Application of two quadruple lactone antibiotics as anti-MRSA drugs, and extraction and separation method of two quadruple lactone antibiotics

A technology of antibiotics and esters, used in antibacterial drugs, pharmaceutical formulations, medical preparations containing active ingredients, etc., to achieve the effect of high extraction and separation efficiency

Inactive Publication Date: 2020-08-28
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Dracaena glabra, Latin scientific name: (Dracaena cochinchinensis (Lour.) S.C.Chen) Liliaceae Dracaena genus, so far there is no relevant information about the isolation of

Method used

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  • Application of two quadruple lactone antibiotics as anti-MRSA drugs, and extraction and separation method of two quadruple lactone antibiotics
  • Application of two quadruple lactone antibiotics as anti-MRSA drugs, and extraction and separation method of two quadruple lactone antibiotics
  • Application of two quadruple lactone antibiotics as anti-MRSA drugs, and extraction and separation method of two quadruple lactone antibiotics

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: the preparation of two kinds of quadruple lactone compounds

[0046] 1. Source and identification of the strain

[0047] The compounds of formula 1 and formula 2 were both isolated from the fermentation product of a Dracaena genus genus endophyte, which was provided by Zhang Xiaomei’s research group at the School of Basic Medicine, Yunnan University of Traditional Chinese Medicine, and compared by 16S rRNA sequencing analysis , identified as Streptomyces puniceus S009.

[0048] Isolation and Identification of Streptomyces puniceus S009

[0049] 1.1. Strain isolation

[0050] Healthy plant samples were rinsed with running water, then air-dried at room temperature for 48 hours, and then cleaned ultrasonically at 160W for 5 minutes to remove soil and organic residues on the plant surface. And carry out the surface disinfection of plant samples according to the following process: soak in 70% ethanol for 5 minutes, wash the sample three times in sterile wate...

Embodiment 2

[0065] Embodiment 2: Structural identification of two kinds of quadruple lactone compounds

[0066] The compound Dinactin (1) prepared in Example 1 is a colorless oily substance, which is easily soluble in chloroform, acetone and DMSO. Figure 2 to Figure 7 is the structural analysis spectrum of compound Dinactin (1), HR-ESI-MS: m / z 787.4590[M+Na] + (Positive ion mode), determine its molecular formula as C 42 h 68 o 12 . From 1 H NMR and 13 The C NMR data shows that the NMR data of compound 1 is basically consistent with the data of dinactin (diactin) reported in the literature, and the NOESY related signal And the optical rotation data further confirmed that the three-dimensional configuration of compound 1 was consistent with that reported in the literature. Therefore, identification compound 1 is dinactin, as shown in Table 1:

[0067] Table 1. Compounds of Dinactin 1 H(400MHz) and 13 C (100MHz) NMR data (solvent: CDCl 3 )

[0068]

[0069]

[0070] The...

Embodiment 3

[0072] Embodiment 3: the research of anti-MRSA effect of compound Dinactin (1) and Trinactin (2) in vitro

[0073] 1. Experimental indicator bacteria

[0074] 9 strains of MRSA drug-resistant bacteria used in the present invention: 1505, 1450, 1591, 1957, 2024, I-20, I-67, 28299, 28300, are all isolated from patients in the First People's Hospital of Qujing City. resistant to vancomycin.

[0075] 2. Samples to be tested

[0076] Dinactin(1), Trinactin(2), Vancomycin (positive control), DMSO (negative control)

[0077] 3. Medium

[0078] Liquid LB medium: peptone 10g; yeast extract 5g; NaCl 10g; agar 15g; water 1000mL; PH7.2-7.6.

[0079] 4. Experimental method

[0080] 1) Preparation of bacterial solution

[0081] Inoculate the purified indicator bacteria into the corresponding liquid medium: MRSA was inoculated in the LB medium, cultured at 37°C for 12-24 hours, then diluted with the corresponding liquid medium: Bacteria 0.5×10 6 CFU / mL.

[0082] 2) Preparation of the...

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Abstract

The invention discloses an application of two quadruple lactone antibiotics as anti-MRSA drugs and an extraction and separation method of the two quadruple lactone antibiotics. According to the methoddisclosed by the invention, two quadruple lactone compounds, namely Dinactin and Trinactin, are separated from Dracaena cochinchinensis endophyte Streptomyces punctatus S009 for the first time; in-vitro anti-MRSA activity tests are carried out on the two separated compounds, and results show that the Dinactin and the Trinactin have a stronger inhibition effect on a plurality of clinically separated MRSA strains than a positive reference substance vancomycin, so that the Dinactin and the Trinactin have a better inhibition effect on multiple kinds of clinically separated MRSA strains than a positive control substance, vancomycin, and a molecular docking result shows that such kind of compounds has strong binding activity with anti-MRSA target protein PBP2a. Therefore, the invention not onlycan provide lead compounds for developing a novel anti-MRSA drug, but also can effectively protect rare and endangered medicinal plant resources, and is of great significance for reducing the damageto the diversity of wild medicinal plants.

Description

technical field [0001] The invention belongs to the technical field of natural product chemistry, and relates to the application of two quadruple lactone antibiotics as an anti-MRSA drug and its extraction and separation method, in particular to two quadruple lactones separated from the endophytic bacteria Streptomyces puniceusS009 of Dracaena glabra. Preparation method of lactone antibiotic and its application as anti-MRSA drug. Background technique [0002] Methicillin-resistant Staphylococcus aureus (MRSA) is the main pathogenic bacteria of nosocomial infection. It has the characteristics of high isolation rate, high drug resistance and high fatality rate. hepatitis B, AIDS). Glycopeptide antibiotics are currently the main therapeutic drugs against MRSA, among which vancomycin is known as the "last line of defense" for the treatment of MRSA infection. However, vancomycin-resistant Staphylococcus aureus (VRSA) has emerged, so it is urgent to find new and effective antiba...

Claims

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Application Information

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IPC IPC(8): A61K31/365C07D493/22A61P31/04
CPCA61K31/365C07D493/22A61P31/04
Inventor 张娟利张晓梅李慧玲文爱东
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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