Soufer D
Microbios. 1986;45(184-185):193-8.
A bacterial strain exposed to penicillin may produce an extracellular enzyme called penicillinase which leaves the bacterial cell and degrades the penicillin around it by hydrolysing the cyclic amide bond in the beta-lactam ring of penicillin and thus inactivates the antibiotic. Experiments were conducted to find a competitive and a non-competitive inhibitor which could irreversibly inhibit the activity of penicillinase, allowing penicillin to destroy the bacterial strain. After testing many inhibitors some had synergistic, antagonistic or even no affect on the bacterial strain. The non-competitive inhibitor which had the best result was iodine, and the best competitive inhibitor in its group was sulphoxazole.
暴露于青霉素的细菌菌株可能会产生一种名为青霉素酶的细胞外酶,该酶离开细菌细胞,通过水解青霉素β-内酰胺环中的环状酰胺键来降解其周围的青霉素,从而使抗生素失活。进行了实验以寻找能够不可逆地抑制青霉素酶活性的竞争性和非竞争性抑制剂,使青霉素能够破坏该细菌菌株。在测试了许多抑制剂后,有些对该细菌菌株具有协同、拮抗甚至无影响。效果最佳的非竞争性抑制剂是碘,其同类中最佳的竞争性抑制剂是磺胺恶唑。