可可链霉菌β-内酰胺酶的相互作用。I. 克拉维酸和PS-5。

Interaction of beta-lactamase of Streptomyces cacaoi. I. Clavulanic acid and PS-5.

作者信息

Ogawara H, Mantoku A

出版信息

J Antibiot (Tokyo). 1981 Oct;34(10):1341-6. doi: 10.7164/antibiotics.34.1341.

DOI:10.7164/antibiotics.34.1341

Abstract

Inactivation of a beta-lactamase of Streptomyces cacaoi by clavulanic acid and PS-5 was investigated and compared with that of a beta-lactamase of Bacillus cereus. Inhibition of the enzymes induced by clavulanic acid and the beta-lactam antibiotic PS-5 was found to be progressive with time. However, the degree of inhibition of the beta-lactamase from S. cacaoi increased more progressively with time than that of the enzyme from B. cereus. Conformative response constants were determined. As compared with clavulanic acid, over ten times higher concentrations of PS-5 were necessary to give a similar degree of inhibition. At lower concentrations, both clavulanic acid and PS-5 behaved as competitive inhibitors. Ki values calculated from the integrated form of the LINEWEAVER-BURK type were 1.1 X 10(-7) M and 7.6 X 10(-6) M for clavulanic acid and PS-5, respectively.

摘要

研究了棒酸和PS - 5对可可链霉菌β-内酰胺酶的灭活作用，并与蜡样芽孢杆菌的β-内酰胺酶进行了比较。发现棒酸和β-内酰胺抗生素PS - 5对酶的抑制作用随时间逐渐增强。然而，可可链霉菌β-内酰胺酶的抑制程度随时间的增加比蜡样芽孢杆菌的酶更显著。测定了构象反应常数。与棒酸相比，需要超过十倍浓度的PS - 5才能产生相似程度的抑制。在较低浓度下，棒酸和PS - 5均表现为竞争性抑制剂。根据LINEWEAVER - BURK类型的积分形式计算得到的棒酸和PS - 5的Ki值分别为1.1×10⁻⁷M和7.6×10⁻⁶M。