首页> 美国卫生研究院文献>Iranian Journal of Pharmaceutical Research : IJPR >Preparation of Diaminedicarboxyplatinum (II) Functionalized Single-Wall Carbon Nanotube via Bingel Reaction as a Novel Cytotoxic Agent
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Preparation of Diaminedicarboxyplatinum (II) Functionalized Single-Wall Carbon Nanotube via Bingel Reaction as a Novel Cytotoxic Agent

机译:通过新型的细胞毒剂Bingel反应制备二胺二羧基铂(II)功能化的单壁碳纳米管

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摘要

Carbon nanotubes have unique properties like high stability, high surface to mass ratio and so on which make them suitable for medicinal purpose applications. Treatment of cancer by organoplatinum agents like Cisplatin has become unresponsive in most cases due to low distribution of drug in biological fluids, inability of drug to cross cellular membranes and low stability in biological environments. Recently, carbon nanotubes (CNT) have stimulated much interest to overcome these limitations. ‎‎ Herein, we report the preparation of single-wall carbon nanotube functionalized by diaminedicarboxyplatinum (II) as an analogy of SWCNT-based Carboplatin. Functionalization was started by cyclopropanation through Bingel reaction and by use of diethylmalonate to yield cyclopropane-1,1-dicarboxy ethyl ester. Final product was obtained by hydrolysis of ester group and then chelation of platinum (IV) by dicarboxylate groups on the surface of SWCNT. Raman and Fourier transform -Infrared ‎spectroscopy (IR), ‎Thermogravimetric ‎analysis ‎(TGA) and energy dispers‎ive X-ray‎spectroscopy ‎(EDAX) truly showed and confirmed the presence of the platinum (II) complex on the side wall of SWCNT. Cytotoxicity evaluation of the functionalized-SWCNTs on HeLa cells showed its higher anticancer ability than Cisplatin as indicated by IC50 value of 13 µg/mL.
机译:碳纳米管具有独特的特性,例如高稳定性,高表面质量比等,使其适合于医疗用途。在大多数情况下,由于有机液体中药物的分布较低,药物无法穿过细胞膜以及在生物环境中稳定性较低,因此使用有机铂类药物(如顺铂)治疗癌症已无反应。最近,碳纳米管(CNT)引起了人们对克服这些局限性的极大兴趣。这里,我们报告了以二胺二羧基铂(II)功能化的单壁碳纳米管的制备方法,该方法类似于基于SWCNT的卡铂。通过通过Bingel反应进行环丙烷化并通过使用丙二酸二乙酯来产生环丙烷-1,1-二羧乙基酯来开始官能化。通过水解酯基团,然后在SWCNT表面上通过二羧酸酯基团螯合铂(IV),可以得到最终产物。拉曼光谱和傅里叶变换-红外光谱(IR),热重分析(TGA)和能量色散X射线光谱(EDAX)真正显示并确认了侧面存在铂(II)络合物SWCNT的墙。通过IC50值为13 µg / mL,功能化SWCNT对HeLa细胞的细胞毒性评估显示,其抗癌能力比顺铂高。

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