Gonadotropin-inhibitory hormone (GnIH) is a hypothalamic neuropeptide that inhibits gonadotropin secretion and socio-sexual behaviours. Oestrogen (neuroestrogen) synthesized in the brain from androgen by aromatase regulates male socio-sexual behaviours. Here we show that GnIH directly activates aromatase and increases neuroestrogen synthesis in the preoptic area (POA) and inhibits socio-sexual ...

A series of 5alpha-androst-3-enes and 3alpha,4alpha-epoxy-5alpha-androstanes were synthesized and tested for their abilities to inhibit aromatase in human placental microsomes. In these series the original C-17 carbonyl group was replaced by hydroxyl, acetyl and hydroxyimine groups. Inhibition kinetic analysis on the most potent steroid of these series revealed that it inhibits the enzyme in a ...

Aromatase catalyzes the conversion of testosterone to estradiol and is the main source of endogenous estrogen in postmenopausal women. Aromatase inhibitors (AIs) are used to treat postmenopausal women with hormone receptor-positive breast cancer. Norendoxifen [4-(1-(4-(2-aminoethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol], an active metabolite of the selective estrogen receptor modulator tamoxife...

The inhibitory effects of miconazole, an antimycotic agent, on aromatase activity for androstenedione in human placenta (105,000 X g pellet fraction) and ovary (800 X g supernatant fraction) were investigated. Various concentrations (0.1-100 microM) of miconazole, aminoglutethimide or delta 1-testololactone were added to the human placental preparation (1 mg protein) and then the mixture was in...

the conversion of androst-4-ene-3,17-dione (androstenedione) to estrone through three sequential oxygenations of the 19-methyl group. Inhibitors of aromatase have recently attracted interest not only in the treatment of advanced estrogen-dependent breast cancer but also in the elucidation of the spatial aspects of the active-site of the enzyme as well as the still unsolved mechanism of the arom...

Aromatase catalyzes the conversion of testosterone to estradiol and is the main source of endogenous estrogen in postmenopausal women. Aromatase inhibitors (AIs) are used to treat postmenopausal women with hormone receptor–positive breast cancer. Norendoxifen [4‐(1‐(4‐(2‐aminoethoxy)phenyl)-2‐phenylbut‐1‐en‐ 1‐yl)phenol], an active metabolite of the selective estrogen receptor modulator tamoxif...

Aromatase, the key enzyme responsible for estrogen biosynthesis, is present in the brain of all vertebrates. Much evidence has accumulated that aromatase is highly and exclusively expressed in proliferating mature radial glial cells in the brain of teleost fish even in adulthood, unlike in other vertebrates. However, the physiological significance of this expression remains unknown. We recently...

Objectives: This study aimed to examine the safety, effects on proliferation of hair papilla cells, and anti-inflammatory antioxidant mechanisms Artemisia sieversiana Ehrh. ex Willd. (AS) extract.Methods: Safety tests through purity testing, acute toxicity tests, repeated were performed using AS extract (ASE) which had been dried for over two years. Cell culture conducted; VEGF (vascular endoth...