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

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...

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 have the advantages of clear targets like TNF-α biological antagonists, and do not have the disadvantages of inconvenient administration. They are currently novel drugs to be developed urgently. No small-molecule drug against TNF-α overexpression has come out

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