Qiaonan mycin serving as fungus metabolism product and preparation method and application thereof

A technology of qiaonanmycin and metabolites, which can be used in the field of pharmacy and can solve the problems of high price and inconvenient administration.

Active Publication Date: 2012-07-18
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, such biological antagonists are expensive, and the cost of treatment for one year is about 10,000 US dollars, and they can only be given by injection, which brings a lot of inconvenience to patients.
Oral TNF-α inhibitors of small molecules ha...

Method used

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  • Qiaonan mycin serving as fungus metabolism product and preparation method and application thereof
  • Qiaonan mycin serving as fungus metabolism product and preparation method and application thereof
  • Qiaonan mycin serving as fungus metabolism product and preparation method and application thereof

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Embodiment Construction

[0023] The following embodiments will further illustrate the present invention in conjunction with the accompanying drawings.

[0024] The fungal metabolite qiaonanmycin is isolated and purified from the Aspergillus CM9a Aspergillus sp.CM9a of Cephalotaxus mannii. in Xishuangbanna, Yunnan Province, which belongs to the derivative of quinoline carboxamide, and its molecular formula is C 22 h 18 N 4 o 4 , molecular weight 402, white powder, specific rotation [α] D =-27.9 (C=0.43, in MeOH), easily soluble in methanol, poorly soluble in low polarity solvents such as chloroform. The structure of this compound has not been reported so far. On the cell model for TNF-α antagonist screening, the compound exhibits good antagonistic activity.

[0025] The preparation method of the fungal metabolite bridgenamycin is as follows:

[0026] 1) Fermentation produces:

[0027] Make a seed plate, inoculate the fungus in a streaking manner, and ferment and cultivate the fungus; the ferment...

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Abstract

The invention discloses a Qiaonan mycin serving as a fungus metabolism product and a preparation method and an application thereof, relating to a separating and purifying method of a novel structural compound of an antitumor necrosis factor and an application thereof. The Qiaonan mycin serving as the fungus metabolism product is shown as C22H18N4O4, which has the molecular weight 402, belongs to a derivative of quinolineformylamine, is white powder, has the specific rotatory power [alpha]D of -27.9(C=0.43, in MeOH), is easily dissolved into methanol, and is hardly dissolved into low-polarity solvents such as chloroform and the like. The structure of the compound is not reported till now. On a cell model for screening a TNF-alpha antagonist, the compound shows high antagonistic activity. The Qiaonan mycin serving as the fungus metabolism product can be used for preparing an anti-inflammatory medicament or other bioactive primers. The Qiaonan mycin serving as the fungus metabolism product can be used for preparing an anti-inflammatory medicament or other bioactive primers by fermenting, generating, separating and purifying.

Description

technical field [0001] The invention relates to a separation and purification method and application of a new structural compound of anti-tumor necrosis factor, which belongs to the category of pharmacy. technical background [0002] The overexpression of tumor necrosis factor-alpha (TNF-α) is an important cause of various diseases that cannot be completely cured in clinical practice, such as internal rheumatoid arthritis, Rohn's disease, and ischemic necrosis of brain cells. . At present, the treatment methods for such diseases are to delay and prevent the progression of the disease and relieve the pain caused by the disease, including the use of glucocorticoids (such as prednisone), non-steroidal anti-inflammatory drugs (such as COX-2 inhibitors) And immunosuppressants (such as abatacept), etc., but these drugs can not cure the disease. Antibody antagonist drugs developed for the protein properties of TNF-α, such as Etanercept, Infliximab, Adalimumab, etc., can utilize t...

Claims

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Application Information

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IPC IPC(8): C07D498/22C12P17/18A61P29/00C12R1/66
Inventor 徐庆妍刘军亮胡志钰黄耀坚郑忠辉
Owner XIAMEN UNIV
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