• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>RSC Advances >Nanodelivery of parthenolide using functionalized nanographene enhances its anticancer activity
【24h】

Nanodelivery of parthenolide using functionalized nanographene enhances its anticancer activity

机译：使用功能化的纳米石墨烯对小白菊内酯的纳米递送可增强其抗癌活性

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Advances in anticancer chemotherapy have been hindered by the lack of biocompatibility of new prospective drugs. One significant challenge concerns water insolubility, which compromises the bioavailability of the drugs leading to increased dosage and higher systemic toxicity. To overcome these problems, nanodelivery has been established as a promising approach for increasing the efficacy and lowering the required dosage of chemotherapeutics. The naturally derived compound, parthenolide (PTL), is known for its anti-inflammatory and anticancer activity, but its poor water solubility limits its clinical value. In the present study, we have used carboxyl-functionalized nanographene (fGn) delivery to overcome the extreme hydrophobicity of this drug. A water-soluble PTL analog, dimethylaminoparthenolide (DMAPT), was also examined for comparison with the anticancer efficacy of our PTL-fGn complex. Delivery by fGn was found to increase the anticancer/apoptotic effects of PTL (but not DMAPT) when delivered to the human pancreatic cancer cell line Panc-1. The IC50 value for PTL decreased from 39 mu M to 9.5 mu M when delivered as a mixture with fGn. The IC50 of DMAPT did not decrease when delivered as DMAPT-fGn and was significantly higher than that for PTL-fGn. There were significant increases in ROS formation and in mitochondrial membrane disruption in Panc-1 cells after PTL-fGn treatment as compared to PTL treatment, alone. Increases in toxicity were also seen with apoptosis detection assays using flow cytometry, ethidium bromide/acridine orange/DAPI staining, and TUNEL. Thus, fGn delivery was successfully used to overcome the poor water solubility of PTL, providing a strategy for improving the effectiveness of this anticancer agent.
机译：由于新的前瞻性药物缺乏生物相容性，阻碍了抗癌化学疗法的进展。一个重大挑战涉及水不溶性，水不溶性损害了药物的生物利用度，导致剂量增加和更高的全身毒性。为了克服这些问题，已经建立了纳米递送作为增加疗效和降低所需化学治疗剂量的有前途的方法。天然衍生的化合物，单苯乙内酯（PTL），以其抗炎和抗癌活性而著称，但其水溶性差限制了其临床价值。在本研究中，我们已经使用了羧基官能化的纳米石墨烯（fGn）来克服这种药物的极端疏水性。还检查了水溶性PTL类似物二甲基氨基酚（DMAPT），以与我们的PTL-fGn复合物的抗癌功效进行比较。当递送至人胰腺癌细胞系Panc-1时，发现fGn的递送增加了PTL（但不是DMAPT）的抗癌/凋亡作用。当与fGn混合时，PTL的IC50值从39μM降低到9.5μM。当以DMAPT-fGn的形式交付时，DMAPT的IC50不会降低，并且明显高于PTL-fGn。与单独使用PTL处理相比，PTL-fGn处理后Panc-1细胞的ROS形成和线粒体膜破坏显着增加。使用流式细胞仪，溴化乙锭/ ac啶橙/ DAPI染色和TUNEL进行凋亡检测测定，还发现毒性增加。因此，fGn传递已成功用于克服PTL较差的水溶性，从而提供了提高该抗癌剂有效性的策略。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号