Interaction of melatonin with model membranes and possible implications in its photoprotective activity.
It is well known that administration of antioxidants represents a successful strategy for preventing the occurrence and for reducing the severity of UV-mediated oxidative damage. Melatonin was recently shown to be an efficacious photoprotective agent. The aim of the present study was to better investigate the interaction of melatonin with model membranes and the possible implications in its photoprotective activity. The antioxidant activity of melatonin was tested in two 'in vitro' experimental models: (a) UV radiation-induced peroxidation in phosphatidylcholine multilamellar vesicles (MLVs); (b) scavenging activity against nitric oxide (NO). Furthermore, we investigated the melatonin/biomembrane interaction by differential scanning calorimetry (DSC) on dimyristoylphosphatidylcholine (DMPC) MLVs and unilamellar vesicles (LUVs). The findings of in vitro antioxidant tests suggest that the photoprotective effect of melatonin should be due, partially at least, to the drug scavenging activity against aqueous and lipophilic free radicals, including NO; besides, melatonin might provide its protective effect against UV radiation-induced damage also by acting as a UV-absorbing screen. The results of DSC experiments have evidenced a good capability of melatonin to interact with DMPC bilayers, causing a significant fluidifying effect; however, the transfer of melatonin in the LUVs is faster than that observed for MLVs, even if both values tend to the maximum values reachable. Our present data allow us to emphasize two points: (1) the fluidifying effect induced by melatonin on lipidic bilayers might act as a cooperative mechanism in its protective effect against peroxidative membrane damage; (2) melatonin appears able to cross biomembranes, so that it could protect intracellular components against peroxidative insult.
Saija
Antonella
A
Department of Pharmacology of Natural Substances and General Physiology, University of Rome, La Sapienza, Italy. saija@pharma.unime.it
Tomaino
Antonio
A
Trombetta
Domenico
D
Pellegrino
Maria Luisa
ML
Tita
Beatrice
B
Caruso
Sebastiana
S
Castelli
Francesco
F
D000975:Antioxidants / Q000737:chemistry* / Q000494:pharmacology; D008051:Lipid Bilayers / Q000737:chemistry / Q000494:pharmacology; D015227:Lipid Peroxidation / Q000187:drug effects; D008081:Liposomes / Q000737:chemistry* / Q000494:pharmacology; D008550:Melatonin / Q000737:chemistry* / Q000494:pharmacology; D013473:Sunscreening Agents / Q000737:chemistry* / Q000494:pharmacology; D014466:Ultraviolet Rays / Q000009:adverse effects
D000975:Antioxidants; D008051:Lipid Bilayers; D008081:Liposomes; D013473:Sunscreening Agents; D008550:Melatonin