332 results about "Glucosidase Inhibitor" patented technology

The combination of a HMG CoA reductase inhibitor like a statin, such as simvastatin, with a pFox inhibitor such as trimetazidine (“Simetazidine”) is particularly advantageous for treatment of end-stage complications, such as acute coronary syndrome (ACS) and chronic angina, especially in type II diabetics. The combination therapy is also useful in the treatment and/or prevention of chronic heart failure (CHF) and peripheral arterial disease (PAD). The combination of a nitric oxide (NO) mechanism with increased NO production with pFox inhibition simultaneously treats both the effect and the cause of angina. One or more oral hypoglycemic compounds (biguanides, insulin sensitizers, such as thiazolidinediones, α-glucosidase inhibitors, insulin secretagogues, and dipeptidyl peptidase IV inhibitors), protein kinase C (PKC) inhibitors, and acetyl-CoA carboxylase inhibitors can also be used in combination with the HMG CoA reductase inhibitors and/or pFox inhibitors, especially in type II diabetics, to control glucose levels and treat endothelial dysfunction. The drugs can be given in combination (e.g. a single tablet) or in separate dosage forms, administered simultaneously or sequentially. In the preferred form the statin is given in a dose of between 5 and 80 mg/day in two separate doses, and the pFox inhibitor is administered in a sustained or extended dosage formulation at a dose of 20 mg three times a day or 35 mg two times a day. The dose of the oral hypoglycemic, PKC inhibitor, or acetyl-CoA carboxylase inhibitor varies with the type of drug used.

Disclosed is a method and composition for nutritional compositions containing -glucosidase inhibitors, and more specifically Touchi Extract and its uses in the treatment of many disorders. These disorders include diabetes, hyperlipidemia, obesity, Metabolic syndrome/Syndrome X, COPD, malabsorption, Crohn's disease, diarrhea, constipation, irritable bowel syndrome, human immunodeficiency virus, cystic fibrosis, non-alcoholic steatohepatitis, polycystic ovarian syndrome including associate infertility, and erectile dysfunction. Further, -glucosidase inhibitors, and more specifically Touchi Extract can be used to aid healing in critical care patients and for general wound healing. Additionally, -glucosidase inhibitors, including Touchi Extract can be used to enhance athletic performance.

The present invention provides pharmaceutical compositions and methods for the treatment of diabetes mellitus using combination therapy. The compositions relate to a compound of Formula I selected from one or more of betaines, lipidic betaines, betaine lipids and an antidiabetic agent such as sulfonylureas, biguanides, glitazones, .alpha.-glucosidase inhibitors, potassium channel antagonists, aldose reductase inhibitors, glucagon antagonists, activators of RXR, insulin therapy or other anti-obesity agent. The methods include the administration of the combination of compound of Formula I with antidiabetic agent where the two components are delivered in a simultaneous manner, where the compound of Formula I is administered first, followed by the antidiabetic agent, as well as wherein the antidiabetic agent is delivered first followed by the compound of Formula I.

The invention relates to a method for preparing timosaponin BIII. The method separates an effective constituent of timosaponin BIII from a Chinese traditional medicine anemarrhenae in a chemical way. Simultaneously in-vivo and in-vitro pharmacological tests verify that: as the compound can remarkably inhibit the activity of alpha-glucosaccharase, and effectively reduce animal blood sugar, the compound can be applicable to the preparation of alpha-glucosaccharase inhibitors and medicines for curing diabetes. The method for preparing the timosaponin BIII replaces HPLC preparation with processes such as crystallization with simple operation, thereby facilitating industrialized production more effectively. Simultaneously, the compound displays good anti-diabetes activity in vivo and vitro, thereby not only widening the application field of the compound, but also becoming the effective medicine for curing diabetes in future.

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 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 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.

Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.

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 invention relates to a process for preparing alpha- glucosidase depressant from Cinnamomum cassia, which comprises removing low-polarity constituents with no inhibiting activity to alpha-glucosidase from Cinnamomum cassia by means of fluid extraction technique, and carrying out solid-liquid oscillation extraction to the residual of extracting with anhydrous alcohol. The extracted effective portion has rather strong inhibiting activity to alpha-glucosidase.

The invention discloses a preparation method for a compound 3 alpha-Akebonolic acid and the application of the compound in the preparation of a glycosidase inhibitor drug. According to the invention, an alpha-glucosaccharase inhibitor is extracted and separated from akebia plants; the source of the plant material is abundant, the extraction and preparation method is easy to operate, and the plants can be utilized for a long term without being damaged through adopting fruits for extraction, so that the economic benefit can be improved, and the monomeric compound is environmentally friendly, stable, and easy to store. Pharmacology experiments show that the activity of the alpha-glucosaccharase inhibitor of the compound 3 alpha-Akebonolic acid is higher than that of the first-line diabetes drug acarbose, so that the compound 3 alpha-Akebonolic acid is expected to be developed into a drug for preventing and treating type 2 diabetes mellitus, and has excellent application and development prospects.

The invention discloses space lactobacillus plantarum SS18-37 capable of reducing activity of alpha-glucosaccharase and an application of the space lactobacillus plantarum SS18-37. The lactobacillus plantarum Fullarton-SS18-37 is provided and has the collection number of CGMCC NO.14918. Ground original lactobacillus plantarum GS18 is taken as a control, the space lactobacillus plantarum Fullarton-SS18-37 with higher inhibition on activity of alpha-glucosaccharase is screened out, and the space lactobacillus plantarum Fullarton-SS18-37 has higher tolerance capability for the inverse environmentof the gastrointestinal tract, can smoothly have healthcare efficacy through the gastrointestinal tract and can be the most potential strain for controlling DM (diabetes mellitus).

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 discloses a method for separating an alpha-glucosidase inhibitor from a laver enzymolysis product, which belongs to the technical field of separation and purification of biological products. The invention relates to a method for compounding porphyra yezoensis to obtain a rough alpha-glucosidase inhibitor product, wherein the enzymolysis is controllable and the cost is low. The rough product is separated and purified through SPSepharoseHighPerformance cation exchange chromatography, SephadexG-10 gel chromatography and Mono Q anion exchange chromatography, and the purity and main composition of an LGI (lactate glucose index) part with high inhibitory activity on alpha-glucosidase are analyzed through reversed phase high performance liquid chromatography and ultra-high performance liquid chromatography-mass spectrography. The IC 50 value of LGI on the alpha-glucosidase is 97.63mu g/ml, and the temperature and pH stability are good; the inhibitory activity is kept to be higher than 80% in 80 DEG C water bath for 7 h, and the inhibitory activity is still kept to be higher than 87% after being maintained in a buffer solution with pH of 3-12 at 50 DEG C for 2 h. The LGI is small in molecular weight, good in stability, low in cost and safe to use, thereby having a quite wide application prospect in such fields as medicine, food, etc.

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.