Inhibition of androgen aromatization in human breast cancer |
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| Affiliation: | 1. Xiangya School of Pharmaceutical Sciences, Hunan Key Laboratory of Pharmacogenetics, Central South University, Changsha, 410013, P. R. China;2. School of Pharmacy, Hangzhou Normal University, Hangzhou, 311121, PR China;3. Key Laboratory of Elemene Class Anti-Cancer Chinese Medicines, Engineering Laboratory of Development and Application of Traditional Chinese Medicines, Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou, 311121, P.R. China;4. INSERM U1231, Label LipSTIC and Ligue Nationale contre le Cancer, Dijon, France;5. Faculté de médecine, Université de Bourgogne, Dijon, Centre de lutte contre le cancer Georges François Leclerc, 21000, Dijon, France;6. Université de Franche Comté, France, University Hospital of Besançon (CHU), France |
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| Abstract: | The inhibitory activity of aminoglutethimide, 4-hydroxy-androstenedione and 7α-(4'-amino) phenylthioandrostenedione on human placental and mammary tumor aromatase activity was examined. [14C]-Androstenedione was incubated with placental microsomes and mammary tumor homogenates in the presence of an NADPH generating system with or without inhibitor. All three inhibitors were equally effective in inhibiting microsomal placental aromatase at various inhibitor concentrations. Inhibitions of mammary tumor aromatase using 12 μM inhibitor concentrations were essentially similar to results on placental aromatase inhibition and ranged from 81–97% inhibition. These findings are discussed in regard to the potential clinical use of aromatase inhibitors in the treatment of estrogen dependent metastatic breast carcinoma. |
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