Potential antipsoriatic avarol derivatives as antioxidants and inhibitors of PGE(2) generation and proliferation in the HaCaT cell line

Journal of Natural Products
M AmigóS de Rosa

Abstract

The synthesis and structure-activity relationships for a series of 14 new avarol derivatives as antioxidants and inhibitors of cell proliferation and PGE(2) generation in human keratinocytes are described. Compound 6 (thiosalicylic derivative) was the most potent inhibitor of superoxide generation in human neutrophils and also potently inhibited PGE(2) generation in the human keratinocyte HaCaT cell line. Compound 7(3'-methylaminoavarone) presented the best antiproliferative profile, by the inhibition of (3)H-thymidine incorporation in HaCaT cells, with potency similar to the reference compound anthralin. None of the avarol derivatives showed any sign of cytotoxicity measured as LDH release in treated keratinocytes. The potency and pharmacological profile of derivatives are also discussed.

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Citations

Feb 23, 2011·Marine Drugs·Marina Gordaliza
Jun 19, 2014·Journal of Enzyme Inhibition and Medicinal Chemistry·Giuseppina TommonaroSalvatore De Rosa
Jun 27, 2015·Journal of Enzyme Inhibition and Medicinal Chemistry·Giuseppina TommonaroSalvatore De Rosa
Oct 27, 2007·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Dusan Sladić, Miroslav J Gasić
Jul 30, 2016·Marine Drugs·Chun-Yu ChenTsong-Long Hwang
Aug 31, 2014·Immunology Letters·Sabrina LisiMargherita Sisto
Sep 18, 2007·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Maria TsoukatouVassilios Roussis
Jul 28, 2005·Natural Product Reports·Braulio M Fraga
Oct 3, 2014·Basic & Clinical Pharmacology & Toxicology·Marilia Trindade de Santana SouzaLucindo José Quintans-Júnior
Nov 15, 2008·Journal of Natural Products·Boris PejinSalvatore De Rosa
Feb 23, 2018·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Li LiuHou-Wen Lin
Aug 3, 2018·Journal of Medicinal Chemistry·Feng ChenPeter J Sadler
Aug 27, 2021·Marine Drugs·Roberta EspositoMaria Costantini

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