193 results about "Anti tuberculosis" patented technology

Compounds having the general structure:

wherein A is selected from the group consisting of oxygen, sulfur, and NR₁₅, and R₁₅ is selected from the group consisting of H, alkyl, aryl, substituted alkyl, and substituted aryl; B,D, and E are each independently selected from the group consisting of CH, nitrogen, sulfur and oxygen; R₁ is selected from the group consisting of nitro, halo, alkyl ester, arylsulfanyl, arylsulfinyl, arylsulfonyl and sulfonic acid; t is an integer from 1 to 3; and X is a substituted amide, and methods of using the novel compounds for treating infections caused by microorganisms, including Mycobacterium tuberculosis.

The invention discloses streptomyces atratus and application of cyclic peptide compounds with the same to preparing mycobacterium tuberculosis resistant medicines. A structural formula of the cyclic peptide compounds is shown. A preservation number of the streptomyces atratus SCSIO Zh16 is CGMCC No.12198. The streptomyces atratus and the application have the advantages that the six cyclic peptide compounds are obtained from fermentation cultivation substances of the streptomyces atratus SCSIO Zh16 by means of separation, the cyclic peptide compound 6 is high in mycobacterium tuberculosis resistant activity, obvious effects of inhibiting mycobacterium tuberculosis can be realized by the cyclic peptide compound, accordingly, the cyclic peptide compounds can be used for preparing anti-tuberculosis medicines and can be used for treating tuberculosis, alternative compounds can be provided for developing novel anti-tuberculosis medicines, and the streptomyces atratus and the application have important significance on developing marine medicinal materials in China.

The invention discloses an in-situ gel slow-release preparation for local drug delivery, which comprises drug active ingredient microspheres and in-situ gel. The in-situ gel slow-release preparation is characterized in that the gel forming temperature is kept within the scope of 15-25 DEG C and the calcium ion effect exists; the drug active ingredient is anti-tuberculosis drugs; the proportional relationship of the drug active ingredient microsphere and the temperature-ion sensitive gel is 5-50 mg:1-50 ml; the drug active ingredient microspheres are uniformly dispersed in the in-situ gel under the agitation condition; the in-situ gel slow-release preparation can restrain the excessive release of the drugs and lead the drugs to release stably and detain at the lung of a rat for 120 h at most; and a drug system detains at the local part for a long time, thereby realizing the treatment purpose.

The invention is the use of a therapeutically effective amount of glutathione (reduced) in a liposome encapsulation for oral administration to improve symptoms of illnesses that are related to tuberculosis and HIV and more generally viruses and for the treatment and prevention of virus, particularly HHV-6 and EBV, which liposomal encapsulation of glutathione (reduced) is referred to as liposomal glutathione. The application references specifically reduced glutathione and its importance, and how to stabilize it effectively so it can be taken orally, and need not be refrigerated. New uses for tuberculosis are discussed. The combination is proposed of reduced glutathione and Highly Active Anti-Retroviral Therapy having at least one pharmaceutical composition selected from the group of Nucleoside/tide Reverse Transcriptase Inhibitors (NRTIs), Protease Inhibitors (PIs), and Non-nucleoside Reverse Transcriptase Inhibitors (NnRTIs), and further anti-tuberculosis drugs.

The invention provides for the use of antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit anti-mycobacteria activity, including the mycobacterium causing tuberculosis. Multiple compounds were synthesized and screened for anti-tuberculosis activity. Disclosed herein are a series of compounds with anti-tuberculosis activity, including six leads that completely inhibited bacterial growth at 5 micrograms per ml or less. Three of these compounds were tested to determine MIC and these ranged between 1 and 4 micrograms per ml against both drug susceptible Mycobacterium tuberculosis strains and strains that are multi-drug resistant (MDR) including XDR strains. The compounds developed are derived from parent compound nitazoxanide, which had no inhibitory activity in the stringent testing format used herein. The derivatives were synthesized using a di-nitro-thiophene or 4-Chloro-5-Nitro-thiazole scaffold and R groups connected via a peptide bond (NHCO) to cyclic compounds such as benzene, thiophene or furans. Many of these compounds have broad spectrum activity against Gram positive bacteria including Staphylococcus aureus (MRSA) and Staphylococcus epidermidis. Several of these lead compounds were not toxic for mice at 200 mg/Kg doses administered over a period of three days.

The invention discloses an active antibacterial biological protective mask and a synthetic process of an antibacterial agent material thereof. The biological protective mask has dust filtering and active antibacterial dual functions. The structure of the protective mask is composed of a three-layer structure, namely an outside (inside) all cotton fabric woven layer, a sub-outer activated carbon filtering layer and an intermediate active antibacterial agent layer. The active antibacterial biological protective mask has the characteristics that materials in different functional layers are configured, the sub-outer layer is the activated carbon filtering layer and has a dust filtering function; the intermediate layer is an active antibacterial functional layer, a porous calcium phosphate ceramic antibacterial agent doped with silver ions has the active antibacterial function, and the biological protective mask is endowed with the dust filtering and active antibacterial dual functions. The active antibacterial biological protective mask disclosed by the invention has the characteristics of excellent dust protection effect, uniform antibacterial functional material particles, narrow particle size distribution, broad spectrum antibacterial property, high efficiency, non-toxicity, outstanding anti-tuberculosis effect and the like.

The invention discloses a pyrazolo[1, 5-a]pyridine compound with the structure characteristic shown in the formula (I) or its pharmaceutically acceptable salt, stereoisomer or prodrug molecule and a use thereof. The compound has good in-vitro anti-tubercle bacillus activity, has the minimal inhibitory concentration (MIC) less than 0.1 micrograms per milliliter and partial MIC of 0.01 micrograms per milliliter and has strong inhibition effects on a clinically sorted multi-drug-resistant tuberculosis (MDR-TB) strain. In an in-vivo experiment, at a dosage of 20mg/kg/d, the pyrazolo[1, 5-a]pyridine compound can effectively eliminate H37Ra infection in a mouse and is a novel anti-tuberculosis compound.

The invention discloses a genetic engineering bacterial strain for directionally producing compounds having anti-tuberculosis activity and anti-tumor activity and an application thereof. The genetic engineering bacterial strain is a genetic engineering bacterial strain obtained by knocking out an ialL gene or ilaR gene in a genome of streptomyces atratus SCSIO ZH16, wherein the ialL gene has the nucleotide sequence shown in SEQ ID NO.1, and the ialR gene has the nucleotide sequence shown in SEQ ID NO.2. The genetic engineering bacterial strain can produce the compounds 1, 2, 3, 4 and 5 having anti-tuberculosis activity and anti-tumor activity and shows great value in development of anti-tuberculosis drugs. Therefore, the successful construction of the genetic engineering bacterial strain for directionally producing the compounds having anti-tuberculosis activity and anti-tumor activity can accelerate the process of industrialization of the compounds and promote the development of Chinese marine drugs.

The invention discloses a machine-taking electronic monitor for a patient with tuberculosis, and mainly relates to the field of medicine-taking management of the patient with tuberculosis. The machine-taking electronic monitor comprises a housing, wherein a refrigerating cavity is arranged in the housing; a medicine storage bottle is arranged in the refrigerating cavity; one end of the medicine storage bottle is provided with a bottleneck; threads are arranged on the bottleneck; the bottom of the refrigerating cavity is provided with a threaded hole adaptive to the bottleneck; a funnel is arranged below the threaded hole; the bottom of the funnel is provided with a guide barrel; a medicine taking barrel is arranged on the side wall of the guide barrel; the bottom of the guide barrel is provided with a medicine outlet channel; and a medicine taking slot is formed in the outer wall of the housing. The medicine-taking electronic monitor has the beneficial effects that: the medicine-taking electronic monitor can replace a supervisor for the patient with tuberculosis to remind the patient to regularly take medicines with proper dosage on time and to take periodic review, so that working pressure of the tuberculosis prevention and treatment institution can be relieved, a proper temperature can be provided for storing anti-tuberculosis medicines, medicine-taking and reviewing moments can be set, the medicines can be stored and can be automatically taken out, and the medicine-taking moments of the patient can be recorded.

The present invention provides antibiotics of urinate glucoside peptide category with a structural formula (I) and the acceptable salt in pharmaceutics. The antibiotics can be prepared through fermentation and cultivation of produced fungus. The compound of the present invention is a group of cell-wall peptidoglycan synthesized inhibitor, has anti-tuberculosis activity and pyocyanic fungus, and can be used for preparing anti-infective drugs.

The invention provides an application of compounds Pyrrocidines in preparation of an anti-tuberculosis drug, namely, an application of the compounds Pyrrocidines, derivatives of the compound Pyrrocidines or pharmaceutically acceptable salts of the compounds Pyrrocidines as tyrosine phosphatase inhibitors or in preparation of the tyrosine phosphatase inhibitors. The compounds 19-O-methyl-pyrrrocidine B and pyrrrocidine B have inhibitory activity on mycobacterium tuberculosis tyrosine phosphatase B, and IC50 of the compounds is 3.9 mu M and 75.5 mu M respectively. The compounds can effectively inhibit dephosphorylation activity of the mycobacterium tuberculosis tyrosine phosphatase B and has the clinical application potential for tuberculosis treatment; besides, the compounds Pyrrocidines are natural-metabolism active micro-molecular products separated from microorganisms and can be produced through chemical synthesis and large-scale fermentation separation, the sources are abundant, the production cost is low, and the possibility of medicine preparation is high.

A method for metabolomically evaluating a subject's response to an anti-mycobacterial agent. The method includes the steps of generating multiple small molecule profiles using samples collected from the subject at or immediately prior to the start of treatment and at a times subsequent to the start of treatment with the anti-mycobacterial agent, identifying predetermined biomarkers in the small molecule profiles of the subject and comparing to a known standard established for the agent as an indication of whether the human is benefiting from treatment with the agent. Also provided are methods of monitoring treatment compliance, methods for establishing biomarkers indicative of treatment efficacy and validated biomarkers shown to be effective in assessing efficacy of anti-tuberculosis drugs.

Bacterial resistance to antibiotics is increasing worldwide creating a global threat. Tuberculosis (TB), caused by the bacterium Mycobacterium tuberculosis, is a bacterial infectious disease that results in over one million deaths annually. The discovery outlined here involves a tablet composition for patient administration and subsequently a new paradigm in drug delivery vehicles in vivo and in vitro and is applied to existing TB antibiotics in order to increase their efficacy. The drug delivery system is a three component complex that is administered with the TB antibiotic or a combination of TB antibiotics. The components are a saccharide or saccharides, a transition metal ion or a combination of metal ions that can bind a nitrogen and/or oxygen atom(s), and a water soluble polymer capable of aggregating and enclosing the other constituents. The three component molecular delivery approach has demonstrated ability to overcome M. tuberculosis bacterial resistance to an existing antibiotic.

Compounds having the general structure:

wherein A is selected from the group consisting of oxygen, sulfur, and NR₁₅, and R₁₅ is selected from the group consisting of H, alkyl, aryl, substituted alkyl, and substituted aryl; B,D, and E are each independently selected from the group consisting of CH, nitrogen, sulfur and oxygen; R₁ is selected from the group consisting of nitro, halo, alkyl ester, phenylsulfanyl, phenylsulfinyl, phenylsulfonyl and sulfonic acid; t is an integer from 1 to 3; and X is a substituted amide and methods of using the novel compounds for treating infections caused microorganisms, including Mycobacterium tuberculosis.

The invention relates to a Chinese medicine composition for treating tuberculous pleurisy. The composition is prepared from the following Chinese medicines, by weight: 3 to 25 parts of ardisia japonica herbs, 3 to 20 parts of veronicastrum herbs, 3 to 20 parts of sweetgum fruits, 3 to 20 parts of selfheal spikes, 3 to 20 parts of houttuynia herbs, 3 to 20 parts of bletilla rhizomes, and 3 to 9 parts of licorice roots. The composition is a substitute for hormone medicines to reduce swelling and cure tuberculous pleural effusion. The composition has effects of dispelling wind, eliminating dampness, soothing the liver, invigorating the collaterals, and promoting dieresis, has some inhibition effect on mycobacterium tuberculosis, has an astringent effect on a tuberculous focus, can reduce fluid exudation at the tuberculous focus, and promotes circulation in lymphatic vessels, so that interstitial fluid is rapidly removed and absorbed. If the composition is orally taken and combined with anti-tuberculosis drugs to treat the tuberculous pleurisy, the effective rate and the cure rate are 100% and 98.7% respectively; it takes no more than 30 days to remove effusion; a whole treatment takes no more than 12 months; no significant toxic and side effects are observed; and there is no damage to liver, kidney, and stomach functions.

The invention relates to the technical field of molecular biology, in particular to preparation and application of mycobacteriophage lyase Lysin-Guo1. The invention provides the preparation and application of the mycobacteriophage lyase. The invention provides a bacteriostatic agent; the bacteriostatic agent is prepared from main active components selected from at least one of the mycobacteriophage lyase Lysin-Guo1, a carrier containing a Lysin-Guo1 expression element, an expression cassette containing a Lysin-Guo1 expression element, or host cells containing Lysin-Guo1 expression elements; the Lysin-Guo1 has an amino acid sequence shown in SEQ ID No 1. The invention also provides a preparation method of the mycobacteriophage lyase Lysin-Guo1. The mycobacteriophage lyase Lysin-Guo1 is capable of cleaving multiple types of mycobacterium tuberculosis, and is also found to have a certain inhibiting effect on other bacteria including escherichia coli, staphylococcus aureus, acinetobacter baumannii and pseudomonas aeruginosa. The preparation and application of the mycobacteriophage lyase Lysin-Guo1 lay a foundation for anti-tuberculosis substitution therapy of drug-resistant tuberculousbacillus.

The invention discloses application of cobimetinib in preparation of medicaments for treating tuberculosis. The application is high in safety, and the efficiency of killing mycobacterium tuberculosisis high. According to the application of cobimetinib in preparation of the medicaments for treating tuberculosis, the medicaments for treating tuberculosis are resistant to mycobacterium tuberculosis.The invention also provides a pharmaceutical composition for treating tuberculosis. The pharmaceutical composition comprises cobimetinib. Cobimetinib serving as a potential medicament for targeting HDT has been approved by FDA, is high in safety and has a great development value, so that by applying cobimetinib as a main component in anti-tuberculosis medicaments, the safety is high. Experimentsshow that cobimetinib in macrophages can obviously enhance the activity of the macrophages to kill tubercle bacillus.

The present invention relates to applications of Mycobacterium tuberculosis antigen protein Rv0446c and a T-cell epitope peptide thereof in preparation of tuberculosis detection reagents, vaccines and medicines, wherein the amino acid sequences of the antigen protein Rv0446c and the T-cell epitope peptide thereof are respectively represented by SEQ ID NO:1-5. According to the present invention, the Mycobacterium tuberculosis antigen protein Rv0446c and the T-cell epitope peptide thereof are used as the stimulants for the specific T cell and B cell immune response caused by Mycobacterium tuberculosis infection, and the false positive caused by the impure antigen can be reduced compared with the use of the complete antigen in the prior art; and the detection reagents prepared from the antigen protein Rv0446c and the T-cell epitope peptide thereof can be widely used for assisted diagnosis of tuberculosis, epidemiological surveillance and other related fields, and the tuberculosis vaccines and the anti-tuberculosis drugs prepared from the antigen protein Rv0446c and the T-cell epitope peptide thereof can be used for prevention and treatment of tuberculosis.

The invention discloses a mycobacterium tuberculosis surface lipolysaccharide-antistatic nucleic acid aptamer and application thereof. The aptamer is a small molecular single-stranded deoxyribonucleic acid (ssDNA) which is specific to toxic mycobacterium tuberculosis surface lipolysaccharide ManLAM (Mannosylated Lipoarabinomannan) and has tuberculosis infection resisting and cellular immunity enhancing functions, and the nucleotide sequence of the ssDNA is shown as SEQIDNo.1. The small molecular ssDNA has a novel target spot and a novel structure which are different from those of the conventional anti-tuberculosis medicament, and has the immunologic suppression function of directly enclosing the ManLAM. The aptamer is easy to prepare and has low price; the obtained ssDNA aptamer is specifically combined on the surface of toxic mycobacterium tuberculosis; and the treatment targeting is further enhanced. The problems of increasing medicament tolerance and large side effect existing in the conventional treatment of tuberculosis are solved, and the aptamer can be taken as an effective novel anti-tuberculosis medicament or a tuberculosis diagnosis reagent.

The invention relates to a shikimic acid compound and a preparation method and application thereof. Specifically, the invention relates to the shikimic acid compound having the following structural general formula, wherein the definition of each substituting group is as shown in the specification. The shikimic acid compound can be used for preparing anti-tumor and/or anti-tuberculosis medicaments.

The present invention relates to a biodegradable microparticle composition useful for the target specific drug delivery to manage pulmonary tuberculosis, said composition comprising two anti-tuberculosis drugs, and a biodegradable polymer for drug delivery in a ratio of about 1:2 to 2:1, wherein the anti-tubercular drugs are in the ratio of 1:2 to 2:1, also, a process for the preparation of the composition, and lastly, a method of treating pulmonary tuberculosis in a subject, said method comprising administering by inhalation alone or in combination with oral route, pharmaceutically effective amount of the composition to the subject in need thereof, wherein the dosage for inhalation is ranging between 0.5 to 10 mg/kg body weight/day and that for oral route is ranging between 4 to 32 mg/kg body weight/day.

The invention relates to a special Chinese patent medicine for resisting phthisis-astragalus fritillaria capsules, which is prepared from 120-150g of radix astragali, 20-50g of aweto, 80-100g of gecko, 50-80g of fritillaria cirrhosa, 50-70g of stemona, 48-70g of lily root, 30-50g of ginkgo, 56-76g of hyacinth bletilla, 120-150g of coix seed, 20-50g of radix glehniae, 80-102g of radix rehmanniae preparata, 60-85g of radix ophiopogonis, 55-75g of tuckahoe, 80-130g of taraxacum and 60-75g of oyster. The Chinese patent medicine not only can be made into capsules according to the formula of the composition, but also can be made into tablets, pills, powder and oral liquids according to the formula of the composition. The capsules are prepared from Chinese medicinal herbs, and can treat tuberculosis (mainly phthisis) by utilizing the comprehensive conditioning actions of the Chinese medicinal herbs; the capsules can not generate toxic or side effect, and also can not generate drug resistance, and the effective rate is up to more than 95%; and the capsules can be combined with other antituberculosis medicines to enhance the curative effect (especially for drug-resistant strain infected cases), and can also be independently used for patients who are allergic to western antituberculosis medicines or can not stand for the toxic or side effect.

The invention relates to a quinoline carboxylic acid derivative containing isatin substitute, a preparation method, medical purposes, and an anti-tuberculosis drug combination containing the quinoline carboxylic acid derivative. More specifically, the invention relates to a new fluoroquinolone carboxylic acid derivative. The 7-site of the derivative on a quinoline core is 3-[N- methyl-N-2-(beta-substitute imino isatin-1-radical) ethyl] amino-1- piperidyl, the 8-site is methoxy group, and the 1-site is cyclopropyl. Compared with the traditional clinical anti-tuberculosis drug of a fluoroquinolone class (such as Ciprofloxacin), the quinoline carboxylic acid derivative has more excellent anti-tuberculosis mycobacterium activity.

The invention discloses mycobacterium tuberculosis fusion protein EAMMH and a constructing, expressing and purifying method and application thereof. The fusion protein is expressed in a soluble form, and greatly improves EAMM inclusion body form expression weakness. Tuberculosis subunit vaccine (LT69) constructed by combination of the fusion protein and an adjuvant has strong protective immunity, is superior to traditional BCG (Bacillus Calmette-Guerin) vaccine and EAMM+MH combined vaccine; the vaccine as an enhanced vaccine can significantly enhance the BCG initial immune immunity and protection effect of anti tuberculosis, and to a certain extent, reduces the pathological injury of the lung; in addition, the subunit vaccine contains a wide variety of antigens of growth period and latency period of mycobacterium tuberculosis, can induce strong specific cellular immune and humoral immune response aiming at each period of tubercle bacillus antigen, has protective effect on the tubercle bacillus in different metabolic states, is long in protection time, and is expected to become an effective vaccine for clinical tuberculosis prevention.

The invention relates to a novel mycobacterium tuberculosis specific fusion protein as well as preparation and application thereof and belongs to the technical field of tuberculosis medical immunologic diagnosis. The fusion protein is formed by sequentially connecting antigenic epitopes of two proteins Rv0057 and Rv1352, wherein the nucleotide sequence of the antigenic epitope of the protein Rv0057 is shown in a sequence 1 in a sequence table; and the nucleotide sequence of the antigenic epitope of the protein Rv1352 is shown in a sequence 2 in a sequence table. Compared with the current commercial antibody detection kit, the mycobacterium tuberculosis specific fusion protein disclosed by the invention has the advantages of high sensitivity, strong specificity and complementarity with other antigens in the aspect of tuberculosis serodiagnosis, and can be used for detecting specific anti-tuberculosis antibodies in body fluid samples such as blood serum and pleural effusion.

The present invention relates to a biodegradable microparticle composition useful for the target specific drug delivery to manage pulmonary tuberculosis, said composition comprising two anti-tuberculosis drugs, and a biodegradable polymer for drug delivery in a ratio of about 1:2 to 2:1, wherein the anti - tubercular drugs are in the ratio of 1:2 to 2:1, also, a process for the preparation of the composition, and lastly, a method of treating pulmonary tuberculosis in a subject, said method comprising administering by inhalation alone or in combination with oral route, pharmaceutically effective amount of the composition to the subject in need thereof, wherein the dosage for inhalation is ranging between 0.5 to 10 mg/kg body weight/day and that for oral route is ranging between 4 to 32 mg/kg body weight/day.