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Glucocorticoid derivatives have been clinically used to treat inflammatory and/or immune-malfunctional diseases. Glucocorticoid derivatives bind to cytosolic receptor protein, which is transformed to DNA-binding form. This glucocorticoid-receptor complex moves and binds to GRE region of nulear DNA. Through transcriptional control of various proteins, glucocorticoidal, anti-inflammatory and immunosuppressive activities are expressed. The mechanism of anti-inflammation by glucocorticoid derivatives involves alteration of inflammation-related cell traffics and regulation of production of inflammatory mediators from these cells. And production of lipocortin having PLA2 inhibitory action might be an important factor in anti-inflammatory activity of glucocorticoids. Glucocorticoidsaffect more profoundly on cellular immuniy than humoral immunity. And regulation of cytokine production and ex. cretion is one of the essential mechanism in immunosuppressive effect of the derivatives. Glucocorticoid derivatives having anti-inflammatory and/or immune suppressive activity might show adverse systemic side-effects, expecial. ly when prolonged therapy or massive dose therapy is used. To overcome this problem, local anti-inflammatory steroid derivatives have been developed, which may lead to safer use of anti-inflamrnatoty steroids.
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