卡那霉素 kanamycin - PubMed 文献(第 2 页)
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卡那霉素 的 PubMed 搜索结果(第 2 页)
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Kanamycin susceptibility testing of Mycobacterium tuberculosis using Mycobacterium Growth Indicator Tube and a colorimetric method. 使用分枝杆菌生长指示管和比色法对结核分枝杆菌进行卡那霉素敏感性检测
Two novel systems were evaluated for performing indirect kanamycin susceptibility tests on 72 strains of Mycobacterium tuberculosis. The microplate Alamar blue colorimetric method (breakpoint, 2.5 microg/ml) and the Mycobacterium Growth Indicator Tube (MGIT) system (breakpoint, 5.0 microg/ml) both produced 98.6% agreement when compared with the conventional proportion method performed on 7H10 agar using 5.0 microg of kanamycin/ml. Both systems provided results within an average of 1 week.
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[Studies on secondary derivative differential pulse polarography and its applications]. [二次导数示差脉冲极谱法及其应用研究]
Secondary derivative differential pulse polarography was developed and used for the quantitative analysis of ribostamycin sulfate, kanamycin and their preparations. By using sodium hydroxide-potassium dihydrogen phosphate solution as the base solution, ribostamycin sulfate and kanamycin showed good peaks at 0.105 V and -0.37 V (vs Ag/AgCl) respectively. The linear relationship of ribostamycin sulfate and kanamycin between concentration and peak height was obtained in the concentration range of 1.8-10.8 x 10(-4) mol/L and 3.1-18.6 x 10(-4) mol/L and the determination limit was 7.2 x 10(-9) mol/L and 4.6 x 10(-8) mol/L respectively. This method is simple, rapid and sensitive. The result is accurate.
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Integration specificity of an artificial kanamycin transposon constructed by the in vitro insertion of an internal Tn5 fragment into IS2. 通过将内部Tn5片段体外插入IS2构建的人工卡那霉素转座子的整合特异性
IS2 has been marked genetically by the in vitro insertion into its HindIII site of a 3.3 Kb HindIII fragment of Tn5 conferring resistance to kanamycin. The transposition of the IS2::Km, thus obtained, to lambda has been found and insertion sites were characterised. Each of ten independent IS2::Km insertions were found at the same site at 61.2% of the lambda map, always in the same orientation (orientation II relative to the xis gene). The integration sites of IS2::Km in five of the kanamycin-transducing phages were determined by DNA sequence analysis, and were found to be identical at the nucleotide level. Further transposition of IS2::Km from lambda to the bacterial chromosome was demonstrated.
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In vitro synergism between carbenicillin and aminoglycosidic aminocyclitols against Acinetobacter calcoaceticus var. anitratus. 羧苄西林与氨基糖苷类氨基环醇对乙酸钙不动杆菌不动杆菌变种的体外协同作用
Acinetobacter caleoaceticus var. anitratus is a nonfermentative, gram-negative bacillus that has been demonstrated to cause severe infections, usually in hospitalized patients. Since mild to moderate resistance of A. calcoaceticus to one or more aminoglycosidic aminocyclitols has been noted to occur, a study was undertaken to evaluate the activity of combinations of carbenicillin with either kanamycin, tobramycin, or gentamicin against 28 isolates of A. calcoaceticus obtained from clinical sources. Synergism (defined as at least 100-fold-increased killing at 24 h by the combination as compared with the most efficacious of the individual antibiotics) was demonstrated against 26 of 28 strains of A. calcoaceticus with carbenicillin plus kanamycin and carbenicillin plus tobramycin and against 25 of 28 strains with carbenicillin plus gentamicin. The median increased killing for the 28 strains was 4.2 log(10) with carbenicillin plus kanamycin and with carbenicillin plus tobramycin and 3.1 log(10) with carbenicillin plus gentamicin. The most important determinant of synergistic potential of each combination was the level of resistance of each strain of A. calcoaceticus to the aminoglycoside component of the combination.
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Kanamycin and its derivative, arbekacin: significance and impact. 卡那霉素及其衍生物阿贝卡星：意义与影响
On the occasion of the 60th anniversary of the discovery (1957) of kanamycin (KM), a series of research achievements on KM and its semisynthetic derivative Arbekacin (ABK) are outlined. KM was first used clinically in 1958 and was appreciated for its remarkable curing effect on various bacterial infections, especially tuberculosis. ABK is a KM derivative rationally semisynthesized to overcome KM resistance due to enzymatic phosphorylation and acetylation. Since its approval in 1990 as an anti-MRSA drug, ABK has been and still is effectively used in chemotherapy because MRSA rarely develops high ABK-resistance. Research that illuminated the unique features of ABK enabling it to resist the development of resistance by MRSA are also described.
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Synthesis of kanamycin-azole hybrids and investigation of their antifungal activities. 卡那霉素-唑类杂合物的合成及其抗真菌活性研究
The World Health Organization (WHO) recognizes Candida albicans and Cryptococcus neoformans as the critical priority fungal pathogens for which therapeutic solutions are needed. Azole-based antifungal agents, including triazoles, diazoles, and thiazoles, are widely used in the treatments for fungal infections. In light of past successes in the transformation of antibacterial kanamycin into antifungal derivatives via chemical modifications, a new library of kanamycin-azole hybrids was synthesized and tested against a panel of azole-resistant and susceptible Candida and Cryptococcus strains. Structure activity relationship (SAR) studies revealed pivotal roles for antifungal activity of the azole ring (imidazole vs triazole) and halogen substituents on the benzene ring (F vs Cl). Most notably, hybrids 13, 14 and 15 were active against resistant C. albicans, C. tropicalis and C. neoformans strains and non-toxic towards mammalian cells. Mode of action investigations using fluorogenic dyes, (SYTOX) showed the fungal active compounds could permeabilize fungal membranes even at ¼ MICs. These findings reveal novel azole-based antifungals that could offer new therapeutic options for candidiasis and cryptococcosis.
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Clinical pharmacology of amikacin and kanamycin. 阿米卡星与卡那霉素的临床药理学
During and after a 4-hr intravenous infusion of amikacin and kanamycin in a cross-over study in healthy adult male volunteers, average concentrations of drug in serum were similar, with half-lives of approximately 2 hr. Apparent volumes of distribution at the steady state averaged 30% of body weight, and the rate of renal clearance was less than the rate of creatinine clearance (83 vs. 120 ml/min), a finding that indicates tubular reabsorption. The rate of serum clearance was greater than the rate of renal clearance (100 vs 83 ml/min). Urinary excretion in 24 hr averaged 94% of the dose, and there was no binding of serum proteins. In another cross-over study, volunteers received single intramuscular injections of these antibiotics. Peak concentrations of drug in serum after 45 min to 2 hr averaged 19.9 and 19.0 mug/ml for amikacin and kanamycin, respectively. Serum half-lives between 4 and 8 hr after administration of drug were 2 hr, and an average of 94% of the dose was recovered in the urine in 24 hr. Thus, the pharmacologic properties of amikacin and kanamycin were virtually identical.
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Comparative ototoxicity of kanamycin A and kanamycin B in the guinea pig. 卡那霉素A和卡那霉素B在豚鼠中的比较耳毒性
It has previously been shown that simple compounds with multiple amine groups are ototoxic, the degree of ototoxicity depending on the number of amine groups in the molecule. The relationship between the number of amino groups and ototoxicity in aminoglycoside was studied using kanamycin A and kanamycin B, which contain 4 and 5 amino groups respectively. Forty-five pigmented guinea pigs were injected intratympanically with 0.1 ml of different concentrations of kanamycin A and kanamycin B. The animals were sacrificed 4 days after injection and the organ of Corti was studied by scanning electron microscopy. It was found that on an equimolar basis, kanamycin B (with 5 amino groups) is more cochleotoxic than kanamycin A (with 4 amino groups). The greater cochleotoxic potential of kanamycin B may be explained by the higher cationic nature of the molecule due to protonation of the amino--NH2 groups at physiological pH, resulting in a greater affinity between the drug and the cell membrane.
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Synthesis and Bioactivities of Kanamycin B-Derived Cationic Amphiphiles. 卡那霉素B衍生阳离子两亲物的合成及生物活性
Cationic amphiphiles derived from aminoglycosides (AGs) have been shown to exhibit enhanced antimicrobial activity. Through the attachment of hydrophobic residues such as linear alkyl chains on the AG backbone, interesting antibacterial and antifungal agents with a novel mechanism of action have been developed. Herein, we report the design and synthesis of seven kanamycin B (KANB) derivatives. Their antibacterial and antifungal activities, along with resistance/enzymatic, hemolytic, and cytotoxicity assays were also studied. Two of these compounds, with a C12 and C14 aliphatic chain attached at the 6″-position of KANB through a thioether linkage, exhibited good antibacterial and antifungal activity, were poorer substrates than KANB for several AG-modifying enzymes, and could delay the development of resistance in bacteria and fungi. Also, they were both relatively less hemolytic than the known membrane targeting antibiotic gramicidin and the known antifungal agent amphotericin B and were not toxic at their antifungal MIC values. Their oxidation to sulfones was also demonstrated to have no effect on their activities. Moreover, they both acted synergistically with posaconazole, an azole currently used in the treatment of human fungal infections.
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Molecular detection of drug resistance to ofloxacin and kanamycin in Mycobacterium tuberculosis by using multiplex allele-specific PCR. 使用多重等位基因特异性PCR分子检测结核分枝杆菌对氧氟沙星和卡那霉素的耐药性
Drug resistance in tuberculosis (TB) is the biggest global health challenge as it hinders the tuberculosis control program and makes the disease more worsen. Molecular methods interrupt the spread of drug resistance by facilitating the appropriate anti- tuberculosis therapy at correct time through rapid diagnosis of multi drug resistant (MDR) and extensively drug resistant tuberculosis (XDR-TB). In this study we standardized and evaluated the diagnostic utility of multiplex allele specific PCR (MAS-PCR) targeting gyrA D94G and rrs A1401G mutations for detection of resistance against two key drugs (ofloxacin and kanamycin) of second line anti tuberculosis treatment. MAS-PCR assays targeting gyrA D94G and rrs A1401G for ofloxacin (OFL) and kanamycin (KAN) resistance respectively were carried out on 150 multidrug resistant isolates of Mycobacterium tuberculosis. The results were compared with phenotypic drug susceptibility test against ofloxacin and kanamycin by using proportion method on MGIT 960. Of 150 MDR isolates 50 were resistant to both ofloxacin and kanamycin, 36 were resistant to ofloxacin only, 8 were resistant to kanamycin only and 56 were susceptible to both the drugs. MAS-PCR correctly identified gyrA D94G and rrs A1401G mutations in phenotypically resistant isolates with a specificity of 100%. The sensitivity of MAS-PCR was 88.66%, 93.55% and 86% for OFL, KAN and XDR-TB respectively. There was no mutation detected at gyrA D94G region of 12.86% (11 of 86) OFL resistant isolates while 6.89% (4 of 58) of KAN resistant isolates did not carry rrs A1401G substitution. MAS-PCR proves to be a rapid tool for detection of drug resistance which could also be used as an initial marker for screening of XDR-TB.