Search results for "Lipids"
showing 10 items of 2228 documents
Toward the Discovery of New Agents Able to Inhibit the Expression of Microsomal Prostaglandin E Synthase-1 Enzyme as Promising Tools in Drug Developm…
2010
In our recent studies, we focused our attention on the synthesis of several γ-hydroxybutenolides designed on the basis of petrosaspongiolide M 1 (PM) structure that has been recognized to potently inhibit the inflammatory process through the selective PLA2 enzyme inhibition. By means of a combination of computational methods and efficient synthetic strategies, we generated small collections of PM modified analogs to identify new potent PLA2 inhibitors, suitable for clinical development. In the course of the biological screening of our compounds, we discovered a potent and selective inhibitor of mPGES-1 expression, the benzothiophene γ-hydroxybutenolide 2, which so far represents the only pr…
Docosahexaenoic acid and other fatty acids induce a decrease in pHiin Jurkat T-cells
2003
Docosahexaenoic acid (DHA) induced rapid (t1/2=33 s) and dose-dependent decreases in pHi in BCECF-loaded human (Jurkat) T-cells. Addition of 5-(N,N-dimethyl)-amiloride, an inhibitor of Na+/H+ exchanger, prolonged DHA-induced acidification as a function of time, indicating that the exchanger is implicated in pHi recovery. Other fatty acids like oleic acid, arachidonic acid, eicosapentaenoic acid, but not palmitic acid, also induced a fall in pHi in these cells. To assess the role of calcium in the DHA-induced acidification, we conducted experiments in Ca2+-free (0% Ca2+) and Ca2+-containing (100% Ca2+) buffer. We observed that there was no difference in the degree of DHA-induced transient ac…
Modulation of Cox-1, 5-, 12- and 15-Lox by Popular Herbal Remedies Used in Southern Italy Against Psoriasis and Other Skin Diseases
2014
Acanthus mollis (Acanthaceae), Achillea ligustica, Artemisia arborescens and Inula viscosa (Asteraceae) are used in Southern Italy against psoriasis and other skin diseases that occur with an imbalanced production of eicosanoids. We here assessed their in vitro effects upon 5-, 12-, 15-LOX and COX-1 enzymes as well as NFκB activation in intact cells as their possible therapeutic targets. All methanol crude extracts inhibited both 5-LOX and COX-1 activities under 200 µg/mL, without significant effects on the 12-LOX pathway or any relevant in vitro free radical scavenging activity. NFκB activation was prevented by all extracts but A. mollis. Interestingly, A. ligustica, A. arborescens and A. …
Changes induced by pravastatin treatment on hemostatic and fibrinolytic patterns in patients with type IIb hyperlipoproteinemia
1994
Abstract A randomized, double-blind, parallel-group study of pravastatin versus placebo was carried out for 24 weeks in 20 patients with type IIb primary hyperlipoproteinemia. Total cholesterol, triglycerides, high-density lipoprotein (HDL) cholesterol, low-density lipoprotein (LDL) cholesterol, blood glucose, apolipoproteins (apo) A1 and B, and lipoprotein (a) (Lp[a]) levels were determined. A venous occlusion test was also performed in all patients. Pre- and postvenous occlusion tests were determined: tissue plasminogen activator antigen (t-PA[Ag]), plasminogen activator inhibitor (PAI) activity, factor VII, fibrinogen, plasminogen, and hematocrit. Compared with placebo, pravastatin signi…
Inhibiting fatty acid amide hydrolase normalizes endotoxin-induced enhanced gastrointestinal motility in mice
2012
Background and purpose Gastrointestinal (GI) motility is regulated in part by fatty acid ethanolamides (FAEs), including the endocannabinoid (EC) anandamide (AEA). The actions of FAEs are terminated by fatty acid amide hydrolase (FAAH). We investigated the actions of the novel FAAH inhibitor AM3506 on normal and enhanced GI motility. Experimental approach We examined the effect of AM3506 on electrically-evoked contractility in vitro and GI transit and colonic faecal output in vivo, in normal and FAAH-deficient mice treated with saline or LPS (100 µg·kg(-1), i.p.), in the presence and absence of cannabinoid (CB) receptor antagonists. mRNA expression was measured by quantitative real time-PCR…
Über die Beeinflussung der Ca-Aufnahme in Lipidextrakte aus Mikrosomen und Mitochondrien des Herzens durch Digitoxin
1970
Lipids were isolated by chloroform-methanol extraction from mitochondrial and microsomal fractions of guinea-pig hearts. In the presence of digitoxin (10−9-10−6 g/ml) 15–30% more radioactive Ca was taken up by the lipid extracts than under control conditions, but the total amount of Ca in this phase remained unchanged. Thus, digitoxin produced an increase in the specific activity of the lipid-bound Ca which may be explained by an increased exchangeability of this Ca fraction. This effect of digitoxin might result in an improved availability of the lipid-bound Ca for Ca-dependent functions (e.g. contraction) of the heart muscle cell.
Effects ofThymus species extracts on rat duodenum isolated smooth muscle contraction
1989
The diethylether, ethylacetate and butanolic extracts from Thymus webbianus and Thymus leptophyllus were tested for spasmolytic activity. Pre-incubation of the isolated rat duodenum with these extracts for 10 min produced a concentration-dependent inhibition of acetylcholine-induced contractions. This effect was at least ten times greater with the apolar extracts than with the polar extracts.
Increased thrombin generation and complement activation in patients with type IIA hyperlipoproteinemia: effects of simvastatin treatment
1997
Abstract The aim of this study was to demonstrate the existence of increased thrombin generation and complement activation in patients with type IIa primary hyperlipoproteinemia, but no signs of atherosclerotic vascular disease and to assess the effects of simvastatin treatment in these patients. We studied 40 patients with type IIa primary hyperlipoproteinemia and 40 healthy subjects matched for sex, age, body mass index, and smoking status. The study was divided into two phases. In the first phase, a cross-sectional comparison of lipid and hemostatic patterns was performed between patients and controls. In the second phase, we assessed the effect of a persistent reduction in cholesterol s…
Effect of gemfibrozil treatment on fibrinolysis system in patients with hypertriglyceridemia
1992
Abstract The effect of gemfibrozil on lipidic, coagulative, and fibrinolytic pattern was studied in 20 patients with primary type IV hyperlipoproteinemia. After a 4-week stabilization period during which administration of lipid-lowering drugs was stopped and an isocaloric diet (20% protein, 30% fat, and 50% carbohydrates) was prescribed, 20 patients (12 men and 8 women; mean age, 38 ± 4 years; body mass index, 23.4 ± 1.5) suffering from primary hypertriglyceridemia were included in this study and treated for a 12-week period with gemfibrozil (600 mg BID). Every 4 weeks the following parameters were checked: glycemia, triglycerides, total cholesterol, high density lipoprotein-cholesterol, to…
The cAMP Pathway Sensitizes VR1 Expressed in Oocytes from <i>Xenopus laevis</i> and in CHO Cells
2003
The vanilloid receptor 1 (VR1) is a heat-activated cation channel which also responds to capsaicin and other chemical stimuli. Protein kinase C has a stimulatory effect on VR1 activity, either alone or after activation with capsaicin. The influence of the cAMP-signaling pathway on the effects of capsaicin is controversial. To clarify this, the actions of capsaicin and the modulatory effects of forskolin, pCPT-cAMP, and isobutylmethylxanthine were studied in <i>Xenopus laevis</i> oocytes expressing rat VR1 and in CHO cells expressing human VR1. Capsaicin activated the VR1 channel and increased the intracellular calcium concentration. The effects of capsaicin were enhanced by fors…