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Furocoumarin having DPPIV enzyme inhibition activity and preparation method of furocoumarin having DPPIV enzyme inhibition activity

A technology of furanocoumarin and methyl benzofuran propionate, which is applied in the field of furanocoumarin and its preparation, to achieve good economic benefits, stable properties, and good DPPIV enzyme inhibitory activity

Active Publication Date: 2020-02-18
SERICULTURE & AGRI FOOD RES INST GUANGDONG ACAD OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no research report on the coumarin component with DPPIV enzyme inhibitory activity in yellow skin

Method used

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  • Furocoumarin having DPPIV enzyme inhibition activity and preparation method of furocoumarin having DPPIV enzyme inhibition activity
  • Furocoumarin having DPPIV enzyme inhibition activity and preparation method of furocoumarin having DPPIV enzyme inhibition activity
  • Furocoumarin having DPPIV enzyme inhibition activity and preparation method of furocoumarin having DPPIV enzyme inhibition activity

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Example 1: Preparation of furanocoumarin compound 6-β-D-glucosyl-6,7-dihydroxy-5-benzofuran propionate methyl ester

[0024] 1.1 Plant source and identification

[0025] The fruit sample of Clausena lansium (Lour.) Skeels, the plant material used for extraction, was collected from Yunan County, Guangdong Province in August 2018, and was identified by researcher Chen Hongfeng of South China Botanical Garden, Chinese Academy of Sciences.

[0026] 1.2 Extraction and separation

[0027] Homogenize the fresh seedless yellow-skinned fruit with ethanol aqueous solution with a volume fraction of 95% and extract it. The extract is concentrated under reduced pressure to remove the organic solvent to obtain a suspension. The suspension is sequentially extracted with ethyl acetate and n-butanol, and the n-butanol The alcohol extract was concentrated under reduced pressure to obtain the total extract. The total extract was subjected to normal phase silica gel column chromatography...

Embodiment 2

[0035] Example 2: Detection of DPPIV enzyme inhibitory activity of furanocoumarin compound 6-β-D-glucosyl-6,7-dihydroxy-5-benzofuran propionate methyl ester

[0036] 1. Instruments and materials

[0037] Dipeptide ground state enzyme-4 (DPPIV), sitagliptin phosphate, glycine-proline-p-nitroaniline, and dimethyl sulfoxide (DMSO) were all purchased from sigma, USA. The microplate reader was Genois microplate reader (Tecan GENios, Switzerland).

[0038] 2. Evaluation of DPPIV enzyme inhibitory activity

[0039] DPPIV was dissolved in 1 mL of 100 mM Tris buffer solution (pH=0.8), and then diluted 50 times to prepare DPPIV working solution. Both samples and sitagliptin phosphate (positive control) were dissolved in DMSO. Add different concentrations of samples and sitagliptin phosphate into a 96-well plate, then add 50 μL of DPPIV working solution, and incubate the 96-well plate in a microplate reader at 37°C for 10 minutes, and then add 50 μL to each well 1 mM glycine-proline-...

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Abstract

The invention provides furocoumarin having DPPIV enzyme inhibition activity and a preparation method of the furocoumarin having DPPIV enzyme inhibition activity. The structural formula of a furocoumarin type compound 6-beta-D-glucosyl-6,7-dihydroxy-5-benzfuran methyl propionate is as shown in a formula (I), and the furocoumarin type compound is separated from dry products or fresh products of fruits, roots, stems, branches or leaves of clausena lansium. In vitro pharmacological experiment confirms the compound 6-beta-D-glucosyl-6,7-dihydroxy-5-benzfuran methyl propionate has significant inhibition effects on DPPIV enzymes, the IC50 value of the compound 6-beta-D-glucosyl-6,7-dihydroxy-5-benzfuran methyl propionate is 117+ / -8.7[mu]M, which illustrates that the compound 6-beta-D-glucosyl-6,7-dihydroxy-5-benzfuran methyl propionate has favorable DPPIV enzyme inhibition activity. The furocoumarin type compound 6-beta-D-glucosyl-6,7-dihydroxy-5-benzfuran methyl propionate is hopeful to be used as a lead compound for developing a novel DPPIV enzyme inhibitor medicine.

Description

technical field [0001] The invention belongs to the technical field of natural medicines, and in particular relates to a furanocoumarin with DPPIV enzyme inhibitory activity and a preparation method thereof. Background technique [0002] Diabetes has developed into the third most serious chronic non-communicable disease after cardiovascular and cerebrovascular diseases and cancer, and is one of the three major killers that endanger the health of modern humans. In 2017, about 425 million people worldwide suffered from diabetes, of which 134 million were diagnosed in China. The huge patient population has brought a heavy economic burden to individuals, families and society, and the prevention and treatment of diabetes has become one of the most serious challenges facing the world. Dipeptidylpeptidase IV (Dipeptidylpeptidase IV, DPPIV) is a transmembrane serine protease that is distributed in various tissues and organs in the body, and its inhibitors can rapidly activate endog...

Claims

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Application Information

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IPC IPC(8): C07H17/04C07H1/08A61P3/10A61K31/7048
CPCA61P3/10C07H1/08C07H17/04
Inventor 贾栩超张名位张瑞芬刘磊池建伟黄菲董丽红马勤
Owner SERICULTURE & AGRI FOOD RES INST GUANGDONG ACAD OF AGRI SCI
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