59 results about "Butyrylcholine esterase" patented technology

The invention relates to a preparation method and application of 9-bit substituent double-functional group berberine derivatives. In-vitro biological activity assay research shows that the 9-bit substituent double-functional group berberine derivatives provided by the invention has acetylcholinesterase inhibition activity higher than that of berberine serving as a leading compound, and also has higher inhibition activity on butyrylcholine esterase. After being further optimized and screened, the derivatives have favorable foreground of being developed into medicaments for treating diseases such as AD disease, vascular dementia, cognitive dysfunction and the like. The general formula of the derivatives is shown as the following formula, wherein X, Y and Z are defined in specifications.

The invention belongs to the field of medicines and chemical industries, and discloses a method for preparing a series of tacrine heterocomplexes and use in medicines for curing neurodegenerative diseases. The invention further relates to use of the tacrine heterocomplex for preparing medicines for curing the neurodegenerative diseases independently or with other medicines. The structural formula of the tacrine heterocomplex is as follows: FORMULA, wherein when X is O or CH2 and Y is N, R1, R2 and R3 are H; n is 2, 3, 4, 5, 6, 8, 9, 10, 11 or 12; when X is O or CH2 and Y is C, R1 is H, OH or OCH3; R2 is H, OH or OCH3; R3 is H, OH or OCH3; R4 is H, OH or OCH3; and n is2, 3, 4, 5, 6, 8, 9, 10, 11 or 12. The tacrine heterocomplex disclosed by the invention has strong inhibitory activity to acetylcholinesterase (AChE) and butyrylcholine esterase (BuChE), which are effectively used for curing the neurodegenerative diseases, such as Alzheimer's diseases.

It is intended to provide a preventive / remedy for urinary disturbance containing a compound, which shows an acetylcholine esterase inhibitory activity but substantially has no butyrylcholine esterase inhibitory activity, showing no side effect and being safe and efficacious without inhibiting the urine collection function; a preventive / remedy for dry mouth induced by the administration of a remedy for urinary disturbance and a preventive or remedy for hyperactive bladder not accompanied by dry mouth; and a method of screening a substance preventing / treating urinary disturbance without inhibiting the urine collection function characterized by comprising measuring and comparing the acetylcholine esterase inhibitory activity and the butyrylcholine esterase inhibitory activity of a test compound.

The invention relates to a tacrine-coumarin derivative containing triazole and an application of the derivative and belongs to the technical field of biological medicine. The derivative comprises compounds represented as a formula I and pharmaceutically acceptable salt, and three preparation methods of the derivative are provided; a pharmacological experiment proves that the derivative is acetylcholinesterase inhibitor and can inhibit activity of acetylcholin esterase, butyrylcholine esterase and MAO (monoamine oxidase), and meanwhile, the derivative can inhibit autopolymerization of beta-amyloid protein, delay hydrolysis of acetyl choline and autopolymerization of beta-amyloid protein, improve the function of acetyl choline on synapsis and be used for treating Alzheimer's disease effectively.

The invention discloses a 3-aminoalkaneacylamino-rutaecarpine and 3- aminoalkaneacylamino-7,8-dehydrorutaecarpine derivative and a synthetic method and an appliance thereof. As shown in experiments, the 3-aminoalkaneacylamino-rutaecarpine and 3-aminoalkaneacylamino-7,8-dehydrorutaecarpine derivative of the invention has strong inhibition perforance on acetylcholine esterase and good inhibition selectivity and the inhibition ability to acetylcholine esterase is 500 times higher than that to butyrylcholine esterase. The compound is shown to have an application prospect of being the medicines for curing Alzheimer's disease, cerebral vascular dementia, etc.

The invention discloses a butyrylcholine esterase selective inhibitor and a preparation method and application thereof. The invention discloses a compound shown in a formula (I), and also discloses application of the compound in preparation of medicines for preventing or treating Alzheimer's disease. An inventor uses the inhibiting activity of butyrylcholine esterase, selective screening and Morris water maze experiment as carriers to evaluate the function of the compound in the formula (I) for treating the Alzheimer's disease (especially medium and severe Alzheimer's disease), the good in-vitro and in-vivo activities and higher selectivity are found, and the compound can be further developed into a precursor substance which can selectively inhibit the butyrylcholine esterase to reach thefunction of treating the Alzheimer's disease. The formula (I) is shown in the specification.

The invention provides a method for producing recombinant human butyrylcholine esterase on large scale by utilizing a biological platform of the mammary gland of a transgenic animal. The method comprises the following steps: utilizing the biological platform of the mammary gland of the transgenic animal to efficiently produce holonomic and monomeric recombinant human butyrylcholine esterase on large scale for the first time, namely cut-off type enzyme without containing the last 40 amino acid residues of the holonomic butyrylcholine esterase, and a protein fused with monomeric butyrylcholine esterase and albumin. The produced recombinant protein can be used for preventing and treating apnea caused by poisoning of nerve gas, poisoning of organophosphorus pesticide, poisoning of cocaine and succinylcholine, and is used for detecting and removing residues of organophosphorus pesticide on vegetables, melons, fruits, other crops, surfaces of various articles and soil.

The present invention provides recombinant butyrylcholinesterase fusion proteins, including Fc fusion proteins and multi-armed high MW polymers containing hydrophilic groups conjugated to the fusion proteins, and methods of preparing such polymers.

The invention discloses a butyrylcholine esterase, a preparation method thereof and a kit for quickly detecting pesticide residue and prepared by butyrylcholine esterase. The preparation method comprises the following steps: performing purification to bovine serum, homogenating, extracting via the buffer solution, and centrifuging to remove sediment so as to obtain crude enzyme; precipitating the crude enzyme via ammonium sulfate, centrifuging, removing the liquid supernatant, redissolving and dialyzing the sediment, performing chromatography via the DEAE column, collecting eluant, dialyzing, obtaining the enzyme after purification, and then freezing and drying; the kit comprises butyrylcholine esterase, substrate, developer and phosphoric acid buffer solution; the concentration of the phosphate buffer is 0.9-0.11 mol / L, and the pH value of the phosphate buffer is 7.5-8.5. The kit of the invention adopts the matching of semi-purified butyrylcholine esterase to be matched with the stabilizing agent, so that the stability of butyrylcholine esterase is remarkably enhanced; the butyrylcholine esterase is obtained through the purification of the bovine serum, the sensitivity is strong, and the sensitivity of the kit prepared by the butyrylcholine esterase is strong.

The invention relates to a 4-cyclamine alkoxy-3-methoxyl cinnamic acid benzamide compound, a preparation method and application of the compound.The chemical structure general formula of the compound is shown as a formula (I) (please see the formula in the description), wherein m represents 1-12, R1 represents C1-C12 alkyl or benzyl or substituted benzyl, X represents C1-C12 alkyl or benzyl or substituted benzyl, phenyl of which a benzene ring is substituted with 1-4 groups selected from F, Cl, Br, I, C(1-4) alkyl, C(1-4) alkoxy, trifluoromethyl, trifluoromethoxy, nitryl, a cyano group, and the substituent groups can be located at any position of the benzene ring.Accordingly, the compound has the significant inhibiting effect on acetylcholinesterase, the IC50 of the compound is 0.01-5 micromoles per liter, the inhibiting activity on acetylcholinesterase is greatly higher than the inhibiting activity on butyrylcholine esterase, and therefore the compound has the certain selective inhibiting effect on acetylcholinesterase.

The invention discloses a diaryl-containing imidazole compound. The invention further discloses application of the diaryl-containing imidazole compound to preparation of drugs for preventing or treating Alzheimer's disease. The inventor screens butyrylcholine esterase and IDO1 as carriers for inhibiting the activity to evaluate the effect of the diaryl imidazole compound to treat Alzheimer's disease, and finds that the diaryl imidazole compound has good in vitro activity, and can be further developed as a precursor substance for performing the Alzheimer's disease resistant effect by inhibitingthe activity of cholinesterase. (The formula is shown in the description).

The present invention relates to synthesis of a series of rivastigmine derivatives, wherein the structural formula is represented by a formula (I). According to the present invention, with the substituent changing, the inhibition of acetylcholine / butyrylcholine esterase by adjusting the rivastigmine derivatives, the inhibition of glutamic acid-induced oxidative stress, the reduction of damage of H2O2 and other ROS on HT22 cells, the inhibition of beta-amyloid protein self-aggregation, and the clearing of DPPH free radicals, the rivastigmine derivatives can simultaneously act on multiple targets. The rivastigmine derivatives can be made into the suitable pharmaceutical dosage form for Alzheimer's disease treatment.

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 relates to an ethyl acetate extract product of Chinese fevervine herb and root and an application thereof. The ethyl acetate extract product of Chinese fevervine herb and root can substantially inhibit activity of butyrylcholine esterase in AD model. Therefore, the ethyl acetate extract product of Chinese fevervine herb and root can be used to prepare drugs for preventing and treating senile dementia.

The invention discloses an application of a tetrahydro-beta-carboline dimer derivative in the preparation of a medicine for preventing or treating Alzheimer's disease. The tetrahydro-beta-carboline dimer derivative is as shown in a structural formula I, which is described in the specification, L-tryptophan and tryptamine are used as raw materials; a tetrahydro-beta-carboline monomer is generated through a Picet-Spengler reaction and aldehyde cyclization, then a tetrahydro-beta-carboline dimer is generated through acyl chloride connection and a click chemical reaction, the synthesis steps are simple, the raw materials are easy to obtain, the yield is high, and the tetrahydro-beta-carboline dimer has remarkable inhibitory activity on butyrylcholine esterase and A[beta]1-42 aggregation. According to the neural protective effect under three AD models on cells, after the cells are independently treated by A[beta]1-42, H2O2 and OA, the survival rate of the cells is low, and apoptosis or necrosis of the cells occurs. The compounds 11, 12, 13, 17 and 19 are used for co-treatment, the compounds 11, 12, 13, 17 and 19 successfully block A[beta]1-42, H2O2 and OA induced cell death, and it is proved that the compounds 11, 12, 13, 17 and 19 have a remarkable neural protective effect.

The invention belongs to the technical field of medicine, and relates to a (N-1,2,3,4-tetrahydroisoquinolinyl)-feruloylagmatine compound, and a preparation method and application thereof. The structure is as shown in a formula I (the formula I is as shown in the description). The (N-1,2,3,4-tetrahydroisoquinolinyl)-feruloylagmatine compound provided by the invention has excellent butyrylcholine esterase inhibiting activity, remarkable Abeta1-42 aggregation inhibiting activity, anti-oxidation activity and high neuroprotective activity on PC12 cell injury induced by hydrogen peroxide in in-vitro experiments; and the (N-1,2,3,4-tetrahydroisoquinolinyl)-feruloylagmatine (I) compound is a multi-target-point inhibitor, further shows a good effect of treating alzheimer disease in in-vivo experiments, and has low toxicity and a good clinical application prospect.

The invention relates to a 4-amine alkoxy-3-methoxyl cinnamic acid ester compound, a preparation method and application of the compound.The preparation method of the compound comprises the following steps that 1, a ferulic acid acyl chloride compound is obtained by taking ferulic acid as a staring material under the condition of in first solvent under the condition of an acylating agent; 2, the ferulic acid acyl chloride compound reacts with alcohol or phenol in second solvent under a first alkaline condition to obtain a corresponding cinnamic acid ester compound; 3, the cinnamic acid ester compound reacts with a dihalogen alkyl compound in third solvent under a second alkaline condition to generate a corresponding halogen compound; 4, the halogen compound reacts with an organic amine compound in fourth solvent to obtain the 4-amine alkoxy-3-methoxyl cinnamic acid ester compound.Accordingly, the compound has the significant inhibiting effect on acetylcholinesterase, the inhibiting activity on acetylcholinesterase is greatly higher than the inhibiting activity on butyrylcholine esterase, and the certain selective inhibiting effect on acetylcholinesterase is achieved.

The invention discloses a selective butyrylcholine esterase inhibitor with a structure represented by a general formula (I), a preparation method and applications thereof. According to the invention,by evaluating the effect of the selective butyrylcholine esterase inhibitor to a butyrylcholine esterase target through the cholinesterase inhibition activity and the selectivity, the results show that the selective butyrylcholine esterase inhibitor has good in-vitro activity and extremely high selectivity, and is further developed to be used in preparation of drugs for preventing or treating Alzheimer's disease.

The invention discloses an application of mulberone H in preparation of an anti-Alzheimer's disease medicine. Through experimental screening, the applicant finds that mulberrin H has a good inhibition effect on butyrylcholine esterase, the inhibition effect is enhanced along with the increase of the drug concentration, and compared with a positive drug, the inhibition rate of butyrylcholine esterase is obviously higher, so that mulberrin H has the prospect of being developed into an anti-Alzheimer's disease drug.

The invention discloses a compound with a benzimidazole structure and a preparation method and application thereof. The invention discloses a compound shown in a formula (I), and further discloses application of the compound in preparation of a medicine for preventing or treating Alzheimer's disease. The inventor uses butyrylcholine esterase inhibitory activity, selective screening and Morris water maze experiments as carriers to evaluate the compound shown in the formula (I) for treating the Alzheimer's disease (especially moderate and severe Alzheimer's disease), and finds that the compound has good in-vitro and in-vivo activity and extremely high selectivity, and can be used for preparing the compound for treating the Alzheimer's disease. The compound can be used as a precursor substance for further developing the effect of treating the Alzheimer's disease by selectively inhibiting butyrylcholine esterase.

The invention relates to the technical field of marine organisms and medicines, in particular to a preparation method and application of an anti-senile dementia compound separated from marine sponge Aaptos suberitodes. The anti-senile dementia compound disclosed by the invention is an aaptamine compound separated from sponge Aaptos suberitodes, the preparation method of the compound is simple andeasy to implement, and artificial synthesis of the compound is also easy to realize. Meanwhile, the invention discloses that the compound has better activity of inhibiting acetylcholin esterase and butyrylcholin esterase for the first time, wherein the IC50 values of the compound are 6.071 [mu]g / mL and 1.492 [mu]g / mL respectively; the invention provides application of the compound having undergonestructural modification and optimization to a lead compound used for preparing acetylcholin esterase inhibiting medicines and butyrylcholin esterase inhibiting medicines for the first time; and a scientific basis is provided for development and utilization of marine biological resources in China and research and development of new anti-senile dementia compounds.

The presently-disclosed subject matter includes isolated polypeptides that comprise a butyrylcholinestrase (BChE) polypeptide and a second polypeptide. The BChE polypeptide as well as the second polypeptide can be variants and / or fragments thereof. The presently-disclosed subject matter also includes a pharmaceutical composition that comprises the present isolated polypeptide and a suitable pharmaceutical carrier. Further still, methods are provided for treating cocaine-induced conditions, and comprise administering the isolated polypeptide and / or pharmaceutical compositions thereof to an individual.

The invention belongs to the technical field of biochemical analysis and biosensors, and relates to a 3D folding ratio fluorescent microfluidic device and method for simultaneously detecting alkaline phosphatase and butyrylcholine esterase. The device includes four layers of rectangular channels, which are arranged on filter paper, and every two layers of channels can be folded; the first layer of rectangular channel comprises a central sample area and an I-shaped path, the central sample area is located in the middle of the I-shaped path, and the two ends of the I-shaped path are circular areas; the second layer of rectangular channel adjacent to the first layer of rectangular channel comprises the I-shaped path; circular areas are arranged at the two ends of the third-layer rectangular channel and the fourth-layer rectangular channel respectively, wherein the circular areas correspond to the circular areas in the first-layer rectangular channel and the second-layer rectangular channel. The three-dimensional folding [mu]PAD has the characteristics of low cost, simplicity in operation, high efficiency, good precision, high sensitivity, good selectivity and the like, and therefore, an innovative method may be provided for the POCT field.

The invention discloses a pesticide residue detection method for food detection. The method comprises the following steps: (1) preparing a reagent; (2) preparing a sample; (3) detecting a reference solution: adding a buffer solution and a butyrylcholine esterase solution into a reaction bottle through extraction equipment, then adding a color developing agent, adding a substrate, transferring thesolution into a cuvette, taking a supernatant prepared in the step (2), the butyrylcholine esterasesolution and the color developing agent, and transferring the solution into the cuvette through the extraction equipment; and (4) detecting a to-be-detected sample solution. Through the up-and-down displacement action of an extraction part, a first needle tube or a second needle tube can be fixed andseparated by the extraction part, different solutions can be sequentially subjected to pipetting, pipetting of different volumes can also be carried out, and in a sealed environment, a pollution problem is avoided; and therefore, in the detection of the reference solution in the step (3), the extraction equipment can flexibly and quickly operate the solution without errors.

The invention discloses a butyrylcholine esterase selective inhibitor as well as a preparation method and application thereof. The inhibitor is a compound shown as a formula (I). The invention also discloses application of the compound in preparation of drugs for preventing or treating Alzheimer's disease. Experiments such as butyrylcholine esterase inhibitory activity, selective screening, Nrf2 activation activity, Morris water maze and the like are used as carriers to evaluate the treatment of Alzheimer's disease (especially moderate and severe Alzheimer's disease) by the compound shown in the formula (I), and the compound is found to have good in-vitro and in-vivo activity and extremely high selectivity. The compound can be used as a precursor substance for further development of Alzheimer's disease by selectively inhibiting butyrylcholine esterase.

The invention discloses a tacrine-sinapic acid heterozygote, a medicinal composition containing the tacrine-sinapic acid heterozygote, and a preparation method and application thereof. The tacrine-sinapic acid heterozygote has the following structure: the formula is as shown in the description. Experiments prove that the tacrine-sinapic acid heterozygote has high inhibitory activity on acetylcholin esterase (AChE) and butyrylcholine esterase (BuChE), has acetylcholin esterase inhibition capability which is 15 times that of tacrine, has strong inhibition effect on amyloid protein (Abeta) self-aggregation, has remarkable anti-oxidation activity, does not have remarkable in-vitro neurocytotoxicity and in-vivo acute hepatotoxicity, shows remarkable in-vitro nerve cell protective activity, andcan be applied to treatment on Alzheimer's disease.

The invention belongs to the technical field of medicine, and particularly relates to application of an (N-isopropylpiperazine)-2-hydroxybenzamide compound to preparation of drugs for treating neurodegenerative disease, especially the application of preparation of drugs for treating Alzheimer's disease. The chemical structural formula of a salicylate compound is shown as the formula I. The (N-isopropylpiperazine)-2-hydroxybenzamide compound provided by the invention has butyrylcholine esterase inhibiting activity, antioxidant activity and metal ion coordination activity, has an obvious neuroprotection effect on hydrogen peroxide induced PC12 cellular damage, further shows a better effect in treating Alzheimer's disease in experiments in vivo, is relatively low in toxicity and has good clinical prospect.

The invention relates to tacrine derivatives containing aldoxime selective butyrylcholinesterase inhibitors, a preparation method and application thereof. The compound has the structure shown in formula I or II. The present invention also relates to pharmaceutical compositions containing compounds of formula I and formula II. The present invention also provides the application of the above compounds and compositions containing one or more of these compounds in the preparation of anti-Alzheimer's disease drugs.

The present invention relates to synthesis of a series of rivastigmine derivatives, wherein the structural formula is represented by a formula (I). According to the present invention, with the substituent changing, the inhibition of acetylcholine / butyrylcholine esterase by adjusting the rivastigmine derivatives, the inhibition of glutamic acid-induced oxidative stress, the reduction of damage of H2O2 and other ROS on HT22 cells, the inhibition of beta-amyloid protein self-aggregation, and the clearing of DPPH free radicals, the rivastigmine derivatives can simultaneously act on multiple targets. The rivastigmine derivatives can be made into the suitable pharmaceutical dosage form for Alzheimer's disease treatment.

The invention relates to an ethyl acetate extract product of Chinese fevervine herb and root and an application thereof. The ethyl acetate extract product of Chinese fevervine herb and root can substantially inhibit activity of butyrylcholine esterase in AD model. Therefore, the ethyl acetate extract product of Chinese fevervine herb and root can be used to prepare drugs for preventing and treating senile dementia.