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NOT Open Access | Evaluation of Mongolian compound library for potential antimalarial and anti-Toxoplasma agents

July 28, 2021 - 13:25 -- NOT Open Access
Banzragchgarav O, Ariefta NR, Murata T, Myagmarsuren P, Battsetseg B, Battur B, Batkhuu J, Yoshifumi N
Parasitol Int. 2021 Jul 22:102424

179 compounds in a Mongolian compound library were investigated for their inhibitory effect on the in vitro growth of Plasmodium falciparum and Toxoplasma gondii. Among these compounds, brachangobinan A at a half-maximal inhibition concentration (IC50) of 2.62 μM and a selectivity index (SI) of 27.91; 2-(2'-hydroxy-5'-O-methylphenyl)-5-(2″,5″-dihydroxyphenyl)oxazole (IC50 3.58 μM and SI 24.66); chrysosplenetin (IC50 3.78 μM and SI 15.26); 4,11-di-O-galloylbergenin (IC50 3.87 μM and SI 13.38); and 2-(2',5'-dihydroxyphenyl)-5-(2″-hydroxyphenyl)oxazole (IC50 6.94 μM and SI 11.48) were identified as potential inhibitors of P. falciparum multiplication.

The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance

July 28, 2021 - 12:53 -- Open Access
Murithi JM, Pascal C, Leroy D, et al.
Sci Transl Med. 2021 Jul 21;13(603):eabg6013

The emergence and spread of Plasmodium falciparum resistance to first-line antimalarials creates an imperative to identify and develop potent preclinical candidates with distinct modes of action. Here, we report the identification of MMV688533, an acylguanidine that was developed following a whole-cell screen with compounds known to hit high-value targets in human cells.

Does subsidizing the private for-profit sector benefit the poor? Evidence from national antimalarial subsidies in Nigeria and Uganda

July 28, 2021 - 12:49 -- Open Access
Tougher S, Hanson K, Goodman CA
Health Econ. 2021 Jul 22

Subsidising quality-assured artemisinin combination therapies (QAACTs) for distribution in the for-profit sector is a controversial strategy for improving access. The Affordable Medicines Facility-malaria (AMFm) was the largest initiative of this kind. We assessed the equity of AMFm in two ways using nationally representative household survey data on care seeking for children from Nigeria and Uganda.

Not Open Access | Murine pharmacokinetics and antimalarial pharmacodynamics of dihydroartemisinin trimer self-assembled nanoparticles

July 20, 2021 - 14:30 -- NOT Open Access
Guo W, Li N, Ren G, Wang R, Chai L, Li Y, Wang X, Yang Q, Wang R, Zhang G, Yang L, Yi B, Zhang S
Parasitol Res. 2021 Jul 17

Currently, conjugation of artemisinin-derived dimers, trimers, and tetramers is a viable strategy for developing new effective antimalarial candidates. Furthermore, nanotechnology is an effective means to achieve intravenous administration of hydrophobic drugs. In this paper, an ester-linked dihydroartemisinin trimer (DHA3) was synthesized and further prepared as self-assembled nanoparticles (DHA3NPs) by a one-step nanoprecipitation method. The pharmacokinetics and antimalarial pharmacodynamics of DHA3NPs were studied in rats and mice infected with Plasmodium yoelii BY265 (PyBY265). DHA3NPs had a regular spherical shape with a uniform size distribution of 140.27 ± 3.59 nm, entrapment efficiency (EE) of 99.63 ± 0.17%, and drug loading efficiency (DL) of 79.62 ± 0.11%.

Plasmodium falciparum kelch 13 Mutations, 9 Countries in Africa, 2014-2018

July 6, 2021 - 13:16 -- Open Access
Schmedes SE, Patel D, Talundzic E, et al.
Emerg Infect Dis. 2021 Jul;27(7):1902-1908

The spread of drug resistance to antimalarial treatments poses a serious public health risk globally. To combat this risk, molecular surveillance of drug resistance is imperative. We report the prevalence of mutations in the Plasmodium falciparum kelch 13 propeller domain associated with partial artemisinin resistance, which we determined by using Sanger sequencing samples from patients enrolled in therapeutic efficacy studies from 9 sub-Saharan countries during 2014-2018.

Antimalarial Activity of 2,6-Dibenzylidenecyclohexanone Derivatives

June 23, 2021 - 14:25 -- Open Access
Eagon S, Hammill JT, Kiplin Guy R, et al.
Bioorg Med Chem Lett. 2021 Jun 19:128216

Malaria remains one of the deadliest diseases on the planet, infecting an estimated 229 million individuals in 2019 with more than 400,000 associated deaths, primarily in young children and pregnant women. Malaria is caused by Plasmodium parasite infection of the liver and blood, with P. falciparum accounting for the vast majority of deaths.

NOT Open Access | Heparin-decorated nanostructured lipid carriers of artemether-protoporphyrin IX-transferrin combination for therapy of malaria

June 23, 2021 - 13:50 -- NOT Open Access
Dong X, Zhang X, Wang M, Gu L, Li J, Gong M
Int J Pharm. 2021 Jun 15:120813

Heme is a prosthetic group of hemoglobin comprising protoporphyrin IX (PPIX) with Fe2+. Studies have shown that modulating heme synthesis pathway in Plasmodium could greatly affect the action mechanism and antimalarial effect of artemisinin and its derivatives. Herein, an intraerythrocytic parasite targeted nanostructured lipid carrier (NLC) was developed for potentiation of artemether (ARM) by combination with PPIX and iron-loaded transferrin (holo-Tf). Firstly, ARM and PPIX were co-loaded into NLCs with high entrapment efficiency.

Composition and stage dynamics of mitochondrial complexes in Plasmodium falciparum

June 23, 2021 - 13:25 -- Open Access
Evers F, Cabrera-Orefice A, Elurbe DM, Kea-Te Lindert M, Boltryk SD, Voss TS, Huynen MA, Brandt U, Kooij TWA
Nat Commun. 2021 Jun 21;12(1):3820

Our current understanding of mitochondrial functioning is largely restricted to traditional model organisms, which only represent a fraction of eukaryotic diversity. The unusual mitochondrion of malaria parasites is a validated drug target but remains poorly understood.

Properties of Plasmodium falciparum with a deleted apicoplast DNA gyrase

June 22, 2021 - 15:12 -- Open Access
Tan S, Mudeppa DG, Kokkonda S, White J 3rd, Patrapuvich R, Rathod PK
Antimicrob Agents Chemother. 2021 Jun 21:AAC0058621

Malaria parasites have three genomes: a nuclear genome, a mitochondrial genome, and an apicoplast genome. Since the apicoplast is a plastid organelle of prokaryotic origin and has no counterpart in the human host, it can be a source of novel targets for antimalarials. Plasmodium falciparum DNA gyrase (PfGyr) A and B subunits both have apicoplast-targeting signals.

NOT Open Access | Intranasal artesunate-loaded nanostructured lipid carriers: A convenient alternative to parenteral formulations for the treatment of severe and cerebral malaria

June 15, 2021 - 15:09 -- NOT Open Access
Agbo CP, Ugwuanyi TC, Ugwuoke WI, McConville C, Attama AA, Ofokansi KC
J Control Release. 2021 Jun 10;334:224-236

Early treatment with parenteral antimalarials is key in preventing deaths and complications associated with severe and cerebral malaria. This can be challenging in 'hard-to-reach' areas in Africa where transit time to hospitals with facilities to administer drugs parenterally can be more than 6 h. Consequently, the World Health Organization has recommended the use of artesunate (ATS) suppositories for emergency treatment of patients, however, this treatment is only for children under 6 years. The intranasal route (INR) can provide a safe and effective alternative to parenteral and rectal routes for patients of all ages; thus, reducing delays to the initiation of treatment.


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