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Application of depside derivatives

A technology of use and medicine, applied in the field of depsidic acid derivatives, can solve the problems of flatulence, diarrhea, hypoglycemia, cardiotoxicity, etc., and achieve the effects of reducing fasting blood sugar, improving lipid metabolism, and good hypoglycemic and lipid-lowering activities

Inactive Publication Date: 2014-03-26
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

】, such as, phenformin in biguanides can cause severe lactic acidosis; α-glucosidase inhibitor acarbose can cause flatulence and diarrhea; sulfonylureas can cause hypoglycemia; insulin The sensitizer thiazolidinedione compound rosiglitazone has side effects such as edema, hepatotoxicity and cardiotoxicity

Method used

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  • Application of depside derivatives
  • Application of depside derivatives
  • Application of depside derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Take 100 grams of Baixue tea (purchased from Fuqintang, Guandu District, Kunming City, Yunnan Province), heat and reflux 3 times with 1.2 liters of absolute ethanol for 1 hour each time, filter, recover the ethanol, and obtain 14.3 grams of Baixuecha extract I powder.

[0041] Get 10 grams of white snow tea extract I and dissolve it in an appropriate amount of methanol, and through silica gel (200-300 mesh) column chromatography, CHCl 3 -CH 3 OH gradient elution gave flaky acid (compound 1, 460 mg) and choic acid (compound 2, 500 mg).

[0042] Squamatic acid (compound 1, squamatic acid): C 19 h 18 o 9 ; White powder, soluble in dimethyl sulfoxide, insoluble in methanol, ethanol. ESI-MS: m / z389.1[M-H] - ; 1 H NMR (C 5 D. 5 N,300MHz): δ7.02(1H,s,H-5′),6.55(1H,s,H-5),3.90(3H,s,OMe-4),2.81(3H,s,Me-8 '), 2.61 (3H, s, Me-8), 2.57 (3H, s, Me-9'); 13 C NMR (C 5 D. 5 N, 75MHz): 114.5(C-1), 166.9(C-2), 104.5(C-3), 162.4(C-4), 104.9(C-5), 144.0(C-6), 163.0(C -7), 21.2...

Embodiment 2

[0046] Take 100 grams of Baixue tea, heat and reflux twice with 1.0 liter of anhydrous methanol, each time for 3 hours, filter, recover methanol, and obtain 12.4 grams of Baixue tea extract II powder. The content of capric acid in the obtained Bai Xue tea extract II is 19.2wt%, and the content of flaky acid is 19.1wt%.

Embodiment 3

[0048] Take 100 grams of Baixue tea, heat and reflux twice with 1.0 liter of 50% ethanol for 1 hour each time, filter, recover methanol, and obtain 5.3 grams of Baixue tea extract III powder. The content of capric acid in the obtained Bai Xue tea extract III is 3.0wt%, and the content of flaky acid is 2.6wt%.

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Abstract

The invention provides application of compounds or pharmaceutically acceptable salts shown as the general formula I, and application of pharmaceutical compositions and plant extract products both containing the compounds or the pharmaceutically acceptable salts. The compounds or pharmaceutically acceptable salts of the general formula I, the pharmaceutical compositions and the plant extract products are capable of increasing the transcription of lipoprotein lipase in adipocyte in cell level, thereby improving lipid metabolism. Therefore, the compounds or pharmaceutically acceptable salts of the general formula I, the pharmaceutical compositions and the plant extract products are applicable to prepare medicines for treating II type diabetes and hypertriglyceridemia.

Description

technical field [0001] The present invention relates to the use of a depsipepsic acid derivative shown in general formula I, in particular to a depsipsic acid derivative shown in general formula I and a composition containing the depsipsic acid derivative in the preparation of prevention or treatment with increased Use in medicine for diseases related to the transcription of lipoprotein lipase in adipocytes. Background technique [0002] Diabetes mellitus is mainly caused by a series of metabolic disorders of sugar, protein, fat, water and electrolytes caused by the absolute deficiency of insulin secretion or the relative deficiency of insulin secretion caused by the decreased sensitivity of target tissue cells to insulin. . At present, diabetes is generally divided into two types, type 1 diabetes and type 2 diabetes, and 90% of diabetes is type 2 diabetes. Type 2 diabetes also has strong genetic and environmental factors, and shows significant heterogeneity. The pathogene...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/92C07C67/48A61K31/235A61P3/10A61P3/06
CPCC07C69/92A61K31/235C07C67/48
Inventor 胡立宏沈旭蒋华良雷敏陈静黄勇虞靓
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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