Biotechnology Centre, Silesian University of Technology, 44-100 Gliwice, Poland.
Department of Systems Biology and Engineering, Faculty of Automatic Control, Electronics and Computer Science, Silesian University of Technology, 44-100 Gliwice, Poland.
Molecules. 2022 Aug 17;27(16):5255. doi: 10.3390/molecules27165255.
The phenothiazine derivatives, tricyclic 10-3,6-diazaphenothiazine () and pentacyclic 7-(3'-dimethylaminopropyl)diquinothiazine (), have recently been shown to exhibit promising anticancer activities in vitro. In this report, we demonstrated that and could be pro-apoptotic agents in lung carcinoma, the human lung carcinoma A549 and non-small lung carcinoma H1299, in the range of IC = 1.52-12.89 µM, with a protective potential to healthy cell lines BEAS-2B and NHDF. The compounds showed higher activity in the range of the tested concentrations and low cytotoxicity in relation to normal healthy cells than doxorubicin, used as the reference drug. The cytostatic potential of and was demonstrated with the use of MTT assay. Cell cycle analysis via flow cytometry using Annexin-V assay showed the pro-apoptotic and pro-necrotic role of the studied diazaphenothiazines in the cell cycle. and initiated a biological response in the investigated cancer models with a different mechanism and at a different rate. Based on these findings, it can be concluded that and have potential as chemotherapeutic agents.
苯并噻嗪衍生物，三环 10-3,6-二氮杂苯并噻嗪 () 和五环 7-(3'-二甲基氨基丙基)二喹喔啉 ()，最近已被证明在体外具有有前景的抗癌活性。在本报告中，我们证明 和 可以作为肺癌（人肺癌 A549 和非小细胞肺癌 H1299）的促凋亡剂，IC = 1.52-12.89 μM 范围内，对健康细胞系 BEAS-2B 和 NHDF 具有保护潜力。与用作参考药物的阿霉素相比，在测试浓度范围内，这些化合物表现出更高的活性和低细胞毒性。用 MTT 测定法证明了 和 的细胞抑制潜力。通过使用 Annexin-V 测定法的流式细胞术进行细胞周期分析表明，所研究的二氮杂苯并噻嗪在细胞周期中具有促凋亡和促坏死作用。 和 以不同的机制和不同的速度在研究的癌症模型中引发了生物学反应。基于这些发现，可以得出结论， 和 具有作为化疗药物的潜力。
