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Functionalisation of Fe3O4 nanoparticles by 2-((pyrazol-4-yl) methylene) hydrazinecarbothioamide enhances the apoptosis of human breast cancer MCF-7 cells.
IET Nanobiotechnology ( IF 2.3 ) Pub Date : 2020-08-06 , DOI: 10.1049/iet-nbt.2019.0199
Mohammad Reza Izadpanah 1 , Ali Salehzadeh 1 , Mohammad Zaefizadeh 2 , Mohammad Nikpasand 3
Affiliation  

Cancer is a major cause of death. Thus, the incidence and mortality rate of cancer is globally important. Regarding vast problems caused by chemotherapy drugs, efforts have progressed to find new anti-cancer drugs. Pyrazole derivatives are known as components with anti-cancer properties. In here, Fe 3 O 4 nanoparticles were first functionalized with (3-chloropropyl) trimethoxysilane, then 2-((pyrazol-4-yl) methylene) hydrazinecarbothioamide (P) was anchored on the surface of magnetic nanoparticles (PL). The synthesized nano-compounds were characterized using Fourier transform infrared spectroscopy, X-ray diffraction, scanning electron microscopy, Zeta potential, dynamic light scattering, and energy-dispersive x-ray spectrometry analyses. The cytotoxicity effect was evaluated using MTT assay, apoptosis test by Flow cytometry, cell cycle analysis, Caspase-3 activity assay and Hoechst staining on MCF-7 cell line. The high toxicity for tumor cells and low toxicity on normal cells (MCF10A) was considered as an important feature (selectivity index, 10.9). Based on results, the IC50 for P and PL compounds were 157.80 and 131.84 μM/ml respectively. Moreover, apoptosis inducing, nuclear fragmentation, Caspase 3 activity and induction of cell rest in sub-G1 and S phases, were also observed. The inhibitory effect of PL was significantly higher than P, which could be due to the high penetrability of Fe 3 O 4 nanoparticles.

中文翻译:

2-((pyrazol-4-yl) methylene) hydrazinecarbothioamide 对 Fe3O4 纳米颗粒的功能化可增强人乳腺癌 MCF-7 细胞的凋亡。

癌症是导致死亡的主要原因。因此,癌症的发病率和死亡率具有全球重要性。对于化疗药物引起的巨大问题,人们一直在努力寻找新的抗癌药物。吡唑衍生物被称为具有抗癌特性的成分。在这里,Fe 3 O 4纳米粒子首先用(3-氯丙基)三甲氧基硅烷官能化,然后将 2-((吡唑-4-基)亚甲基)肼硫代酰胺(P)锚定在磁性纳米粒子(PL)的表面上。使用傅里叶变换红外光谱、X 射线衍射、扫描电子显微镜、Zeta 电位、动态光散射和能量色散 X 射线光谱分析对合成的纳米化合物进行了表征。采用MTT法、流式细胞术凋亡试验、细胞周期分析、Caspase-3活性测定和对MCF-7细胞系的Hoechst染色评价细胞毒性作用。对肿瘤细胞的高毒性和对正常细胞的低毒性(MCF10A)被认为是一个重要特征(选择性指数,10.9)。根据结果​​,P 和 PL 化合物的 IC50 分别为 157.80 和 131.84 μM/ml。此外,还观察到细胞凋亡诱导、核碎裂、半胱天冬酶 3 活性和诱导亚 G1 和 S 期细胞静止。PL的抑制作用显着高于P,这可能是由于Fe的高渗透性 3 O 4纳米粒子。
更新日期:2020-08-20
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