Further in vitro evaluation of cytotoxicity of the marine natural product derivative 4'-leucine-avarone

Nat Prod Res. 2014;28(5):347-50. doi: 10.1080/14786419.2013.863201. Epub 2014 Jan 14.

Abstract

The cytotoxicity of 4'-leucine-avarone, amino derivative of the sponge Dysidea avara secondary metabolite avarone, was evaluated by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide assay in vitro against seven human solid tumours for the first time. The compound tested induced dose-dependent cytotoxic response in all cancer cells showing better activity towards the lung A-549 and colon HT-29 cell lines (IC50 7.40 μM and 9.62 μM, respectively) than towards the breast adenocarcinoma ER positive MCF-7 and ER negative MDA-MB-231 cells (IC50 11.64 μM and 17.31 μM, respectively), the prostate adenocarcinoma PC-3 and epiteloid cervix carcinoma HeLa cells (IC50 14.24 μM and 15.54 μM, respectively). No toxicity was found towards the foetal lung fibroblast MRC-5 cell line at the concentrations used. According to experimental data obtained, the sesquiterpenoid quinone structure of avarone may inspire development of new drug-like substances with improved cytotoxicity on lung cancer in humans.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Biological Products / chemistry
  • Biological Products / pharmacology*
  • Cyclohexenes / chemistry
  • Cyclohexenes / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Female
  • HT29 Cells
  • HeLa Cells
  • Humans
  • Inhibitory Concentration 50
  • Leucine / analogs & derivatives*
  • Leucine / chemistry
  • Leucine / pharmacology*
  • Lung Neoplasms / drug therapy
  • Male
  • Molecular Structure
  • Porifera / chemistry*
  • Quinones / chemistry
  • Quinones / pharmacology*
  • Sesquiterpenes / chemistry
  • Sesquiterpenes / pharmacology*

Substances

  • 4'-leucine-avarone
  • Antineoplastic Agents
  • Biological Products
  • Cyclohexenes
  • Quinones
  • Sesquiterpenes
  • avarone
  • Leucine