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 fa 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
Carla Di Chio;Santo Previti;Fabiola De Luca;Alessandro Allegra;Maria Zappalà;Roberta Ettari
2022-01-01
Abstract
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 fa values a nearly additive effect for the reduction of rhodesain activity from 40% to 90%, thus considering a promising strategy their use in combination.Pubblicazioni consigliate
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