13 results about "Tigecycline" patented technology

The invention discloses a preparation method of a tigecycline USP impurity G. The tigecycline USP impurity G is obtained by taking tigecycline as a raw material, adding an oxidizing agent metachloroperbenzoic acid, and carrying out oxidation rearrangement reaction, separation and purification. The invention discloses a method for preparing a tigecycline USP impurity G, and aims to provide a method for preparing the tigecycline USP impurity G. The purity of a target product obtained through the method is 95% or above, the target product can be directly used as a tigecycline impurity detection reference substance, specific economic benefits are generated, and the method has a good application prospect. Belongs to the technical field of medicine.

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 discloses a preparation method of nano bamboo charcoal for treating areca yellow leaf disease, and relates to the technical field of polymer modified materials. According to the method, a multifunctional slow-release system is constructed through a five-stage process; gradient pyrolysis and superfine grinding are adopted to prepare a bamboo charcoal precursor; (2) liquid nitrogen assisted ball milling is combined with hydrothermal activation to form nano bamboo charcoal with a specific surface area, and a 2-5nm mesoporous structure is synchronously constructed; (3) surface charge regulation and control are realized through polyethyleneimine grafting and sodium hexachloroiridate loading, and the antibacterial activity is enhanced; (4) coating the tigecycline-bamboo charcoal complex with mesoporous silica to form a 20-30nm slow-release unit, so as to realize targeted drug release; and (5) preparing stable suspension through high-pressure homogenization. The technology provides an efficient and environment-friendly solution for areca yellow leaf disease treatment, and has the functions of soil remediation and plant health care.

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 present application relates to a new use of curcumin in synergistic tigecycline antibacterial effect. The use amount of curcumin is 32 μg / mL-128 μg / mL, and the use amount of tigecycline is 0.015-4 μg / mL. In the preparation of composition or compound preparation, when curcumin is used to synergize the antibacterial effect of tetracycline antibiotic tigecycline, the ratio of the use amount of curcumin to tigecycline is between 8:1-8533:1. The present application can restore the sensitivity of drug-resistant bacteria to tigecycline, reduce the dosage of tigecycline, improve the antibacterial treatment effect, reduce the toxic side effects, and has important clinical application value.

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 relates to the technical field of biological medicines, and discloses preparation and application of targeted gram-negative bacterium-resistant bionic dual-modified nanoparticles. Comprising the following steps: S1, synthesis of GBP1c peptide; S2, preparation of PLGA / tigecycline nanoparticles; S3, preparation of GBP1c modified PLGA / tigecycline nanoparticles; S4, preparation of GBP1c-neobaicalein dual modified PLGA / tigecycline nanoparticles; according to the invention, through functional linkage of the GBP1c peptide, the neobaicalein and the macrophage membrane, a synergistic system of targeting anchoring, drug resistance antagonism and inflammation chemotaxis is constructed. The GBP1c peptide is specifically combined with Gram-negative bacterium outer membrane lipopolysaccharide by virtue of a multi-basic amino acid sequence to realize accurate targeting, NEO synchronously blocks LPS transport to destroy the bacterium outer membrane and inhibit a P-glycoprotein efflux pump to prolong drug retention, and MM guides nanoparticles to enrich an infected part by virtue of inflammation chemotactic characteristics, so that the drug retention is prolonged. The three are linked to solve the core problems of poor DDS targeting and insufficient drug permeation in the prior art.

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 invention discloses an application of cinacalcet hydrochloride in preparation of drugs for resisting drug-resistant bacteria. The invention finds that the cinacalcet hydrochloride (CC) has dual effects, on one hand, the sensitivity of a strain carrying a tmexCD-toprJ gene cluster to tigecycline can be recovered, and on the other hand, the conjugational metastasis of antibiotic resistance genes can be inhibited by reducing over 99% of plasmid propagation. The synergistic effect of the CC and the tigecycline is that the minimum inhibitory concentration of the tigecycline is reduced by at least 8 times by dissipating proton dynamic potential and inducing active oxygen to damage an excretion function. Besides, the CC also reduces propagation of various drug-resistant plasmids by synergistically inhibiting expression of an Mpf and Dtr conjugation system and inhibiting SOS response, so that plasmid transfer and stable colonization of exogenous DNA (Deoxyribose Nucleic Acid) are blocked. The CC overcomes the tigecycline drug resistance mediated by tmexCD-topJ by destroying energy metabolism and oxidative stress, and meanwhile, limits horizontal transfer of other drug-resistant genes.

The present invention includes novel molecules and methods for using the same to treat Alcohol Use Disorder (AUD), Substance Use Disorder (SUD), tobacco use, pain, or proinflammatory disorders comprising: identifying a subject in need of treatment for at least one of AUD, SUD, pain, or a proinflammatory disorder; and providing the subject with an effective amount of a modified minocycline to ameliorate or eliminate the AUD, SUD, pain, or proinflammatory disorder and that has reduced, or no, antimicrobial activity, wherein the modified tetracycline has a formula, e.g., or the modified doxycycline, minocycline, and tigecycline and their tautomerized structures, where the R-groups shown in the minocycline example above could be different combination of halogen, acetyl ester, methyl ester, and diacetal.

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.