Rotundifolone, a monoterpene isolated from the essential oil of the leaves of Mentha x villosa, is a constituent of several essential oils and known to have antinociceptive activity. Our recent study demonstrated that the analogues of rotundifolone showed also a significant antinociceptive effect. In the present report, to investigate the correlation between the structure and antinociceptive ac...

Epoxide hydrolase and glutathione S-transferase activities toward trans- and cis-stilbene oxides were measured in 3 strains of Drosophila melanogaster. Differences in age dependence, substrate selectivity and subcellular location were detected suggesting the presence of multiple forms of these enzymes. In addition, interstrain differences indicate the presence of genetic variation for epoxide h...

BACKGROUND The first-pass metabolism of foreign compounds in the lung is an important protective mechanism against oxidative stress. We investigated whether polymorphisms in the gene for microsomal epoxide hydrolase (mEPHX), an enzyme involved in this protective process, had any bearing on individual susceptibility to the development of chronic obstructive pulmonary disease (COPD) and emphysema...

The major mutational hot spots in human cancers occur at CpG sequences in the p53 gene. It is generally presumed that the majority of mutations at these sites result from the endogenous deamination of methylated cytosine. Using a UvrABC incision method, we have found that cytosine methylation greatly enhances guanine alkylation at all CpG sites in the p53 gene by a variety of carcinogens, inclu...

HC toxin, the host-selective toxin of the maize pathogen Cochliobolus carbonum, inhibited maize histone deacetylase (HD) at 2 microM. Chlamydocin, a related cyclic tetrapeptide, also inhibited HD activity. The toxins did not affect histone acetyltransferases. After partial purification of histone deacetylases HD1-A, HD1-B, and HD2 from germinating maize embryos, we demonstrated that the differe...

The distribution of rat liver epoxide hydrolase in various subcellular fractions was investigated by immuno-electron-microscopy. Ferritin-linked monospecific anti-(epoxide hydrolase) immunoglobulins bound specifically to the cytoplasmic surfaces of total microsomal preparations and smooth and rough microsomal fractions as well as the nuclear envelope. Specific binding was not observed when the ...

Simultaneous monitoring of carbamazepine and its metabolities is helpful in providing information on the induction process via the epoxide-diol route. The present method involves the liquid-chromatographic analysis of 1.0 mL of plasma for carbamazepine at concentrations of 0.025 to 4.0 mg/L and for both the 10,11-epoxide and 10,11-transdiol metabolites at concentrations of 0.01 to 1.0 mg/L. Wei...

The anionic ring-opening polymerizations (AROP) of bio-based N-acetyl homocysteine thiolactone (NHTL) and different epoxides were carried out using benzyl alcohol 2-tert-butylimino-2-diethylamino-1,3-dimethylperhydro-1,3,2-diazaphosphorine (BEMP) as initiating system. This polymerization is a rare example AROP in the presence an acidic moiety (acetamido group). Well-defined alternating poly(est...

Triterpenoid There is a growing interest in natural triterpenoids, also know as phytosterols, due to their wide spectrum of biological activities [1] . Triterpenes are a wide-spread group of natural compounds with considerable practical significance which are produced by arrangement of squalene epoxide in a chair-chair, chai-boat arrangement followed by condensation. Triterpense are important s...

A 192-member library of N,N'-disubstituted urea inhibitors was synthesized by a solid-phase method. The ureas were tested for their inhibitory activities against recombinant human soluble epoxide hydrolase. Simple carbocyclic or para/meta-substituted phenyl groups showed inhibition potencies that were equal to or greater than adamantane-based sEH inhibitors, while the presence of bulky or ioniz...