Polyketone compound pyoluterin, and preparation method and application thereof

A compound, the technology of the target compound, applied in the preparation of anticancer drugs, polyketide pyoluteorin and its preparation field, can solve the problem of less research on Aspergillus niger compounds, achieve significant cytotoxic activity, rich resources, and diverse sources Effect

Active Publication Date: 2019-12-31
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In view of the remarkable antitumor activity of the secondary metabolites of Aspergillus niger and the lack of research on soil-derived Aspergillus niger compounds in the prior art, it is urgent to conduct systematic chemical composition research on Aspergillus niger derived from wetland soil, in order to isolate and obtain better compounds from them. Compounds with Antitumor Activity

Method used

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  • Polyketone compound pyoluterin, and preparation method and application thereof
  • Polyketone compound pyoluterin, and preparation method and application thereof
  • Polyketone compound pyoluterin, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: the preparation of polyketide pyoluteorin

[0036] 1. Sample source

[0037] Wetland soil from Gongqing National Forest Park, Shanghai.

[0038] 2. Strain fermentation, extraction, separation and purification methods

[0039] Dilute and mix the retrieved fresh wetland soil with distilled water at a ratio of 1:100. Take 100 μL of the soil dilution and spread it on the separation medium (separation medium: improved Martin solid medium (5.0 g / L peptone, 1.0 g / L L dipotassium hydrogen phosphate, 0.5g / L magnesium sulfate, 2.0g / L yeast extract powder, 20.0g / L glucose, 14.0g / L agar, etc.), add potassium dichromate (50mg / L) and nalidixic acid (20mg / L) as a bacteriostatic agent.), at a temperature of 28 ° C, cultivated for 4 days, after the bacterial strain grew out, it was picked and purified to obtain Aspergillus niger (Aspergillus niger) bacterial strain .

[0040] The above-mentioned purified Aspergillus niger strain was inoculated on the improved Martin s...

Embodiment 2

[0046] Example 2: Cytotoxic activity test

[0047] 1. Experimental materials

[0048] Human glioma cells (U87), human lung adenocarcinoma cells (A549), human colon cancer cells (HCT116), human breast cancer cells (MCF-7, HCC1954), human chronic myelogenous leukemia cells (K562), human Triple-negative breast cancer cells (MDA-MB-231, MDA-MB-468), human triple-positive breast cancer cells (BT474) and human normal breast epithelial cells (MCF-10A) were purchased from ATCC.

[0049] The polyketide compound pyoluteorin was prepared from Example 1.

[0050] 2. Cytotoxic activity screening and mechanism research methods

[0051] (1) CTG method to detect cytotoxic activity

[0052] Different tumor cells growing in the logarithmic phase were collected, counted and inoculated in 96-well culture plate, 2000 cells / well, and 90 μL DMEM culture solution (4.5 g / L D-glucose, L-glutamic acid, 110 mg / well) was added to each well. L sodium pyruvate, etc., containing serum), 37 ° C, 5% CO 2 ...

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Abstract

The invention discloses a polyketone compound pyoluteorin. The chemical structure of the polyketone compound pyoluteorin is shown as formula I; the polyketone compound pyoluteorin is separated and prepared from aspergillus niger derived from wetland soil. The polyketone compound pyoluterin disclosed by the invention has relatively good cytotoxic activity on human lung adenocarcinoma cells, human colon cancer cells, human breast cancer cells, human triple-negative breast cancer cells and human triple-positive breast cancer cells; and the cytotoxic activity on human triple-negative breast cancercells MDA-MB-231 is particularly remarkable, and the toxicity on normal mammary epithelial cells MCF-10A is relatively low, so that the compound can be used for preparing antitumor drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a polyketide compound pyoluteorin isolated from Aspergillus niger, a preparation method thereof, and an application of the compound in preparing anticancer drugs. Background technique [0002] There are more than 180 species of Aspergillus fungi in the Mucoraceae family worldwide, and a large number of secondary metabolites with novel structures and good activities have been isolated from the fungi of this genus. The types of compounds are mostly alkaloids, terpenes, cell Relaxin and lignans (Happi G M, Kouam S F, Talontsi F M, et al. ChemInform Abstract: A NewDimeric Naphtho-γ-pyrone from an Endophytic Fungus Aspergillus niger AKRNA associated with the Roots of Entandrophragma congoense Collected in Cameroon[J]. Cheminform, 2015, 70(9):625-630.). Aspergillus niger is a more striking species in the Aspergillus genus, and the secondary metabolites produced by it have...

Claims

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Application Information

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IPC IPC(8): C07D207/34C12P17/10A61P35/00A61K31/40C12R1/685
CPCA61P35/00C07D207/34C12P17/10
Inventor 张卫东沈云亨丁婷李慧梁徐希科
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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