Synthesis,structural characterization and biological activity of novel Knoevenagel condensates on DLD-1 human colon carcinoma |
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| Authors: | Lucia Rišiaňová Eva Fischer-Fodor Jindra Valentová Corina Tatomir Nicoleta Corina Decea Piroska Virag Iveta Pechová Ferdinand Devínsky Natalia Miklášová |
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| Institution: | 1. Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University in Bratislava, Kalini?iakova 8, Bratislava 83232, Slovakia;2. Institute of Oncology “I. Chiricuta”, Cluj-Napoca 400015, Romania;3. Medfuture Research Center, University of Medicine and Pharmacy “Iuliu Hatieganu” Cluj Napoca, 400012 Cluj-Napoca, Romania;4. Department of Physiology, University of Medicine and Pharmacy “Iuliu Hatieganu” Cluj Napoca, 400012 Cluj-Napoca, Romania |
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| Abstract: | Biologically active Knoevenagel condensates (1–14) of diarylheptanoids: 1,7-bis(3-methoxy-4-hydroxyphenyl)hepta-1,7-diene-3,5-dione and 1,7-bis(3-ethoxy-4-hydroxyphenyl)hepta-1,7-diene-3,5-dione, were synthesized and structurally characterized. Compounds 1–14 exhibited cytotoxicity against colon carcinoma cells, and their antiproliferative effect was associated with a significant decrease of multidrug resistance proteins. One of the underlying mechanisms of these effects is the reduction of intracellular and extracellular SOD enzymes by compounds 1, 12 and 14, which render the tumor cells more vulnerable to oxidative stress. |
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| Keywords: | ABTS 2 2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) DPPH di(phenyl)-(2 4 6-trinitrophenyl)iminoazanium MDR1 multidrug resistance gene 1 MRP1 multidrug resistance-associated protein 1 PBS Phosphate-buffered saline SOD superoxide dismutase GSH glutathione GSSG glutathione disulfide Knoevenagel condensates Curcuminoids Antioxidant activity Cytotoxicity SOD-mimetic activity Multidrug resistance |
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