Novel pyridone alkaloid and preparation method therefor

An alkaloid and pyridone technology, applied in the field of medicine, can solve the problems that pyridone alkaloids have not been patented or reported in literature, and achieve the effects of inhibiting tumor cell growth, simple extraction and separation method, and good reproducibility.

Active Publication Date: 2016-01-06
SHENYANG PHARMA UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Such compounds have not been reported in the literature for their antitumor and antibacterial activities.
And the pyridone al

Method used

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  • Novel pyridone alkaloid and preparation method therefor
  • Novel pyridone alkaloid and preparation method therefor
  • Novel pyridone alkaloid and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: Fermentative production and separation and purification of the compound of formula I

[0020] 1 Fermentation production

[0021] Fermentation culture of production bacteria: After resuscitating the endophytic fungus Trametestrogii, transfer it from the inclined plane to 150mL culture medium [medium composition: mannitol 2%; glucose 2%; yeast extract 0.5%; peptone 1%; KH 2 PO 4 0.05%; MgSO 4 ·7H 2 0.03%; corn steep liquor 0.1%; tap water preparation] in the Erlenmeyer flask (500mL), at 28 ℃ shaker 180rpm vibration culture after 2 days as seed culture solution. Then the seed solution was inoculated into a 500mL Erlenmeyer flask containing 200mL of fresh, sterilized fungal No. 4 liquid medium according to the inoculum size of 5%, and was cultured statically at room temperature to obtain about 70L of fermentation broth.

[0022] 2 Obtaining of crude extract

[0023] The fermentation culture is filtered with 16 layers of gauze to separate the mycelium and ...

Embodiment 2

[0026] Embodiment 2: The growth inhibition test of the compound of formula I to human acute promyelocytic leukemia cell line HL-60 and human breast cancer cell MCF-7 in vitro:

[0027] HL-60 cells were cultured in RPMI1640 medium containing 10% heat-inactivated fetal bovine serum, 100 IU / mL penicillin, 100 mg / mL streptomycin, and 1 mmol / LL-glutamine at 37°C, 5% CO 2 Incubate in a saturated humidity incubator. Weigh trypan blue, add a small amount of distilled water to grind, add double distilled water to dilute to 4% storage concentration, filter with filter paper, and store at 4°C. For use, this stock solution was diluted to a working concentration of 0.4% with PBS. Take the above cells (1×10 5 / mL) was inoculated in a 12-well plate, 2 mL per well. Add different concentrations of drugs and incubate to prepare a single cell suspension. Take 50 μL of the cell suspension and add 50 μL of 0.4% trypan blue solution, mix well, and observe under a microscope within 3 minutes. Dea...

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Abstract

The invention belongs to the technical field of medicines and relates to novel pyridone alkaloid extracted and separated from a fermented product of a plant endophytic fungus (Trametes) and application thereof in preparing a tumor cell inhibitor. The pyridone alkaloid compound has a chemical structural formula I. The experiments verify that the compound has a relatively good growth inhibiting effect on a human promyelocytic leukemia cell line HL-60 and a human breast cancer cell MCF-7, and the compound is simple and feasible in preparation method and good in reproducibility, so that further pharmacological and clinical researches on the compound are facilitated, and application of the compound in preparing the tumor cell inhibitor is developed. The formula is shown in the specification.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a new pyridone alkaloid obtained by extracting and separating from the fermentation product of the endophytic fungus Trametestrogii of Speranthes persicae plant, its preparation method and its application in the preparation of tumor cell inhibitors. Background technique [0002] Pyridone alkaloids are secondary metabolites unique to microorganisms, which are mainly isolated from fungi. The compounds involved in the present invention are formed from polyketides and amino acids (leucine, glycine) through the acetic acid pathway. Such compounds have no literature reports on their antitumor and antibacterial activities. And the pyridone alkaloids involved in the present invention have no relevant patents or literature reports at home and abroad so far. Contents of the invention [0003] The present invention provides a new pyridone alkaloid extracted and separated from the ferment...

Claims

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Application Information

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IPC IPC(8): C07D213/82C12P17/12A61P35/00A61P35/02C12R1/645
CPCC07D213/82C12P17/12
Inventor 白皎裴月湖华会明李占林陈刚卞西清
Owner SHENYANG PHARMA UNIVERSITY
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