Synthesis of Curcuminoids and Evaluation of Their Cytotoxic and Antioxidant Properties

Molecules. 2017 Apr 14;22(4):633. doi: 10.3390/molecules22040633.

Abstract

Curcumin (1) and ten derivatives (2-11) were synthesized and evaluated as cytotoxic and antioxidant agents. The results of primary screening by Sulforhodamine B assay against five human cancer cell lines (U-251 MG, glioblastoma; PC-3, human prostatic; HCT-15, human colorectal; K562, human chronic myelogenous leukemia; and SKLU-1, non-small cell lung cancer) allowed us to calculate the half maximal inhibitory concentration (IC50) values for the more active compounds against HCT-15 and K562 cell lines. Compounds 2 and 10 were the most active against both cell lines and were more active than curcumin itself. Thiobarbituric acid reactive substances (TBARS) assay showed that 7 has potent activity; even stronger than curcumin, α-tocopherol, and quercetin.

Keywords: antioxidant; azoles; curcumin; cytotoxic.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Antioxidants / chemical synthesis*
  • Antioxidants / pharmacology*
  • Cell Line, Tumor
  • Cell Survival
  • Curcumin / analogs & derivatives
  • Curcumin / chemical synthesis*
  • Curcumin / pharmacology*
  • Free Radical Scavengers / chemical synthesis
  • Free Radical Scavengers / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Rats

Substances

  • Antineoplastic Agents
  • Antioxidants
  • Free Radical Scavengers
  • Curcumin