Showing papers in "Biochemical Pharmacology in 1996"

TL;DR: It is concluded that NSAIDs inhibit the proliferation rate of the two colon cancer cell lines independent of their ability to inhibit PG synthesis, meaning that alternative mechanisms for their activity on tumor cell growth must be entertained.

TL;DR: Studying combinations of cisplatin/oxaliplatin suggest that the activities of these two agents are at least additive and possibly synergistic, and oxaliplarin has a different spectrum of activity and low cross-resistance to cis platin and should be valuable in cisplins refractory patients or in combination with cisplin.

TL;DR: The enzymatic mechanism of NO production is surveyed, the strategies and pharmacological tools for selective inhibition of distinct NOS isoforms are listed, and the side-effects of the various approaches are considered.

TL;DR: The isoprostanes possess potent biological activity, and their potential role in mediating certain aspects of the detrimental effects of oxidant stress is examined and evidence is presented that these biological effects may be mediated through interaction with a unique receptor.

TL;DR: It is suggested that THC may also exhibit the same physiological and pharmacological properties as the active form of curcumin in vivo by means of the beta-diketone moiety as well as phenolic hydroxy groups.

TL;DR: All pigments investigated had strong antioxidative activity in a liposomal system and reduced the formation of malondialdehyde by UVB irradiation and the scavenging effect of hydroxyl radicals and superoxide anion radicals were influenced by their own structures.

TL;DR: The Steroidogenic Acute Regulatory protein (StAR) is identified and characterized as a family of proteins that are synthesized and imported into the mitochondria in response to hormone stimulation, and for which strong evidence exists indicating that it is the long sought acute regulatory protein.

TL;DR: These strong inhibitory properties of curcumin towards P450s and GSTs, in addition to its well-known antioxidant activity, may help explain the previously observed anticarcinogenic, antimutagenic, and cytoprotective effects of this important natural compound and food constituent.

TL;DR: Antisense oligonucleotide-mediated suppression of MRP synthesis offers a highly specific alternative approach to circumventing resistance mediated by this novel drug resistance protein.

TL;DR: The current evidence supporting a metallopeptidase ECE as the physiological regulator of endothelin production is described and its sensitivity to inhibition by the fungal metabolite phosphoramidon and subsequent cloning of the enzyme indicate it to be a type II integral membrane protein homologous with neural endopeptIDase-24.11.

TL;DR: The results show that cell proliferation and immunoglobulin production (IgG and IgM) depend on the sequence and the chemical modification of the oligonucleotide, and that oligon nucleotides exert their effects mainly on the B cells.

TL;DR: Analysis of possible kinetic schemes revealed that the most likely explanation for the disparity in estimated enzyme concentrations and the incomplete inhibition of p-NPA hydrolysis is that CPT-11 also interacts at a modulator site on the enzyme, which profoundly reduces substrate Hydrolysis.

TL;DR: In vivo findings confirm the results of in vitro tests, conducted separately, showing that meloxicam preferentially inhibitsCOX-2 over COX-1, the inducible isoenzyme implicated in the inflammatory response, whereas COX1 has cytoprotective effects in the gastric mucosa.

TL;DR: Both I3C and DIM are partial Ah receptor antagonists in the T47D human breast cancer cell line and partially inhibited induction of CYP1A1 mRNA levels by TCDD and reporter gene activity.

TL;DR: Data show that several xenobiotic-metabolizing CYP genes are expressed in human placenta at a low level, and the significant of such low-level expression is unknown, but it may have local physiological or toxic consequences.

TL;DR: It is demonstrated here that both unconjugated bilirubin (Bu) and conjugated bilIRUBin (Bc) can protect human low density lipoprotein (LDL) against oxidation by oxyradicals generated by 2,2'-azo-bis (2 amidinopropane) dihydrochloride at 37 degrees.

TL;DR: The levels and substrate specificity of P450s from humans and rats are characterized and catalytic properties in testosterone metabolism different from those of rats are investigated to extrapolate drug metabolism data from experimental animals to humans.

TL;DR: Data establish for the first time that two agents with proven anti-anginal effects inhibit cardiac CPT-1, and this action is likely to contribute to the anti-ischaemic effects of both perhexiline and amiodarone.

TL;DR: Evidence is obtained that c-Src protein Kinase is the protein kinase activated by TCDD and that this kinase is associated specifically with the Ah-receptor-complex proteins in cytosol from adipose tissue and liver of guinea pig and Liver of C57BI/6J mouse and in NIH 3T3 mouse fibroblast cells.

TL;DR: Results show that placental tissue during the first trimester of pregnancy has the potential of expressing several CYP genes, and forms a basis for subsequent analysis of these forms at the protein and functional level.

TL;DR: The characteristics of the cannabinoid-G-protein-adenylyl cyclase system are examined, and the role of cyclic AMP in mediating effects of these drugs is explored.

TL;DR: The results indicated that MDMA ++ was apparently not the single, causative agent for the acute 5-HT depletion, which may also involve a metabolite formed by CYP2D.

TL;DR: Glyoxalase I inhibitor diesters may, therefore, inhibit tumour growth by inducing the accumulation of methylglyoxal in tumour cells, and induction of apoptosis.

TL;DR: The hypothesis that cucurbitacin treatment leads to an inappropriate increase in the filamentous or polymerized actin fraction in prostate carcinoma cells is supported and it is concluded that cucURbitacins are potent disruptors of cytoskeletal integrity.

TL;DR: Isatin may mediate a link between monoamines and the natriuretic peptide system, and its analogues may provide new pharmacological tools.

TL;DR: The most potent antagonist activity was related to good AhR binding characteristics in terms of conforming to previously predicted 14 x 12 x 5 A van der Waals dimensions and the presence of an electron-rich ring nitrogen at or near a relatively unsubstituted X-axis terminal position, consistent with the hypothesis that an electrons-rich center near or along a lateral position of the van Der Waals binding cavity is a characteristic that enhances AhR antagonist activity.

TL;DR: The ability of melatonin to protect against paraquat-induced oxidative damage in rat lung, liver, and serum was examined in this article, where changes in the levels of malondialdehyde (MDA) plus 4-hydroxyalkenals (4-HDA) and reduced and oxidized glutathione concentrations were measured.

TL;DR: The two activities of A77 1726 are demonstrated: inhibition of pyrimidine nucleotide synthesis and interference with tyrosine phosphorylation.

TL;DR: A series of derivatives of 2,3-dihydro-2-(aryl)-4(1H)-quinazolinone (DHQZ) with known antitumor activity was re-evaluated in the National Cancer Institute cancer cell line screen and analysis by the COMPARE algorithm suggested that their cytotoxicity derived from interactions with tubulin.

TL;DR: It is demonstrated that CYP2C9 and CYP1A2 together account for the majority of human liver R- and S-naproxen O-demethylation, precluding the use of either R- or S-magnifying enzyme as a CYP isoform-specific substrate in vitro and in vivo.