title: Biological activities of fusarochromanone: a potent anti-cancer agent.
abstract: BACKGROUND
  Fusarochromanone (FC101) is a small molecule fungal metabolite with a host of interesting biological functions, including very potent anti-angiogenic and direct anti-cancer activity.
  
  
  RESULTS
  Herein, we report that FC101 exhibits very potent in-vitro growth inhibitory effects (IC50 ranging from 10nM-2.5 μM) against HaCat (pre-malignant skin), P9-WT (malignant skin), MCF-7 (low malignant breast), MDA-231 (malignant breast), SV-HUC (premalignant bladder), UM-UC14 (malignant bladder), and PC3 (malignant prostate) in a time-course and dose-dependent manner, with the UM-UC14 cells being the most sensitive. FC101 induces apoptosis and an increase in proportion of cells in the sub-G1 phase in both HaCat and P9-WT cell lines as evidenced by cell cycle profile analysis. In a mouse xenograft SCC tumor model, FC101 was well tolerated, non-toxic, and achieved a 30% reduction in tumor size at a dose of 8 mg/kg/day. FC101 is also a potent anti-angiogenenic agent. At nanomolar doses, FC101 inhibits the vascular endothelial growth factor-A (VEGF-A)-mediated proliferation of endothelial cells.
  
  
  CONCLUSIONS
  Our data presented here indicates that FC101 is an excellent lead candidate for a small molecule anti-cancer agent that simultaneously affects angiogenesis signaling, cancer signal transduction, and apoptosis. Further understanding of the underlying FC101's molecular mechanism may lead to the design of novel targeted and selective therapeutics, both of which are pursued targets in cancer drug discovery.
authors.affiliation: Department of Chemistry and Physics, LSU-Shreveport, One University Place, Shreveport, LA 71115, USA. emahdavi@lsus.edu.
authors.forename: Elahe
authors.initials: E
authors.lastname: Mahdavian
authors.forename: Phillip
authors.initials: P
authors.lastname: Palyok
authors.forename: Steven
authors.initials: S
authors.lastname: Adelmund
authors.forename: Tara
authors.initials: T
authors.lastname: Williams-Hart
authors.forename: Brian D
authors.initials: BD
authors.lastname: Furmanski
authors.forename: Yoon-Jee
authors.initials: YJ
authors.lastname: Kim
authors.forename: Ying
authors.initials: Y
authors.lastname: Gu
authors.forename: Mansoureh
authors.initials: M
authors.lastname: Barzegar
authors.forename: Yang
authors.initials: Y
authors.lastname: Wu
authors.forename: Kaustubh N
authors.initials: KN
authors.lastname: Bhinge
authors.forename: Gopi K
authors.initials: GK
authors.lastname: Kolluru
authors.forename: Quincy
authors.initials: Q
authors.lastname: Quick
authors.forename: Yong-Yu
authors.initials: YY
authors.lastname: Liu
authors.forename: Christopher G
authors.initials: CG
authors.lastname: Kevil
authors.forename: Brian A
authors.initials: BA
authors.lastname: Salvatore
authors.forename: Shile
authors.initials: S
authors.lastname: Huang
authors.forename: John L
authors.initials: JL
authors.lastname: Clifford
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation; D002867:Chromones / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors / Q000502:physiology
chemical_list: D000970:Antineoplastic Agents; D002867:Chromones; D042461:Vascular Endothelial Growth Factor A; C054523:fusarochromanone