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Application of 2-acetylamino gentisic acid to preparing insulin sensitizer

A technology of acetaminogentisic acid and insulin sensitizers, which is applied in the field of preparation of insulin sensitizers, and can solve problems such as difficult drug candidate compounds

Inactive Publication Date: 2010-12-22
JINAN UNIVERSITY +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But most of them are limited to some peptides or peptide-like compounds. Although these peptide inhibitors have strong inhibitory activity and high selectivity, their own physical and chemical properties make it difficult to become drug candidate compounds

Method used

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  • Application of 2-acetylamino gentisic acid to preparing insulin sensitizer
  • Application of 2-acetylamino gentisic acid to preparing insulin sensitizer
  • Application of 2-acetylamino gentisic acid to preparing insulin sensitizer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Streptomyces deep-sea strain 220225 was isolated from the deep-sea mud of the South China Sea (13°24.987′N, 110°9.202′E) using Gaul’s medium. No characteristic sugars. The optimum NaCl concentration for growth is 1% by mass, and the highest tolerable NaCl concentration is 25% by mass. The GenBank accession number of the 16S rRNA gene sequence of the strain is FJ429837, and its sequence is:

[0029] GCGTGGGCGT GCTTACCATG CAAGTCGAAC GATGAACCAC TTCGGTGGGG ATTAGTGGCG

[0030] AACGGGTGAG TAACACGTGG GCAATCTGCC CTGCACTCTG GGACAAGCCC TGGAAACGGG

[0031] GTCTAATACC GGATACTGAT CATCTTGGGC ATCCTTGGTG ATCGAAAGCT CCGGCGGTGC

[0032] AGGATGAGCC CGCGGCCTAT CAGCTTGTTG GTGAGGTAAT GGCTCACCAA GGCGACGACG

[0033] GGTAGCCGGC CTGAGAGGGC GACCGGCCAC ACTGGGACTG AGACACGGCC CAGACTCCTA

[0034] CGGGAGGCAG CAGTGGGGAA TATTGCACAA TGGGCGAAAG CCTGATGCAG CGACGCCGCG

[0035] TGAGGGATGA CGGCCTTCGG GTTGTAAACC TCTTTCAGCA GGGAAGAAGC GAAAGTGACG

[0036] GTACCTGCAG AAGAAGCGCC GGCTAACTAC GTGCCAGCAG CCGCGGTA...

Embodiment 2

[0054] Example 2: Large-scale fermentation of bacterial strain 220225 and its fermentation product sample pretreatment method

[0055] Streptomyces deep-sea 220225 was activated on a slope, inoculated in FM3 medium, 28°C, 220r min -1 Shake culture for 3 days, inoculate into 30L FM3 medium according to 5% inoculum size, 28°C, 220r min -1 Shaking culture was carried out for 7 days to obtain the fermented product. The fermented product was concentrated under reduced pressure at 60°C to an extract, added an appropriate amount of methanol (3 L) for extraction, filtered off the extract (repeated twice), and concentrated to dryness to obtain a crude extract. The FM3 medium is composed of the following components by weight to volume: soluble starch 20g / L, yeast powder 5g / L, soybean powder 15g / L, peptone 2g / L, calcium carbonate 4g / L, sea salt 18g / L, The pH was adjusted to 7.0 (Garcia, G.D.; Romero, M.F.; Perez, B.J.; Garcia, D.T. Thiodepsipeptide isolated from a marine actinomycete W...

Embodiment 3

[0056] Embodiment 3: the separation of compound

[0057] The crude extract obtained in Example 2 is suspended with methanol aqueous solution of 90% by volume (the mass volume ratio of the crude extract and methanol aqueous solution is 10g / L), and then with equal volumes of cyclohexane, chloroform and Extract with ethyl acetate to obtain cyclohexane extract layer (A), chloroform extract layer (B), ethyl acetate extract layer (C) and water layer (D). Perform Sephadex LH-20 column chromatography on the ethyl acetate extraction layer (C), elute with chloroform / methanol with a volume ratio of 1:1, and obtain 025C-B1, 025C-B2, and 025C in the order of elution -B3, 025C-B4, 025C-B5, 025C-B6 and 025C-B7, a total of 7 fractions, 025C-B4 was subjected to Sephadex LH-20 column chromatography again, and eluted with chloroform / methanol with a volume ratio of 1:1 , to obtain compound 1.

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PUM

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Abstract

The invention discloses application of a 2-acetylamino gentisic acid compound with protein tyrosine phosphatase 1B inhibitory activity to preparing an insulin sensitizer. The 2-acetylamino gentisic acid can be used for preparing drugs for treating diabetes, obesity and complications thereof caused by insulin resistance and is obtained by fermenting and separating deep-sea streptomyces sp. 220225.

Description

technical field [0001] The invention belongs to the field of microbial medicine. It particularly relates to the use of a compound 2-acetylaminogentisic acid (2-Acetylaminogentisic acid) with protein tyrosine phosphatase 1B (PTP 1B) inhibitory activity as an insulin sensitizer. Background technique [0002] Diabetes Mellitus (DM) is a chronic disease and frequently-occurring disease characterized by chronic hyperglycemia. A series of metabolic disorders. With the continuous improvement of human living standards, the incidence of diabetes has increased year by year, and it has become the third chronic disease that seriously threatens human health after cancer and cardiovascular disease. WHO predicts that due to population aging, obesity, unhealthy diet and inactive lifestyle, the number of diabetic patients will increase from 135 million in 1995 to 300 million by 2025. Therefore, diabetes and its complications have become a worldwide public health problem that seriously thr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/196A61P3/10A61P5/50A61P3/04C12P13/02C12R1/465
Inventor 姚新生李佳洪葵唐金山高昊高立信林海鹏曾雪容盛丽庄令
Owner JINAN UNIVERSITY
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