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Antioxidant Serine-(NSAID) Hybrids with Anti-Inflammatory and Hypolipidemic Potency
| Content Provider | MDPI |
|---|---|
| Author | Theodosis-Nobelos, Panagiotis Papagiouvannis, Georgios Tziona, Paraskevi Kourounakis, Panos Rekka, Eleni |
| Copyright Year | 2021 |
| Description | A series of L-serine amides of antioxidant acids, such as Trolox, (E)-3-(3,5-di-tert-butyl-4-hydroxyphenyl)acrylic acid (phenolic derivative of cinnamic acid) and 3,5-di-tert-butyl-4-hydroxybenzoic acid (structurally similar to butylated hydroxytoluene), was synthesized. The hydroxy group of serine was esterified with two classical NSAIDs, ibuprofen and ketoprofen. The Trolox derivatives with ibuprofen (7) and ketoprofen (10) were the most potent inhibitors of lipid peroxidation $(IC_{50}$ 3.4 μΜ and 2.8 μΜ), several times more potent than the reference Trolox $(IC_{50}$ 25 μΜ). Most of the compounds decreased carrageenan-induced rat paw edema (37–67% at 150 μmol/kg). They were moderate inhibitors of soybean lipoxygenase, with the exception of ibuprofen derivative 8 $(IC_{50}$ 13 μΜ). The most active anti-inflammatory compounds exhibited a significant decrease in lipidemic indices in the plasma of Triton-induced hyperlipidemic rats, e.g., the most active compound 9 decreased triglycerides, total cholesterol and low-density lipoprotein cholesterol by 52%, 61% and 70%, respectively, at 150 μmol/kg (i.p.), similar to that of simvastatin, a well-known hypocholesterolemic drug. Since the designed compounds seem to exhibit multiple pharmacological actions, they may be of use for the development of agents against inflammatory and degenerative conditions. |
| Starting Page | 4060 |
| e-ISSN | 14203049 |
| DOI | 10.3390/molecules26134060 |
| Journal | Molecules |
| Issue Number | 13 |
| Volume Number | 26 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2021-07-02 |
| Access Restriction | Open |
| Subject Keyword | Molecules Medicinal Chemistry Antioxidant Serine Conjugates Inflammation Lipoxygenase Inhibition Dyslipidemia Antioxidant Activity Anti-inflammatory Agents |
| Content Type | Text |
| Resource Type | Article |
