irigenin and tectorigenin

Tectorigenin and irigenin are biologically active isoflavones of

Topics: Glucuronides; Glucuronosyltransferase; Humans; Isoflavones; Kinetics; Microsomes, Liver; UDP-Glucuronosyltransferase 1A9

A sensitive and reliable ultra-high-performance liquid chromatography-electrospray ionization-tandem mass spectrometry (UHPLC-ESI-MS/MS) has been developed and validated for the simultaneous determination of three active components, i.e., tectorigenin, irigenin and irisflorentin, in rat plasma and urine after oral administration of Rhizoma Belamcandae extract. Chromatographic separation was achieved on a Zorbax SB-C(18) column (50 mm × 2.1 mm, 1.8 μm; Agilent, USA) with gradient elution using a mobile phase that consisted of acetonitrile - 0.1% formic acid in water at a flow rate of 0.4 mL/min. Detection was performed by a triple-quadrupole tandem mass spectrometer in multiple reaction monitoring (MRM) mode via polarity switching between the negative (for tectorigenin and irigenin) and positive (for irisflorentin) ionization modes. The calibration curve was linear over a range of 50-50,000 ng/mL for tectorigenin, 10-5000 ng/mL for irigenin and 0.1-200 ng/mL for irisflorentin, respectively. The intra- and inter-day precisions (RSD %) were within 11.3% for all analytes, whereas the deviation of assay accuracies ranged from -8.7 to +11.1%. All analytes were proven to be stable during all sample storage and analysis procedures. This method was successfully applied to a pharmacokinetic study of the three isoflavones after oral administration of Rhizoma Belamcandae extract to rats.

Topics: Animals; Chromatography, High Pressure Liquid; Drug Stability; Drugs, Chinese Herbal; Iris; Isoflavones; Limit of Detection; Male; Rats; Rats, Sprague-Dawley; Reproducibility of Results; Tandem Mass Spectrometry

Phytoestrogens are nonsteroidal plant derived compounds with estrogenic activity that have been implicated in protecting against prostate cancer progression. We hypothesized that these compounds would alter cell number and increase the ability of antiandrogens to induce cell death in prostate cancer cells.. RWPE-1, LNCaP and PC-3 cells were treated with or without an extract of Belamcanda chinensis, 2 purified phytoestrogens derived from this extract (irigenin and tectorigenin) and the antiandrogen bicalutamide. We assessed the effect on cell number, proliferation and apoptosis.. Phytoestrogens (50 to 100 microM) and bicalutamide (10 to 50 microM) alone decreased the cell number in all 3 cell lines. Phytoestrogens (50 microM) combined with bicalutamide (10 microM) further decreased the number of RWPE-1 and PC-3 cells compared to these agents alone. Tectorigenin and irigenin inhibited the proliferation of RWPE-1, LNCaP and PC-3 cells, causing G1 arrest and the induction of p21WAF1 or p27 protein expression, whereas bicalutamide induced apoptosis in a dose dependent manner in all 3 cell lines. Phytoestrogens did not have antiandrogenic activity.. These in vitro studies demonstrate a role for tectorigenin and irigenin in regulating prostate cancer cell number by inhibiting proliferation through cell cycle regulation.

Topics: Cell Division; Cell Line, Tumor; Drug Evaluation, Preclinical; Humans; Iridaceae; Isoflavones; Male; Phytoestrogens; Plant Extracts; Prostatic Neoplasms; Tumor Cells, Cultured