Danazol inhibits aromatase activity of endometriosis-derived stromal cells by a competitive mechanism.

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Murakami K, Nomura K, Shinohara K, Kasai T, Shozu M, Inoue M

Danazol inhibits aromatase activity of endometriosis-derived stromal cells by a competitive mechanism.

Fertil Steril. 2006 Aug;86(2):291-7. doi: 10.1016/j.fertnstert.2005.12.074. Epub 2006 Jun 27.

PubMed ID

16806212 [ View in PubMed

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Abstract

OBJECTIVE: To evaluate the inhibitory effect of danazol on estrogen (E) production in endometriosis. DESIGN: Prospective randomized study. SETTING: Academic research unit of the department of obstetrics and gynecology in a university hospital. PATIENT(S): Thirteen patients with endometriosis. INTERVENTION(S): Danazol was added to the culture of endometriosis-derived stromal cells or suspensions of microsomes prepared from chocolate cysts. MAIN OUTCOME MEASURE(S): The aromatase activities as well as mRNA and protein levels of aromatase in endometriosis-derived stromal cells or microsomes of endometriosis were examined. RESULT(S): Danazol treatment with a concentration greater than 10(-6) M significantly suppressed aromatase activity of endometriosis-derived stromal cells under basal and prostaglandin E(2) (PGE(2))-stimulated conditions. Danazol (10(-5) M) did not affect mRNA and protein levels of aromatase. Danazol competitively inhibited aromatase activity (by 1.7 x 10(-6) M of calculated Ki and 2.9 x 10(-5) M of Ki') of endometriosis microsomes. CONCLUSION(S): Danazol competitively inhibited aromatase activity in endometriosis-derived stromal cells without affecting either the mRNA or protein levels of aromatase. These results indicate the efficacy of local application of danazol to endometriotic lesions.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Danazol	Cytochrome P450 19A1	Protein	Humans	Unknown	Inhibitor	Details