103 results about "Choline esterase activity" patented technology

Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure: Formula (I) wherein A is selected from the group consisting of an unsubstituted aryl, a substituted aryl, an unsubstituted heteroaryl and a substituted heteroaryl. The carbamoyl esters are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the carbamoyl esters can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

The present invention relates to a method for analyzing residual agricultural chemicals which comprises the steps of acting a reduced glutathione as a reactive substrate and a glutathione transferase serving as a catalyst for the reaction on a carbofuran derivative or a methomyl derivative as a carbamate type agricultural chemical of a new series to thus derivatize the agricultural chemical into a substance having a high choline esterase-inhibitory activity; reacting the substances formed through the derivatization reaction with a choline esterase; and then detecting the presence of the agricultural chemical as the new series of carbamate type one included in a sample to be examined on the basis of the changes in the choline esterase activity thus detected. The method of the present invention may serve as a powerful tool for the detection of the residual agricultural chemicals in grains such as rice and the detection of the content of agricultural chemicals remaining in agricultural products such as vegetables and fruits.

The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells.

Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

The present invention relates to an application of acetylcholinesterase inhibitor for curing diabetes. The described inhibitor includes all the compounds which can inhibit acetylcholinesterase activity and have the action for curing diabetes. The invented experimental results show that these inhibitors have the actions of inhibiting beta-cell death and reducing blood sugar concentration of diabetic model mouse, and can effectively cure or improve diabetes symptom.

The invention belongs to the field of medical examination and relates to a method capable of synchronously determining the concentrations of a plurality of local anesthetic drugs in human plasma. The method adopts a plasma cholineesterase inhibitor to inhibit the activity of plasma cholinesterase under ice bath condition below 3 DEG C, which controls the hydrolysis of totokaine and assures the accuracy of the method; by utilizing characteristics that lidocaine, ropivacaine and bupivacaine have stronger characteristic of ultraviolet absorption at wavelength of 210nm, and procaine and the totokaine have stronger characteristic of ultraviolet absorption at wavelength of 290nm, an ultraviolet dual-wavelength method is used to detect after the separation of an acid mobile phase at a chromatographic column; and the method can ensure that the sensitivity of synchronous determination of the local anesthetic drugs is greatly improved. The method has less sampling from samples and simple, quickand sensitive pretreatment, does not need expensive equipment or reagents, has short analysis period and low cost, and is suitable for the monitoring of clinical conventional blood concentration of aplurality of drugs.

The invention discloses application of ethyl asterrate in preparation of an anti-alzheimer medicine, and in particular relates to application of diphenyl ether compound ethyl asterrate shown in the structural formula (I) in inhibition of the activity of acetylcholine esterase and preparation of an anti-alzheimer medicine. Experiments prove that the ethyl asterrate can remarkably inhibit the activity of acetylcholine esterase, can remarkably improve the memory and space exploration capability of an alzheimer rat model caused by D-galactose and AlCl3, can be applied to preparation of the anti-alzheimer medicine, and indicates an excellent market application prospect.

The invention relates to the field of traditional Chinese medicine preparation and relates to a preparation method of a chimonanthus inhibited acetylcholinesterase active part and application thereof. The preparation method comprises the following steps of: ethanol lixiviation, low-polarity solvent extraction, acid-solution and alkali-isolation chloroform extraction or alkali-solution and acid-isolation, centrifugation and ethyl acetate extraction. The extracted active part includes three categories of substances, namely alkaloids, flavonoids and coumarins respectively. The active part has relatively strong inhabitation effect on the activity of acetylcholinesterase and has a wide application range in preparing medicaments for preventing and treating related symptoms or diseases caused by acetylcholine deletion, particularly the medicaments for preventing and treating senile dementia.

The invention discloses a marine fungus Trichoderma harzianum DLEN2008005 and application thereof. The marine fungus Trichoderma harzianum DLEN2008005 is collected in China General Microbiological Culture Collection Center (CGMCC) on January 29, 2016, the collection number is CGMCC No.12105, and the collection address is Institute of Microbiology of Chinese Academy of Sciences, Datun Road, Chaoyang District, Beijing City. Meanwhile, active substances in standing fermentation liquid of the marine fungus Trichoderma harzianum DLEN2008005 are extracted and purified, and the strain, a culture of the strain and an extract of the fermentation liquid have very good antioxidant activity and acetylcholin esterase inhibition activity and have very good application prospects in preparation of anti-senile dementia medicines, antioxidant medicines and / or medicines for inhibiting the activity of acetylcholin esterase.

The invention discloses a catechin derivative with the structure represented by formula (I) shown in the description. In the formula (I), R1 and R2 are respectively independently selected from H, OH and OCH3. The catechin derivative with the structure represented by formula (I) is extracted from Zijuan tea for the first time. The catechin derivative has a strong acetylcholinesterase inhibition effect, and the IC50 value of the catechin derivative can reach 2.33 [mu]M, 11.33 [mu]M and 62.10 [mu]M, so the catechin derivative has an acetylcholinesterase activity inhibition effect, has wide application prospect in finding and preparation of anti-acetylcholinesterase medicines, and provides a research direction for researches of the preparation of the anti-acetylcholinesterase medicines.

The invention discloses an electrochemical biosensor based on polypeptide analog with the electrocatalytic activity for acetylcholin esterase detection. The biosensor for acetylcholin esterase detection is characterized by comprising the following steps: (1) intensively stirring and uniformly mixing silver nitrate, L-cysteine and secondary distilled water on a stirrer, and incubating in an oscillator; (2) electrodepositing graphene onto a bare glassy carbon electrode by utilizing an electrochemical method, mixing 0.05 weight percent of a Nafion solution with the solution obtained in the step (1), and dropwise coating GO / GCE to obtain an electrochemical biosensor based on the polypeptide analog with electrocatalytic activity (CP / GO / GCE); (3) performing acetylcholin esterase activity detection, namely catalyzing acetylcholine in one step to generate H2O2, uniformly mixing acetylcholine, AchE and choline oxidase, and incubating to generate H2O2, and detecting the solution with the sensorprepared in the step (2) with good specificity, high sensitivity, high detection speed, accurate and reliable result; and (4) performing AChE inhibitor malathion detection, namely uniformly mixing acetylcholine, AChE, malathion and choline oxidase, incubating, and detecting the solution with the sensor prepared in the step (2). The biosensor has the advantages of good specificity, high sensitivity, high detection speed and accurate and reliable result.

The invention discloses multiple-target effects of an isoflavone derivative and its application in improvement of learning and memory. Specifically, the invention discloses that a compound J39136 has the effects of: upregulating the expression of SIRT1 protein with damage repair and neuroprotective effects; inhibiting the activity of acetylcholinesterase and butyrylcholinesterase, and dose-dependently inhibiting the acetylcholinesterase activity of cells under a safe dose; protecting nerve cells, inhibiting abnormal expression of beta-APP, and reducing Abeta1-42 secretion; and regulating neuroinflammation. Animal experimental results prove that J39136 has low toxicity, can penetrate the blood-brain barrier, and can significantly improve scopolamine caused mouse dementia and strengthen learning and memory functions. Preclinical study results prompt that J39136 is expected to become the drug for prevention and / or treatment of learning and memory disorder and Alzheimer's disease.

The invention belongs to the field of medicine research and development, relates to a medicinal substance, and particularly relates to a medicinal substance with dementia resistance and a preparation method thereof. The medicinal substance is obtained by performing ethanol extraction and macro-porous adsorption resin purification on Kaixin powder, and is enriched with phenolic acid ingredients and terpene ingredients in the Kaixin powder; meanwhile, mouse dysmnesia tests prove that the medicinal substance can be used for strengthening the capability of passive escape electrical stimulation of mice, reducing error times and reducing the activity of acetylcholin esterase in the cerebral cortex of a mouse, so that the aims of improving memory and resisting dementia can be achieved.

The invention provides a determination method capable of sensitively detecting the activity of acetylcholin esterase by using bifunctional quantum dots which can simultaneously generate sensitive response to two reaction substrates of thio-choline and hydrogen ions in an acetylcholin esterase catalytic system. The bifunctional quantum dots capable of simultaneously responding thio-choline and hydrogen ions are provided; and a method for detecting the activity of acetylcholin esterase is established by combining a catalytic reaction of acetylcholin esterase. The system is composed of mercaptoacetic acid-modified bifunctional cadmium telluride quantum dots, acetylthiocholine and a Tris-HCl buffer solution with a pH value of 7.5. The method comprises the following steps of synthesis of the bifunctional quantum dots, preparation of the reaction solution and detection of the activity of acetylcholin esterase by using the bifunctional quantum dot sensor system. The method has the advantages of novel principle, high sensitivity, simple synthetic method, simple system constitution, no need of biological coupling reaction, etc. The method is suitable for the activity determination of acetylcholin esterase and other detections of target objects related to the activity determination.

The invention belongs to the field of biological medicines, and particularly relates to research of an asterric acids compound for inhibition of activity of acetylcholin esterase as shown in general formula (I). The invention provides application of a compound with the structure as shown in general formula (I) and as an acetylcholin esterase inhibitor.

The invention discloses application of pepper plant essential oil, namely application of pepper plant essential oil in the preparation of drugs or health products for treating and preventing Alzheimer's disease; the application of the pepper plant essential oil in the preparation of drugs or health products for treating and preventing Alzheimer's disease is attributed to the action mechanism of the pepper plant essential oil in significantly inhibiting acetylcholinesterase activity, and in-vivo activity experiment further verifies that the pepper plant essential oil can significantly improve Alzheimer's disease and its symptoms, and the application is totally different from that of existing drugs or health products of pepper plant essential oil.

The present invention is related to a composition for preventing and treating dementia containing the extracts of ganoderma lucidum, oleamide and its structural analogues as effective components. Since the composition according to the present invention prevents reduction of the amount of acetylcholine in the brain and shows the protective effect for cerebral tissues damaged by cerebral ischemia as it inhibits the activity of acetylcholinesterase (AChE) of animal cerebral tissues, it may be used for a prevention and treatment agent not only for the Alzheimer's disease but also vascular dementia.

The invention relates to a cholinesterase activity detection test paper strip based on silver nanoparticles. The test paper strip comprises a paper board, wherein water absorbent paper, a detection pad, a reduction pad and a sample pad are sequentially adhered on one side of the paper board from top to bottom, and the adjacent pads are overlapped and connected at the joints; the detection pad is a cellulose nitrate film, three detection lines are arranged on the film from top to bottom, and the detection lines are respectively coated with silver nitrate water solutions with concentrations from high to low; and the reduction pad is glass fiber and is sprayed with a certain concentration of HEPES solution of vitamin C. The test paper strip can be used for rapid detection of activity of cholinesterase and has the advantages of simplicity and convenience in use, high sensitivity, capability of obtaining detection results without relying on analysis of instruments and the like. The detection sensitivity of the established detection test paper strip against active cholinesterase can achieve 0.01nM, so that a new method can be provided for detection of the activity of cholinesterase.

The invention discloses hypocrea lixii DLEN2008010 as well as a preparation method and application of an active extract of fermentation liquor thereof. The hypocrea lixii DLEN2008010 is preserved in China General Microbiological Culture Collection Center (CGMCC) on August 16, 2016, and has a preservation number of CGMCC No. 12868. Active materials of standing fermentation liquor of the hypocrea lixii DLEN2008010 are extracted and purified; the total extract of the fermentation liquor of the hypocrea lixii DLEN2008010 can well resist oxidation and inhibit the activity of acetylcholin esterase; the purified active extract of the fermentation liquor of the hypocrea lixii DLEN2008010 can well inhibit the activity of the acetylcholin esterase; therefore, the active extract of the fermentation liquor of the hypocrea lixii DLEN2008010 has good application prospect in the aspects of preparation of medicines for resisting alzheimer's disease and preparation of medicines for inhibiting the activity of the acetylcholin esterase.

The invention discloses application of fructus ziziphi jujubae in preparing of a medicine or a health-care product for treating Alzheimer disease. An experimental research shows that the fructus ziziphi jujubae and extract thereof can improve the space learning and memory ability of an model mouse with Alzheimer disease, shorten the escape latent period and the search distance of the mouse, meanwhile reduce the oxidative damage degree of the brain tissue of the mouse, inhibit the activity of the acetylcholin esterase in the brain tissue, and achieve a good effect of preventing and treating the Alzheimer disease. The fructus ziziphi jujubae and the extract thereof are expected to be developed to be the new-generation safe and effective medicine or the health-care product for treating the Alzheimer disease.

The invention discloses a compound for inhibiting acetylcholinesterase activity. The compound is characterized as the structure of the compound is described in the description, wherein n=1-3, R1 is selected from oxyl, halogen, alkyl, -H, -CN or -NO<2>. The compound can be simultaneously bound with a plurality of application sites such as a catalytic site of the AChE center and a peripheral anion site, has good inhibition activity for acetylcholinesterase, and can be used in medicine for treating Alzheimer's disease.

Phenserine compounds and pharmaceutically acceptable salts thereof are found to be useful in the management or treatment of diabetes and / or complications, such as vascular dementia, and insulin resistance, associated with diabetes. The phenserine compounds of the invention are carbamates that inhibit the activity of acetylcholinesterase.

The invention relates to an extract of radix sophorae tonkinensis, as well as a preparation method, a detection method and application thereof, and in particular relates to an ethyl acetate extract of radix sophorae tonkinensis, as well as a preparation method, a detection method and application thereof. The ethyl acetate extract is prepared by virtue of the following steps: immersing the radix sophorae tonkinensis with petroleum ether; leaching petroleum ether, recycling residues, and volatizing the petroleum ether in the residues; performing reflux extraction with ethanol, and concentrating the extract until the extract does not have smell of alcohol; extracting the concentrated solution with ethyl acetate of which the volume is the same as that of the concentrated solution; collecting the supernate, and evaporating to obtain the ethyl acetate extract. In vitro tests discover that the ethyl acetate extract of radix sophorae tonkinensis provided by the invention can be used for inhibiting the activity of butyrylcholine esterase, and is remarkable in effect.

The invention discloses herba argyreiae acutae alkali as well as an extraction method and a purpose thereof. The extraction method of the herba argyreiae acutae alkali comprises the following steps of (1) grinding herba argyreiae acutae into powder; adding an ethanol solvent; using a cold soaking method for extraction; evaporating an ethanol solvent to obtain a first extract; (2) adding water into the first extract to form suspension liquid; sequentially adding petroleum ether, ethyl acetate and n-butyl alcohol for extraction; collecting n-butyl alcohol extraction liquid; concentrating the n-butyl alcohol extraction liquid into an extract to obtain a second extract; (3) performing macroporous resin column chromatography separation for the second extract; performing gradient elution with water-ethanol as an eluent; collecting the elution solution with the ethanol mass percentage being 40 to 70 percent; concentrating the elution solution to obtain a third extract; (4) performing methanol recrystallization on the third extract; obtaining a target product of the herba argyreiae acutae alkali. The extraction method is simple and convenient; the implementation is easy; the extraction rate is high; the compound has good anti-inflammatory effects and excellent acetylcholinesterase activity inhibition effects.

The invention relates to the fields of organic chemistry, pharmaceutical chemistry and pharmacology, in particular to an aryl pyridone derivant with the function of inhibiting the activity of acetylcholinesterase, namely a 6-aryl-substituted methylene-pyridone derivant and a medicinal salt thereof. The invention also relates to a method for preparing a compound and medical application thereof. The compound can inhibit activity of acetylcholinesterase and is expected to be used as a drug for preventing and treating senile dementia.

The invention discloses a vegetable oil composition with an effect of preventing and treating Alzheimer's disease as well as a preparation method thereof. The vegetable oil composition is prepared from the following raw materials in parts by weight: 1-20 parts of gardenia oil, 5-50 parts of jujube seed oil, 1-20 parts of ginkgo oil, 1-20 parts of Chinese magnoliavine fruit oil, 10-80 parts of flaxseed oil and 5-50 parts of safflower oil. The vegetable oil composition provided by the invention is prepared by screening and optimizing by virtue of a lot of experiences, and is also prepared by adopting vegetable oil which is prepared from natural traditional medicinal and edible plants with multiple medicinal healthcare effects by virtue of a modern preparation process and has a healthcare effect; and experimental results show that the vegetable oil composition provided by the invention can improve spatial learning and memory abilities of a senile dementia model mouse and shorten the escape latency and the scouting distance of the senile dementia model mouse, can reduce the oxidation damage degree of brain tissues of the mouse and inhibit the activity of acetylcholine esterase in the brain tissues at the same time, has very good prevention and treatment effects on the Alzheimer's disease, and can be used for preventing and treating the symptoms of amnesia, insomnia, dysphoria and the like of the Alzheimer's disease.

The invention discloses a class of carbamate-chalcone cholinesterase inhibitors and a preparation method and application thereof, belonging to the field of medicinal chemistry. The general chemical structure formula of the cholinesterase inhibitor of the present invention is shown in formula (I), wherein A, B, V, X, Y, and Z are as defined in the present invention. The carbamate-chalcone cholinesterase inhibitor of the present invention has stronger acetylcholinesterase inhibitor activity, butyrylcholinesterase inhibitory activity and selective inhibition of butyrylcholinesterase activity, It has lower neurotoxicity and can be applied to the preparation of medicines for treating and preventing diseases caused by cholinesterase.

The invention discloses a choline esterase visual colorimeter and a preparation method for the same, comprising a test paper wool and a standard colorimeter, wherein, the standard colorimeter comprises six color blocks; the color of each color block is the same with the color of blood with corresponding choline esterase activity; each color block represents corresponding choline esterase activity which is relatively 0 percent, 30 percent, 50 percent, 70 percent, 80 percent and 100 percent from light to heavy; an interpretation hole is arranged on the center of each color block; the size of the interpretation hole is equal to the area of a round which is formed by tiling of a drop of blood; the reverse sides of the color blocks of the standard colorimeter are provided with pressed films. The invention also comprises a transparent thin plastic sealing sack with an area which is slightly larger than that of the test paper wool. The preparation method and the use method of the invention are very simple and convenient; because a reagent strip is directly compared with the standard colorimeter and no transparent thin plate is isolated between, the detection result is more accurate; the choline esterase visual colorimeter can be used under a common daylight lamp, does not need a power source and batteries, has smaller volume, is convenient in carrying, and greatly reduces the cost.

The invention provides new application of indole-3-carbinol (I3C), diindolyl methane (DIM) and derivative compounds thereof in preparation of medicaments for treating senile dementia. By improving the expression of intracellular free radical resistant specific genes, the medicaments can enhance the automatic free radical clearing capacity of cells and lighten the harm of free radicals to the cells and tissues. The DIM, the I3C and the derivative compounds can effectively reduce the pathogenetic symptoms of senile dementia animal models, obviously improve the dyskinesia of SAM-P / 8 mice, obviously improve the superoxide dismutase (SOD) activity of brain tissues of the SAM-P / 8 mice, reduce the methylene dioxyamphetamine (MDA) content of brain tissues, reduce the choline esterase activity of the brain tissues and enhance the activities of Na<+>-K<+>-ATP enzyme and Ca<2+>-ATP enzyme of the brain tissues, so the DIM, the I3C and the derivative compounds can be used as candidate medicament molecules for treating the senile dementia. Meanwhile, the adopted small molecular substances are easily obtained, are low in price, stable in properties and convenient for storage and transportation, and have broad application prospect.