Rezaei-Sadabady Rogaie, Eidi Akram, Zarghami Nosratollah, Barzegar Abolfazl
a Department of Biology , Science and Research Branch Tehran, Islamic Azad University , Tehran , Iran.
b Department of Medical Biotechnology , and Biotechnology, Faculty of Advanced Medical Science, Tabriz University of Medical Sciences , Tabriz , Iran.
Artif Cells Nanomed Biotechnol. 2016;44(1):128-34. doi: 10.3109/21691401.2014.926456. Epub 2014 Jun 24.
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.
槲皮素(3,5,7,3',4'-五羟基黄酮)是一种天然生物类黄酮,源自水果、蔬菜、种子、浆果和茶。槲皮素的抗氧化活性及其对心血管疾病的保护作用、抗癌、抗炎和抗病毒活性已有大量文献记载;然而,由于其递送特性很差,槲皮素在癌症治疗中的临床应用受到显著限制。为了提高亲水性和药物递送能力,我们将槲皮素包裹在脂质体中。我们的数据表明,脂质体包裹的槲皮素能显著提高槲皮素的溶解度和生物利用度,可作为一种有效的抗氧化剂用于极性细胞质内的活性氧保护,并且脂质体包裹的纳米级槲皮素增强了细胞摄取(人MCF_7癌细胞)。槲皮素具有许多药物应用,其中许多源于其强大的抗氧化特性。本研究通过在水介质中还原三价铁、细胞内活性氧/毒性测定以及还原DPPH测定的比较研究,考察了槲皮素在极性溶剂中的抗氧化活性。细胞活力和活性氧测定表明,槲皮素能够穿透细胞内的极性介质,并保护它们免受氢过氧化异丙苯的高毒性和致命影响。本研究的目的是确定槲皮素的脂质体制剂是否能显著提高其溶解度和生物利用度,以及是否可能用于肿瘤治疗。作者将槲皮素包裹在脂质体递送系统中。他们使用人MCF-7癌细胞研究了该化合物对增殖的体外作用。在等摩尔浓度下,脂质体包裹的槲皮素的活性等于或优于游离槲皮素。我们的数据表明,脂质体包裹的槲皮素能显著提高槲皮素的溶解度和生物利用度,并且可能在肿瘤治疗中具有潜在应用。