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本文报告国产青霉烷砜、进口青霉烷砜及克拉维酸对13种β-内酰胺酶的抑酶作用比较.以氨苄青霉素为底物,测定了当这种酶抑制剂存在与不存在时,β-内酰胺酶对氨苄青霉素的水解作用.结果表明: (1)各种β-内酰胺酶对氨苄青霉素均有不同程度的水解作用,水解率约在50～100%;(2)国产及进口青霉烷砜、克拉维酸对13种革蓝氏阴性杆菌产生的β-内酰胺酶,除个别酶外,均有明显的抑制作用,浓度为1μg/ml时,对β-内酰胺酶的抑酶率分别为0～82.18%、0～80.08%和6.00～97.5%;浓度为10μg/ml时,抑酶率则分别为5.50～100%、9.76～100%和19.57～100%;(3)国产青霉烷砜及进口青霉烷砜对β-内酰胺酶的抑酶率经统计学检验,无显著差异,提出以氨苄青霉素为底物时两者对β-内酰胺酶的抑制作用相仿.但两者除对TEM-1和P-99酶的抑酶作用大于克拉维酸外,对其余β-内酰胺酶的抑制作用均小于或接近于克拉维酸.本实验结果显示青霉烷砜具有良好的抑制作用,提示了氨苄青霉素与青霉烷砜联合对氨苄青霉素耐药菌株可产生协同抗菌作用.
This paper reports the comparison of aprotinin inhibition of 13 β-lactamases produced by domestic penicillins, penicillins and clavulanic acid.Using ampicillin as a substrate, (1) All kinds of β-lactamase had different degree of hydrolysis to ampicillin, the hydrolysis rate was about 50 ~ 100%; (2) Domestic and imported penicillins, clavulanic acid on 13 kinds of gram-negative bacteria produced by β-lactamase, in addition to individual enzymes, were significantly inhibited at a concentration of 1μg / ml, β-endo The inhibition rates of amidase were 0 ~ 82.18%, 0 ~ 80.08% and 6.00 ~ 97.5%, respectively. The inhibition rates of amidase were 5.50 ~ 100%, 9.76 ~ 100% and 19.57 ~ 100% at the concentration of 10μg / ; (3) domestic penicillin sulfone and imported penicamyl sulfone on β-lactamase inhibition rate by the statistical test, no significant difference, put ampicillin as a substrate for both β-lactamase The inhibitory effects on the other β-lactamases were both less than or close to that of clavulanic acid Acid dimension. The results suggest that penicillanic sulfone having good inhibitory effect, suggesting ampicillin and penicillanic sulphoxide combined ampicillin resistant strains may produce synergistic antibacterial effect.