High-throughput screening of a subset of the CD3 chemical library (Centre for Drug Design and Discovery; KU Leuven) provided us with a lead compound 1, displaying low micromolar potency against dengue virus and yellow fever virus. Within a project aimed at discovering new inhibitors of flaviviruses, substitution of its central imidazole ring led to synthesis of variably substituted pyrazine dic...

OBJECTIVE Alchornea floribunda leaves are widely used in ethnomedicine for the management of immuno-inflammatory disorders. We investigated the in vivo and in vitro antioxidant activity of the leaf extract, fractions and isolated compounds of A. floribunda. MATERIALS AND METHODS The ethyl acetate fraction of the methanol leaf extract was subjected to several chromatographic separations to iso...

BACKGROUND Anaesthetic steroids are established positive allosteric modulators of GABAA receptors, but little is known concerning steroid modulation of strychnine-sensitive glycine receptors, the principal mediators of fast, inhibitory neurotransmission in the brain stem and spinal cord. This study compared the modulatory actions of five anaesthetic pregnane steroids and two non-anaesthetic iso...

Phthalate esters are widely used as plasticizers in the manufacture of products made of polyvinyl chloride. Mono-(2-ethylhexyl)phthalate (MEHP) induces rodent hepatocarcinogenesis by a mechanism that involves activation of the nuclear transcription factor peroxisome proliferator-activated receptor-alpha (PPAR ). MEHP also activates PPAR-gamma (PPAR ), which contributes to adipocyte differentiat...

Despite the increasing use of rare earth elements (REEs) and oxides (REOs) in various technologies, the information on their ecotoxicological hazard is scarce. Here, the effects of La3+, Ce3+, Pr3+, Nd3+, Gd3+, CeO₂, and eight doped REOs to marine bacteria Vibrio fischeri and freshwater protozoa Tetrahymena thermophila were studied in parallel with REO dopant metals (Co2+, Fe3+, Mn2+, Ni2+, Sr2...

As part of our search for new compounds having antiviral effects, the prepared 2-aminonaphthalimide series was examined for its activity against the herpes simplex viruses HSV-1 and HSV-2. This represents the first study of the antiviral effects of this class of compounds. The new series of 2-amino-1H-benzo[de]isoquinoline-1,3-diones was examined against HSV-1 and HSV-2 using a cytopathic effec...

In this paper we present the results of studying the effects of the essential oil of Calamintha glandulosa Silic (EOCG) on the isolated rat ileum. C. glandulosa Silic has been used in folk medicine as an antispasmodic. EOCG (0.003-1 mg/ml) inhibited spontaneous contraction of the ileum (EC50 of 210.48 +/- 9.12 microg/ml). The calcium channel blocking activity was confirmed by inhibition of K(+)...

A single nucleotide polymorphism that substitutes a serine for an asparagine at residue 700 in the Ca2+-binding repeats of thrombospondin-1 is associated with familial premature coronary heart disease. We expressed the Ca2+-binding repeats alone (Ca) or with the third epidermal growth factor-like module (E3Ca), without (Asn-700) or with (Ser-700) the disease-associated polymorphism. The intrins...

The aim of this study was to assess the phenolic composition and nutraceutical potential of tinctures from fruits in two stages of maturity (F3, younger; F25, older), green husks (GH), and leaves (L) of Juglans regia L. In all extracts gallic, protocatechuic, 3-caffeoylquinic, 3-ρ-coumaroylquinic, 4-caffeoylquinic, 4-ρ-coumaroylquinic, and ρ -coumaric acids and quercetin-3-O-deoxyhexoside were ...