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本文报告17种头孢菌素对11种β-内酰胺酶的稳定性比较。实验用Nitrocefin作为底物,以紫外分光光度法测定11种β-内酰胺酶的活性;同时以紫外分光光度法测定11种β-内酰胺酶对17种头孢菌素的相对水解率。实验结果表明,二种染色体介导的酶D-31、K-1的活性为高,分别为22.00μ/ml和145.00μ/ml,9种质粒介导的酶的活性为0.41～17.40μ/ml。在第一代头孢菌素中,环己烯头孢菌素对大多数酶稳定,其余则对不同种酶的稳定性差异很大。除羟苄四唑头孢菌素和氧哌羟苯唑头孢菌素外,所有受试的第二代和第三代头孢菌素对大多数酶均非常稳定。各种头孢菌素类抗生素对不同类型β-内酰胺酶的稳定性可作为新药筛选的指标之一。
This article reports the stability of 17 cephalosporins against 11 β-lactamases. Nitrocefin was used as a substrate to determine the activity of 11 kinds of β-lactamases by UV spectrophotometry. Meanwhile, the relative hydrolysis rate of 11 kinds of β-lactamases to 17 kinds of cephalosporins was determined by UV spectrophotometry. The experimental results showed that the activities of two kinds of chromosome-mediated enzymes D-31 and K-1 were high, which were 22.00μ / ml and 145.00μ / ml respectively. The activity of the 9 plasmid-mediated enzymes was 0.41 ~ 17.40μ / ml. In the first-generation cephalosporins, cyclohexene cephalosporins are stable to most enzymes, while others have very different stability to different enzymes. All tested 2nd and 3rd generation cephalosporins were very stable to most enzymes except for cefepime and oxymetiphone cephalosporins. Various cephalosporins antibiotics for different types of β-lactamase stability can be used as a new drug screening indicators.