385 results about "Alpha-glucosidase" patented technology

The present invention relates to a pentacyclic triterpanoid derivative of multiple-oxide substitution of the A ring and the C ring and the medicine salt or solvate of the derivative, and the present invention also relates to the preparation method, the drug combination, and medical use of the derivative. The compound of the present invention has the functions of inhibiting the activity of six human tumor cell strains in vitro, such as human prostate cancer cell (PC-3), nasopharyngeal carcinoma cells (CNE), oral squamous carcinoma cell(KB), human lung cancer cell (A549), human hepatoma cell (BEL-7404), and human cervix cancer cell (Hela), and the function of the invention is at the same magnitude of the positive control of cisplatin, thereby the compound can be used as expected antitumor drug. The compound of the present invention also inhibits the alpha glucosidase strongly, and the inhibiting effect is greater than the positive control of acarbose, thereby the compound can be used as expected medicine for preventing and treating diabetes and the treatment of the virus diseases.

A medicine with high activity to suppress alpha-glucosidase for treating diabetes, and hyperlipemia, and delaying sanility contains the common alkaloid extracted from mulberry plants and the flavone extract.

The invention provides the application of betulinic acid and salts thereof suitable for medical purpose in the preparation of a drug of a glycosidase inhibitor. The compound of the invention is the compound of lupeol type pentacyclic triterpene acid obtained by separating lagerstroemia plants. Pharmacological tests prove that the compound has obvious effect in inhibiting Alpha-glucosidase, the inhibitory activity of which exceeds acarbose 100% for initial therapy. Therefore, drug compositions made from the compound or the salts thereof suitable for medical purpose and drug excipients or carriers allowable for preparation can be applied to the preparation of drugs for preventing or treating Type II Diabetes, namely, noninsulin-dependent diabetes mellitus. The constitutional formula shown in formula (1) of the invention is shown as above.

The invention relates to separation, selection and identification of lactobacilli having a function of inhibiting activity of alpha-glucosidase, in particular to a lactobacillus plantarum and an application thereof. Lactobacilli are separated out from intestinal canals of longevous people in Bama of Guangxi; on the basis of comprehensive comparison of acid resistance, cholate resistance, in-vitro antioxidant ability and sensitivity to antibiotics, a strain having a best inhibition function to activity of alpha-glucosidase is selected out by means of in-vitro tests; the strain is identified as Lactobacillus plantarum Grx16 by means of physiological and biochemical tests, API reagent strips and 16s rDNA sequencing analysis. The lactobacillus plantarum Grx16 can be used for preparation of fermented milk having the function of inhibiting activity of alpha-glucosidase.

The invention discloses lactobacillus plantarum with the inhibitory activity to alpha-glucosidase. The lactobacillus plantarum is classified and named as Lactobacillus plantarum, is preserved on August 29, 2017 in China General Microbiological Culture Collection Center and has a preservation number of CGMCC NO.14573. By screening, the lactobacillus plantarum has in-vitro inhibitory activity to alpha-glucosidase; the survival rate of the lactobacillus plantarum reaches up to 71.04% under an acid condition that the pH value is 2.0 and is 77.14% in 2.0% cholate deionized water, the tolerances of the lactobacillus plantarum to artificially simulated saliva and intestinal fluid are higher than 90%, the tolerance of the lactobacillus plantarum to gastric fluid reaches 52.49%, and after artificially simulated fluid is sequentially digested, the survival rate reaches 88.27%; the lactobacillus plantarum has good effects on the prevention and treatment of diabetes mellitus type 2; the lactobacillus plantarum is added with a protection agent so as to prepare freeze-drying battier powder with a high viable count, and the viable count reaches up to 87% of the viable count before freeze-drying; and besides, the lactobacillus plantarum further has a good fermentation effect.

The invention discloses a rosa roxburghii polysaccharide, as well as a preparation method and application thereof. The preparation method mainly comprises raw material pretreatment, extraction, deproteinization, de-coloration, alcohol precipitation, as well as separation and purification, wherein the extraction is to mix pretreated rosa roxburghii dry powder and water in a mass volume ratio of (1to 15) to (1 to 35), and perform extraction at a temperature of 55 to 95 DEG C; perform centrifugal separation to obtain a rosa roxburghii polysaccharide extracting solution, and concentrate the rosaroxburghii polysaccharide extracting solution under reduced pressure to 1 / 3 to 1 / 6 of the original volume to obtain a concentrated solution of the rosa roxburghii polysaccharide. The rosa roxburghii polysaccharide prepared by the invention has the advantages of high purity and uniform molecular weight. Compared with the existing rosa roxburghii polysaccharide, as proved by in-vitro fermentation experiments, the rosa roxburghii polysaccharide disclosed by the invention can promote the generation of short-chain fatty acids such as acetic acid, propionic acid and butyric acid, promote the growthof beneficial bacteria such as lactic acid bacteria and bifidobacterium, and can be taken as prebiotics. Meanwhile, the rosa roxburghii polysaccharide can inhibit the activity of alpha-glucosidase, and can be applied to healthy foods or medicines having auxiliary therapy effects on intestinal diseases and diabetes mellitus.

The invention discloses a separation and purification method of main catechin components in tea polyphenol and glycosidase activity thereof. In the separation and purification method, tea polyphenol extracts are absorbed by macroporous adsorption resin of nonpolar or weak polar polystyrene; water and ethanol are used for the elution; alcohol eluates, through polyamide columns for the chromatography and are eluted respectively by water and ethanol. The water recrystallization is carried out on the alcohol eluates of the polyamide columns to obtain EGCG pure products with the purity larger than 95 percent and the yield larger than 50 percent; reversed-phase C18 filled columns are used for the chromatography of water eluates of the polyamide columns to obtain EC and EGC; the ethanol of 50-80 percent is used for the recrystallization to obtain pure products of the EC and EGC with the purity all larger than 96 percent. Tests in vitro show that EGCG, EGC and EC all have inhibitory activity on alpha-glucosidase and alpha-amylase and can be used for preparing weight reduction products reducing the absorption of carbohydrates or drugs or health products lowering the postprandial blood glucose.

The invention relates to a process of producing a fermentation product, such as ethanol, from starch-containing material, including i) subjecting starch-containing material to an alpha-amylase, ii) subjecting the material obtained in step i) to an alpha-glucosidase and / or a maltose-generating enzyme, and iii) fermenting the material in the presence of a fermenting organism, such as yeast. Alternatively the invention relates to a process of producing a fermentation product from starch-containing material, preferably granular starch, which process comprises: a) subjecting starch-containing material to an alpha-glucosidase and optionally a glucose-generating and / or maltose-generating enzyme, and b) fermenting the material in the presence of a fermenting organism.

The invention discloses clone and expression of an Alpha-glucosidase (abbreviated as AGLU enzyme) gene and belongs to the fields of enzyme gene engineering and enzyme engineering. The invention obtains the aglu gene with SEQ ID NO of 1 through an Aspergillus niger (A.niger) WX-07 total DNA, and aglu cDNA uses an expression vector of plasmid pPIC9K and an expression parasitifer of pichia stipitis (P.pastoris), thus realizing extracellular dissolubility expression of the aglu gene; and the aglu cDNA totally has 2880 nucleic acid and encoding of 960 amino acid, constructs eukaryotic expression plasmid and transforms Pichia pastoris KM71 for AGLU enzyme expression. The recombinant enzyme has transnucleosidation activity, can generate isomalto oligosaccharide through maltose transnucleosidation, is applicable to the requirements of industrial application including food, feeding stuffs and medicaments and the like, and can be applied into the industrial production of isomalto oligosaccharide.

The present application provides for compositions comprising high concentrations of acid α-glucosidase in combination with an active site-specific chaperone for the acid α-glucosidase, and methods for treating Pompe disease in a subject in need thereof, that includes a method of administering to the subject such compositions. The present application also provides methods for increasing the in vitro and in vivo stability of an acid α-glucosidase enzyme formulation.

The invention discloses a detecting method (ELISA) of enzyme link immune suction of banqi-enterobacteria and antibody and alpha-glucosidase and coded nucleic acid and carrier of the antibody, which is characterized by the following: using the amino acid sequence of alpha-glucosidase as Seq ID No:2; using ELISA of antibody to make agent box of the antibody; detecting the banqi-enterobacteria rapidly and effectively; providing high sensitivity, strong specificity and reliable result.

The invention discloses sargassum pallidum polysaccharide selenium as well as a preparation method and an application thereof. The preparation method mainly comprises steps as follows: raw material pretreatment, hot water extraction, decoloration, deproteinization, freeze drying and selenylation reaction, wherein the selenylation reaction is implemented as follows: sargassum pallidum polysaccharide and dilute nitric acid are mixed and stirred at the room temperature, sodium selenite and barium chloride are added respectively, the mixture is heated to 60-80 DEG C, stirred and mixed uniformly toreact at the microwave power of 100-500 W for 3-5 min, a sargassum pallidum polysaccharide selenium solution is obtained, cooled to the room temperature, placed in a dialysis bag for dialysis and freeze-dried, and sargassum pallidum polysaccharide selenium is obtained. The preparation method is simple, the reaction condition is mild, the sargassum pallidum polysaccharide selenium is pollution-free and high in selenylation degree, has remarkable alpha-glucosidase inhibition activity, has the activity superior to that of acarbose and can remarkably improve the antioxidase activity of cells andreduce the content of malondialdehyde, a dietary supplement with antioxidant and blood sugar reducing efficacy can be developed, and the sargassum pallidum polysaccharide selenium can be applied to the field of food or medicines.

Asiatic acid and madecassic acid are extracted and prepared from Centella asiatica (L.) Urban, and pharmacological experiments prove that the asiatic acid and the madecassic acid have the activity of inhibiting alpha-glucosidase. The invention discloses a new use of the asiatic acid and the madecassic acid in the preparation of alpha-glucosidase inhibitor drugs, and the asiatic acid, the madecassic acid or a composition containing the asiatic acid and the madecassic acid can be used for preparing the alpha-glucosidase inhibitor drugs. The invention simultaneously discloses a new preparation method of the asiatic acid and the madecassic acid.

The invention discloses a method for comprehensive development and utilization of fruits and vegetables. The method uses fruits and vegetables as raw materials and comprises separating fruit and vegetable juices from fruit and vegetable residues by juicing, carrying out fermentation on the fruit and vegetable juices through a compound liquid of three edible and medical fungi such as needle mushroom, black fungus and grifola frondosa to obtain an antioxidant activity fermented fruit and vegetable juice, wherein in the DPPH free radical scavenging system, IC50 is 40 to 100 microliters per milliliter, and carrying out fermentation on the fruit and vegetable residues through lactic acid bacterium compound solids such as lactobacillus plantarum, lactobacillus acidophilus and lactobacillus rhamnosus to obtain fruit and vegetable ferment having a blood sugar reduction function. An in-vitro blood sugar reduction experiment result shows that the fruit and vegetable ferment has an alpha-glucosidase inhibition rate of 40-55%. The method provides a novel approach for comprehensive development and utilization of fruits and vegetables, can produce the fruit and vegetable juice having antioxidant activity and can produce the fruit and vegetable ferment having a blood sugar reduction function.

The invention discloses a preparation method of extract of effective part of Clinopodium chinense (Benth.) O. Kuntze for preventing and treating diabetes and an application thereof. The extract of the effective part is prepared from Clinopodium chinense (Benth.) O. Kuntze as a raw material, a concentrate is obtained by pulverizing, ethanol extraction and reduced pressure recovery, the concentrate is extracted by petroleum ether and ethyl acetate, and the obtained ethyl acetate extract is purified by macroporous resin. The extract of the effective part mainly comprises total flavone and terpenoids, and has obvious effects of reducing blood sugar of rats with streptozotocin diabetes, reducing the content of serum cholesterol, protecting the islet cells, inhibiting the activity of alpha-glucosidase, and protecting the vascular endothelial cells. Thus, the extract of the effective part of Clinopodium chinense (Benth.) O. Kuntze has favorable functions for reducing blood sugar, reducing blood fat, and protecting the islet cells and the vascular endothelial cells, and can be used for preventing and treating diabetes, dyslipidemia induced by diabetes and diabetic cardiovascular and cerebrovascular complications.

The invention discloses a mulberry active phenolic compound and a pollution-free extraction and purification method thereof. The method comprises the steps that microwave and vapor high temperature instantaneous enzyme deactivation is carried out on fresh mulberries in sequence, then mechanical crushing, centrifugal layering, food grade acidified alcohol extraction, vacuum concentration and ultrafiltration membrane purification are carried out, and therefore a mulberry phenolic compound extracting solution with the biological activity is obtained. An organic reagent with the low concentration is adopted, mulberry crushing and phenolic compound extraction and purification are achieved under the mild condition, and the natural character and biological activity of the mulberry phenolic compound can be maintained. Compared with a conventional extraction method, the mulberry extracting solution has the higher-concentration total phenol and total anthocyanins, the extraction solution has the good color and luster and high oxidation resistance, alpha-glucosidase enzymatic inhibitory activity and food safety, and the mulberry active phenolic compound can be used as a safety raw material of antioxidant and hypoglycemic drug and health care product development. The conditions are mild, operation is convenient, and industrial production of high-activity natural products is facilitated.

The invention discloses sanggenone C and sanggenone D extracted from white mulberry root-barks, mulberry twigs and folium leaves and a new medicine application of a composition comprising the sanggenone C and the sanggenone D which are main ingredients, particularly the application of the single ingredient sanggenone C or sanggenone D and the composition composed of the sanggenone C, the sanggenone D, mulberrin, mulberroside, oxidized resveratrol, resveratrol and deoxynojirimycin in preparation of alpha-glucosidase inhibitor medicines. The composition is prepared by respectively extracting medicinal materials containing the chemical components above and blending according to certain proportions, or using several extraction methods for extracting the medicinal materials simultaneously containing the chemical components above. The white mulberry root-barks, the mulberry twigs and the folium leaves are accidentally found to contain the sanggenone C and the sanggenone D apart from containing alkaloids such as deoxynojirimycin; and the sanggenone C and the sanggenone D have stronger pharmacological activity than the alkaloids such as deoxynojirimycin.

The invention discloses a mulberry active polysaccharide and an extracting method thereof. The extracting method comprises: drying mulberries and then carrying out ultrafine grinding-screening and ethanol degreasing pre-treatment; then, carrying out freeze-thawing and wall breaking treatment, hot water extraction, vacuum concentration and protein removal, ethanol precipitation, and freeze-drying, thereby obtaining the mulberry polysaccharide with biological activity, wherein the mulberry polysaccharide with molecular weight ranging from 0.08 million to 0.1 million accounts for 60%-70%, and the mulberry polysaccharide with molecular weight lower than 2000 accounts for 30%-40%. According to the extracting method, freeze-thawing and wall-breaking treatment is carried out on mulberries, so that dissolution of the polysaccharide is facilitated; meanwhile, attention is paid to protection on the polysaccharide in the extraction process; influence on activity of the polysaccharide is reduced; efficient oxidization resistance and effect of inhibiting activities of alpha-amylase and alpha-glucosidase are kept; and the mulberry active polysaccharide can be applied to preparing anti-oxidant and blood-sugar-decreasing health products. The extracting method is simple in process, convenient to operate, high in safety, low in cost and beneficial for realizing industrial application.

The invention discloses a benzimidazole chiral heterocyclic compound as well as a preparation method and application thereof. The structure formula of the benzimidazole chiral heterocyclic compound isshown in formula I, formula II or formula III in the description. The benzimidazole chiral heterocyclic compound is prepared by treating an iridium complex which is prepared through a metal iridium compound and a phosphoramidite ligand as a catalyst, performing intra-molecular allyl amination on allyl substrate, and then synthesizing with high efficiency and high enantioselectivity. The method has the advantages of being high in catalytic reaction activity, mild in reaction conditions, high in enantioselectivity, wide in substrate applicable scope, and environmentally friendly; the primary in-vitro enzyme inhibition activity test shows that the compound is high in alpha-glucosidase inhibiting activity and can be used as an alpha-glucosidase inhibiting agent, and the compound can also be used as a further modified drug intermediate; the compound has a potential application value in preventing or treating II-diabetes, obesity and complication medicines thereof and pilot compounds thereof.

The invention provides a compound with an alpha-glucosaccharase inhibitory activity in a mulberry leaf. The preliminary screening from the mulberry leaf is carried out by immunomagnetic separation and liquid chromatography-mass spectrometry and a nuclear magnetic resonance method; and a separation or configuration target compound is prepared for verifying the alpha-glucosaccharase inhibitory activity, and thus the compound with the alpha-glucosaccharase inhibitory activity is obtained. Compared with a traditional method, no separation compound for preliminary screening is needed, so that the screening efficiency is remarkably increased, the screening time is shortened and the preparation and separation steps of the marked compound are reduced. In addition, the screening method disclosed by the invention has the characteristics of quickness, accuracy, favorable reproducibility and the like. The quick screening of the compound with the alpha-glucosaccharase inhibitory activity in a natural medicament or traditional Chinese mixture can be popularized. The compound with the alpha-glucosaccharase inhibitory activity, which is obtained by the method disclosed by the invention, can be applied to preparation of medicaments for resisting diabetes mellitus.

The invention relates to a pharmaceutical composition having alpha-glucosidase inhibition activity, wherein the pharmaceutical composition comprises a flavone compound and an alpha-glucosidase inhibitor, the flavone compound is at least one selected from a monomer such as baicalein, quercetin, luteolin, baicalein-7-O-glucoside and catechin, an organic salt of the monomer, and an inorganic salt of the monomer, and the alpha-glucosidase inhibitor is at least one selected from a monomer such as acarbose, voglibose and miglitol, an organic salt of the monomer, and an inorganic salt of the monomer. According to the present invention, the pharmaceutical composition can effectively reduce postprandial blood glucose, can inhibit the activity of alpha-glucosidase adopting starch, maltose and sucrose as substrates, and less uses the alpha-glucosidase inhibitor, such that the efficacy can be improved, the side effect of the alpha-glucosidase inhibitor can be effectively reduced, and hypoglycemia and other problems easily caused by drug combination are effectively solved.

The invention belongs to the biotechnical field, especially relates to a pentapeptide with an auxiliary hyperglycemic function, and concretely relates to a pentapeptide KLPGF capable of inhibiting the activity of alpha-glucosidase and inhibiting the activity of alpha-amylase. The amino acid sequence of the pentapeptide KLPGF is Lys-Leu-Pro-Gly-Phe. The pentapeptide can be used to develop auxiliary hpyerglycemic drugs and functional foods.

The invention provides a stable alpha-amylase detection kit. The stable alpha-amylase detection kit is composed of a reagent R1 and a reagent R2, wherein the reagent R1 is prepared from the following components: 0.5-100mM buffer solution, 20-200mM NaCl, 10-100mM CaCl2, 1-10g / L sodium dodecyl benzene sulfonate, 0.1-10KU / L alpha-glucosidase, 0.1-10g / L stabilizer and 0.1-10g / L preservative; the reagent R2 is prepared from the following components: 0.5-100mM buffer solution, 0.5-10g / L 4,6-ethylidene-nitrophenylcarbimide-alpha-D-maltoheptaoside, 1-10g / L sodium dodecyl benzene sulfonate, 0.1-10g / L stabilizer and 0.1-10g / L preservative. The sodium dodecyl benzene sulfonate is added, so that the performances of the kit are improved, the kit has the good repetitiveness, high sensitivity and wide linear range, and reagents are stable.

The invention discloses a use of lactobacillus plantarum ST-III in preparation of an alpha-glucosidase inhibitor or the preparation of a fermented bean product with alpha-glucosidase inhibition activity. The invention further discloses fermented soymilk or fermented beans with the alpha-glucosidase inhibition activity, which can be obtained by inoculating the lactobacillus plantarum ST-III into sterile soymilk or cooked soymilk and fermenting at the temperature of 25-40 DEG C. Water is added into the fermented beans for homogenizing, the pH value is regulated to 6.5-7.5, the boiling is performed for 10-60 minutes, cooling is performed, then solid-liquid separation is performed, and a liquid phase is taken so as to get a water-soluble extract of the fermented soymilk. The lactobacillus plantarum ST-III has high alpha-glucosidase inhibition activity and can be used in glucose-reducing foods, health care products or medicaments. As the oral glucose-reducing foods, the health care products or the medicaments, the high postprandial blood glucose of patients with diabetes can be reduced and the postprandial blood glucose fluctuation can be regulated.

The invention relates to the field of microorganisms, in particular to a bifidobacterium animal and an application thereof in controlling diabetes or hyperlipidemia, particularly in weight gain or obesity. The preservation number of the bifidobacterium animal is CGMCC No.17308. The invention also discloses a product composition. The product composition contains thallus substances and / or metabolites of the bifidobacterium animal. The bifidobacterium animal provided by the invention is suitable for specific physiological physique of Chinese people, and has relatively high advantages in activityinhibition of alpha-glucosidase, transport inhibition of glucose, improvement of glucose tolerance level of organisms, relief of insulin resistance and leptin resistance, improvement of the secretionlevel of glucagon-like peptide-1, increase of islet cell size and islet beta cell number, and the like, so that development of diabetes or hyperlipidemia can be better controlled, and particularly weight gain and obesity of organisms can be controlled.

The invention provides a bisindolyl maleimide derivative and a preparation method and application thereof. The bisindolyl maleimide derivative has an excellent alpha-glucosidase inhibition effect and can be used for preventing and treating diabetes.

The invention provides Rhizome Anemarrhenae use of medicine preparation for treating or preventing diabetes mellitus. Specifically, the Rhizome Anemarrhenae inhibits Alpha-glucosidase, reduces the blood sugar after dinner, promotes the glucose metabolism, balances the blood sugar, reduces the blood fat, advances the insulin secretion and keeps the blood sugar stability.

The invention discloses an aspergillus niger alpha-glucosidase aglu<OP> and a high-efficiency expression method of the aspergillus niger alpha-glucosidase aglu<OP> in pichia pastoris. The nucleotide sequence of the optimized alpha-glucosidase gene is shown in SEQ ID No.1. The gene is constructed into a pichia pastoris expression vector, and the pichia pastoris expression vector and disulphide bond isomerase are transformed into the pichia pastoris for co-expression, and the enzyme activity of the alpha-glucosidase gene can be up to 10.1U / mL after induction is carried out for 110 hours in a 3L tank, and is 2.9 times of the enzyme cavity before optimization. The optimized alpha-glucosidase gene can be used for industrial production of the alpha-glucosidase.

The invention discloses a prunus armeniaca alpha-glucosidase inhibiting peptide as well as a preparation method and application of the inhibiting peptide, wherein the prunus armeniaca alpha-glucosidase inhibiting peptide has an amino acid sequence represented in SEQ ID NO: 1. The prunus armeniaca alpha-glucosidase inhibiting peptide is quite high in alpha-glucosidase inhibiting activity, and is capable of effectively inhibiting the activity of the alpha-glucosidase, thus effectively reducing blood sugar, and preparing medicines for treating hyperglycemia and diabetes; the prunus armeniaca alpha-glucosidase inhibiting peptide is low in production cost, and has huge practical value and economic benefit.