title: Chemical Composition of Roots Flemingia philippinensis and Their Inhibitory Kinetics on Aromatase.
abstract: Aromatase is the key enzyme responsible for catalyzing the conversion of C19steroids to estrogens. Its inhibitors are widely used in breast cancer therapy. The CH2Cl2partition 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 IC50values ranged between 2.98 and 58.08 μm. In kinetic studies, all tested compounds behaved as reversible competitive inhibitors and their Kivalues were calculated by Dixon plots. The most potent inhibitor (6,8-diprenylorobol) had a Kivalue 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.
authors: Pharmaceutical Department, Nanjing Children's Hospital Affiliated to Nanjing Medical University, Nanjing, 210008, P. R. China.
authors: Fang
authors: F
authors: Sun
authors: Institute of Materia Medica, Zhejiang Academy of Medical Sciences, Hangzhou, 310013, P. R. China.
authors: Qin
authors: Q
authors: Li
authors: Pharmaceutical Department, Nanjing Children's Hospital Affiliated to Nanjing Medical University, Nanjing, 210008, P. R. China.
authors: Jin
authors: J
authors: Xu
mesh_terms: D001141:Aromatase / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D007887:Fabaceae / Q000737:chemistry*; D006801:Humans; D007529:Isoflavones / Q000737:chemistry / Q000494:pharmacology; D007700:Kinetics; D010936:Plant Extracts / Q000032:analysis; D018517:Plant Roots / Q000737:chemistry
chemical_list: D004791:Enzyme Inhibitors; D007529:Isoflavones; D010936:Plant Extracts; D001141:Aromatase
keywords: 6,8-Diprenylorobol; Aromatase; Flemingia philippinensis; Prenylated isoflavones; UPLC/TOF-MS