Angucycline compounds and application of angucycline compounds in preparation of anti-tumour or antibacterial medicine

A technology of antitumor drugs and antibacterial drugs, applied in the field of natural products

Inactive Publication Date: 2015-07-01
SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, the so-called "super bacteria" with strong drug-resistant activity continue to appear, making the original antibiotic treatment somewhat out of date with the requirements of the times

Method used

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  • Angucycline compounds and application of angucycline compounds in preparation of anti-tumour or antibacterial medicine
  • Angucycline compounds and application of angucycline compounds in preparation of anti-tumour or antibacterial medicine
  • Angucycline compounds and application of angucycline compounds in preparation of anti-tumour or antibacterial medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027]

[0028] Where compound 1:

[0029] Compound 2:

[0030] Compound 3:

[0031] Preparation and structure identification of compound 1 and compound 2 as shown in formula (I), and compound 3

[0032] 1. Preparation of compound 1, compound 2 or compound 3 as shown in formula (I)

[0033] 1. Seed culture

[0034] (1) Seed medium (MAM2ab formula): by mass fraction, including 0.5% soluble starch, 0.5% soybean flour, 2% glucose, 0.2% yeast extract, 0.2% peptone, K 2 HPO 4 0.05%, MgSO 4 ·7H 2 O 0.05%, NaCl 0.4%, Coarse Sea Salt 0.3%, CaCO 3 0.2%, the balance is water, pH 7.2-7.4. According to the formula, mix all the components and pack them into 250mL Erlenmeyer flasks, fill each bottle with 50mL, sterilize at 121°C for 20 minutes, and use it as a spare seed medium. The fermentation medium is the same as the seed medium. .

[0035] (2) Cultivation of seeds: insert the mycelia or spores of the strain Streptomyces rubrogriseus SCSIO 11594 into the seed medium (...

Embodiment 2

[0054] To the experiment of the antitumor cell of the naphthoquinone sesquiterpenes of embodiment 1-compound 1, compound 2 and compound 3

[0055] International tumor cell lines are used, including lung cancer cell line (A549), nasopharyngeal carcinoma cell line (CNE2), breast cancer cell line (MCF-7), and human liver cancer cell line (HepG-2). The test method is the internationally accepted SRB method, with cisplatin as the positive control and normal hepatocytes (HL7702) as the reference. Three parallel experiments were performed for each cell line. The experimental results are shown in Table 2:

[0056] Table 2 compounds 1, 2 and 3 inhibit tumor cell lines (IC 50 ,μM)

[0057]

[0058] The above experimental results show that compound 2 has significant inhibitory activity on the four tested tumor cell lines, and its inhibitory activity on the tested tumor cell lines is an order of magnitude stronger than that of the positive control drug cisplatin, and its inhibitory ac...

Embodiment 3

[0060] Bacteriostasis experiments on the keratin compounds of Example 1-compound 1, compound 2 and compound 3.

[0061] Escherichia coli ATCC 25922, Staphyloccocus aureus ATCC29213, Enterococcus faecalis ATCC29212, Micrococcus luteus, Methicillin-resistant Staphylococcus aureus (MREA) and Methicillin-resistant Staphylococcus epidermidis (MRSE shhs-E1) was used as the test bacterium, and 100 μl of the compound 1-3 was used to test the activity of the system according to the microplate method of CLSI. Specifically:

[0062] 1) Bacterial culture. Cultivate the experimental bacteria with Mueller-Hinton (MH) broth medium, when it grows for 8-12h to about 0.5 Mcfarland concentration (1×10 8 CFU) for backup. And configure a certain concentration of the sample solution. Concentrations of samples and positive controls were configured, and positive controls were selected from ampicillin and kanamycin (water soluble).

[0063] 2) Prepare samples and dilute bacteria solution. The sa...

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Abstract

The invention discloses angucycline compounds and an application of the angucycline compounds in preparation of an anti-tumour or antibacterial medicine. According to the invention, fermentation extract of marine actinomycete, namely streptomyces rubrogriseus SCSIO 11594, is separated and purified, three cytotoxic active or bacteriostatic active compounds are obtained, and the three cytotoxic active or bacteriostatic active compounds are determined to be angucycline compounds through structural analysis, and a concrete structure is shown in a formula (II) in the specification. The three compounds 1, 2 and 3 are separated from streptomyces rubrogriseus SCSIO 11594, wherein the compounds 2 and 3 have anti-tumour activity and can be used for preparing an anti-tumour medicine, and the compounds 1, 2 and 3 have antibacterial activity and can be used for preparing an antibacterial medicine, so that the angucycline compounds disclosed by the invention provide new or new-functional pilot compounds for development of new anti-tumour or antibacterial medicines and have important significance for developing China marine medicinal resources.

Description

Technical field: [0001] The invention belongs to the field of natural products, and in particular relates to three marine-sourced cantercycline compounds and their application in the preparation of antitumor or antibacterial drugs. Background technique: [0002] All kinds of malignant tumors, pathogenic bacteria, especially the infestation of drug resistance, not only seriously threaten human life and quality of life, but also an important burden for social and economic development. In recent years, with the development of social economy, the harm caused by various cancer diseases caused by malignant tumors has not been alleviated, but has gradually become the main cause of death in our country. At the same time, the so-called "super bacteria" with strong drug-resistant activity continue to appear, making the original antibiotic treatment somewhat out of date with the requirements of the times. Therefore, accelerating the research and development of new drugs with anti-tumo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/04C07D493/14C07D309/10A61K31/7048A61K31/357A61K31/351A61P35/00C12N1/20C12P19/60C12P17/06C12P17/18C12R1/465
CPCC12P17/06C12P17/18C12P19/60C12N1/205C12R2001/465Y02A50/30
Inventor 鞠建华宋永相李洁黄洪波
Owner SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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