Prabhat Anjali M, Kuppusamy M Lakshmi, Bognár Balázs, Kálai Tamás, Hideg Kálmán, Kuppusamy Periannan
Department of Radiology and Medicine, Norris Cotton Cancer Center, Geisel School of Medicine, Dartmouth College, 1 Medical Center Drive, 601 Rubin Building, Lebanon, NH, 03756, USA.
Institute of Organic and Medicinal Chemistry, Medical School, University of Pécs, Pécs, Hungary.
Cell Biochem Biophys. 2019 Mar;77(1):61-67. doi: 10.1007/s12013-018-0862-5. Epub 2018 Dec 14.
The synthesis and antiproliferative effect of a novel curcumin analog, 4,4'-disulfonyldiarylidenyl piperidone, are reported. The design of the molecule is based on the fusion of an antiproliferative segment, namely diarylidenyl piperidone (DAP), with N-hyroxypyrroline, which is known to metabolically convert to nitroxide and protect healthy cells. Cellular uptake, metabolic conversion, cytotoxicity and antiproliferative effect of the DAP derivative against HCT-116 human colon cancer cells have been determined. Based on cell viability and proliferation assays as well as western-blot analysis of major transcription factors and inhibitory proteins, it is determined that the DAP compound is cytotoxic by inhibiting cell survival and proliferation pathways. The findings may have important implications in the design and development of effective anticancer agents.
报道了一种新型姜黄素类似物4,4'-二磺酰基二芳叉基哌啶酮的合成及其抗增殖作用。该分子的设计基于抗增殖片段二芳叉基哌啶酮（DAP）与N-羟基吡咯啉的融合，已知N-羟基吡咯啉可代谢转化为氮氧化物并保护健康细胞。已测定了DAP衍生物对HCT-116人结肠癌细胞的细胞摄取、代谢转化、细胞毒性和抗增殖作用。基于细胞活力和增殖测定以及主要转录因子和抑制蛋白的蛋白质印迹分析，确定DAP化合物通过抑制细胞存活和增殖途径具有细胞毒性。这些发现可能对有效抗癌药物的设计和开发具有重要意义。
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