中文关键词:柱[5]芳烃主客体作用纳米药物输送系统抗肿瘤活性 英文关键词:Pilar[5]areneHost-guest interactionNano drug delivery systemAntitumor activity 基金项目:国家自然科学基金项目（21967004）和广西中药质量标准研究重点实验室项目（桂中重开201803）资助

作者	单位	E-mail
周清清	广西大学化学化工学院 南宁 530004
段文贵	广西大学化学化工学院 南宁 530004
刘陆智	广西大学化学化工学院 南宁 530004	llzh068@163.com
黄艳	广西中医药研究院&广西中药质量标准研究重点实验室 南宁 530022	hy2002-2006@163.com

摘要点击次数:265 全文下载次数:0 中文摘要: 合成了一种新型的丙氨酸取代水溶性柱[5]芳烃DAP5，以此作为构建单元可与十二烷基苯磺酸钠（SDBS）通过主客体作用构筑出可高效包载抗癌药物阿霉素（DOX）的超分子纳米载体SDBS⊂DAP5，包封率为62.6%。该纳米载药体系不仅具有较好的pH响应性能并在模拟肿瘤弱酸性微环境中可持续释放药物，而且对正常肝细胞（LO2）具有较低的毒性（半抑制浓度IC₅₀>10μmol/L），重要的是对四种测试的癌细胞（Hela、HepG2、MGC-803和T24）表现出比裸药更强的增殖抑制活性和更短的用药时间。其中，对于HepG2效果更为显著，作用24h后，其IC₅₀为0.77μmol/L，约为裸药DOX（3.43μmol/L）的22%。上述结果为超分子载药体系在未来肿瘤的治疗中提高药物的有效性以及降低毒副作用提供了重要的参考信息。 英文摘要: A novel alanine substituted water-soluble pillar[5]arene DAP5 was synthesized, which could be used as building block to construct a supramolecular nano drug loading carrier SDBS⊂DAP5 through host-guest interaction with sodium dodecylbenzene sulfonate (SDBS). This carrier can efficiently encapsulate DOX with an entrapment efficiency of 62.6%. And its nano drug delivery system DOX⊂SDBS⊂DAP5 not only had good pH response performance and could continuously release the drug in a simulated weak acid tumor microenvironment, but also had low toxicity to normal liver cells (LO2) (IC₅₀ >10μmol/L). More importantly, DOX⊂SDBS⊂DAP5 exhibited stronger proliferation inhibition activity and shorter medication time over free drug for four tested cancer cells (Hela, HepG2, MGC-803 and T24). Especially for HepG2, after 24 hours of incubation with drug, IC₅₀ of DOX⊂SDBS⊂DAP5 was 0.77 μmol/L, about 22% of that of DOX (3.43 μmol/L). These results provide important reference information for improving the efficacy and reducing the side effects of supramolecular drug delivery system in the future cancer treatment. 查看全文查看/发表评论下载PDF阅读器 相关附件：图文摘要审稿意见回复版权转让声明书 -->