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Preparation of dianthrone compound and application of dianthrone compound in prevention and treatment of insulin resistance related metabolic diseases such as diabetic hyperlipemia

A technology of dianthrone and compounds, applied in the fields of metabolic diseases, separation/purification of carbonyl compounds, preparation of sugar derivatives, etc., can solve problems such as rosiglitazone heart attack hidden danger, weight gain, etc.

Pending Publication Date: 2022-04-22
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main side effects of this type of drug are edema and weight gain. Rosiglitazone has been withdrawn from the market or restricted in use due to the risk of heart attack

Method used

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  • Preparation of dianthrone compound and application of dianthrone compound in prevention and treatment of insulin resistance related metabolic diseases such as diabetic hyperlipemia
  • Preparation of dianthrone compound and application of dianthrone compound in prevention and treatment of insulin resistance related metabolic diseases such as diabetic hyperlipemia
  • Preparation of dianthrone compound and application of dianthrone compound in prevention and treatment of insulin resistance related metabolic diseases such as diabetic hyperlipemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Take Polygonum multiflorum Thunb. (Polygonum multiflorum Thunb.) dry root tuber 2kg, pulverize, heat and reflux with 70% ethanol to extract three times, combine the extracts, recover the solvent under reduced pressure, and obtain the 70% ethanol extract. 70% ethanol extract, dissolved in water, separated by macroporous adsorption resin (DM-8 type), and eluted with water, 20% ethanol, 40% ethanol and 95% ethanol in sequence to obtain four different components, which are group Divided into A, B, C and D. Component D, through YMC C 18 Reverse-phase silica gel and Sephadex LH-20 gel chromatographic column, separated and purified to obtain 13 known dianthrone compounds, respectively compounds 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 and 13.

[0049]

[0050]

[0051]

[0052] Compound 1: Cis-emodin-emodin dianthrone, light yellow solid, ESI-MS m / z 509.12[M-H] - ; 1 H-NMR (400MHz, CD 3 COCD 3 )δ H :11.99(OH-8,8′); 11.87(OH-1,1′); 9.62(OH-6, 6′); 6.69(2H,s,H-2,2′)...

Embodiment 2

[0072] Take 2 kg of dried cane of Polygonum multiflorum Thunb., crush it, extract it under reflux with 70% ethanol for three times, combine the extracts, recover the solvent under reduced pressure, and obtain the 70% ethanol extract. 70% ethanol extract, dissolved in water, separated by macroporous adsorption resin (DM-8 type), eluted with water, 20% ethanol, 40% ethanol and 95% ethanol in turn to obtain four different components, which are washed with water respectively Eluted fraction (fraction A1), 20% ethanol eluted fraction (fraction B1), 40% ethanol eluted fraction (fraction C1) and 95% ethanol eluted fraction (fraction D1). 95% ethanol elution part (component D1), through YMC C 18 Reverse-phase silica gel and Sephadex LH-20 gel chromatography column, separation and purification, to obtain 13 known dianthrone compounds, respectively Cis-emodin-emodin dianthrone (1), Trans-emodin-emodin Dianthrone(2), Polygonumnolide C1(3), Polygonumnolide C2(4), Polygonumnolide C3(5), P...

experiment example 1

[0074] Experimental example 1: Inhibitory effect of dianthrone compounds on recombinant human PTP1B

[0075] method:

[0076] The recombinant human protein tyrosine phosphatase 1B (PTP1B) engineering bacteria were prepared by using BL21 E. coli E. coli, and the protein was purified by GST affinity chromatography to obtain the PTP1B protein. Using nitrophosphate as a substrate, carry out the enzymatic reaction of PTP1B, and observe the effect of drugs on the activity of PTP1B protein.

[0077] result:

[0078] The results show that the dianthrone compounds such as compounds 1, 2, 3, and 4 have the activity of obviously inhibiting the human PTP1B of gene recombination, the inhibitory rate of PTP1B and the concentration (IC 50 ) see Table 1.

[0079] Table 1. Inhibitory effect of dianthrone compounds on PTP1B activity (n=3)

[0080]

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PUM

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Abstract

The invention belongs to the technical field of medicines, relates to application of a dianthrone compound in preparation of a medicine for treating diabetes or hyperlipidemia, and particularly discloses application of the dianthrone compound shown in a general formula (I) and pharmaceutically acceptable salt thereof in preparation of a human protein tyrosine phosphatase 1B inhibitor. Application in preparation of drugs for preventing and / or treating diabetes mellitus and related metabolic diseases thereof; the invention also relates to an application in preparation of drugs for preventing and / or treating hyperlipemia and related metabolic diseases. The dianthrone compound is extracted and separated from plants (including polygonum multiflorum), and can be used for preparing medicines for treating and preventing insulin resistance related metabolic diseases such as diabetes mellitus, hyperlipidemia and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the extraction of dianthrone compounds capable of increasing insulin sensitivity from Polygonum genus Fallopia, and the preparation method of the dianthrone compounds, which contains Polygonum multiflorum (Polygonum multiflorum Thunb) or the The pharmaceutical composition belonging to the dianthrone compound, and Polygonum multiflorum Thunb. or the use of the dianthrone compound and its pharmaceutical composition as medicines, especially for the preparation of treatment and prevention of diabetes, hyperlipidemia Drugs and health products for insulin resistance-related metabolic diseases such as hyperemia and their complications. Background technique [0002] Insulin resistance refers to the reduced sensitivity and (or) responsiveness of the body to insulin, which is the main pathophysiological basis of metabolic syndrome, and is related to impaired glucose tolerance, type 2 diabet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K31/122A61P3/10A61P3/00A61P3/06C07C45/78C07C45/79C07C49/747C07C49/755C07H15/244C07H1/08
CPCA61K31/704A61K31/122A61P3/10A61P3/00A61P3/06C07C45/78C07C45/79C07C49/747C07C49/755C07H15/244C07H1/08C07C2603/24
Inventor 杨建波叶菲田金英马双成张晓琳魏锋李雪晨蔡伟尹震马生军姜楠高博闻宋云飞高慧宇刘越汪褀王莹程显隆
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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