Synthesis and structural characterization of novel 2-pyrazoline derivatives: Evaluation of their antiproliferative activity and fluorescence properties

IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY
Zefine Uğraş, F. Tok, E. Şalva, G. Ultav, Bedia Kaymakcıoğlu-Koçyiğit
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引用次数: 0

Abstract

In this study, a series of novel 2-pyrazoline derivatives were synthesized and their structures were established by using spectral methods. The antiproliferative activities of compounds were investigated against human cell lines A-549 and MCF-7 by MTT assay and L-929 (mouse normal fibroblast) cell cytotoxicity was also examined. Apoptotic effects of the compounds in breast and lung cancer cells were assessed by Annexin V-FITC apoptosis assay using flow cytometry. The antiproliferative effect on lung carcinoma of the synthesized compounds was higher than breast carcinoma. Moreover, it was observed that none of all synthesized compounds have cytotoxic activity in healthy cells. Flow cytometry studies have shown that compounds induced apoptosis at high concentration. Additionally, fluorescence cell imaging studies were performed for the first time in A-549 and MCF-7 cancer cell lines to determine the potential of the biosensor compounds by fluorescence microscopy. Compounds 4b, 4d, 4e and 4f showed fluorescence properties by considering microscopic imaging.
新型2-吡唑啉衍生物的合成和结构表征:抗增殖活性和荧光性能的评价
本研究合成了一系列新的2-吡唑啉衍生物,并用光谱方法建立了它们的结构。用MTT法研究了化合物对人细胞系A-549和MCF-7的抗增殖活性,并检测了L-929(小鼠正常成纤维细胞)的细胞毒性。通过使用流式细胞术的Annexin V-FITC凋亡测定来评估化合物在乳腺癌和肺癌癌症细胞中的凋亡作用。所合成的化合物对肺癌的抗增殖作用高于乳腺癌。此外,观察到所有合成的化合物中没有一种在健康细胞中具有细胞毒性活性。流式细胞术研究表明,化合物在高浓度下诱导细胞凋亡。此外,首次在A-549和MCF-7癌症细胞系中进行荧光细胞成像研究,以通过荧光显微镜确定生物传感器化合物的潜力。通过考虑微观成像,化合物4b、4d、4e和4f显示出荧光性质。
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来源期刊
CiteScore
0.80
自引率
0.00%
发文量
74
审稿时长
6-12 weeks
期刊介绍: The international journal of the Polish Pharmaceutical Society is published in 6 issues a year. The journal offers Open Access publication of original research papers, short communications and reviews written in English, in all areas of pharmaceutical sciences. The following areas of pharmaceutical sciences are covered: Analysis, Biopharmacy, Drug Biochemistry, Drug Synthesis, Natural Drugs, Pharmaceutical Technology, Pharmacology and General. A bimonthly appearing in English since 1994, which continues “Acta Poloniae Pharmaceutica”, whose first issue appeared in December 1937. The war halted the activity of the journal’s creators. Issuance of “Acta Poloniae Pharmaceutica” was resumed in 1947. From 1947 the journal appeared irregularly, initially as a quarterly, then a bimonthly. In the years 1963 – 1973 alongside the Polish version appeared the English edition of the journal. Starting from 1974 only works in English are published in the journal. Since 1995 the journal has been appearing very regularly in two-month intervals (six books a year). The journal publishes original works from all fields of pharmacy, summaries of postdoctoral dissertations and laboratory notes.
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