Anti-atherogenic Effects of a New Thienylacylhydrazone Derivative, LASSBio-788, in Rats Fed a Hypercholesterolemic Diet

Autor: Nadia Alice Vieira da Motta, Arthur Eugen Kümmerle, Elisabeth Marostica, Caroline Fernandes dos Santos, Carlos Alberto Manssour Fraga, Eliezer Jesus Barreiro, Ana Luisa Palhares de Miranda, Fernanda Carla Ferreira de Brito
Jazyk: angličtina
Rok vydání: 2013
Předmět:
Zdroj: Journal of Pharmacological Sciences, Vol 123, Iss 1, Pp 47-57 (2013)
Druh dokumentu: article
ISSN: 1347-8613
DOI: 10.1254/jphs.13016FP
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
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