摘要

Four curcuminoid analogues, namely 1,7-dianthryl-1,6-heptadiene-3,5-dione,1a, 1,7-bis(2- hydroxynapthyl)-1,6-heptadiene-3,5-dione, 1b,1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione,1c, 1,7bis (4-methoxyphenyl)-1,6-heptadiene-3,5-dione,1d and their aluminium (III) complexes of ML3 stoichiometry were synthesized and characterized by UV, IR, H-1 NMR and mass spectral data The compounds were investigated for their possible cytotoxic and antitumour activities It was found that aluminium chelates are remarkably active compared to free curcuminoid analogues All the compounds were found to be cytotoxic towards Ehrlich ascites carcinoma cells and cultured L929 cells In the case of culture studies, concentrations needed for 50% cell death were around 41 mu g/ml for aluminium complexes and 10 mu g/ml for curcuminoid analogues Aluminium complex of 1b with hydroxyl group in the naphthyl ring was found to be most active towards L929cells (1 mu g/ml produced 62 5 +/- 1 9% cell death) Compound 1a which is the unsubstituted analogue is found to be the least active compound towards Increase in life span of tumour-bearing mice (percentage increase in life span is 29 5) Aluminium chelates of all curcuminoid analogues showed a significant reduction (P< 001) of solid tumour volume in mice

  • 出版日期2010