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Two kinds of triple benzodioxazine derivatives and their application

A technology of drug and action, applied in the field of triple benzodioxazine derivatives and its application, can solve the problems of heart system risk, toxic and side effects, etc., achieve strong inhibition of α-glucosidase, safety guarantee, huge social The effect of benefits and economic benefits

Active Publication Date: 2015-09-02
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The α-glucosidase inhibitors currently on the market are mainly acarbose, voglibose, miglitol, etc., but it is worth noting that these inhibitors currently used have brought different Degree of toxic side effects, such as gastrointestinal side effects, urticaria, liver dysfunction, cardiac system risk, etc.

Method used

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  • Two kinds of triple benzodioxazine derivatives and their application
  • Two kinds of triple benzodioxazine derivatives and their application
  • Two kinds of triple benzodioxazine derivatives and their application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Preparation of compound shown in embodiment 1, formula I and compound shown in formula II

[0028] One, the preparation of compound shown in formula I and compound shown in formula II

[0029] Take fresh Sarcodon leucopus fruiting bodies, dry and pulverize them, weigh 200 grams, then soak them in 2 liters of absolute ethanol, ultrasonically crush them for 60 minutes, soak them overnight (12-16 hours), and collect the filtrate by filtration. Repeat the operation of soaking in absolute ethanol-ultrasonic-filtration three times, then combine the filtrates, concentrate under reduced pressure, and dry to obtain 12.6 grams of ethanol extract extract.

[0030] Use 500 ml of ethanol aqueous solution with a volume fraction of 20% to dissolve the above-mentioned extract, and pass the resulting solution into a macroporous adsorption resin column (D101 type, the total column volume is 1500 ml, and the diameter-to-height ratio is 1:10), and repeatedly adsorb 4 times, and then use 2...

Embodiment 2

[0042] Preparation of compound shown in embodiment 2, formula I and compound shown in formula II

[0043] Take freshly collected fruiting bodies of Sarcodon leucopus (see Example 1 for identification), weigh 50 g after drying and pulverizing, soak in 1000 ml of ethyl acetate, ultrasonicate for 60 minutes, soak overnight (12-16 h), and collect the filtrate by filtration. Repeat the above-mentioned ethyl acetate soaking-ultrasonic-filtration operation 6 times, then combine the filtrates, concentrate under reduced pressure, and dry to obtain 2.8 grams of ethyl acetate extract.

[0044] Use 100 ml of ethanol aqueous solution with a volume fraction of 20% to dissolve the above-mentioned extract, and pass the resulting solution into a macroporous adsorption resin column (D101 type, the total volume of the column is 300 ml, and the ratio of diameter to height is 1:8), and repeatedly adsorb 3 times, and then eluted with 800 ml of 50% ethanol water solution by volume fraction, and then...

Embodiment 3

[0047] Embodiment 3, the in vitro inhibition alpha-glucosidase activity test of two kinds of compounds

[0048] Test sample solution: final concentrations of 25.0μM, 12.5μM, 6.3μM, 3.1μM, 1.6μM, 0.8μM compound solution shown in formula I and compound solution shown in formula II (dissolved in a small amount of DMSO, diluted with distilled water To the corresponding concentration, control the final volume fraction of DMSO < 0.1%); and as a positive control, acarbose solutions with final concentrations of 4000 μM, 1000 μM, 250 μM and 62.5 μM (dissolved in a small amount of DMSO, diluted with distilled water to the corresponding Concentration, control the final volume fraction of DMSO <0.1%).

[0049] Take 25 μL of the above test sample solutions with different concentrations, add 25 μL α-glucosidase aqueous solution (concentration: 0.2 U / mL) and 175 μL phosphate buffer solution (50 mM, pH7.0). After the mixed solution was left at room temperature for 10 minutes, 25 μL of 4-nitr...

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Abstract

The invention aims to provide two terphenylzidioxazine derivatives and applications thereof. The two terphenylzidioxazine derivatives provided by the invention are compounds shown in formulas I and II. Two new sarcoviolin compounds in the invention can efficiently suppress the activity of alpha-glucosidase, thereby improving the control on type II diabetes. Meanwhile, Animal experiments also show that the two new sarcoviolin compounds can effectively reduce the blood glucose of animals. The compounds disclosed by the invention are derived from edible fungi, so that the compounds have a certain secure base. In conclusion, the two new sarcoviolin compounds in the invention have various market application values of developing alpha-glycosidase inhibitors, preparing drugs for preventing and treating type II diabetes, preparing foods or functional health-care foods, and the like.

Description

technical field [0001] The present invention relates to two ternary benzodioxazine derivatives and applications thereof, in particular to two new ternary benzodioxazine compounds and their application as alpha-glucosidase inhibitors. Background technique [0002] Diabetes is a common clinical disease caused by the lack or relative lack of insulin in the human body. The World Health Organization (WHO) divides diabetes into two main types: type I diabetes (or insulin-dependent, IDDM) and type II diabetes (or insulin-dependent diabetes mellitus) called non-insulin-dependent, NIDDM). Among them, type 2 diabetes accounts for the majority. There are more than 20 million diabetic patients in my country, and nearly 90% of them are type 2 diabetes, and it appears multiple and younger, which seriously threatens national health. [0003] α-glucosidase is a hydrolase of maltose, sucrose or other oligosaccharides in the small intestine. The hydrolysis eventually produces glucose, which ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D498/04A61K31/5395A61P3/10A23L1/30A23L33/10
CPCC07D498/04
Inventor 刘宏伟马轲韩俊杰宝丽
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI