生物活性 | |||
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描述 | Cephalosporin C zinc salt is a potent inhibitor of SAMHD1 (Sterile alpha motif and histidine-aspartate domain-containing protein 1) with an IC50 of 1.1 ± 0.1 μM, 200-fold more potent than Na+ salt form of Cephalosporin C (ICC50CC-Na = 213 ± 30 μM). Cephalosporin C zinc salt is an antibiotic used to study the effect of transpeptidase expression, binding, and inhibition on bacterial cell wall mucopeptide synthesis. Cephalosporin C zinc salt, as is expected of a Cephalosporin, will disrupt the synthesis of the peptidoglycan layer of bacterial cell walls[2]. A loss in activity of the zinc-activated enzyme which occurred on prolonged hydrolysis of cephalosporin C was not restored by further addition of zinc[3]. The minimum inhibitory concentration of cephalosporin C(A) (pyridine) upon penicillinase-producing staphylococci increased 4 to 8-fold with a 500-fold increase in inoculum size; with cephalosporin C there was a 2-fold increase. Cephalosporin C(A) (pyridine) was about 8 times more active than cephalosporin C in protecting mice from an experimental streptococcal infection, nine doses of 6.25 mg/kg affording complete protection[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.09mL 0.42mL 0.21mL |
10.44mL 2.09mL 1.04mL |
20.89mL 4.18mL 2.09mL |
参考文献 |
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