its biological activity.