In vitro andin vivo antiinflammatory activities of C10 substituted anthralin derivatives

In model systems where anthralin and butanthrone have a high anti-proliferative activity, e.g., inhibition of keratinocyte metabolism in culture or inhibition of ornithine decarboxylase inductionin vivo, CD 003 is inactive. However, in the skin disease psoriasis there is both an inflammatory as well as a differentiation/proliferation component, and consequently we have evaluated anthralin and butanthrone for their potentialin vivo antiinflammatory activities. In addition, we have compared a new analogue, substituted at C10, with these two compound. Our results support the belief that modification of the anthralin structure can result in the formation of less toxic, less irritant and less staining analogues, which maintain or significantly improve upon the topical antiinflammatory properties of anthralin. The possibility that such analogues will be of use in the treatment of skin diseases with a major inflammatory component is at present being investigated.