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Preparation method of new aromatic polyketone compound and antibacterial use thereof

A compound and polyketide technology, applied in the field of pharmacy, can solve problems such as increased clinical complications and deaths, reduced therapeutic effect, and mutation of pathogenic bacteria

Inactive Publication Date: 2016-08-10
PEKING UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the widespread use of antibiotics and immune preparations, pathogenic bacteria have also mutated, and a large number of drug-resistant strains have emerged, leading to increasingly serious problems of antibiotic resistance
Traditional antibiotics such as penicillin have become less effective in treating infections caused by resistant bacteria such as methicillin-resistant Staphylococcus aureus (MRSA), leading to increased clinical complications and deaths

Method used

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  • Preparation method of new aromatic polyketone compound and antibacterial use thereof
  • Preparation method of new aromatic polyketone compound and antibacterial use thereof
  • Preparation method of new aromatic polyketone compound and antibacterial use thereof

Examples

Experimental program
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Embodiment approach

[0031] According to the technical contents disclosed in the present invention, other embodiments of the present invention will be apparent to those skilled in the art, and the following embodiments are only examples.

example 1

[0032] Example 1: Solid fermentation culture of deep-sea fungus Spiromastix sp.

[0033] 1. Strain Background

[0034] Spiromastix sp. was isolated from 2869-meter underwater sediments in the South Atlantic Ocean (13.7501° West Longitude, 15.1668° South Latitude).

[0035] 2. Preparation of Solid Medium

[0036] Add 100mL of artificial seawater and 100g of rice into a 500mL Erlenmeyer flask, let it stand for 12 hours, then sterilize it at 121°C for 30 minutes, and let it cool for later use.

[0037] 3. Strain fermentation

[0038] On the PDA (potato, glucose, agar) petri dish, pick the agar piece (1 ~ 2cm) with fresh Spiromastix sp. 2 ), inoculated on the rice culture medium, and cultured at 25° C. for 30 days at a constant temperature in the dark to obtain a fermentation product.

example 2

[0039] Example 2: Preparation of Formula I~Formula VI Compound

[0040] After mashing the fermentation product, it was ultrasonically extracted with ethyl acetate for 3 times, each time for 1.5 h, and concentrated under reduced pressure to obtain a crude extract (52.4 g). The extract was prepared with equal proportions of silica gel (160-200 mesh), and eluted by vacuum silica gel column chromatography with petroleum ether / acetone as the mobile phase gradient. Petroleum ether / acetone (10:1, v / v) elution fraction (4.8g) uses ODS column chromatography to use methanol / water as mobile phase (20%~100%, v / v) gradient elution, 60% elution De-fractionation was carried out by semi-preparative high-performance liquid chromatography with 68% methanol / water as the mobile equipotential elution, and purified to obtain the compound of formula I (12.3 mg), the compound of formula II (17.8 mg) and the compound of formula IV (22.6 mg); ODS The 80% eluted components of column chromatography were...

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Abstract

The invention discloses a new aromatic polyketone compound and a preparation method thereof. The invention also discloses the antibacterial use of the polyketone compound.

Description

technical field [0001] The invention belongs to the field of pharmacy. The invention discloses a new class of aromatic polyketide compounds and a preparation method thereof. The invention also relates to the antibacterial application of the compound and the composition thereof. Background technique [0002] Bacterial infection is an acute systemic infection caused by pathogenic bacteria or conditional pathogenic bacteria invading the blood circulation to grow and reproduce, producing toxins and other metabolites, which can cause various pathological symptoms such as high fever, typhoid fever and tuberculosis, and seriously affect human health , endangering the safety of human life. Before the nineteenth century, diseases caused by bacterial infections claimed countless lives. The invention and use of penicillin have effectively controlled bacterial infections. Then, with the continuous advent of the second-generation, third-generation and other new-generation antibiotics, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C43/295C07D311/76C07C69/84C12P7/22C12P7/62C12P17/06A61P31/04C12R1/645
Inventor 林文翰邵宗泽牛四文刘东
Owner PEKING UNIV
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