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Novel application of auroglaucin compounds

A compound and drug technology, which is applied in the field of new medical applications of golden gray chlorophyllin compounds, can solve problems that have not been reported, and achieve good protein tyrosine phosphatase inhibitory effect

Active Publication Date: 2014-06-18
NCPC NEW DRUG RES & DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Aspergillus aureus compounds are a class of microbial secondary metabolites derived from Aspergillus or Cystis spp.[Mycological Research, 2009, 113(4): 480-490], and their chemical structure is 6-position linkage 2,5-dihydroxy 3-isopentenyl benzaldehyde with fatty chains of different degrees of unsaturation, reported in the literature that this type of compound has antifungal, antimalarial, and anti-Leishmania [Med Chem Res, 2012, 21: 3080- 3086], antioxidation [Biosci Biotechnol Biochem, 2009, 73(6): 1323-1327; J Food Sci, 1985, 50(6): 1742-1744], good binder of human opioid receptor and cannabinoid receptor [J Nat Prod, 2011, 74, 1636-1639] and other biological activities, the activity of this type of compound in anti-diabetes and obesity has not been reported

Method used

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  • Novel application of auroglaucin compounds
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  • Novel application of auroglaucin compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Embodiment 1 The preparation of golden gray chlorophyllin compound A-D of the present invention

[0060] The slant strain of fungus F07Z1575 was inoculated on the seed medium (the mass fractions of each component were: starch 2%, glucose 1%, soybean cake powder 0.2%, malt powder 0.6%, yeast powder 0.5%, CaCO 3 0.2%, MgSO 4 ·7H 2 O 0.2%, NaCl 0.2%, pH 7.0), cultured in shake flasks at 27°C and 220rpm for 72 h, inoculated in 150 g rice medium (soaked rice for 3 days, added 2.5% hot-pressed Soybean cake powder, stirred evenly, sterilized at 120°C for 30 min) in a 1000 mL Erlenmeyer flask, and cultured at 27°C for 14 days.

[0061] The fermentation product (solid fermentation) is about 3Kg, add 6L of ethyl acetate to soak and stir, filter after 2h and evaporate the filtrate to dryness under reduced pressure to obtain 10.1g of dark brown paste.

[0062] Dissolve the ointment with chloroform and a small amount of methanol, and pass through silica gel for rough separation ...

Embodiment 2

[0068] Embodiment 2: the biological activity assay of the compound of the present invention

[0069] The protein tyrosine phosphatases PTP1B, SHP2, LAR, and MEG2 used for activity determination are all expressed in E. coli by our company using genetic engineering methods and purified by affinity chromatography.

[0070] The method for assaying the inhibitory activity of samples on protein tyrosine phosphatases PTP1B, SHP2, LAR, and MEG2 is as follows: Dilute the golden chlorophyllin compound prepared in Example 1 and add it to a 96-well plate, and add it to each well 100 μl 0.01 M NaAc-HAc pH 6.0 enzyme reaction buffer containing 0.5-2nM PTP1B, SHP2, LAR or MEG2 enzyme protein, incubated at room temperature for 15 minutes, then added 100 μl containing 5 mM disodium p-nitrophenylphosphate ( pNPP) reaction substrate 0.01 M NaAc-HAc pH6.0, 1mmol / L EDTA sodium salt buffer. The reaction was incubated at 37oC for 30 min, and 0.2 M NaOH was added to terminate the reaction, and the l...

Embodiment 3

[0080] Tablets are prepared according to methods known in the art, each containing the following ingredients:

[0081] Compound A 15mg

[0082] Lactose 180mg

[0083] Magnesium Stearate 5mg

[0084] Corn starch 50mg

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Abstract

The invention belongs to the technical field of medicinal chemistry, and in particular relates to application of auroglaucin compounds in preparation of medicaments for preventing or treating protein tyrosine phosphatases induced related diseases, especially obesity, diabetes mellitus, tumors and the like. The application provides more choices for clinical administration.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a new medical application of a golden gray chlorophyll compound. Background technique [0002] Protein-tyrosine phosphatase (Protein-tyrosine phosphatase, PTP) is a class of signaling enzymes, they control the growth, differentiation and metabolism of cells by regulating the phosphorylation level of protein tyrosine in cells; cell migration, gene transcription, Ion channel opening and closing, immune response, apoptosis, and osteogenesis are also regulated. Disorders of protein tyrosine phosphatases can lead to various diseases such as cancer, diabetes, obesity and osteoporosis [Desai, et al. 1996, Cell, 84: 599-609; Kishihara , et al. 1993, Cell , 74: 143-156; Hardy S, et al. Anticancer Agents Med Chem, 2012 Jan; 12(1): 4-18]. [0003] Protein tyrosine phosphatase is a large family, mainly divided into two types: transmembrane receptor type (such as CD4...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/11A61P3/04A61P3/10A61P35/00
Inventor 郑智慧路新华徐岩郑海洲可爱兵任晓李业英石英崔晓兰范玉玲霍培元赵峰沈文斌穆栋段宝玲
Owner NCPC NEW DRUG RES & DEV