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Cyclopeptide compound and preparation method and application thereof

A compound and cyclic peptide technology, applied in the field of cyclic peptide compounds and their preparation and application, can solve the problems of unseen drugs and the like, and achieve the effects of short reproduction cycle, low cost and simple purification process

Active Publication Date: 2017-09-08
NINGBO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The study found that the cyclic peptide compound shown has α-glucosidase inhibitory activity, and the chemical structure of the compound and the report as an α-glucosidase inhibitor have not yet been seen, so there is no related drug on the market

Method used

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  • Cyclopeptide compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] A cyclic peptide compound, its structural characteristics are: a cyclic tetrapeptide compound composed of 1 leucine residue, 2 N-methyl leucine residues and a phenylalanine residue, the structural formula is shown in I :

[0026] (I).

Embodiment 2

[0028] The preparation method of the cyclic peptide compound shown in I formula specifically comprises the following steps:

[0029] (1) Fermentation production and extraction of extract

[0030] The preservation number is CCTCC No: M2014098 Cladosporium ( Cladosporium sphaerospermum YS3-1-5) colonies were inoculated into 300mL liquid medium (mannitol 10.0g, yeast extract 3.0g, maltose 20.0g, monosodium glutamate 10.0g, glucose 20.0g, KH2PO4 0.5g, MgSO4 0.3g and seawater 1L) In a 1L Erlenmeyer flask (100 flasks in total), culture at 28°C and 180 r / min on a shaker for 10 days to obtain a fermentation broth, which was extracted with ethyl acetate three times, and the combined ethyl acetate extracts were concentrated under reduced pressure and evaporated to dryness , to obtain crude extract (a total of 100 bottles to obtain 20g crude extract);

[0031] (2) Separation and refining

[0032] Dissolve the above crude extract (20g) in a mixed solvent of dichloromethane and methanol...

Embodiment 3

[0038] α-glucosidase inhibitory activity test (96-well plate method)

[0039] (1) Experimental samples

[0040] Preparation of test sample solution: The test sample is the pure compound I isolated and purified in Example 1 above, and an appropriate amount of sample is accurately weighed to prepare a solution with a required concentration for testing the activity.

[0041] (2) Experimental method

[0042] 4-Nitrophenyl-α-D-glucopyranoside was used as the substrate, reacted on a 96-well microtiter plate, and the final reaction volume was 200 μL, and the α-glucosidase inhibitory activity was determined. Add different concentrations of sample solutions (40 μL) to 40 μL 0.04 U / mL α-glucosidase solution, react at 37°C for 5 minutes, add 20 μL 0.5 mmol / L 4-nitrophenyl-α-D-glucopyranose Glycoside solution, after reacting at 37°C for 30min, add 100μL 0.1mol / L Na 2 CO 3 The solution terminates the reaction, and the absorbance of the solution is measured at a wavelength of 405nm. Ac...

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Abstract

The invention discloses a cyclopeptide compound and a preparation method and application thereof. The cyclopeptide compound is characterized in that the structural formula is as shown in I. The preparation method comprises the following steps: fermental cultivation is performed on Cladosporium sphaerospermum, then the obtained fermentation product is extracted by use of ethyl acetate to obtain a crude extract, and the crude extract is subjected to reduced-pressure silica gel column chromatography, Sephadex LH-20 gel column chromatography and reversed-phase preparative high performance liquid chromatography separation and purification to obtain the cyclopeptide compound. The cyclopeptide compound has the alpha-glucosidase inhibition function, and also has the advantage that the cyclopeptide compound can serve as a drug lead compound for treating diabetes and obesity when combined with various pharmaceutically acceptable carriers, excipients or auxiliary materials. The preparation method is low in cost, short in reproductive cycle and simple in purification process.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a cyclic peptide compound and its preparation and application. Background technique [0002] Diabetes has become the third major threat to human health after cardiovascular disease and tumors. Type 2 diabetes is caused by decreased sensitivity of target cells to insulin, resulting in high postprandial blood glucose levels. α-glucosidase inhibitors are currently the first-line oral hypoglycemic drugs (such as acarbose, voglibose, and miglitol) for the clinical treatment of type 2 diabetes, which reversibly inhibit the growth of the mesenteric brush border. α-glucosidase, delaying the decomposition of polysaccharides into glucose by α-glucosidase, thereby slowing down the absorption rate of glucose, thereby reducing postprandial blood sugar. [0003] Marine natural products are an important source of drug development, and finding new α-glucosidase inhibitors from them is of great signi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/12C12P21/04A61K38/07A61K38/12A61P3/04A61P3/10C12R1/645
CPCA61K38/00C07K5/126C12P21/02
Inventor 孙晴镁丁立建何山姚佳晓斯拉瓦·爱泼斯坦
Owner NINGBO UNIV
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