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Application of thymol isobutyrate in the preparation of hypolipidemic drugs

A technology of genol isobutyrate and blood lipid-lowering drugs, which is applied in the field of blood-lipid-lowering drugs, can solve the problems of difficult-to-reversal diseases and poor long-term curative effect, and achieve high safety and good lipid-lowering effects

Active Publication Date: 2022-07-01
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current lifestyle intervention and allopathic treatment for disease symptoms have poor long-term efficacy and are difficult to reverse the development of the disease, highlighting the importance of developing new intervention strategies and prevention and treatment drugs
However, there is no report on the hypolipidemic activity of 8,9-epoxy-10-isobutoxythymol isobutyrate

Method used

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  • Application of thymol isobutyrate in the preparation of hypolipidemic drugs
  • Application of thymol isobutyrate in the preparation of hypolipidemic drugs
  • Application of thymol isobutyrate in the preparation of hypolipidemic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Preparation of 8,9-epoxy-10-isobutoxythymol isobutyrate

[0029] Prepared according to the following method:

[0030] (1) Preparation of the alcoholic extract of Xiaoheiyao: 100g of the dried rhizomes of Xiaoheiyao were pulverized by a medicinal material pulverizer (Huangcheng HC-2500Y304, Wuyi Haina Electric Co., Ltd.), passed through a 100-mesh sieve, and added at a mass volume ratio of 1:20. 95% ethanol (analytical grade, Changzhou Hengguang Chemical Reagent Co., Ltd.) was placed in an ultrasonic cleaning machine (Dongsen DS-100S, Shenzhen Pinhuang Technology Co., Ltd.) for ultrasonic extraction for 1 hour, and the supernatant was centrifuged for a rotary evaporator. (Shanghai Yarong RE-52A, Shanghai Yarong Biochemical Instrument Factory) was concentrated to dryness under reduced pressure to obtain 9.5 g of ethanolic extract of black medicine.

[0031] (2) Extract medium and low polar parts: Disperse 9.0 g of ethanol extract of Xiaohei Yao in 90 mL of dis...

Embodiment 2

[0034] Example 2: Regulation of cellular lipid metabolism (A) and oxidative stress (B) by 8,9-epoxy-10-isobutoxythymol isobutyrate

[0035] Sodium oleate and sodium palmitate (Sigma-Aldrich) with a molar ratio of 1:2 were respectively coupled with fatty acid-free bovine serum albumin (Shanghai Yisheng Biotechnology Co., Ltd.) and mixed to obtain mixed free fatty acids. 1.2 mM mixed free fatty acids were added to preadherently grown human hepatoma HepG2 cells (Cell Bank of the Type Culture Collection, Chinese Academy of Sciences) in a 6-well plate at 37°C in 5% CO. 2 The cells were cultured in a cell incubator (Forma, Thermo Scientific) for 24 h to establish a free fatty acid-induced lipid accumulation model. In the established cellular model, the oxidative stress-reducing effect of 8,9-epoxy-10-isobutoxythymol isobutyrate (XHY-1) was evaluated, and the results are shown in Tables 1 and 2. The experimental results showed that 8,9-epoxy-10-isobutoxythymol isobutyrate concentrat...

Embodiment 3

[0041] Example 3: Weight-reducing and lipid-lowering effects of 8,9-epoxy-10-isobutoxythymol isobutyrate

[0042] 40 4-week-old ICR male mice (Shanghai Slack Laboratory Animal Co., Ltd.) with an initial body weight of 30 g were randomly divided into 4 groups of 10 mice after adaptive feeding for 1 week, namely the normal group CON and the high-fat group. HFD, high-fat 8,9-epoxy-10-isobutoxythymol isobutyrate intervention group HFD+XHY-1. The CON group was given normal diet and 0.2 mL of normal saline was given daily; HFD was given high-fat diet (Jiangsu Synergy Medicine Bioengineering Co., Ltd.), and 0.2 mL of normal saline was given daily; HFD+XHY-1 A high-fat diet (Jiangsu Synergy Pharmaceutical Bioengineering Co., Ltd.) was given, and 8,9-epoxy-10-isobutoxythymol isobutyrate was administered by gavage at 20 mg / kg body weight every day. From the 5th week, the average body weight of the mice in the HFD group was 130% higher than that in the CON group, indicating that the hig...

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Abstract

The invention discloses the application of thymol isobutyrate in the preparation of blood lipid lowering drugs, and belongs to the technical field of blood lipid lowering drugs. The invention provides an application of thymol isobutyrate in the preparation of blood lipid-lowering drugs, wherein the thymol isobutyrate is 8,9-epoxy-10-isobutoxy thymol isobutyrate, With high safety and good lipid-lowering properties, it can be used in the prevention and adjuvant treatment of obesity, alcoholic fatty liver, non-alcoholic fatty liver, type 2 diabetes, metabolic syndrome, coronary heart disease, and atherosclerotic diseases. , food or functional food.

Description

technical field [0001] The invention relates to the application of thymol isobutyrate in the preparation of blood lipid lowering drugs, and belongs to the technical field of blood lipid lowering drugs. Background technique [0002] Hyperlipidemia is a systemic disease in which one or more lipids in plasma or serum are higher than the normal range due to abnormal fat transport or metabolism. Abnormal elevation is a common chronic disease. Existing studies have shown that hyperlipidemia can lead to fatty liver, liver cirrhosis, pancreatitis, fundus hemorrhage, peripheral vascular disease, hyperuricemia and other diseases. In addition, hyperlipidemia is also an important risk factor for the occurrence and development of coronary heart disease, stroke, myocardial infarction, cerebral infarction, hypertension, impaired glucose tolerance, diabetes, and atherosclerosis (McFarlane SI, Jacober S J, Winer N, et al. al.Control of cardiovascular risk factors inpatients with diabetes a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/336A61K36/28A61P3/06A61P3/04A61P1/16A61P3/10A61P3/00A61P9/10A23L33/105A23K20/111
CPCA61K31/336A61K36/28A61P3/06A61P3/04A61P1/16A61P3/10A61P3/00A61P9/10A23L33/105A23K20/111A23V2002/00A23V2200/30A23V2250/21
Inventor 成向荣董文乐赵蔚孙进乐国伟
Owner JIANGNAN UNIV
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