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01.12.2012 | Primary research | Ausgabe 1/2012 Open Access

Cancer Cell International 1/2012

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

Zeitschrift:
Cancer Cell International > Ausgabe 1/2012
Autoren:
Henry I C Lowe, Charah T Watson, Simone Badal, Ngeh J Toyang, Joseph Bryant
Wichtige Hinweise

Electronic supplementary material

The online version of this article (doi:10.​1186/​1475-2867-12-46) contains supplementary material, which is available to authorized users.

Competing interest

The authors declare no competing interest at this time.

Authors’ contribution

Conceived and designed the experiments: HL and JB, Acquisition of data: CW and NT, Analyzed and interpreted the data: NT and SB. Wrote the paper: SB and NT, Critical and intellectual revision of the article contents: SB and NT. All authors read and approved the final manuscript.

Abstract

Background

Given the high occurrence of prostate cancer worldwide and one of the major sources of the discovery of new lead molecules being medicinal plants, this research undertook to investigate the possible anti-cancer activity of two natural cycloartanes; cycloartane-3,24,25-diol (extracted in our lab from Tillandsia recurvata) and cycloartane-3,24,25-triol (purchased). The inhibition of MRCKα kinase has emerged as a potential solution to restoring the tight regulation of normal cellular growth, the loss of which leads to cancer cell formation.

Methods

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.

Results

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.

Conclusions

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.
Zusatzmaterial
Authors’ original file for figure 1
12935_2012_366_MOESM1_ESM.pdf
Authors’ original file for figure 2
12935_2012_366_MOESM2_ESM.tiff
Authors’ original file for figure 3
12935_2012_366_MOESM3_ESM.docx
Literatur
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