Abstract
Semisynthesis of 13 new thio avarol derivatives (4-16) and in vitro evaluation on the photodamage response induced by UVB irradiation are described. Their ability to inhibit NF-kappaB activation and TNF-alpha generation in HaCaT cells as well as their antioxidant capacity in human neutrophils has also been studied. Among them we have identified two monophenyl thio avarol derivatives (4-5) lacking cytotoxicity which can be considered promising UVB photoprotective agents through the potent inhibition of NF-kappaB activation with a mild antioxidant pharmacological profile.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antioxidants / pharmacology*
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Cell Line, Tumor
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Humans
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Magnetic Resonance Spectroscopy
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Models, Chemical
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Molecular Conformation
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NF-kappa B / antagonists & inhibitors
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Neutrophils / drug effects
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Photochemistry / methods*
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Reactive Oxygen Species
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Sesquiterpenes / chemical synthesis*
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Sesquiterpenes / pharmacology*
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Tumor Necrosis Factor-alpha / antagonists & inhibitors
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Ultraviolet Rays
Substances
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Antioxidants
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NF-kappa B
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Reactive Oxygen Species
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Sesquiterpenes
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Tumor Necrosis Factor-alpha
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avarol