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Antitumor antibiotics, pharmaceutically acceptable salts thereof, preparation method thereof and use thereof

A glycopeptide antibiotic and pharmaceutical technology, which is applied in the direction of antineoplastic drugs, microbial-based methods, biochemical equipment and methods, etc., and can solve problems such as application limitations

Inactive Publication Date: 2010-01-20
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

However, its use is limited by the side effects of dose-dependent pulmonary fibrosis

Method used

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  • Antitumor antibiotics, pharmaceutically acceptable salts thereof, preparation method thereof and use thereof
  • Antitumor antibiotics, pharmaceutically acceptable salts thereof, preparation method thereof and use thereof
  • Antitumor antibiotics, pharmaceutically acceptable salts thereof, preparation method thereof and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Example 1 Fermentation

[0075] Glucose 1.0%; peptone 0.5%; starch 1.0%; NaCl 0.5%; agar 2.0% (pH7.2-7.5) as slant medium, sterilized at 120°C for 30 minutes to make slant, and kept at 37°C for 3 days . When the surface moisture is slightly dry and there is no growth of miscellaneous bacteria, inoculate Streptomyces verticillus var. Pingyangensis n.sp with spores of Streptomyces verticillus var. Pingyangensis n.sp, and cultivate at 28°C for 8 days. It is fluffy and can be collected and used when there is no bacteria. Fill 100ml medium respectively in a plurality of 500ml glass bottles (medium composition: starch 2.5%, glucose 0.5%, bean cake powder 3.5%, KH 2 PO 4 0.1%, ZnSO 4 0.05%, CuSO 4 0.01%, pH natural). Add a cotton plug, sterilize at 120°C for 30 minutes, and inoculate by digging blocks from an inclined plane. After 48 hours of rotary culture in a rotary shaker at 28°C, they were used as seeds.

[0076] Then with the fermenting medium (pH nature) of th...

Embodiment 2

[0077] Example 2 Extraction and Purification

[0078] The fermented culture liquid (25 liters) of embodiment 1 is adjusted pH2~3 with oxalic acid solution, filters, and filtrate passes through 122 (H + ) cation exchange resin (1 liter) adsorption, and then eluted with 0.3mol / L HCl (4 liters), the active part was adjusted to pH 7.0, and an appropriate amount of CuSO was added 4 solution to fully chelate Cu 2+ , and then desalted with macroporous adsorption resin, eluted with 20% acetone solution containing 0.01M HCl, collected the eluate and removed acetone and carried out CM-SephadexC-25 (NH 4 + ) column chromatography, with 0.1 ~ 1M NH 4 Cl gradient elution, separated to obtain NC0604 copper-containing eluate, and then desalted by macroporous adsorption resin, the desalted eluate was vacuum concentrated and freeze-dried to obtain blue NC0604 copper-containing pure product (313mg). The copper-containing product is decopper-treated with diphenylsulfocarbezone in acidic meth...

Embodiment 3

[0079] Embodiment 3 extraction and purification

[0080] The fermented culture liquid (25 liters) of embodiment 1 is adjusted pH2~3 with oxalic acid solution, filters, and filtrate passes through 151 (H + ) ion exchange resin (1 liter) adsorption, washed with 0.3mol / L HCl (4 liters) to elute, the active part adjusts the pH to 6.5 and adds an appropriate amount of CuSO 4 solution to fully chelate Cu 2+ , then desalted with macroporous adsorption resin 4006, eluted with 10% acetone solution containing 0.01M HCl, collected the eluate, adjusted pH 6.5 with ammonia water after removing acetone, and carried out CM-Sephadex C-25 (NH 4 + ) column chromatography, after washing the column with water, use 0.1 ~ 1M NH 4 Cl gradient elution, collected according to the peak position, combined. The NC0604 copper-containing eluate was separated, and then desalted by macroporous adsorption resin. The desalted eluate was vacuum-concentrated and freeze-dried to obtain the blue NC0604 copper-...

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Abstract

The invention provides a novel compound having a structural formula (I), and a pharmaceutically acceptable salts formed by the compound. The compound is obtained by fermentation culture of producing bacteria thereof. The compound is the novel compound of a bleomycin group, has better antitumor activity than that of the clinical bleomycin, and can be used for preparing an antitumor medicament.

Description

technical field [0001] The invention relates to an anti-tumor antibiotic NC0604 and a pharmaceutically acceptable salt thereof, a preparation method and application thereof, and belongs to the field of microbial fermentation. Background technique [0002] Bleomycin is a class of broad-spectrum antibacterial and anti-tumor antibiotics with a unique structure and unique effects. The molecular structure of Bleomycin antibiotics: [0003] [0004] A 2 R=-NH(CH 2 ) 3 S(CH 3 ) 3 [0005] B 2 R=-NH(CH 2 ) 4 NHC(=NH)NH 2 [0006] Bleomycin (A 2 +B 2 Mainly) has effective anti-lymphatic, head, neck cancer and germ cell tumors. Bleomycin has very low myelosuppressive and immunosuppressive effects during tumor treatment, so it has become a widely used antineoplastic drug in clinic. However, its application is limited because of the side effects of dose-dependent pulmonary fibrosis. Therefore, the development of new bleomycin compounds with good curative effect and...

Claims

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Application Information

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IPC IPC(8): C07K9/00C12P21/00A61K38/14A61P35/00C12R1/625
Inventor 陈汝贤许鸿章陈彩霞鲁敏石莲英解云英
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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