Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol
Apstrakt
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 mu g and IC50 0.05 mM and 0.50 mu g 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 mu g/mL and 1.25 mu g/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.
Ključne reči:
sesquiterpenoid hydroquinone derivatives / Dysidea avara / antitumour activity / Acetylcholinesterase inhibitory activityIzvor:
Journal of Enzyme Inhibition and Medicinal Chemistry, 2016, 31, 4, 684-686Izdavač:
- Taylor & Francis Ltd, Abingdon
DOI: 10.3109/14756366.2015.1057724
ISSN: 1475-6366
PubMed: 26114310
WoS: 000379783200022
Scopus: 2-s2.0-84964612009
Institucija/grupa
Institut za multidisciplinarna istraživanjaTY - JOUR AU - Tommonaro, Giuseppina AU - Pejin, Boris AU - Iodice, Carmine AU - Tafuto, Antonietta AU - De Rosa, Salvatore PY - 2016 UR - http://rimsi.imsi.bg.ac.rs/handle/123456789/995 AB - 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 mu g and IC50 0.05 mM and 0.50 mu g 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 mu g/mL and 1.25 mu g/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. PB - Taylor & Francis Ltd, Abingdon T2 - Journal of Enzyme Inhibition and Medicinal Chemistry T1 - Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol EP - 686 IS - 4 SP - 684 VL - 31 DO - 10.3109/14756366.2015.1057724 ER -
@article{ author = "Tommonaro, Giuseppina and Pejin, Boris and Iodice, Carmine and Tafuto, Antonietta and De Rosa, Salvatore", year = "2016", 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 mu g and IC50 0.05 mM and 0.50 mu g 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 mu g/mL and 1.25 mu g/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.", publisher = "Taylor & Francis Ltd, Abingdon", journal = "Journal of Enzyme Inhibition and Medicinal Chemistry", title = "Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol", pages = "686-684", number = "4", volume = "31", doi = "10.3109/14756366.2015.1057724" }
Tommonaro, G., Pejin, B., Iodice, C., Tafuto, A.,& De Rosa, S.. (2016). Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol. in Journal of Enzyme Inhibition and Medicinal Chemistry Taylor & Francis Ltd, Abingdon., 31(4), 684-686. https://doi.org/10.3109/14756366.2015.1057724
Tommonaro G, Pejin B, Iodice C, Tafuto A, De Rosa S. Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol. in Journal of Enzyme Inhibition and Medicinal Chemistry. 2016;31(4):684-686. doi:10.3109/14756366.2015.1057724 .
Tommonaro, Giuseppina, Pejin, Boris, Iodice, Carmine, Tafuto, Antonietta, De Rosa, Salvatore, "Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol" in Journal of Enzyme Inhibition and Medicinal Chemistry, 31, no. 4 (2016):684-686, https://doi.org/10.3109/14756366.2015.1057724 . .