Synthesis and characterization of novel PUFA esters exhibiting potential anticancer activities: an in vitro study

Eur J Med Chem. 2011 Oct;46(10):4878-86. doi: 10.1016/j.ejmech.2011.07.044. Epub 2011 Aug 3.

Abstract

Polyunsaturated fatty acids (PUFAs) have been reported to play a regulatory role in tumour growth progression. In the present study, we have synthesized ester derivatives of two important PUFA viz., linoleic acid (LA) and arachidonic acid (AA) with propofol, a widely used general anaesthetic-sedative agent. The novel propofol ester analogues have been found to inhibit various cancer cell lines in a dose-dependent manner. Moreover, the compounds have been found to induce apoptotic cell death by enhancing the release of cytochrome c and expression of caspase-3. The data of the present study suggest that novel propofol-PUFA esters have strong potential to emerge as effective anticancer agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Arachidonic Acid / chemical synthesis
  • Arachidonic Acid / chemistry
  • Arachidonic Acid / pharmacology
  • Caspase 3 / metabolism
  • Cell Line, Tumor
  • Esters / chemical synthesis
  • Esters / chemistry
  • Esters / pharmacology
  • Fatty Acids, Unsaturated / chemical synthesis
  • Fatty Acids, Unsaturated / chemistry*
  • Fatty Acids, Unsaturated / pharmacology*
  • Humans
  • Hypnotics and Sedatives / chemical synthesis
  • Hypnotics and Sedatives / chemistry
  • Hypnotics and Sedatives / pharmacology
  • Linoleic Acid / chemical synthesis
  • Linoleic Acid / chemistry
  • Linoleic Acid / pharmacology
  • Neoplasms / drug therapy
  • Propofol / chemical synthesis
  • Propofol / chemistry*
  • Propofol / pharmacology*

Substances

  • Antineoplastic Agents
  • Esters
  • Fatty Acids, Unsaturated
  • Hypnotics and Sedatives
  • Arachidonic Acid
  • Linoleic Acid
  • Caspase 3
  • Propofol