ABSTRACT
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. CONCLUSION: Alkyl ethers of D1 were more cytotoxic against tumour cells in vitro as well as in vivo.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Carcinoma, Ehrlich Tumor/drug therapy , Ethers/pharmacology , Naphthoquinones/pharmacology , Animals , Cell Line, Tumor , Humans , Lipid Peroxidation , Mice , Reactive Oxygen Species/metabolism , Xenograft Model Antitumor AssaysABSTRACT
Three derivatives and one structural analogue of diospyrin were synthesized and investigated for their inhibitory activity against Mycobacterium tuberculosis employing the rapid radiometric method in vitro. A novel aminoacetate derivative was found to be more active than the parent compound, the MICs being 50 and 100 mg/L, respectively, for a drug-susceptible strain, H37Rv, of M. tuberculosis. This derivative also exhibited an MIC of 50 mg/L for a few multidrug-resistant strains of M. tuberculosis. The other two derivatives and the analogue did not show any significant antimycobacterial activity at the highest concentration (100 mg/L) tested.
