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Rhodesain is a cysteine protease crucial for the survival of  Trypanosoma brucei rhodesiense , the parasite able to induce the acute lethal form of Human African Trypanosomiasis.  PS-1  is a synthetic peptidyl inhibitor of rhodesain, characterised by a picomolar binding affinity ( Ki  = 1.1 pM). Thus, considering the well-known antiparasitic properties of quercetin, in this study, we decided to carry out drug combination studies of  PS-1  and quercetin against rhodesain, according to Chou and Talalay method, which allowed us to obtain for the most relevant f a  values a nearly additive effect for the reduction of rhodesain activity from 40% to 90%, thus considering a promising strategy their use in combination.

Drug combination studies of PS-1 and quercetin against rhodesain of Trypanosoma brucei rhodesiense