Lipopeptide compound as well as compositions, preparation method and application thereof

A technology of compounds and extracts, applied in biochemical equipment and methods, drug combinations, microbial-based methods, etc., can solve the problems of small number and types of compounds

Inactive Publication Date: 2011-09-07
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Fellutamide lipopeptide derivatives have so far reported a small number of compounds and their

Method used

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  • Lipopeptide compound as well as compositions, preparation method and application thereof
  • Lipopeptide compound as well as compositions, preparation method and application thereof
  • Lipopeptide compound as well as compositions, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Embodiment 1: Microbial fermentation culture and the preparation of compound I-V

[0077] 1. Fermentation culture and extraction of fermented products

[0078] 1) Production strain

[0079] The toxin-producing bacteria used to ferment and produce compounds I-V in this example is the Penicillium purpurogenum AD-2-1 strain preserved in the General Microorganism Center of China Microbiological Culture Collection Management Committee, and the preservation number is 3561, which is CGMCC No. 3561.

[0080] 2) Fermentation culture

[0081] According to the conventional method of microbial culture, take out the slant of Penicillium purpurogenum (Penicillium purpurogenum) AD-2-1 test tube from the refrigerator at 4 °C, scrape an appropriate amount of spores with an inoculation loop under sterile conditions, and inoculate them in 5 newly prepared PDA by streaking Solid medium (composition: 2% glucose, 2% agar, 1.5% NaCl, prepared with 20% potato boiled liquid) plate, activate...

Embodiment 2

[0102] Embodiment 2: Antitumor activity test of compound I-V

[0103] 1. Experimental materials

[0104] 1) Preparation of the tested sample solution

[0105] The test samples were pure compounds I-V isolated and refined in Example 1 above. Precisely weigh an appropriate amount of sample, and use methanol to make a solution of the required concentration for testing the activity.

[0106] 2) Subculture of cell lines and cells

[0107] The human myelogenous chronic leukemia K562 cell line was used for the activity test. K562 cells were routinely passaged with RPMI-1640 medium containing 10% fetal bovine serum and 100 μg / ml penicillin and streptomycin, and maintained at 37°C in a cell culture incubator with 5% carbon dioxide.

[0108] 2. Activity test method

[0109] The anti-tumor activity of the samples was tested by MTT method combined with cell morphology detection. Take K562 cells in the logarithmic growth phase, and use fresh RPMI-1640 medium to prepare a cell densi...

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PUM

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Abstract

The invention belongs to the field of pharmaceutical chemical industry and relates to a lipopeptide compound as well as compositions, a preparation method and application thereof, in particular to a compound I or pharmaceutically acceptable salts thereof, wherein R represents hydroxymethyl, C1-10 linear chain or branch chain alkoxy, C2-10 linear chain or branch chain alkenyloxy, C2-10 linear chain or branch chain alkynyloxy, C6-10 linear chain or branch chain aryloxy or C2-18 saturated or unsaturated fat acyloxy methyl. The invention also relates to penicillium purpurogenum for preparing the compound. Tests prove that the compound can be used for preparing a lethal cytotoxin reagent or an antitumor agent on tumor cells. The compound disclosed by the invention has favorable antitumor activity.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and relates to a lipopeptide compound, its composition, its preparation method and application. Background technique [0002] Tumor is a new organism formed by the body under the action of various carcinogenic factors, a certain cell in the local tissue loses its normal regulation of its growth at the gene level, resulting in abnormal clonal proliferation. Tumors are generally divided into benign and malignant. All malignant tumors are collectively called cancer. [0003] Lipopeptide compounds refer to peptide compounds containing fatty acid residues in their molecular structure, and some lipopeptide compounds are known to have antitumor activity. [0004] For example, fellutamide A and B and their analogs are tripeptide derivative compounds containing a fatty acid residue, and some compounds of this class are known to have antitumor activity. For example, fellutamide A and B all ...

Claims

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Application Information

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IPC IPC(8): C07K5/072C12N1/14C12P21/02A61K38/05A61P35/00A61P35/02C12R1/80
Inventor 崔承彬吴长景李长伟田从魁杨明姚志伟
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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