Anti-atherogenic effects of a new thienylacylhydrazone derivative, LASSBio-788, in rats fed a hypercholesterolemic diet
| Autor: | Fernanda Carla Ferreira de Brito, Eliezer J. Barreiro, Ana L.P. Miranda, Nadia Alice Vieira da Motta, Carlos A. M. Fraga, Arthur Eugen Kümmerle, Elisabeth Maróstica, Caroline Fernandes dos Santos |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Male
medicine.medical_specialty medicine.drug_class Cholesterol VLDL Vasodilation Thiophenes Anti-inflammatory chemistry.chemical_compound Enos Internal medicine Malondialdehyde medicine Animals Molecular Targeted Therapy Rats Wistar Phenylephrine Triglycerides Pharmacology biology lcsh:RM1-950 Hydrazones Cholesterol LDL biology.organism_classification Atherosclerosis Rats Nitric oxide synthase Disease Models Animal lcsh:Therapeutics. Pharmacology Endocrinology chemistry Biochemistry Anti atherogenic biology.protein Molecular Medicine Diet Atherogenic Nitric Oxide Synthase Derivative (chemistry) medicine.drug |
| Zdroj: | Journal of Pharmacological Sciences, Vol 123, Iss 1, Pp 47-57 (2013) |
| ISSN: | 1347-8648 |
| Popis: | The compound LASSBio-788 (N-Allyl (2-thienylidene) 3,4-methylenedioxybenzoylhydrazine) is a thienylacylhydrazone derivative shown to have antiplatelet, vasodilatory, and anti-inflammatory properties in vitro. We hypothesize that LASSBio-788 may exert beneficial effects on atherosclerosis. Male wistar rats were divided into 4 groups: Control group received standard rat chow, hypercholesterolemic group (HC) and HC+788 (compound LASSBio-788 group) received hypercholesterolemic diet for 45 days. HC+788 group received compound LASSBio-788 (100 μmol/kg) once daily in the last 15 days. LASSBio-788 reduced the levels of total cholesterol (109.1 ± 4.3 vs. 361.0 ± 12.8 mg/dl), triglycerides (66.1 ± 1.1 vs. 186.9 ± 17.7 mg/dl), LDLc (63.2 ± 6.1 vs. 330.9 ± 9.7 mg/dl), VLDLc (9.8 ± 1.1 vs. 45.0 ± 4.6 mg/dl) and malondialdehyde (4.8 ± 0.3 vs. 9.4 ± 0.5 nmol/ml) compared to the HC group. LASSBio-788 presented antiplatelet properties and decreased inflammatory markers levels. LASSBio-788 promoted a decrease in contractile response to phenylephrine and an improvement in endothelium-dependent vasorelaxant response by increasing two-fold the expression of nitric oxide synthase (eNOS). Our results suggest that the compound LASSBio-788 represents a new multi-targeted drug candidate for the treatment of atherosclerosis. Keywords:: atherosclerosis, anti-platelet, anti-inflammatory, lipid-lowering, thienylacylhydrazone derivative |
| Databáze: | OpenAIRE |
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