Drug combination studies of PS-1 and quercetin against rhodesain of Trypanosoma brucei rhodesiense.
Carla Di ChioSanto PrevitiFabiola De LucaAlessandro AllegraMaria ZappalàRoberta EttariPublished in: Natural product research (2021)
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.
Keyphrases
- endothelial cells
- drug induced
- case control
- liver failure
- air pollution
- particulate matter
- respiratory failure
- adverse drug
- emergency department
- heavy metals
- squamous cell carcinoma
- transcription factor
- intensive care unit
- lymph node
- radiation therapy
- acute respiratory distress syndrome
- fluorescent probe
- living cells
- hepatitis b virus
- water soluble