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Application of isopentene group flavonoid compound used as pancreatic lipase inhibitor

A technology of pancreatic lipase and compounds, applied in the field of prenyl flavone compounds as pancreatic lipase inhibitors, can solve problems such as difficult to control intestinal symptoms

Inactive Publication Date: 2011-08-24
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, the best-selling pancrelipase inhibitor in the market is Xenical, which has the characteristics of strong activity and good stability, but at the same time has the disadvantages of difficult-to-control intestinal symptoms, greasy stools, vomiting and abdominal distention.

Method used

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  • Application of isopentene group flavonoid compound used as pancreatic lipase inhibitor
  • Application of isopentene group flavonoid compound used as pancreatic lipase inhibitor
  • Application of isopentene group flavonoid compound used as pancreatic lipase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1 Extracting compound (E)-2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-3-(3-methyl-2-butenyl)-6 from Osmanthus glabra -(3-Methyl-1-butenyl)-4H-benzopyran-4-one

[0013] (1) Extraction: after 20 kilograms of dried osmanthus laurel leaves are powdered, soak 12 hours with 100 liters of 95% aqueous ethanol and then percolate, add 95% aqueous ethanol after soaking, collect 400 liters of percolate, concentrate and dry to obtain Extract 1.5 kg. The extract was dissolved in water and extracted with chloroform, and the recovered solvent was concentrated to dryness to obtain 50 g of chloroform extract.

[0014] (2) Separation: 10 g of the chloroform extract was subjected to silica gel column chromatography, and gradient elution with petroleum ether-acetone (10:1 → 7:1 → 4:1 → 2:1) was performed, and the amount of each gradient was 1500 ml. The eluents were collected; the petroleum ether-acetone 4:1 eluate was concentrated and then subjected to silica gel column chromatography,...

Embodiment 2

[0022] The compound of embodiment 2 structural formula (I) measures the inhibitory activity of pancreatic lipase

[0023] The assay method of pancreatic lipase inhibitory activity is as follows:

[0024] First, the substrate p-nitrophenyl acetate (p-Nitrophenyl acetate) (sigma company) was made into 1.35M with phosphate buffer solution (PBS, pH 7.4); porcine pancreatic lipase (sigma company) was prepared with phosphate buffer solution (PBS, pH 7.4). 7.4) Prepared to 10 mg / ml; the compound of structural formula (I) was prepared into solutions of different concentrations with phosphate buffer solution (PBS, pH7.4). Then, 50 μl of 20-fold diluted enzyme solution, 40 μl of 1000-fold diluted substrate solution, and 10 μl of test samples of different concentrations were sequentially added to the 96-well plate, and mixed. React at 25°C for 20 minutes, and detect the absorbance of each well at 405 nm every 2 minutes.

[0025] According to the absorbance at 405nm, the activity inhibi...

Embodiment 3

[0032] Embodiment 3: the compound of structural formula (I) is to the weight loss effect of Zucker obese rat

[0033] Zucker obese rats (genetically obese rats) were bred by the animal room of Shanghai Institute of Materia Medica, Chinese Academy of Sciences, male, 6 weeks old. Six normal Zucker rats were used as the blank control group. The obese Zucker rats were divided into two groups, namely the model control group and the administration group, with 6 rats in each group. The compound of structural formula (I) was dissolved with 0.5% CMC-Na at a dose of 120 mg / kg; the blank and model control groups were given the same volume of 0.5% CMC-Na, and were administered orally orally for two weeks. Monitor diet and weight regularly.

[0034] Results: See Table 1.

[0035] The impact of the compound of table 1 structural formula (I) on Zucker rat body weight and diet

[0036]

[0037] Compared with the model group, * P<0.05.

[0038] As can be seen from Table 1, the compoun...

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Abstract

The invention belongs to the technical field of medicaments, and in particular relates to application of isopentene group flavonoid compound used as a pancreatic lipase inhibitor. The flavonoid compound has the following structural formula and has a chemical name of: (E)-2-(2,4-dihydroxy phenyl)-5,7-dihydroxy-3-(3-methyl-2-butenyl)-6-(3-methy-l-butenyl)-4H-chromene-4-ketone, and can be extracted from artocarpus nitidus. Pancreatic lipase activity tests and experiments of weight loss action in animals prove that the compound has obvious pancreatic lipase inhibitory activity and weight loss action, can be taken as the lead compound for developing novel medicaments for preventing or curing obesity and related metabolic diseases, and also can be used for preparing the medicaments for preventing and curing clinically common multiple obesity and the related metabolic disease.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically, the invention relates to the use of a prenyl flavonoid compound isolated from laurel wood as a pancreatic lipase inhibitor. Background technique [0002] In 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 can lead to obesity and related diseases, such as diabetes, cancer, heart disease, hyperlipidemia, and fatty liver. [0003] Currently, the treatment of obesity consists mainly in the development of d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P43/00A61P3/04
Inventor 王贺瑶侯爱君朱维良闫桂蕊赵婷
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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