Search results for "Thromboxane B2"
showing 10 items of 22 documents
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase …
2000
A series of 1-imidazolyl(alkyl)-substituted quinoline, isoquinoline, naphthalene, benzo[b]furan, and benzo[b]thiophene derivatives was synthesized as dual inhibitors of thromboxane A(2) synthase (P450 TxA(2)) and aromatase (P450 arom). Dual inhibition of these enzymes could be a novel strategy for the treatment of mammary tumors and the prophylaxis of metastases. The most potent dual inhibitors, 5-(2-imidazol-1-ylethyl)-7,8-dihydroquinoline (31) (P450 TxA(2): IC(50) = 0.29 microM; P450 arom: IC(50) = 0.50 microM) and its 5, 6-saturated analogue 30 (P450 TxA(2): IC(50) = 0.68 microM; P450 arom: IC(50) = 0.38 microM), showed a stronger inhibition of both target enzymes than the reference comp…
The effect of two low doses of aspirin on whole blood thromboxane and prostacyclin generation in healthy subjects
1983
SummaryThe effects of two low doses of aspirin (20 mg and 100 mg) on prostacyclin and thromboxane formation during whole blood clotting were studied in 8 healthy volunteers.A single 100 mg aspirin dose caused more than 90% reduction of both serum TXB2 and 6-keto-PGF1α; a single 20 mg dose of aspirin inhibited serum TXB2 more than 6-keto-PGF1α but effects on these two products could not be completely dissociated.However, the effect of a single 20 mg aspirin dose on serum TXB2, was of much longer duration than its inhibitory effect on PGI2 synthesis during whole blood clotting.
Cerebral protection against ischemia by locomotor activity in gerbils. Underlying mechanisms.
1995
Background and Purpose A previous communication of this laboratory demonstrated reduced mortality and neuronal damage by spontaneous locomotor activity preceding forebrain ischemia in Mongolian gerbils. The present experiments seek to elucidate potential mechanisms of protection by measurement of cerebral blood flow, cerebral tissue conductance as an indicator of ischemic cell swelling, and the cerebral release of eicosanoids. Methods Gerbils were maintained either in conventional cages (nonrunners) or with free access to running wheels (runners) for 2 weeks preceding 15 minutes of forebrain ischemia. During ischemia and 2.5 hours of reperfusion, cerebral tissue conductance was determined …
POSTPRANDIAL HYPERGLYCEMIA IS A DETERMINANT OF PLATELET ACTIVATION IN EARLY 2 DIABETES MELLITUS
2010
BACKGROUND: Chronic hyperglycemia is a major contributor to in vivo platelet activation in diabetes mellitus. OBJECTIVES: To evaluate the effects of acarbose, an alpha-glucosidase inhibitor, on platelet activation and its determinants in newly diagnosed type 2 diabetic patients. METHODS: Forty-eight subjects (26 males, aged 61 +/- 8 years) with early type 2 diabetes (baseline hemoglobin A(1c) < or = 7% and no previous hypoglycemic treatment) were randomly assigned to acarbose up to 100 mg three times a day or placebo, and evaluated every 4 weeks for 20 weeks. The main outcome measures were urinary 11-dehydro-thromboxane (TX)B(2) (marker of in vivo platelet activation) and 8-iso-prostaglandi…
Circulating immune complexes and platelet thromboxane synthesis in patients with insulin-dependent (type I) diabetes mellitus
1984
Platelets from diabetic subjects with circulating immune complexes (CIC) synthesized greater amounts of thromboxane than did platelets from CIC-negative patients or controls. In view of the known action of CIC on platelet function, a relationship between these two factors may be suggested in the initiation and progression of microangiopathy in diabetes.
Anti-inflammatory and analgesic activity of a novel inhibitor of microsomal prostaglandin E synthase-1 expression
2009
Abstract In a previous study, we reported a new γ-hydroxybutenolide derivative, 4-benzo[ b ]thiophen-2-yl-3-bromo-5-hydroxy-5 H -furan-2-one (BTH), as inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) expression in lypopolysaccharide (LPS) stimulated RAW 264.7 and TPH-1 cells, without affecting cyclooxygenase-2 (COX-2). In this study, we evaluated the in vivo effect of BTH on some acute and chronic inflammatory animal models in relation to its inhibitory profile on mPGES-1 expression. In the zymosan-induced mouse air pouch model, BTH produced a dose-dependent inhibition of prostaglandin E 2 (PGE 2 ) production and mPGES-1 protein expression in pouch exudates without any effect on…
Inhibition of thromboxane biosynthesis by triflusal in type 2 diabetes mellitus.
2004
Abstract Triflusal is an antiplatelet drug related to aspirin, with different pharmacological properties and a lower haemorrhagic risk. We aimed at comparing their effects on platelet and endothelial activation in type 2 diabetes mellitus (T2DM). In a randomized, double-blind, parallel group study, we compared the effects of three daily regimens (300, 600, and 900mg) of triflusal, and aspirin (100mg/day) on urinary 11-dehydro-thromboxane (TX)B 2 , index of in vivo platelet activation, ex vivo platelet function using the analyzer PFA-100, plasma von Willebrand factor (vWF), P-selectin, intercellular adhesion molecule-1 (ICAM-1), vascular cell adhesion molecule-1 (VCAM-1), and serum nitrite a…
Eight-week consumption of milk enriched with omega 3 fatty acids raises their blood concentrations yet does not affect lipids and cardiovascular dise…
2014
Adequate concentrations of omega 3 fatty acids (FA) may be maintained by consuming foods naturally rich in or functional foods enriched with those essential FA. We assessed the effects of an 8-week consumption of milk enriched with 400. mg of omega 3 FA on blood lipid levels and selected cardiovascular risk factors in adult healthy volunteers. Participants (n= 157) were randomized to consume - for eight weeks - either 500. mL/day of 1% fat milk providing 150. mg of eicosapentaenoic (EPA), 150. mg of docosahexaenoic (DHA), and 100. mg of α-linolenic (ALA) acids or 500. mL/day of non-enriched 1% fat milk. At week 8, we observed significant increments of blood EPA and DHA in the intervention g…
Effect of bakuchiol on leukocyte functions and some inflammatory responses in mice.
1996
Abstract The effects of bakuchiol, a meroterpenoid isolated from the leaves of Psoralea glandulosa L., on phospholipase A2 (PLA2) activity from different sources, human neutrophil responses, zymosan air pouch and topical inflammation in mice, were investigated. This natural product was a weak inhibitor of secretory and intracellular PLA2 but dose-dependently reduced the formation of LTB4 and TXB2 by human neutrophils and platelet microsomes, respectively. In addition, bakuchiol inhibited degranulation in human neutrophils, whereas superoxide generation was not affected. In mice, bakuchiol decreased cell migration, myeloperoxidase activity and eicosanoid levels in the air pouch inflammation …