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Citrinin compound dicitrinone D and its application in malignant melanoma

A technology for malignant melanoma, compounds, applied in the direction of microorganism-based methods, biochemical equipment and methods, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2019-07-09
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have found that the citrinin compounds shown have anti-malignant melanoma activity, and there is no report on the anti-proliferation activity of this compound on human malignant melanoma cell A375, so there is no related drug on the market.

Method used

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  • Citrinin compound dicitrinone D and its application in malignant melanoma
  • Citrinin compound dicitrinone D and its application in malignant melanoma
  • Citrinin compound dicitrinone D and its application in malignant melanoma

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Fermentative production and separation and purification of the compound of embodiment 1

[0021] 1 Fermentation production

[0022] Fermentation culture of production bacteria: according to the conventional method of cultivating microorganisms, take Penicillium citrinum ( Penicillium citrinum ) IBPT-5 (preserved in China Center for Type Culture Collection on December 25, 2013, address: Wuhan University, Wuhan, deposit number: CCTCC NO: M 2013713) appropriate amount, inoculated on PDA solid slant medium at 28 Cultivate in an incubator for 4 days.

[0023] Get the Penicillium citrinum ( Penicillium citrinum ) appropriate amount of IBPT-5, inoculated into 400mL culture medium [composition of culture medium (g / L): mannitol 20.0, yeast extract 3.0, maltose 20.0, monosodium glutamate 10.0, glucose 10.0, KH 2 PO 4 0.5, MgSO 4 0.3, NaCl 30.0 constant volume] in a 1000mL Erlenmeyer flask, after 30 days of static culture at 28°C, the mycelia and fermentation broth were ...

Embodiment 2

[0031] Example 2 Test of Anti-tumor Activity in Vitro

[0032] 1 Experimental samples and experimental methods

[0033] Preparation of the tested sample solution The test sample is the pure product of the compound separated and refined in the above-mentioned implementation 1. Precisely weigh an appropriate amount of sample, and prepare a solution with the required concentration with DMSO for activity measurement.

[0034] Tumor cell lines were used for the subculture of cell lines and cells, and RPMI 1640 medium containing 10% FBS was used for malignant melanoma cells at 37°C in 5% CO 2 Subculture in an incubator.

[0035] Cell Proliferation Inhibitory Activity Test Method

[0036] WST-1 method Take tumor cells in the logarithmic growth phase, adjust the cell density to 5×10 per ml 4 Cells were inoculated into 96-well cell culture plates at 100 μL per well, and placed in 5% CO at 37°C. 2 cultured overnight in an incubator. Aspirate the supernatant, add 100 μL of sample-c...

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Abstract

The invention discloses a citrinin compound dicitrinone D and an application thereof in respect of malignant melanoma. The citrinin compound dicitrinone D has a structural formula shown in the description. The compound is obtained by culturing penicillium citrinum IBPT-5 through fermentation to obtain a fermented object, and performing separation and purification to the fermented object. It is proved by the experiments that the compound has preferable antitumor activity to human malignant melanoma cells A375, and can be used to prepare a malignant melanoma cell proliferation inhibition medicine or an antitumor medicine, which are used to research malignant melanoma.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a citrinin compound dicitrinone D and its application in malignant melanoma. Background technique [0002] Citrinin is a kind of nitrogen-containing organic compound produced by biological secondary metabolism. There are many kinds of citrinin in nature, most of which come from plants, so it is also called plant alkaloid. Citrinin has important physiological effects on humans and animals, including anti-asthma and antitussive, hypoglycemic, hypolipidemic, antibacterial, antitumor, analgesic, etc., among which the antibacterial and antitumor activities are the most prominent. The natural structure of citrinin is an important source for discovering lead compounds in the research of innovative drugs. There are nearly a hundred kinds of citrinin drugs currently used in clinical practice. Studies have found that some marine fungi can produce citrinin with novel structure and go...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D407/06C12P17/16A61K31/366A61P35/00C12R1/80
CPCC07D407/06C12P17/162
Inventor 陈立赵杨杨王丙帅周彤张其清
Owner FUZHOU UNIV
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