Cytotoxicity of diospyrin and its derivatives in relation to the generation of reactive oxygen species in tumour cells in vitro and in vivo.

BACKGROUND

Alkyl ethers (D2 and D7) synthesized from diospyrin (D1), a naphthoquinonoid isolated from Diospyros montana Roxb., were evaluated for cytotoxicity and capacity to generate reactive oxygen species (ROS) in tumour cells.

METHODS

The tumour inhibitory activity of the quinonoids was assessed in vivo against Ehrlich ascites carcinoma (EAC), while cytotoxicity was determined in vitro on EAC and MCF-7 cancer cells by MTT assay. ROS generated by quinonoids in MCF-7 cells was measured fluorimetrically.

RESULTS

The tumour inhibitory activity, cytotoxicity and ROS generation capacity of quinonoids were found to be D7 > D2 > D1.

CONCLUSIONS

Alkyl ethers of D1 were more cytotoxic against tumour cells in vitro as well as in vivo.