objective: orexin is a hypothalamic orexigenic neuropeptide, which third cerebral injection of it mainly exerts inhibitory effects on reproductive functions. it increases significantly the aromatase (cyp19) gene expression in the hypothalamus of male rats. aromatase is an enzyme which converts androgens to estradiol in the hypothalamus of rats. prenatal or neonatal exposure of females to testos...

7 alpha-(4'-Amino)phenylthio-1,4-androstadiene-3,17-dione (7 alpha-APTADD), a potent enzyme-activated irreversible inhibitor, was examined in two different human cell culture lines, MCF-7 human mammary carcinoma cells and JAr choriocarcinoma cells. Both the MCF-7 and JAr cell culture systems exhibit aromatase activity, and 7 alpha-APTADD was evaluated for its aromatase-inhibitory activity, for ...

The effects of aromatase within the brain on sexual behavior have been studied in a wide variety of species. Relatively few non-mating behaviors have been considered, despite evidence that estrogen affects many social behaviors. Testosterone promotes paternal behavior in California mouse (Peromyscus californicus) fathers, acting primarily via aromatization to estradiol. Virgin male California m...

Inhibition of aromatase is an efficient approach for the prevention and treatment of breast cancer. New A,D-ring modified steroid analogues of formestane and testolactone were designed and synthesized and their biochemical activity was investigated in vitro in an attempt to find new aromatase inhibitors and to gain insight into their structure-activity relationships (SAR). All compounds tested ...

In breast cancer, in situ estrogen production has been demonstrated to play a major role in promoting tumor growth. Aromatase is the enzyme responsible for the conversion of androgen substrates into estrogens. This enzyme is highly expressed in breast cancer tissue compared with normal breast tissue. A wine extract fraction was recently isolated from red wine that exhibited a potent inhibitory ...

Objective Orexin is a hypothalamic orexigenic neuropeptide, which third cerebral injection of it mainly exerts inhibitory effects on reproductive functions. It increases significantly the Aromatase (Cyp19) gene expression in the hypothalamus of male rats. Aromatase is an enzyme which converts androgens to estradiol in the hypothalamus of rats. Prenatal or neonatal exposure of females to testost...

In the last few years, nonsteroidal aromatase inhibitors (AIs) have been emerged as promising agents for treating hormone-dependent breast cancer in postmenopausal women because of their inhibitory effect on estrogen synthesis. Indeed, these compounds can block activity aromatase, enzyme that intervenes steps production pathway. Triazoles are core structures AIs. The nitrogen atom triazole moie...

Both 7 and 19-substituted androstenediones exhibit good inhibitory activities against aromatase. The combination effects of those two functional groups were examined by comparing the activity of19-methylthiomethoxy-7-phenylthioandrost-4-en-3,17-dione (IC50591 nM) with 19methylthiomethoxy-androst-4,6-dien-3,17-dione (IC50389 nM). The addition of a 7-phenylthio functional group leads to a slig...

catalyzed the synthesis of estrone and estradiol from the 4-en-3-one androgens androstenedione (AD) and testosterone. The aromatization process appears to proceed with three oxygenations at the C-19 position of the androgens, followed by the eventual loss of the C-19 angular methyl group and the elimination of the 1b ,2b-hydrogens, resulting in aromatization of the A-ring of the androgen molecu...