Comparative Protein Kinase inhibitory activity of three Acacia species growing in Nigeria

Abstract

Significant improvements have been made in the field of drug discovery targets against cancer over the years, which have necessitated the search for novel chemical entities for the therapeutic treatment and management of cancer from natural sources.In this present work, we report herein the kinase inhibitory effect of the crude chloroform extract and the partitioned fractions of the hydroalcoholic stem bark extract of Acacia ataxacantha against a panel of disease related protein kinases and the comparison of the activity with that of Acacia nilotica and Acacia auriculiformis.The extract and the fractions of the stem bark of Acacia ataxacantha were subjected to Kinase enzymatic activities performed in 384-well plates using the ADP-Glo assay kit as recommended by the manufacturer (Promega, Madsion,WI). The result showed that the chloroform extract was inactive, while the ethyl acetate fraction gave the highest activity against haspin kinase with IC50 of 0.1 µg/ml, followed by aurora B kinase with IC50 of 0.45 µg/ml, while against CDK2, CDK5 and CDK9 kinases, the IC50 were 0.6, 0.88 and 0.9 µg/ml respectively. The n-butanol fraction gave an IC50 of 0.59 µg/ml and 0.7µg/ml against haspin and aurora B Kinases respectively. Comparison with Acacia nilotica and Acacia auriculiformis showed that the ethyl acetate fraction of acacia ataxacantha is the most active. The results revealed the potentials of the ethyl acetate fraction of Acacia ataxacantha as source of inhibitors against Haspin, aurora B and CDK kinases which might serve as lead for antimitotic agent against cancer.