126 results about "Cholinesterase" patented technology

The invention discloses a carvacrol / thymol derivative with a structure as shown in the following formula (I), and pharmaceutically acceptable salts of the derivative: # imgabs0 #, wherein R is selected from 1-piperidyl or 1-pyrrolidinyl. The carvacrol / thymol derivative has remarkable inhibitory activity and high selectivity on butyrylcholine esterase, has good anti-neuroinflammation activity, can be used as a selective butyrylcholine esterase inhibitor with the anti-neuroinflammation activity, can be used for preparing medicines for preventing or treating Alzheimer's disease, and has wide application prospects. The compound has a good application prospect in treatment of Alzheimer's disease.

The invention belongs to the technical field of medical diagnosis, and discloses a marker for evaluating the curative effect of treating hepatocellular carcinoma by combining TACE with Czodili monoclonal antibody and bevacizumab, and a construction method and application of an FAAP prognostic scoring model. The invention develops and verifies an FAAP prognostic scoring system, and a novel composite model integrates four indexes of fibrin degradation product / cholinesterase ratio * 1000 (FCR), aspartate aminotransferase (AST), alpha fetoprotein (AFP) and portal vein tumor thrombus (PVTT), and is used for predicting the survival condition of uHCC patients subjected to TACE-Czodimab-bevacizumab triple therapy. The tool has an instant clinical value, can optimize patient selection, guides adaptive treatment upgrading, and provides a standardized curative effect evaluation basis for a clinical test for exploring a TACE-immunotherapy-anti-angiogenesis combined scheme.

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 present invention belongs to the field of medicinal chemistry and discloses quinoline derivatives containing a hydroxamic acid fragment as shown in Formula I. Wherein, R1 is selected from H, 7-Cl, 2-Me, 2-Ph; R2 is selected from ‑(CH2)2-, ‑(CH2)3-, ‑(CH2)6-, ‑C6H4-; and R3 is selected from ‑(CH2)2-, ‑(CH2)3-, ‑(CH2)4-, ‑(CH2)6-, ‑C6H4-. The synthetic raw materials of the quinoline derivatives containing a hydroxamic acid fragment of the present invention are readily available, the preparation method is simple, and the operation is easy. The quinoline derivatives containing a hydroxamic acid fragment have good cholinesterase inhibitory activity, and some of the compounds have stronger activity than the clinical drug rivastigmine, and are expected to be developed into new cholinesterase inhibitors for Alzheimer's disease.

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 invention relates to the technical field of pesticides, in particular to an environment-friendly composite pesticide based on marine microorganisms and a preparation method thereof.The environment-friendly composite pesticide is prepared from, by weight, 40%-52% of functional microspheres, 5%-6% of matrine, 2%-3% of rotenone, 3%-4% of rhamnolipid, 1%-1.5% of sodium alginate, 30%-35% of kieselguhr, 1%-2% of zinc sulfate, 2%-4% of hydroxyapatite and the balance water. Natural marine materials such as algin, sodium alginate and kieselguhr are used as carriers, plant source active ingredients and a biological surfactant are matched, matrine serves as a cholinesterase inhibitor, rotenone serves as a mitochondrial compound I inhibitor, a dual-action mechanism is formed, and meanwhile pollution caused by chemical pesticide residues is avoided.

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 invention discloses a method for preparing isopentenyl indole alkaloid Debromolustramine B. The isopentenyl indole alkaloid Debromolustramine B belongs to the technical field of organic synthesis, an o-bromo aniline aldehyde compound is used as an initial raw material, and on the basis of novel chiral p-toluene sulfinyl guidance, cheap copper catalysis amido alpha-position arylation and 3, 3-dimethyl allyl bromide cyclization reaction, the isopentenyl indole alkaloid Debromolustramine B is synthesized, and the isopentenyl indole alkaloid Debromolustramine B is obtained. According to the present invention, the key aryl quaternary carbon chiral center in the isopentenyl indole alkaloid Debomolustramine B is constructed, and the isopentenyl indole alkaloid Debomolustramine B with the butyrylcholine esterase inhibition activity is prepared through the subsequent series of chemical conversion, such that the material basis is provided for the further research of the natural product Debomolustramine B and the analogue thereof. The method has the advantages that the reaction conditions are mild, the cheap metal copper is used as the catalyst, the synthesis route is short, the energy consumption is low, the environmental protection is facilitated, and the large-scale chiral preparation of the isopentenyl indole alkaloid Debromofloutramine B is facilitated; the method also has the characteristics of relatively good atom economy and high product yield.

The invention discloses a preparation method and application of Y2O3-Co (OH) 2 particles, and belongs to the technical field of material preparation. The preparation method of the Y2O3-Co (OH) 2 particles comprises the following steps: mixing L-type amino acid containing amino and carboxyl functional groups with metal yttrium salt, carrying out microwave radiation heating reaction to obtain a deep eutectic solvent (y-DES), sequentially adding metal cobalt salt and an alkaline solution into the y-DES, continuously carrying out microwave radiation heating reaction until the metal cobalt salt and the alkaline solution are dissolved to obtain a brown mixed solution, and drying the brown mixed solution to obtain the Y2O3-Co (OH) 2 particles. And carrying out solid-liquid separation on the brown mixed solution after the reaction is completed, washing the precipitate, and drying to obtain Y2O3-Co (OH) 2 particles. According to the preparation method, the morphology of the Y2O3-Co (OH) 2 particles can be accurately regulated and controlled, the preparation process is simple, and an organic solvent does not need to be additionally added; the catalytic activity and the anti-interference capability are remarkably enhanced by constructing an efficient oxidation-reduction circulating system, and efficient determination of the organophosphorus pesticide in the acetylcholin esterase and inhibitor industrial wastewater is realized.

The invention provides a detection sensor and application thereof, and belongs to the field of pesticide detection. The detection sensor provided by the invention comprises an acetylcholine solution, an acetylcholin esterase solution, a choline oxidase solution, a Cu-BTC dispersion liquid and a solution containing a color developing agent capable of generating a hydroxyl color developing group, or comprises acetylcholine, a color developing agent capable of generating a hydroxyl color developing group and a Cu-BTC-based composite material; the Cu-BTC based composite material is prepared from Cu-BTC, choline oxidase and acetylcholin esterase, wherein the choline oxidase and the acetylcholin esterase are loaded on the Cu-BTC. Acetylcholine is hydrolyzed by acetylcholin esterase to generate choline, the choline is oxidized by choline oxidase to generate H2O2, the H2O2 is oxidized by Cu-BTC to generate. OH, and the. OH can oxidize a color developing agent to generate a colored substance. The organophosphorus pesticide can inhibit the activity of acetylcholin esterase to change the color of the solution, and then quantitative analysis of the organophosphorus pesticide is realized through the absorbance and the absorbance of a standard solution.

The present invention relates to a composite pharmaceutical composition for treating cerebral diseases, comprising a cholinesterase inhibitor and an antioxidant, and more specifically, to a composition for preventing or treating cerebral diseases, the composition comprises a cholinesterase inhibitor and an antioxidant, wherein the cholinesterase inhibitor and the antioxidant have a synergistic effect in the aspects of neuronal protection and neuronal differentiation promotion.

The invention relates to clinical medicine, and more particularly to lymphology, surgery, plastic surgery and oncology, for treating lymphatic swelling in the case of primary or secondary lymphoedema in adults and children, inter alia accompanied by infectious complications, and even more particularly relates to methods for treating lymphoedema and to the use of accessible drugs in the treatment of lymphatic swelling at any stage and in any location. The claimed method for the lymphotropic treatment of lymphoedema involves consecutively preparing an injectable drug composition A containing an adrenergic alpha-1 receptor agonist and a glucocorticoid, administering same by lymphotropic interstitial injection by puncturing the interstitial tissue of the lymphatic region of interest and introducing the drug composition, preparing an injectable drug composition B containing a cholinesterase inhibitor, administering same by lymphotropic interstitial injection by puncturing the interstitial tissue of the lymphatic region of interest and introducing the drug composition, and also, if necessary, preparing an injectable drug composition C containing bovhyaluronidase azoximer, and administering same by interstitial injection by puncturing the interstitial tissue of the lymphatic region of interest. The technical result consists in improving the drainage of free fluid from the tissues and reducing limb swelling in the case of lymphoedema.

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 discloses a pinanyl fluorescent probe for detecting the organophosphorus pesticide methyl parathion based on an enzyme inhibition mechanism, as well as its preparation method and application. The fluorescent probe is: 4-(2-(4-(cyclopropylformyloxy-4′-(6,6-dimethyl-2-(4-nitrophenyl)-4,5,6,7-tetrahydro-2H-5,7-methyleneindazole-3-yl)-[1,1′-biphenyl]-3-yl)vinyl)-1-methylpyridinium iodide (abbreviated as: THIP-OCP). The compound can undergo enzymatic hydrolysis reaction with butyrylcholinesterase and, under irradiation with ultraviolet light at a wavelength of 365nm, The solution's fluorescence color changes from colorless to orange-yellow. Since methyl parathion effectively inhibits butyrylcholinesterase activity, when methyl parathion is added to the solution, the solution's fluorescence gradually changes from orange-yellow to colorless under ultraviolet irradiation at a wavelength of 365 nm. Therefore, this compound can be used as a fluorescent probe for detecting methyl parathion. This compound has many advantages, including a low detection limit (0.79 μg / mL) and a wide pH range (5-10), and has great application prospects.

The invention belongs to the technical field of biomedical materials, and particularly relates to a response type near-infrared fluorescent probe targeting butyrylcholine esterase and beta amyloid protein as well as a preparation method and application of the response type near-infrared fluorescent probe. The response type near-infrared fluorescent probe is formed by connecting positively charged hemicyanine serving as a strong electron withdrawing group, carbon-carbon double bonds and thiophene serving as bridging units and phenylcyclopropionic acid carboxylate with a BChE recognition group, so that an organic small molecular fluorescent compound with a typical D-pi-A structure is formed. The fluorescent compound not only prolongs a conjugated structure to reach a near-infrared region, but also shows good biocompatibility, has no obvious toxic or side effect, is combined with a main marker BChE of AD and is converted into a fluorescence mode from a non-fluorescence mode, and in order to overcome the defect of single-target response, a fluorescent mode probe is further combined with A beta protein, so that the specific response is enhanced; the problem of false positive of a single target spot is effectively solved.

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 detection sensor and application thereof, and belongs to the field of pesticide detection. The detection sensor provided by the invention comprises acetylcholine, acetylcholin esterase, choline oxidase, two-dimensional Cu-TCPP (Fe) NSs and a color developing agent capable of generating a hydroxyl color developing group. The acetylcholin esterase can hydrolyze acetylcholine to generate choline, the choline is oxidized by the choline oxidase to generate H2O2, the H2O2 is oxidized by the two-dimensional Cu-TCPP (Fe) NSs to generate hydroxyl free radicals (. OH), and the. OH can oxidize a color developing agent capable of generating hydroxyl color developing groups to generate colored substances. When the organophosphorus pesticide exists in the to-be-detected liquid, the color of the solution is light blue or colorless; otherwise, the color of the solution is dark blue. The organophosphorus pesticide can inhibit the activity of acetylcholin esterase, so that the color of the solution is changed in the whole cascade catalytic amplification reaction, and then quantitative analysis of the organophosphorus pesticide is realized through a concentration-absorbance curve of the solution absorbance and the standard solution.

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 invention discloses bifidobacterium adolescentis capable of reducing related metabolic disorder occurrence risk caused by low estrogen level and application, and belongs to the technical field of microorganisms. The bifidobacterium adolescentis CCFM1507 provided by the invention can improve the level of estrogen in serum of ovariectomized rats, increase the expression quantity of CYP19 and ER alpha in adrenal gland tissues, and effectively inhibit the increased level of IL-10 and TNF-alpha and the reduced level of IL-4 in the serum; triglyceride (TG) and cholinesterase (CHE) in serum are remarkably reduced, and dyslipidemia is relieved; and the content of glutamine in serum is increased. The bifidobacterium adolescentis CCFM1507 disclosed by the invention is a food safety strain, can be used for preparing food, functional food or medicines, and has a wide application prospect.

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 invention relates to a method for purifying total phenylpropanoid from a lonicera macranthoides extract and application of the total phenylpropanoid in medicines. Relates to the technical field of traditional Chinese medicines, in particular to application of lonicera macranthoides total phenylpropanoid (TP) in preparation of medicines with functions of promoting oxidation resistance, reducing blood sugar, inhibiting cholinesterase and resisting inflammation. According to the present invention, a lonicera macranthoides extract is purified by using a macroporous resin, in particular an HPD100 resin, to obtain high-purity TP. The method comprises the following specific steps: (1) loading a sample containing the lonicera macranthoides extract into a macroporous adsorption resin column with the diameter-height ratio of 1: 5 at the flow rate of 1.5-2.5 mL / min; (2) eluting by using deionized water to remove unadsorbed liquid, wherein the dosage is 40-120mL; and (3) carrying out elution by using a 60% alcoholic solution at an elution flow rate of 1.5-2.5 mL / min to obtain the lonicera macranthoides TP. In-vitro experiments show that the purified product has remarkable antioxidant activity, blood sugar lowering activity, acetylcholin esterase inhibition activity and anti-inflammatory activity.

The invention relates to clinical medicine, and more particularly to lymphology, surgery, plastic surgery and oncology, for treating lymphatic swelling in the case of primary or secondary lymphoedema in adults and children, inter alia accompanied by infectious complications, and even more particularly relates to methods for treating lymphoedema and to the use of accessible drugs in the treatment of lymphatic swelling at any stage and in any location. The claimed method for the lymphotropic treatment of lymphoedema involves consecutively preparing an injectable drug composition A containing an adrenergic alpha-1 receptor agonist and a glucocorticoid, administering same by lymphotropic interstitial injection by puncturing the interstitial tissue of the lymphatic region of interest and introducing the drug composition, preparing an injectable drug composition B containing a cholinesterase inhibitor, administering same by lymphotropic interstitial injection by puncturing the interstitial tissue of the lymphatic region of interest and introducing the drug composition, and also, if necessary, preparing an injectable drug composition C containing bovhyaluronidase azoximer, and administering same by interstitial injection by puncturing the interstitial tissue of the lymphatic region of interest. The technical result consists in improving the drainage of free fluid from the tissues and reducing limb swelling in the case of lymphoedema.

The present disclosure pertains to a method of detecting an opioid in a sample by (1) determining a butyrylcholinesterase inhibition activity of the sample; and (2) correlating the butyrylcholinesterase inhibition activity of the sample to the presence or absence of opioid in the sample, where no relative inhibition of butyrylcholinesterase activity is correlated to the absence of opioid in the sample, and where a relative inhibition of butyrylcholinesterase activity is correlated to the presence of opioid in the sample. The present disclosure also pertains to assays for detecting opioid in a sample in accordance with the methods of the present disclosure.

The invention provides application of boxthorn leaf total alkaloids in preparation of an acetylcholin esterase inhibitor, and belongs to the technical field of traditional Chinese medicines. The invention proposes that the boxthorn leaf total alkaloid has an acetylcholin esterase inhibiting effect for the first time, and the boxthorn leaf total alkaloid can be developed into an acetylcholin esterase inhibitor for preventing and treating diseases related to abnormal rise of acetylcholin esterase. Meanwhile, compared with an existing boxthorn leaf total alkaloid preparation method in the field, the boxthorn leaf total alkaloid preparation method provided by the invention is simpler, and the boxthorn leaf total alkaloid can be obtained without extracting by using organic solvents such as ethyl acetate and the like which are mutually soluble with water.