Panagiotis Theodosis-Nobelos1, Panos N Kourounakis1, Eleni A Rekka1.
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
Entities:
Keywords:
Antioxidant acid conjugates; antioxidant activity; dyslipidemia; inflammation; lipoxygenase inhibition
Mesh：
Substances：
Year: 2017
PMID： 27823562 DOI： 10.2174/1573406412666161104122310
Source DB: PubMed Journal: Med Chem ISSN： 1573-4064 Impact factor: 2.745