AI Article Synopsis
- Aromatase is the enzyme that converts steroids into estrogens, and its inhibitors are important in treating breast cancer.
- A crude extract from Flemingia philippinensis roots showed strong aromatase inhibition, with five purified isoflavones tested, displaying varying potency.
- The most effective inhibitor, 6,8-diprenylorobol, exhibited a low IC value and was found in high amounts in the plant's roots, suggesting potential for further application in therapy.
Article Abstract
Aromatase is the key enzyme responsible for catalyzing the conversion of C steroids to estrogens. Its inhibitors are widely used in breast cancer therapy. The CH Cl 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 IC values ranged between 2.98 and 58.08 μm. In kinetic studies, all tested compounds behaved as reversible competitive inhibitors and their K values were calculated by Dixon plots. The most potent inhibitor (6,8-diprenylorobol) had a K 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.
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| http://dx.doi.org/10.1002/cbdv.201600193 | DOI Listing |
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