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A class of depsipphenolic acid compounds derived from marine fungi and their application in the treatment of type 2 diabetes

A technology of depacids and marine fungi, applied in the directions of microorganisms, metabolic diseases, organic chemistry, etc., can solve the problems of elevated blood sugar, defects, insufficient insulin secretion, etc., and achieves the effects of low cost, simple method and good market prospects.

Active Publication Date: 2017-05-17
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In type 2 diabetes, the body is able to produce insulin, but relative insufficiency or defective action of insulin (also known as insulin resistance) results in elevated blood sugar

Method used

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  • A class of depsipphenolic acid compounds derived from marine fungi and their application in the treatment of type 2 diabetes
  • A class of depsipphenolic acid compounds derived from marine fungi and their application in the treatment of type 2 diabetes
  • A class of depsipphenolic acid compounds derived from marine fungi and their application in the treatment of type 2 diabetes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Marine fungus Meyerozyma sp.HZ-Y of the present invention 2 It is isolated from the root of the mangrove plant Candela chinensis in the sea area of ​​Huizhou, Guangdong. The separation method refers to the conventional separation method in this field. After isolation, the marine fungus Meyerozyma sp.HZ-Y 2 It was deposited in the China Center for Type Culture Collection on April 6, 2015. The deposit address is Wuhan University, Wuhan, China, and the deposit number is CCTCC NO: M 2015203.

[0029] From the marine fungus Meyerozyma sp.HZ-Y 2 Separate and obtain depsipated phenolic acid compounds in the fermented liquid of the method, concrete steps are as follows:

[0030] S1. Seed cultivation:

[0031] S11. Preparation of seed medium: 200g of potatoes, 20g of glucose, 1L of tap water, evenly distributed in five 500mL Erlenmeyer flasks, and extinguished at 121°C for 30 minutes.

[0032] S12. Cultivation of seeds: the marine fungus Meyerozyma sp.HZ-Y 2 The strain of t...

Embodiment 2

[0039] The compound in embodiment 1 is carried out structural analysis test, obtains following physical and chemical property data:

[0040] Compound 1: light yellow powder, melting point 146-147°C (the thermometer is not corrected), EI-MS (m / z): 288 [M] + .

[0041] Compound 2: Pale yellow needle-like crystals, melting point 165-166°C (the thermometer is not corrected), EI-MS (m / z): 300[M] + .

[0042] Compound 3: white powder, melting point 147-148°C (the thermometer is not corrected), EI-MS (m / z): 302[M] + .

[0043]Compound 4: light yellow powder, melting point 143-144°C (the thermometer is not corrected), EI-MS (m / z): 316[M] + .

[0044] Compound 5: Pale yellow oil, EI-MS (m / z): 302[M] + .

[0045] Compound 6: Pale yellow needle-like crystals, melting point 169-170°C (the thermometer is not corrected), EI-MS (m / z): 314[M] + .

[0046] The NMR data of compounds 1-3 are shown in Table 1, and the NMR data of 4-5 are shown in Table 2.

[0047] NMR data (100MHz / 400MH...

Embodiment 3

[0055] Compound 1-6 in embodiment 1 is carried out α-glucosidase inhibition test:

[0056] Using p-nitrophenol-α-glucoside (pNPG) as a substrate, it was carried out in 0.01M phosphate buffer (pH=7.0). pNPG was enzymatically hydrolyzed into p-nitrophenol by α-glucosidase, and the enzyme activity was calculated by measuring the change of its absorbance at a wavelength of 400nm with a UV-visible spectrophotometer. Both the sample and the positive control (acarbose) were made into DMSO solution (both 10 μmol / mL), and the enzyme and substrate were made into a suitable concentration solution with 0.01M phosphate buffer. 1 mL of the initial reaction system contained 0.1 unit enzyme, 20 μL Substrate, 20 μL DMSO. Take an appropriate amount of enzyme solution, add the blank DMSO solution or sample DMSO solution, mix well, keep the temperature at 37°C for 20 minutes, add the substrate, mix well, and immediately detect the change value of the absorbance of the system within 1min at a wav...

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Abstract

The invention belongs to the field of medicinal compounds, and concretely discloses marine fungus-derived depside compounds and an application thereof in treatment of type 2 diabetes. The structure of the depside compounds is represented by formula (I). The compounds 1-6 can substantially inhibit the activity of alpha-glucosidase, the IC50 value of the compound 1 is 10.4[mu]M, the IC50 value of the compound 2 is 13.3[mu]M, the IC50 value of the compound 3 is 2.1[mu]M, the IC50 value of the compound 4 is 12.4[mu]M, the IC50 value of the compound 5 is 9.8[mu]M, and the IC50 value of the compound 6 is 11.7[mu]M, wherein the IC50 value of positive control acarbose is 553.7[mu]M. Kinetic researches of the alpha-glucosidaseinhibition effect show that the compounds 1, 3 and 5 are noncompetitive inhibitors. The compounds can be used for preparing alpha-glucosidase inhibitor medicines in order to prevent and treat the type 2 diabetes.

Description

technical field [0001] The present invention relates to the field of pharmaceutical compounds, in particular to pharmaceutical compounds derived from marine fungi, more specifically, to a class of depsipphenolic acid compounds derived from marine fungi and their application in treating type II diabetes. Background technique [0002] Currently, there are more than 370 million people with type 2 diabetes worldwide, and the number of patients is still growing rapidly. This increase is associated with economic development, aging populations, increasing urbanization, changing dietary habits, reduced physical activity, and other lifestyle changes. Therefore, type II diabetes is considered to be one of the most serious challenges to public health security in countries around the world in the 21st century. In type 2 diabetes, the body is able to produce insulin, but relative insufficiency or defective action of insulin (also known as insulin resistance) results in elevated blood su...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D321/10C12P17/08A61P3/10C12R1/645
CPCC07D321/10C12P17/08
Inventor 佘志刚陈森华刘昭明刘亚月谭春兵陆勇军何磊
Owner SUN YAT SEN UNIV
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