Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, India.
Department of Chemistry, C. U. Shah University, Wadhwancity, India.
J Biomol Struct Dyn. 2021 Aug;39(12):4555-4562. doi: 10.1080/07391102.2020.1776641. Epub 2020 Jun 11.
The current cancer research focuses on the design and synthesis of chemical compounds that can modulate cell apoptosis or programmed cell death. So we synthesized and characterized ciprofloxacin based copper(II) complexes and studied their anticancer activity against HCT 116 cancer cells by MTT assay. We further investigated the influence of compound-2 (better IC value than cisplatin) on cancer cells to know the exact mechanism of anticancer activity. The distinct morphological change of cells due to compound-2 was observed in bright field microscopy. The trypan blue assay clearly demonstrated inhibition of cell viability. The clonogenic ability inhibition assay showed a low percentage of the plating efficiency of HCT 116 cells. The mechanism of cell death, either apoptotic or necrotic was distinguished by annexin V-FITC/PI (propidium iodide) staining assay and LDH (lactate dehydrogenase) release assay. The positive annexinV/PI cells in presence of compound-2 and absence of LDH in the LDH release assay confirmed the cell apoptotic mechanism of cell death. We also checked antibacterial activity of compounds against Gram and Gram bacteria in terms of MIC (minimum inhibitory concentration) and the data were in good agreement with the standard drug data. SOD mimic activity of synthesized Cu(II) complexes was also studied in terms of IC value. The brine shrimp lethality bioassay was also performed to evaluate the cytotoxic properties of the Cu(II) complexes.Communicated by Ramaswamy H. Sarma.
目前的癌症研究集中在设计和合成可以调节细胞凋亡或程序性细胞死亡的化学化合物。因此，我们合成并表征了基于环丙沙星的铜（II）配合物，并通过 MTT 测定法研究了它们对 HCT 116 癌细胞的抗癌活性。我们进一步研究了化合物 2（比顺铂具有更好的 IC 值）对癌细胞的影响，以了解抗癌活性的确切机制。在明场显微镜下观察到细胞由于化合物 2 而发生明显的形态变化。台盼蓝测定法清楚地表明细胞活力受到抑制。集落形成能力抑制测定法显示 HCT 116 细胞的种植效率百分比较低。通过 Annexin V-FITC/PI（碘化丙啶）染色测定法和 LDH（乳酸脱氢酶）释放测定法区分细胞死亡的机制，无论是凋亡还是坏死。在存在化合物 2 且不存在 LDH 释放测定法中的 LDH 的情况下，阳性 AnnexinV/PI 细胞证实了细胞凋亡的细胞死亡机制。我们还根据 MIC（最小抑菌浓度）检查了化合物对革兰氏阳性和革兰氏阴性细菌的抗菌活性，数据与标准药物数据非常吻合。还根据 IC 值研究了合成的 Cu（II）配合物的 SOD 模拟活性。还进行了盐水虾致死生物测定法以评估 Cu（II）配合物的细胞毒性。由 Ramaswamy H. Sarma 传达。
