Procymidone is a dicarboximide fungicide structurally related to vinclozolin. In vitro, procymidone inhibits DHT-induced transcriptional activation at 0.2 |imol/l in CV-1 cells cotransfected with the human AR and a mouse mammary tumor virus (MMTV)-luciferase reporter gene; at 10 |imol/l, DHT-in-duced transcriptional activity is completely inhibited . Using a Chinese hamster ovary (CHO) cell promoter interference assay, we demonstrated that
1 |imol/l procymidone also blocked DHT-induced AR-DNA binding. The fact that these effects were seen at a concentration more than a 1000-fold below the Ki of the parent material for AR suggests that a procymidone metabolite(s) is the active antiandrogenic compound(s).
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