Abstract

Aromatase is the key enzyme responsible for catalyzing the conversion of C19 steroids to estrogens. Its inhibitors are widely used in breast cancer therapy. The CH2 Cl2 partition of a crude ethanolic extract from the roots of Flemingia philippinensis showed potent inhibitory activity of aromatase. The constituents of the extract were analyzed and identified by liquid chromatography tandem mass spectrometry. Five purified prenylated isoflavones were evaluated for aromatase inhibition and their IC50 values ranged between 2.98 and 58.08 μm. In kinetic studies, all tested compounds behaved as reversible competitive inhibitors and their Ki values were calculated by Dixon plots. The most potent inhibitor (6,8-diprenylorobol) had a Ki value of 1.42 μm. Furthermore, using UPLC and LC/MS, 6,8-diprenylorobol was proven to be present in the native roots in high quantities.

Full Text
Paper version not known

Talk to us

Join us for a 30 min session where you can share your feedback and ask us any queries you have

Schedule a call

Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.