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Alpha-mangostin derivative and application thereof in preparation of metabolic syndrome resistant medicine

A technology for metabolic syndrome and mangostin, applied in the application field of treatment or prevention of metabolic syndrome, to achieve a clear effect of the drug

Inactive Publication Date: 2016-04-13
成都普瑞法科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no therapeutic drug that can effectively correct multiple clinical disorders of MS at the same time, so the development of drugs that can correct multiple disorders of MS through long-term administration has become a research hotspot in this field
At present, there is no relevant report on the use of the above-mentioned modified α-mangostin in the treatment or / and prevention of metabolic syndrome

Method used

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  • Alpha-mangostin derivative and application thereof in preparation of metabolic syndrome resistant medicine
  • Alpha-mangostin derivative and application thereof in preparation of metabolic syndrome resistant medicine
  • Alpha-mangostin derivative and application thereof in preparation of metabolic syndrome resistant medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Preparation of 3,6-diangeloyl-α-mangostin

[0029] (1) Add 2galpha-mangostin into 250mL acetonitrile, dissolve and clarify after ultrasonication, then add 3g cesium carbonate solid, the solution becomes turbid. Then add 5mL of angelic anhydride, stirring and monitoring at room temperature. After the reaction substrate has completely reacted, stop the reaction, add 150 mL of dichloromethane, and then add 150 mL of purified water to extract 3 times, combine the organic phases and concentrate.

[0030] (2) Take 1.5g of the product obtained in step (1) and add it to 150mL of absolute ethanol, heat it in a water bath at 60°C until it dissolves and becomes clear, leave it at room temperature for 8 hours to crystallize, filter and dry to obtain 1.28g of yellow needle crystals, the yield is 85.3%, and the purity is 99.6% (HPLC).

[0031] The NMR results are as follows:

[0032] 1 H-NMR (400MHzinCDCl3): 6.64 (1H, s, H-4), 7.17 (1H, s, H-5), 13.44 (1H, s, C1-OH), 3.75 (3H, s,...

Embodiment 2

[0035] Effects of 3,6-Diangeloyl-α-Mangostin on Rats with Experimental Metabolic Syndrome

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Abstract

The invention provides an alpha-mangostin derivative and application thereof in preparation of a metabolic syndrome preventing and / or treating medicine. Through experimental proof, the alpha-mangostin derivative can simultaneously improve multiple metabolic disorders factors, and can obviously improve abnormal lipids metabolism, increase insulin sensitivity and reduce blood pressure. The compound provided by the invention has obvious treatment effect for the metabolic syndromes caused by gathering of the factors such as the abnormal lipids metabolism, blood pressure abnormity, blood glucose metabolic disorder and obesity and can be used as a metabolic syndrome clinic treatment medicine for use.

Description

technical field [0001] The invention belongs to the field of natural medicinal chemistry, and relates to the structural derivatives of α-mangostin, in particular to derivatives or salts formed by introducing angelicayl groups at the 3 and 6 positions of α-mangostin, and their use in treating or preventing metabolism Syndrome applications. Background technique [0002] Metabolic syndrome (metabolicsyndrome, MS) is a group of obesity, hyperglycemia (diabetes or impaired sugar regulation), dyslipidemia (referring to hypertriglyceridemia and (or) low high-density lipoprotein cholesterol) and high Aggregation of blood pressure and other clinical syndromes that seriously affect the health of the body is a combination of a group of risk factors that are metabolically interrelated, and these factors directly promote the occurrence of atherosclerotic cardiovascular disease (cardiovascular disease, CVD). Increased risk of developing type 2 diabetes (thetype2diabetesmellitus, T2DM). ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/86A61K31/352A61P3/00A61P3/04A61P3/06A61P3/10A61P9/12
CPCC07D311/86
Inventor 谢海峰邝彬潘萌罗明锋
Owner 成都普瑞法科技开发有限公司
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