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Uridine peptide antibiotic, pharmaceutically acceptable salt, producing method and uses thereof

A technology for uridine peptides and antibiotics, applied in the field of uridine peptide antibiotics and their pharmaceutically acceptable salts, capable of solving the problems of low toxicity

Inactive Publication Date: 2008-04-02
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

[0002] At present, uridine peptide antibiotics have been reported, such as Mureidomycins (US Patent No.5039663) and pacidamycins (US Patent No.6228842B), these compounds mainly act on the cell wall, inhibit the synthesis of cell wall peptidoglycan, have very little toxicity, and At present, there is no drug acting on this target clinically, so the research of such compounds is of great significance for the discovery of drugs against drug-resistant bacteria

Method used

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  • Uridine peptide antibiotic, pharmaceutically acceptable salt, producing method and uses thereof
  • Uridine peptide antibiotic, pharmaceutically acceptable salt, producing method and uses thereof
  • Uridine peptide antibiotic, pharmaceutically acceptable salt, producing method and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] From glucose 0.5%; soluble starch 2.4%; beef extract 0.3%; yeast extract 0.5%; peptone 0.5%; corn steep liquor 0.4%; CoCl 2 0.002%; CaCO 3 0.4%, all the other are water, 100 milliliters of culture medium (pH value is 7.2) of composition are filled in the Erlenmeyer flask of 500 milliliters, after sterilization, inoculate Streptomyces SS (Streptomyces SP.) CGMCC No.1764, at 27 ℃ Rotate and shake (220 times / min, amplitude 7cm) for 2 days and use as seeds.

[0063] Then glucose 0.5%; yeast extract 0.5%; peptone 0.5%; beef extract 0.5%; corn steep liquor 0.4%; soybean meal 1%; starch 2%; 3 0.4%; CoCl 2 ·6H 2 0.4‰, all the other are water, form fermented medium (pH value is 7.2), sub-pack 100 milliliters in the Erlenmeyer flask of 500 milliliters, add the seed of 2% above-mentioned cultivation after sterilization, at 27 ℃, rotary oscillation ( 220 times / min, amplitude 7cm) cultivated for 4 days to obtain the fermented liquid.

[0064] Take the fermentation broth (20 lit...

Embodiment 2

[0102] Basically the same as Example 1, the difference is that the fermentation medium is: 0.4% glucose; 0.4% yeast extract; 0.6% peptone; 0.6% beef extract; 0.3% corn steep liquor; 3 0.5%; CoCl 2 ·6H 2 O0.3‰, the rest is water, and the pH value is 7.2.

[0103] The crude product containing SS-1, SS-2 and SS-3 obtained by fermentation is separated, extracted and refined to obtain antibiotics containing SS-1, SS-2 and SS-3. Then use neutralization reaction to make ammonia salt. Then 50 grams of its ammonium salt and 100 grams of base semi-synthetic glyceride are heated and mixed to be placed in a mould, and made into a suppository after cooling.

Embodiment 3

[0105] Basically the same as Example 1, the difference is that the fermentation medium is: 0.6% glucose; 0.6% yeast extract; 0.4% peptone; 0.4% beef extract; 0.5% corn steep liquor; 3 0.3%; CoCl 2 ·6H 2 O0.5‰, the rest is water, and the pH value is 7.2.

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Abstract

The present invention provides antibiotics of urinate glucoside peptide category with a structural formula (I) and the acceptable salt in pharmaceutics. The antibiotics can be prepared through fermentation and cultivation of produced fungus. The compound of the present invention is a group of cell-wall peptidoglycan synthesized inhibitor, has anti-tuberculosis activity and pyocyanic fungus, and can be used for preparing anti-infective drugs.

Description

technical field [0001] The invention relates to a group of uridine peptide antibiotics and pharmaceutically acceptable salts thereof, a preparation method and application thereof, and belongs to the field of microbial fermentation. Background technique [0002] At present, uridine peptide antibiotics have been reported, such as Mureidomycins (US Patent No.5039663) and pacidamycins (US Patent No.6228842B), these compounds mainly act on the cell wall, inhibit the synthesis of cell wall peptidoglycan, have very little toxicity, and At present, there is no drug acting on this target clinically, so the research of such compounds is of great significance for the discovery of drugs against drug-resistant bacteria. [0003] During the research process, the researchers of the present invention have found a bacterial strain capable of producing novel uridine peptide antibiotics SS-1, SS-2 and SS-3. The structures of the antibiotics SS-1, SS-2 and SS-3 have been It is clarified that i...

Claims

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Application Information

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IPC IPC(8): C07K5/023A61K38/07A61P31/04
Inventor 许鸿章陈汝贤解云英
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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