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The direct antioxidative and anti-inflammatory effects of peroxisome proliferator-activated receptors ligands are associated with the inhibition of angiotensin converting enzyme expression in
TLDR
The results suggest that the direct anti-oxidant and anti-inflammatory effects of PPARs ligands in the aorta of streptozotocin-induced diabetic rats were not likely to be mediated by the normalization of glucose or lipid metabolism, but instead these salutary effects appear to have been associated with the inhibition of the expression of ACE. Expand
Gas Chromatography-Mass Spectrometric Determination of Activity of Human Placental Aromatase Using 16α-Hydroxyandrostenedione as a Substrate
Aromatization of 16alpha-hydroxyandrostenedione (16alpha-OH AD) with aromatase in human placental microsomes was studied by gas chromatography-mass spectrometry (GC-MS) usingExpand
Gas chromatography-mass spectrometric determination of activity of human placental aromatase using 16alpha-hydroxyandrostenedione as a substrate.
TLDR
In this assay, aromatase activity, estriol formation, could be determined at a level as low as 1 pmol/min/mg protein, and aromatase inhibitors, 4-hydroxy- and 6-oxo-androstenediones, prevented the estRIol formation in a competitive manner with 25 and 30 nM of apparent Ki values, respectively. Expand
Calcium Channel Blockades Exhibit Anti-Inflammatory and Antioxidative Effects by Augmentation of Endothelial Nitric Oxide Synthase and the Inhibition of Angiotensin Converting Enzyme in the
TLDR
The direct anti-inflammatory and antioxidative effects of calcium channel blockades in the aorta of rats with L-NAME-induced hypertension were not likely to be mediated by the blood pressure-lowering action of these agents, but instead these beneficial effects appear to have been mediated by an augmentation of eNOS expression and by the inhibition of the expression of ACE. Expand
Enzymic aromatization of 6-alkyl-substituted androgens, potent competitive and mechanism-based inhibitors of aromatase.
TLDR
It is implied that alignment of 6alpha-methyl ADD in the active site could favour the pathway leading to oestrogen over the inactivation pathway, compared with that of ADD. Expand
Structure–activity relationships of 2-, 4-, or 6-substituted estrogens as aromatase inhibitors
TLDR
6alpha-Phenylestrone was the most powerful inhibitor among the estrogens studied, and its affinity was comparable to that of the androgen substrate androstenedione, indicating that the 17-carbonyl group plays a critical role in the formation of a thermodynamically stable enzyme-inhibitor complex. Expand
Biological aromatization of Δ4,6- and Δ1,4,6-androgens and their 6-alkyl analogs, potent inhibitors of aromatase
Abstract Enzymic aromatization of Δ 6 - and Δ 1,6 -derivatives of the natural substrate androstenedione with human placental aromatase was first studied using gas-chromatography-mass spectrometry.Expand
Calcium Channel Blockers Reduce Angiotensin II-Induced Superoxide Generation and Inhibit Lectin-Like Oxidized Low-Density Lipoprotein Receptor-1 Expression in Endothelial Cells
Calcium channel blockers have been shown to limit the progression of atherosclerosis and decrease the incidence of cardiovascular events. To investigate vasoprotective effects beyond the bloodExpand
HYPERINSULINAEMIA INCREASES THE GENE EXPRESSION OF ENDOTHELIAL NITRIC OXIDE SYNTHASE AND THE PHOSPHATIDYLINOSITOL 3‐KINASE/AKT PATHWAY IN RAT AORTA
TLDR
It is concluded that hyperinsulinaemia itself can lead to the upregulation of eNOS and the PI3‐K/Akt pathway in the vasculature and may also induce the overexpression of VEGF and IGF‐I receptor genes. Expand
Aromatization of 16α-hydroxyandrostenedione by human placental microsomes: effect of preincubation with suicide substrates of androstenedione aromatization
TLDR
Differences exist in the binding site structures responsible for aromatization of 16alpha-OHAD and AD, which are suggested to be related to estrone and estriol formation. Expand
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