Anti-inflammatory and Hypolipidemic Effect of Novel Conjugates with Trolox and Other Antioxidant Acids

Title:Anti-inflammatory and Hypolipidemic Effect of Novel Conjugates with Trolox and Other Antioxidant Acids

Volume: 13 Issue: 3

Author(s): Panagiotis Theodosis-Nobelos, Panos N. Kourounakis and Eleni A. Rekka*

Affiliation:

• Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54124,Greece

Keywords: Antioxidant acid conjugates, inflammation, lipoxygenase inhibition, dyslipidemia, antioxidant activity.

Abstract: Objectives: A series of esters and amides, incorporating an antioxidant residue, such as trolox or caffeic acid, and various moieties with different biological activities, were synthesised.

The obtained compounds demonstrated considerable anti-inflammatory, radical scavenging and antioxidant action. Thus, they could reduce carrageenan-induced rat paw oedema by 31-60% at 150 μmol/kg and inhibit rat microsomal membrane lipid peroxidation with IC50 values as low as 1.4 μM, which is much lower than that of trolox. Most of them could also inhibit soybean lipoxygenase. The thiomorpholine derivatives decreased significantly all lipidemic indices of Triton-induced hyperlipidemia in rats. The most active, the caffeic acid derivative (6), decreases triglycerides, total cholesterol and low density lipoprotein, in the plasma of hyperlipidemic rats, by 70%, 67%, and 73%, respectively, at 150 μmol/kg (i.p.).

Conclusion: The synthesised compounds, designed to exhibit two or more pharmacological actions, may be considered useful in the study of agents addressed to conditions involving inflammation and oxidative stress.

Cite this article as:

Theodosis-Nobelos Panagiotis, Kourounakis N. Panos and Rekka A. Eleni*, Anti-inflammatory and Hypolipidemic Effect of Novel Conjugates with Trolox and Other Antioxidant Acids, Medicinal Chemistry 2017; 13 (3) . https://dx.doi.org/10.2174/1573406412666161104122310

DOI https://dx.doi.org/10.2174/1573406412666161104122310	Print ISSN 1573-4064
Publisher Name Bentham Science Publisher	Online ISSN 1875-6638