Erythroidine Alkaloids: A Novel Class of Phytoestrogens

摘要: Erythrina poeppigiana is a medicinal plant which widely used in Asia, Latin America, and Africa traditional remedies for gynecological complications maladies. In continuation of studies the discovery novel phytoestrogens, four erythroidine alkaloids, namely α-erythroidine, β-erythroidine, their oxo-derivatives 8-oxo-α-erythroidine 8-oxo-β-erythroidine, were isolated structurally characterized from methanolic extract stem bark E. poeppigiana. Due to high amounts erythroidines in considering widespread utilization preparations medicine, exploration estrogenic properties was performed. The estrogenicity assayed various estrogen receptor-(ER)-dependent test systems, including receptor binding affinity, cell culture based ER-dependent reporter gene assays, expression cultured cells using reverse transcription polymerase chain reaction techniques. α-Erythroidine β-erythroidine showed affinity values ERα 0.015 ± 0.010 % 0.005 ± 0.010 %, respectively, whereas only bound ERβ (0.006 ± 0.010 %). both exhibited significant dose-dependent stimulation activity osteosarcoma detectable already at 10 nM. Results confirmed MVLN cells, bioluminescent variant MCF-7 breast cancer cells. Further, α-erythroidine induced enhanced specific ERα-dependent genes trefoil factor-1 serum/glucocorticoid regulated kinase 3 confirming estrogenicity. Additionally, molecular docking simulations, potential mode on ERα, proposed, supporting experimental evidences. This first time that an profile reported potentially new class phytoestrogens.