Binding of aromatic amines to the rat hepatic Ah receptor in vitro and in vivo and the 8S and 4S estrogen receptor of rat uterus and rat liver

Journal Article · Wed Aug 01 04:00:00 EDT 1990 · Environmental Health Perspectives; (USA)

DOI:https://doi.org/10.1289/ehp.9088213· OSTI ID:5718442

Cikryt, P; Kaiser, T; Gottlicher, M ^[1]

---

1. Univ. of Wuerzburg (West Germany)

Studies on structurally related aromatic amines with different carcinogenic properties have shown that 2-acetylaminofluorene (2-AAF) and 2-acetylaminophenanthrene (AAP) inhibit the binding of 2,3,7,8-tetrachlorodibenzo-p-dioxin to the Ah receptor in vitro. The apparent inhibitor constants (K{sub i}) are 2.3 {mu}M for 2-AAF and 2.7 {mu}M for AAP. In contrast, 4-acetylaminofluorene, an isomer of 2-AAF, and trans-4-acetylaminostilbene do not bind to the rat hepatic cytosolic Ah receptor. Pretreating female Wistar rats with 2-AAF or AAP leads to the induction of the P-450 isoenzymes that are under the control of the Ah receptor. Ornithine decarboxylase activity is induced by all aromatic amines tested irrespective of their Ah receptor affinity. The aromatic amines used as model compounds do not inhibit the binding of 17-{beta}-estradiol to the 8S and 4S estrogen receptor of rat uterus or rat liver in a competition assay analyzed using sucrose density gradient centrifugation. On the other hand, the aromatic amines bind to varying extents to another estrogen-binding protein of rat liver whose function and identity is still unknown. The study demonstrates that structurally related aromatic amines in their unmetabolized form interact differentially with a cellular target protein, the Ah receptor, in vitro as well as in vivo. However, a relationship between these effects and the postulated promoting properties of 2-AAF remains to be established.

• OSTI ID: 5718442
• Journal Information: Environmental Health Perspectives; (USA), Journal Name: Environmental Health Perspectives; (USA) Vol. 88; ISSN 0091-6765; ISSN EVHPA
• Country of Publication: United States
• Language: English

Related Subjects

560300* -- Chemicals Metabolism & Toxicology
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ACETYLAMINOFLUORENES
AMINES
ANIMALS
AROMATICS
BIOLOGICAL EFFECTS
BODY
CHLORINATED AROMATIC HYDROCARBONS
DIGESTIVE SYSTEM
DIOXIN
ESTROGENS
FEMALE GENITALS
GLANDS
HALOGENATED AROMATIC HYDROCARBONS
HETEROCYCLIC COMPOUNDS
HORMONES
ISOTOPE APPLICATIONS
LIVER
MAMMALS
MEMBRANE PROTEINS
ORGANIC CHLORINE COMPOUNDS
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANIC OXYGEN COMPOUNDS
ORGANS
POLYCYCLIC AROMATIC AMINES
PROMOTERS
PROTEINS
RADIORECEPTOR ASSAY
RATS
RECEPTORS
RODENTS
STEROID HORMONES
TRACER TECHNIQUES
TUMOR PROMOTERS
UTERUS
VERTEBRATES