title: Intracellular ROS protection efficiency and free radical-scavenging activity of quercetin and quercetin-encapsulated liposomes.
abstract: Quercetin (3,5,7,3',4'-pentahydroxyflavone) is a natural bio-flavonoid originating from fruits, vegetables, seeds, berries, and tea. The antioxidant activity of quercetin and its protective effects against cardiovascular disorders, anti-cancer, anti-inflammatory, and anti-viral activities have been extensively documented; however, the clinical request of quercetin in cancer treatment is significantly limited due to its very poor delivery features. In order to increase the hydrophilicity and drug delivery capability, we encapsulated quercetin into liposomes. Our data indicated that liposomal quercetin can significantly improve the solubility and bioavailability of quercetin and can be used as an effective antioxidant for ROS protection within the polar cytoplasm, and the nano-sized quercetin encapsulated by liposomes enhanced the cellular uptake (cancer cell human MCF_7). Quercetin has many pharmaceutical applications, many of which arise from its potent antioxidant properties. The present research examined the antioxidant activities of quercetin in polar solvents by a comparative study using reduction of ferric iron in aqueous medium, intracellular ROS/toxicity assays, and reducing DPPH assays. Cell viability and ROS assays demonstrated that quercetin was able to penetrate into the polar medium inside the cells and to protect them against the highly toxic and deadly belongings of cumene hydroperoxide. The purpose of this study was to determine whether a liposomal formulation of quercetin can suggestively improve its solubility and bioavailability and can be a possible request in the treatment of tumor. The authors encapsulated quercetin in a liposomal delivery system. They studied the in vitro effects of this compound on proliferation using human MCF-7 carcinoma cells. The activity of liposomal quercetin was equal to or better than that of free quercetin at equimolar concentrations. Our data indicated that liposomal quercetin can significantly improve the solubility and bioavailability of quercetin and can be a potential application in the treatment of tumor.
authors: a Department of Biology , Science and Research Branch Tehran, Islamic Azad University , Tehran , Iran.
authors: Rogaie
authors: R
authors: Rezaei-Sadabady
authors: a Department of Biology , Science and Research Branch Tehran, Islamic Azad University , Tehran , Iran.
authors: Akram
authors: A
authors: Eidi
authors: b Department of Medical Biotechnology , and Biotechnology, Faculty of Advanced Medical Science, Tabriz University of Medical Sciences , Tabriz , Iran.
authors: Nosratollah
authors: N
authors: Zarghami
authors: c Research Institute for Fundamental Sciences (RIFS), University of Tabriz , Tabriz , Iran.
authors: Abolfazl
authors: A
authors: Barzegar
mesh_terms: D001555:Benzene Derivatives / Q000037:antagonists & inhibitors / Q000494:pharmacology; D001682:Biological Availability; D001713:Biphenyl Compounds / Q000037:antagonists & inhibitors / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects; D016166:Free Radical Scavengers / Q000737:chemistry / Q000494:pharmacology*; D005609:Free Radicals / Q000037:antagonists & inhibitors* / Q000737:chemistry; D006801:Humans; D007501:Iron / Q000737:chemistry; D008081:Liposomes / Q000138:chemical synthesis*; D061986:MCF-7 Cells; D010084:Oxidation-Reduction; D010851:Picrates / Q000037:antagonists & inhibitors / Q000737:chemistry; D011794:Quercetin / Q000737:chemistry / Q000494:pharmacology*; D012995:Solubility
chemical_list: D001555:Benzene Derivatives; D001713:Biphenyl Compounds; D016166:Free Radical Scavengers; D005609:Free Radicals; D008081:Liposomes; D010851:Picrates; D011794:Quercetin; C004931:1,1-diphenyl-2-picrylhydrazyl; D007501:Iron; C007164:cumene hydroperoxide
keywords: anti-cancer activity; antioxidant; liposome; nanoparticles; quercetin