17 results about "Acarbose" patented technology

The invention discloses a thiochromanone derivative containing a thiosemicarbazone structure and application of the thiochromanone derivative, relates to the technical field of medicines, and particularly relates to the technical field that the compound has better oxidation resistance and alpha-glucosidase resistance activity, the IC50 value of the compound 1-(7-chloro-4, 4-dioxothiochromanone-3-N-propyl) thiosemicarbazone to ABTS clearance activity is 2.86 [mu] g / mL, the IC50 value of the compound 1-(7-chloro-4, 4-dioxothiochromanone-3-N-propyl) thiosemicarbazone to alpha-glucosidase inhibition activity is 9.51 [mu] g / mL, and the effect is the best and is superior to that of a control agent vitamin E and acarbose. The thiochromanone derivative containing the thiosemicarbazone structure has a general formula shown in the specification,

The invention discloses a stenotrophomonas sp. A322 strain and an application of the stenotrophomonas sp. A322 strain in synthesis of acarbose. The stenotrophomonas sp. A322 is preserved in the China Center for Type Culture Collection, and the preservation number of the stenotrophomonas sp. A322 is CCTCC (China Center for Type Culture Collection) NO: M 2025917. The stenotrophomonas sp. A322 can be used for synthesizing acarbose by using maltose and glucose as carbon sources, and the acarbose can be synthesized by using the stenotrophomonas sp. The stenotrophomonas sp. A322 is subjected to fermentation culture in a 100 mL shake flask fermentation system for 1 to 7 days, and the acarbose yield is 0.4 to 4 g / L. The high performance liquid chromatography retention time and the nuclear magnetic resonance carbon spectrum chemical shift of the acarbose obtained by fermentation, separation and purification of the Stenotrophomonas sp. A322 are consistent with those of a standard substance, and the high performance liquid chromatography retention time and the nuclear magnetic resonance carbon spectrum chemical shift of the acarbose obtained by fermentation, separation and purification of the Stenotrophomonas sp. A322 are consistent with those of the standard substance. Activity detection shows that the separated and purified acarbose sample has alpha-amylase inhibitory activity.

The invention discloses a pyrimidine derivative containing a thiosemicarbazide structure and application of the pyrimidine derivative, and relates to the technical field of medicines, the compound has good oxidation resistance and alpha-glucosidase resistance activity, and the compound is 2-(4, 4 '-difluorophenyl)-2-(4, 4'-difluorophenyl)-2-(4, 4 '-difluorophenyl)-2-(4, 4' The IC50 values of the compound 2-(4, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1-methylsulfamide on DPPH (1, 1-diphenyl-2-picrylhydrazyl) scavenging activity and ABTS (2, 2, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1-methylsulfamide are 3.96 mu g / mL and 2.01 mu g / mL respectively, the IC50 value of the compound 2-(4, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1-methylsulfamide on alpha-glucosidase inhibitory activity is 38.62 mu g / mL, the effect is best, and the compound 2-(4, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1 The pyrimidine derivative containing the thiosemicarbazide structure has a general formula shown in the specification, and is superior to control medicaments such as vitamin C, vitamin E and acarbose.

The application discloses methyl phenolic compounds, a preparation method and application thereof. Six new methyl phenolic compounds are separated from the skin of eleocharis tuberosa, and the compounds all show good inhibitory activity on alpha-glucosidase, and are stronger than the clinical first-line drug acarbose. The inhibitory activity of compound 3 is the best, enzyme kinetics research shows that the compound 3 plays a role as a reversible mixed inhibitor, ADME predicts that the compound 3 has good drug properties, including high gastrointestinal absorption and no CYP450 enzyme inhibition. The cytotoxicity experiment shows that the six compounds have no obvious growth inhibition on human embryonic kidney cells HEK293 at a concentration of 100 muM, and have good safety. The compounds can be combined with a pharmaceutically acceptable carrier to form a pharmaceutical composition, and are used for preparing a health care product for reducing blood sugar or a drug for treating diabetes. The preparation method is simple, easy to operate, suitable for industrial production, and is helpful to the high-value reuse of the skin of eleocharis tuberosa.

The present application relates to a kind of spent grain protein peptide and its preparation method and application. Specifically, with beer brewing by-product spent grain as raw material, it is prepared by protease enzymolysis to prepare spent grain enzymolysis oligopeptide, and it is proved by mouse in-vivo experiment that the enzymolysis complex has the function of improving blood sugar, obesity, blood fat. On this basis, from the enzymolysis product, the key blood sugar reducing active peptide segment FPQPPQ, FPQQPPFG, FPQPQQPFP is identified, and it is verified that its alpha amylase inhibition rate is superior to the same concentration of acarbose. The spent grain protein peptide complex and spent grain protein peptide of the present application have the effect of reducing blood sugar, and can be applied to the development of food, health food, medicine and the like.

The invention provides a preparation method and application of smallanthus sonchifolius polysaccharide YAPa-1, and belongs to the field of food biotechnology and natural polysaccharide development. A main chain in the molecular structural formula of the yacon polysaccharide YAPa-1 is formed by alternating galactose and mannose, and side chains are arabinose, glucose and rhamnose; the molar ratio of the galactose to the mannose to the glucose to the arabinose to the rhamnose is 1.00 to 0.82 to 0.25 to 0.11 to 0.25. The molecular weight of the smallanthus sonchifolius polysaccharide YAPa-1 is 10873 Da, the smallanthus sonchifolius polysaccharide YAPa-1 is of a triple helix structure, the microstructure of the smallanthus sonchifolius polysaccharide YAPa-1 is of a spongy porous network structure, and an alpha-glucosidase / alpha-amylase inhibition mechanism of the smallanthus sonchifolius polysaccharide YAPa-1 can According to the invention, the high-activity single yacon polysaccharide YAPa-1 is directionally obtained through cellulase-assisted hydrothermal extraction and a two-step column chromatography purification process. The smallanthus sonchifolius polysaccharide YAPa-1 can effectively inhibit the activity of alpha-glucosidase and alpha-amylase, the inhibition effect is close to that of a common hypoglycemic drug acarbose, and the smallanthus sonchifolius polysaccharide YAPa-1 is free of common side effects of synthetic drugs and can be applied to development of hypoglycemic products.

The invention discloses application of banana peel melanin to preparation of a medicine for treating diabetes mellitus, and belongs to the technical field of medicines. The melanin is separated from the banana peel through the technologies of ethanol extraction, AB-8 macroporous adsorption resin purification, infrared spectrum identification and the like, the melanin has remarkable inhibitory activity on alpha-glucosidase, the median inhibitory concentration (IC50) is as low as 3.04 mu g / mL, the inhibitory effect is superior to that of a positive control drug acarbose (IC50 is 11.10 mu g / mL), and the melanin has a good application prospect. And a high-quality natural raw material is provided for developing a novel medicine for treating diabetes. In addition, enzyme kinetic research shows that the banana peel melanin inhibits the activity of alpha-glucosidase through an anti-competitive inhibition mechanism, can effectively delay decomposition and absorption of starch substances in intestinal tracts and reduce the postprandial blood sugar peak value, and can be used for preparing safe and efficient blood sugar reducing drugs; meanwhile, high-value utilization of the banana peel waste is achieved, and the method has important economic value and environmental protection significance.

The present invention relates to a modified-release composition comprising orlistat and acarbose, comprising individually distinct parts with different release patterns:a) a first part, G1, comprising from about 5 to about 70% w / w of the total dose of acarbose,b) a second part, G2A, comprising from about 30 to about 95% w / w of the total dose of acarbose,c) a third part, G2B, comprising from about 10 to about 90% w / w of the total dose of orlistat, andd) a fourth part, G3, comprising from about 10 to about 80% w / w of the total dose of orlistat, and the total concentration of acarbose and orlistat, respectively, in the composition is 100% w / w.

The invention discloses multistage amine carbon chain microspheres, a preparation method, a chromatographic column and application. The multistage amine carbon chain microspheres are microspheres of which the surface modification structure is a compound shown as a formula (I). The microspheres not only have the same hydrophilic effect as a traditional amino chromatographic column filler, but also can generate an anion exchange effect through a secondary amine or tertiary amine structure, and can effectively separate acarbose and impurities thereof in combination with steric hindrance selectivity generated by a long-chain structure, the peak separation degree is greater than 2.0, and a base line is completely separated. Meanwhile, the multistage amine carbon chain microsphere is simple in preparation process, a chromatographic column taking the multistage amine carbon chain microsphere as a filler is insensitive to column temperature, pH and solvent composition, the method is easy to develop, the multistage amine carbon chain microsphere can be used for daily analysis, the analysis efficiency is high, and the multistage amine carbon chain microsphere has a good industrial application prospect. Formula (I)

This invention relates to the field of food processing technology and discloses a meal replacement powder composition with hypoglycemic activity and its preparation method. The meal replacement powder uses buckwheat flour, yam flour, bitter melon flour, konjac oligosaccharide, polygonatum powder, and hawthorn powder as raw materials, with an optimized ratio of 2.00g buckwheat flour, 1.00g yam flour, 0.50g bitter melon flour, 0.40g konjac oligosaccharide, 0.40g polygonatum powder, and 0.45g hawthorn powder. The preparation method includes raw material pretreatment and precise ingredient mixing steps. The meal replacement powder of this invention is rich in total polysaccharides, total flavonoids, and total phenolic active ingredients. Its in vitro α-glucosidase inhibition rate is similar to that of acarbose, and its α-amylase inhibition rate is superior to that of acarbose. With a GI value of 53.92 (low GI food), it can effectively delay the rise in postprandial blood glucose, meeting the blood sugar control needs of people with prediabetes. The process is simple, the raw materials are natural, and it has the potential for large-scale industrialization.

The invention belongs to the technical field of industrial microbial fermentation process optimization, and discloses a bulk drug production strain culture method based on morphology and physiological parameters. According to the method, through dual verification of physiological trend and form peak, the misjudgment risk of single parameter judgment is avoided, meanwhile, the trend is captured as soon as possible through change rate analysis, and transplanting can be conducted at the golden moment when the thallus activity reaches the peak but does not decline. By quantifying morphology and setting a clear threshold value, human subjective factors are eliminated, the process reproducibility is extremely high, the principle of the method is suitable for production of raw material medicines fermented by various filamentous bacteria, such as acarbose, moxidectin and tobramycin, and finally accurate seed transfer is realized, so that the fermentation period is effectively shortened, the yield of the raw material medicines is improved, and the method is suitable for industrial production. And remarkable economic benefits are brought.

This invention discloses a strain of oligotrophomonas ( Stenotrophomonas Oligotrophozoites A322 and their application in acarbose synthesis. The oligotrophozoite A322 is deposited at the China Center for Type Culture Collection (CCTCC), accession number CCTCC NO: M 2025917. Oligotrophozoites A322 can synthesize acarbose using maltose and glucose as carbon sources. The acarbose yield of Oligotrophozoites A322 in a 100 mL shake-flask fermentation system for 1–7 days is 0.4–4 g / L. The acarbose isolated and purified from Oligotrophozoites A322 showed consistent high-performance liquid chromatography (HPLC) retention time and NMR chemical shift with the standard. Activity assays showed that the isolated and purified acarbose sample possessed α-amylase inhibitory activity.

The invention relates to the technical field of pharmaceutical analysis, and discloses a purification method of acarbose impurities. The method comprises the following steps: S1, adjusting the pH value of the acarbose waste liquid to be alkaline to obtain a to-be-separated liquid containing an impurity 1-impurity N, loading the to-be-separated liquid to a silica gel column, and carrying out gradient elution I to obtain M primary fractions corresponding to peak values of one or more impurities in the impurity 1-impurity N, M < = N, and N > = 3; s2, respectively adjusting the pH values of the M primary fractions in the step S1 to be alkaline, loading the M primary fractions to a silica gel column for gradient elution II, and collecting secondary fractions corresponding to the peak values of the primary fractions; and S3, concentrating the secondary fraction obtained in the step S2, loading the concentrated secondary fraction into a silica gel column filled with an amino-bonded chromatographic filler, carrying out gradient elution III, and collecting a purified fraction corresponding to a single impurity peak value. The method is simple to operate, various impurities can be separated from a large sample, the purity and the yield of a single impurity are relatively high, and the industrial requirements can be met.

The invention discloses a 2, 3-substituted physalis alkekengi sugar ester compound as well as a preparation method and application thereof. The compound has a structural general formula as shown in a formula (1), in the formula (1), R1 and R2 are-CH3 or-(CH2) XCH3, and X is 1-7. The preparation method comprises the following steps: with calyx seu fructus physalis as a raw material, carrying out ethanol extraction, silica gel column chromatography and thin-layer chromatography separation, recrystallization and the like. In-vitro alpha-glucosidase inhibition experiments show that the compound has significant inhibition activity, the IC50 of the physalis alkekengi sugar ester A1 is 2.06 + / -0.03 mu g / mL, and the activity is superior to that of acarbose. In an STZ-induced diabetic mouse model, the physalis alkekengi glycoester A1 (30 mg / kg) can significantly reduce fasting blood-glucose to a near-normal level, and the effect is superior to that of a positive control. A series of specific compounds (physalis alkekengi sugar esters A1-A8) with the structural characteristics of the general formula (1) are separated and identified from the physalis alkekengi, and specific substances with the hypoglycemic efficacy of the physalis alkekengi are defined.

The application discloses an ester-substituted sugar ester compound, a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The compound has a structural general formula shown in formula (1), wherein R1, R2 and R3 are all -CH3 or -(CH2) X CH3, and X is 1-7. The application first separates and identifies a class of sugar ester compounds with ester substitution on a sucrose parent nuclear skeleton from Physalis alkekengi L. and establishes a high-efficiency preparation method through steps of ethanol extraction, silica gel column chromatography and preparative high performance liquid chromatography. In vitro alpha-glucosidase inhibition experiments show that the compound has significant inhibition activity, wherein the IC 50 value of Physalis alkekengi L. sugar ester C1 reaches 1.05±0.01 μg / mL, and the activity intensity is significantly better than that of the drug acarbose. In a STZ-induced diabetic mouse model, the fasting blood glucose of the Physalis alkekengi L. sugar ester C1 can be reduced from 23.4 mmol / L to 6.2 mmol / L, and the effect is better than that of a positive control group. It is further revealed that introduction of straight-chain alkyl groups at R1, R2 and R3 positions is a structural basis for the class of compounds to exert hypoglycemic activity.

The invention discloses a sugar ester compound as well as a preparation method and application thereof, and belongs to the field of medicinal chemistry. The compound has a structural general formula as shown in a formula (1), R1, R2 and R3 are-CH3 or-(CH2) XCH3, and X is 1-7. The preparation method comprises the following steps: with calyx seu fructus physalis as a raw material, carrying out ethanol extraction, silica gel column chromatography and thin-layer chromatography separation, recrystallization and the like. In-vitro alpha-glucosidase inhibition experiments show that the compound has significant inhibition activity, the IC50 of the physalis alkekengi glycosyl ester B1 is 3.49 + / -0.05 mu g / mL, and the activity is superior to that of acarbose. In an STZ-induced diabetic mouse model, the physalis alkekengi glycoester B1 (30 mg / kg) can significantly reduce fasting blood-glucose to a near-normal level, and the effect is superior to that of a positive control. According to the invention, a series of specific compounds (physalis alkekengi sugar esters B1-B8) with the structural characteristics of the general formula (1) are separated and identified from the physalis alkekengi for the first time, and specific substances with the hypoglycemic efficacy of the physalis alkekengi are defined.

The present application belongs to the technical field of extraction of natural bioactive substances, and particularly relates to a method for extracting flavonoids from hawthorn leaves. The method comprises the following steps: mixing hawthorn leaves with a hydrophobic eutectic solvent, performing ultrasonic treatment, and then centrifuging to obtain an extraction solution. The total flavonoid content extracted by the method is 3.69 times that of ethyl acetate extraction solution and 6.11 times that of ethanol extraction solution. The average DPPH free radical scavenging rate of the extracted extract is 74.35% of the same concentration of vitamin C, the alpha-glucosidase activity inhibition rate is 1.24 times the inhibition rate of the same concentration of acarbose, and the alpha-amylase activity inhibition rate is 2.80 times the inhibition rate of the same concentration of acarbose.