Abstract
Rhodesain is an enzyme essential for the life of Trypanosoma brucei rhodesiense, a parasite causing a rapid-onset form of Human African Trypanosomiasis. RK-52 is a synthetic inhibitor of rhodesain, characterized by an impressive k second value (k second = 67000 × 103 M-1 min-1) and by a picomolar affinity toward the trypanosomal protease (K i = 38 pM). Differently, curcumin, the golden multitarget nutraceutical obtained from Curcuma longa L., was proven to inhibit rhodesain noncompetitively with an IC50 of 7.75 μM. In the present study, we carried out studies of a combination of RK-52 and curcumin toward rhodesain, by applying the Chou and Talalay approach, which led us to obtain a combination index <1 for the most relevant fa values, which means a potent synergistic effect for the reduction of rhodesain activity from 40% to 99%.
Highlights
Trypanosoma brucei rhodesiense, a parasite causing a rapid-onset form of Human African Trypanosomiasis
We carried out studies of a combination of RK-52 and curcumin toward rhodesain, by applying the Chou and Talalay approach, which led us to obtain a combination index
Human African Trypanosomiasis (HAT) is a parasitic disease occurring in sub-Saharan Africa, inducing mortality despite a significant decrease of novel cases recently having been observed.[1]
Summary
Trypanosoma brucei rhodesiense, a parasite causing a rapid-onset form of Human African Trypanosomiasis. We carried out studies of a combination of RK-52 and curcumin toward rhodesain, by applying the Chou and Talalay approach, which led us to obtain a combination index
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