Anti-tumor and antibacterial compound and application thereof

A compound and anti-tumor technology, applied in the direction of anti-tumor drugs, anti-bacterial drugs, hybrid peptides, etc., can solve problems such as differences and achieve strong antibacterial activity

Active Publication Date: 2018-12-18
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, it has been found that hemastatin and chloptosin are similar cyclic hexapeptide antibiotics, but the latter two have obvious differences in amino acid composition from de-Cl-dialboflavusin A

Method used

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  • Anti-tumor and antibacterial compound and application thereof
  • Anti-tumor and antibacterial compound and application thereof
  • Anti-tumor and antibacterial compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 : Isolation and structure identification of Dialboflavusin A and de-Cl-dialboflavusin A

[0023] 1.1 Isolation and structure identification of Dialboflavusin A

[0024] Streptomyces alboflavus 313-HmtS mutant strain fermentation broth (60L) was centrifuged to remove bacteria (5000 rpm, 30 minutes), and 2kg HP20 macroporous resin was used to absorb and enrich the active ingredients, first eluted with 5L distilled water, and the eluate was discarded . Then 10 L was eluted with methanol. Concentrate 10L of the methanol eluate to dryness, perform silica gel column chromatography, and use ethyl acetate, ethyl acetate / methanol (50% / 50%, volume ratio) and methanol system for elution, and 5 L of each fraction is eluted. Concentrate ethyl acetate / methanol (50% / 50%, volume ratio) to a small volume, filter through a 0.45-micron filter membrane, and perform dextran gel SephexLH20, eluting with methanol at a flow rate of 1 mL / min, and each fraction is 5 mL. The fractio...

Embodiment 2

[0037] Example 2 : Antibacterial activity of Dialboflavusin A and de-Cl-dialboflavusin A

[0038] The effect of dialboflavusin A and de-Cl-dialboflavusin A on Bacillus subtilis (Bacillus subtilis BS168), Bacillus cereus (CGMCC 1.0230), Staphylococcus aureus (Staphylococcus aureus ATCC 6538) and four different resistant Methicillin-resistant Staphylococcus aureus methicillin-resistant Staphylococcus aureus 113 (MRSA-1), methicillin-resistant Staphylococcus aureus 1.2386 (MRSA-2), methicillin-resistant Staphylococcus aureus 09R496 (MRSA-3), and methicillin-resistant Staphylococcus aureus (08Lucoccus aureus MRSA-4) and other seven kinds of bacteriostatic activity of tested Gram-positive bacteria. Methicillin-resistant Staphylococcus aureus was provided by the State Key Laboratory of Early Development of Microbial Resources, Institute of Microbiology, Chinese Academy of Sciences, and the rest of the strains were purchased from the China General Microbiology Collection Center.

...

Embodiment 3

[0044] Example 3 : Dialboflavusin A and de-Cl-dialboflavusin A inhibit the activity of tumor cells.

[0045] MTT method was used to determine the effects of dialboflavusin A and de-Cl-dialboflavusin A on cervical cancer cell line Hela, human ovarian adenocarcinoma cell line SKOV3, human breast cancer cell line MCF-7, human lung cancer cell line A549, human liver cancer cell line Antitumor activity of HepG2 line, human glioma cell line U251 and human gastric cancer cell line SGC-7901. All tumor cell lines were obtained from the Institute of Basic Medical Sciences, Chinese Academy of Military Sciences.

[0046] Tumor cell lines were formulated to 5×10 3 100 μL of each concentration of the suspension was inoculated into each well of a 96-well plate, cultured overnight, and the samples of dialboflavusin A and de-Cl-dialboflavusin A at the concentration to be tested were added, and 5-fluorouracil was used as a positive control. After culturing for 72 hours, Add 20 μL of MTT rea...

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Abstract

Belonging to the technical field of drug research and development, the invention in particular relates to an anti-tumor and antibacterial compound and application thereof. The anti-tumor and antibacterial compound is named as dialboflavusin A or de-Cl-dialboflavusin A. The anti-tumor and antibacterial compounds dialboflavusin A and de-Cl-dialboflavusin A have strong bacteriostatic activity on 7 gram positive bacteria for test: Bacillus subtilis, Bacillus cereus, Staphylococcus aureus, and four different methicillin-resistant Staphylococcus aureus strains. The anti-tumor and antibacterial compounds dialboflavusin A and de-Cl-dialboflavusin A have strong inhibiting effect on cervical cancer cell line Hela, human ovarian adenocarcinoma cell line SKOV3, human breast cancer cell line MCF-7, human lung cancer cell line A549, human hepatoma cell line HepG2, human glioma cell line U251 and human gastric carcinoma cell line SGC-7901. The anti-tumor and antibacterial compound provided by the invention can be used for study of anti-tumor active lead compounds or preparation of antibacterial and anti-tumor drugs.

Description

technical field [0001] The invention belongs to the technical field of drug research and development, and in particular relates to an antitumor and antibacterial compound and its application. Background technique [0002] Biphenyl is one of the structural units with important functions in natural products. Studies have shown that compounds with biphenyl structure have higher biological activity. Although the chemical synthesis of molecules containing this structural unit has been studied for more than 100 years, complex natural products containing this structure are still difficult in chemical synthesis. Due to the cumbersome reaction conditions and low yields seriously affected its follow-up in-depth research. Therefore, the use of efficient and specific biocatalytic methods to obtain highly active compounds containing biphenyl structures can break through the above-mentioned bottleneck. [0003] Dialboflavusin A is a dimerized cyclic hexapeptide antibiotic isolated from ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/64A61K38/12A61P35/00A61P31/04
CPCA61K38/12A61P31/04A61P35/00C07K7/64C07K19/00
Inventor 陈义华郭正彦李鹏伟
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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