Epicatechin derivative shows promise in melanoma therapy

02 September 2009

Human melanoma is a significant clinical problem because it is resistant to treatment by most chemotherapeutic agents, including antifolates. Non naturally occuring (-)-epicatechin derivates, in particular the 3-O-(3,4,5-trimethoxybenzoyl)-(-)-epicatechin derivative, when used as a prodrug is activated by the melanocyte enzyme tyrosinase which strongly inhibits dihydrofolate reductase in an irreversible manner.

The treatment of melanoma cells with this derivative also affected cellular folate transport and the gene expression of DHFR, which supported the antifolate nature of this compound. In addition, its pharmacological efficacy has been confirmed in a mouse melanoma model, in which tumor growth and metastasis were inhibited, significantly enhancing the mean survival of the treated groups.

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