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首页> 外文期刊>BMC Microbiology >Emodin targets the β-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori: enzymatic inhibition assay with crystal structural and thermodynamic characterization
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Emodin targets the β-hydroxyacyl-acyl carrier protein dehydratase from Helicobacter pylori: enzymatic inhibition assay with crystal structural and thermodynamic characterization

机译：大黄素靶向幽门螺杆菌的β-羟酰基-酰基载体蛋白脱水酶：具有晶体结构和热力学特征的酶抑制试验

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Background The natural product Emodin demonstrates a wide range of pharmacological properties including anticancer, anti-inflammatory, antiproliferation, vasorelaxant and anti-H. pylori activities. Although its H. pylori inhibition was discovered, no acting target information against Emodin has been revealed to date. Results Here we reported that Emodin functioned as a competitive inhibitor against the recombinant β-hydroxyacyl-ACP dehydratase from Helicobacter pylori (HpFabZ), and strongly inhibited the growth of H. pylori strains SS1 and ATCC 43504. Surface plasmon resonance (SPR) and isothermal titration calorimetry (ITC) based assays have suggested the kinetic and thermodynamic features of Emodin/HpFabZ interaction. Additionally, to inspect the binding characters of Emodin against HpFabZ at atomic level, the crystal structure of HpFabZ-Emodin complex was also examined. The results showed that Emodin inhibition against HpFabZ could be implemented either through its occupying the entrance of the tunnel or embedding into the tunnel to prevent the substrate from accessing the active site. Conclusion Our work is expected to provide useful information for illumination of Emodin inhibition mechanism against HpFabZ, while Emodin itself could be used as a potential lead compound for further anti-bacterial drug discovery.
机译：背景天然产品大黄素具有广泛的药理特性，包括抗癌，抗炎，抗增殖，血管舒张和抗H。幽门活动。尽管发现了其抑制幽门螺杆菌的作用，但迄今为止尚未发现针对大黄素的作用靶标信息。结果在这里我们报道了大黄素起着针对幽门螺杆菌（HpFabZ）的重组β-羟酰基ACP脱水酶的竞争性抑制剂的作用，并强烈抑制了幽门螺杆菌SS1和ATCC 43504的生长。表面等离振子共振（SPR）和等温基于滴定热法（ITC）的测定表明大黄素/ HpFabZ相互作用的动力学和热力学特征。另外，为了在原子水平上检查大黄素与HpFabZ的结合特性，还检查了HpFabZ-大黄素复合物的晶体结构。结果表明，大黄素对HpFabZ的抑制作用可通过其占据通道的入口或嵌入通道中来实现，以防止底物进入活性位点。结论我们的工作有望为阐明大黄素对HpFabZ的抑制机制提供有用的信息，而大黄素本身可以用作进一步抗菌药物发现的潜在先导化合物。

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