19 results about "Monoamine Oxidase Type B" patented technology

The present invention relates to the field of medical technology, and in particular to a compound of formula (I) which is a dual inhibitor of butyrylcholinesterase and monoamine oxidase B, and a preparation method and application thereof.

The invention belongs to the technical field of active substance screening, and particularly relates to a method for high-throughput screening of a monoamine oxidase B inhibitor. The method comprises the following steps: incubating monoamine oxidase B and a drug-containing brain homogenate extracting solution, removing components which are not specifically bound by using an affinity ultrafiltration technology, eluting by using methanol to obtain a potential ligand, and identifying by using UPLC-Q-Exactive-MS (Ultra Performance Liquid Chromatography-Quantitative Exactive-Mass Spectrometry). Meanwhile, inactivated monoamine oxidase B is used as a control, interference of the control, false positive and non-specific binding is eliminated, the in-vitro monoamine oxidase B inhibition effect of the identification ligand is measured, and the result proves that the compound screened by using the affinity ultrafiltration-liquid chromatography-mass spectrometry technology has the monoamine oxidase B inhibition activity. The method disclosed by the invention is rapid, simple, convenient, stable, high in precision and good in reproducibility, and has a wide application prospect in the aspect of rapidly screening target compounds in natural medicines.

One aspect provides a pharmaceutical composition for preventing or treating metabolic diseases or autoimmune diseases, the composition comprising a novel terthiophene derivative compound or a pharmaceutically acceptable salt thereof. The pharmaceutical composition effectively inhibits monoamine oxidase B (MAO-B), and thus can be used in various fields for the prevention or treatment of metabolic diseases, such as obesity and fatty liver, or autoimmune diseases, such as rheumatoid disease.

The invention provides a plant-derived active polypeptide and application thereof in prevention or treatment of Parkinson's syndrome, and belongs to the technical field of polypeptide bioengineering. The amino acid sequence of the active polypeptide is MKGASSIMYALG, and the active polypeptide is prepared from Fuding white tea raw materials through a directional two-step enzymolysis process. According to the polypeptide, the damage of 6-OHDA induced BZ555 nematode dopaminergic neurons can be remarkably reduced, and the dyskinesia of Parkinson's syndrome model animals can be remarkably improved; meanwhile, the expression level of proinflammatory factors such as IL-1beta and IL-18 in serum of a model mouse can be lowered, the content of dopamine in a nigra area of brain tissue of the model mouse can be increased, and the activity of monoamine oxidase B can be reduced. The results show that the Fuding white tea-derived active polypeptide has exact prevention and treatment effects on Parkinson's syndrome, and has important development value and wide application prospects in the field of medicines.

The application belongs to the technical field of medicine, and relates to a monoamine oxidase B inhibitor and a pharmaceutical application thereof. The monoamine oxidase B is a coumarin compound, and has the characteristics of high activity, high selectivity, high blood-brain barrier permeability and low neurocyte toxicity. The monoamine oxidase B can be clinically used for treating Parkinson's disease, Alzheimer's disease, neurodegenerative disease and depression.

The present invention relates to antisense oligomers against monoamine oxidase B and uses thereof, and more particularly, to antisense oligomers that modulate the expression level of a gene encoding monoamine oxidase B, specifically the mRNA of the gene, or a protein encoded thereby, and uses thereof for preventing, alleviating or treating liver disease, obesity or neurological disease.

The present invention provides a compound represented by formula (I) that can image monoamine oxidase-B with high specificity and selectivity for monoamine oxidase-B and with good sensitivity, or a pharmaceutically acceptable salt or solvate thereof.

This invention relates to the fields of radiopharmaceutical chemistry and clinical nuclear medicine, specifically to an aryl benzyl ether compound with high affinity for monoamine oxidase B (MAO-B) and its applications. This aryl benzyl ether compound has the structure of general formula (I). After radiolabeling, this compound and its derivatives can be used to image MAO-B in the brain, serving as molecular probes for direct targeting of MAO-B and potential surrogate markers for reactive astrocytes.

Provided are a cannabichromenic acid derivative, a method for preparing same, and a composition for cognitive function improvement comprising same, in which the cannabichromenic acid derivative exhibits acetylcholinesterase inhibitory activity and butyrylcholinesterase inhibitory activity, as well as inhibitory activity against monoamine oxidase B, therefore simultaneously treating a decrease in acetylcholine levels in brain tissue and a decrease in blood butyrylcholine levels, shown in patients with dementia, and providing a more effective cognitive function improvement treatment by preventing brain cell damage.

This invention provides a plant-derived bioactive polypeptide and its use in the prevention or treatment of Parkinson's syndrome, belonging to the field of polypeptide bioengineering technology. The amino acid sequence of the bioactive polypeptide is MKGASSIMYALG, and it is prepared from Fuding white tea raw materials through a directed two-step enzymatic hydrolysis process. This polypeptide can significantly alleviate 6-OHDA-induced damage to dopaminergic neurons in BZ555 nematodes and significantly improve motor dysfunction in Parkinson's syndrome model animals. Simultaneously, it can downregulate the expression levels of pro-inflammatory factors such as IL-1β and IL-18 in the serum of model mice, upregulate dopamine content in the substantia nigra region of brain tissue in model rats, and reduce monoamine oxidase B activity. These results indicate that the Fuding white tea-derived bioactive polypeptide of this invention has definite preventive and therapeutic effects on Parkinson's syndrome, and has significant development value and broad application prospects in the pharmaceutical field.

The present invention relates to novel compounds which are capable of inhibiting semicarbazide-sensitive amine oxidase (SSAO / VAP-1) and monoamine oxidase B (MAO-B). These compounds are useful for treatment of a variety of neuromuscular diseases, such as muscular dystrophies, and neuroinflammatory diseases, including both peripheral and central disorders 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.

The invention provides a specific fluorescent probe for human monoamine oxidase B. The invention also provides a preparation method of the specific fluorescent probe of the human monoamine oxidase B. According to the specific fluorescent probe of the human monoamine oxidase B, high-precision imaging of living cell mitochondria is achieved through a double-targeting mechanism of enzyme aiming and charge driving, the selectivity of hMAO-B is obviously higher than that of hMAO-A, and the specific fluorescent probe has high specificity and can be used for early diagnosis and curative effect monitoring of neurodegenerative diseases (such as Parkinson's disease and Alzheimer's disease).

The invention discloses a benzoxo (carbon / sulfur) aza compound and application thereof. The structural general formula of the benzoxo (carbon / sulfur) aza compound is shown as the following formulas (I) and (II): # imgabs0 #, wherein A is selected from methyl (raceme, R configuration and S configuration), ethyl (raceme, R configuration and S configuration) or cyclopropyl; x1 is selected from oxygen, ammonia or sulfur; x2 is selected from methylene, oxygen or sulfur; r1 is selected from hydrogen, fluorine, chlorine, bromine or methyl; r2 is selected from hydrogen, fluorine, chlorine, bromine or methyl. The benzoxo (carbon / sulfur) aza compound disclosed by the invention has good monoamine oxidase B inhibitory activity, and shows extremely high selectivity in a monoamine oxidase family; in a mouse Parkinson's disease model, the benzoxo (carbon / sulfur) aza compound disclosed by the invention shows a relatively good treatment effect.

The invention relates to application of an MAO-B inhibitor in preparation of a medicine for treating neurodegenerative diseases, and belongs to the technical field of medicines. The tussilagone is found to have a monoamine oxidase B inhibition effect for the first time, and can be used for preventing and treating neurodegenerative diseases caused by overexpression of monoamine oxidase B. According to the invention, zebra fish is used as a model animal for detection to find that tussilagone can achieve the protection effect of a second-generation MAO-B inhibitor rasagiline (Rasagiline), and tussilagone is a potential compound for preventing and treating the Parkinson's disease, has important significance in research on treatment and prevention of the Parkinson's disease, and has a wide market prospect.

The present invention relates to antisense oligomers against monoamine oxidase B and uses thereof, and more particularly, to antisense oligomers that modulate the expression level of a gene encoding monoamine oxidase B, specifically the mRNA of the gene, or a protein encoded thereby, and uses thereof for preventing, alleviating or treating liver disease, obesity or neurological disease.

The present invention relates to novel compounds capable of inhibiting semicarbazide-sensitive amine oxidase (SSAO / VAP-1) and monoamine oxidase B (MAO-B). These compounds can be used to treat a variety of neuromuscular diseases, such as muscular dystrophy, and neuroinflammatory diseases, including peripheral and central diseases in human subjects, as well as peripheral and central diseases in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.

The present invention relates to an antisense oligomer against monoamine oxidase B and its use, and to an antisense oligomer that regulates the amount of a gene encoding monoamine oxidase B, specifically mRNA or protein, and its use for the prevention, alleviation or treatment of liver diseases, obesity or neurological diseases.

The application discloses a monoamine oxidase B inhibitor and a pharmaceutical application thereof. A beta-carboline compound or a pharmaceutically acceptable salt thereof is shown in formula (I): R 1 is H or halogen; R 2 is H or halogen; X is O or NH; R 3 is,,,,,,,,,, or. The application discloses a use of the beta-carboline compound or the pharmaceutically acceptable salt thereof in preparation of a high-efficiency, high-selectivity and reversible MAO-B inhibitor. The application discloses a use of the beta-carboline compound or the pharmaceutically acceptable salt thereof in preparation of a drug for treating and / or preventing a monoamine oxidase B-mediated disease.

This invention discloses a benzo[a]oxo(carbon / sulfur)nitrogen compound and its applications. The general structural formulas of the benzo[a]oxo(carbon / sulfur)nitrogen compounds of this invention are shown in formulas (I) and (II): wherein: A is selected from methyl (racemic, R configuration, S configuration), ethyl (racemic, R configuration, S configuration), or cyclopropyl; X1 is selected from oxygen, ammonia, or sulfur; X2 is selected from methylene, oxygen, or sulfur; R1 is selected from hydrogen, fluorine, chlorine, bromine, or methyl; R2 is selected from hydrogen, fluorine, chlorine, bromine, or methyl. The benzo[a]oxo(carbon / sulfur)nitrogen compounds of this invention exhibit good monoamine oxidase B inhibitory activity and show extremely high selectivity within the monoamine oxidase family; in a mouse Parkinson's disease model, the benzo[a]oxo(carbon / sulfur)nitrogen compounds of this invention show good therapeutic effects.