Enhancement in Anticancer Activity of Chitosan Tailored Imidazole-2-Thiosemicarbazones against MCF-7 Cancer Cell Line by Coordination with Copper(II) Ions

Hari Sharan Adhikari
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Abstract

The coordination behavior of new batch synthesized chitosan imidazole-2-thiosemicarbazones tailored from both the low molecular weight commercial chitosan and high molecular weight crab shell chitosan was confirmed by Fourier Transform Infrared (FT-IR) and magnetic susceptibility measurements. Chlorine content in the complexes was estimated by potentiometric titration technique. The study showed the tridentate NNS tridentate coordination with copper (II) ion in a square planar orientation with the remaining valence satisfied by coordination with chloride ion. The MTT assay studies showed an enhancement in the anticancer activity of these chitosan thiosemicarbazone ligands upon their coordination with copper (II) ions against the human breast cancer (MCF-7) cell line in vitro. The minimal cytotoxicity of both the ligands and complexes against the normal mouse embryonic fibroblast (NIH3T3) cells revealed the selective attraction of these biomaterial chitosan derivatives towards the cancer cells with non-toxicity to healthy cells. There was only a marginal effect of molecular weight (Mw) and degree of deacetylation (DDA) of chitosan upon the anticancer activity of these chitosan derivatives.
通过与铜(II)离子配位增强壳聚糖定制咪唑-2-硫代氨基甲酸盐对 MCF-7 癌细胞系的抗癌活性
通过傅立叶变换红外光谱(FT-IR)和磁感应强度测量,证实了由低分子量商用壳聚糖和高分子量蟹壳壳聚糖定制的新型批量合成壳聚糖咪唑-2-硫代氨基羰基化合物的配位行为。复合物中的氯含量是通过电位滴定技术估算的。研究结果表明,三叉NNS与铜(II)离子的配位呈方形平面,其余价态则通过与氯离子的配位来满足。MTT 试验研究表明,这些壳聚糖硫代氨基甲酸配体与铜(II)离子配位后,对体外人类乳腺癌(MCF-7)细胞系的抗癌活性增强。配体和复合物对正常小鼠胚胎成纤维细胞(NIH3T3)的细胞毒性极小,这表明这些生物材料壳聚糖衍生物对癌细胞具有选择性吸引力,而对健康细胞无毒性。壳聚糖的分子量(Mw)和脱乙酰化程度(DDA)对这些壳聚糖衍生物的抗癌活性影响甚微。
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