Cysestermerol A and application thereof in aspect of improving diabetes mellitus

A diabetes drug and hypoglycemic technology, which is applied in the field of medicine, can solve the problems of few active ingredients, and achieve the effects of improving insulin resistance, inhibiting activity, and lowering blood sugar levels

Active Publication Date: 2019-12-27
ENLIGHTEN-AFRICA (SHENZHEN) BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Bermudagrass is widely distributed in our country. In recent years, studies have shown that it has antibacterial, diuretic, hypoglycemic and o

Method used

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  • Cysestermerol A and application thereof in aspect of improving diabetes mellitus
  • Cysestermerol A and application thereof in aspect of improving diabetes mellitus
  • Cysestermerol A and application thereof in aspect of improving diabetes mellitus

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The extraction and identification of embodiment 1 Cysestermerol A

[0042] 1. Extraction method

[0043] Bermudagrass is extracted with 95% ethanol aqueous solution to obtain extract extract, which is sequentially extracted with petroleum ether, ethyl acetate and n-butanol to obtain ethyl acetate extract; the ethyl acetate extract is loaded on a silica gel chromatographic column (200~ 300 mesh), different proportions of CH 2 Cl 2 / Acetone gradient elution gives 5 fractions Fr.1, Fr.2, Fr.3, Fr.4, Fr.5; after testing the target compound is concentrated in Fr.5 (CH 2 Cl 2 : acetone=1:1), Fr.5 was subjected to MCI gel CHP 20P column chromatography, SephadexLH-20 gel column chromatography and semi-preparative chromatography to obtain the target monomer compound, denoted as Cysestermerol A.

[0044] 2. Structural identification method

[0045] The planar structure and relative configuration of Cysestermerol A were determined by HR-ESI-MS and NMR, and its absolute config...

Embodiment 2

[0056] Example 2 The improvement effect of Cysestermerol A on IR-HepG2 cells

[0057] 1. HepG2 cell culture

[0058] After recovery, HepG2 cells were cultured in DMEM high-glucose medium containing 10% fetal bovine serum in a 25cm 2 culture flasks, stored in constant temperature CO 2 37°C in an incubator, 5% CO 2 cultivated under conditions. When the cells adhered to 90%, they were washed twice with PBS, digested with 0.25% trypsin, passaged at a ratio of 1:3, and the cells in the logarithmic growth phase were used for the experiment.

[0059] 2. Determination of the safety range of drug administration (CCK8 method)

[0060] (1) Experimental method

[0061] HepG2 cells in the logarithmic growth phase were mixed with 3x10 4 Cells were seeded in a 96-well plate at 37°C, 5% CO 2 to cultivate. After the cells adhered to the wall, Cysestermerol A with a concentration gradient of 50, 25, 12.5, 6.25, 3.125, and 1.5625 μmol / L diluted with DMEM culture solution containing 10% F...

Embodiment 3

[0074] The influence of embodiment 3 Cysestermerol A on α-glucosidase inhibition

[0075] 1. Experimental method

[0076] Weigh (Na 2 HPO 4 )12H 2 0 3.58g dilute to 1000mL with distilled water as liquid A; weigh KH 2 PO 4 1.36g was made up to 1000mL with distilled water as solution B; take 49.6mL of solution A and 50.4mL of solution B, mix evenly, set the volume to 1000mL, pipette 100mL from it and then set the volume to 1000mL, adjust the pH to 6.8 to get 0.1mmol / L PB solution.

[0077] Both the substrate PNPG and α-glucosidase were dissolved in PB solution at concentrations of 20 mmol / L and 0.1 mg / ml. Take 0.5mL α-glucosidase solution and a certain amount of sample solution to be tested, supplement the buffer solution until the volume of the mixed solution is 3.5mL, mix well, incubate in a constant temperature water bath at 37°C for 10min, add 0.5mL PNPG, mix well to start the reaction, and 37°C constant temperature reaction for 30min, then add 1mol / L Na 2 CO 3 The...

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Abstract

The invention belongs to the technical field of medicines, and particularly discloses a compound Cysestermerol A and application thereof in the aspect of improving diabetes mellitus. The novel compound Cysestermerol A is extracted from Cynodon dactylon; the compound can improve the insulin resistance state of IR-HepG2 cells, promote glucose consumption of insulin resistance cells and inhibit the activity of alpha-glucosidase, so that the blood glucose level can be effectively reduced, a new choice and a new way are provided for research and development of novel blood glucose reducing drugs, and the compound has a good application prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine. More specifically, it relates to Cysestermerol A, a bermudagrass compound, and its application in improving diabetes. Background technique [0002] Diabetes mellitus is a metabolic disorder of sugar, fat and protein caused by multiple etiologies, and is a lifelong metabolic disease characterized by hyperglycemia and glycosuria. There are more than 400 million people with diabetes in the world. According to the epidemiological survey in 2014, the number of people with diabetes in China has reached 140 million. Therefore, the prevention and treatment of diabetes is imminent. [0003] At present, the drug treatment of diabetes includes oral drug therapy and insulin therapy, but these drugs often have obvious side effects. Long-term medication will cause many organ damages to patients, and some reactions are serious and even cause death. Adverse reactions include hypoglycemia, cardiovascular side ...

Claims

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Application Information

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IPC IPC(8): C07D311/94A61P3/10A61P5/50A61K31/352
CPCA61P3/10A61P5/50C07B2200/07C07D311/94
Inventor 王峰张丽李碧君鄢琼芳王淑美
Owner ENLIGHTEN-AFRICA (SHENZHEN) BIOTECHNOLOGY CO LTD
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