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Natural Product Research
Formerly Natural Product Letters
Volume 36, 2022 - Issue 16
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Short Communications

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

, , , , & ORCID Icon
Pages 4282-4286 | Received 03 May 2021, Accepted 31 Aug 2021, Published online: 17 Sep 2021
 

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.

Graphical Abstract

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was financially supported by the ‘FFABR 2020’ financed by UNIME.

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