Cycloartane-3,24,25-triol inhibits MRCKα kinase and demonstrates promising anti prostate cancer activity in vitro

Kinase inhibition was investigated using competition binding (to the ATP sites) assays which have been previously established and authenticated and cell proliferation was measured using the WST-1 assay.Cycloartane-3,24,25-triol demonstrated strong selectivity towards the MRCKα kinase with a Kd50 of 0.26 μM from a total of 451 kinases investigated. Cycloartane-3,24,25-triol reduced the viability of PC-3 and DU145 cell lines with IC50 values of 2.226？±？0.28 μM and 1.67？±？0.18 μM respectively.These results will prove useful in drug discovery as Cycloartane-3,24,25-triol has shown potential for development as an anti-cancer agent against prostate cancer.Prostate cancer is the second most frequently diagnosed cancer and sixth leading cause of cancer death in males, worldwide [1]. The search for new molecules to combat the rising cases of prostate cancer especially those resistant to current chemotherapy calls for urgent action. Medicinal plants have been one of the major sources for the discovery of a number of current clinically used anticancer drugs.Previous research conducted in our lab demonstrated the promising anti-cancer properties of Tillandsia recurvata L. (Bromeliaceae) commonly called the Jamaican Ball Moss or the Old Man’s beard [2]. In an attempt to identify the critical isolate from this plant that is responsible for the observed said bioactivity, this research uncovered the cycloartane, cycloart-23-ene-3,25-diol (Figure 1) [3]. Further literature research led us to a closely related cycloartane, cycloartane-3,24,25-triol (Figure 1), which had previously been extracted from the Chrysanthemum morifolium plant and was shown to possess promising chemopreventive properties [4].Essential biological functions such as the provision of a structural frame work and the driving force for cellular motility and division are mediated by the actin cytoskeleton in all eukaryotic cells. A comprehensive overview of the biological processes that regulate the organization of a