Aminosugar compound and process for production thereof

A production method and compound technology are applied in the field of amino sugar compounds to achieve the effect of inhibiting sugar absorption

Inactive Publication Date: 2011-03-30
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is a problem of side effects such as digestive organ symptoms (abdominal distension, diarrhea, loose stools, flatulence, farting, etc.) caused by glucosidase inhibition

Method used

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  • Aminosugar compound and process for production thereof
  • Aminosugar compound and process for production thereof
  • Aminosugar compound and process for production thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0130] (nourish)

[0131] In a Erlenmeyer flask with a volume of 100mL, add 30mL each time the culture medium (pH=7.0) containing 20g soluble starch, 10g Pindex #3 (manufactured by Matsutani Chemical Co., Ltd.), 20g soybean flour and 1L distilled water, at 121°C Sterilize in a pressure cooker for 30 minutes to prepare a stock culture medium.

[0132] A slant culture of the Streptomyces sp-6982 strain was inoculated into the stock culture medium by 1 platinum spoon, and cultured with shaking at 30° C. for 3 days.

[0133] Into a Erlenmeyer flask with a capacity of 100mL, 30mL each time, add 100g soluble starch, 60g soybean flour, 2.5g NaCl, 2g CaCO 3 and a culture medium (pH=7.0) of 1 L of distilled water were autoclaved at 121° C. for 30 minutes to prepare a production medium.

[0134] Into this production medium, 2 mL each time, each flask was inoculated with the above-mentioned mother seed culture solution, and cultured with shaking at 25° C. for 7 days.

[0135] Roughly ...

Embodiment 2

[0226] The α-amylase inhibitory activity of the compounds of the present invention was confirmed by the following method.

[0227] (1) Experimental method

[0228] ICR mice (male, 8 weeks old, purchased from SLC, Japan), SD rats (male, 8 weeks old, purchased from Japan’s Chayaru Srivier), beagle dogs (male, 35 months old, purchased from Naruku Co., Ltd.) and rhesus monkey (male, 10 years old, purchased from Japan CLEA) to prepare mouse, rat, dog and monkey pancreas α-amylase solutions. Human salivary and pancreatic alpha-amylases were prepared from enzymes purchased from Sigma-Aldrich. These α-amylase solutions were all assayed with buffer (48mM NaCl, 5.4mM KCl, 28mM Na 2 HPO 4 , 43mMNaH 2 PO 4 , 35mM mannitol, pH=7.0) diluted to 800U / mL. Various α-amylase solutions (20 U, 25 μL) and compounds (25 μL) dissolved in assay buffer were added to 96-well microplates and incubated at 37° C. for 10 minutes. Then starch solution (5 mg / mL, 50 μL) was added and incubated at 37° C. f...

Embodiment 3

[0232] The oral activity of the compound of the present invention was confirmed by the following method.

[0233] (1) Experimental method

[0234] As animals, male ICR (normal) mice (6 weeks old, purchased from Japan SLC) were used. Compounds were made into solutions with 0.5% methylcellulose solution. Blood was collected from mice fasted overnight for determination of blood glucose and plasma insulin levels, and immediately after oral administration of solvent or compound A (0.3 mg / kg, 1 mg / kg, 3 mg / kg, 10 mg / kg) Carbohydrate solution (75 mg / mL starch, 25 mg / mL sucrose, 20 mL / kg). Next, blood was collected 0.25 hours, 0.5 hours, and 1 hour later for measuring plasma insulin levels, and blood was collected 0.5 hours, 1 hour, and 2 hours later for measuring blood sugar levels.

[0235] Blood glucose levels were measured using Glucos CII-Testowako reagent (manufactured by Wako Pure Chemical Industries, Ltd.), and plasma insulin concentrations were measured using a mouse insul...

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PUM

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Abstract

Disclosed is a compound useful as an active ingredient for a pharmaceutical composition having an a-amylase-inhibiting activity, particularly a pharmaceutical composition for the treatment of diabetes. Studies have been made for discovering a compound having an a-amylase-inhibiting activity among the compounds produced by Streptomyces sp. Strain 6982 which is a ray fungus belonging to the genus streptomyces, and it is confirmed that an aminosugar compound has an a-amylase-inhibiting activity. The aminosugar compound has an a-amylase-inhibiting activity, and therefore can be used as a prophylactic or therapeutic agent for diabetes, obesity, NASH (non-alcoholic steatohepatitis), particularly as an ameliorating agent for postprandial blood glucose elevation.

Description

technical field [0001] The present invention relates to an amino sugar compound which can be used as an active ingredient of a pharmaceutical composition (especially a pharmaceutical composition for treating diabetes). Background technique [0002] Some of the polysaccharides ingested during meals are digested by α-amylase derived from saliva in the oral cavity and stomach, and most of them are digested by α-amylase derived from the pancreas in the duodenum and jejunum. Disaccharides or oligosaccharides are thus formed. They are hydrolyzed into monosaccharides by glucosidases represented by maltase and sucrase locally present on the microchorion of the epithelial epithelium of the small intestine, and the monosaccharides are absorbed by the intestine. If the absorbed simple sugar enters the blood and the blood sugar level rises, the pancreas will secrete insulin, so that the sugar released from the liver will decrease, and at the same time, the sugar uptake by muscle or fat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P19/04A61K31/715A61K35/74A61P3/10A61P43/00C08B37/00C12N1/20A61K31/7034C07H15/203A61P1/16A61P3/04C12R1/465
CPCA61K38/00C08B37/0066C08B37/0063C07H15/203C12P19/26C12R1/465C12N1/20A61P1/16A61P3/04A61P43/00A61P3/10C12R2001/465C12N1/205
Inventor 屉村智司屉村裕美西胁真哉
Owner ASTELLAS PHARMA INC
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