Dimer citrinin compounds and preparation and use thereof

A kind of compound and application technology, applied in the field of preparing cell proliferation inhibitor

Inactive Publication Date: 2010-06-16
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 dimer citrinin compound has anti-tumor activity, but there is no report on the chemical structure of the compound and the activity of inhibiting cell proliferation and inducing apoptosis, so there is no drug related to it in the market

Method used

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  • Dimer citrinin compounds and preparation and use thereof
  • Dimer citrinin compounds and preparation and use thereof
  • Dimer citrinin compounds and preparation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Fermentative production and separation and purification of compound I and II of embodiment 1

[0014] 1 Fermentation production

[0015] Fermentation culture of production bacteria: according to the conventional method of cultivating microorganisms, take an appropriate amount of Penicillium citrinum HGY1-5 (preservation number: CCTCC M 208170), inoculate it on the PDA solid slant medium, and cultivate it at 28 degrees Celsius 4 days in the box.

[0016] Take an appropriate amount of Penicillium citrinum HGY1-5 (Penicillium citrinum) cultured on the slant for 4 days, and inoculate it into 200mL culture medium [medium composition (g / L): maltose 20.0, mannitol 20.0, monosodium glutamate 10.0, KH 2 PO 4 0.5, MgSO 4 0.3, yeast extract 3.0, pH natural] in a 500mL Erlenmeyer flask, cultured on a shaker at 28°C and 160 rpm for 15 days to obtain mycelium and fermentation broth.

[0017] 2 Obtaining the extract

[0018] Separate the mycelium and fermentation broth with a c...

Embodiment 2

[0033] The test of embodiment 2 in vitro antitumor activity

[0034] Cell Proliferation Inhibition Activity Test and Cell Apoptosis Induction Activity Test

[0035] 1 Experimental samples and experimental methods

[0036] Preparation of test sample solution The test samples are pure compounds I and II isolated and refined in Example 1 above. Accurately weigh an appropriate amount of sample, and prepare a solution with the required concentration with methanol for activity measurement.

[0037] Cell lines and subculture of cells use cancer cell lines such as human lung cancer A549 cells, human liver cancer BEL-7402 cells, human leukemia HL60 cells and human leukemia MOLT-4 cells. All kinds of cells were subcultured in RPMI-1640 medium containing 10% FBS at 37°C in an incubator filled with 5% carbon dioxide.

[0038] Cell Proliferation Inhibitory Activity Test Method

[0039]Human lung cancer A549 cells and human liver cancer BEL-7402 cells in the logarithmic growth phase wer...

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Abstract

The invention relates to a preparation method and a use of two dimer citrinin compounds. The dimer citrinin compounds with novel structures are produced by adopting Penicillium Citrinum HGY1-5 in samples collected from a crater. Tests prove that the compounds can be used as a cell proliferation inhibitor, an apoptosis inducer or an anti-tumor agent.

Description

Technical field: [0001] The present invention relates to a method for producing dimeric citrinins by using Penicillium citrinum HGY1-5 (Penicillium citrinum HGY1-5) (preservation number: CCTCC M208170, preservation date: October 27, 2008); the present invention also relates to Use of the compounds in the preparation of cell proliferation inhibitors, apoptosis inducers or antitumor agents. Background technique: [0002] Citrinin is an active polyketide compound produced by Penicillium citrinum or some Aspergillus sp., and five dimers have been reported, but the five six-membered rings are fused to each other The formation of novel citrinin dimers has not been reported. The inventors have learned from studies that the crude extract of the liquid fermentation product of Penicillium citrinum HGY1-5 (Penicillium citrinum HGY1-5) (preservation number: CCTCC M 208170) has good cell proliferation inhibition and cell apoptosis after ultrasonic crushing. Death-inducing activity, and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/16C12P17/18A61K31/352A61P35/00
Inventor 顾谦群杜林朱天骄
Owner OCEAN UNIV OF CHINA
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