用于细胞成像和细胞毒性研究的氮芥基荧光团的合成。

IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics
Yuanwei Liang, Maojun Liang, Cuiyu Li, Daini Wang, Xiaoxuan Gong, Kaiji Zheng
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引用次数: 0

摘要

氮芥是用于肿瘤治疗的重要烷基化抗癌药物。然而,关于将发光体整合到氮芥基化合物中用于成像和治疗应用的研究很少。在本研究中,我们报道了一系列新的含氮霉素的1-呋喃基-2-烯-1-酮和1-噻吩基-2-烯1-酮衍生物作为分子内电荷转移发光体,用于研究对癌症细胞的亚细胞定位和抗增殖成像。通过Knoevenagel缩合制备了目标产物,并用核磁共振和高分辨率质谱仪对其进行了表征。吸收和荧光研究分别用紫外-可见光和荧光分光光度计进行。在倒置显微镜下观察细胞形态。MTT法检测细胞毒性。用共聚焦激光扫描显微镜观察细胞定位。集落形成能力通过集落形成试验进行测定。transwell迁移实验检测细胞迁移能力。通过双尾Student t检验分析两组之间的差异。P<0.05(*)的差异被认为具有统计学意义。这些化合物以高产率合成。这些化合物的λmax和斯托克斯位移分别达到567和150nm。这些化合物对肺癌癌症细胞表现出良好的抗增殖活性,其中化合物3h表现出13.1±2.7μM的最佳IC50。此外,所选择的化合物3h优先位于溶酶体中,少量位于细胞核中,有效抑制细胞集落的形成和向A549细胞的迁移能力。这些发现表明,氮霉基荧光团可能是一种潜在的有效化疗剂在肺癌癌症治疗。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Synthesis of nitrogen mustard-based fluorophores for cell imaging and cytotoxicity studies.

Synthesis of nitrogen mustard-based fluorophores for cell imaging and cytotoxicity studies.

Synthesis of nitrogen mustard-based fluorophores for cell imaging and cytotoxicity studies.

Synthesis of nitrogen mustard-based fluorophores for cell imaging and cytotoxicity studies.

Nitrogen mustards are important alkylating anticancer drugs used for neoplasms treatment. However, little research about the integration of luminophore into nitrogen mustard-based compounds for both imaging and therapeutic application was reported. In this study, we report a series of novel nitrogen mustard-containing 1-furyl-2-en-1-one and 1-thienyl-2-en-1-one derivatives as intramolecular charge transfer-based luminophore for research in both imaging subcellular localization and antiproliferation toward lung cancer cells. The target products were prepared by Knoevenagel condensation and characterized by nuclear magnetic resonance and high-resolution mass spectrometer. The absorption and fluorescence studies were carried out by ultraviolet-visible and fluorescence spectrophotometers, respectively. Cell morphology was observed under an inverted microscope. Cytotoxicity test was detected by MTT assay. Cellular localization was observed by a confocal laser scanning microscope. Colony formation ability was carried out by colony formation assay. Cell migration ability was detected by transwell migration assay. Differences between the two groups were analyzed by two-tailed Student's t-test. The difference with P < 0.05 (*) was considered statistically significant. The compounds were synthesized in high yield. The λmax and Stokes shift of these compounds reach up to 567 and 150 nm, respectively. These compounds exhibited good antiproliferative activity against lung cancer cells, with compound 3h exhibiting the best IC50 of 13.1 ± 2.7 μM. Furthermore, the selected compound 3h is located preferentially in lysosomes and a small amount in nuclei, effectively inhibiting cell colony formation and migration abilities toward A549 cells. These findings suggested that nitrogen mustard-based fluorophores might be a potential effective chemotherapeutic agent in lung cancer therapy.

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来源期刊
CiteScore
2.00
自引率
7.10%
发文量
44
审稿时长
20 weeks
期刊介绍: Journal of Advanced Pharmaceutical Technology & Research (JAPTR) is an Official Publication of Society of Pharmaceutical Education & Research™. It is an international journal published Quarterly. Journal of Advanced Pharmaceutical Technology & Research (JAPTR) is available in online and print version. It is a peer reviewed journal aiming to communicate high quality original research work, reviews, short communications, case report, Ethics Forum, Education Forum and Letter to editor that contribute significantly to further the scientific knowledge related to the field of Pharmacy i.e. Pharmaceutics, Pharmacology, Pharmacognosy, Pharmaceutical Chemistry. Articles with timely interest and newer research concepts will be given more preference.
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