Marine fungus-derived polyketone compound and application thereof in treatment of type 2 diabetes

A technology of polyketides and marine fungi, applied in the fields of microorganisms, metabolic diseases, organic chemistry, etc., can solve the problems of lack of specific drugs, etc., achieve significant inhibitory activity, simple method, and broad application prospects

Active Publication Date: 2015-10-21
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] The development of medical science and the enhancement of human self-health awareness have greatly improved human beings in overcoming diseases and maintaining their own health. disease, there is still no cure for it

Method used

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  • Marine fungus-derived polyketone compound and application thereof in treatment of type 2 diabetes
  • Marine fungus-derived polyketone compound and application thereof in treatment of type 2 diabetes
  • Marine fungus-derived polyketone compound and application thereof in treatment of type 2 diabetes

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The compounds of the present invention can be obtained from marine fungi Aspergillus isolated from the fermentation broth of sp. 16-5B. marine fungi Aspergillus sp. 16-5B is a mangrove plant from Dongzhaigang Mangrove National Nature Reserve, Hainan Island Sonneratia apetala isolated from leaves. Marine fungus Aspergillus Aspergillus The sp. 16-5B strain was deposited in the China Center for Type Culture Collection on April 6, 2015 at Wuhan University, Wuhan, China, with the accession number CCTCC M 2015204.

[0028] The separation method of polyketide is as follows:

[0029] S1. Seed culture:

[0030] S11. Prepare seed medium: glucose 40g, peptone 4g, yeast extract 4g, sea salt 5g, tap water 2000mL, evenly distribute in 8 500mL Erlenmeyer flasks, extinguish at 121°C for 25 minutes.

[0031] Cultivation of seeds: the marine fungus Aspergillus The sp. 16-5B strain was inoculated into the seed medium, and placed on a shaker at a speed of 150 rpm at a tempe...

Embodiment 2

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

[0040] White powder, melting point 121.1-121.6 °C (thermometer uncalibrated), EI-MS (m / z): 372 [M] + ; HR-EI-MS (m / z): 372.1209 [M] + (Theoretical value 372.1204).

[0041] 1 H NMR (500 MHz, CDCl 3 ) δ 11.27 (s, 1H), 6.58 (dd, J = 15.8, 6.7 Hz, 1H), 6.28 (dd,J = 15.8, 1.4 Hz, 1H), 6.16 (s, 1H), 6.08 (d, J = 1.8 Hz, 1H), 6.03 (d, J = 1.8 Hz, 1H), 5.11 (dd, J = 10.5, 6.1 Hz, 1H), 3.07 (dd, J = 16.6, 5.5 Hz, 1H), 2.70 (dd, J = 16.6, 10.5 Hz, 1H), 2.39 (s, 3H), 1.83 (d, J = 6.7 Hz, 3H), 1.56 (s, 3H).

[0042] 13 C NMR (125 MHz, CDCl 3 ) δ 181.9, 170.3, 164.9, 161.6, 161.0, 144.2, 144.1, 138.7, 134.2, 119.0, 112.2, 107.8, 104.8, 101.2, 87.3, 69.6, 24.4, 18.9, 16.

[0043] According to the above data, it is known that the structural formula of polyketides is as shown in formula (I):

[0044]

[0045] Formula (Ⅰ).

Embodiment 3

[0047] The compound in embodiment 1 is carried out α-glucosidase inhibition experiment:

[0048] Using p-nitrophenol-α-glucoside (pNPG) as the substrate, carried out in 0.01M phosphate buffer (pH7.0). 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. Sample and positive control (acarbose) were all made into DMSO solution (both 10 mu mol / mL), the enzyme and the substrate were formulated with 0.01M phosphate buffer solution at a suitable concentration, 1mL initial reaction system contained 0.1unit enzyme, 60 mu L substrate, 20 mu L 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 wavele...

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PUM

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Abstract

The invention belongs to the field of medicinal compounds, and concretely discloses a marine fungus-derived polyketone compound, a preparation method thereof, and an application thereof in treatment of type 2 diabetes. The structure of the polyketone compound is represented by formula (I). The compound can substantially inhibit the activity of alpha-glucosidase, and the IC50 value of the compound is (9.05+ / -0.60)[mu]M. Enzyme kinetic researches show that the compound is a typical noncompetitive inhibitor. The compound 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 polyketide compound derived from marine fungi and its application in treating type II diabetes. Background technique [0002] The development of medical science and the enhancement of human self-health awareness have greatly improved human beings in overcoming diseases and maintaining their own health. disease, there is still no cure for it. Due to the particularity of the growth environment of marine fungi, such as high pressure, high salinity, and lack of oxygen, in order to adapt to this habitat different from that of land, they have formed unique metabolic pathways, and then produced various secondary metabolites with novel structures and significant physiological activities. generation provides the possibility. At present, searching for new drug sources from marine microorganisms inc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/79A61P3/10C12P17/04C12R1/66
CPCC07D307/79C12P17/04
Inventor 佘志刚刘亚月肖泽恩丁博
Owner SUN YAT SEN UNIV
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