Cytotoxicity effects of di- and tri-hydroxybenzaldehydes as a chemopreventive potential agent on tumor cells

As part of our earlier search for new compounds with improved biological activities including antioxidant, anti-inflammatory, and tumor growth inhibition activities, we synthesized 2,4,5-trihydroxybenzaldehyde (2,4,5-THBA) from commercially available Sesamol. First we examined the free radical-quenching capacity of 2,4,5-THBA, 3,4-dihydroxybenzaldehyde (3,4-DHBA), and 2,5-dihydroxybenzaldehyde (2,5-DHBA) in vitro by 1,1-diphenyl-1,2-picryhydrazylradical (DPPH) test. The antioxidant bioactivity was also evaluated using the model of t-butyl hydroperoxide (t-BHP)-induced cytotoxicity in rat primary hepatocytes. Finally, three chemicals were tested by tl;e 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay on human nasopharynx carcinoma cells (KB calls), human hepatoblastoma (HepG2), and human leukemia HL-60 cells. The 2,4,5-THBA shows significant cytotoxicity on HL-60 cells. The results suggest that 2,4,5-THBA may be a potential chemopreventor or chemotherapy agent against HL-60 cells. (C) 2001 Elsevier Science Ireland Ltd. All rights reserved.