Anti-atherogenic Effects of a New Thienylacylhydrazone Derivative, LASSBio-788, in Rats Fed a Hypercholesterolemic Diet
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- da Motta Nadia Alice Vieira
- Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Brazil
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- Kümmerle Arthur Eugen
- Department of Chemistry, Institute of Exact Sciences, Federal Rural University of Rio de Janeiro (UFRRJ), Brazil
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- Marostica Elisabeth
- Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Brazil
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- dos Santos Caroline Fernandes
- Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Brazil
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- Fraga Carlos Alberto Manssour
- Laboratory of Evaluation and Synthesis of Bioactive Substances (LASSBio®), Federal University of Rio de Janeiro (UFRJ), Center for Health Sciences (CCS), Brazil
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- Barreiro Eliezer Jesus
- Laboratory of Evaluation and Synthesis of Bioactive Substances (LASSBio®), Federal University of Rio de Janeiro (UFRJ), Center for Health Sciences (CCS), Brazil
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- de Miranda Ana Luisa Palhares
- Laboratory of Evaluation and Synthesis of Bioactive Substances (LASSBio®), Federal University of Rio de Janeiro (UFRJ), Center for Health Sciences (CCS), Brazil
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- de Brito Fernanda Carla Ferreira
- Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Brazil
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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.
収録刊行物
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- Journal of Pharmacological Sciences
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Journal of Pharmacological Sciences 123 (1), 47-57, 2013
公益社団法人 日本薬理学会
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詳細情報 詳細情報について
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- CRID
- 1390282680157215744
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- NII論文ID
- 10031202962
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- NII書誌ID
- AA11806667
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- COI
- 1:CAS:528:DC%2BC3sXhsF2ktrzN
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- ISSN
- 13478648
- 13478613
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- NDL書誌ID
- 024863703
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- PubMed
- 24018841
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 使用不可