Dienogest, a synthetic steroid, suppresses both embryonic and tumor-cell-induced angiogenesis.

摘要: Abstract Orally administered dienogest (17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one) is efficacious against human hormone-dependent cancer xenografts in severely immunodeficient mice and rats with experimental endometriosis, but its mechanisms of action remain unclear. We assessed the effect on angiogenesis, because these two diseases that are sensitive to known be angiogenesis-dependent. Topical treatment dose-dependently inhibited embryonic ID50 value being 6.4 nmol/egg. Oral administration (1 mg kg−1 day−1) for 5 consecutive days significantly suppressed angiogenesis induced by S-180 mouse tumor cells dorsal air sac assay. In vitro experiments showed at concentrations up 10 μM had little or no proliferation plasminogen activator activity formation tube-like structures microvascular endothelial cells. These results suggest a new, orally active antagonist anti-angiogenic may involved therapeutic effects endometriosis we observed previously.