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Two new alkaloids and preparation method thereof, and applications of two new alkaloids in preparation of anti-MRSA antibacterial agents

A technology of alkaloids and antibacterial agents, which is applied in antibacterial, antiseptic and pharmaceutical fields, can solve the problems of increased MRSA drug resistance, low tissue penetration rate, and slow bactericidal activity, etc., and achieves controllable preparation process conditions, wide application potential, and convenient extraction Effect

Active Publication Date: 2019-04-02
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, only a few antibiotics such as vancomycin can be used clinically for the treatment of MRSA infection, but the few clinical antibiotics such as vancomycin that have anti-MRSA effects are showing slow bactericidal activity, low tissue penetration rate and MRSA infection. A series of problems such as the increasing resistance to

Method used

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  • Two new alkaloids and preparation method thereof, and applications of two new alkaloids in preparation of anti-MRSA antibacterial agents
  • Two new alkaloids and preparation method thereof, and applications of two new alkaloids in preparation of anti-MRSA antibacterial agents
  • Two new alkaloids and preparation method thereof, and applications of two new alkaloids in preparation of anti-MRSA antibacterial agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the preparation of maslinic acid in the dried bitter blue blue product

[0027] 1.1 Plant source and identification

[0028] The leaf samples of Akebia trifolia (Thumb.) Koidz., a plant material for extraction, were collected from Neileizhou Peninsula, Guangdong Province in September 2010, and were identified by Professor Li Bingtao of South China Agricultural University.

[0029] 1.2 Extraction and separation

[0030] Using supercritical CO 2 Extraction technology, at 15MPa and 30°C, crush 12kg of bitter blue leaves and extract for 15 minutes to obtain supercritical CO 2 Extract (116g). The extract was subjected to silica gel column chromatography and eluted with petroleum ether / acetone (from 100:0 to 0:100, v / v) to obtain pooled fractions F1-F6. The obtained F4 fraction (2.02 g) was eluted with petroleum ether / acetone (70:30, v / v) and then carried out with chloroform / methanol gradient elution (100:100 to 100:10) by silica gel column chromatography to...

Embodiment 2

[0039] Embodiment 2: the anti-MRSA activity detection of two kinds of new alkaloid compounds

[0040] 1. The type of bacteria used in the experiment

[0041] Methicillin-resistant Staphylococcus aureus (MRSA) strain (No. 11646) was provided by Guangzhou Institute of Respiratory Diseases. It is resistant to methicillin and sensitive to vancomycin.

[0042] 2. Experimental drugs

[0043] Positive control substance: vancomycin (vancomycin)

[0044] Negative control: MeOH

[0045] Myoporumine A and Myoporumine B are prepared by the above experimental examples

[0046] 3. Experimental method:

[0047] Myoporumine A, Myoporumine B, and vancomycin were respectively prepared into 1 mg / ml solutions in methanol (MeOH). Using the resazurin color reaction method, the minimum inhibitory concentration (MIC) of the three compounds against drug-resistant MRSA was determined through a 96-well cell culture plate.

[0048] Firstly, 100 μg / mL resazurin indicator was added to the 11th column...

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Abstract

The present invention provides two new alkaloids and a preparation method thereof, and applications of the two new alkaloids in preparation of anti-MRSA antibacterial agents. According to the presentinvention, the new alkaloid antibacterial agents capable of strongly inhibiting MRSA are extracted and separated from a Myoporum bontioides plant, wherein the plant source is abundant, the extractionmethod is convenient, the plant can be recycled for a long time, and the two alkaloid monomer compounds are stable and easily stored; the anti-MRSA activity test results show that Myoporumine A and Myoporumine B have strong MRSA inhibitory effects close to the positive control vancomycin, such that Myoporumine A and Myoporumine B can be used for the preparation of effective and safe anti-MRSA antibacterial agents or new anti-MRSA drugs; the lead compounds are provided for the development of new anti-MRSA antibacterial agents and anti-MRSA drugs, and the great significance is provided in the promoting of the high value utilization of Myoporumine A, Myoporumine B and plant Myoporum bontioides; and the structural formulas of the new alkaloid compounds Myoporumine A (1) and Myoporumine B (2) are represented by the following formula (I). The formulas 1, 2 and I are defined in the specification.

Description

Technical field: [0001] The invention belongs to the field of antibacterial anticorrosion and medical technology, in particular to two new alkaloid compounds Myoporumine A (1) and Myoporumine B (2), their preparation method and their use in the preparation of methicillin-resistant Staphylococcus aureus ( That is anti-MRSA) antibacterial agents and antibacterial drugs. Background technique: [0002] The long-term inappropriate use of antibiotics has caused many human pathogens to increase and accumulate drug resistance, which has led to the emergence of strong resistance to many existing antibiotics such as methicillin-resistant Staphylococcus aureus (MRSA). Pathogenic 'superbugs' refractory to existing antibiotics. The infection of drug-resistant bacteria MRSA is a serious threat to human health worldwide. MRSA can cause many diseases in humans, including skin and soft tissue infection, sepsis, endocarditis, pneumonia, enteritis, meningitis, osteomyelitis, and toxic shock s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/38C07D405/04A61P31/04A61K31/4025A61K31/4015
CPCA61P31/04C07D207/38C07D405/04Y02P20/54
Inventor 谭建文谷文祥董丽梅徐巧林
Owner SOUTH CHINA AGRI UNIV
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