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Use of compound metabolized by diaporthe phaseolorum fungus

A compound and fungal technology, applied in the field of compounds produced by fungal metabolism, can solve problems such as unreported anti-tumor physiological activities

Inactive Publication Date: 2007-08-29
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Compound acetic acid 2-(8-methyl-9-oxa-bicyclo[4.2.1]nona-2,4-dien-7-yl)-6-oxo-3,6-dihydro-2H-pyran -3-yl ester (Mycoepoxydiene) was first reported in 1999 (Ping Cai, Andrew T et al. Mycoeoxydiene represents a novel class of fungal metabolites [J]. Tetrahedron Letters, 1999, 40: 1479-1482), it was derived from a Isolated from the fermentation broth of the rare fungus OS-F66617, but it has no anti-tumor physiological activity reported in the literature

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0022] Take the strains on the slant and inoculate them in semi-seawater PD and cultivate them until fermentation. The fermentation broth is filtered through gauze to remove the bacteria, and the supernatant is collected. The collected supernatant is divided into 3L conical flasks (1L / bottle), and the same The volume of ethyl acetate was stirred and extracted for 6 hours; the organic phase was collected and concentrated under reduced pressure at 50°C with a rotary evaporator to a paste. Get the silica gel (80 order) that quality is 8 times of loading sample amount, use dry method to pack column, column internal diameter is selected as 6cm, and column length is 8cm, and the sedimentation of silica gel is sucked with vacuum pump to no longer change; The sample after concentration is used After mixing the sample with silica gel (60 mesh), it is compacted and spread flat on the cylinder surface, and then the surface of the sample is covered with sea sand with a thickness of 1 cm. ...

Embodiment 2

[0028] Its preparation process is similar to Example 1, the difference is that the collected supernatant is divided into 3L Erlenmeyer flasks (1L / bottle), and the addition of ethyl acetate with a volume of 0.8 times the fermentation broth is stirred and extracted for 10h; the organic phase is collected, Concentrate under reduced pressure at 45°C with a rotary evaporator to a paste. Take 60-mesh silica gel whose mass is 6 times of the sample volume, and pack the column by dry method. The concentrated sample was mixed with 100-mesh silica gel, compacted and spread on the cylinder surface, and then covered with sea sand with a thickness of 1 cm on the sample surface. The temperature for concentration under reduced pressure was 55°C. When performing further silica gel column separation, take 60 mesh silica gel whose mass is 8 times of the loading amount.

[0029] The antitumor activity of the compound was determined by cytotoxic MTT assay, and it was found that its IC on human o...

Embodiment 3

[0031] Its preparation process is similar to Example 1, and its difference is that the collected supernatant is divided into 3L Erlenmeyer flasks (1L / bottle), adding ethyl acetate whose volume is 1.2 times of the fermentation broth and stirring and extracting for 15h; collecting the organic phase, Concentrate under reduced pressure at 55°C with a rotary evaporator to a paste. Take 100-mesh silica gel whose mass is 10 times of the sample volume, and pack the column by dry method. The concentrated sample was mixed with 80-mesh silica gel and spread flat on the cylinder surface, and then covered with sea sand with a thickness of 1 cm on the sample surface. The temperature for concentration under reduced pressure was 45°C. When performing further silica gel column separation, take 100 mesh silica gel whose mass is 6 times of the loading amount.

[0032] The antitumor activity of the compound was determined by cytotoxic MTT assay, and it was found that its IC on human oral dermoi...

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Abstract

The invention relates to the application of the compound metabolized of fungus between kidney beans. The analysis would take X-Ray, MS and biological activity testing processes. According to the test of biological testing of compound Mycoepoxydiene, using MTT method to testing the anti-tumor activity, the human oral cavity cancer KB cell is IC50<6.25ug / ml, and the human osteosarcoma MG63 cell is IC50=34.6ug / ml. The compound Mycoepoxydiene has anti-tumor activity, and could be used in anti-tumor medicine or the primer of other biology activity.

Description

[0001] This application is a divisional application with the application number 200410084809.3, the filing date is 2004.10.1, and the title of the invention is a compound metabolized by the fungus Mesenterocystis bean and its preparation method. technical field [0002] The present invention relates to a compound produced by the metabolism of fungi, especially a compound acetic acid 2-(8-methyl-9-oxa-bicyclo[4.2.1] produced by the metabolism of the newly isolated Mesenterocystis bean HLY2 Nona-2,4-dien-7-yl)-6-oxo-3,6-dihydro-2H-pyran-3-yl ester (Mycoepoxydiene) in the preparation of antitumor drugs or other biologically active leads Applications. Background technique [0003] Diaporhe paseolorum was isolated from mangrove leaf rot in the mangrove ecological zone of Caoputou Village, Fugong Town, Fugong Town, Jiulongjiangkou, Zhangzhou City, Fujian Province. Beijing: Science Press, 1998), this bacterial strain grows well on semi-seawater formula PD (potato agar medium) medi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/08C12P17/18A61K31/366A61P35/00
Inventor 林昕黄耀坚徐庆研郑忠辉宋思扬苏文金
Owner XIAMEN UNIV
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