Drug synergism: Studies of Combination of RK-52 and Curcumin against Rhodesain of Trypanosoma brucei rhodesiense

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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 ksecond value (ksecond = 67000 × 103 M−1 min−1) and by a picomolar affinity toward the trypanosomal protease (Ki = 38 pM). Differently, curcumin, the golden multitarget nutraceutical obtained from Curcuma longa L., was proven to inhibit rhodesain non-competitively 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%.

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Ettari, R., Previti, S., Di Chio, C., Maiorana, S., Allegra, A., Schirmeister, T., & Zappala, M. (2020). Drug synergism: Studies of Combination of RK-52 and Curcumin against Rhodesain of Trypanosoma brucei rhodesiense. ACS Medicinal Chemistry Letters, 11(5), 806–810. https://doi.org/10.1021/acsmedchemlett.9b00635

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