posted on 2021-09-17, 12:40authored byCarla Di Chio, Santo Previti, Fabiola De Luca, Alessandro Allegra, Maria Zappalà, Roberta Ettari
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.
Funding
This work was financially supported by the ‘FFABR 2020’ financed by UNIME.