Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors
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 ext...
| Main Authors: | , , , , , , , |
|---|---|
| Format: | Article |
| Published: |
American Chemical Society
2014
|
| Subjects: |
| _version_ | 1825719900504588288 |
|---|---|
| author | Beniddir, M.A.A. Le Borgne, E.A. Iorga, B.L.A. Loaëc, N.B.C. Lozach, O.B. Meijer, L.B.C. Awang, K.D. Litaudon, M.A. |
| author_facet | Beniddir, M.A.A. Le Borgne, E.A. Iorga, B.L.A. Loaëc, N.B.C. Lozach, O.B. Meijer, L.B.C. Awang, K.D. Litaudon, M.A. |
| author_sort | Beniddir, M.A.A. |
| collection | UM |
| description | 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. |
| first_indexed | 2024-03-06T05:26:47Z |
| format | Article |
| id | um.eprints-10701 |
| institution | Universiti Malaya |
| last_indexed | 2024-03-06T05:26:47Z |
| publishDate | 2014 |
| publisher | American Chemical Society |
| record_format | dspace |
| spelling | um.eprints-107012014-06-24T07:22:05Z http://eprints.um.edu.my/10701/ Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors Beniddir, M.A.A. Le Borgne, E.A. Iorga, B.L.A. Loaëc, N.B.C. Lozach, O.B. Meijer, L.B.C. Awang, K.D. Litaudon, M.A. QD Chemistry 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. American Chemical Society 2014 Article PeerReviewed 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 https://doi.org/10.1021/np400856h <https://doi.org/10.1021/np400856h>. http://www.scopus.com/inward/record.url?eid=2-s2.0-84901664872&partnerID=40&md5=4dca11a45560165c4a7f967402c60421 10.1021/np400856h |
| spellingShingle | QD Chemistry Beniddir, M.A.A. Le Borgne, E.A. Iorga, B.L.A. Loaëc, N.B.C. Lozach, O.B. Meijer, L.B.C. Awang, K.D. Litaudon, M.A. Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors |
| title | Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors |
| title_full | Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors |
| title_fullStr | Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors |
| title_full_unstemmed | Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors |
| title_short | Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors |
| title_sort | acridone alkaloids from glycosmis chlorosperma as dyrk1a inhibitors |
| topic | QD Chemistry |
| work_keys_str_mv | AT beniddirmaa acridonealkaloidsfromglycosmischlorospermaasdyrk1ainhibitors AT leborgneea acridonealkaloidsfromglycosmischlorospermaasdyrk1ainhibitors AT iorgabla acridonealkaloidsfromglycosmischlorospermaasdyrk1ainhibitors AT loaacnbc acridonealkaloidsfromglycosmischlorospermaasdyrk1ainhibitors AT lozachob acridonealkaloidsfromglycosmischlorospermaasdyrk1ainhibitors AT meijerlbc acridonealkaloidsfromglycosmischlorospermaasdyrk1ainhibitors AT awangkd acridonealkaloidsfromglycosmischlorospermaasdyrk1ainhibitors AT litaudonma acridonealkaloidsfromglycosmischlorospermaasdyrk1ainhibitors |