载有 5-氟尿嘧啶的纤维素纤维可能具有抗癌活性，这些纤维素纤维来自稻草。
The Potential Anticancer Activity of 5-Fluorouracil Loaded in Cellulose Fibers Isolated from Rice Straw.
机构信息
Malaysia-Japan International Institute of Technology, Universiti Teknologi Malaysia, Kuala Lumpur 54100, Malaysia.
Department of Chemical Engineering, College of Engineering, Northeastern University, Boston, MA 02115, USA.
出版信息
Int J Nanomedicine. 2020 Jul 29;15:5417-5432. doi: 10.2147/IJN.S250047. eCollection 2020.
INTRODUCTION
Green-based materials have been increasingly studied to circumvent off-target cytotoxicity and other side-effects from conventional chemotherapy.
MATERIALS AND METHODS
Here, cellulose fibers (CF) were isolated from rice straw (RS) waste by using an eco-friendly alkali treatment. The CF network served as an anticancer drug carrier for 5-fluorouracil (5-FU). The physicochemical and thermal properties of CF, pure 5-FU drug, and the 5-FU-loaded CF (CF/5-FU) samples were evaluated. The samples were assessed for in vitro cytotoxicity assays using human colorectal cancer (HCT116) and normal (CCD112) cell lines, along with human nasopharyngeal cancer (HONE-1) and normal (NP 460) cell lines after 72-hours of treatment.
RESULTS
XRD and FTIR revealed the successful alkali treatment of RS to isolate CF with high purity and crystallinity. Compared to RS, the alkali-treated CF showed an almost fourfold increase in surface area and zeta potential of up to -33.61 mV. SEM images illustrated the CF network with a rod-shaped structure and comprised of ordered aggregated cellulose. TGA results proved that the thermal stability of 5-FU increased within the drug carrier. Based on UV-spectroscopy measurements for 5-FU loading into CF, drug loading encapsulation efficiency was estimated to be 83 ±0.8%. The release media at pH 7.4 and pH 1.2 showed a maximum drug release of 79% and 46%, respectively, over 24 hours. In cytotoxicity assays, CF showed almost no damage, while pure 5-FU killed most of the both normal and cancer cells. Impressively, the drug-loaded sample of CF/5-FU at a 250 µg/mL concentration demonstrated a 58% inhibition against colorectal cancer cells, but only a 23% inhibition against normal colorectal cells. Further, a 62.50 µg/mL concentration of CF/5FU eliminated 71% and 39% of nasopharyngeal carcinoma and normal nasopharyngeal cells, respectively.
DISCUSSION
This study, therefore, showed the strong potential anticancer activity of the novel CF/5-FU formulations, warranting their further investigation.
简介
为了规避传统化疗的脱靶细胞毒性和其他副作用，人们越来越多地研究基于绿色的材料。
材料与方法
本文中，我们使用环保的碱处理方法从稻秸（RS）废料中分离出纤维素纤维（CF）。CF 网络可用作 5-氟尿嘧啶（5-FU）的抗癌药物载体。评估了 CF、纯 5-FU 药物和负载 5-FU 的 CF（CF/5-FU）样品的物理化学和热性能。使用人结肠癌细胞（HCT116）和正常（CCD112）细胞系以及人鼻咽癌细胞（HONE-1）和正常（NP 460）细胞系，在 72 小时的治疗后，进行了体外细胞毒性测定评估。
结果
XRD 和 FTIR 表明 RS 的碱处理成功分离出高纯度和结晶度的 CF。与 RS 相比，碱处理后的 CF 的表面积增加了近四倍，达到-33.61 mV。SEM 图像说明了 CF 网络的棒状结构，由有序聚集的纤维素组成。TGA 结果证明，药物载体内 5-FU 的热稳定性增加。基于 CF 负载 5-FU 的紫外光谱测量，药物负载包封效率估计为 83±0.8%。在 pH 值为 7.4 和 1.2 的释放介质中，分别在 24 小时内最大释放 79%和 46%的药物。在细胞毒性测定中，CF 几乎没有损伤，而纯 5-FU 杀死了大部分正常和癌细胞。令人印象深刻的是，CF/5-FU 药物负载样品在 250 µg/mL 浓度下对结肠癌细胞的抑制率为 58%，而对正常结肠癌细胞的抑制率仅为 23%。此外，CF/5FU 的浓度为 62.50 µg/mL 时，消除了 71%和 39%的鼻咽癌细胞和正常鼻咽细胞。
讨论
因此，本研究表明新型 CF/5-FU 制剂具有很强的抗癌活性潜力，值得进一步研究。
Zotero 插件