3,23-Dioxo-9,19-cyclolanost-24-en-26-oic acid
3,23-Dioxo-9,19-cyclolanost-24-en-26-oic acid inhibits the MRCKα kinase with Kd50 of 3.0 uM, it also inhibits the MRCKβ kinase with Kd50 of 3.2 uM; the role of Kinases in cancer onset and progression has made kinases a target for the control of some cancers, suggests that it may possess anticancer activity.
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Cycloartane anticancer activity[Reference:
WebLink]
New cancer diagnoses remain on the rise despite significant improvements in early detection and treatment. The role of Kinases in cancer onset and progression has made kinases a target for the control of some cancers. The MRCKα/β kinases have recently been implicated in cancer onset and progression and as such could serve as a potential drug target. The discovery that kinases are most effectively inhibited by small molecules has also resulted in an increased search for small molecule kinase inhibitors. Cycloartanes are small molecules found in many medicinal plants including the Jamaican Ball Moss (Tillandsia recurvata). Recent studies on T. recurvata have demonstrated that it possesses significant anticancer activity.Cycloartane-3,24,25-triol, an analog of a cycloartane identified in Ball moss was also shown to have inhibitory activity against MRCKα kinase.
METHODS AND RESULTS:
This study was as such set up to determine the MRCKα/β kinase inhibition activity of other cycloartanes in Ball Moss and their analogs. The kinase inhibitory activity of 6 cycloartanes was investigated using the ligand-kinase binding assay while the WST-1 reagent assay was used to determine the antiproliferative activity of the cycloartanes against some prostate and breast cancer cell lines.
Cycloart-23-ene-3,25-diol (1), Cycloartane-3,24,25-triol (2), Cycloart-25-ene-3,24-diol (3), 3,23-Dioxo-9,19-cyclolanost-24-en-26-oic acid (4), 24,25-Dihydroxycycloartan-3-one (5) inhibited the MRCKα kinase with Kd of 0.21 μM, 0.25μM, 0.36 μM, 3.0 μM, and 2.1 μM respectively. Hydroxycycloart-23-en-3-one,25, (6) showed no inhibition against the MRCKα kinase. Compounds 1, 3, 4, 5 inhibited the MRCKβ kinase with Kd of 4.7 μM, 1.10 μM, 3.2 μM, and 9.8 μM, respectively. Three of the six cycloartanes exhibited antiproliferation activity against two prostate and breast cancer cell lines each.
CONCLUSIONS:
In conclusion, cycloart-23-ene-3,25-diol (1) showed the most promising activity against the MRCKα/β kinase out of the 6 cycloartanes screened demonstrating an interesting structure activity relationship profile when compared with the other molecules. Cycloart-23-ene-3,25-diol (1) deserves further studies to determine its in vivo efficacy and safety.
