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键合紫杉醇和姜黄素的金纳米棒的制备及体外抗肿瘤多药耐药研究
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| 篇名： | 键合紫杉醇和姜黄素的金纳米棒的制备及体外抗肿瘤多药耐药研究 |
| TITLE： | |
| 摘要： | 目的：制备键合紫杉醇（PTX）和姜黄素（CUR）的金纳米棒（GNR）（PTX/CUR-BPGNR），并初步研究其体外抗肿瘤多药耐药（MDR）作用及机制。方法：用晶种生长法制备GNR，然后经生物素-聚乙二醇修饰制成GNR（BPGNR）。分别合成PTX和CUR的硫辛酸酯（PTXLA和CURLA），使用核磁共振氢谱（1H-NMR）和质谱等手段确定其化学结构。利用金硫键牢固的结合作用，将PTXLA和CURLA连接到BPGNR表面，得到键合PTX和CUR的BPGNR（PTX/CUR-BPGNR）。观察其形貌，考察其载药量和体外释药情况（近红外光照和酯酶条件下）。以阿霉素（ADR）的MDR人乳腺癌细胞MCF-7/ADR为研究对象，分别经PTX、CUR、PTX/CUR混合物和PTX/CUR-BPGNR处理后，采用MTT法考察MCF-7/ADR细胞的存活率，酶联免疫吸附测定法检测细胞中P-糖蛋白（P-gp）表达水平。结果：成功制得PTX/CUR-BPGNR，其大小、形状均一，最大吸收波长为808 nm，其中PTX和CUR的载药量分别为16.1％、8.4％，同时给予近红外光照和酯酶能促进PTX和CUR释放，64 h的累积释放度分别可达37.2％、39.1％。BPGNR、PTX、CUR、PTX/CUR混合物和PTX/CUR-BPGNR处理后MCF-7/ADR细胞的存活率分别为95.8％、71.2％、91.9％、45.8％、22.5％，细胞中P-gp的相对表达水平分别为105.6％、75.2％、73.8％、51.7％。结论：成功制得PTX/CUR-BPGNR，其可提高CUR抑制P-gp表达的能力，从而增强药物抗MDR的作用。 |
| ABSTRACT： | OBJECTIVE： To prepare paclitaxel（PTX） and curcumin （CUR） chemically conjugated gold nanorod （GNR） （PTX/CUR-BPGNR）， and to preliminarily study its anti-multidrug-resistant（MDR） tumor effect in vitro and mechanisms. METHODS： GNR was prepared by seed growth method and modified with biotin-polyethylene glycol （Biotin-PEG） to obtain BPGNRs. Lipoic acid PTX and CUR （PIXLA and CURLA） were synthesized； 1H-NMR and MS were used to confirm their chemical structures. PTXLA and CURLA were connected to BPGNR surface to obtain PIX and CUR-bonding BPGNR （PTX/CUR-BPGNR） via strong binding of Au-S bond. The morphology of PTX/CUR-BPGNR was observed， and drug-loading amount and in vitro drug release were investigated （under near-infrared illumination and esterase condition）. Adriamycin （ADR） MDR breast cancer MCF-7/ADR cells were selected as research objects， and MTT assay was used to investigate the survival rate of cells after treated with BPGNR， PTX， CUR， PTX/CUR mixture and PTX/CUR-BPGNR， and ELISA was used to detect the expression of P-gp. RESULTS： PTX/CUR-BPGNR was prepared successfully with uniform size and shape. The maximum absorption wavelength was 808 nm， and drug-loading amount of PTX and CUR were 16.1％ and 8.4％， respectively. The preparations were given near-infrared illumination and esterase to promote the release of PTX and CUR. 64 h accumulative drug release rates were 37.2％ and 39.1％. Survival rates of MCF-7/ADR cells after treated with BPGNR， PTX， CUR and PTX/CUR mixture， PTX/CUR-BPGNR were 95.8％， 71.2％， 91.9％， 45.8％ and 22.5％， respectively. The relative expressions of P-gp in cells were 105.6％， 75.2％， 73.8％， 51.7％， respectively. CONCLUSIONS： PTX/CUR-BPGNR is successfully prepared and can improve the ability of CUR inhibiting the expression of P-gp so as to strengthen its anti-MDR effects. |
| 期刊： | 2018年第29卷第15期 |
| 作者： | 徐绍辉，张志鹏，黄胜堂，沈园园，于坤宏 |
| AUTHORS： | XU Shaohui，ZHANG Zhipeng，HUANG Shengtang，SHEN Yuanyuan，YU Kunhong |
| 关键字： | 紫杉醇；姜黄素；金纳米棒；抗肿瘤多药耐药；P-糖蛋白 |
| KEYWORDS： | Paclitaxel； Curcumin； Gold nanorods； Multidrug resistant cancer； P-gp |
| 阅读数： | 477 次 |
| 本月下载数： | 7 次 |
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