62 results about "Cholinesterase" patented technology

The invention discloses a rapid screening and detecting method for vegetable pesticide residues, a multi-dimensional judgment basis is provided for pesticide residue detection by combining a PCR amplification result with the inhibition rate of acetylcholin esterase and butyrylcholin esterase, different types of pesticides may induce different gene expression changes, and the detection result is accurate. According to the rapid screening and detecting method for the pesticide residues in the vegetables, the accuracy of a detection result is improved, meanwhile, the variety of the pesticide residues in the vegetables can be accurately determined, the defect that specific pesticide varieties are difficult to distinguish by purely relying on an enzyme inhibition method is overcome, and the detection result is more targeted and accurate.

The invention discloses a synthetic carbamate compound based on 3-substituted dioxazolone as well as a preparation method and application of the synthetic carbamate compound, and belongs to the technical field of organic synthesis. The synthesis method comprises the following steps: (1) preparing 3-substituted dioxazolone from hydroximic acid with different substituent groups and phosgene under an ice bath condition; and (2) reacting the 3-substituted dioxazolone obtained in the step (1) with different phenols (alcohols) under an alkaline condition to obtain corresponding carbamate compounds. According to the method, the yield of carbamate is further improved by adjusting the conditions of alkali, equivalent weight, temperature and the like; the preparation method provided by the invention is novel and has the advantages of mild reaction conditions, few generated impurities, high yield, high safety, convenience in operation and the like; and the compound shows good cholinesterase activity in activity screening, and can be used in insecticides or pesticides.

The present application belongs to the technical field of pharmaceutical therapy, and particularly relates to an amide-substituted tryptophan ketone derivative, a preparation method and application thereof. The structural formula of the tryptophan ketone derivative is shown in formula (A) or formula (B). In the formula, n=1 or 2, and R is any one of dimethylamine group, diethylamine group, morpholine group, 1-methylpiperazine group, cyclopropylamine group and 4-hydroxypiperidyl group. The compound can selectively inhibit the activity of acetylcholinesterase, and has the potential to develop into a drug for treating Alzheimer's disease due to the abilities of self-aggregation and the like. 1‑42 ​

The invention relates to an asymmetric iridium monatomic nano enzyme Ir-S / N-C and a preparation method thereof. S atoms are introduced, an active center with an Ir-S1N3 asymmetric coordination structure is constructed, the electronic structure of the iridium active center is effectively changed, the center position of a d band of the iridium active center is moved upwards, the adsorption / desorption behavior of a reaction intermediate is optimized, a reaction energy barrier is remarkably reduced, and the reaction efficiency is improved. The activity of the oxidoid enzyme reaches 27.98 U / mg, and the activity of the peroxidase reaches 330.24 U / mg; the invention further relates to application of the asymmetric iridium monatomic nano enzyme Ir-S / N-C in preparation of a product for detecting cholinesterase. According to the detection strategy, unstable H2O2 does not need to be additionally added, the operation steps are simplified, the stability and anti-jamming capability of a system are improved, and false positive signals are effectively reduced. Experiments prove that the constructed detection method has a good linear relation and high sensitivity on detection of cholinesterase, the detection limit is as low as 0.21 U.L <-1 >, and great application potential in the fields of biomedical diagnosis and environmental monitoring is shown.

The invention belongs to the field of traditional Chinese medicine extraction and separation, and particularly relates to a heterocyclic alkaloid compound in purslane as well as an extraction and separation method and application thereof. The molecular formula of the compound is C9H12N4O5, and the chemical name of the compound is 5-(4-hydroxy-3-((hydroxymethyl) amine) isoxazolidin-5-yl)-5H-pyrrolo [3, 4-d] isoxazolidin-4-ol. The structural formula of the compound is shown in the specification, and the structural formula of the compound is shown in the specification. The invention also provides an extraction and separation method of the compound. Ethanol extraction, ODS column chromatography separation, sephadex gel chromatographic column separation and ultra-high performance liquid chromatography are adopted for separation, purification and preparation. The structure of the compound is determined as a new compound by mass spectrum, hydrogen spectrum, carbon spectrum and two-dimensional nuclear magnetic spectrum analysis methods, and the compound has anti-inflammatory, anti-cholinesterase and antioxidant activity. The heterocyclic alkaloid compound and the salt or derivative thereof can be used as raw materials for drug development and pharmacological activity research.

The application relates to the technical field of drug synthesis, in particular to a synthesis method and application of a 2-(cyclopropylamide)thiazole-4-amide derivative. The thiazole structure is shown in formula I. The preparation method of the 2-(cyclopropylamide)thiazole-4-amide derivative is as follows: the compound shown in formula I is obtained by reacting the compound shown in formula II in the presence of HATU, DIPEA, a primary amine or a secondary amine and tetrahydrofuran. The 2-(cyclopropylamide)thiazole-4-amide derivative has the effect of relieving Alzheimer's disease, and is characterized by strong cholinesterase inhibition activity.

The invention discloses a 2, 4-dihydroxy-6-benzyl formic acid polyol ester compound in a gold wire brush and an extraction and separation method and application thereof, the structure of the 2, 4-dihydroxy-6-benzyl formic acid polyol ester compound adopts 1H-NMR (nuclear magnetic resonance), 13C-NMR (nuclear magnetic resonance) and two-dimensional nuclear magnetic spectrum analysis methods to determine that compounds I-1-I-3 are new compounds, and the 2, 4-dihydroxy-6-benzyl formic acid polyol ester compound has the following structure. The 2, 4-dihydroxy-6-benzyl formic acid polyol ester compound can effectively inhibit the activity of acetylcholin esterase (AChE), so that the compound disclosed by the invention can be used as a lead compound for resisting the acetylcholin esterase, and a material basis and a theoretical basis are provided for developing new drugs and new components.

The present application relates to a kind of tetrahydropyrrolizino [2, 3-c] quinoline alkaloid compound and derivative with novel structure and preparation method and purposes thereof.The new compound bungeanoline G provided in the present application is extracted and separated from Papaveraceae Corydalis bungeana Turcz.The present application also proposes a method for artificially synthesizing bungeanoline G, and a series of derivatives of bungeanoline G are prepared.Biological activity experiments show that the compounds have acetylcholinesterase and butyrylcholinesterase inhibitory activity, and can be applied in the preparation of drugs for treating or improving various neurodegenerative diseases such as Alzheimer's disease, vascular dementia, myasthenia gravis and the like.

Compositions and methods are provided for inactivating ghrelin in mammalian cells by administration of a polynucleotide encoding a butyrylcholinesterase (BChE) enzyme. The compositions and methods disclosed herein may be administered to mammals or mammalian cells for reducing drug-seeking behavior.

The present invention provides a pyranone compound represented by formula (I). The pyranone compound has excellent anti-inflammatory activity and cholinesterase inhibitory activity, features a high blood-brain barrier penetration potential and good safety, and can ameliorate cognitive impairment related to Alzheimer's disease, reduce glial cell activation, decrease Aβ deposition and alleviate neuroinflammation.

The invention provides a cholinesterase application method based on nano-gold stars. The cholinesterase application method comprises the following steps: synthesis and characterization of a nano-gold star material, morphology regulation and control of the nano-gold star material, and application of nano-gold star etching inhibition to cholinesterase activity detection. The embodiment of the invention provides a simple, stable and sensitive nano-gold star material morphology control method, the method is applied to cholinesterase activity detection and cholinesterase inhibitor and revivifier screening, and the method has the advantages of rapidness, low cost, ultrasensitivity, quantitative colorimetric reading and the like.

This invention discloses a biosensor membrane for the detection of organophosphorus pesticides, comprising a base membrane on which multiple glucose oxidase catalytic modules and multiple acetylcholinesterase catalytic modules are loaded. Each glucose oxidase catalytic module includes a first carrier immobilized on the base membrane and glucose oxidase loaded thereon. Each acetylcholinesterase catalytic module includes a second carrier immobilized on the base membrane and acetylcholinesterase loaded thereon. The weight ratio of glucose oxidase to acetylcholinesterase is 1:1 to 1:4. This invention reveals the structure-activity relationship of enzyme ratio-enzyme load synergistic regulation of sensing interface performance. By establishing a competitive inhibition advantage through changing the enzyme ratio, the enzyme load is optimized to achieve a balance between high activity and high mass transfer, thereby synergistically improving signal change and inhibition rate, achieving highly sensitive detection of organophosphorus pesticides. The biosensor membrane provided by this invention is suitable for the detection of various organophosphorus pesticides in food (especially crops and dairy products).

The present application provides a biological product and a method and an application thereof. The biological product is used for the preparation of a therapeutic agent for cancer treatment, and it includes at least one of the recombinant butyrylcholinesterase-albumin (rBChE-albumin) fusion protein and the recombinant butyrylcholinesterase-Fc (rBChE-Fc) fusion protein. The biological product adjusts the balance of acetylcholine and other related metabolic pathways by supplementing at least one of the exogenous rBChE-albumin fusion protein and rBChE-Fc fusion protein to treat cancer. The present invention solves the problem that the extraction and purification of BChE from human serum may not meet the huge demand for cancer treatment. The present application further provides a biological product for neutralizing and degrading nerve agents and organophosphate compounds, hydrolyzing ghrelin, and anti-wrinkle.

The application discloses a strain of Bifidobacterium adolescentis for reducing the risk of related metabolic disorders caused by low estrogen levels and an application thereof, and belongs to the technical field of microorganisms. The Bifidobacterium adolescentis CCFM1507 provided by the application can increase the estrogen level in serum of ovariectomized rats, increase the expression amount of CYP19 and ERa in adrenal gland tissue, and effectively inhibit the levels of increased IL-10 and TNF-alpha and decreased IL-4 in serum. The Bifidobacterium adolescentis CCFM1507 significantly reduces triglyceride (TG) and cholinesterase (CHE) in serum, relieves dyslipidemia, and increases the content of glutamine in serum. The Bifidobacterium adolescentis CCFM1507 is a food safety strain, and can be used for preparing food, functional food or medicine, and has a wide application prospect.

The application belongs to the technical field of biosensing and specifically relates to a biosensor for detecting active acetylcholinesterase and application thereof. The biosensor comprises nanotubes with nanometer apertures at tips for generating current blocking signals; and a ring bundle DNA tetrahedron carrier for loading a solution containing active acetylcholinesterase to be detected, wherein the ring bundle DNA tetrahedron carrier is TDN1 or TDN4, the sequences of the four DNA single strands in TDN1 are shown as SEQ ID NO. 1 to SEQ ID NO. 4, and the sequences of the four DNA single strands in TDN4 are shown as SEQ ID NO. 1, SEQ ID NO. 3, SEQ ID NO. 5 and SEQ ID NO. 6. The application utilizes a closed-loop DNA tetrahedron nanostructure anchored at two ends of an aptamer to generate a difference in current signals in a nanometer hole before and after the active AChE is combined, so that high-sensitivity and high-selectivity detection of the active AChE at a single-molecule level is achieved.

The application provides an organic phosphorus poisoning relief composite enzyme and application thereof, and belongs to the technical field of biological medicine. The organic phosphorus poisoning relief composite enzyme provided by the application comprises polyethylene glycol modified organic phosphorus hydrolase and butyrylcholine esterase, and the mass ratio of the polyethylene glycol modified organic phosphorus hydrolase to the butyrylcholine esterase is (4-8):(2500-10000). The rat acute organic phosphorus poisoning treatment result shows that the organic phosphorus poisoning relief composite enzyme provided by the application fully plays the efficient catalytic hydrolysis capacity of the enzyme as a catalyst, efficiently removes organic phosphorus and acetylcholine by using the organic phosphorus hydrolase and the butyrylcholine esterase respectively, provides a drug combination for treating the cause for the organic phosphorus poisoning injury first aid, and the treatment effect is significantly better than that of the single drug.

The invention discloses a compound which has anti-neuroinflammation activity and can selectively inhibit butyrylcholine esterase activity, and belongs to the technical field of medicinal chemistry. The compound and the pharmaceutical composition containing the compound have good anti-neuroinflammatory activity and selective butyrylcholine esterase inhibition activity, and have important application prospects in treatment of neurodegenerative diseases such as Alzheimer's disease.

The present application relates to nematode disease prevention and treatment agent technical field, especially to a kind of pine wood nematode disease prevention and treatment agent and preparation method thereof, by weight parts, including the following components: sophocarpidine 10-30 parts;Azadirachtin 5-20 parts;Turpentine 40-70 parts;Emulsifier 5-15 parts;Efficiency agent 1-5 parts;Stabilizer 0.5-3 parts, the synergistic effect of sophocarpidine and azadirachtin constitutes the core of the present application;Quinolone ring and pyridine ring structure in sophocarpidine molecule endow it with strong insecticidal activity, mainly by inhibiting acetylcholinesterase to interfere with the nerve conduction of nematode;And the complex triterpenoid structure of azadirachtin can interfere with the hormone system of nematode, inhibit its growth and development and reproduction.The two different mechanisms of action form complementation at molecular level, both can quickly kill nematode, and can long-term inhibit its population growth;Second, turpentine as natural terpene compound, the permeability of other active ingredients is enhanced.

The invention relates to the therapeutic application of multifunctional compounds that act as α2 adrenoreceptor antagonists and cholinesterase inhibitors for the treatment of Alzheimer's disease and other neurodegenerative diseases, or the concomitant use of a mixture of an α2 adrenoreceptor antagonist and a cholinesterase inhibitor to achieve the same effect.

The invention discloses a biosensing membrane for organophosphorus pesticide detection, which comprises a base membrane, a plurality of glucose oxidase catalysis modules and a plurality of acetylcholin esterase catalysis modules are loaded on the base membrane, each glucose oxidase catalysis module comprises a first carrier fixed on the base membrane and glucose oxidase loaded on the first carrier, and each acetylcholin esterase catalysis module comprises a second carrier fixed on the base membrane. The acetylcholin esterase catalysis module comprises a second carrier fixed on the base membrane and acetylcholin esterase loaded on the second carrier, and the weight ratio of glucose oxidase to acetylcholin esterase is (1: 1)-(1: 4). The invention discloses a structure-function relationship of the performance of an enzyme ratio-enzyme loading quantity coordinated regulation sensing interface, and optimizes the enzyme loading quantity to pursue the balance of high activity and high mass transfer on the basis of establishing a certain competitive inhibition advantage by changing the enzyme ratio, so that the signal change and inhibition ratio are synergistically improved, and the high-sensitivity detection of the organophosphorus pesticide is realized. The biosensing film provided by the invention is suitable for detecting various organophosphorus pesticides in food (especially crops and dairy products).

The present invention relates to a galantamine analog having a cholinesterase inhibitory activity, and a preparation method therefor and the use thereof. The galantamine analog has a general structural formula as shown in formula (IA), (IB) or (IC). In formula (IA), R1 is selected from hydrogen, o-fluoro, m-fluoro, p-fluoro, 2,4-difluoro, m-trifluoromethyl, p-methyl, 3,5-dimethoxy, p-chloro, p-nitro, p-cyano or p-trifluoromethoxy. In formula (IB), R2 is selected from phenyl, o-fluorophenyl, m-fluorophenyl, p-fluorophenyl, 2,4-difluorophenyl, 3,5-difluorophenyl, o-methylphenyl, p-methylphenyl, p-methoxyphenyl, indole, p-cyanophenyl, p-trifluoromethylphenyl, p-trifluoromethoxyphenyl, p-nitrophenyl or naphthalene ring. In formula (IC), R3 is selected from hydrogen, o-fluoro, m-fluoro, p-fluoro, m-chloro, p-chloro, p-methyl, o-methoxy, m-methoxy or p-methoxy. The galantamine analog of the present invention has a cholinesterase inhibitory activity superior to that of galantamine, and is expected to be used for treating diseases associated with cholinergic dysfunction.

This invention relates to a galantamine analogue with cholinesterase-inhibiting activity, its preparation method, and its application. The general structural formula is shown in formula (IA), (IB), or (IC). In formula (IA), R1 is selected from hydrogen, o-fluorine, m-fluorine, p-fluorine, 2,4-difluoro, m-trifluoromethyl, p-methyl, 3,5-dimethoxy, p-chloro, p-nitro, p-cyano, or p-trifluoromethoxy. In formula (IB), R2 is selected from phenyl, o-fluorophenyl, m-fluorophenyl, p-fluorophenyl, 2,4-difluorophenyl, 3,5-difluorophenyl, o-methylphenyl, p-methylphenyl, p-methoxyphenyl, indole, p-cyanophenyl, p-trifluoromethylphenyl, p-trifluoromethoxyphenyl, p-nitrophenyl, or a naphthalene ring. In formula (IC), R3 is selected from hydrogen, o-fluorine, m-fluorine, p-fluorine, m-chloro, p-chloro, p-methyl, o-methoxy, m-methoxy, or p-methoxy. The galantamine analogue of this invention exhibits superior inhibitory activity against cholinesterase compared to galantamine, and holds promise for the treatment of cholinergic dysfunction-related diseases.

Compositions and methods are provided for inactivating ghrelin in mammalian cells by administration of a polynucleotide encoding a butyrylcholinesterase (BChE) enzyme.

The application discloses a clinical biochemical composite quality control product, which comprises detection item raw materials, a matrix liquid and a protective agent; the detection item raw materials are alkaline phosphatase, amylase, sodium glycocholate, cholinesterase, creatinine, leucine aminopeptidase, lactate dehydrogenase, lipase, triglyceride, cholesterol, uric acid, urea, alanine aminotransferase, aspartate aminotransferase, gamma-glutamyl transferase, glucose, alpha-hydroxybutyric acid dehydrogenase, sodium hydrogen phosphate, magnesium chloride, calcium chloride, ferrous chloride, bilirubin, pancreatic amylase and sodium bicarbonate; the matrix liquid is bovine serum albumin and human serum albumin; and the protective agent is dithiothreitol (DTT), mannitol, trehalose, sodium chloride, a composite enzyme stabilizer AES and sodium azide. The quality control product can realize the detection of 27 clinical biochemical items, and the freeze-drying process is adopted, so that the freeze-dried composite quality control product has low viscosity, is easy to be re-dissolved and mixed, has high stability and has small matrix effect.

The invention belongs to the technical field of medicines, and particularly relates to a group of butyrylcholine esterase (BChE) inhibitors with high selectivity and a screening method thereof, in particular to two BChE specific inhibitors, namely methyl 4-hydroxybenzyl carbamate and moringa seed extract, which are screened from a moringa seed extract. The invention also relates to application of the BChE specific inhibitor in preparation of drugs for preventing or treating Alzheimer's disease. The invention provides a brand new strategy for efficiently screening the anti-Alzheimer disease medicine.

This invention provides a vinylpyranone compound, which exhibits excellent antioxidant activity, anti-inflammatory activity, and Aβ inhibition. 1‑42 Aggregation activity and inhibition of cholinesterase activity.

The invention discloses a compound with a benzamide-oxadiazole skeleton as well as a preparation method and application thereof. The structure of the compound is shown in the specification. According to the present invention, butyrylcholine esterase inhibition activity, Nrf2 activation activity, in vitro pharmacodynamic experiment and Morris water maze experiment are adopted as carriers to evaluate the treatment of Alzheimer's disease (especially moderate and severe Alzheimer's disease) by using the compound represented by the general formula I, and the results show that the compound has good in vitro and in vivo activity and extremely high selectivity; the compound can be used as a candidate lead compound for further development of an anti-Alzheimer's disease effect by selectively inhibiting butyrylcholine esterase and activating Nrf2.

The invention discloses a compound with a benzimidazole-amino furazan-oxadiazole skeleton as well as a preparation method and application of the compound. The structure of the compound is shown in general formulas I and II. According to the present invention, butyrylcholine esterase inhibition activity, Nrf2 activation activity, in vitro pharmacodynamic experiment and Morris water maze experiment are adopted as carriers to evaluate the treatment of Alzheimer's disease (especially moderate and severe Alzheimer's disease) by using the compounds represented by the general formulas I and II, and the results show that the compounds have good in vitro and in vivo activity and extremely high selectivity; the compound can be used as a candidate lead compound for further development of an anti-Alzheimer's disease effect by selectively inhibiting butyrylcholine esterase and activating Nrf2.