Corina Danciu, Florina Bojin, Iulia Pinzaru, Cristina Dehelean, Rita Ambrus, Alexandra Popescu, Virgil Paunescu, Hancianu Monica, Daliana Minda, Codruta Soica
Department of Pharmacognosy, Faculty of Pharmacy, "Victor Babes" University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Romania.
Department of Functional Sciences, Faculty of Medicine, "Victor Babes" University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Romania.
Curr Pharm Biotechnol. 2017;18(13):1067-1077. doi: 10.2174/1389201019666180209165523.
Recent studies have shown that rutin presents a heightened interest due to the plethora of biological activities. The major drawback for this phytocompound is the poor water solubility, a parameter that limits its bioavailability. The study aimed to prepare and assess the inclusion complexes of rutin with β-cyclodextrin (BCD) and hydroxypropyl-β-cyclodextrin (HPBCD), followed by the evaluation of the antioxidant, antiproliferative and pro-apoptotic activity against B164A5 murine melanoma cell line.
Inclusion complexes were prepared by kneading method. Scanning electron microscopy, differential scanning calorimetry and X-ray powder diffraction were used in order to assess their formation. Antioxidant activity was determined by DPPH assay. Antiproliferative and pro-apoptotic effects where tested by MTT, respectively Annexin V-PI assays. Physico-chemical methods proved that incorporation took place.
Results show that rutin presents antioxidant activity, and complexation increases this property. After 72 h of incubation at the concentration of 100 µM rutin proved to be an active antiproliferative and pro-apoptotic compound against B164A5 cells.
Incorporation in BCD and HBCD maintained the activity, thus representing an important finding and open path for in vivo experiments.
最近的研究表明，由于芦丁具有多种生物活性，它受到了越来越多的关注。这种植物化合物的主要缺点是水溶性差，这一参数限制了其生物利用度。本研究旨在制备并评估芦丁与β-环糊精（BCD）和羟丙基-β-环糊精（HPBCD）的包合物，随后评估其对B164A5小鼠黑色素瘤细胞系的抗氧化、抗增殖和促凋亡活性。
采用捏合法制备包合物。使用扫描电子显微镜、差示扫描量热法和X射线粉末衍射法来评估它们的形成。通过DPPH法测定抗氧化活性。分别通过MTT法和Annexin V-PI法检测抗增殖和促凋亡作用。物理化学方法证明了包合作用的发生。
结果表明芦丁具有抗氧化活性，络合作用增强了这一特性。在100μM浓度下孵育72小时后，芦丁被证明是一种对B164A5细胞具有活性的抗增殖和促凋亡化合物。
包合到BCD和HBCD中保持了活性，因此这是一个重要的发现，并为体内实验开辟了道路。
