Grace M E, Fu K P, Gregory F J, Hung P P
Drugs Exp Clin Res. 1987;13(3):145-8.
The inhibitory effects of clavulanic acid, sulbactam and cephamycin antibiotics on chromosomally-mediated or plasmid-mediated beta-lactamases were investigated. The inhibition constants were determined by a non-linear regression analysis. Clavulanic acid and sulbactam had high affinities for the purified plasmid-mediated beta-lactamases such as SHV-1, TEM-1 and PSE-4, and were potent inhibitors as shown by their low Ki values. Except for Bacteroides beta-lactamase, which is sensitive to inhibition by cephamycin antibiotics, clavulanic acid and sulbactam were found not to be as effective against chromosomally-mediated beta-lactamases. The cephamycin antibiotics were better inhibitors of chromosomally-mediated beta-lactamases than those that are plasmid mediated. Except for P99 beta-lactamase, against which sulbactam and clavulanic acid were inactive, the cephamycin antibiotics were less effective inhibitors than sulbactam and clavulanic acid.
研究了克拉维酸、舒巴坦和头孢霉素类抗生素对染色体介导或质粒介导的β-内酰胺酶的抑制作用。通过非线性回归分析确定抑制常数。克拉维酸和舒巴坦对纯化的质粒介导的β-内酰胺酶如SHV-1、TEM-1和PSE-4具有高亲和力，并且如它们的低Ki值所示是强效抑制剂。除了对头孢霉素类抗生素抑制敏感的拟杆菌β-内酰胺酶外，发现克拉维酸和舒巴坦对染色体介导的β-内酰胺酶的效果不佳。头孢霉素类抗生素对染色体介导的β-内酰胺酶的抑制作用优于质粒介导的β-内酰胺酶。除了舒巴坦和克拉维酸对其无活性的P99β-内酰胺酶外，头孢霉素类抗生素作为抑制剂的效果不如舒巴坦和克拉维酸。
