Binding of 2-hydroxybenzo(a)pyrene to estrogen receptors in rat cytosol.
نویسندگان
چکیده
The potent carcinogen 2-hydroxybenzo(a)pyrene (2-OH-BP) competes for binding to the estrogen receptor in the cytosol of rat uterus and liver. The dissociation constant (K1) for this interaction is congruent to 2 X 10(-5) M. In contrast, 4-hydroxybenzo(a)pyrene does not bind to the estrogen receptor; 1-hydroxybenzo(a)pyrene, 5-hydroxybenzo(a)pyrene, 6-hydroxybenzo(a)pyrene, and 12-hydroxybenzo(a)pyrene bind less tightly than does 2-OH-BP. These five chemicals are not carcinogenic. We suggest that the estrogen receptor may mediate the carcinogenic effect of 2-OH-BP or of related chemicals. One possibility is that the receptor might convey 2-OH-BP to specific sites in DNA.
منابع مشابه
Inhibition of Microsome-Mediated Binding of Benzo (Α) Pyrene to "Dna By Cytosolic Reaction From Liver And Skin Rats in Cvitro
Purpose: The aim of this study was to evaluate the effect of age on the capacity of liver and epiderm of adult and weanging rats in transformation of Benzo (α) Pyrene. Materials and Methods: In a metabolic activiation assay system, cytochorome P-50 (from microsomal fraction) catalyses the formation of reactive epoxide of BaP which can then interact with exogenous DNA The capacity of cytochrome...
متن کاملMICROSOME-MEDIATED BENZO[A]PYRENE-DNA BINDING AND INHIBITION BY CYTOSOLIC FRACTIONS FROM LIVER AND SKIN OF ADULT AND WEANLING RATS
Biotransformation of benzo[a]pyrene (BaP) in the presence of microsomal fractions derived from liver and epiderm of adult and weanling rats was examined. The aim of this study was to evaluate the effect of age on the capacity of two organs in transformation of BaP. Subcellular fractions were prepared from skin and liver by ultracentrifugation and were used as the source of BaP metabolizing enzy...
متن کاملMetabolism and macromolecular binding of carcinogenic and noncarcinogenic metabolites of benzo(a)pyrene by hamster embryo cells.
The metabolism and macromolecular binding of four metabolites of benzo(a)pyrene in hamster embryo fibroblasts has been studied. Two noncarcinogenic phenolic derivatives, 3-hydroxybenz(a)pyrene and 9-hydroxybenzo(a)pyrene, are rapidly metabolized, primarily to their respective glucuronic acid conjugates and other H2O-soluble conjugates (78.4 to 80.8% of total radioactivity). Water-soluble conjug...
متن کاملIntestinal bioavailability and biotransformation of 3-hydroxybenzo(a)pyrene in an isolated perfused preparation from channel catfish, Ictalurus punctatus.
The intestinal bioavailability and biotransformation of 3-hydroxybenzo(a)pyrene, a major metabolite of benzo(a)pyrene in many animal species, was investigated in an in situ isolated intestinal preparation from the channel catfish, and in vitro with preparations of catfish intestine and blood. 3-Hydroxybenzo(a)pyrene was a good substrate for adenosine 3'-phosphate 5'-phosphosulfate (PAPS)-sulfot...
متن کاملEffects of chronic ethanol consumption on benzo(a)pyrene metabolism and glutathione S-transferase activities in Syrian golden hamster cheek pouch and liver.
The metabolism of benzo(a)pyrene (BaP) by hepatic or cheek pouch epithelium microsomes obtained from Syrian golden hamsters which had been consuming an ethanol-containing liquid diet for 4 wk and from pair-fed controls was measured. Glutathione S-transferase activity with 1-chloro-2,4-dinitrobenzene or (+/-)-r-7,t-8-dihydroxy-t-9,10-epoxy-7,8,9,10-tetrahydrobenzo(a)pyrene as substrates was meas...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Cancer research
دوره 46 5 شماره
صفحات -
تاریخ انتشار 1986