RETRACTED ARTICLE: Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol |
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| Authors: | Giuseppina Tommonaro Boris Pejin Carmine Iodice Antonietta Tafuto Salvatore De Rosa |
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| Institution: | 1. National Research Council of Italy, Institute of Biomolecular Chemistry, CNR-ICB, Pozzuoli-Naples, Italy and giuseppina.tommonaro@icb.cnr.it gtommonaro@icb.cnr.it;3. National Research Council of Italy, Institute of Biomolecular Chemistry, CNR-ICB, Pozzuoli-Naples, Italy and;4. Department of Life Sciences, Institute for Multidisciplinary Research – IMSI, University of Belgrade, Belgrade, Serbia;5. National Research Council of Italy, Institute of Biomolecular Chemistry, CNR-ICB, Pozzuoli-Naples, Italy and |
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| Abstract: | The acetylcholinesterase inhibitory and/or antitumour activities of amino-, thio- and ester-derivatives of avarol selected were evaluated for the first time at in vitro conditions. Avarol-3′,4′-dithioglycol (1) and avarol-4′-(3)mercaptopropionic acid (3) were shown to be the best inhibitors of the enzyme tested (0.50?µg and IC50 0.05?mM and 0.50?µg and IC50 0.12?mM, respectively), while 4′-tryptamine-avarone (9) and avarol-3′-(3)mercaptopropionic acid (2) exhibited the highest cytotoxicity against the human breast T-47D cancer cell line (IC50 0.66?µg/mL and 1.25?µg/mL, respectively). According to experimental data obtained, the sesquiterpenoid hydroquinone structure of bioactive avarol derivatives may inspire development of new pharmacologically useful substances to be used in the treatment of Alzheimer's disease and/or human breast tumour. |
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| Keywords: | Acetylcholinesterase inhibitory activity antitumour activity Dysidea avara sesquiterpenoid hydroquinone derivatives |
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