title: Erythrina excelsa exhibits estrogenic effects in vivo and in vitro and is cytotoxic on breast and colon cancer cell lines.
abstract: BACKGROUND
  Eythrina excelsa Baker (Fabaceae) is a medicinal plant used to treat various ailments including those of the female genital tract.
  
  
  OBJECTIVE
  The objective of this study is to investigate the estrogenic and cytotoxic effects of the ethanol extract of the stem bark of E. excelsa.
  
  
  METHODS
  Erythrina excelsa was evaluated in vitro using the yeast estrogen screen (YES). The extract was then tested in a 3-day uterotrophic assay on ovariectomised Wistar rats at doses of 50 and 100 mg/kg BW/d. Cytotoxic effects were assessed on breast (MCF-7) and colon (HT-29) cancer cell lines using the MTT cell viability assay. Additionally, a LC-PDA-ESI (+)-HRMS and HRMS/MS method was developed and applied for the identification of representative secondary metabolites scaffolds in the extract.
  
  
  RESULTS
  In the YES, the extract stimulated the transactivation of the estrogen receptor in a dose-dependent manner with an EC50 value of 1.8 μg/mL. In rats, E. excelsa increased uterine wet weight, uterine epithelial height, and the mRNA expression of estrogen-responsive genes in the uterus and liver at 50 whereas at 100 mg/kg BW/d anti-estrogenic effects were observed. In the MTT-assay, a dose-dependent decrease of the viability of both cell lines was observed with EC50 values of 13.6 μg/mL (MCF-7) and 27.7 μg/mL (HT-29). The phytochemical analysis revealed that the extract is rich in isoflavonoids, mainly prenylated and pyran-derivatives thereof.
  
  
  CONCLUSIONS
  Erythrina excelsa is rich in prenylated and pyran-substituted isoflavonoids, exhibits estrogenic/anti-estrogenic and cytotoxic effects and warrant sufficient interest for deeper investigations.
authors.affiliation: a Department of Molecular and Cellular Sports Medicine , German Sport University , Cologne, Germany ;
authors.forename: Sadrine
authors.initials: S
authors.lastname: Tchoukouegno Ngueu
authors.affiliation: b Department of Pharmacognosy and Natural Products Chemistry, School of Pharmacy , University of Athens , Greece ;|c Laboratory of Animal Physiology, Department of Animal Biology and Physiology , University of Yaoundé I , Cameroon.
authors.forename: Job
authors.initials: J
authors.lastname: Tchoumtchoua
authors.affiliation: c Laboratory of Animal Physiology, Department of Animal Biology and Physiology , University of Yaoundé I , Cameroon.
authors.forename: Dieudonné
authors.initials: D
authors.lastname: Njamen
authors.affiliation: b Department of Pharmacognosy and Natural Products Chemistry, School of Pharmacy , University of Athens , Greece ;
authors.forename: Maria
authors.initials: M
authors.lastname: Halabalaki
authors.affiliation: a Department of Molecular and Cellular Sports Medicine , German Sport University , Cologne, Germany ;
authors.forename: Ute
authors.initials: U
authors.lastname: Laudenbach-Leschowski
authors.affiliation: a Department of Molecular and Cellular Sports Medicine , German Sport University , Cologne, Germany ;
authors.forename: Patrick
authors.initials: P
authors.lastname: Diel
mesh_terms: D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D003110:Colonic Neoplasms / Q000188:drug therapy / Q000378:metabolism; D003603:Cytotoxins / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004895:Erythrina; D004967:Estrogens / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D019073:HT29 Cells; D006801:Humans; D061986:MCF-7 Cells; D051381:Rats; D017208:Rats, Wistar
chemical_list: D003603:Cytotoxins; D004967:Estrogens
keywords: Fabaceae; LC–HRMS; MTT assay; Orbitrap; prenylated isoflavonoids; uterotrophic assay; yeast estrogen screen