Danazol inhibits aromatase activity of endometriosis-derived stromal cells by a competitive mechanism.
OBJECTIVE
To evaluate the inhibitory effect of danazol on estrogen (E) production in endometriosis.


METHODS
Prospective randomized study.


METHODS
Academic research unit of the department of obstetrics and gynecology in a university hospital.


METHODS
Thirteen patients with endometriosis.


METHODS
Danazol was added to the culture of endometriosis-derived stromal cells or suspensions of microsomes prepared from chocolate cysts.


METHODS
The aromatase activities as well as mRNA and protein levels of aromatase in endometriosis-derived stromal cells or microsomes of endometriosis were examined.


RESULTS
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.


CONCLUSIONS
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.
Murakami
Koichi
K
Department of Obstetrics and Gynecology, Graduate School of Medical Science, Kanazawa University, Kanazawa, Ishikawa, Japan. k-muraka@med.kanazawa-u.ac.jp
Nomura
Kazuhito
K
Shinohara
Kazunori
K
Kasai
Tadayuki
T
Shozu
Makio
M
Inoue
Masaki
M
D001141:Aromatase / Q000235:genetics / Q000378:metabolism*; D047072:Aromatase Inhibitors / Q000008:administration & dosage* / Q000494:pharmacology; D015153:Blotting, Western; D002478:Cells, Cultured; D003613:Danazol / Q000008:administration & dosage* / Q000494:pharmacology; D004715:Endometriosis / Q000201:enzymology* / Q000473:pathology; D005260:Female; D006801:Humans; D007700:Kinetics; D012333:RNA, Messenger / Q000378:metabolism; D020133:Reverse Transcriptase Polymerase Chain Reaction; D017154:Stromal Cells / Q000187:drug effects / Q000201:enzymology*
D047072:Aromatase Inhibitors; D012333:RNA, Messenger; D001141:Aromatase; D003613:Danazol