Application of compounds aszonalenin and acetylaszonalenin in the preparation of antidiabetic drugs

An anti-diabetic, compound technology, applied in the field of natural medicinal chemistry, achieves the effect of inhibiting α-glucosidase, taking a small amount and having a significant effect

Active Publication Date: 2019-11-12
SHANGHAI PUKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there are no relevant literature reports on whether the aforementioned two compounds have α-glucosidase inhibitory activity; It is still a blank area of ​​research in this field

Method used

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  • Application of compounds aszonalenin and acetylaszonalenin in the preparation of antidiabetic drugs
  • Application of compounds aszonalenin and acetylaszonalenin in the preparation of antidiabetic drugs
  • Application of compounds aszonalenin and acetylaszonalenin in the preparation of antidiabetic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: the preparation method of compound 1 and 2

[0020] 1.1 Preparation of Neosartorium fischii ferment by fermentation culture

[0021] 1) Strains: Neosartorium fischii was purchased from the German Biological Resources Collection (DSMZ), and the strain number is DSM3700.

[0022] 2), strain preservation and activation

[0023] Slant strain preparation: 30.0g sucrose, NaNO 3 3.0g, MgSO 4 ·7H 2 O 0.5g, KCl 0.5g, FeSO 4 ·7H 2 O10.0 mg, K 2 HPO 4 1.0g, 13.0g agar, 1000mL distilled water, adjust the pH to 7.2. After high-temperature sterilization, make a slant, insert the purchased bacteria on the solid medium slant, and cultivate at 28°C for 2-5 days. After the end, place it in a refrigerator at 4°C for later use.

[0024] Plate activation: 200g of potatoes, 20g of glucose (or sucrose), 15-20g of agar, 1000mL of tap water, natural pH, and make plates after sterilization. Inoculate the Neosartoria fischii on the slant into the plate, place it at 28° C. ...

Embodiment 2

[0031] Example 2: Physicochemical properties and spectral data of compound 1

[0032] Compound 1: colorless transparent crystal; molecular formula is C 23 h 23 N 3 o 2 , optical rotation [α] 20 D =+41.538 (c=0.26, CHCl 3 ),That 1 H-NMR and 13 The C-NMR data are as follows: 1 H-NMR (500MHz, DMSO-d 6 )δ H 10.62(1H,s),7.67(1H,dd,7.9,1.4),7.45–7.54(1H,m),7.19(1H,dd,11.2,4.0),7.13(1H,d,7.4),7.08(1H ,d,7.8),6.95–7.00(1H,m),6.68(1H,s),6.63(2H,dd,16.0,7.9),6.11(1H,dd,17.3,10.8),5.47(1H,s) ,4.99–5.18(2H,m),3.99(1H,dd,8.8,7.4),3.31(1H,dd,13.9,7.2),2.30(1H,dd,13.9,9.1),1.06(3H,s), 0.96(3H,s); 1 H NMR (500MHz, CDCl 3 )δ H7.92(1H,s),7.84(1H,d,7.8),7.45(1H,m),7.22(1H,t,7.6),7.16(1H,d,7.5),7.09(1H,t,7.4), 6.90(1H,d,8.2),6.72(1H,t,7.4),6.62(1H,d,7.9),6.12(1H,dd,17.6,10.6),5.59(1H,s),5.14(1H,d ,10.5),5.11(1H,d,17.6),3.99(1H,t,8.1),3.47(1H,dd,14.2,7.6),2.42(1H,dd,14.0,9.0),1.13(3H,s) ,1.06(3H,s); 13 C-NMR (125MHz, DMSO-d 6 )δ C 169.3, 165.9, 149.2, 144.2, 135.4, 132.3, 13...

Embodiment 3

[0035] Example 3: Physicochemical properties and spectral data of compound 2

[0036] Compound 2: Colorless transparent crystal; Molecular formula is C 25 h 25 N 3 o 3 , optical rotation [α] 20 D =-335.71° (c=0.28, MeOH), which 1 H-NMR and 13 The C-NMR data are as follows: 1 H-NMR (500MHz, DMSO-d 6 )δ H 10.68(1H,s),7.81(1H,d,7.9),7.45(2H,m),7.35(1H,d,7.4),7.23(1H,t,7.5),7.09(3H,m),6.06( 1H,s),5.87(1H,dd,17.3,10.8),5.06(2H,m),3.84(1H,t,8.3),3.20(1H,dd,13.7,8.3),2.47(3H,s), 2.42(1H,dd,13.7,8.4),1.25(1H,d,12.2),1.10(3H,s),0.92(3H,s); 1 H NMR (500MHz, CDCl 3 )δ H 8.02(1H,d,7.9),7.72(1H,d,7.8),7.64(1H,s),7.41(1H,t,7.5),7.28(1H,t,7.6),7.24(1H,d,7.6 ),7.19(1H,t,7.6),7.07(1H,t,7.5),6.86(1H,d,8.2),5.93(1H,s),5.89(1H,dd,17.5,10.4),5.15(1H ,d,10.4),5.12(1H,d,17.5),3.90(t,8.4),3.37(1H,dd,13.9,8.5),2.59(3H,s),2.45(1H,dd,13.9,8.2) ,1.20(3H,s),0.99(3H,s); 13 C NMR (125MHz, DMSO-d 6 ) δ C 169.7,168.7,165.9,143.7,141.6,135.1,134.1,132.1,130.0,128.3,126.9,125.1,124.2,123.6,...

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Abstract

The invention discloses an application of compounds aszonalenin and acetylaszonalenin to preparing glycosidase inhibitor medicine, and particularly discloses an application to preparing anti-diabetic medicine. Monomeric compounds of aszonalenin and acetylaszonalenin are stable and easy to store, and alpha-glycosidase can be remarkably inhibited. An experiment shows that the activity of the monomeric compounds is obviously better than that of post-marketing medicine acarbose, and the effect is remarkable; in addition, the molecular weights of the compounds aszonalenin and acetylaszonalenin are smaller than that of the acarbose, and the compounds aszonalenin and acetylaszonalenin have the advantages of being small in dose; in conclusion, the compounds aszonalenin and acetylaszonalenin have the potential value of being developed into anti-diabetic candidate medicine.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry, and in particular relates to the application of compounds aszonalenin and acetylaszonalenin in the preparation of antidiabetic drugs. Background technique [0002] Diabetes is a common clinical metabolic disease characterized by hyperglycemia caused by insulin secretion defect or its biological action disorder, and is an important killer of human health. With the progress of society and the improvement of people's living standards, it has become a global The incidence of diabetes in China is increasing. According to statistics from the world-renowned medical journal Lancet, there are currently nearly 400 million people with diabetes in the world, and nearly 100 million people in my country, showing a trend of increasing year by year. Diabetes is causing increasing losses to our country's health and national economy. Diabetes cannot be cured at the current medical level, but controlling ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5517A61P3/10
Inventor 单伟光王石磊占扎君应优敏马列峰陈艳吴睿唐岚
Owner SHANGHAI PUKANG PHARMA
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