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Titolo:
SUICIDE INACTIVATION OF AROMATASE IN HUMAN PLACENTA AND UTERINE LEIOMYOMA BY 5-ALPHA-DIHYDRONORETHINDRONE, A METABOLITE OF NORETHINDRONE, AND ITS EFFECT ON STEROID-PRODUCING ENZYMES
Autore:
YAMAMOTO T; TAMURA T; KITAWAKI J; OSAWA Y; OKADA H;
Indirizzi:
KYOTO PREFECTURAL UNIV MED,DEPT OBSTET & GYNECOL KYOTO 602 JAPAN MED FDN BUFFALO INC,RES INST,DEPT ENDOCRINE BIOCHEM BUFFALO NY 14203
Titolo Testata:
European journal of endocrinology
fascicolo: 6, volume: 130, anno: 1994,
pagine: 634 - 640
SICI:
0804-4643(1994)130:6<634:SIOAIH>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
ESTROGEN BIOSYNTHESIS; NORETHISTERONE; AROMATIZATION; CONVERSION; WOMEN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
19
Recensione:
Indirizzi per estratti:
Citazione:
T. Yamamoto et al., "SUICIDE INACTIVATION OF AROMATASE IN HUMAN PLACENTA AND UTERINE LEIOMYOMA BY 5-ALPHA-DIHYDRONORETHINDRONE, A METABOLITE OF NORETHINDRONE, AND ITS EFFECT ON STEROID-PRODUCING ENZYMES", European journal of endocrinology, 130(6), 1994, pp. 634-640

Abstract

Norethindrone (NET; 17 alpha-ethynyl-19-nortestosterone), a progestogen component of the contraceptive pill, irreversibly inhibits aromatase activity in human placental microsomes. However, it is known also tobe aromatized in vitro and in vivo to produce a biologically very active estrogen called ethynylestradiol (EE(2)). It is therefore inappropriate to administer a high dose of NET to estrogen-dependent cancer patients for a prolonged time period. In this study, we focused on 5 alpha-dihydronorethindrone (5 alpha-DHNET), a metabolite of NET that is not aromatizable, and the inhibitory effects of 5 alpha-DHNET on human placental and uterine leiomyoma microsomal aromatase and other steroidsynthetases. 5 alpha-Dihydronorethindrone showed weak affinity for both estrogen and progestogen receptors. It inhibited significantly human placental aromatase activity in a dose-dependent manner (K-i = 9.0 mu mol/l; Kinact = 0.024/min), as well as that of uterine leiomyoma, but did not influence cholesterol side-chain cleavage or 17 alpha-hydroxylase, 21-hydroxylase or 11 beta-hydroxylase activities. These resultssuggest that 5 alpha-DHNET may be useful as an aromatase inhibitor, whose use in large doses is expected to reduce the size of estrogen-dependent tumors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/11/20 alle ore 18:56:27