三氧化二砷抗肿瘤作用机制及其药物递送系统的研究进展  

Research progress on anti-tumor mechanisms of arsenic trioxide and its drug delivery system

作　　者：黄剑宇 梁启凡 李俊松[1,2] 王若宁 狄留庆 HUANG Jian-yu;LIANG Qi-fan;LI Jun-song;WANG Ruo-ning;DI Liu-qing(College of Pharmacy,Nanjing University of Chinese Medicine,Nanjing 210046,China;Jiangsu Engineering Research Center for Efficient Delivery System of TCM,Nanjing 210023,China)

机构地区：[1]南京中医药大学药学院,江苏南京210046 [2]江苏省中药高效给药系统工程技术研究中心,江苏南京210023

出　　处：《中草药》2020年第23期6102-6111,共10页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(81903557);国家自然科学基金资助项目(82074024);江苏省自然科学基金资助项目(BK20190802);江苏省高等学校自然科学研究项目(19KJB350003);江苏省科协青年科技人才托举工程资助项目;南京中医药大学自然科学基金青年项目(NZY81903557)。

摘　　要：传统中药矿物药三氧化二砷具有显著的治疗作用,已被美国食品药品监督管理局(FDA)批准用于治疗急性早幼粒细胞白血病,近年来还发现其具有良好的治疗实体瘤的效果。其抗肿瘤机制主要包括促进细胞凋亡、抑制Hedgehog信号通路、逆转耐药性以及抑制血管生成等。然而三氧化二砷的体内靶向性较差、肾脏清除速率快、以及高剂量对正常组织的不良反应,限制了其对实体瘤的治疗应用与临床转化。新型药物递送系统在传统纳米制剂的基础上,提高了药物在肿瘤部位的聚集、控制释放以及诊断等能力,在精准治疗、提高生物利用度和降低毒副作用等方面具有重要意义。对三氧化二砷的抗肿瘤机制及抗肿瘤新型药物递送系统的研究进展进行总结和分析,以期为三氧化二砷抗肿瘤的深入研究和临床应用提供思路。Arsenic trioxide, a mineral drug of Chinese medicine material medica with significant therapeutic effect, has been approved by USA Food and Drug Administration(FDA) for the treatment of acute promyelocytic leukemia. In recent years, it has also been found to have a great therapeutic effect on the treatment of solid tumors. The anti-tumor mechanisms mainly include promoting apoptosis, inhibiting Hedgehog signaling pathway, reversing drug resistance and inhibiting angiogenesis. However, the poor targeting ability in vivo, the rapid renal clearance rate, and the toxic and side effects of high dose on normal tissues of arsenic trioxide limit the application and clinical transformation for the treatment of solid tumor. On the basis of traditional nanoparticles, the novel drug delivery system improves the drug aggregation, controlling-release and diagnosis in tumor sites, which is of great significance in accurate treatment, improvement of bioavailability and reduction of toxic and side effects. Research progress on anti-tumor mechanisms of arsenic trioxide and its drug delivery system in recent years was summarized and analyzed in this paper, in order to provide ideas for the in-depth research and clinical application of arsenic trioxide.

关 键 词：三氧化二砷 抗肿瘤机制 药物递送系统 被动靶向 主动靶向 物理化学靶向 细胞凋亡 逆转耐药性 抑制血管生成 

分 类 号：R285[医药卫生—中药学] R283.6[医药卫生—中医学]