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Novel antibiotic Chemomycin A and preparation method thereof

A technology of carmomycin and antibiotics, applied in the field of application in the preparation of anti-tumor drugs, to achieve good anti-tumor effects

Inactive Publication Date: 2007-03-07
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

So far, among the angucycline antibiotics that have been discovered, no angucycline antibiotics have been listed as anti-tumor drugs.

Method used

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  • Novel antibiotic Chemomycin A and preparation method thereof
  • Novel antibiotic Chemomycin A and preparation method thereof
  • Novel antibiotic Chemomycin A and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: the fermentation of carmomycin A

[0042] (2% soluble starch, 1% KNO 3 , 0.05% NaCl, 0.05% K 2 HPO4 ,, 0.001% FeSO 4 ·7H 2 O, 0.05% MgSO 4 ·7H 2 O, 2% agar, pH7.0) Nocardiamediterranei var.kanglensis 1747-64 bacteria were inoculated in the seed medium (2% glucose, 1% soybean powder, 0.5% yeast powder, 0.5% CaCO 3 , pH6.5) 50ml / 250ml shake flask, cultivated on a rotary shaker at 28°C for 48 hours, then transferred to fermentation medium (3% glucose, 1% peanut powder, 1% yeast powder, 0.5% peptone, 0.1% CaCO 3 ,, pH6.5) 100ml / 500ml Erlenmeyer flask, cultured on a reciprocating shaking shaker at 28°C for 72 hours, and harvested a total of 20L of fermentation broth.

Embodiment 2

[0043] Embodiment 2: the extraction of carmomycin A

[0044] Use 2N HCl to adjust the pH of the fermented liquid to 3-4, put filter paper in the Buchner funnel and filter with suction to remove hyphae, etc., to obtain the supernatant fermented liquid. Extract three times with 1 / 3 volume of ethyl acetate of the fermentation broth, combine the ethyl acetate obtained by the three extractions, add anhydrous sodium sulfate to dry and dehydrate, let stand for 3-4 hours, concentrate under reduced pressure to obtain the extract.

Embodiment 3

[0045] Embodiment 3: the separation of carmomycin A

[0046] The extractant was first subjected to silica gel column chromatography, and carried out preliminary separation with chloroform: methanol gradient elution, and the elution gradient was respectively chloroform: methanol=100:1 (202ml in total), chloroform: methanol=20:1 (300ml in total) , chloroform:methanol=9:1 (being 200ml in all), collect each fraction, the component that contains target compound-camomycin A is combined and concentrated; Then adopt Sephadex LH-20 to implement further separation to the component that contains target compound , the elution solvent is methanol, the flow rate is 3ml / min, and 350ml of methanol is shared, each component in the eluent is collected, and the components containing the target compound (camomycin A) are combined and concentrated; Prepared by HPLC, the preparation column is an ODS column (20mm × 250mm, 10 μm) of Shimadzu Company, the flow rate is 4ml / min, the injection volume is ...

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Abstract

The invention discloses a new Chemomycin A and preparing method and drug component and application in the tumour prevention drug, which is characterized by the following: separating Angucycline from Nocardia Mediterranei Var. Kanglensis 1747-64 to obtain the product; displaying excellent anti-tumour activity in the external activity test.

Description

Technical field: [0001] The present invention relates to a new angucycline antibiotic (Angucycline) carmomycin A and its preparation method, a pharmaceutical composition with carmomycin A as an active ingredient and the use of carmomycin A in the preparation of antitumor drugs Applications. Background technique: [0002] Nearly 10,000 antibiotics derived from microorganisms have been found so far, many of which have been widely used as medicines and pesticides. Angucycline is a class of secondary metabolites derived from microorganisms, the first such antibiotic was discovered in the 1960s. This is a brand-new four-ring structure compound. Its structure is similar to anthracycline antibiotics. It has an anthraquinone four-ring structure. An asymmetric tetracyclic structure. Most angucycline antibiotics have different degrees of cytotoxic activity, and the activity against Gram-positive bacteria and Gram-negative bacteria is weak. Individual antibiotics of this type also h...

Claims

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Application Information

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IPC IPC(8): C07D303/32A61K31/336C12P17/02A61P35/00C12R1/365
Inventor 孙承航王振周建琴汪月金文藻游雪甫高红赵立勋栾迎春
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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