| Title | Hypolipidaemic and antioxidant properties of novel squalene synthase inhibitors | ||
| Authors | A. Matralis and Α. Κourounakis
Div. of Medicinal Chemistry, Dept. of Pharmacy, University of Athens, Greece |
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| Citation | Matralis, A., Kourounakis, A.: Hypolipidaemic and antioxidant properties of novel squalene synthase inhibitors, Epitheorese Klin. Farmakol. Farmakokinet. 22(2): 238-240 (2008) | ||
| Publication Date | 23-25 May 2008 | ||
| Full Text Language | English | ||
| Order – Buy | Ηλεκτρονική Μορφή: pdf (10 €) – Digital Type: pdf (10 €)
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| Keywords | Squalene synthase inhibitor, hypercholesterolaemia, atherosclerosis, antioxidant compounds. | ||
| Other Terms | Review article | ||
| Summary | Elevated as well as oxidized levels of LDL-cholesterol and lipids in plasma are major factors in the pathogenesis of atherosclerosis. The aim of this study is the design and evaluation of new compounds for the treatment of atherosclerosis, that act on the multiple mechanisms involved in this disease. Towards this direction, new compounds that combine structural moieties with potential antihypercholesterolaemic, anti-hyperlipidaemic as well as antioxidant activity were synthesized and their activity was determined in vitro and in vivo. The six new derivatives were found to inhibit rat hepatic microsomal lipid peroxidation (IC50 = 650-170 μΜ) as well as the activity of squalene synthase (IC50 = 0.7-48 μΜ), the enzyme that catalyzes the first committed step towards cholesterol biosynthesis. Further, after administration to hyperlipidaemic rats, they reduced plasma levels of total cholesterol, LDL-cholesterol as well as triglycerides up to 80%. The combined activities of these compounds provide them with potential antiatherosclerotic activity. | ||
| References | 1. Kourounakis et al.: submitted for publication
2. Tavridou A., et al.: Eur. J. Pharmacol. 535(1-3): 34-42 (2006) 3. Kourounakis A., et al.: Drug Development Res. 41: 9 (1999) 4. Chrysselis M., et al.: J. Med. Chem. 43: 609 (2000) 5. Pandit J.: J. Biol. Chem. 275: 30610 (2000) |
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| Relative Papers | |||
Online ISSN 1011-6575
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Articles published in this Journal are Indexed or Abstracted in: • Chemical Abstracts • Elsevier’s Bibliographic Databases: Scopus, EMBASE, EMBiology, Elsevier BIOBASE SCImago Journal and Country Rank Factor
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