酶石墨烯氧化物相互作用:β-lactamases的案例系统
Alessandra Piccirilli1, Mariagrazia Perilli1, Fabrizia Brisdelli1
1Department of Biotechnological and Applied Clinical Sciences, University of L'Aquila L'Aquila Italy.
RSC advances
|June 24, 2025
概括
石墨烯氧化物 (GO) 有效抑制了血清酶和金属β-乳酸酶 (BLs). GO通过阳性残留物与BLs相互作用,显示出非竞争性抑制机制并影响基质结合.
科学领域:
- 生物化学 生物化学
- 材料科学 材料科学 材料科学
- 药物发现 药物发现 药物发现
背景情况:
- β-乳酸酶 (BLs) 是赋予抗生素耐药性的酶.
- 氧化石墨烯 (GO) 是一种具有潜在抗菌应用的新型纳米材料.
- 了解GO与BL的互动对于开发新的抗击突破策略至关重要.
研究的目的:
- 研究石墨烯氧化物 (GO) 对广泛的血清β-乳酸酶 (SBL) 和金属β-乳酸酶 (MBL) 的抑制作用.
- 为了阐明GO-BL相互作用的分子机制.
- 探索GO作为β-乳酸酶活性抑制剂的潜力.
主要方法:
- 使用尼特洛塞芬作为基质的剂量依赖性动力学测试.
- X射线光发射光谱 (XPS) 用于研究酶-GO相互作用.
- 密度函数理论 (DFT) 模型对酸-GO系统进行建模.
主要成果:
- 在低度 (0.5μg ml-1) 时,GO显示出对所有测试的SBL和MBL的强烈抑制.
- XPS分析显示,GO与MBLs通过带正电荷的残留物相互作用,而不是活性位点原子,表明非竞争性抑制.
- DFT 建模显示,GO 结合了酸基质,阻碍了它与酶的相互作用.
结论:
- 氧化石墨烯是各种β-乳酸酶的强有力的抑制剂.
- 抑制机制涉及与酶的非竞争性结合和与基质的直接相互作用.
- 在抗生素耐药性方面,GO是一种有前途的途径,可以通过β-lactamases调解抗生素耐药性.
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