An aminocyclitol antibiotic
Spectinomycin is an aminocyclitol antibiotic produced by S. spectabilis with activity against gram-negative bacterial species. Spectinomycin has been used for the treatment of gonorrhea, where it inhibits microbial protein synthesis by binding to the 30S ribosomal subunit, protects the N‐7 position of E. coli 16S rRNA residue G1064 from methylation by dimethyl sulfate. Binding of spectinomycin at this location is thought to stabilize helix 34, inhibiting the binding of elongation factor G, thereby blocking translocation of peptidyl‐tRNAs from the ribosomal A site to the P site [1].
Spectinomycin selectively inhibited protein synthesis in cells and in extracts of E. coli. Mutations to high-level resistance to this antibiotic map close to the streptomycin locus, and the site of action of spectinomycin, like that of streptomycin, is the 30S ribosomal subunit, as shown by experiments with reconstituted 70S ribosomes containing subunits from sensitive and from resistant ribosomes [2].
链霉素素霉素是一种由观赏链霉菌产生的氨基环醇类抗生素，对革兰氏阴性细菌有活性。链霉素素霉素已被用于治疗淋病，它通过与30S核糖体亚基结合抑制微生物蛋白质合成，并保护大肠杆菌16S rRNA上G1064核苷酸的N-7位置不被二甲基硫酸甲基化。链霉素素霉素结合于该位置被认为稳定了34号螺旋，从而抑制了伸长因子G的结合，阻止了肽-tRNA从核糖体A位点转移到P位点[1]。
链霉素素霉素选择性地抑制了大肠杆菌细胞和提取物中的蛋白质合成。对该抗生素高水平抗性的突变位点与链霉素位点相邻，链霉素素霉素的作用位点与链霉素相同，均为30S核糖体亚基。这一点已通过含有敏感和耐药核糖体亚基的重组70S核糖体的实验得到证实[2]。
参考文献:
[1] Zimmerman J M, Maher L J.? In vivo selection of spectinomycin‐binding RNAs[J]. Nucleic acids research, 2002, 30(24): 5425-5435.
[2] Davies J, Anderson P, Davis B D.? Inhibition of protein synthesis by spectinomycin[J]. Science, 1965, 149(3688): 1096-1098.
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Animal experiment: |
Rats: Spectinomycin (10 mg/kg) is administered intravenously to rats. Serial blood samples (approx. 250 μL) are collected pre-dose, and at 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 4.0, 6.0, 8.0, 12.0, 24.0, 36.0 and 48.0 h post-dose. Plasma is separated immediately by centrifugation (10,000g for 5 min at 4°C) and stored at ?80°C until analysis. Urine samples are collected at an interval of 0-6, 6-12, 12-24, 24-36 and 36-48 h post-dose and stored at ?80°C until analysis[4]. |
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参考文献: [1]. Davies J, et al. Inhibition of protein synthesis by spectinomycin. Science. 1965 Sep 3;149(3688):1096-8. |
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