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Benzotroponoid compounds and preparation method and applications thereof

A technology of pharmaceutical preparations and compounds, applied in the field of benzotropolone analogues and its preparation, can solve problems such as long-term medication, easy rebound, safety concerns and heated discussions

Inactive Publication Date: 2019-03-05
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the clinical first-line drugs for lowering blood lipids are mainly statins, which have definite curative effect and quick onset, but have the disadvantages of easy rebound, high recurrence rate, and the need for long-term medication.
In 2001, cerivastatin was withdrawn from the market due to serious adverse reactions caused by rhabdomyolysis and death, which also aroused concerns and heated discussions about the safety of other statins

Method used

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  • Benzotroponoid compounds and preparation method and applications thereof
  • Benzotroponoid compounds and preparation method and applications thereof
  • Benzotroponoid compounds and preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 Preparation of compound 1

[0047]

[0048] Take respectively 50 g of epigallocatechin gallate and rutin, dissolve in 10 L of citric acid-sodium hydrogen phosphate buffer (substrate concentration 1%) with a pH of 4.0, add a certain amount of apple polyphenols Oxidase (addition amount is 1.5g / L), oxygen flow rate is 10L / min, stir and react at 80rpm at 25°C for 1.5 hours, after the reaction is over, stop feeding oxygen, and heat to rapidly increase the temperature to 100°C to make the polyphenol Oxidase inactivation, hold for 5 minutes.

[0049] The resulting reaction solution was subjected to polyamide resin column chromatography, the diameter-to-height ratio of the column chromatography was 1:10, the sample volume to column bed volume ratio was 1:4, and the sample loading flow rate was 2 BV / h, followed by water and 5% ethanol aqueous solution , 95% ethanol aqueous solution for elution, collect the eluted part of 95% ethanol, concentrate and dry under reduc...

Embodiment 2

[0054] Example 2 Preparation of Compound 2

[0055]

[0056] Weigh respectively 60 g of epigallocatechin and rutin, dissolve in 10 L of citric acid-disodium hydrogen phosphate buffer (substrate concentration 1.2%) with a pH of 4.5, add a certain amount of blueberry polyphenol oxidase ( The addition amount is 1.5g / L), the ventilation rate is 12L / min, and the reaction is stirred at 80rpm at 25°C for 2 hours. live, hold for 5 minutes.

[0057] The resulting reaction solution was subjected to polyamide resin column chromatography, the diameter-to-height ratio of the column chromatography was 1:10, the ratio of sample volume to column bed volume was 1:4, and the sample loading flow rate was 2 BV / h, followed by water and 5% ethanol aqueous solution , 95% ethanol aqueous solution for elution, collect the eluted part of 95% ethanol, concentrate and dry under reduced pressure at 40°C to obtain a crude extract, use BUCHI medium pressure preparation for further separation and purif...

Embodiment 3

[0059] Example 3 Preparation of compound 3

[0060]

[0061] Weigh 75g each of epigallocatechin gallate and isoquercitrin, dissolve them in 10L of citric acid-sodium hydrogen phosphate buffer (substrate concentration 1.5%) with a pH of 5.0, add a certain amount of apple Polyphenol oxidase (addition amount is 2.0g / L), ventilation rate is 14L / min, under 30 ℃ 120rpm stirring reaction for 2 hours, after the reaction is finished, stop feeding oxygen, heat up the temperature rapidly to 100 ℃ to make polyphenol oxidase Inactivate phenoloxidase by holding for 5 minutes.

[0062] The resulting reaction solution was subjected to polyamide resin column chromatography, the diameter-to-height ratio of the column chromatography was 1:10, the ratio of sample volume to column bed volume was 1:4, and the sample loading flow rate was 2 BV / h, followed by water and 5% ethanol aqueous solution , 95% ethanol aqueous solution for elution, collect the eluted part of 95% ethanol, concentrate and...

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Abstract

The invention belongs to the field of drugs or health care products, and specifically relates to benzotroponoid compounds and a preparation method and applications thereof. The structure of the benzotroponoid compounds is represented in the description. Compared with theaflavin, theaflavin-3-gallate, theaflavin-3'-gallate, and theaflavin-3,3'-digallate, the provided benzotroponoid compounds have abetter effect on inhibiting the weight gain of mice and reducing the blood fat, and have a better curative effect on the non-alcoholic fatty liver disease.

Description

technical field [0001] The invention belongs to the field of medicines or health care products, and in particular relates to benzotropolone analogues and their preparation methods and applications. Background technique [0002] Obesity is a chronic metabolic disease caused by a variety of factors, characterized by an increase in the volume and number of fat cells in the body, resulting in an abnormally high percentage of body fat as a percentage of body weight, and excessive fat deposition in some areas. A large number of studies have shown that obesity can cause many chronic diseases such as hypertension, diabetes, and coronary heart disease, and has become a serious global public health problem. According to statistics, in 2015, the number of obese children and adults in the world was 107.7 million and 603.7 million respectively. In the same year, about 4 million people died directly related to high BMI, accounting for 7.1% of all deaths. [0003] The current weight-loss ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/07C07D311/58A61K31/7048A61K31/353A61P3/04A61P3/06A61P1/16C12P17/16
CPCA23L29/06A23L33/10A23V2002/00C07D311/58C07H17/07C12P17/162A23V2200/3324A23V2200/326A23V2200/30
Inventor 温尧林
Owner CATCH BIO SCI & TECH