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

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

doi:10.1254/jphs.13016FP

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

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

Author information

Nadia Alice Vieira da Motta
Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Brazil
Arthur Eugen Kümmerle
Department of Chemistry, Institute of Exact Sciences, Federal Rural University of Rio de Janeiro (UFRRJ), Brazil
Elisabeth Marostica
Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Brazil
Caroline Fernandes dos Santos
Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Brazil
Carlos Alberto Manssour Fraga
Laboratory of Evaluation and Synthesis of Bioactive Substances (LASSBio®), Federal University of Rio de Janeiro (UFRJ), Center for Health Sciences (CCS), Brazil
Eliezer Jesus Barreiro
Laboratory of Evaluation and Synthesis of Bioactive Substances (LASSBio®), Federal University of Rio de Janeiro (UFRJ), Center for Health Sciences (CCS), Brazil
Ana Luisa Palhares de Miranda
Laboratory of Evaluation and Synthesis of Bioactive Substances (LASSBio®), Federal University of Rio de Janeiro (UFRJ), Center for Health Sciences (CCS), Brazil
Fernanda Carla Ferreira de Brito
Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Brazil

Keywords: atherosclerosis, anti-platelet, anti-inflammatory, lipid-lowering, thienylacylhydrazone derivative

JOURNAL FREE ACCESS

2013 Volume 123 Issue 1 Pages 47-57

DOI https://doi.org/10.1254/jphs.13016FP

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Abstract

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.

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