Compound in cyclocarya paliurus and application thereof in medicament field

A kind of compound, the technology of pennywort, the compound applied in pennywort and its application field in the field of medicine

Inactive Publication Date: 2009-11-04
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there is no report on the anti-diabetic...

Method used

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  • Compound in cyclocarya paliurus and application thereof in medicament field
  • Compound in cyclocarya paliurus and application thereof in medicament field
  • Compound in cyclocarya paliurus and application thereof in medicament field

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The following examples further describe the separation and preparation of (1R,2R,4R)-1,2,4-trihydroxy-1,2,3,4-tetrahydro-naphthalene-1-O-β-D-glucopyranoside.

[0027] Select 10Kg of dry leaves of Cyclocarya paliurus growing in the provinces and regions south of the Yangtze River Basin in China, use 15 times the amount (weight) of 70% ethanol to reflux and extract 3 times, filter the extract, reclaim the ethanol under reduced pressure to no alcohol smell, and then The concentrated solution is filtered and divided into two parts, the precipitate and the filtrate. After the filtrate is extracted with petroleum ether (10L), it is concentrated, filtered, passed through a Diaion HP20 macroporous adsorption resin column, washed with water and 10% ethanol in turn, and the 10% ethanol eluate is collected. , The solvent was recovered under reduced pressure to obtain 80 g of extract. Take the extract, filter, concentrate, pass through MCI gel CHP20P column, rinse with water, 10%, ...

Embodiment 2

[0028] Example 2. Protein tyrosine phosphatase 1B (PTP1B) inhibition experiment

[0029] Purpose of the experiment: Insulin resistance is the most important pathological basis of type II diabetes, and a large number of studies have shown that PTP1B is a key negative regulator of the insulin signaling pathway. In animal models, abolishing or reducing PTP1B levels can sufficiently increase insulin signaling, reverse insulin resistance, and improve insulin sensitivity. Therefore, highly active PTP1B inhibitors have important value in the treatment of diabetes and obesity. The inhibitory effect of the new compound in Cyclocarya paliurana prepared in Example 1 on PTP1B was detected.

[0030] Experimental method: The protein tyrosine phosphatase PTP1B used for screening is a GST fusion protein expressed and purified from Escherichia coli. The ultraviolet substrate pNPP was used to observe the inhibition of 1,2,4-trihydroxy-1,2,3,4-tetrahydro-naphthalene-1-O-β-D-glucopyranoside on ...

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Abstract

The invention relates to the technical field of medicaments, and in particular discloses a novel compound which is separated from cyclocarya paliurus and is used for treating diabetes and adiposis. Through various modern spectral analyses, particularly by applying various comprehensive analysis and X-diffraction analysis of advanced two-dimensional NMR spectrums, the chemical structure and the spatial configuration of the compound is defined, and the chemical structural formula of the compound is a formula (1). A protein tyrosine phosphatase 1B (PTP1B) inhibition experiment shows that the compound has remarkable PTP1B inhibitory effect. The compound can provide a lead compound for developing a novel medicament or a heath product for reducing glycemia and treating the adiposis, and has important values in developing and using Chinese herbal medicament resources.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular to the use of a traditional Chinese medicine extract, i.e. Cyclocarya paliurus extract, for the preparation and treatment of diabetes, and in particular to a traditional Chinese herbal medicine Cyclocarya paliurus isolated from leaves Use of the novel compound (1R, 2R, 4R)-1,2,4-trihydroxy-1,2,3,4-tetrahydro-naphthalene-1-O-β-D-glucopyranoside for the preparation of antidiabetic products. Background technique [0002] (1) Research overview of Cyclocarya paliurus [0003] Cyclocarya paliulus leaves are the leaves of Cyclocarya paliulus (Batalin.) Iijinsk, a deciduous tree of the Juglandaceae Cyclocarya genus. There is only one plant of the genus Cyclocarya in the family Juglandaceae, namely Cyclocarya, which is distributed in the provinces and regions south of the Yangtze River Basin in my country, and Guangdong is only distributed in the northern region (Chen Fenghuai. Vol...

Claims

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Application Information

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IPC IPC(8): C07H15/203C07H1/08A61K31/704A61P3/10A61P3/04A23L1/29A23L33/00
Inventor 肖凯李佳张娟沈强张薇孙铭学
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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