BIOMAT Database Logo BIOMAT Database Logo

Effect of the aromatase inhibitor 4-hydroxyandrostene-3,17-dione progesterone synthesis by human luteal cells. 1991

L Devoto, and M Vega, and O Castro, and P Kohen
University of Chile, School of Medicine, Santiago.

The authors studied the effects of 4-hydroxyandrostene-3,17-dione (4-OHA) on progesterone (P), 17 beta-estradiol (E2), and 20 alpha-hydroxy-4-pregnen-3-one synthesis and pregnenolone accumulation in cultured human midluteal cells. A dose-dependent inhibition with and without human chorionic gonadotropin (hCG) of E2 and P production was observed. The accumulation of pregnenolone was significantly enhanced three to fourfold by 4-OHA in this culture system, as compared with control value. In addition, a sevenfold increase on pregnenolone accumulation was observed in the presence of 4-OHA plus 10 IU of hCG as compared with control values and 2.2-fold as compared with the 4-OHA treatments. These in vitro findings indicate a direct effect of 4-OHA on luteal steroidogenesis. Nevertheless, the suppressive effect of 4-OHA on P and E2 production is located at different sites of the steroidogenic pathway. In addition, the results demonstrate that hCG in the presence of 4-OHA stimulated pregnenolone accumulation, suggesting that the inhibition of P synthesis is in some steps after the formation of pregnenolone. These data indicate that the actions of 4-OHA on P or E2 formation have different inhibitory mechanisms.

UI MeSH Term Description Entries
D008184 Luteal Cells PROGESTERONE-producing cells in the CORPUS LUTEUM. The large luteal cells derive from the GRANULOSA CELLS. The small luteal cells derive from the THECA CELLS. Lutein Cells,Granulosa-Luteal Cells,Granulosa-Lutein Cells,Large Luteal Cells,Small Luteal Cells,Theca-Luteal cells,Theca-Lutein Cells,Cell, Granulosa-Luteal,Cell, Granulosa-Lutein,Cell, Large Luteal,Cell, Luteal,Cell, Lutein,Cell, Small Luteal,Cell, Theca-Lutein,Cells, Granulosa-Luteal,Cells, Granulosa-Lutein,Cells, Large Luteal,Cells, Luteal,Cells, Lutein,Cells, Small Luteal,Cells, Theca-Lutein,Granulosa Luteal Cells,Granulosa Lutein Cells,Granulosa-Luteal Cell,Granulosa-Lutein Cell,Large Luteal Cell,Luteal Cell,Luteal Cell, Large,Luteal Cell, Small,Luteal Cells, Large,Luteal Cells, Small,Lutein Cell,Small Luteal Cell,Theca Luteal cells,Theca Lutein Cells,Theca-Luteal cell,Theca-Lutein Cell,cell, Theca-Luteal,cells, Theca-Luteal
D011284 Pregnenolone A 21-carbon steroid, derived from CHOLESTEROL and found in steroid hormone-producing tissues. Pregnenolone is the precursor to GONADAL STEROID HORMONES and the adrenal CORTICOSTEROIDS. 5-Pregnen-3-beta-ol-20-one,5 Pregnen 3 beta ol 20 one
D011374 Progesterone The major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production. Progesterone, converted from PREGNENOLONE, also serves as an intermediate in the biosynthesis of GONADAL STEROID HORMONES and adrenal CORTICOSTEROIDS. Pregnenedione,Progesterone, (13 alpha,17 alpha)-(+-)-Isomer,Progesterone, (17 alpha)-Isomer,Progesterone, (9 beta,10 alpha)-Isomer
D002478 Cells, Cultured Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others. Cultured Cells,Cell, Cultured,Cultured Cell
D004092 20-alpha-Dihydroprogesterone A biologically active 20-alpha-reduced metabolite of PROGESTERONE. It is converted from progesterone to 20-alpha-hydroxypregn-4-en-3-one by the 20-ALPHA-HYDROXYSTEROID DEHYDROGENASE in the CORPUS LUTEUM and the PLACENTA. Dihydroprogesterone,20 alpha-Dihydroprogesterone,20 alpha-Hydroxy-4-Pregnen-3-One,20 alpha-Hydroxyprogesterone,20-alpha-Hydroxyprogesterone,20alpha-Hydroxypregn-4-Ene-3-One,Pregn-4-en-3-one, 20-alpha-hydroxy-,20 alpha Dihydroprogesterone,20 alpha Hydroxy 4 Pregnen 3 One,20 alpha Hydroxyprogesterone,20-alpha-hydroxy- Pregn-4-en-3-one,20alpha Hydroxypregn 4 Ene 3 One,Pregn 4 en 3 one, 20 alpha hydroxy
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004958 Estradiol The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. 17 beta-Estradiol,Estradiol-17 beta,Oestradiol,17 beta-Oestradiol,Aerodiol,Delestrogen,Estrace,Estraderm TTS,Estradiol Anhydrous,Estradiol Hemihydrate,Estradiol Hemihydrate, (17 alpha)-Isomer,Estradiol Monohydrate,Estradiol Valerate,Estradiol Valeriante,Estradiol, (+-)-Isomer,Estradiol, (-)-Isomer,Estradiol, (16 alpha,17 alpha)-Isomer,Estradiol, (16 alpha,17 beta)-Isomer,Estradiol, (17-alpha)-Isomer,Estradiol, (8 alpha,17 beta)-(+-)-Isomer,Estradiol, (8 alpha,17 beta)-Isomer,Estradiol, (9 beta,17 alpha)-Isomer,Estradiol, (9 beta,17 beta)-Isomer,Estradiol, Monosodium Salt,Estradiol, Sodium Salt,Estradiol-17 alpha,Estradiol-17beta,Ovocyclin,Progynon-Depot,Progynova,Vivelle,17 beta Estradiol,17 beta Oestradiol,Estradiol 17 alpha,Estradiol 17 beta,Estradiol 17beta,Progynon Depot
D005260 Female Females
D006063 Chorionic Gonadotropin A gonadotropic glycoprotein hormone produced primarily by the PLACENTA. Similar to the pituitary LUTEINIZING HORMONE in structure and function, chorionic gonadotropin is involved in maintaining the CORPUS LUTEUM during pregnancy. CG consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is virtually identical to the alpha subunits of the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity (CHORIONIC GONADOTROPIN, BETA SUBUNIT, HUMAN). Chorionic Gonadotropin, Human,HCG (Human Chorionic Gonadotropin),Biogonadil,Choriogonadotropin,Choriogonin,Chorulon,Gonabion,Human Chorionic Gonadotropin,Pregnyl,Gonadotropin, Chorionic,Gonadotropin, Human Chorionic
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

Related Publications

L Devoto, and M Vega, and O Castro, and P Kohen
Synthesis of 2,2-dimethyl-4-hydroxy-4-androstene-3,17-dione as an inhibitor of aromatase.
January 1990, Journal of enzyme inhibition,
L Devoto, and M Vega, and O Castro, and P Kohen
Metabolism of the aromatase inhibitor 4-hydroxy-4-androstene-3,17-dione by male rhesus monkeys.
August 1981, Journal of steroid biochemistry,
L Devoto, and M Vega, and O Castro, and P Kohen
Aromatase inhibition by 4-thiosubstituted-4-androstene-3,17-dione derivatives.
January 1990, Journal of steroid biochemistry,
L Devoto, and M Vega, and O Castro, and P Kohen
Synthesis of 10 beta-(1'-azirinyl)estr-4-en-3,17-dione as an aromatase inhibitor.
March 1996, Steroids,
L Devoto, and M Vega, and O Castro, and P Kohen
Synthesis and evaluation of 4-substituted-4-androstene-3,17-dione derivatives as aromatase inhibitors.
August 1995, The Journal of steroid biochemistry and molecular biology,
L Devoto, and M Vega, and O Castro, and P Kohen
Synthesis and evaluation of analogues of 4-androstene-3,17-dione as aromatase inhibitors.
January 1987, Steroids,
L Devoto, and M Vega, and O Castro, and P Kohen
Novel 19-(cyclopropylamino)-androst-4-en-3,17-dione: a mechanism-based inhibitor of aromatase.
January 1996, Journal of enzyme inhibition,
L Devoto, and M Vega, and O Castro, and P Kohen
The effect of the aromatase inhibitor, 4-(phenylthio)-4-androstene-3,17-dione, on dimethylbenz(A)anthracene-induced rat mammary tumors.
January 1989, Journal of steroid biochemistry,
L Devoto, and M Vega, and O Castro, and P Kohen
Inactivation of aromatase in vitro by 4-hydroxy-4-androstene-3,17-dione and 4-acetoxy-4-androstene-3,17-dione and sustained effects in vivo.
December 1981, Steroids,
L Devoto, and M Vega, and O Castro, and P Kohen
Aromatase inhibitors III. Studies on the antifertility effect of 4-acetoxy-4-androstene-3,17-dione.
April 1978, Biology of reproduction,
Copied contents to your clipboard!