34 results about "Antituberculous drug" patented technology

The invention relates to a triple compound microsphere vascular targeted embolization sustained-release preparation containing an antituberculous drug as well as a preparation method and application of the preparation. The sustained-release agent comprises a carrier and drugs, wherein the drugs are coated with the carrier; the carrier is sodium alginate or chitosan, and the drugs are triple antituberculous compound drugs including rifampicin, isoniazid and pyrazinamide or moxifloxacin. The three antituberculous drugs are matrix drug solutions, the sodium alginate or chitosan is a carrier solution, the matrix drug solutions and the carrier solutiona are mixed to prepare a solution, the polymer solution containing drugs is dispersed into fogdrops with a certain diameter by adopting a high-voltage electrostatic droplet mode, and the fogdrops are sprayed into a solidifying liquid to prepare antituberculous drug microspheres under the action of calcium ions. The embolization sustained-release preparation can be used for treating tuberculosis, massive hemoptysis of pulmonary tuberculosis, tuberculosis cavity, renal tuberculosis, osteoarticular tuberculosis, genital tuberculosis, tuberculosis of thyroid gland, tuberculosis of cervical lymph nodes, tuberculosis of pericardium, tuberculosis of chest wall, pleural tuberculosis and other kinds of tuberculosis in a body.

The invention discloses an antituberculous drug drug-resistance gene and a screening method thereof. The antituberculous drug drug-resistance gene is pks12, pks5, PPE34, Rv1978, Rv1847, hemK, PPE3, glyA1, PE_PGRS27, PE_PGRS19, Rv1520, Rv1505c, Rv2407, mmuM, vapB17, Rv3727 and Rv3737. The novel candidate drug target gene is provided for a further understanding of drug resistance mechanism of MDR/XDR mycobacterium tuberculosis and the therapy of MDR/XDR-TB.

The invention discloses an ubiquitin-interacting motif-like (UIML) structural domain of mycobacterium tuberculosis secretory protein, and belongs to the field of cytobiology. The ubiquitin-interacting motif-like structural domain of PtpA and a key binding site (A140) thereof are determined for the first time; the ubiquitin-interacting motif-like structural domain comprises the 115th amino acid of PtpA protein to the 161th amino acid of the PtpA protein, wherein hydrophobic interaction of hydrophobic amino acid sequence EEVFAVIESA (136-145) with ubiquitin (Ub) can be realized; and mutation of the A140 site of the UIML structural domain is capable of resulting in loss of binding capacity of Ub with PtpA, and loss of enzyme activity regulatory functions of Ub. The ubiquitin-interacting motif-like (UIML) structural domain is capable of providing specific sequences for screening of PtpA molecule-based antituberculous drugs and vaccine development, providing treatment of a plurality of diseases in clinic with novel tools and ideas, possesses promising prospect in development and clinical application of a plurality of drugs such as antitumor drugs, and can be directly used for scientific research field or for guiding development of preparations used for reversible control of JNK and P38 signal channels.

The invention relates to mycobacterium tuberculosis antigen protein Rv1798 and application of a T cell epitope peptide of the mycobacterium tuberculosis antigen protein Rv1798 in preparation of tuberculosis detection reagents, vaccines and drugs. An amino acid sequence of the mycobacterium tuberculosis protein antigen Rv1798 and an amino acid sequence of the T cell epitope peptide of the protein antigen Rv1798 are shown in SEQ ID NO:1-3 respectively. The mycobacterium tuberculosis protein antigen Rv1798 and the T cell epitope peptide thereof are applied to a specific T cell and B cell immune response caused by mycobacterium tuberculosis by serving as irritants; and when the mycobacterium tuberculosis protein antigen Rv1798 and the T cell epitope peptide thereof are applied to the specific T cell and B cell immune response caused by the mycobacterium tuberculosis by serving as the irritants, the condition that a false positive result is caused due the fact that an antigen is not pure can be reduced compared with an original method that a complete antigen is adopted. The detection reagents prepared from the protein antigen Rv1798 and the epitope peptide thereof can be widely applied to the related fields of assistant diagnosis of tuberculosis, epidemiological monitoring and the like. The tuberculosis vaccines and the antituberculous drugs which are prepared from the protein antigen Rv1798 can be used for preventing and treating the tuberculosis.

The invention discloses a near-infrared cyanine colorimetric fluorescent probe and a preparation method and application thereof. The structural formula of the probe is shown as a formula (I). The fluorescent probe can identify and detect N2H4 in a mixed solution of absolute ethyl alcohol and a PBS by utilizing fluorescence and an ultraviolet-visible absorption spectrum. The probe has high selectivity and sensitivity in N2H4 identification, strong anti-interference capability and very low detection limit; the fluorescent probe can be applied to detection of environmental pollution or in-vitro and in-vivo antituberculous drug metabolites N2H4.

The invention discloses an LC-MS/MS method for quantitatively analyzing the plasma concentration of an antituberculous drug. The method can simultaneously detect isoniazide, rifampicin, pyrazinamide and ethambutol through S1 standard working solution preparation, S2 sample preparation, S3 sample treatment, S4 sample detection and S5 standard curve making and quantitative analysis, the sample pretreatment process is simple and is easy to operate, and all the reagents are conventional reagents, so that the cost is lower. According to the method, a reversed-phase C18 column of 150 mm*2.1 mm is adopted, the flow rate is controlled to be 0.3 mL/min, and the column temperature is 30 DEG C; the problem that the polarity difference of isoniazide, rifampicin, pyrazinamide and ethambutol is large can be well solved, the separation effect is better, and the cost is lower. The method has the advantages of higher sensitivity, accuracy and precision, wide detection linear range and short detection time, and can be used as a reliable detection method suitable for popularization and for monitoring the treatment concentration of clinical first-line anti-tuberculosis drugs.

The invention discloses application of polymorphism of retinoid X receptor alpha (RXRA) genes to adverse reactions of antituberculous drugs, and relates to the field of screening of adverse reactionsof tuberculous drugs. The invention discloses application of the polymorphism of the RXRA genes to tuberculosis treatment, it is found that through detection of the polymorphism of the RXRA genes, therisk of generating the adverse reactions after tuberculous patients are treated by the antituberculous drugs can be predicted, certain support is provided for avoiding the adverse reactions caused bythe related antituberculous drugs, and certain guidance is also provided for drug use of the tuberculous patients.

The invention discloses application of L-alanine in preparation of a medicine for preventing and treating tuberculosis. By means of a C57BL/6 mouse and SCID mouse infection model, a macrophage in-vitro infection model, an exogenous metabolite adding mode and the like, it is proved that L-alanine resists tubercle bacillus infection through natural immune cell protection host, L-alanine promotes macrophage antibacterial peptide generation and limits tubercle bacillus intracellular survival; and the L-alanine is expected to assist the current antituberculous drugs, can shorten the course of treatment and improve the curative effect, and provides reference for clinical treatment.

The invention relates to a preparation method of an antituberculous drug Pretomanid and an application of the antituberculous drug Pretomanid. According to the preparation method, 2, 5-dibromo-4-nitroimidazole is taken as an initial raw material, and a nucleophilic substitution reaction, a reduction elimination reaction, an oxidation cyclization reaction, an epoxy ring-opening reaction, a nucleophilic substitution reaction, a deprotection reaction and a cyclization reaction are sequentially carried out to prepare the target product, namely the antituberculous drug Pretomanid. The raw materials used in the whole process are cheap and easy to obtain, explosive dinitroimidazole is prevented from being used, generation of 4-nitro isomers is avoided, and the method is simple in process operation, easy to control and convenient to purify and can be used for industrial production.

The invention discloses a high-throughput sequencing detection method for drug-resistant sites of Mycobacterium tuberculosis. The method uses the existing mutation database of drug-resistant Mycobacterium tuberculosis and combines the second-generation high-throughput sequencing technology to achieve a more comprehensive, effective and rapid Detecting resistance loci to anti-TB drugs in Mycobacterium tuberculosis. This method overcomes the limitation of the number of detected gene loci in other drug resistance locus detection methods, and the inability to distinguish silent mutations of important genes, which leads to the difficulty of false positive results. With the help of high-throughput detection technology, it can provide better Treatment of drug-resistant tuberculosis provides more comprehensive diagnostic information that can help improve efficacy and reduce the use of ineffective drugs.

The invention discloses an exosome compound with a tumor inhibition effect. The exosome compound comprises exosomes of human mesenchymal stem cells and rifampicin. According to the invention, an exosome drug loading technology is utilized to load an antituberculous drug rifampicin into the human-derived mesenchymal stem cell exosome, and experiments find that the human-derived mesenchymal stem cell exosome has remarkable curative effects of inhibiting growth, proliferation, migration and invasion of tumors, can promote apoptosis and cell cycle arrest of the tumors, and can be used for preparing a medicine for treating the tumors. Particularly, the compound has an obvious growth inhibition effect on osteosarcoma cells. After being prepared into the tumor treatment medicine, the compound has important significance on improving the treatment effect of osteosarcoma patients, improving prognosis and increasing the survival rate.

The invention discloses an isocryptolepine analogue, and a preparation method and application thereof. The chemical structure of the isocryptolepine analogue is shown as a formula I. The substituent group R in the formula I can be independently -H, -OCH3, -F, -Cl or -SO2NH2. According to the isocryptolepine analogue disclosed by the invention, ofloxacin is taken as a raw material, so that effective chemical construction from a fluoroquinolone structure to an indoloquinoline skeleton is realized, and a new way for structural modification of isocryptolepine is expanded, so that the anti-tubercle bacillus activity and the anti-drug resistance of the compound are improved, the toxicity to normal cells is reduced, and the isocryptolepine analogue can be further developed as an antituberculous drug with a brand new structure.

The invention provides a gene detection reagent for predicting liver injury caused by antituberculous drug, a test kit and a detection method, and relates to the technical field of tuberculosis treatment. The reagent is used for predicting the risk of adverse liver reaction caused by the antituberculous drug received by tuberculosis patients. The reagent comprises a genotype used for detecting anyone of the following SNPs sites of the LEPR gene: rs2025804 and rs2104564. According to the present invention, with the detection of the polymorphism of the LEPR gene, the risk of the adverse reaction after the tuberculosis patient receives the anti-tuberculosis drug treatment can be predicted, the certain support is provided for the prevention of the adverse reaction caused by the related anti-tuberculosis drug, and the certain guidance is provided for the medication of the tuberculosis patient.

The invention discloses an antituberculous drug composition, prepared from the following components in parts by weight: 20 to 50 parts of Chinese honeylocust fruit, 10 to 30 parts of mineral Zilusha, 10 to 30 parts of flos sophorae, 5 to 10 parts of donkey-hide gelatin and 5 to 10 parts of rhizoma picrorhizae. The antituberculous drug composition has the advantages that growth of mycobacterium tuberculosis can be inhibited, the antibacterial activity is higher, and various tuberculosis diseases can be treated.

The invention discloses an isoniazide and rifampicin co-loaded microsphere sustained release preparation and a preparation method thereof, two antituberculous drugs, isoniazide and rifampicin, are jointly entrapped in PLGA microspheres by using an electrostatic fluid spraying technology, the average particle size of the microspheres meets the effective particle size of pulmonary administration, and the entrapment efficiency is high. A 15-day in-vitro drug release experiment shows that the cumulative drug release rate of the drug in the microspheres is 40%-60%, and the technical requirement of slow release is met. The local drug concentration of tuberculosis drugs in the lung can be effectively improved, the administration frequency is reduced, toxic and side effects are reduced, and the economic benefit ratio of the drugs is improved.

The invention discloses application of Rv1773c in preparing a drug for resisting infection of mycobacterium tuberculosis and belongs to the technical field of biology. The invention determines that functional protein Rv1773c of the mycobacterium tuberculosis can promote the mycobacterium tuberculosis to intrude macrophage. The Rv1773c can be used as a novel drug target for resisting tuberculous infection. The results provided by the invention can provide a novel tool and an idea for preventing and treating clinical tuberculosis; particularly, the Rv1773c has a broad prospect in the aspects ofdevelopment, clinical application and the like of anti-tuberculosis drugs and vaccine, or can be directly applied to the field of scientific research or guides the development of an inhibitor for inhibiting the intrusion of the mycobacterium tuberculosis to host macrophages. The Rv1773c disclosed by the invention has important application value of obtaining a novel antituberculous drug target andscreening a novel drug.

The invention discloses a spinal internal fixing device containing a carrier for implanting antituberculous drugs into an artificial bone in a sustained-release mode. The spinal internal fixing device containing the carrier for implanting the antituberculous drugs into the artificial bone in a sustained-release mode comprises fixing screws arranged at intervals and a connecting rod connecting the two fixing screws, wherein tuberculosis treatment drugs are arranged in the fixing screws and/or the connecting rod, the outer wall of each fixing screw and the outer wall of the connecting rod are provided with drug passing holes allowing the tuberculosis treatment drugs to be released, positioning devices used for fixing the tuberculosis treatment drugs are arranged in the fixing screws and the connecting rod, and the tuberculosis treatment drugs comprise a slow-release drug carrier, isoniazide, rifampicin and streptomycin.

The invention relates to an application of nintedanib or a pharmaceutical salt thereof in preparation of a medicine for treating tuberculosis, preferably, the invention provides a combined use of the nintedanib or the pharmaceutical salt thereof and other anti-tuberculosis medicines for treating tuberculosis, or an auxiliary medicine for treating tuberculosis. Wherein the other antituberculous drugs are selected from rifampicin, isoniazide, pyrazinamide, ethambutol, fluoroquinolones, streptomycin, kanamycin, amikacin, capreomycin, sodium p-aminosalicylate, ethionamide, cycloserine, clofazimine and linezolid.