金属-有机骨架-5 (MOF-5) 作为抗肿瘤药物冬凌草素缓释载体的研究,Molecules

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金属-有机骨架-5 (MOF-5) 作为抗肿瘤药物冬凌草素缓释载体的研究
Molecules ( IF 4.2 ) Pub Date : 2019-09-16 , DOI: 10.3390/molecules24183369
Gongsen Chen ₁ , Juyuan Luo ₁ , Mengru Cai ₁ , Liuying Qin ₁ , Yibo Wang ₁ , Lili Gao ₁ , Pingqing Huang ₁ , Yingchao Yu ₁ , Yangming Ding ₁ , Xiaoxv Dong ₁ , Xingbin Yin ₁ , Jian Ni _{1,

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Affiliation

Oridonin (ORI) 是一种天然活性成分，具有很强的抗癌活性。但由于其水溶性差、半衰期短、生物利用度低，其临床应用受到限制。本研究的目的是利用金属有机骨架材料 MOF-5 负载 ORI，以提高其释放特性和生物利用度。在此，MOF-5 通过溶剂热法和直接添加法合成，并通过扫描电子显微镜 (SEM)、X 射线衍射 (XRD)、傅里叶变换红外光谱仪 (FTIR)、热重分析 (TG)、Brunauer-分别是 Emmett-Teller (BET) 和动态光散射 (DLS)。选用最优合成方法制备的MOF-5进行载药和体外释放实验。HepG2 细胞是模型细胞。MTT 测定，4'，采用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、尺寸均匀、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%。缓释效果可靠，60h累积释放率约87%。ORI@MOF-5对HepG2细胞具有显着的细胞毒性（IC50：22.99 μg/mL）和凋亡作用。ORI@MOF-5有望成为一种新型的抗癌缓释制剂。MOF-5 作为药物载体材料具有巨大的潜力。

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Investigation of Metal-Organic Framework-5 (MOF-5) as an Antitumor Drug Oridonin Sustained Release Carrier

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.

更新日期：2019-09-16

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