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Pharmaceutical and food composition for preventing or treating diabetes or obesity

一种糖尿病、肥胖症的技术，应用在药物组合、食品制备、食品成分等方向，能够解决降低选择性和生物学利用可能性等问题

Inactive Publication Date: 2013-08-14
KOREA OCEAN RES & DEV INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0025] However, since most protein tyrosine phosphatase-1b inhibitors were developed as non-hydrolyzable phosphotyrosine analogs targeting the active site of positively charged protein tyrosine phosphatase-1b, Reduced selectivity and biological availability (Liu, S. et al., J. Am. Chem. Soc., 130: 17075, 2008)

Method used

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  • Pharmaceutical and food composition for preventing or treating diabetes or obesity
  • Pharmaceutical and food composition for preventing or treating diabetes or obesity
  • Pharmaceutical and food composition for preventing or treating diabetes or obesity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0226] Preparation of Lobaric acid from Lichens Stereocaulon alpinum Extract

[0227] 1-1: Preparation of lichen-like alpine coral branch lichen (Stereocaulon alpinum) extract

[0228] Lichens Stereocaulon alpinum (Hedw.) G.L.Sm.) were collected from Barton Peninsula around King Sejong Station (S62°13.3', W58°47.0') on King George Island, Antarctica in January 2003, It is a lichen that is easily collected in the Barton Peninsula.

[0229] 50 g of dried alpine coral branch lichen (Stereocaulon alpinum) was extracted twice with 1 L of methanol over 24 hours to obtain 3.6 g of methanol extract. The extract obtained above was filled with silica gel (C 18 ), and add 10%, 20%, 30%, 40%, 50%, 60%, 70%, 80%, 90% and 100% (v / v) methanol (MeOH), the fractions were obtained separately.

[0230] 1-2: Preparation of Robbalic Acid from Lichen Stereocaulon alpinum Extract

[0231] The 204.6 mg fraction obtained by eluting with 80% methanol in Example 1-1 was repacked into a silica gel (...

Embodiment 2

[0238] Synthetic sodium lobarate

[0239] 2-1: Preparation of Robabaic Acid Sodium from Robabaic Acid

[0240] 10mg (22umol) of Robabaic acid obtained from Example 1-2 was dissolved in 3ml of acetone (Acetone), to which 50ul of 1M NaHCO was added 3 Stir for 1-2 minutes afterwards. For adding NaHCO 3The co-formed solid was filtered and immediately concentrated completely on a rotary evaporator. At the end of the concentration, sodium robalate (figure 1 ). The obtained sodium robalate is 100% dissolved in water, ensuring water solubility,

[0241] chemical formula 2

[0242]

[0243] Molecular formula: C 25 h 27 NaO 8

[0244] Molecular weight: 478.47

[0245] 2-2: Structural analysis of sodium robalate

[0246] The structure of sodium lobalate was confirmed by comparing the NMR data of the compound with that of lobalic acid. Dissolve each sample in DMSO-d 6 After the solvent, using a JEOL ECP-400 spectrometer (JEOL, Japan), each NMR data was measured, with DMSO-...

Embodiment 3

[0256] Analysis of protein tyrosine phosphatase-1b inhibitory activity of sodium robalate

[0257] To analyze protein tyrosine phosphatase-1b (PTP-1b) inhibitory activity, enzyme activity was measured spectroscopically.

[0258] That is, protein tyrosine phosphatase-1b (Bioneer Company, Korea) and protein tyrosine phosphatase-1b buffer (20mM Tris-HCl, pH8.0, 0.75mM sodium chloride , 0.5mM EDTA, 5mMβ-mercaptoethanol, 50% glycerol), add sodium robalate 0, 1, 3, 10, 30, 100, 300, 1000, 3000nM and matrix [pTyr1146] insulin receptor (Insulin Receptor ) (1142-1153, Sigma Company, U.S.), react at normal temperature for 10 minutes-30 minutes, then, add malachite green (Malachite Green)-molybdate dye solution (Molybdate Dye Solution) (1142-1153, Sigma Company , USA), and reacted at room temperature for 10 minutes, after finishing the reaction with protein tyrosine phosphatase-1b, sodium robalate and substrate, the absorbance was measured at 620nm.

[0259] results, such as Figure 6...

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PUM

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Abstract

The present invention relates to a pharmaceutical and food composition for preventing or treating diabetes or obesity, and more particularly, to a pharmaceutical composition and functional food for preventing or treating diabetes or obesity and which contain, as active ingredients, novel compounds synthesized from compounds separated from extracts of Stereocaulon alpinum, which is an Antarctic lichen. The novel compounds of the present invention have an excellent activity of inhibiting protein tyrosine phosphatase-1b (PTP-1b), may selectively influence only PTP-1b from among protein tyrosine phosphatases, and may be used as a substantial PTP-1b inhibitor in treating diabetes, and thus may be effectively used in preventing or treating diabetes and obesity.

Description

technical field [0001] The present invention relates to a pharmaceutical composition and a food composition for preventing or treating diabetes or obesity, and more specifically, to a compound containing as an active ingredient a compound isolated from an extract of Stereocaulon alpinum of Antarctic lichens Pharmaceutical compositions and functional foods for the prevention or treatment of diabetes or obesity of new synthetic compounds. Background technique [0002] It is known that lichens produce unique secondary metabolites different from those of higher plants (Ingolfsdottir, K., Phytochemistry, 61: 729, 2002), and most of the secondary metabolites produced by these lichens belong to depside , depsidone and dibenzfurane, it is speculated that these compounds are associated with lower growth rates of lichens (Kumar, K.C.S. et al., J. Nat. Prod., 62: 817, 1999; Huneck, S., Naturwissenschaften, 86:559, 1999). In addition, multiple biological activities of lichen metabolit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61K31/343C07D307/88A61P3/10A61P3/04
CPCA23L1/3002C07D307/89C07D307/88C07D321/10A23V2002/00C07D313/12A23L1/30A61K36/09A23V2200/3262A23V2200/332A23V2250/202A23L33/105A61P3/04A61P3/08A61P43/00A61P5/48A61P3/10
Inventor 任挺汉金一赞金德圭韩世钟李亨锡巴塔拉伊·哈里·达塔金正恩金兑勍吴贤哲赵东奎李哲顺金建锡李平天朴美罗朴洧卿金星珍康弼盛朴喜勇朴荷主
Owner KOREA OCEAN RES & DEV INST
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