35 results about "Anti acetylcholinesterase" patented technology

The invention discloses preparation and application of total alkaloids extract and effective components in peganum plant seeds. The peganum plant (comprising harmel, multisectum peganum and peganum nigellastrum) seeds are heated, refluxed and extracted by ethanol, dissolved along with heat, acidulated by added 2 to 10 percent hydrochloric acid, and basified by ammonia water to separate out sediment; and the sediment is dried to obtain the total alkaloids extract mainly containing dehydrogenized peganine and peganine according to a proportion of between 0.18 to 1 and 4.30 to 1, wherein the content of the total alkaloids is more than 50 percent. The total alkaloids extract is separated by chromatography to obtain ten effective monomer components such as the dehydrogenized peganine, the peganine, and the like. Through thin layer chromatography and biological self-developing analysis, the total alkaloids extract and the effective monomer components thereof have the effect of resisting activity of acetylcholine esterase, and can be used for preparing medicament for resisting the activity of the acetylcholine esterase and medicament for treating neurodegenerative diseases.

The invention discloses an amino sugar thiazole derivative as well as a synthetic method thereof. When synthesis is carried out, glucosamine hydrochloride is taken as a raw material, and benzyl ether protection is carried out on hydroxy, so that the selective reaction of amino is realized, a novel intermediate glycosyl thiourea-N-(1,3,4,6-tetra-0-benzyl-2-deoxygenation- beta-D-glucopyranose-2-group) thiocarbamide is synthesized, and glycosyl thiazole-N-(1,3,4,6-tetra-0-benzyl-beta-D-glucopyranose-2-group)-2-amido-4-substituted thiazole is synthesized by cyclizing the novel intermediate glycosyl thiourea-N-(1,3,4,6-tetra-0-benzyl-2-deoxygenation beta-D-glucopyranose-2-group) thiocarbamide with 1-bromine-2-substituted ethyl ketone. The synthetic method disclosed by the invention has the advantages of easiness and safety for operation, wide application scope, low cost of the raw material, easiness for raw material obtaining, easiness and convenience for post-processing and high yield, is a fast high-efficiency synthetic method and has a wide application prospect on the aspect of preparing an acetylcholinesterase resistant drug because the synthesized compound has high inhibiting effect on acetylcholinesterase.

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 provides a 1,3,4-oxadiazole derivative containing glucosamine molecules. R in the molecular formula is selected from -CH3, -C2H5, -C4H11, -C6H5, -C5H4N, 4-OHC6H4-, 3-CH3C6H4, 4-CH3C6H4-, 3-CH3OC6H4-, 2-NO2C6H4-, 4-NO2C6H4-, 2-FC6H4-, 4-FC6H4-, 2-ClC6H4-, 3-ClC6H4-, 3-BrC6H4-, 4-IC6H4-, 4-N (CH3)2C6H4-, -C4H3S, and -C4H3O. The invention further discloses a synthesis method and application of the 1,3,4-oxadiazole derivative containing the glucosamine molecules. The adopted synthesis method has the advantages of being easy and convenient to implement, rapid, high in applicability, efficient and the like. An adopted cyclization reagent has the advantages of being low in price, low in toxicity and the like. The glucosamine molecules are introduced into the 1,3,4-oxadiazole molecules, and the synthesized target compound has the strong inhibitory activity for acetylcholin esterase, thereby having the wide application prospect in the aspect of preparation of anticholinesterase medicine.

The invention belongs to the technical field of fungus biological medicine application, and particularly relates to a styela plicata-derived fungus and application thereof. The styela plicata-derived fungus, Beauveria felina fungus strain SYSU-MS7908, can be metabolized to synthesize a pyridine-containing novel skeleton meroterpenoid compound--amphichoterpenoid. Experimental verification shows that the compound has remarkable acetylcholinesterase activity resistance, and has a good development prospect in the preparation of medicines for preventing and / or treating acetylcholinesterase-mediated diseases; and modern microbial fermentation engineering technology is used for reproduction, and worries about raw materials are avoided. Meanwhile, the invention has the advantages that ecological balance is not destroyed, industrialization is easy to achieve, etc. The styela plicata-derived fungus is a renewable drug resource with development prospects, and abundant raw materials are provided for research and development of marine microbial products and marine microbial drugs.

The invention relates to a glucosamine-containing 1,3,4-thiadiazole derivative and a synthesis method of the lucosamine-containing 1,3,4-thiadiazole derivative. The method comprises the following steps: reacting 2-desoxy-2-isorhodanate-1,3,4,6-tetra-O-benzyl-beta-D-glucopyranose with hydrazine hydrate to synthesize an intermediate glycosyl thiosemicarbazide, and reacting with substituted aldehyde and a Fe<3+> compound to synthesize the N-(5-substituted-1,3,4-thiadiazolyl-2-yl)-1,3,4,6-tetra-O-benzyl-2-desoxy-beta-D-glucosamine. The synthesis method is simple and safe to operate, and has the advantages of small environmental pollution, high yield and simple after-treatment. The synthesized compound has a strong inhibiting effect on acetylcholinesterase, and has wide application prospects in the aspect of preparation of anti-acetylcholinesterase drugs.

The invention discloses a club moss alkaloid compound or a pharmaceutical salt thereof represented by the structural formula (I) where R1 is hydrogen, aryl, substituted aryl, alkyl or substituted alkyl, R2 is hydrogen, hydroxyl or a halogen atom, R3 is hydrogen, aryl, substituted aryl, alkyl or substituted alkyl, R4 is hydrogen, hydroxyl or a halogen atom, and n is an integer from 0 to 4, as well as a preparation method of the club moss alkaloid compound, a medicine composition containing the compound of the type, a plant extract and application of the compound of the type, the medicine composition of the compound and the extract in preparation of an anticholinesterase inhibitor medicine, preparation of a medicine for treating the alzheimer's disease and preparation of a medicine for treating the memory and cognitive impairment diseases of middle-aged and old people. Club moss alkaloids are diversified natural alkaloids which are of similar and unique structures, separated from fern club moss and relative plants thereof, and have the same biogenesis.

The invention relates to carboline compounds, and a synthetic method and anti-acetylcholinesterase activity thereof. The carboline compounds have been proved to have a plurality of biological activities like anti-microbe activity, anticancer and anti-virus activity; however, researches on the anti-acetylcholinesterase activity and anti-cholinesterase activity have not been reported in the prior art. The carboline compounds provided by the invention are classified into a class A, a class B, a class C and a class D, wherein the class B and the class D are 2-aryl carboline salt compounds while the class A and the class C are 2-aryl-3,4-dihydrocarboline salt compounds. Results of activity determination show that the compounds provided by the invention have substantial anti-acetylcholinesterase and anti-cholinesterase activities and have great potential as active ingredients for preparation of drugs used for treating the Alzheimer disease.

The gram Liewei mellow preparation method and in the system anti-acetylcholin esterase medicine's application, relates to one kind of gram Liewei to be mellow, and provides one kind to originate from the mangrove forest endogenous fungus secondary metabolite gram Liewei mellow preparation method and the application. The preparation method is: dwarf rods Aspergillus BYY-1 seed culture; submerged fermentation; broth filter strains; concentrated filtrate decompression after repeatedly using organic solvent extraction, collection and decompression organic phase was concentrated extracts; Extracts of the silica gel column chromatography and recrystallization obtained after refining grams Levy alcohol. Levy alcohol grams of acetylcholinesterase inhibition with notable is a reversible inhibitor of acetylcholinesterase, can be used for the treatment of Alzheimer's and other associated with a lack of acetylcholine diseases drugs.

The present invention relates to novel uses of antisense oligonucleotides targeted to the coding region of acetylcholinesterase (AChE) for treating inflammatory disorders other than inflammatory disorders of the central nervous system or the peripheral nervous system innervating voluntary muscles. More particularly, the present invention relates to uses of antisense oligodexoynucleotides targeted to AChE mRNA for treating inflammatory disease of the gastrointestinal tract including inflammatory bowel disease.

The invention provides an anti-acetylcholinesterase active composition in Chinese mahonia stem, and a screening method and application of the anti-acetylcholinesterase active composition. The composition is prepared from columbamine, jateorhizine, palmatine and berberine. According to the anti-acetylcholinesterase active composition, the traditional Chinese medicine Chinese mahonia stem is taken as a study object, based on an affinity chromatography principle, an immobilized enzyme technology is combined, an acetylcholinesterase reactor is prepared, an active compound fishing platform is constructed, four active components for anti-acetylcholinesterase are successfully screened and identified, an effective screening method for discovery of extracting anti-acetylcholinesterase active substances from the Chinese mahonia stem, when the compounds columbamine and jateorhizine are fixed, other compounds are correspondingly added to be mixed with the columbamine and the jateorhizine, when theconcentration of the columbamine or the jateorhizine is below IC60 or IC70, the obvious synthesis or summation effect occurs, according to the research, the compound components developing the anti-AChE activity in the Chinese mahonia stem extraction are discovered and identified for the first time, the combination with synthesis or summation is obtained, and the combination can be assuredly developed to a potential anti-AChE inhibitor.

The present invention relates to new substituted carbamic acid quinoline-6-yl esters of formulae 1 and 2 where R1=alkyl, aryl; R2=H, alkyl, aralkyl useful as acetylcholinesterase inhibitors, and which show potent antiacetylcholinesterase activity and have potential therapeutic use for prevention or cure of acetylcholinesterase related disorders including peripheral as well as central nervous system.

The invention discloses a colloidal gold chromatographic rapid diagnosis test paper strip used for detecting acetylcholine esterase and a preparation method thereof. The diagnosis test paper strip comprises, in a successively connected manner on a hard plastic bottom board, water-absorbing filter paper, a cellulose acetate membrane detection pad on which an anti-acetylcholine esterase monoclonal antibody (detection zone) and a rabbit-anti-mouse IgG (quality control zone) are immobilized, a colloidal gold pad on which the anti-acetylcholine esterase monoclonal antibody is labeled, and a sample pad for placing a sample. The colloidal gold test paper strip is used for detecting the acetylcholine esterase in a solution by naked eyes and has the following advantages: 1) usage amounts of reagents and sample are very low, wherein the sample size is low to 10-20 [mu]l, so that the concentration of the acetylcholine esterase in a specimen eluant can be increased without less possibility of false negative results; 2) the test paper strip is free of expensive instruments and adapts field application better; 3) detection time is greatly reduced and detection speed is increased; and 4) the test paper strip can be preserved at room temperature and only needs to keep dry.

The present invention relates to novel uses of antisense oligolucleotides targeted to the coding region of acetylcholinesterase (AChE) for treating inflammatory disorders other than inflammatory disorders of the central nervous system or the peripheral nervous system innervating voluntary muscles. More particularly, the present invention relates to uses of antisense oligodexoynucleotides targeted to AChE mRNA for treating inflammatory disease of the gastroinstestinal tract including inflammatory bowel disease.

The invention discloses preparation and application of total alkaloids extract and effective components in peganum plant seeds. The peganum plant (comprising harmel, multisectum peganum and peganum nigellastrum) seeds are heated, refluxed and extracted by ethanol, dissolved along with heat, acidulated by added 2 to 10 percent hydrochloric acid, and basified by ammonia water to separate out sediment; and the sediment is dried to obtain the total alkaloids extract mainly containing dehydrogenized peganine and peganine according to a proportion of between 0.18 to 1 and 4.30 to 1, wherein the content of the total alkaloids is more than 50 percent. The total alkaloids extract is separated by chromatography to obtain ten effective monomer components such as the dehydrogenized peganine, the peganine, and the like. Through thin layer chromatography and biological self-developing analysis, the total alkaloids extract and the effective monomer components thereof have the effect of resisting activity of acetylcholine esterase, and can be used for preparing medicament for resisting the activity of the acetylcholine esterase and medicament for treating neurodegenerative diseases.

The invention relates to the field of extraction and separation of traditional Chinese medicines, in particular to a novel oxygen-containing benzoic acid compound extracted, separated and identified from purslane and an extraction and separation method thereof. The molecular formula of the novel compound is C14H16O7, and the new compound is named as 4-((4-ethoxy-1,4-dioxobutan-2-yl)oxy)benzoic acid according to the structure of the new compound. The invention also provides an extraction and separation method of the novel compound. The extraction and separation method sequentially adopts ethanol reflux extraction, silica gel column chromatography, polyamide column chromatography, ODS medium-pressure column purification, Bond Elut SI silica gel column chromatography and HPLC for separation, purification and preparation. The structure of the compound is identified as a novel oxygen-containing benzoic acid compound by adopting UHPLC-ESI-QTOF / MS, 1H-NMR, 13C-NMR and two-dimensional nuclear magnetic spectrum analysis methods. The novel oxygen-containing benzoic acid compound has potential neuro-protection activity, acetylcholin esterase resistance activity and the like, and the novel oxygen-containing benzoic acid compound and the salt or the derivative thereof can be used as a synthesis primer of other compounds and a raw material for new drug development and pharmacological activity research. The compound is used for preparing medicines or health-care products for protecting nerves and resisting acetylcholin esterase.

The invention discloses application of a series of 8-substituted oxoisoaporphine derivatives, specifically application of 8-substituted oxoisoaporphine derivatives or pharmaceutically acceptable salts thereof in preparation of Abeta aggregation inhibitor drugs, as well as application in preparation of drugs inhibiting acetylcholin esterase and resisting Abeta aggregation at the same time. The inventor finds that the derivatives not only has very good inhibitory activity in vitro to acetylcholin esterase, but also has good anti-acetylcholin esterase in vivo, and the compounds have very good anti-Abeta aggregation activity both at the molecular level and at the cellular level. More rarely, most of the compounds can penetrate the blood-brain barrier and have low toxicity, and have good application prospects in treatment of Alzheimer disease, cerebrovascular dementia and other diseases. The structure of the8-substituted oxoisoaporphine derivatives is shown as the specification, wherein n=1-5.

The invention relates to a compound of formula I or pharmaceutically acceptable salt and a preparation method thereof, as well as a drug composition containing the same. The compound of formula I is novel piperazine and homopiperazine derivative, which can be used for preparing cervical cancer-treating medicine, anti-acetylcholinesterase and butyrylcholinesterase medicine, and medicine for treating staphylococcus aureus infection.

The invention relates to a compound of formula I or pharmaceutically acceptable salt and a preparation method thereof, as well as a drug composition containing the same. The compound of formula I is novel piperazine and homopiperazine derivative, which can be used for preparing cervical cancer-treating medicine, anti-acetylcholinesterase and butyrylcholinesterase medicine, and medicine for treating staphylococcus aureus infection.

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 relates to a pregabalin derivative shown in formula I and application thereof in medicine for resisting senile dementia. Acetylcholinesterase in vitro test model shows that the pregabalin derivative has remarkable acetylcholinesterase resistance activity so as to be used for preparing the medicine for resisting senile dementia. The pregabalin derivative has the chemical structural formula shown by the formula I, and R in the formula is defined by the specification. Formula I.

The invention discloses application of 2-gylcosyl chinoline compound in preparing acetylcholine esterase resisting medicines. The 2-gylcosyl chinoline compound is of a structural formula as shown in formula (I), wherein R1, R2, R3 and R4 independently choose -H, -OCH3 or -Br. A preparation method of the 2-gylcosyl chinoline compound can be produced according to the prior art. The 2-gylcosyl chinoline compound is strong in dissolubility in water, high in biological utilization, strong in restrain activity on acetylcholine esterase and wide in application prospect on preparing acetylcholine esterase resisting medicines. The 2-gylcosyl chinoline compound is simple in preparation path, low in cost, small in environment pollution and suitable for large-scale industrial production.

The invention discloses a huperzia serrata endophytic fungus Eurotiaceae Penicillium L10Q37 strain which is collected in China Center for Type CultureCollection on January 12, 2014 with a collection number of CCTCC NO. M2014021. A fermentation product, a fermentation liquor extract and a thallus extract, obtained by fermenting the fungus, have anti-acetylcholine activity and can be used for preparing drugs for treating Alzheimer's disease.

The invention belongs to the technical field of fungal extraction compounds, and in particular relates to a pyridine-containing novel skeleton heteroterpenoid compound and its preparation method and application. The compound has significant anti-acetylcholinesterase activity through experimental verification, and has good development prospects in the preparation of drugs for the prevention and / or treatment of diseases mediated by acetylcholinesterase; and it is reproduced by using modern microbial fermentation engineering technology, without Raw materials are worry-free, and at the same time, they have the advantages of not destroying the ecological balance and easy industrialization. They are renewable drug resources with development prospects, and provide abundant raw materials for the research and development of marine microbial products and marine microbial drugs.

The present invention provides anti-acetylcholinesterase active composition and its screening method and application in Gongluomu. Object, based on the principle of affinity chromatography, combined with immobilized enzyme technology, prepared an acetylcholinesterase reactor, constructed an active compound fishing platform, successfully screened and verified 4 kinds of anti-acetylcholinesterase active ingredients, and the anti-acetylcholinesterase of Gongluomu extract The discovery of active substances provides an efficient screening method. When the compound Tetrandrine and Jatrorrhizine are fixed, other compounds are added to mix with it. When the concentration of Tetrandrine or Jatrorrhizine is lower than the IC 60 or IC 70 When there is an obvious synergistic or additive effect, this study first discovered and verified the anti-AChE activity of the compound components in the Gonggongo wood extract, and the obtained combination has a synergistic or additive effect, which can undoubtedly be developed into a potential anti-AChE. Inhibitor.

The invention relates to a glucosamine-containing 1,3,4-thiadiazole derivative and a synthesis method of the lucosamine-containing 1,3,4-thiadiazole derivative. The method comprises the following steps: reacting 2-desoxy-2-isorhodanate-1,3,4,6-tetra-O-benzyl-beta-D-glucopyranose with hydrazine hydrate to synthesize an intermediate glycosyl thiosemicarbazide, and reacting with substituted aldehyde and a Fe<3+> compound to synthesize the N-(5-substituted-1,3,4-thiadiazolyl-2-yl)-1,3,4,6-tetra-O-benzyl-2-desoxy-beta-D-glucosamine. The synthesis method is simple and safe to operate, and has the advantages of small environmental pollution, high yield and simple after-treatment. The synthesized compound has a strong inhibiting effect on acetylcholinesterase, and has wide application prospects in the aspect of preparation of anti-acetylcholinesterase drugs.

The invention relates to a 1,2,4-triazole-3-thioketone derivative containing glucosamine molecules. The invention further relates to a synthesizing method of the 1,2,4-triazole-3-thioketone derivative containing the glucosamine molecules. The method particularly comprises the following steps that 2-deoxy-2-isothiocyanate-1,3,4,6-tetra-O-benzyl-beta-D-glucopyranose reacts with various substituted hydrazide, and by means of the action of a sodium hydroxide aqueous solution, 4-(2-deoxy-1,3,4,6-tetra-O-benzyl-beta-D-pyranose)-5-substituted-1,2,4-triazole-3-thioketone is generated through reacting. The synthesizing method has the advantages of being easy and safe to operate, small in environmental pollution, high in yield, simple in aftertreatment and the like. The synthesized compound has a high inhibiting effect on acetylcholinesterase and has a wide application prospect in preparing drugs for resisting acetylcholinesterase.