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Prenylflavonoid compound and application thereof in preparation of pancrelipase inhibitor

A technology of prenyl flavonoids and compounds, applied in organic chemistry, drug combinations, medical preparations containing active ingredients, etc., can solve problems such as difficult to control intestinal symptoms

Inactive Publication Date: 2012-11-28
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the best-selling pancreatic lipase inhibitor in the market is Xenical, which has the advantages of strong activity and good stability, but it also has the disadvantages of difficult-to-control intestinal symptoms, greasy stools, vomiting and abdominal distention.

Method used

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  • Prenylflavonoid compound and application thereof in preparation of pancrelipase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Extract and isolate the compound of the present invention from laurel wood

[0021] (1) Extraction: After 20 kg of dried stems and branches of Artocarpus hypargyreus Hance were crushed, they were extracted by percolation with 20 times the amount of 95% ethanol, the leachate was collected, concentrated and dried to obtain 1.63 kg of extract, which was dissolved in After extracting with chloroform, the recovered solvent was concentrated to dryness to obtain 214 g of chloroform extract;

[0022] (2) Separation: 50 g of chloroform extract was subjected to silica gel column chromatography, and gradient elution was carried out with petroleum ether-acetone (10:1→6:1→3:1→1:1), and the amount of each gradient was 5000 ml. Fractions were collected; the petroleum ether-acetone 1:1 fraction was subjected to silica gel column chromatography, and eluted with chloroform-acetone 4:1 (amount of 1000 ml) to obtain the compound 5-methoxy-2,2-dimethyl -9-(3-methyl-2-butenyl)-8...

Embodiment 2

[0025] Example 2 Determination of inhibitory activity of compound (I) of the present invention on pancreatic lipase

[0026]Firstly, the substrate p-Nitrophenyl acetate (Sigma Company) was formulated with phosphate buffer solution (PBS, pH 7.4) to 1.35 M; porcine pancreatic lipase (Sigma Company) was formulated with phosphate buffer solution to 10 mg / ml; compound (I) was formulated with Phosphate buffer solution was prepared into solutions of different concentrations, and then 50 μl of enzyme solution diluted 20 times, 40 μl of substrate solution diluted 1000 times, and 10 μl of test samples of different concentrations were sequentially added to a 96-well plate, and mixed Evenly, react at 25°C for 20 minutes, and detect the absorbance of each well at 405 nm every 2 minutes;

[0027] According to the absorbance at 405 nm, the inhibitory rate (%) of the test sample to pancreatic lipase was calculated, and distilled water was used as a control, and the concentration of the inhi...

Embodiment 3

[0036] Example 3 Preparation of tablets containing the compound of the present invention (I)

[0037] Grind 20 g of compound (I) and 69 g of lactose, sieve, mix evenly, moisten with water to make a soft material, pass through a 20-mesh sieve to make wet granules, dry at 80°C, sieve the granules with a 20-mesh sieve, add starch 10 g and 1 g of magnesium stearate, fully mixed and compressed into tablets, each tablet weighs 100 mg, and the active ingredient content is 20 mg.

[0038]

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PUM

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Abstract

The invention belongs to the technical field of medicine, and relates to a prenylflavonoid compound separated from artocarpus hypargyreus hance and having a structure of a formula (I) and application thereof. Pancrelipase inhibiting activity experiment results show that the compound has obvious pancrelipase inhibiting activity. The compound can be used as a pilot compound for preparing new medicaments for preventing or treating obesity and related metabolic diseases, and can also be used for preparing medicaments for preventing or treating clinically common obesity and related metabolic diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a prenyl flavonoid compound, in particular to a prenyl flavonoid compound isolated from laurel wood and its application in the preparation of pancreatic lipase inhibitors. Background technique [0002] Over the past 20 years, the incidence of obesity has been increasing all over the world, especially in developed countries. Due to the rapid development of the economy and the continuous improvement of living standards, the problems of insufficient exercise and relative excess energy intake have always existed in the lifestyle of modern people, which has led to the energy intake of many modern people exceeding energy consumption, and the excess energy will be Part of it is stored as fat in adipose tissue, and its accumulation will lead to obesity and related diseases, such as diabetes, cancer, heart disease, hyperlipidemia and fatty liver. [0003] Currently, one of the main approac...

Claims

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Application Information

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IPC IPC(8): C07D493/04A61K31/352A61P3/04
Inventor 侯爱君王贺瑶雷春赵婷闫桂蕊俞媚华
Owner FUDAN UNIV
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