卡那霉素 kanamycin - PubMed 文献
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关于 卡那霉素
卡那霉素（kanamycin）是一种氨基糖苷类抗生素（aminoglycoside antibiotic），由卡那霉素链霉菌产生，主要通过抑制细菌蛋白质合成发挥杀菌作用。其作用机制为不可逆地结合细菌30S核糖体亚基，干扰mRNA翻译的起始和延伸过程。临床上主要用于治疗革兰阴性菌感染，如大肠杆菌、克雷伯菌、变形杆菌等所致呼吸道、泌尿道、腹腔及软组织感染，也用于结核病的二线治疗。在分子生物学研究中，卡那霉素抗性基因（kanamycin resistance gene）常作为筛选标记用于质粒构建和基因工程。该概念属于药理学、微生物学及感染病学交叉领域。中文常称卡那霉素，英文同义词包括 kanamycin A、kanamycin sulfate 等。
卡那霉素相关研究热点涵盖多个方向：细菌耐药机制（如氨基糖苷修饰酶、16S rRNA甲基化酶）、新型氨基糖苷类衍生物的开发与结构优化、卡那霉素在结核病联合治疗方案中的定位、耳毒性与肾毒性等不良反应的分子基础及防护策略。经典议题还包括卡那霉素抗性基因在环境微生物和临床病原体中的传播规律，以及其作为基因工程筛选标记的适用性改进。代表性期刊包括 Antimicrobial Agents and Chemotherapy、Journal of Antimicrobial Chemotherapy、Antimicrobial Resistance and Infection Control 等。学者如 Wright、Davies 等在氨基糖苷类抗生素耐药领域有长期贡献。
PubMed增强版为关注卡那霉素的研究者提供多项实用功能：支持中英文摘要对照翻译，帮助快速理解非母语文献；显示期刊影响因子与分区信息，辅助评估文献学术影响力；提供原文PDF下载链接，便于获取全文；集成AI阅读工具，可自动提炼研究要点、方法与结论，提升文献调研效率。这些功能有助于从大量卡那霉素相关文献中高效筛选关键信息，覆盖临床、药理及分子生物学等多学科需求。
卡那霉素 的 PubMed 搜索结果
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Crystal structure, conformation, and absolute configuration of kanamycin A. 卡那霉素A的晶体结构、构象和绝对构型
Kanamycin, an antibiotic complex produced by Streptomyces kanamycetius isolated from Japanese soil, was described by Okami and Umezawa as early as 1957 and consists of three components: Kanamycin A (the major component), B, and C. The disulfate salt of kanamycin A [4-O-(6-amino-6-deoxy-alpha-d-glucopyranosyl)-6-O-(3-amino-3-deoxy-alpha-d-glucopyranosyl)-2-deoxystreptamine] is a broad-spectrum antibiotic that is used to treat gonorrhea, salmonella, tuberculosis, and many other diseases. Crystals of kanamycin A monosulfate monohydrate obtained from water are triclinic, space group P1, with a=7.2294(14), b=12.4922(15), c=7.1168(9), alpha=94.74(1), beta=89.16(1), gamma=91.59(1), V=640.2(2)A(3), micro(CuKalpha)=18.4cm(-1), FW 600.6, D(calc)=1.558g/cm(3), CAD-4 diffractometric data (2693 reflections, 25543sigma(I)), structure by shelx-86 and refined by full-matrix least squares to a final R value of 0.038. The wrong conformer had an R value of 0.043. Both of the d-glucose moieties are attached to the deoxystreptamine by alpha linkages. This absolute configuration agrees with the earlier determination by both chemical and X-ray methods with photographic data. The (phi,psi) values for the glycosidic linkages are 101.6 degrees , -121.1 degrees , 106.3 degrees , and -140.4 degrees , respectively. Kanamycin interacts with the ribosomal S12 protein to stabilize the codon-anticodon binding between mRNA and the aminoacyl tRNA and inhibits the elongation of peptide chains through a series of reactions resulting in the prevention of ribosomes from moving along mRNA.
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Cloning, overexpression, and purification of aminoglycoside antibiotic 3-acetyltransferase-IIIb: conformational studies with bound substrates. 氨基糖苷类抗生素3-乙酰转移酶-IIIb的克隆、过表达和纯化：与结合底物的构象研究
Aminoglycoside 3-acetyltransferase-IIIb (AAC3), which acetylates N3 amine of aminoglycoside antibiotics, was cloned from P. Aeruginosa and purified from overexpressing E. coli BL21 (DE3) cells. Bound conformations of kanamycin A and ribostamycin, in the active site of the enzyme that modifies the essential N3B of aminoglycoside antibiotics, were determined by NMR spectroscopy. Experimentally determined interproton distances were used in a simulated annealing protocol to determine enzyme-bound conformations of both antibiotics. Two conformations, consistent with the NOE restraints, were determined for ribostamycin. The only difference between the two conformers was the orientation of the A ring with respect to the rest of the molecule. The average glycosidic dihedral angles were Phi(1A) = -22 degrees +/- 3 and Psi(1A) = -42 degrees +/- 1 (conformer 1) and Phi(1A) = -67 degrees +/- 0.7 and Phi(1A) = -59 degrees +/- 0.8 (conformer 2). Three conformers were determined for the enzyme-bound kanamycin A. Two conformers of kanamycin A were matched well with the two conformers of ribostamycin when the A and the B rings of the antibiotics were superimposed. Conformations of kanamycin A and ribostamycin were compared to those of other aminoglycosides that are bound to different enzymes and RNA. The results lend further support to our earlier hypothesis that the A and B rings of aminoglycosides adopt a conformation that is recognized not only by the aminoglycoside-modifying enzymes but also by RNA (Serpersu, E. H., Cox, J. R., Digiammarino, E. L., Mohler, M. L., Akal, A., Ekman, D. R., and Owston, M. (2000) Cell Biochem. Biophys. 33, 309-321). These results may be useful in designing new antibiotics to combat the antibiotic resistance against infectious diseases.
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[Effect of aminoglycosides on experimentally induced endolymphatic hydrops]. [氨基糖苷类药物对实验性诱发内淋巴积水的影响]
Gentamycin or kanamycin have no effect on endolymph formation in experimental induced endolymphatic hydrops. The increase of endolymphatic volume after obliteration of endolymphatic duct and sac is not influenced by aminoglycosides as well as the decrease of DC-potential and the increase of sodium-activity in endolymphatic hydrops. The way of action of intratympanal injected gentamycin seems to be in a partial chemical induced labyrinthectomy.
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Denaturation map of the ColE1-Km plasmid pCR11. ColE1-Km质粒pCR11的变性图谱
The denaturation map of EcoRI-digested pCR11, a ColE1-Km plasmid, is described. The 2.0 kilobase ColE1-derived segment contains an adenine+thymine rich site in the colicin immunity gene region. In the 7.2 kilobase kanamycin resistance region, the transposon Tn903 consists of an adenine+thymine rich 0.98 kilobase kan gene region flanked by a guanine+cytosine rich 1.09 kilobase inverted duplication.
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Detection of R plasmids in naturally occurring fish-pathogenic bacteria, Edwardsiella tarda. 自然发生的鱼类致病菌——迟钝爱德华氏菌中R质粒的检测
The conjugative R plasmids were detected from fish-pathogenic Edwardsiella tarda isolated from cultured eels. These R plasmids were resistant to sulfonamide and tetracycline, or sulfonamide, streptomycin, chloramphenicol, tetracycline and kanamycin. There were no inhibitions in growth of phages W-31, P1, T1, T3, T7, and lambda. They were classified into incompatibility group A.
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[Physicochemical properties of some antibiotics]. [某些抗生素的理化性质]
Some physico-chemical properties of 3 antibiotics, i.e. kanamycin, neomycin and monomycin dried in the evaporating-drying apparatus IDA-ITE-6 constructed at the Institute of Technical Thermophysics of the UkSSR Academy of Sciences were studied. The properties of their 6 and 18 percent solutions and sorption properties of the antibiotic powders were described. It was found that the properties of the 3 antibiotics were close.
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Clearence of antibiotics from the intestines after termination of antibiotic decontamination. 抗生素脱污终止后肠道中抗生素的清除
The clearance of neomycin and kanamycin from the intestines after stopping oral supply has been determined in mice. Both antibiotics, although given in different doses, were excreted in essentially the same way; the clearance being a little faster than logarithmically in both cases. The importance of this observation with regard to isolation and the moment of reconventionalization is discussed.
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The relationship between the cytotoxicity of kanamycin and ethacrynic acid for mammalian cells in vitro and their ototoxicity in vivo. 卡那霉素和依他尼酸对体外哺乳动物细胞的细胞毒性与体内耳毒性之间的关系
Dose-effect curves for inhibition of growth of P388/P mouse lymphoma cells by ethacrynic acid and kanamycin used alone and in combination were determined in vitro. Ethacrynic acid was 600 times more potent than kanamycin and combinations of the drugs resulted in overall additive effects. These results were compared with known dose-effect data on the ototoxicity of these drugs in vivo. Kanamycin was highly selective in its toxicity for cochlear hair cells compared to cultured cells. The dose-effect data for ethacrynic acid was coincident with that reported for functional and biochemical effects on the cochlea following perilymphatic perfusion with the drug. The potentiation observed following the ototoxic interaction the two drugs in vivo was not observed following combinations of the drugs in vitro.
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Aminoglycoside ototoxicity in adult CBA, C57BL and BALB mice and the Sprague-Dawley rat. 成年CBA、C57BL和BALB小鼠及Sprague-Dawley大鼠中的氨基糖苷类耳毒性
The availability of genetic information, transgenic and knock-out animals make the mouse a primary model in biomedical research. Aminoglycoside ototoxicity, however, has rarely been studied in mature mice because they are considered highly resistant to the drugs. This study presents models for kanamycin ototoxicity in adult CBA/J, C57BL/6 and BALB/c mouse strains and a comparison to Sprague-Dawley rats. Five-week-old mice were injected subcutaneously twice daily with 400-900 mg kanamycin base/kg body weight for 15 days. Kanamycin induced dose-dependent auditory threshold shifts of up to 70 dB at 24 kHz as measured by auditory brain stem-evoked responses. Vestibular function was also affected in all strains. The functional deficits were accompanied by hair cell loss in both cochlear and vestibular neurosensory epithelia. Concomitant administration of the antioxidant 2,3-dihydroxybenzoate significantly attenuated the kanamycin-induced threshold shifts. In adult male Sprague-Dawley rats, doses of 1 x 500 mg or 2 x 300 mg kanamycin base/kg body weight/day x 14 days induced threshold shifts of approximately 50 dB at 20 kHz. These were accompanied by loss of outer hair cells. The order of susceptibility, BALB>CBA>C57, was not due to differences in the pharmacokinetics of kanamycin. It also did not correlate with the presence of Ahl/Ahl2 genes which predispose C57 and BALB strains, respectively, to accelerated age-related hearing loss. Pigmentation, however, paralleled this rank order suggesting an influence of melanin on cochlear antioxidant status.
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Enhancement of antimicrobial activity by synthetic ion channel synergy. 合成离子通道协同作用增强抗菌活性
Hydraphile synthetic ion channels were found to enhance the cytotoxicity to E. coli and B. subtilis of erythromycin, kanamycin, rifampicin, and tetracycline when co-administered with the antibiotic at sublethal concentrations of channel.