175 results about "Alpha-glucosidase inhibitor" patented technology

This invention is directed to a novel method and composition for the treatment of diabetes mellitus (Type I, Impaired Glucose Tolerance ["IGT"]and Type II). More specifically, this invention pertains to a novel method of treating diabetes mellitus by incorporating a therapeutic amount of one or more insulin sensitizers along with one or more of an orally ingested insulin, an injected insulin, a sulfonylurea, a biguanide or an alpha-glucosidase inhibitor for the treatment of diabetes mellitus.

The present invention discloses an alpha-glucosidase inhibitor for prevention of transition from high-risk IGT to diabetes mellitus, for prophylaxis of diabetes mellitus, as well as for treating high-risk IGT.

This invention is directed to a novel method and composition for the treatment of diabetes mellitus (Type I, Impaired Glucose Tolerance ["IGT"] and Type II). More specifically, this invention pertains to a novel method of treating diabetes mellitus by incorporating a therapeutic amount of one or more insulin sensitizers along with one or more of an orally ingested insulin, an injected insulin, a sulfonylurea, a biguanide or an alpha-glucosidase inhibitor for the treatment of diabetes mellitus.

The invention relates to compositions comprising three inhibitors, one pancreatic lipase inhibitor, an alpha glucosidase inhibitor, and a sodium dependent glucose transporter inhibitor. The invention also provides methods of using the compositions for controlling glucose and lipid uptake.

The invention relates to compositions comprising at least two inhibitors selected from the group consisting of an alpha amylase inhibitor, an alpha glucosidase inhibitor, and a sodium dependent glucose transporter inhibitor. The invention also provides methods of using the compositions for controlling glucose uptake.

The methods of the invention relate to the treatment of diabetes, including type 2 diabetes, and related disorders by administration of a PDE10A inhibitor. Such PDE10A inhibitors may be administered in conjunction with alpha-glucosidase inhibitors, insulin sensitizers, insulin secretagogues, hepatic glucose output lowering compounds, B-3 agonist, or insulin. Such PDE10A inhibitors may also be administered in conjunction with body weight reducing agents. Further methods of the invention relate to stimulating insulin release from pancreatic cells, for example, in response to an elevation in blood glucose concentration, by administration of a PDE10A inhibitor.

The invention discloses anextract of Chinese herbs containing alpha-glycoside enzyme inhibitor, which comprises cytidine, 2-(1',2',3',4'-tetrahydroxylbutyl)-5-(2'',3'',4''-trihydroxybutyl)-pyrazine and 1-deoxynojirimycin. The extract can be obtained from leaves, branches and peels of mulberries. The extract can be used for preparing medicament for treating diabetes.

A process for degradating the agar polyose to obtain agar oligose includes such steps as dissolving the agar powder or agar strips in the solution of sodium hydrogen phosphate and sodium dihydrogen phosphate, adding H2O2 for degradating under existance of Fe ions, adding VC for triggering reaction, adding hydrogen peroxidase for stopping reaction, high-speed centrifugal treating, depositing in alcohol, taking supernatant, evaporating and freeze drying. The resultant product has the molecular weight of about 3000 and the action and function of alpha-glucosidase inhibitor. Its advantages are high output rate (more than 85%) and low cost.

The present invention relates to the use of a combination of a certain DPP-4 inhibitor and an alpha-glucosidase inhibitor for use in therapy, e.g. for use in treating and / or preventing a metabolic disease such as type 2 diabetes mellitus and / or conditions related thereto. The invention also relates to the use of such combination for improving body weight control, reducing body weight, inducing satiety, inhibiting gastric emptying and / or reducing food intake, in a patient in need thereof.

The invention provides a dogberry medicament having alpha-glucosaminidase inhibiting activity, and the water or organic solvent extract of dogberry, wherein the dogberry extract comprises total glycosides and poly phenols constitution.

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 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 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 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 aims at disclosing a virtual screening method of an alpha-glucosidase inhibitor, the virtual screening method and the application of screened compounds in pharmaceutical preparations forpreventing and / or treating 2-type diabetes. The method comprises the steps of 1, the obtaining, analyzing and treating of the three-dimensional structure of a large molecular protein; 2, the construction of a traditional Chinese medicine natural product library and the preparation of a small molecular compound; 3, the calibration of the prediction capability of a virtual screen model and the establishment of the screen model; 4, the virtual screening of the natural product library and the analyzing of a mutual impacting mechanism; 5, in vivo and in vitro biological activity verification of ascreening result. The method is used for screening and can be used for the discussing of a structure-activity relationship of compounds of the type, and the further modification of a structure based on a biological compound is guided.

The invention relates to an alpha-glucosidase inhibitor and a preparation method thereof. The preparation method comprises the following steps: culturing and activating a strain; culturing seeds; inoculating the stain into a shake flask for fermentation culture; collecting fermentation liquor; and performing separation and purification to obtain the alpha-glucosidase inhibitor. In the invention, the alpha-glucosidase inhibitor is obtained by microbial fermentation and can be used for developing hypoglycemic medicaments and provide a new tool for further research on active site of enzymes such as the alpha-glucosidase.

The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R2 is H, halogen, C1-12 alkyl or C1-12 haloalkyl; and R3 is C3-6 cycloalkyl, C1-12 alkyl, C1-12 haloalkyl, C3-6 cycloalkyl-C1-4-alkylene, aryl-C1-4-alkylene or heteroaryl-C1-4-alkylene, wherein said aryl-C1-4-alkylene and heteroaryl-C1-4-alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.

The present invention relates to a method for providing alpha -glucosidase inhibition to a subject by administering a pharmaceutical composition comprising a alpha -glucosidase inhibitory agent selected from pipataline (formula 1a), sesamin (formula 1b), pellitorine (Formula 1c), guineensine (Formula 1d) and brachystamide-B (formula 1e) having therapeutic application for diabetes mellitus, cancer, viral diseases such as hepatitis B and C, HIV, AIDS etc; also the invention provides a process for the isolation of said alpha -glucosidase inhibitory agent from the plant source Piper longum in significant yields.

The present invention provides methods for treating a flavivirus infection, including hepatitis C virus (HCV) infection, in an individual suffering from a flavivirus infection. In some embodiments, the methods involve administering to an individual in need thereof an effective amount of an agent that inhibits enzymatic activity of a membrane-bound α-glucosidase inhibitor. In other embodiments, the methods involve administering to an individual in need thereof effective amounts of an α-glucosidase inhibitor and at least one additional therapeutic agent.

The invention discloses an inonotus obliquus submerged fermentation product and application. The inonotus obliquus submerged fermentation product comprises a composition A, a composition B and a composition C. By the utilization of a biological fermentation technology, inonotus obliquus strains are fermented to obtain the new composition, and the composition belongs to a natural alpha-glucosidase inhibitor, and is low in price and environmentally friendly; the preparation technology is easy to industrialize. The inonotus obliquus submerged fermentation product is suitable for a broad crowd of people, convenient to eat and capable of serving as a daily drink to be drunk by people with diabetes, will not generate adverse reactions such as abdominal discomfort, flatulence and exsufflation, and can achieve a health-care effect after being drunk by average persons.

The present invention provides a plant-derived carbohydrase inhibitor, wherein the inhibitor is effective for preventing or alleviating diabetes, or preventing obesity, and foods, drinks, and medicines containing the same. The present invention is accomplished by use of an alpha-amylase inhibitor or an alpha-glucosidase inhibitor as a carbohydrase inhibitor that is extracted from astringent skins of a chestnut using ethanol or aqueous ethanol solution. The present invention can also be accomplished by adding the carbohydrase inhibitor to a food or medical composition as an active ingredient for delaying saccharide digestion or absorption, suppressing a rise in postprandial blood glucose levels or blood insulin levels, or preventing obesity.

The invention discloses an application of radix acanthopanacis trifoliate extract in inhibiting alpha-glucosidase. The radix acanthopanacis trifoliate extract is extracted and concentrated by ethanol and then extracted respectively by petroleum ether, ethylacetate and normal butanol. The radix acanthopanacis trifoliate extract is identified to have 9 terpenoids. The invention also discloses an alpha-glucosidase inhibitor, and the alpha-glucosidase inhibitor comprises radix acanthopanacis trifoliate extract as well as one or more additives acceptable on the medicine. The experiment shows that the extract of radix acanthopanacis trifoliate leaves, stalks and roots has inhibitory activity for the alpha-glucosidase; in 9 terpenoids of the radix acanthopanacis trifoliate extract, the compound 6 has best activity for inhibiting the alpha-glucosidase, which is far higher than a reference product acarbose.

The invention discloses a method for extracting an alpha-amylase and alpha-glucosidase inhibitor from bangia fusco-purpurea,which comprises the following steps of 1, extraction: cleaning, drying and smashing fresh bangia fusco-purpurea to obtain bangia fusco-purpurea powder, adding distilled water, extracting and concentrating to obtain a concentrated solution; 2, alcohol precipitation: dropwise adding ethyl alcohol, centrifuging, taking sediments, performing freeze drying to prepare crude polysaccharide; 3, gel chromatography: dissolving the crude polysaccharide into distilled water, sample loading, eluting, tracing and checking, collecting eluting peaks, performing dialysis desalting, andperformingfreeze drying to obtain purified polysaccharide, so that the alpha-amylase and alpha-glucosidase inhibitor is prepared. The method provided by the invention has the advantages that the preparation technology is simple, the cost is low, and the extracted alpha-amylase and alpha-glucosidase inhibitor has the activity for inhibiting blood glucose elevation.

The invention provides applications of four kaurane diterpene compounds in preparation of glycosidase inhibitor medicines. The four compounds capable of highly inhibiting alpha-glycosidase activity are natural compounds which are high in safety and capable of rapid natural degradation without residue in the environment. The four compounds are obtained by separation from wedelia trilobata, and other plant materials. The plant materials are rich in source. A preparation process is easy in operation. Monomers of the four compounds are stable and liable to store. The alpha-glucosidase inhibition activity of the four compounds is obviously higher than or equivalent to that of acarbose that is a clinic medicine. The four compounds are extremely likely developed into effective and safe alpha-glucosidase inhibitor medicines used for preventing and treating type II diabetes, and have good prospects.

The invention relates to a preparation method for an alpha-glucosidase inhibitor. The preparation method is characterized by comprising the following steps: carrying out ultrasonic extraction on hizikia fusiforme powder in a circulating ultrasound instrument with addition of distilled water, centrifuging, taking supernatant, carrying out vacuum rotary evaporation concentration on the supernatant until the volume is one fifth of the original volume of the supernatant, adding the supernatant into absolute ethyl alcohol, leaving the solution to stand, centrifuging and freeze-drying precipitates under a vacuum condition; dissolving freeze-dried precipitates in water to prepare into a sample loading solution, injecting the sample loading solution into D311 macroporous resin for adsorption to remove protein and pigment, so as to obtain first eluent; carrying out adsorption eluting on the obtained first eluent in a DEAE-52 anion exchange fiber column and carrying out constant-gradient elution through a NaCl-Tris-HCl buffer solution system with the NaCl concentration of 0-3 M; collecting eluent under the conditions that the wavelength is 215 nm and the concentration of NaCl is 0.5-1 M, carrying out membrane concentration desalination on the eluent under a 3.5 KD tangential flow ultrafiltration membrane until the volume is one fifth of the original volume and carrying out vacuum freeze-drying so as to obtain the alpha-glucosidase inhibitor.

The invention discloses a new application of total aglycone of himalayan teasel roots and single-component hederagenin in medicaments preparing Alpha-glucosidase inhibitor; the medicaments preparing the Alpha-glucosidase inhibitor can be the total aglycone of himalayan teasel roots, the single-component hederagenin, or a compound containing the total aglycone of himalayan teasel roots and the single-component hederagenin, which all can be prepared into tablets, capsules, granules, injections and suspensions.

The invention relates to a method for extracting effective ingredient as Alpha-glucosidase inhibitor, which belongs to the fields of Chinese herbal medicine preparation and chemical technology. The method comprises the following steps of: performing liquid extraction with organic solvent to remove ingredients with low Alpha-glucosidase inhibitory activity, and extracting effective ingredients with high Alpha-glucosidase inhibitory activity by using macroporous adsorptive resin and Sephadex LH-20 column chromatography technique. The yield of the inhibitor is 4%. The inventive method has the advantages of simple process, easy operation, high product purity, no harmful substances in product, and no environmental pollution. The obtained plant extract in the invention can be used for developing hypoglycemic drugs and further researching physical structure thereof.

The invention discloses a preparation method of an Inonotus obliquus extract which can be used as an Alpha-glucosaccharase inhibitor. In the preparation method, ethanol is firstly adopted to heat and reflow the Inonotus obliquus so as to obtain an ethanol extract, then the ethanol extract is fully dispersed into distilled water and is extracted by sherwood oil so as to remove low-polarity components in the extract, which have no inhibition activity to the Alpha-glucosaccharase; and then the raffinate is extracted by ethyl acetate, thereby obtaining the extract which has strong inhibition activity to the Alpha-glucosaccharase; and the yield rate is 2 to 4 percent. Experiment proves that the Inonotus obliquus extract obtained by the preparation method provided by the invention has very strong inhibition activity to the Alpha-glucosaccharase; when the dosage is 400 Mug, the inhibition rate can reach 80.5 percent, with the IC50 of 103.9 Mug / ml; therefore, the method can be used for developing sugar-reducing medicament. Moreover, the preparation method also has the advantages of simple technique, convenient operation, and the like.

The invention provides a method for extracting water-soluble alpha-glucosidase inhibitor, which comprises the following steps: crushing and screening medicinal fungal fruiting bodies (inonotus obliquus and phellinus igniarius) through a sieve with 60 to 100 meshes;, weighting and quantifying; adding water of 20 to 40 times by weight; treating through ultrasound for 20 to 40 minutes; adding liquid-state high-temperature amylase, and extracting in boiling water for 2 to 4h; centrifuging and deslagging the material of more than 3800g; vacuum condensing supernate to be 1 / 10 to 1 / 15 of the original volume; adding edible ethanol until the concentration reaches 80 percent and depositing in alcohol for over 8h; precipitating and adding distilled water for re-dissolving; ultrafiltering through a 10 thousand molecular weight cutoff film for 12 to 24h; vacuum condensing filtrate; and freezing and drying extracts (medicinal fungus water-soluble alpha-glucosidase inhibitor). By adopting the method provided by the invention, the water-soluble alpha-glucosidase inhibitor with better activity can be obtained; the inonotus obliquus and the phellinus igniarius as the raw materials are medicinal fungi having longer application history and fewer toxic or side effects. In addition, the process flow adopted in the invention does not involve toxic or harmful steps, has high safety and is especially favorable for the subsequent development of medical healthcare foods.

The invention discloses a preparation method for an alpha-glucosidase inhibitor as well as a product and a usage thereof. The preparation method comprises the following steps: centrifugalizing fermented soy bean milk and taking supernatant, extracting the obtained supernatant by using ethyl acetate, depressurizing and evaporating the obtained ethyl acetate-phase to be dry, adding ethyl acetate to prepare an alpha-glucosidase inhibitor crude extraction liquid, separating and eluting the obtained crude extraction liquid by using a silica gel column, testing inhibition of the obtained eluant to alpha-glucosidase, combining and collecting the eluants of component peak according to inhibition effects and freeze-drying to obtain the alpha-glucosidase inhibitor. The invention provides an active ingredient which is separated from a soy bean fermentation product and has obvious inhibition effect to alpha-glucosidase, and offers new ideas for industrial preparation and usage of soy bean fermentation-originated alpha-glucosidase inhibitor. According to the invention, the obtained alpha-glucosidase inhibitor can be directly used in production of products for controlling absorption of carbohydrate in intestinal tract, so as to achieve the purpose of blood glucose fluctuation control.