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Sulfur-bridge-containing complex-ring-series alkaloids compound, preparation method and application thereof

A compound and compound structure technology, applied in the field of complex ring system alkaloid compounds containing sulfur bridges

Active Publication Date: 2015-11-11
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The study found that the compound shown has anti-tumor activity, but there is no report on the chemical structure and cell proliferation inhibitory activity of the compound, so there is no related drug on the market

Method used

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  • Sulfur-bridge-containing complex-ring-series alkaloids compound, preparation method and application thereof
  • Sulfur-bridge-containing complex-ring-series alkaloids compound, preparation method and application thereof
  • Sulfur-bridge-containing complex-ring-series alkaloids compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Fermentative production and separation and purification of embodiment 1 compound I

[0016] 1 Fermentation production

[0017] Fermentation culture of production bacteria: according to the conventional method of cultivating microorganisms, an appropriate amount of bacterial strain Penicilliumsp.

[0018] Take an appropriate amount of Penicilliumsp.HDN13-309 cultured on a slope for 5 days, and inoculate it into 300mL medium [medium composition (g / L): maltose 20.0, glucose 10.0, mannitol 20.0, monosodium glutamate 10.0, yeast extract 3.0, Corn steep liquor 1.0, KH 2 PO 4 0.5, MgSO 4 ·7H 2 00.3, pH adjusted to 6.5] in the 1000mL Erlenmeyer flask, under the condition of 28 degrees centigrade, cultivated statically for 30 days to obtain the fermentation product.

[0019] 2 Obtaining the extract

[0020] Separate the fermentation broth and mycelium with gauze. The mycelium was extracted three times with acetone, concentrated under reduced pressure until no acetone was ...

Embodiment 2

[0028] The antitumor activity test of embodiment 2 compound

[0029] 1 Experimental samples and experimental methods

[0030] Preparation of the test sample solution The test sample is the pure compound I isolated and refined in the above-mentioned Example 1. Precisely weigh an appropriate amount of sample, and prepare a solution with the required concentration with DMSO for activity measurement.

[0031] SRB method: Hela, HCT116, HO-8910 and MGC803 cells in the logarithmic growth phase were prepared with fresh RPMI-1640 medium to a density of 2×10 per ml 5 The cell suspension of two cells was inoculated in a 96-well plate at 200 microliters per well, and 2 microliters of samples or blank solutions of different concentrations were added to each well, and incubated at 37°C for 72 hours. Take the cells cultured under the action of drugs, first observe the morphological changes caused by the drug treatment under an optical microscope, and judge whether there are morphological c...

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Abstract

The invention relates to a sulfur-bridge-containing complex-ring-series alkaloids compound, a preparation method and an application thereof, wherein the novel sulfur-bridge-containing complex-ring-series alkaloids compound is produced from Penicillium sp.HDN13-309. A test proves that the compound can be used as a cell proliferation inhibitor or an anti-tumor agent.

Description

Technical field: [0001] The present invention relates to a Penicilliumsp. No.: CGMCC9429 Deposit date: July 9, 2014) A method for producing a complex ring system alkaloid compound containing a sulfur bridge; the present invention also relates to the anti-tumor application of the compound. [0002] Background technique: [0003] The present inventor isolated a complex ring system alkaloid compound containing a sulfur bridge from the liquid fermentation product of the strain Penicillium sp. HDN13-309 (preservation number: CGMCC9429). The study found that the compound shown has anti-tumor activity, but there is no report on the chemical structure and cell proliferation inhibitory activity of the compound, so there is no drug related to it in the market. [0004] Invention content: [0005] The present invention aims to provide a new compound with novel structure and antitumor activity. Its structural formula is [0006] [0007] Formula I [0008] Detailed ways: ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D513/22C12P17/18A61P35/00C12R1/80
CPCC07D513/22C12P17/188
Inventor 李德海朱美林李静顾谦群朱天骄车茜
Owner OCEAN UNIV OF CHINA