School of Chinese materia medica, Beijing University of Chinese Medicine, Beijing 102488, China.
Beijing Research Institute of Chinese Medicine, Beijing University of Chinese Medicine, Beijing 100029, China.
Molecules. 2019 Sep 16;24(18):3369. doi: 10.3390/molecules24183369.
Oridonin (ORI) is a natural active ingredient with strong anticancer activity. But its clinical use is restricted due to its poor water solubility, short half-life, and low bioavailability. The aim of this study is to utilize the metal organic framework material MOF-5 to load ORI in order to improve its release characteristics and bioavailability. Herein, MOF-5 was synthesized by the solvothermal method and direct addition method, and characterized by Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD), Fourier Transform Infrared Spectrometer (FTIR), Thermogravimetric Analysis (TG), Brunauer-Emmett-Teller (BET), and Dynamic Light Scattering (DLS), respectively. MOF-5 prepared by the optimal synthesis method was selected for drug-loading and in vitro release experiments. HepG2 cells were model cells. MTT assay, 4',6-diamidino-2-phenylindole (DAPI) staining and Annexin V/PI assay were used to detect the biological safety of blank carriers and the anticancer activity of drug-loaded materials. The results showed that nano-MOF-5 prepared by the direct addition method had complete structure, uniform size and good biocompatibility, and was suitable as an ORI carrier. The drug loading of ORI@MOF-5 was 52.86% ± 0.59%. The sustained release effect was reliable, and the cumulative release rate was about 87% in 60 h. ORI@MOF-5 had significant cytotoxicity (IC50:22.99 μg/mL) and apoptosis effect on HepG2 cells. ORI@MOF-5 is hopeful to become a new anticancer sustained release preparation. MOF-5 has significant potential as a drug carrier material.
冬凌草甲素（ORI）是一种具有强抗癌活性的天然活性成分。但其临床应用受到水溶性差、半衰期短、生物利用度低等因素的限制。本研究旨在利用金属有机骨架材料 MOF-5 负载 ORI，以改善其释放特性和生物利用度。本文采用溶剂热法和直接添加法合成 MOF-5，分别采用扫描电子显微镜（SEM）、X 射线衍射（XRD）、傅里叶变换红外光谱（FTIR）、热重分析（TG）、比表面积和孔径分析（BET）、动态光散射（DLS）对其进行了表征。选择最佳合成方法制备的 MOF-5 进行载药和体外释放实验。HepG2 细胞为模型细胞。MTT 法、4',6-二脒基-2-苯基吲哚（DAPI）染色和 Annexin V/PI 法检测空白载体的生物安全性和载药材料的抗癌活性。结果表明，直接添加法制备的纳米 MOF-5 结构完整、粒径均匀、生物相容性好，适合作为 ORI 载体。ORI@MOF-5 的载药量为 52.86%±0.59%。具有可靠的缓释效果，60 h 累积释放率约为 87%。ORI@MOF-5 对 HepG2 细胞具有显著的细胞毒性（IC50：22.99μg/mL）和凋亡作用。ORI@MOF-5 有望成为一种新的抗癌缓释制剂。MOF-5 作为药物载体材料具有重要的应用潜力。
