40 results about "Myeloperoxidase" patented technology

Compounds of formula (I), processes for their preparation and their use in medicine. Specifically, provided are compounds of formula (I) or stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, and also relate to pharmaceutical compositions containing these compounds and uses of the compounds in drugs for treatment and / or prevention of cardiovascular diseases. These compounds are inhibitors of myeloperoxidase (MPO). # imgabs0 #

The application belongs to the technical field of biological detection, and discloses a cardiovascular marker control article and a preparation method thereof. The cardiovascular marker control article comprises a serum matrix, antigens, a preservative and a stabilizer. The antigens include cardiac troponin I antigens, creatine kinase isoenzyme antigens, myoglobin antigens, amino-terminal brain natriuretic peptide precursor antigens, brain natriuretic peptide antigens, D-dimer antigens, heart-type fatty acid-binding protein antigens, myeloperoxidase antigens and lipoprotein phospholipase A2 antigens. The stabilizer includes at least one of D-trehalose, sucrose, glycine, inositol and polyethylene glycol. The cardiovascular marker control article can cover various cardiovascular disease markers, including heart failure, pulmonary embolism, vasculitis and atherosclerosis, myocardial injury, myocardial infarction and the like. The control article can be used as a third-party control article for indoor and inter-laboratory quality control of a cardiovascular disease screening and auxiliary diagnosis measurement system.

The invention discloses a preparation method and application of hydrogen sulfide donor modified polylysine responding to myeloperoxidase. The hydrogen sulfide donor modified polylysine has the effects of eliminating hypochlorous acid and releasing hydrogen sulfide, and a final product C, namely the hydrogen sulfide donor modified polylysine, is obtained by combining the biological material A with a polylysine molecule B modified with the hydrogen sulfide donor based on myeloperoxidase response. A donor capable of releasing hydrogen sulfide molecules under the action of hypochlorous acid generated by myeloperoxidase is modified into a polylysine structure, so that the functions of effectively relieving wound inflammation and promoting angiogenesis are realized. Specifically, polylysine is widely applied to the field of wound repair due to excellent biocompatibility and antibacterial activity. Besides, donor molecules capable of responding to hydrogen sulfide release of myeloperoxidase are introduced, so that the anti-inflammatory effect is further enhanced, the proinflammatory factor level is remarkably reduced, and angiogenesis is promoted.

The technology relates to a method for detecting high-risk unstable atherosclerotic plaque in a subject, the method comprising: a) administering to the subject a magnetic resonance imaging (MRI) contrast agent capable of being activated by myeloperoxidase (MPO) in atherosclerotic plaque; b) allowing the contrast agent to be activated by myeloperoxidase in atherosclerotic plaque; c) obtaining an image of the atherosclerotic plaque from the subject using such molecular MRI, wherein enhanced imaging is indicative of unstable plaque. In some embodiments an MPO inhibitor is administered to a subject identified as having a high-risk unstable atherosclerotic plaque.

A compound of formula (I), and a preparation method therefor and a use thereof in medicine. Specifically, the present invention provides a compound of formula (I) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, and also relates to a pharmaceutical composition containing the compound and a use of the compound in the preparation of a drug for treating and / or preventing cardiovascular diseases. The compound is an inhibitor for myeloperoxidase (MPO).

The present invention relates to the field of enzymology. More particularly, the present invention relates to artificial bifunctional enzymes and their applications.

Crystalline 2-thioxo-1-((2-((2R,4S)-4-(trifluoromethyl)piperidin-2-yl)pyridin-3-yl)methyl)- 1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one (compound 1) in form A and crystalline 2- thioxo-1-((2-((2R,4S)-4-(trifluoromethyl)piperidin-2-yl)pyridin-3-yl)methyl)-1,2,3,5-tetrahydro- 4H-pyrrolo[3,2-d]pyrimidin-4-one (compound 1) dihydrate in form B.

The invention provides an anti-neuroinflammation medicine as well as a preparation method and application thereof. The anti-neuroinflammation medicine comprises an active component and lipidosome, the active component is an inhibitor 4-aminobenzoyl hydrazine of myeloperoxidase; the liposome is prepared from phospholipid, cholesterol and distearoyl phosphatidyl ethanolamine-thioketal-polyethylene glycol; the method comprises the following steps: weighing lipidosome and 4-aminobenzoyl hydrazine, dissolving, and carrying out rotary evaporation to obtain a lipid membrane; adding a phosphate buffer solution into the lipid membrane, stirring in a water bath, performing ultrasonic treatment, filtering, centrifuging and purifying to obtain the medicine, according to the active oxygen response-based liposome delivery system disclosed by the invention, 4-aminobenzoyl hydrazine is encapsulated in liposome to form a drug, and after the drug enters a brain inflammation microenvironment area of the Alzheimer's disease, the active oxygen can break a thioketal bond, so that local release of 4-aminobenzoyl hydrazine is triggered, targeted inhibition of myeloperoxidase is realized, and the drug delivery effect is improved. The oxidative stress level is reduced, the neuroinflammation is relieved, and the cognitive impairment is effectively improved.

The invention relates to application of folliclostatin in treatment of inflammatory bowel diseases, and belongs to the technical field of biological medicines. The invention provides application of folliclostatin FST in preparation of a medicine for treating acute inflammatory bowel disease. The invention relates to an application of folliclostatin FST in preparation of a medicine for treating acute inflammatory bowel disease by inhibiting myeloperoxidase. The invention relates to an application of folliclostatin FST in preparation of a medicine for treating chronic inflammatory bowel diseases. The invention relates to an application of folliclostatin FST in preparation of a medicine for treating chronic inflammatory bowel disease by improving mesenteric fat quality. The invention relates to an application of folliclostatin FST in preparation of drugs for treating inflammatory bowel diseases by blocking Th17 induction effect of activin A. The folliclostatin FST can be used for treating inflammatory bowel diseases. The invention discloses the treatment effect of FST, and discloses a new target spot of IBD treatment, namely an FST-activin A-Th17 axis, which has important clinical significance and transformation value.

The application belongs to the technical field of chemical drugs, and particularly relates to a pyrazole compound and a preparation method and application thereof. The application provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, which not only has good myeloperoxidase (MPO) inhibitory activity, but also can be used for treating and / or preventing cardiovascular diseases. (I)

Provided herein are compounds useful as imaging agents. Exemplary compounds provided herein are useful as myeloperoxidase imaging agents using positron emission tomography or fluorescence imaging techniques. Methods for preparing the compounds provided herein and diagnostic methods using radiolabeled arid unlabeled compounds are also provided.

The present invention relates to the field of in vitro detection technology. Specifically, a fluorescent probe for detecting myeloperoxidase, a preparation method, and an application thereof are provided. The fluorescent probe has the following general structural formula: wherein R1 and R2 are each independently selected from hydrogen, a substituted or unsubstituted aliphatic hydrocarbon group, a substituted or unsubstituted alicyclic hydrocarbon group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group; and X ‑ The fluorescent probe of the present invention can directly and quickly measure the MPO content in biological samples.

The present invention discloses a fluorescent diagnostic and therapeutic prodrug and its application in the selective detection and drug release of acute myeloid leukemia (AML) cells with high expression of myeloperoxidase (MPO). The fluorescent diagnostic and therapeutic prodrug FNC constructed by the present invention can selectively detect ClO in AML cells with high MPO expression ‑ . This fluorescent prodrug can be used to identify AML cells with high MPO expression and perform selective drug release. FNC can also be used as a cell differentiation indicator.

The present invention relates to a CXCR4 inhibitor compound for use in the treatment of a severe acute respiratory distress syndrome (sARDS), wherein the sARDS is characterized by a dysregulation of NETosis which may be measured by the plasmatic levels of cDNA, citrullinated histone H3, neutrophil elastase, interleukin-8, myeloperoxidase-DNA complexes and / or calprotectin. The present invention also relates to a method of prognostic of severe ARDS, a pharmaceutical composition for use in the treatment of severe acute respiratory distress syndrome (ARDS), a kit of prognostic of severe ARDS in a subject and the use of NETosis biomarkers.

The present invention relates to a CXCR4 inhibitor compound for use in the treatment of a severe acute respiratory distress syndrome (sARDS), wherein the sARDS is characterized by a dysregulation of NETosis which may be measured by the plasmatic levels of cDNA, citrullinated histone H3, neutrophil elastase, interleukin-8, myeloperoxidase-DNA complexes and / or calprotectin. The present invention also relates to a method of prognostic of severe ARDS, a pharmaceutical composition for use in the treatment of severe acute respiratory distress syndrome (ARDS), a kit of prognostic of severe ARDS in a subject and the use of NETosis biomarkers.

The application provides a fluorescent probe for myeloperoxidase detection, and a preparation method and application thereof. The fluorescent probe can detect MPO in living cells, greatly shortens the detection time, has low production cost, high specificity, and can be fixed on the protein of the cell after response, thereby avoiding non-specific fluorescent signal transmission and reducing false positives in the detection process. Meanwhile, the fluorescent probe can realize the function of distinguishing myeloid leukemia cells from lymphoid leukemia cells.

A joint detection kit for detecting intestinal polyp factors, and a preparation method therefor, a detection method therefor and the use thereof. The joint detection kit at least comprises a plurality of test strips for detecting the following indicators: M2-pyruvate kinase, matrix metalloproteinase 9, myeloperoxidase, glutathione S-transferase Pi, cytidine deaminase, retinol binding protein 4, serine protease inhibitor F2, calprotectin and fecal occult blood. Conjugate pads (2) of each reagent strip are coated with detection antibody-colloidal gold conjugates. Detection lines (3) of the reagent strip are coated with specific capture antibodies, and the specific capture antibodies on each test strip are different. The joint detection performed by the joint detection kit can effectively improve the sensitivity and specificity of the detection on intestinal polyps. The detection time is merely 15 min, with the detection rate of more than 91%. Therefore, the accuracy on the detection and diagnosis of colorectal cancer caused by intestinal polyps is improved.

There are disclosed certain 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one compounds of formula (I),and pharmaceutically acceptable salts thereof, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions.

The present invention relates to hydrogen sulfide (H2S) releaser compounds and compositions for use in the treatment of myeloperoxidase (MPO) induced neutrophil mediated tissue damage, in particular positive anti-neutrophil cytoplasmic autoantibody (ANCA) associated vasculitis (AAV), comprising myeloperoxidase granulomatous polyvasculitis (Wegner's granulomatous disease), eosinophilic granulomatous polyvasculitis (EGPA; ), polyvasculitis under microscope (MPA), and various forms of diseases in various organs, such as kidney and lung.

This invention discloses a sulfur-containing 5-aminosalicylic acid prodrug and its uses, belonging to the field of biomedical technology. The sulfur-containing 5-aminosalicylic acid prodrug of this invention has the structure shown in general formula I. This type of compound has good intervention effects on inflammation-related diseases, exhibiting more ideal anti-inflammatory activity than 5-ASA and sulfasalazine. It can also inhibit the production of hypochlorous acid and related inflammatory mediators by inhibiting myeloperoxidase (MPO), and can be used to prepare drugs for the prevention and / or treatment of inflammatory bowel disease, and drugs for the prevention and / or treatment of diseases related to abnormal oxidative stress.

The invention belongs to the technical field of medicines, and provides a medicine capable of preventing and treating gastric ulcer. Evaluation of the acute gastric ulcer treatment effect of early chick embryo amniotic fluid finds that the early chick embryo amniotic fluid can reduce the gastric tissue ulcer area and inflammatory factor infiltration, and the protective effect of the mucosal barrier on the gastric tissue is enhanced by reducing the calcium ion content in the gastric tissue and myeloperoxidase, so that the gastric ulcer treatment effect is improved. In addition, the oxidative stress level caused by ethanol is obviously inhibited, and the level of tight junction protein of stomach tissue is up-regulated. The invention has the potential of treating gastric ulcer.

The invention discloses a bioluminescence kit for detecting myeloperoxidase in whole blood as well as a use method and application of the bioluminescence kit. The bioluminescence kit comprises a nucleic acid hairpin probe, H2O2, NaCl, a PBS (Phosphate Buffer Solution), a Cas12a / crRNA binary complex, a bioluminescence type molecular beacon, an NEBuffer 2.1 and a luminescent substrate Furimazine. The 5'end and the 3 'end of the bioluminescence type molecular beacon are respectively marked with Cy3 and cpHNLuc, and a bioluminescence resonance energy transfer phenomenon (BRET) can occur. A BRET signal does not need an external excitation light source, interference of autofluorescence of a blood sample and environmental factors can be effectively avoided, meanwhile, the excellent signal amplification capacity of a CRISPR / Cas12a system is combined, rapid and ultra-sensitive detection of MPO in a whole blood sample can be achieved, and therefore the method has a great application prospect in the fields of biosensing and medical examination.

The invention discloses a synthesis method and application of a mitochondrial division inhibitor 1 with myeloperoxidase responsiveness and fluorescence biological imaging capability, the mitochondrial division inhibitor 1, 5-hydroxytryptamine and carbon quantum dots are integrated through a chemical bonding method, and a novel multifunctional nano system CDs-5HT-Mdivi-1 is obtained. The synthesized CDs-5HT-Mdivi-1 is of a lattice structure, the diameter is 2.51 + / -0.88 nm, the height is 2.5 nm, the surface potential is 16.01 + / -0.78 mV, medicine targeted accumulation, synergistic interaction and diagnosis and treatment integration under MPO triggering can be achieved, myocardial infarction can be treated in a targeted mode, and myocardial ischemia reperfusion injury can be improved.

This disclosure relates to a method for identifying subjects likely to respond to treatment with myeloperoxidase (MPO) inhibitors based on neutrophil levels and / or concentrations of at least one protein biomarker. This disclosure further relates to a method for selecting subjects for treatment with MPO inhibitors, a method for predicting whether subjects will respond to treatment with MPO inhibitors, and a method for treating subjects likely to respond to treatment with MPO inhibitors. This disclosure further relates to a method for predicting improved clinical response in subjects with MPO-related disorders after treatment with MPO inhibitors.

The present disclosure relates to methods of identifying a subject likely to respond to treatment with a myeloperoxidase (MPO) inhibitor based on neutrophil levels and / or a concentration of at least one protein biomarker in the subject. The disclosure also relates to methods of selecting a subject for MPO inhibitor treatment, methods of predicting whether a subject will respond to MPO inhibitor treatment, and methods of treating a subject likely to respond to MPO inhibitor treatment. The present disclosure also relates to a method of predicting an improved clinical response in a subject having an MPO-related disorder following treatment with an MPO inhibitor.

The application discloses a lactobacillus gasseri for repairing a vaginal barrier and relieving a vaginal infection, and a postbiotic thereof, and belongs to the technical field of microorganisms.The lactobacillus gasseri and the postbiotic thereof can repair a vaginal barrier and relieve a vaginal infection when being used externally.The lactobacillus gasseri is separated from vaginal secretion of a healthy female, has the functions of repairing a vaginal mucosa barrier and relieving a vaginal infection, and specifically has the following effects: improving a cell monolayer barrier transendothelial electrical resistance value, increasing integrity, reducing FITC-labeled dextran permeability of the cell monolayer barrier, and reducing permeability;adjusting a mouse vaginal mucin level;improving a mouse vaginal tissue protein expression level;reducing mouse vaginal tissue IL-1 beta secretion and myeloperoxidase content;and improving a mouse vaginal tissue pathological condition.Therefore, the lactobacillus gasseri has great application prospects in products for repairing a vaginal mucosa barrier and relieving a vaginal infection caused by pathogenic bacteria.

This invention discloses a myeloperoxidase-responsive fluorescent probe liposome, its preparation method, and its applications. The raw materials for this fluorescent probe liposome include lecithin, cholesterol, collagen, luminol, and Cy5. These raw materials are prepared using a thin-film dispersion method to obtain the fluorescent probe liposome. This invention combines luminol with Cy5, solving the problem of low sensitivity or even undetectability of luminol to deep inflammatory foci in body tissues. It enables imaging detection of deep inflammatory cells in the body, which has significant application value in evaluating inflammatory responses caused by tumors, epilepsy, etc., and is of great significance for guiding clinical treatment of tumors and epilepsy and assessing efficacy.

The invention belongs to the technical field of chemical drugs, and relates to application of a myeloperoxidase (MPO) inhibitor in preparation of drugs for preventing and / or treating non-alcoholic fatty liver diseases.

A method of determining a likelihood of developing cancer therapy-related cardiac dysfunction (CTRCD) in a subject receiving an anthracycline and / or HER2 targeted therapy cancer treatment. Also disclosed herein is a method for treating a subject who is identified as being at risk of developing CTRCD. This disclosure also relates to a method of identifying if a subject with cancer to be treated with or an anthracycline and / or a HER2 targeted therapy treatment is likely to benefit from a cardioprotective treatment. Further disclosed is a panel or kit, the panel or kit comprising a plurality of detection agents specific for each of a set of biomarkers in a sample obtained from a subject with cancer, optionally selected from: angiopoietin-2 (ANGPT2), Endoglin (ENG), E-selectin, endothelin-1 (ET-1), myeloperoxidase (MPO), Interferon gamma-induced protein-10 (IP-10) and Interferon-α, and optionally a solid support.