47 results about "Myeloperoxidase" patented technology

The present invention relates to novel compounds which are capable of inhibiting semicarbazide-sensitive amine oxidase and myeloperoxidase. These compounds are useful for the treatment of a variety of inflammatory indications, e.g., autoimmune diseases, respiratory disease, fibrosis, vasculitis, neurological diseases or disorders, and the complications resulting from infectious disease, obesity, diabetes / metabolic syndrome and / or cardiovascular disease in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.

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 invention discloses a combined lactobacillus salivarius CCFM1397 for improving osteoblast activity and relieving bone resorption and periodontal tissue damage and a metagen thereof, and belongs to the technical field of microorganisms. The lactobacillus salivarius combination CCFM1397 provided by the invention is separated from oral dental plaque of healthy teenagers, has the effects of relieving bone resorption and resisting inflammation, and is specifically reflected in that: the expression of MC3T3-E1 cell osteoprotegerin (OPG) protein and gene level is improved in vitro; the bone absorption amount of orthodontic bone absorption rat alveolar bone is reduced, the number of alveolar bone osteoclasts is reduced, and the level of rat serum OPG is improved; the secretion of inflammatory factors IL-1beta, IL-6 and TNF-alpha and myeloperoxidase MPO of the orthodontic bone absorption rats is reduced; and the pathological condition of orthodontic bone absorption rat alveolar bone tissue is improved. Therefore, the combined lactobacillus salivarius has a huge application prospect in products for relieving bone resorption and assisting in inhibiting periodontal tissue inflammation.

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)

A method of treating systemic lupus erythematosus in a subject is provided in which a therapeutically effective amount of PIC1 is administered to the subject. A method of treating transfusion-related acute lung injury is also provided where a therapeutically effective amount of PIC1 is administered to the subject. PIC1 can modulate immune complex activation of the complement system and NET formation in the subject. PIC1 can also inhibit myeloperoxidase (MPO) activity in the subject.

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.

The present invention relates to a method for preparing a releasate from a buffy coat sample obtained from one or more subjects comprising the steps of: a) contacting said sample with at least 1 µmol of one or more water-soluble calcium salts per ml of said sample thereby obtaining a mixture; b) allowing the mixture obtained in step a) to coagulate, thereby obtaining a coagulum, blood cells, and releasate; and c) recovering the releasate obtained in step b) from the mixture. Also provided herein is a releasate, such as a releasate obtained by the aforementioned method, comprising at least 1.0 µg / mL of myeloperoxidase (MPO) and / or having an MPO activity of 60 U / mL, and the uses thereof, such as in cell culture or tissue culture.

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.

The present invention belongs to the technical field of medicinal chemistry, and specifically relates to a coumarin selenoether thiazolylhydrazone derivative, a preparation method thereof, and an application thereof. The coumarin selenoether thiazolylhydrazone derivative has a chemical structural formula shown in Formula I. Based on the principle of drug design and splicing, the present invention designs and synthesizes a series of coumarin selenoether thiazolylhydrazone derivatives, a total of 8 coumarin selenoether thiazolylhydrazone compounds. All 8 coumarin selenoether thiazolylhydrazone compounds have good free radical scavenging ability. The coumarin selenoether thiazolylhydrazone derivative mainly binds to myeloperoxidase through π-H interaction and hydrogen bond force, and has the potential to become a myeloperoxidase inhibitor.

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.