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Novel antibiotic Chemomycin A, B, C, D and preparation method thereof

A technology of carmomycin and antibiotics, which is applied in the field of preparation of anti-tumor drugs, and achieves a significant anti-tumor effect

Inactive Publication Date: 2007-10-17
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 angucyclinone antibiotics that have been discovered, no angucyclinone antibiotics have been listed as anti-tumor drugs.

Method used

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  • Novel antibiotic Chemomycin A, B, C, D and preparation method thereof
  • Novel antibiotic Chemomycin A, B, C, D and preparation method thereof
  • Novel antibiotic Chemomycin A, B, C, D and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] : the fermentation of carmomycin B, C, D

[0057] (2% soluble starch, 1% KNO 3 , 0.05% NaCl, 0.05% K 2 HPO 4 ,, 0.001% FeSO 4 ·7H 2 O, 0.05% MgSO 4 ·7H 2 O, 2% agar, pH7.0) Nocardia MediterraneiVar.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

[0058] : the extraction of carmomycin B, C, D

[0059] 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

[0060] : separation of carmomycin B, C, D

[0061] Above gained medicinal extract is carried out preliminary separation with chloroform: methanol gradient elution earlier through silica gel column chromatography, and elution gradient is respectively chloroform: methanol=100: 1 (202mL in total), chloroform: methanol=20: 1 (300mL in total), Chloroform:methanol=9:1 (200mL in total), collect each fraction, combine and concentrate the components containing the target compound-camomycin B; then use SephadexLH-20 to further separate the components containing the target compound, elute The solvent is methanol, the flow rate is 1mL / 3 minutes, and 350mL of methanol is shared. The components in the eluate are collected, and the components containing the target compound (camomycin B) are combined and concentrated; then the polyamide membrane is used to prepare (20×20cm, chloroform:methanol:water=9:1:0.5), collect R f =0.65 green fluorescent band (camomycin B), concentrated after methanol...

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PUM

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Abstract

The present invention relates to a group of novel compound Chemomicin B,C,D and its preparation method, pharmaceutical composition containing Chemomicin B,C,D as active ingredients and its uses of Chemomicin B,C,D in preparing antineoplastic drug. Chemomicin B,C,D is Angucyclinone antibiotic separated from Nocardia Mediterranei Var.Kanglensis 1747-64 culture. In vitro activity test prove Chemomicin B,C,D has strong suppressing activity for human oesophagus cancer cell KYSE150 and has good development prospect as a novel antineoplastic drug.

Description

Technical field: [0001] The present invention relates to a group of new angucyclinone antibiotics (Angucyclinone): carmomycin B, C and D and their preparation methods, pharmaceutical compositions with carmomycin B, C and D as active ingredients and carmomycin Application of mycin B, C and D in the preparation of antitumor drugs. Background technique: [0002] So far, more than ten thousand kinds of antibiotics derived from microorganisms have been discovered, many of which have been widely used as medicines and pesticides. Angucyclinone antibiotics are a class of antibiotics discovered in the 1960s with a wide range of biological activities. Their structures are relatively similar to anthracycline antibiotics, in which the A ring is in the form of an angle and is attached to the anthracycline. Most angucyclinone antibiotics have anti-tumor activity, and weak activity against Gram-positive bacteria and Gram-negative bacteria. Some of these antibiotics also have enzyme inhibi...

Claims

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Application Information

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IPC IPC(8): C07J63/00C12P15/00A61K31/56A61P35/00C12R1/365
Inventor 孙承航汪月周建琴金文藻何琪杨韩宁宁高红赵立勋
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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