ABSTRACT
Besides causing functional and clinical damage, hypercholesterolaemia also causes morphological alterations of vascular endothelium. Rabbits fed a diet with 1% cholesterol for 4, 6, or 8 weeks are experimental models for hypercholesterolaemia, with pathological structural changes in vascular luminal surface. Morphological investigation by scanning electron microscopy was performed to reveal the tridimensional growth of these lesions and the differences in this growth induced by concomitant dietary assimilation of fish-oil (2 g/day). Macroscopic reduction in fatty-streak production was clearly seen in rabbits fed fish-oil. Scanning electron microscopy confirmed that the area of intimal lesions was only 21 +/- 6% in this group, while in the group fed cholesterol without fish oil, the lesioned area attained 76 +/- 5%. Endothelial swelling was less marked, probably due to reduced intracellular lipid accumulation into the foam cells. Adherent macrophages were also fewer. The differences might be correlated with protection against the lipoproteins' atherogenic effects and to hemorheological benefits produced by the Omega-3 fatty acid (85%) present in fish-oil.
Subject(s)
Docosahexaenoic Acids/therapeutic use , Eicosapentaenoic Acid/analogs & derivatives , Endothelium, Vascular/drug effects , Hypercholesterolemia/drug therapy , Platelet Aggregation Inhibitors/therapeutic use , Animals , Cholesterol/blood , Diet , Eicosapentaenoic Acid/therapeutic use , Endothelium, Vascular/pathology , Hypercholesterolemia/pathology , Microscopy, Electron, Scanning , RabbitsABSTRACT
A series of new esters of glycerol and 2-O-methyl-glycerol with nicotinic and 5-fluoro-nicotinic acids were synthesized and their hypolipidemic activities were comparatively tested. The two most interesting compounds, 5 and 12, show a higher activity than both nicotinic and 5-fluoro-nicotinic acids in the following experimental models: Triton and olive oil hyperdyslipemia and tests on old rats.
Subject(s)
Glyceryl Ethers/chemical synthesis , Hypolipidemic Agents/chemical synthesis , Nicotinic Acids/chemical synthesis , Animals , Chemical Phenomena , Chemistry , Glyceryl Ethers/pharmacology , Guinea Pigs , Hypercholesterolemia/chemically induced , Hypercholesterolemia/drug therapy , Hyperlipidemias/chemically induced , Hyperlipidemias/drug therapy , Hypolipidemic Agents/pharmacology , Male , Mice , Nicotinic Acids/pharmacology , Rats , Rats, Inbred StrainsABSTRACT
The effects of 3 alpha, 7 beta-dihydroxy-12-cheto-cholan-24-oic acid (SF-482) were compared with those of ursodeoxycholic acid on bile flow and composition, on gallstones formation and on experimental hyperlipemias. SF-482, like ursodeoxycholic acid, increases the bile flow and residue in normal and ethynylestradiol-treated rats. The two compounds increase the biliary excretion of bile acids and phospholipids with a desaturation of bile cholesterol. SF-482 and ursodeoxycholic acid decrease the incidence of gallstones in mice; both compounds are active in Triton WR-1339, in olive oil and margarine hyperlipemias in rats and in ethanol intoxication in mice. In general, SF-482 is more active than ursodeoxycholic acid.
Subject(s)
Bile/drug effects , Chenodeoxycholic Acid/analogs & derivatives , Cholelithiasis/prevention & control , Deoxycholic Acid/analogs & derivatives , Hyperlipidemias/prevention & control , Hypolipidemic Agents/pharmacology , Ursodeoxycholic Acid/pharmacology , Alcoholic Intoxication , Animals , Chenodeoxycholic Acid/pharmacology , Cholesterol/metabolism , Female , Male , Mice , Phospholipids/metabolism , Rats , Rats, Inbred Strains , Time FactorsSubject(s)
Expectorants/chemical synthesis , Pyrrolidinones/chemical synthesis , Sulfhydryl Compounds/chemical synthesis , Thiophenes/chemical synthesis , Animals , Chemical Phenomena , Chemistry , Female , Guinea Pigs , In Vitro Techniques , Male , Mice , Pyrrolidinones/pharmacology , Pyrrolidinones/toxicity , Rats , Rats, Inbred Strains , Sulfhydryl Compounds/pharmacology , Sulfhydryl Compounds/toxicity , Swine , Thiophenes/pharmacology , Thiophenes/toxicityABSTRACT
alpha-Mercaptopropionylglycine (tiopronin, Mucolysin), a drug endowed with an interesting mucolytic activity, was tested for mutagenicity by means of the following in vitro and in vivo tests: mutagenesis on S. typhimurium with and without metabolic activation, genetic mutation on S. pombe P1 with and without metabolic activation, gene conversion on S. cerevisiae D4 with and without metabolic activation, urinary assay in the mouse with S. cerevisiae D4, host mediated assay in the mouse with S. cerevisiae D4 and micronucleus test in the mouse. On the basis of the results obtained tiopronin proved to be free of mutagenic activity.
Subject(s)
Amino Acids, Sulfur/toxicity , Mutagens , Tiopronin/toxicity , Animals , Cell Nucleus/drug effects , Female , Gene Conversion/drug effects , Male , Mice , Mitosis/drug effects , Mutagenicity Tests , Saccharomyces cerevisiae/drug effects , Saccharomyces cerevisiae/genetics , Salmonella typhimurium/genetics , Schizosaccharomyces/genetics , Tiopronin/urineABSTRACT
The analgesic, spasmolytic, antiinflammatory, C.N.S., cardiovascular, respiratory, and anaphylactogenic activities of PTT-119 were investigated. PTT-119 possesses good peripheral but only slight central analgesic activity. It presents an interesting in vitro spasmolytic activity of non-competitive type against acetylcholine and histamine. PTT-119 is inactive in rat carrageenin oedema, on the C.N.S. of mice, on cardiovascular and respiratory parameters of cats, and in guinea-pig anaphylaxis.
Subject(s)
Nitrogen Mustard Compounds/pharmacology , Analgesics , Anaphylaxis/prevention & control , Animals , Anti-Inflammatory Agents , Cats , Central Nervous System/drug effects , Female , Guinea Pigs , Hemodynamics/drug effects , In Vitro Techniques , Male , Mice , Parasympatholytics , Rats , Rats, Inbred Strains , Respiration/drug effectsSubject(s)
Bacterial Infections/prevention & control , Cefuroxime/therapeutic use , Cephalosporins/therapeutic use , Adult , Aged , Clinical Trials as Topic , Drug Evaluation , Female , Genital Diseases, Female/surgery , Humans , Middle Aged , Obstetric Labor Complications/prevention & control , Pregnancy , Surgical Wound Infection/prevention & controlABSTRACT
The antibiotic activity was determined at different intervals of time on plasma samples, taken from rats treated with a certain number of commonly used antibiotics, and kept at -20 C up to 8 weeks. The results of the microbiological assays demonstrate that the stability of the antibiotics in the frozen plasma decreases in the following order: oxytetracycline > cephalexin, streptomycin, erythromycin > demeclocycline > ampicillin, amoxycillin > penicillin G, cephaloridine, rolitetracycline, and tetracycline.
