Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors

Beniddir, M.A.A. and Le Borgne, E.A. and Iorga, B.L.A. and Loaëc, N.B.C. and Lozach, O.B. and Meijer, L.B.C. and Awang, K.D. and Litaudon, M.A. (2014) Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors. Journal of Natural Products, 77 (5). pp. 1117-1122. ISSN 15206025, DOI

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Two new acridone alkaloids, chlorospermines A and B (1 and 2), were isolated from the stem bark of Glycosmis chlorosperma, together with the known atalaphyllidine (3) and acrifoline (4), by means of bioguided isolation using an in vitro enzyme assay against DYRK1A. Acrifoline (4) and to a lesser extent chlorospermine B (2) and atalaphyllidine (3) showed significant inhibiting activity on DYRK1A with IC50's of 0.075, 5.7, and 2.2 μM, respectively. Their selectivity profile was evaluated against a panel of various kinases, and molecular docking calculations provided structural details for the interaction between these compounds and DYRK1A. © 2014 The American Chemical Society and American Society of Pharmacognosy.

Item Type: Article
Uncontrolled Keywords: acrifoline; atalaphyllidine; casein kinase I; chlorospermine a; chlorospermine b; cyclin dependent kinase; glycogen synthase kinase 3; plant extract; protein kinase inhibitor; unclassified drug
Subjects: Q Science > QD Chemistry
Divisions: Faculty of Engineering
Depositing User: Zanaria Saupi Udin
Date Deposited: 24 Jun 2014 07:20
Last Modified: 24 Jun 2014 07:22

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