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Studies of estrogen metabolism, formation of DNA adducts, carcinogenicity, cell transformation and mutagenicity have led to the hypothesis that reaction of certain estrogen metabolites, predominantly catechol estrogen-3,4-quinones, with DNA can generate the critical mutations initiating breast, prostate and other cancers. The endogenous estrogens estrone(More)
Gamma linolenic acid (GLA), a polyunsaturated fatty acid, promoted lipid peroxidation in Raji lymphoma suspension cultures, in a dose (10 microM-100 microM) and time-dependent (4 h-48 h) manner. The increase in lipid peroxidation could be correlated to an increase in cytotoxicity. The plant flavonoids (quercetin, luteolin, butein, rutin) and the fat-soluble(More)
Flavonoids, the dominant colouring pigments of plants, as well as the related polyphenol tannic acid significantly inhibit single-strand breaks in plasmid pBR322 DNA induced by singlet molecular oxygen ((1)O2). This reactive species of oxygen was generated in an aqueous buffer system by the thermal dissociation of the endoperoxide of(More)
2,4-Toluenediamine [(TDA) CAS: 95-80-7] was administered to rats pretreated with the microsomal enzyme inducers phenobarbital (PB), beta-naphthoflavone (beta NF), or 3-methylcholanthrene (MCA). The 24-hour urines of male F344 rats were examined for their mutagenic potency by means of the Salmonella assay, with the Aroclor 1254-pretreated rat liver S-9(More)
In vitro studies showed that several flavonoids, tannic acid, gallic acid and fat-soluble vitamins inhibited HeLa and Raji lymphoma cell growth. The inhibition trend exhibited by these compounds was similar for both cell lines, and their growth was inhibited dose dependently. Butein, (10 microM), the most potent anti-proliferative agent, exerted 30% growth(More)
The effect of thirty-one flavonoids on monolayer HeLa cell proliferation was studied and their structure activity relationship was rationalised. The flavones, flavonols and chalcones possessing the C2,3-double bond were the most potent cytotoxic groups of compounds. The IC50 values for 2-hydroxy chalcone (the most potent flavonoid) and the cytotoxic drug(More)
Salmonella mutagenesis assays were used to evaluate the mutagenicity of several chemical carcinogens as mediated by liver S-9 fractions from rats fed a choline-supplemented (CS) or choline-devoid (CD) diet. The liver S-9 fraction from CD diet-fed rats was found to have a significantly decreased ability to activate 2-acetylaminofluorene (2-AAF),(More)
Vicriviroc (formerly SCH 417690), a CCR5 receptor antagonist, is currently under investigation for the treatment of HIV infection. Human liver microsomes (HLM) metabolized vicriviroc via N-oxidation (M2/M3), Odemethylation (M15), N, N-dealkylation (M16), Ndealkylation (M41) and carboxylic acid formation (M35b/M37a). The metabolites generated under in vitro(More)
An external source electrospray ionization (ESI) Fourier transform ion cyclotron resonance (FTICR) mass spectrometer has been used to study the organometallic complexes Ag 2(DPM) 2(BF4) 2 (where DPM = bis-diphenylphosphinomethane), Ag 2 (DPM) 3 (BF4) 2 and Ru(ll)(bpy)3 (PF6)2 (where bpy = 2,2'-bipyridyl). The high mass resolution and accurate mass(More)
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