Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells |
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| Affiliation: | 1. Department of Medical Biology, Faculty of Health Sciences, UiT-The Arctic University of Norway, 9037 Tromsø, Norway;2. School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, PO Box 1068, N-0316 Oslo, Norway;1. Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China;2. School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China;3. School of Life Science & Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China;4. Department of Pharmacy, Hainan Medical College, Haikou 571101, PR China;5. Mount Sinai School of Medicine, New York, NY 10029, USA |
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| Abstract: | Thujaplicins are tropolone-derived natural products with antiproliferative properties. We recently reported that certain tropolones potently and selectively target histone deacetylases (HDAC) and inhibit the growth of hematological cell lines. Here, we investigated the mechanisms by which these compounds exert their antiproliferative activity in comparison with the pan-selective HDAC inhibitor, vorinostat, using Jurkat T-cell leukemia cells. The tropolones appear to work through a mechanism distinct from vorinostat. These studies suggest that tropolone derivatives may serve as selective epigenetic modulators of hematological cells with potential applications as anti-leukemic or anti-inflammatory agents. |
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| Keywords: | HDAC inhibitor Tropolone Natural product Vorinostat Leukemia |
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