The mutagenicity of anthracene, anthraquinone, and four structurally similar compounds of each was evaluated in the Ames/Salmonella microsome assay. Anthraquinone was shown to be mutagenic for strains TA1537, TA1538, and TA98 in the absence of rat liver homogenate. The four anthraquinone derivatives tested were mutagenic for TA1537 exclusively. None of the anthracenes exhibited mutagenic activity.

Rapidly proliferating normal and malignant cells had a greater initial rate of amino acid incorporation into microsomal proteins than did normal cells. The rate of micro.somal protein renewal in Novikoff hepatoma was greater than that of liver cells. The initial rates of amino acid incorporation into hepatoma and liver ribonucleoprotein particles were approximately equal. The soluble fractions ...

Starting from small molecule mTOR inhibitor Torin1, replacement of the piperazine ring with a phenyl ring resulted in a new series of mTOR inhibitors (as exemplified by 10) that showed superior potency and selectivity for mTOR, along with significantly improved mouse liver microsome stability and a longer in vivo half-life.

In the liver microsome cyanide (CN)-trapping assays, piperazine-containing compounds formed significant N-methyl piperazine CN adducts. Two pathways for the N-methyl piperazine CN adduct formation were proposed: 1) The α-carbon in the N-methyl piperazine is oxidized to form a reactive iminium ion that can react with cyanide ion; 2) N-dealkylation occurs followed by condensation with formaldehyd...

A cell fractionation procedure is described which allows the preparation from rat liver of a rough microsome population containing almost 50% of the membrane-bound ribosomes of the tissue. The fraction is not contaminated with free ribosomes or smooth microsomes, and, by various other criteria, is suitable for studies of ribosome-membrane interaction.

background: this study was performed to evaluate the levels of heavy metals in the livers and kidneys of cattle, sheep and goats from a mining region in the west of iran. methods: in this cross-sectional study, 90 samples were collected from the livers and kidneys of cattle (n=30), sheep (n=30) and goats (n=30) from a slaughterhouse in hamedan city, western iran. lead, cadmium, manganese, zinc,...

conclusions the current study findings indicated that echinacea purpurea extract played an important role in the protection against den toxicity in rats. results den induced hepatotoxicity and nephrotoxicity in all the treated animals by elevated serum alt, ast, alp and bun, creatinin and total and direct bilirubin levels. ast, bun and total and direct bilirubin significantly decreased in den +...

BACKGROUND A rapid and comprehensive metabolic stability screen at the top of a drug discovery flow chart serves as an effective gate in eliminating low value compounds. This imparts a significant level of efficiency and saves valuable resources. While microsomes are amenable to high throughput automation and are cost effective, their enzymatic make-up is limited to that which is contained in e...