In Vitro Characterization of Derrone as an Aurora Kinase Inhibitor

Cited 4 time in webofscience Cited 0 time in scopus
  • Hit : 225
  • Download : 0
Among mitotic kinases, Aurora kinases are the most widely studied, since their expression is restricted to mitosis. They play a key role in chromosome segregation and cell polyploidy. Aurora kinases are important therapeutic targets, and several research groups have directed their efforts toward the identification of kinase inhibitors. The aim of this study is to screen and characterize Aurora kinase inhibitors from natural substances extracted from plants that are used in the Vietnamese pharmacopoeia. We have characterized in vitro Derrone, extracted from Erythrina orientalis L. MURR, as a novel Aurora kinase inhibitor. This compound exhibited an ability to inhibit the phosphorylation of histone H3 at ser10 both in kinase assay and at the cellular level. The compound was more effective against Aurora kinase B, with a lower IC50 value as compared to Aurora A. Moreover, it impaired the mitotic spindle checkpoint and led to endoreduplication in cancer cells, a phenomenon caused by an Aurora B inhibitor. Interestingly, using the xCelligence system and real-time cell analysis (RTCA) software, we set up a comparison of cell proliferation profiles between cancer cells treated with Derrone and VX680-a well-known Aurora kinase inhibitor-and we found that these profiles exhibited considerable similarity in cell morphology, growth, and death. Additionally, Derrone significantly inhibited the formation and growth of MCF7 tumor spheroids
Publisher
PHARMACEUTICAL SOC JAPAN
Issue Date
2016-06
Language
English
Article Type
Article
Keywords

CHROMOSOMAL PASSENGER COMPLEX; CANCER CELL-LINES; HISTONE H3; XCELLIGENCE SYSTEM; B KINASE; PHOSPHORYLATION; GROWTH; TIME; OVEREXPRESSION; TUMORIGENESIS

Citation

BIOLOGICAL & PHARMACEUTICAL BULLETIN, v.39, no.6, pp.935 - 945

ISSN
0918-6158
URI
http://hdl.handle.net/10203/210017
Appears in Collection
Files in This Item
There are no files associated with this item.
This item is cited by other documents in WoS
⊙ Detail Information in WoSⓡ Click to see webofscience_button
⊙ Cited 4 items in WoS Click to see citing articles in records_button

qr_code

  • mendeley

    citeulike


rss_1.0 rss_2.0 atom_1.0