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Compound used as anti-obesity agent

A compound and obesity technology, applied in the field of food chemistry, can solve the problems of α-glucosidase inhibition and other unknown inhibitory effects, and achieve excellent lipase inhibitory activity, inhibition of absorption, and high safety effects

Inactive Publication Date: 2016-06-08
CHONGQING NINGMU ECOLOGICAL AGRI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the lipase inhibitory action related to fat absorption, and the inhibitory action related to blood sugar level increase are not known for benzocycloheptatrienolone ring-containing compounds other than theaflavins and epitheaflavins. α-glucosidase inhibition

Method used

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  • Compound used as anti-obesity agent
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  • Compound used as anti-obesity agent

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the preparation of formula I compound

[0022] Longjing green tea leaves were extracted with hot water at 90°C, and distilled water was added to the freeze-dried product to make it 10 mg / ml, followed by heating and dissolving. While heating to 60-70° C. in a water bath, 15 ml was added to 60 ml of Sephadex LH-20 (manufactured by GE HEALTHCARE BIOSCIENCES Co., Ltd.). Wash with 20% acetone (acetone: distilled water=2:8, v / v) 45ml, then with 60ml (1 column volume), then wash with 30% acetone (acetone: distilled water=3:7, v / v), 50% acetone (acetone: distilled water = 1:1, v / v) and 60% acetone (acetone: distilled water = 6:4, v / v) were eluted with 4 column volumes each, and each column volume was separated . Extract 2 ml from each 60 ml of 14 fractions in total, and supply 0.1 ml of 50% dimethyl sulfoxide aqueous solution (dimethyl sulfoxide: distilled water = 1:1, v / v) prepared by concentration under reduced pressure to the fat Enzyme inhibitory activity a...

Embodiment 2

[0024] Embodiment 2: biological activity test

[0025] The lipase activity was measured by using fluorescent 4-methylumbelliferone oleate (4-MUO; manufactured by Sigma) as a substrate and measuring the fluorescence of 4-methylumbelliferone produced by the reaction. implement. The buffer used in the determination contains 150mM NaCl, 1.36mM CaCl 2 13mM Tris-HCl (pH8.0). 4-MUO as a substrate was diluted 4,000-fold with the above-mentioned buffer in 0.1M DMSO solution, and then used for enzyme measurement. For lipase, 400 U of porcine pancreatic lipase (manufactured by Sigma) was prepared in the same manner as in the above-mentioned buffer. / ml solution for enzyme assay.

[0026] The enzyme reaction was started by adding and mixing 50 μl of 4-MUO buffer solution and 25 μl of distilled water (or sample aqueous solution) on a 96-well microplate at 25° C., and then adding 25 μl of lipase buffer solution. After reacting for 30 minutes, 100 µl of 0.1 M citrate buffer (pH 4.2) was ...

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Abstract

The invention relates to a compound used as an anti-obesity agent, and the structure of the compound is shown as formula I in the specification. (formula I).

Description

technical field [0001] The present invention relates to the field of food chemistry, in particular, the present invention relates to compounds useful as anti-obesity. Background technique [0002] Obesity is one of the most serious diseases in modern society, the main reason of which is the excessive intake of fat. It is also known that excessive intake of fat causes not only obesity symptoms but also symptoms such as diabetes, hyperlipidemia, hypertension, and arteriosclerosis caused by obesity. Visceral fat-type obesity plus any two or more of hyperglycemia, hypertension, and lipid abnormalities is called metabolic syndrome (visceral fat syndrome), and symptoms of heart disease and stroke occur The risk is high, so it has been regarded as a problem in recent years. As a therapeutic drug for obesity, for example, Xenical (registered trademark) is commercially available as an obesity-improving drug. Xenical uses lipase inhibitory activity to inhibit fat absorption from the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/107A23F3/18A23L1/30A61K31/5415A61P3/04
Inventor 张华春
Owner CHONGQING NINGMU ECOLOGICAL AGRI