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Geldanamycin biosynthetic analog 19-O-glycyl geldana

A technology of glycylgeldanamycin and geldanamycin, applied in the field of biosynthetic analogues of geldanamycin, can solve the problem of 19-O-glycylgeldanamycin, etc. question

Inactive Publication Date: 2010-08-04
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] So far, there have been no reports on the discovery and acquisition of 19-O-glycylgeldanamycin (Gdm-CT-1-3) from Gdm-producing bacteria at home and abroad

Method used

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  • Geldanamycin biosynthetic analog 19-O-glycyl geldana
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  • Geldanamycin biosynthetic analog 19-O-glycyl geldana

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Fermentation of Streptomyces hygroscopicus 17997

[0032] Get fresh Streptomyces hygroscopicus 17997 slant (medium composition: yeast extract 0.4%, malt extract 1.0%, glucose 0.4%, agar powder 1.5%), dig a piece and inoculate in liquid seed medium (glucose 0.5%, yeast extract 0.4% corn syrup, 0.5% corn syrup, 0.25% cottonseed meal, KH 2 PO 4 0.05%, MgSO 4 0.05%, CaCO 3 0.3%), shake (100-300r / min) at 28°C, and cultivate for 24-48h; 5%-20% of the transfer amount is inoculated in the liquid fermentation medium (starch 2%, cottonseed cake powder 0.5%, glucose 0.5%) , corn steep liquor 1.0%, yeast powder 0.5%, CaCO 3 0.2%) at 28°C and continue shaking culture until 80-120h, centrifuge the obtained fermentation broth, discard the bacterial cells, and keep the supernatant for detection and separation of Gdm-CT-1-3.

Embodiment 2

[0033] Detection of Gdm-CT-1-3 in Streptomyces hygroscopicus 17997 fermentation culture

[0034] The supernatant obtained in Example 1 was extracted with an equal volume of ethyl acetate, dissolved in a certain volume of ethyl acetate, spotted on a TLC silica gel plate, and mixed in ethyl acetate: dichloromethane: n-hexane: methanol (9 : 6: 6: 2.5) in the solvent system; spraying with a small amount of NaOH (2.0mol / L) solution, a line R can be observed on the silica gel platef The brown band with a value of 0.1 is Gdm-CT-1-3.

Embodiment 3

[0035] Separation, purification and preparation of Gdm-CT-1-3

[0036] The fermentation supernatant obtained in Example 1 was extracted with an equal volume of ethyl acetate, concentrated by rotary evaporation, and then applied to a silica gel column, and the gradient was carried out with petroleum ether:ethyl acetate (the volume ratio of the two was 10:0 to 10:90). For elution, the eluate was collected in parts, and after being detected by TLC silica gel plate, the part containing Gdm-CT-1-3 was combined, concentrated by rotary evaporation, and separated by Sephadex LH-20 column chromatography, and the elution solvent was methanol. The eluate was collected in parts, and after being detected by TLC silica gel plate, the parts containing Gdm-CT-1-3 were combined, concentrated by rotary evaporation, and then reversed-phase HPLC (ODS-C18 column, 150mm×20mm, mobile phase was methanol: Water (14:11), the flow rate was 2-5ml / min, the eluate containing Gdm-CT-1-3 was collected and c...

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Abstract

The invention relates to the discrimination and a preparation method of a geldanamycin biosynthetic analog which obtains 19-O-glycyl geldanamycin (Gdm-CT-1-3 for short) from streptomyces strains 17997 generated by geldanamycin. Proved by experiment research, the analog has the antiviral activity, and the water solubility and the light stability of the analog are obviously superior to those of the geldanamycin so that the analog is prospectively used for researching clinically effective antiviral medicines.

Description

Technical field: [0001] The invention relates to the identification and preparation method of geldanamycin biosynthetic analogs. Background technique: [0002] Streptomyces hygrocopicus 17997 (Streptomyces hygrocopicus 17997) is a geldanamycin (Gdm) producing bacterium isolated from Chinese soil by the Institute of Pharmaceutical Biotechnology, Chinese Academy of Medical Sciences. Gdm has various biological activities such as antiprotozoal, antitumor, antiviral and immunosuppressive [Sasaki K et al.J Antibiot (Tokyo), 1979, 32(8): 849-51]; [Tao Peizhen et al., Chinese Journal of Antibiotics , 1997, 22: 368-372]. [0003] The specific action target of Gdm is human heat shock protein 90 (heat shock protein90, Hsp90), and Hsp90 is a chaperone molecule of many signaling proteins. Gdm can indirectly affect the function of signaling proteins in human cells by inhibiting Hsp90, so it is expected to become a potential antitumor and antiviral drug. However, Gdm has disadvantages s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D225/06C12P17/10A61K31/395A61P31/12A61P31/22C12R1/55
Inventor 武临专王以光倪四阳王红远赫卫清王玉成
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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