89 results about "Acetylcholinesterase" patented technology

The invention belongs to the technical field of biological bacterial fertilizers, and discloses a Chinese herbal medicine carrier-based multifunctional microbial bacterial fertilizer, which comprises a microbial strain group, a Chinese herbal medicine active component group, an organic matter and nutrition carrier, mineral elements and auxiliary components, and a functional synergist. Through the synergistic interaction of Chinese herbal medicine active ingredients and functional microbial flora, breeding of harmful bacteria in soil is inhibited, synthesis of acetylcholin esterase of nematodes is interfered, a continuous cropping disease occurrence chain is blocked from the source, and meanwhile, organic acid and flavonoid substances slowly released by a Chinese herbal medicine carrier are utilized to activate resistance gene expression of a plant system, so that the disease resistance of the nematodes is improved. The tolerance threshold of crops to high temperature, cold damage and diseases is enhanced; in the composite carrier, humic acid and diatomite are crosslinked through hydrogen bonds to form a stable granular structure, the cation exchange capacity and porosity of soil are effectively improved, the strong hydration capacity of polyglutamic acid is combined to lock nutrients and moisture, and development of meristem of a root system and proliferation of capillary roots are promoted.

The invention belongs to the technical field of functional grease processing, and particularly relates to an enzymolysis preparation method and application of diglyceride with an effect of improving Alzheimer's disease. The method comprises the following steps: mixing low-erucic acid rapeseed oil, glycerol and water, and heating to obtain a pre-reaction mixture; adding compound enzyme for reaction, and then adding candida antarctica lipase B and pseudomonas fluorescens lipase for reaction; and after the reaction is completed, carrying out molecular distillation, collecting a light-phase product, carrying out adsorption filtration, and collecting filtrate to obtain the diglyceride oil. The compound enzyme is composed of rhizomucor miehei lipase, candida rugosa lipase and candida antarctica lipase B in a weight ratio of (2-4): 2: 1. According to the method, the content of diglyceride is effectively increased, the prepared composition has the efficacy of preventing and treating Alzheimer's disease, and the efficacy is shown as improvement of reaction capacity and cognitive function, inhibition of brain apoptosis and acetylcholin esterase, enhancement of SOD and CAT vitality and improvement of related gene expression.

This invention belongs to the field of microbial technology, specifically relating to a strain of *Pediococcus pentosaceus* SUN02 with acetylcholinesterase inhibitory activity and its applications. This *Pediococcus pentosaceus* SUN02 is deposited at the China General Microbiological Culture Collection Center (CGMCC) with accession number CGMCC No. 29705. The *Pediococcus pentosaceus* SUN02 provided by this invention exhibits strong acid and bile salt resistance, good tolerance in simulated gastric and intestinal fluids, and can successfully reach the human intestine. *Pediococcus pentosaceus* SUN02, in its bacterial suspension and inactivated cells, possesses strong acetylcholinesterase inhibitory activity, produces γ-aminobutyric acid (GABA), and has antioxidant and other probiotic functions. Its application in probiotic products may help improve Alzheimer's disease, enhance learning and memory abilities, regulate mood, and improve sleep.

The application relates to a preparation method of a biosensor. The application relates to a preparation method of a portable pesticide detection biosensor based on acetylcholinesterase (AChE)@poly(allylamine hydrochloride)-hydrogen bond organic framework (PAH-HOF) and application of the biosensor in on-site rapid chlorpyrifos detection, and belongs to the technical field of biosensors. According to the method, AChE is combined with poly(allylamine hydrochloride) (PAH) to change the surface charge and promote self-assembly of the AChE and the hydrogen bond organic framework (HOF), so that an AChE@PAH-HOF composite material with high catalytic activity, high embedding rate and high stability is formed; then the material is integrated into a water-retaining glycerol-sodium alginate hydrogel (G-SA) matrix to construct a disc-shaped sensor. The sensor can be attached to the surface of plants and used for long-term in-situ monitoring of organophosphorus pesticides. In combination with an image processing algorithm, the system realizes accurate tracking of the chlorpyrifos degradation process on the surface of tomato plants, and the detection limit reaches 1 ng / mL. The application provides non-invasive and low-cost technical support for crop health management and sustainable precision agriculture.

Described herein are compounds that reactivate acetylcholinesterase and associated methods of treating organophosphate poisoning.

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 ​

本发明公开了一种基于静电驱动的双酶级联放大荧光传感器及其制备方法和应用，所述纳米酶荧光传感器由探针Azo‑Bodipy 685、胆碱氧化酶（CHO）和氯化乙酰胆碱（ACh）组成。本发明基于静电吸附原理，提出静电络合共固定化‑酶级联反应协同策略，构建一种新的静电驱动荧光传感器，利用ACh的季铵盐正电荷与CHO表面负电荷的静电作用，在特异性荧光探针Azo‑Bodipy 685表面构建纳米尺度空间限域的酶反应微环境。当有机磷农药抑制乙酰胆碱酯酶（AChE）时，氯化胆碱生成减少导致CHO催化产生的过氧化氢量下降，荧光信号强度减弱，一系列荧光强度的变化可以实现检测AChE活性和测定有机磷农药残留含量。

The invention discloses a benzofuran glycoside compound as well as a separation and extraction method, a pharmaceutical composition and application thereof. The compound 1 is separated from an eupatorium chinense extract. And separating and purifying chemical components of the n-butyl alcohol part of the eupatorium chinense root to obtain the benzofuran compound. The inhibition activity of target cyclooxygenase-2 of inflammatory related diseases of all the separated compounds 1 is tested, and the compounds 1 have good inhibition activity on COX-2 enzyme and have good binding energy with target protein. In addition, the compound also has a good NLRP3-related inhibition effect, can be independently used or combined with other medicines to regulate NLRP3-related proteins, and is used for treating NLRP3-related mediated diseases and / or diseases and preparing medicines for preventing or treating the diseases or diseases. The compound 1 also has a good inhibition effect on acetylcholin esterase, and can be used for treating Alzheimer's disease, myasthenia gravis, Parkinson's disease and other diseases.

This application relates to the field of medicinal chemistry, specifically disclosing a piperidine derivative, a pharmaceutical composition, its uses, and a method for preparation. The piperidine derivative has the structure of general formula (I). This piperidine derivative can significantly improve the learning and memory abilities of Aβ-induced Alzheimer's disease model rats and effectively reduce acetylcholinesterase activity in brain tissue, providing a potential candidate for the development of novel Alzheimer's disease treatments.

The invention relates to a preparation method of a biosensor, in particular to a construction method of an acetylcholin esterase (at) amorphous covalent organic framework (AChE (at) aCOFs-DB) photoenzyme integrated biosensor, and belongs to the technical field of biosensors. According to the method, an in-situ growth mineralization strategy is adopted, effective packaging of AChE in aCOFs-DB is achieved, the fluorescence performance of aCOFs is enhanced through a hydrogen bond auxiliary intramolecular rotation limitation design, and meanwhile the structural stability and catalytic activity of AChE are improved; the biosensor with high sensitivity and high selectivity is constructed based on the synergistic effect of fluorescence characteristics and enzyme catalytic performance; the sensor can be used for sensitive detection of organophosphorus pesticides such as chlorpyrifos, and the detection limit can reach a nanogram / milliliter level; the detection principle is as follows: AChE catalyzes a substrate to generate a product, and fluorescence quenching is caused by an inner filtering effect; when the organophosphorus pesticide (such as chlorpyrifos) exists, the AChE activity is inhibited, the catalytic capability is reduced, and a fluorescence signal is recovered, so that quantitative detection of the pesticide is realized; the preparation method is simple and convenient to operate and controllable in structure, is suitable for rapid detection of organophosphorus pesticides in agricultural products and environmental samples, and has a good application prospect.

The application discloses a kind of photoactivation manganese ion bridging type deoxyribozyme probe preparation and its application in Cistanche inhibiting acetylcholinesterase activity.The probe is pSD@MnO2 Composite structure, which is composed of manganese dioxide nanosheet and functional nucleic acid assembly adsorbed on its surface, the assembly includes S chain labeled with fluorescence / quenching group and containing deoxyribozyme cleavage site, and pD chain partially hybridized with S chain and containing photocleavage site.Its preparation includes nucleic acid probe assembly, MnO2 Nanosheet complexing and purification steps.When applied, AChE catalytic product decomposes MnO2, releases Mn 2+ And nucleic acid chain; after centrifugation, pD chain is cut by ultraviolet light activation trigger, and released DNAzyme is cut under the assistance of Mn 2+ It produces amplified fluorescence signal; by comparing signal change before and after adding inhibitor, inhibition activity can be quantitatively evaluated.The application combines photocontrol activation with enzyme cascade amplification, realizes high sensitivity and operation synchronism of detection process, and is especially suitable for high-throughput rapid screening of AChE inhibitor in Cistanche and other natural products.

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.

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).

This invention belongs to the field of pharmaceutical technology and relates to eight glycoside compounds extracted and isolated from the dried leaves of *Picrasma quassioides* Benn, a plant belonging to the genus *Picrasma* in the family Simaroubaceae. The compounds were obtained using chromatographic methods including silica gel chromatography, HP20 column chromatography, ODS column chromatography, and HPLC. This invention also relates to the acetylcholinesterase inhibitory activity of compounds 1-8 and their pharmaceutical uses. The preparation method of this invention is simple, reproducible, and of high purity.

The present application relates to a controllable multi-enzyme cascade AChE-HRP-CHO@HNF composite material preparation and plant wearable sensor application, belong to biosensing, enzyme immobilization material and plant in-situ rapid detection field. The composite material is prepared by biomimetic mineralization and layer-by-layer protein crown assembly, takes enzyme-inorganic hybrid nanoflower as carrier, realizes spatial ordered fixation of choline oxidase (CHO), horseradish peroxidase (HRP) and acetylcholinesterase (AChE) in nanostructure, and forms hierarchical distribution multi-enzyme cascade system. The structure can shorten the transmission distance of intermediate product in cascade reaction, improve the cascade catalytic efficiency and pesticide inhibition response sensitivity. Further embedding it in double network hydrogel, a hydrogel sensing disc suitable for plant surface attachment can be prepared, the hydrogel sensing disc has good flexibility, surface adaptability and storage stability, can be used for on-site visual detection of organophosphorus pesticides such as chlorpyrifos, has the characteristics of simple operation and non-invasive detection.

The application discloses a FRET fluorescent probe with dual response to acetylcholinesterase and viscosity, a preparation method and application thereof, wherein the structure of the FRET fluorescent probe is shown in the following formula: The fluorescent probe is based on a fluorescence resonance energy transfer (FRET) mechanism, responds to acetylcholinesterase (AChE) at a short wave of 520 nm, and the detection limit is as low as 0.104 U / L, and responds to viscosity at a long wave of 680 nm, and the wavelength difference is as high as 160 nm, and the dual-channel response has no crosstalk. Cell toxicity test shows that the probe has good biocompatibility, and confocal fluorescence microscopic imaging experiment shows that the probe has good light stability for cells, has the ability of simultaneously monitoring the concentration change of AChE in cells and the viscosity fluctuation of cells, and is suitable for confocal fluorescence imaging for tracing the concentration change of AChE in cells and the viscosity fluctuation.

The invention discloses a high-flux toxicity pre-evaluation substitution method based on an acetylcholin esterase target. By integrating an SH-SY5Y nerve cell endogenous AChE and recombinant exogenous AChE dual detection system and relying on an automatic screening system constructed by integrating core equipment such as an automatic pipetting workstation, a constant-temperature incubator and a multifunctional microplate reader, a high-flux toxicity pre-evaluation substitution method based on an AChE target is successfully established and is used for evaluating the neurotoxicity of a compound, and the method has the advantages of high sensitivity, high sensitivity, high sensitivity and the like. The method solves the limitation that a single screening method in the prior art cannot evaluate factors such as target inhibition, cell permeability and metabolic transformation at the same time, and the method is simple, convenient, rapid, high in accuracy and suitable for large-scale primary screening of the AChE inhibitor and early warning of neurotoxicity risks.

The application is suitable for the technical field of pesticide detection, and provides a method for double-signal detection of trace residues of organophosphorus pesticides based on gold nanoscale enzyme, polypeptide is used as a protective agent to synthesize gold nanoscale enzyme, the double properties of fluorescence and peroxidase-like activity of the gold nanoscale enzyme are used, and the enzyme inhibitor method is combined to establish a detection method, and the specific steps are as follows: step one, synthesizing gold nanoscale enzyme and storing for standby; step two, preparing sodium alginate hydrogel blocks, and physically adsorbing gold nanoscale enzyme into the sodium alginate hydrogel through soaking and storing for standby; step three, establishing an acetylcholinesterase / choline oxidase cascade reaction to generate H2O2; step four, based on the H2O2 generated in step three, and combining the prepared sodium alginate hydrogel in step two, realizing rapid visual quantitative detection of OPs, the double-signal output detection result of the application has self-correction, can resist interference, improves detection accuracy, and expands the practical application range of detection.

Carbamate-substituted styryl sulfone compounds have a structure of general formula (I). The compounds not only has a significantly enhanced acetylcholinesterase inhibitory activity compared with carbamates as positive drugs, but also has a significantly enhanced therapeutic effect on Parkinson's disease compared with caffeic acid phenethyl ester compounds having similar structures.

The invention provides a phenolic compound with an effect of accelerating alcohol metabolism and a preparation method of the phenolic compound. The structural formula of the polyphenol compound 1-(2-hydroxyl, 4-O-glucosylphenyl)-2-(4-hydroxyphenyl) ethanone is as shown in formula (I), and the polyphenol compound 1-(2-hydroxyl, 4-O-glucosylphenyl)-2-(4-hydroxyphenyl) ethanone is separated from radix puerariae. In-vitro pharmacological experiments prove that the compound 1-(2-hydroxyl, 4-O-glucosylphenyl)-2-(4-hydroxyphenyl) ethanone has good acetylcholin esterase inhibitory activity, and the EC50 value of the compound 1-(2-hydroxyl, 4-O-glucosylphenyl)-2-(4-hydroxyphenyl) ethanone is 1.41 + / -0.12 mM, which indicates that the compound 1-(2-hydroxyl, 4-O-glucosylphenyl)-2-( The polyphenol compound 1-(2-hydroxyl, 4-O-glucosylphenyl)-2-(4-hydroxyphenyl) ethanone is expected to be used as a lead compound to develop a novel alcohol effect dispelling and liver protecting medicine.

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 present application relates to the technical field of medicine, and specifically discloses a mangrove sediment mud-derived fungal fermentation extract, a preparation method and application thereof. Pseudallescheria angusta SYSU-M4 is inoculated into a liquid culture medium to obtain a spore liquid; the preservation number of the mangrove sediment mud-derived fungus is GDMCC No: 66263; (2) the spore liquid is inoculated into a solid culture medium to obtain a fermentation product; (3) the fermentation product is extracted by an extraction solvent, extracted by an extraction solvent, and separated by a separation solvent, and a component with a detection relative migration value of 0.4 in thin layer chromatography is collected, and the fermentation extract is obtained. The fermentation extract has obvious acetylcholinesterase and NO inhibitory activity, and has a good application prospect in the preparation of anti-inflammatory drugs and anti-inflammatory health products. The preparation method is simple in operation and suitable for large-scale production.

This invention provides a fluorescent probe for detecting acetylcholinesterase, its preparation method, and its application, belonging to the field of detection and analysis technology. The fluorescent probe is particularly suitable for detecting acetylcholinesterase in vivo. It is constructed by connecting an electron donor, diphenylamineoxanthracene, to an electron acceptor, benzoindolesulfonate, via an ethylene bridge, with the following structural formula: The fluorescent probe of this invention has advantages such as high detection sensitivity, good selectivity, and fast response time. This invention also marks the first successful in vivo imaging analysis of changes in AChE in the brains of depressed rats, demonstrating significant practical application value.

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 technical field of medicines, in particular to a piperidine alkyl pyridone compound and pharmaceutically acceptable salt, a preparation method, a pharmaceutical composition and application of the piperidine alkyl pyridone compound. The piperidine alkyl pyridone compound disclosed by the invention has a structure as shown in a formula (I), and has relatively strong inhibitory activity on acetylcholin esterase, A beta 1-42 oligomer aggregation and neuroinflammation; the compound can be used for preparing medicines for treating and / or preventing nervous system and muscle system diseases; .

The application discloses a benzofuran glycoside compound, a separation and extraction method thereof, a pharmaceutical composition and application, and the compound 1 is separated from a macleaya cordata extract. A benzofuran compound is obtained by separating and purifying a n-butanol part chemical component of a macleaya cordata root. The inhibitory activity of all separated compounds 1 on a target point cyclooxygenase-2 of an inflammatory related disease is tested, the compound 1 has good inhibitory activity on COX-2 enzyme, and the compound 1 has better binding energy with the target point protein. The compound also has good NLRP3 related inhibitory effect, can be used alone or in combination with other drugs to regulate NLRP3 related proteins, is used for treating NLRP3 related mediated diseases and / or diseases, and is used for preparing drugs for preventing or treating the diseases. The compound 1 also has better inhibitory effect on acetylcholinesterase, and can be used for treating diseases such as Alzheimer's disease, myasthenia gravis and Parkinson's disease.

The application discloses a kind of Ascophyllum nodosum fucoidan ANFS and its preparation method and application in preparation for preventing and treating alzheimer's disease preparation, belong to marine biological medicine technical field.The main chain of the Ascophyllum nodosum fucoidan ANFS is composed of (1→3) connected α-L fucose residue, and branch is monosaccharide or sulfate group.Sulfated modification occurs at C-2 and C-4 of fucose residue, and its molecular weight is 15-30 kDa.The application proves by experiment, ANFS can significantly improve the motion behavior defect of zebra fish, inhibit acetylcholinesterase activity, improve catalase and glutathione peroxidase activity, reduce intracellular reactive oxygen species level, reduce brain neuron apoptosis, and effectively protect the integrity of blood-brain barrier.The polysaccharide is rich in source, and preparation process is simple, and safety is high, has wide application prospect in the development of marine medicine and functional product for treating alzheimer's disease.

This invention discloses the use of cyanidin anthocyanins or their pharmaceutically acceptable salts, esters, and solvates in the preparation of drugs for the prevention and / or treatment of neurodegenerative diseases. The cyanidin anthocyanins are selected from cyanidin-3-O-rutin glycoside, cyanidin-3-O-sophoroside, or cyanidin-3-O-xyloside. These compounds can inhibit acetylcholinesterase activity, upregulate α7 nicotinic acetylcholine receptor expression, and activate the PI3K / AKT / GSK3β signaling pathway, thereby inhibiting Tau protein hyperphosphorylation and reducing neuroinflammatory responses. Furthermore, it has been confirmed that cyanidin-3-O-rutin glycoside directly binds to acetylcholinesterase, verifying AChE as its key target, providing new natural active compounds and their mechanisms of action for the prevention and treatment of neurodegenerative diseases.

The use of deep eutectic solvents in enzyme-based biosensors improves the robustness of the sensors with regard to storage conditions. For example, phosphotriesterase or acetylcholinesterase enzymes can be used to detect organophosphates using electrochemistry.