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一种新型生物活性纳米粒子,通过 3-氯丙基三甲氧基硅烷功能化 FeO 和 1-((3-(4-氯苯基)-1-苯基-1H-吡唑-4-基)亚甲基)-2-(4-苯基噻唑-2-基)腙的偶联合成:对胃 AGS 癌细胞的抗癌评估。

A novel bioactive nanoparticle synthesized by conjugation of 3-chloropropyl trimethoxy silane functionalized FeO and 1-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-2-(4-phenylthiazol-2-yl) hydrazine: assessment on anti-cancer against gastric AGS cancer cells.

机构信息

Department of Biology, Rasht Branch, Islamic Azad University, Rasht, Iran.

Department of Chemistry, Faculty of Sciences, University of Guilan, P.O. Box 41335-1914, Rasht, Iran.

出版信息

Mol Biol Rep. 2020 Mar;47(3):1637-1647. doi: 10.1007/s11033-020-05251-7. Epub 2020 Jan 13.

DOI:10.1007/s11033-020-05251-7
PMID:31933263
Abstract

Gastric cancer is one of the common types of cancer around the world which has few therapeutic options. Nitrogen heterocyclic derivatives such as thiazoles are used as the basis for the progression of the drugs. The objective of this study was to synthesize the 1-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl) methylene)-2-(4-phenylthiazol-2-yl) hydrazine (TP) conjugating with (3-Chloropropyl) trimethoxysilane (CPTMOS)-coated FeO nanoparticles (NPs) for anti-cancer activities against gastric AGS cancer cell line. The synthesized FeO@CPTMOS/TP NPs were characterized by FT-IR, XRD, EDX, SEM, TEM and Zeta potential analyses. To evaluate the toxicity of the above compound after AGS cell culture in RPMI medium, the cells were treated at different concentrations for 24 h. The viability of the cells was investigated by MTT assay. Moreover, apoptosis induced by FeO@CPTMOS/TP NPs was assessed by Hoechst 33432 staining, oxygen activity specification evaluation, caspase-3 activity assay, cell cycle analysis and annexin V/PI staining followed by flow cytometry analysis. The IC value in AGS cells was estimated to be 95.65 µg/ml. The flow cytometry results of FeO@CPTMOS/TP NPs revealed a large number of cells in the apoptotic regions compared to the control cells and the cells treated with TP. In addition, the amount of ROS production and caspase-3 activity increased in the treated cells with FeO@CPTMOS/TP NPs. The percentage of inhibited cancer cells in the G/G phase increased under the treatment in the binding state to the nonionic iron oxide nanoparticles. Overall, this study showed that FeO@CPTMOS/TP NP had effect on induction of apoptosis and inhibiting the growth of AGS cancer cells. Thus, FeO@CPTMOS/TP NP can be considered as a new anti-cancer candid for next phase of studies on mouse models.

摘要

胃癌是全球常见的癌症类型之一,治疗选择有限。氮杂环衍生物如噻唑被用作药物发展的基础。本研究的目的是合成 1-((3-(4-氯苯基)-1-苯基-1H-吡唑-4-基)亚甲基)-2-(4-苯基噻唑-2-基)腙 (TP),并将其与 (3-氯丙基)三甲氧基硅烷 (CPTMOS) 包覆的 FeO 纳米粒子 (NPs) 偶联,用于抗胃癌 AGS 细胞系的抗癌活性。合成的 FeO@CPTMOS/TP NPs 通过傅里叶变换红外光谱 (FT-IR)、X 射线衍射 (XRD)、能谱 (EDX)、扫描电子显微镜 (SEM)、透射电子显微镜 (TEM) 和 Zeta 电位分析进行了表征。为了评估在 RPMI 培养基中培养 AGS 细胞后上述化合物的毒性,将细胞在不同浓度下处理 24 小时。通过 MTT 测定法评估细胞活力。此外,通过 Hoechst 33432 染色、氧活性测定评价、caspase-3 活性测定、细胞周期分析和 Annexin V/PI 染色后进行流式细胞术分析,评估 FeO@CPTMOS/TP NPs 诱导的细胞凋亡。AGS 细胞的 IC 值估计为 95.65 µg/ml。FeO@CPTMOS/TP NPs 的流式细胞术结果显示,与对照细胞和用 TP 处理的细胞相比,凋亡区域的细胞数量较多。此外,FeO@CPTMOS/TP NPs 处理的细胞中 ROS 产生和 caspase-3 活性增加。在与非离子氧化铁纳米粒子结合的状态下,处理后 G/G 期抑制癌细胞的百分比增加。总的来说,这项研究表明,FeO@CPTMOS/TP NP 对诱导 AGS 癌细胞凋亡和抑制其生长有影响。因此,FeO@CPTMOS/TP NP 可以被认为是一种新的抗癌候选物,用于进一步在小鼠模型上进行研究。

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