Myocardial phospholipase D (PLD) is primarily localized at the sarcolemmal level and selectively hydrolyzes phosphatidylcholine to form phosphatidic acid as part of the signal transduction mechanisms for regulating Ca2' movements in the heart. Since the myocardial cell damage induced by oxidative stress is associated with abnormalities in Ca2' homeostasis and thiol status, we examined the thiol...

A series of N-mustards, which was conjugated to mono- or bis-naphthalimides with a flexible amine link, were synthesized and evaluated for cytotoxicity against five cancer cell lines (HCT-116, PC-3, U87 MG, Hep G2 and SK-OV-3). Several compounds displayed better activities than the control compound amonafide. Further evaluations by fluorescence spectroscopy studies and DNA-interstrand cross-lin...

The purpose of the present study was to identify the cellular processes and targets affected by treatment with bis-benzimidazole derivatives with chloroalkyl and bromoalkyl moieties (1–4) in the estrogen receptor-negative MDA-MB-231 human breast cancer cells. Treatment of the cells revealed that these compounds inhibited DNA synthesis and irreversibly inhibited the proliferative activity of the...

This study underscores the development of Ag hydrogel nanocomposites, as smart substrates for antibacterial uses, via innovative in situ reactive and reduction pathways. To this end, two different synthetic strategies were used. Firstly thiol-acrylate (PSA) based hydrogels were attained via thiol-ene and radical polymerization of polyethylene glycol (PEG) and polycaprolactone (PCL). As a second...

ABSTRACT An earlier developed alkylating path leading to tetraalkylated diaminomaleonitrile derivatives was explored. Attempts to explain the reactivity of the representative dialkylated diaminomaleonitrile 2,3-bis[(3-pyridylmethyl)amino]-2(Z)-butene-1,4-dinitrile during the alkylation reaction were performed using X-ray and density functional theory (DFT) studies. The condensed Fukui functions...

The one-pot synthesis of symmetrical triaryl amines using aryl halides and 5-Methyl-1,3,4-Thiadiazole-2-Amine as a nitrogen-transfer reagent is reported. Copper oxide nanoparticles that does not require the presence of any additional ligand, improved rate and facility of the synthesis of triaryl amines. The introduction of a new N-source, using green solvents PEG/H2O, normal atmospheric conditi...

The localization of Cu,Zn-superoxide dismutase in the mitochondrial intermembrane space suggests a functional relationship with superoxide anion (O2*-) released into this compartment. The present study was aimed at examining the functionality of Cu,Zn-superoxide dismutase and elucidating the molecular basis for its activation in the intermembrane space. Intact rat liver mitochondria neither sca...

Inflammatory signaling pathways orchestrate the cellular response to infection and injury. These pathways are known to be modulated by compounds that alkylate cysteinyl thiols. One class of phytochemicals with strong thiol alkylating activity is the chalcones. In this study we tested fourteen chalcone derivatives, α-X-substituted 2',3,4,4'-tetramethoxychalcones (α-X-TMCs, X = H, F, Cl, Br, I, C...

teins (2, 4) have been demonstrated after in vitro and in vivo exposure to these agents. The work of Schabel et a!. (19) showing that the hamster plasmacytoma is resistant to known alkylating agents and to 1,3-bis(2-chlonoethyl)-1-ni trosoureas hasgeneratedspeculation that the carcinostatic activity of the nitrosourea agents is principally related to their alkylating metabolites. Wheeler and Bo...

Two alternative methods for the attachment of monomethoxypolyethyleneglycols (PEG) to proteins are proposed; they are based upon the replacement of the hydroxy terminal function of PEG to carboxylate followed by its activation with dicyclohexylcarbodiimide and N-hydroxysuccinimide. The methods, which give more homogeneous product than that employing trichloro-s-triazine as coupling reagent, may...