7 results about "Tigecycline" patented technology

This invention belongs to the field of drug metabolism and analytical chemistry, specifically relating to a method for the rapid determination of tigustastat and its active metabolite GD-MET-1 concentrations in a human liver microsome incubation system using liquid chromatography-tandem mass spectrometry (LC-MS / MS). The method first prepares stock solutions of tigustastat, GD-MET-1, and an internal standard, and prepares a series of standard curve solutions, quality control solutions, and precipitant solutions containing the internal standard. Next, the sample with the added precipitant solution undergoes vortexing and centrifugation pretreatment. Finally, chromatographic and mass spectrometric conditions are set, and the analysis is performed by LC-MS / MS. This method has been validated for specificity, accuracy, precision, matrix effects, recovery, residues, and stability, and can be reliably used for metabolic stability studies of tigustastat and GD-MET-1 in a human liver microsome incubation system, GD-MET-1 formation studies, metabolic enzyme identification, enzyme kinetic studies, and drug interaction studies.

The present application relates to the new use of paclitaxel in the synergistic effect of the antibiotic action of tigecycline, and the use of paclitaxel in the preparation of a composition or a compound preparation for the synergistic effect of the antibiotic action of tigecycline, and the ratio of paclitaxel to tigecycline is between 16:1-256:1. In the present application, paclitaxel and tigecycline show significant synergistic effect, and the FICI is 0.1875-0.3125 (all less than 0.5), that is, the combination of the two shows significant synergistic effect. By using the combination of paclitaxel, the use amount of tigecycline can be effectively reduced, and the use amount of tigecycline alone is 1 to 16 times higher than that of the combination of paclitaxel and tigecycline.

The invention relates to a molecular marker of drug-resistant mycobacterium abscessus based on fusA gene mutation and application of the molecular marker, and belongs to the technical field of biological medicines. The invention provides a group of molecular markers for detecting the drug resistance of mycobacterium abscessus. The molecular markers are mutations on a fusA gene of the mycobacterium abscessus, including fusA1318Agt; g, fusA 1613 G gt; a, fusA18721883 dup GGGCGACGTGAT, and the number of the GGGCGACGTGAT is 1: 1. The invention finds that when the mycobacterium abscessus generates fusA1613 G gt; when A is mutated, cross resistance is generated to aminoglycoside drugs, macrolide drugs and tetracycline drug tigecycline. The fusA < 1318 > A < gt > is generated; the mycobacterium abscessus with mutations of G and fusA18721883 dup GGGCGACGTGAT is resistant to aminoglycoside drugs and tigecycline, and meanwhile, the mycobacterium abscessus has lateral sensitivity to macrolide drugs. The mycobacterium abscessus with mutations of G and fusA18721883 dup GGGCGACGTGAT is resistant to aminoglycoside drugs and tigecycline. The method is of great significance to clinical molecular diagnosis and medication.

The invention discloses a Ts-ELP temperature-sensitive self-assembly nano fusion protein, an antibiotic delivery system and a preparation method, and belongs to the technical field of nano preparations. The fusion protein comprises antibacterial peptide Ts and elastin-like polypeptide ELP which are sequentially connected. An MMP-9 restriction enzyme cutting site is introduced between the antibacterial peptide Ts and the elastin-like polypeptide ELP. Fusion protein and tigecycline (Tig) are self-assembled to form an antibiotic delivery system, the delivery system has Gram-negative bacterium surface lipopolysaccharide targeted recognition capability, and drug release is triggered through pH response and a phase separation mechanism in an infection microenvironment, so that the enrichment efficiency of tigecycline in a focus area is enhanced, and the drug delivery efficiency is improved. The antibiotic delivery system has the technical advantages of strong targeting property, enhanced antibacterial activity, low drug-resistant induction risk, good biological safety, simple preparation process, high yield and the like, can be used for treatment of multi-drug-resistant bacterium infection, and is especially suitable for prevention and treatment of carbapenem-resistant klebsiella pneumoniae (CRKP) and drug-resistant gram-negative bacterium infection related diseases.

The invention discloses a phthalylhydrazine derivative functionalized chemiluminescent gold nanocluster and a preparation method thereof. The chemiluminescent gold nanocluster is prepared by taking a phthalylhydrazine derivative as a reducing agent and a ligand through a water phase reduction method. The gold nanocluster acts with potassium persulfate to generate a stable and high-intensity chemiluminescence signal. The invention has the characteristics of simple preparation method, mild reaction conditions, good reproducibility, strong chemiluminescence signal and the like. On the basis of coordination between tigecycline molecules and gold nanoclusters, electron distribution and excited state energy level structures of the gold nanoclusters are changed, so that the chemiluminescence performance of the gold nanoclusters is regulated and controlled, and high-sensitivity chemiluminescence detection of tigecycline is realized. The chemiluminescent probe has important application value in the field of biological medicine analysis.

The present application relates to a kind of continuous evolution system based on T7 RNA polymerase mutant and its application, belong to the technical field of evolutionary engineering.The present application is based on the T7 RNA polymerase mutant with the ability of synthesizing single-stranded DNA, constructs the continuous evolution system comprising single-stranded DNA synthesis template and T7 RNA polymerase mutant, the continuous evolution system is introduced into host, T7 RNA polymerase mutant is recombined with target gene by synthesizing single-stranded DNA, so that host is constructed to obtain mutant library in the process of continuous passage, host is subjected to screening pressure, and host realizes continuous evolution.The system is applied to complete the evolution of tetracycline efflux pump protein in 7 days, and the tryptophan deficiency of saccharomyces cerevisiae is repaired in 24 hours.The tetracycline efflux pump protein mutant screened can tolerate tetracycline and tigecycline, and the tolerance to tigecycline is increased by 8 times, and the tolerance to tetracycline is increased by 2 times, which is of great significance to improve the performance of cell factory.

The application belongs to the technical field of biological medicine, and provides application of ferulic acid in preparation of a photolysis inhibitor of tigecycline and minocycline. The ferulic acid can significantly inhibit degradation of tigecycline or minocycline under light conditions, and further enhance the antibacterial activity of tigecycline or minocycline under light conditions. Compared with the treatment of tigecycline alone, the addition of ferulic acid can significantly enhance the treatment effect of tigecycline or minocycline as an external medicine on skin or soft tissue infection, effectively expand the drug dosage form of tigecycline or minocycline, and provide a safer and more reliable drug preparation for the treatment of complex drug-resistant pathogenic bacterial skin or soft tissue infection.