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NOT Open Access | Novel molecule combinations and corresponding hybrids targeting artemisinin-resistant Plasmodium falciparum parasites

May 5, 2021 - 11:03 -- NOT Open Access
Ouji M, Nguyen M, Mustière R, Jimenez T, Augereau JM, Benoit-Vical F, Deraeve C
Bioorg Med Chem Lett. 2021 May 1;39:127884

Malaria is still considered as the major parasitic disease and the development of artemisinin resistance does not improve this alarming situation. Based on the recent identification of relevant malaria targets in the artemisinin resistance context, novel drug combinations were evaluated against artemisinin-sensitive and artemisinin-resistant Plasmodium falciparum parasites.

NOT Open Access | Atovaquone/Proguanil Resistance in an Imported Malaria Case in Chile

March 31, 2021 - 14:35 -- NOT Open Access
Chenet SM, Oyarce A, Fernandez J, Tapia-Limonchi R, Weitzel T, Tejedo JR, Udhayakumar V, Jercic MI, Lucchi NW
Am J Trop Med Hyg. 2021 Mar 29:tpmd201095

In November 2018, we diagnosed a cluster of falciparum malaria cases in three Chilean travelers returning from Nigeria. Two patients were treated with sequential intravenous artesunate plus oral atovaquone/proguanil (AP) and one with oral AP. The third patient, a 23-year-old man, presented with fever on day 29 after oral AP treatment and was diagnosed with recrudescent falciparum malaria.

NOT Open Access | Inhibition Mechanism of Antimalarial Drugs Targeting the Cytochrome bc1 Complex

February 23, 2021 - 13:16 -- NOT Open Access
Jacobsen L, Husen P, Solov'yov IA
J Chem Inf Model. 2021 Feb 22

Plasmodium falciparum (P. falciparum) is the main parasite known to cause malaria in humans. The antimalarial drug atovaquone is known to inhibit the Qo-site of the cytochrome bc1 complex of P. falciparum, which ultimately blocks ATP synthesis, leading to cell death. Through the years, mutations of the P. falciparum cytochrome bc1 complex, causing resistance to atovaquone, have emerged.

NOT Open Access | Exploring ubiquinone biosynthesis inhibition as a strategy for improving atovaquone efficacy in malaria

January 27, 2021 - 10:19 -- NOT Open Access
Verdaguer IB, Crispim M, Zafra CA, Sussmann RAC, Buriticá NL, Melo HR, Azevedo MF, Almeida FG, Kimura EA, Katzin AM
Antimicrob Agents Chemother. 2021 Jan 25:AAC.01516-20

Atovaquone (AV) acts on the malaria parasite by competing with ubiquinol (UQH2) for its union to the mitochondrial bc1 complex, preventing the ubiquinone-8,9 (UQ) redox recycling, which is a necessary step in pyrimidine biosynthesis. This study focused on UQ biosynthesis in Plasmodium falciparum and adopted proof-of-concept research to better elucidate the mechanism of action of AV and improve its efficacy. Initially, UQ biosynthesis was evaluated using several radioactive precursors and chromatographic techniques.

NOT Open Access | Antimalarial application of quinones: A recent update

January 20, 2021 - 08:02 -- NOT Open Access
Patel OPS, Beteck RM, Legoabe LJ
Eur J Med Chem. 2021 Jan 15;210:113084

Atovaquone belongs to a naphthoquinone class of drugs and is used in combination with proguanil (Malarone) for the treatment of acute, uncomplicated malaria caused by Plasmodium falciparum (including chloroquine-resistant P. falciparum/P. vivax). Numerous quinone-derived compounds have attracted considerable attention in the last few decades due to their potential in antimalarial drug discovery.

Revisiting the mode of action of the antimalarial proguanil using the yeast model

December 15, 2020 - 14:06 -- Open Access
Mounkoro P, Michel T, Meunier B
Biochem Biophys Res Commun. 2020 Dec 11;534:94-98

Proguanil in combination with its synergistic partner atovaquone has been used for malaria treatment and prophylaxis for decades. However its mode of action is not fully understood. Here we used yeast to investigate its activity. Proguanil inhibits yeast growth, causes cell death and acts in synergy with atovaquone. It was previously proposed that the drug would target the system that maintains the mitochondrial membrane potential when the respiratory chain is inhibited.

NOT Open Access | In silico, in vitro and in vivo evaluation of natural Bignoniaceous naphthoquinones in comparison with atovaquone targeting the selection of potential antimalarial candidates

June 1, 2020 - 16:06 -- NOT Open Access
do Nascimento MFA, Borgati TF, de Souza LCR, Tagliati CA, de Oliveira AB
Toxicol Appl Pharmacol. 2020 May 25:115074

The natural naphthoquinones lapachol, α- and β-lapachone are found in Bignoniaceous Brazilian plant species of the Tabebuia genus (synonym Handroanthus) and are recognized for diverse bioactivities, including as antimalarial. The aim of the present work was to perform in silico, in vitro and in vivo studies to evaluating the antimalarial potential of these three naphthoquinones in comparison with atovaquone, a synthetic antimalarial.

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