As a result of studies of guinea-pig liver testosterone 17/J-dehydrogenase (NADP+) (EC 1.1.1.64), anew testosterone 17f8-dehydrogenase was discovered. The new enzyme was purified to a single homogeneous protein from the 105000g-supernatant fraction of guinea-pig liver by (NH4)2SO4 fractional precipitation and two gel-filtration stages, DEAE-cellulose column chromatography and hydroxyapatite col...

A new one-dimensional NiII coordination polymer of 1,3,5-tris-(imidazol-1-ylmeth-yl)benzene, namely catena-poly[[aqua-(sulfato-κO)hemi(μ-ethane-1,2-diol-κ2O:O')[μ3-1,3,5-tris-(1H-imidazol-1-ylmeth-yl)benzene-κ3N3,N3',N3'']nickel(II)] ethane-1,2-diol monosolvate monohydrate], {[Ni(SO4)(C18H18N6)(C2H6O2)0.5(H2O)]·C2H6O2·H2O} n , was synthesized and characterized by elemental analysis, IR spectros...

The metabolism and mutagenic activation of the model carcinogens benzo(a)pyrene [B(a)P] and 2-acetylaminofluorene (AAF) by human and rat kidney cells were measured. A slicing technique followed by enzyme digestion was utilized to obtain the kidney cells. Although levels of total metabolism of B(a)P by rat and human kidney cells were similar, analysis of specific metabolites of B(a)P indicated t...

We have used flow cytometry to monitor the alterations in cell cycle distributions caused by chemical carcinogens. Two closely derived mouse liver cell strains growing in cub lure have been studied with regard to the effect of benzo(a) pyrene and derivatives of benzo(a)pyrene on DNA synthe sis. The derivatives tested were (±)-trans-7a,8$-dihydroxy 7,8-dihydrobenzo(a)pyrene; (±)-7a,8$-dihydrox...

Metabolism of the (+)-(3S,4S)and (-)-(3R,4R)-enantiomers of trnns-3,4-dihydroxy-3,4-dihydrobenz[a]anthracene has been examined with liver microsomes from control rats, as well as rats treated with 3-methylcholanthrene or phenobarbital and by a highly purified and reconstituted system containing cytochrome P-450, and epoxide hydrolase. In contrast to the metabolism of the related (-)-benzo[a]pyr...

Benzo[a]pyrene 7,8-diol 9,10-epoxide adducts in DNA are implicated in mutagenesis, and their formation from the diol epoxides and subsequent incorrect replication by human DNA polymerases provide an attractive mechanism for the induction of cancer by this highly carcinogenic hydrocarbon and its diol epoxide metabolites. Here, we describe the crystal structure of such an adduct at the exocyclic ...

The mutagenic activity of benzo(c)phenanthrene and some of its known and potential metabolites was evaluated in bac terial and mammalian cells either in the presence or absence of a metabolic activation system. trans-3,4-Dihydroxy-3,4-di hydrobenzo(c)phenanthrene [benzo(c)phenanthrene 3,4-di hydrodiol] was metabolized by a cytochrome P-450-dependent monooxygenase system to products which were s...

In this study, androgen UDP-glucuronyl transferase (UDPGT) activity was determined in microsomes of human liver, skin, and prostate. Androgen UDPGT activity was highest in the liver microsomes using 5 alpha-androstane-3 alpha, 17 beta-diol (3 alpha DIOL), androsterone (AN) and dihydrotestosterone (DHT) as substrates. The Km and Vmax values and enzyme velocity at the physiological concentration ...

The reactivity of 3-substituted 4-methyl-4-(3-oxobutyl)-2-cyclohexen-1-ones (1) in the presence of a combination of a Lewis acid and a 1,2-diol was studied. The results suggest several factors that influence 6-membered ring formation, including two types of intramolecular aldol reaction and intramolecular 1,4-addition, due to the C3-substituent, Lewis acid, and the presence of diol. In this stu...