School of Biosciences & Technology, Vellore Institute of Technology, Vellore, TN 632 014, India.
Centre for Nanotechnology Research, Vellore Institute of Technology, Vellore, TN 632 014, India.
IET Nanobiotechnol. 2020 Dec;14(9):796-802. doi: 10.1049/iet-nbt.2020.0103.
Honokiol (HK) is a natural product isolated from the bark, cones, seeds and leaves of plants belonging to the genus Magnolia. It possesses anti-cancer activity which can efficiently impede the growth and bring about apoptosis of a diversity of cancer cells. The major concerns of using HK are its poor solubility and lack of targeted drug delivery. In this study, a combinatorial drug is prepared by combining HK and camptothecin (CPT). Both CPT and HK belong to the genus and induce apoptosis by cell cycle arrest at the S-phase and G1 phase, respectively. The combinatorial drug thus synthesised was loaded onto a chitosan functionalised graphene oxide nanoparticles, predecorated with folic acid for site-specific drug delivery. The CPT drug-loaded nanocarrier was characterised by X-ray diffractometer, scanning electron microscope, transmission electron microscope, UV-vis spectroscopy and fluorescence spectroscopy, atomic force microscopy. The antioxidant properties, haemolytic activity and anti-inflammatory activities were analysed. The cellular toxicity was analysed by 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT assay) and Sulforhodamine B (SRB) assay against breast cancer (MCF-7) cell lines.
厚朴酚（HK）是一种从木兰属植物的树皮、球果、种子和叶子中分离出来的天然产物。它具有抗癌活性，能有效抑制多种癌细胞的生长并诱导其凋亡。使用 HK 的主要问题是其溶解度差和缺乏靶向药物传递。在本研究中，通过将 HK 和喜树碱（CPT）组合制备了一种组合药物。CPT 和 HK 均属于该属，分别通过细胞周期阻滞在 S 期和 G1 期诱导细胞凋亡。因此，将合成的组合药物负载到壳聚糖功能化的氧化石墨烯纳米粒子上，预先用叶酸进行修饰以实现靶向药物传递。通过 X 射线衍射仪、扫描电子显微镜、透射电子显微镜、紫外可见分光光度计和荧光分光光度计、原子力显微镜对载药纳米载体进行了表征。分析了其抗氧化、溶血和抗炎活性。通过 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT 法）和磺基罗丹明 B（SRB）法对乳腺癌（MCF-7）细胞系进行了细胞毒性分析。
