Isolation and syntheses of polymethoxyflavones and hydroxylated polymethoxyflavones as inhibitors of HL-60 cell lines

Bioorg Med Chem. 2007 May 15;15(10):3381-9. doi: 10.1016/j.bmc.2007.03.021. Epub 2007 Mar 13.

Abstract

Fifteen polymethoxyflavones (PMFs) and hydroxylated PMFs were isolated from sweet orange (Citrus sinensis) peel extract and synthesized to investigate their biological activity. All obtained compounds were tested in HL-60 cancer cell proliferation and apoptosis induction assays. While some PMFs and hydroxylated PMFs had moderate anti-carcinogenic activities, 5-hydroxy-6,7,8,3',4'-pentamethoxyflavone and 5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone showed strong inhibitory activities against the proliferation and induced apoptosis of HL-60 cell lines.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticarcinogenic Agents / chemical synthesis
  • Anticarcinogenic Agents / pharmacology
  • Antineoplastic Agents, Phytogenic / chemical synthesis*
  • Antineoplastic Agents, Phytogenic / isolation & purification
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Apoptosis / drug effects
  • Cell Proliferation / drug effects
  • Chromatography, High Pressure Liquid
  • Citrus / chemistry*
  • Flavones / isolation & purification
  • Flavones / physiology*
  • Fruit / chemistry
  • HL-60 Cells
  • Humans
  • Hydroxylation
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Plant Extracts / chemistry
  • Spectrometry, Mass, Electrospray Ionization
  • Spectrophotometry, Ultraviolet

Substances

  • Anticarcinogenic Agents
  • Antineoplastic Agents, Phytogenic
  • Flavones
  • Indicators and Reagents
  • Plant Extracts