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Haloenol lactone: a new synergist of chemotherapy in vitro.

Over-expression of glutathione S-transferases (GST) has been found to play a significant role in multiple drug resistance in cancer chemotherapy. To combat GST-mediated drug resistance, GST inhibitors are being studied as potential synergists for effective cancer chemotherapy. We have designed and synthesized a haloenol lactone derivative as a mechanism-based inactivator of GST-pi isozyme. In the current study, we examined the inhibitory effect of the haloenol lactone compound on GST of a human renal carcinoma cell line UOK130 and found that this compound shows time-dependent GST inhibition in these cancer cells. The enzyme activity lost upon incubation with the haloenol lactone could not be restored by extensive dialysis against buffer. Pretreatment of the cancer cells with 1.0 microM of haloenol lactone increased cytotoxicity induced by cisplatin in the UOK130 cell line. This report further supports the possibility of synergizing alkylating agents in cancer chemotherapy by use of selective GST inhibitors.