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Scientific Articles

NOT Open Access | Dihydroartemisinin, an active metabolite of artemisinin, interferes with Leishmania braziliensis mitochondrial bioenergetics and survival

January 12, 2021 - 14:55 -- NOT Open Access
Author(s): 
Grazzia N, Boaventura S Jr, Garcia VL, Gadelha FR, Miguel DC
Reference: 
Parasitol Res. 2021 Jan 8

Leishmaniasis is one of the most neglected parasitic infections of the world and current therapeutic options show several limitations. In the search for more effective drugs, plant compounds represent a powerful natural source. Artemisinin is a sesquiterpene lactone extracted from Artemisia annua L. leaves, from which dihydroartemisinin (DQHS) and artesunic acid (AA)/artesunate are examples of active derivatives.

Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box

January 12, 2021 - 14:50 -- Open Access
Author(s): 
Reader J, van der Watt ME, Birkholtz LM, et al.
Reference: 
Nat Commun. 2021 Jan 11;12(1):269

Chemical matter is needed to target the divergent biology associated with the different life cycle stages of Plasmodium. Here, we report the parallel de novo screening of the Medicines for Malaria Venture (MMV) Pandemic Response Box against Plasmodium asexual and liver stage parasites, stage IV/V gametocytes, gametes, oocysts and as endectocides. Unique chemotypes were identified with both multistage activity or stage-specific activity, including structurally diverse gametocyte-targeted compounds with potent transmission-blocking activity, such as the JmjC inhibitor ML324 and the antitubercular clinical candidate SQ109.

NOT Open Access | Highly potent anti-malarial activity of benzopyrano(4,3-b)benzopyran derivatives and in silico interaction analysis with putative target Plasmodium falciparum lactate dehydrogenase

January 12, 2021 - 14:39 -- NOT Open Access
Author(s): 
Joshi N, Hada R, Gupta S, Khan J, Dobrowolski J, Dhar PK, Kumar N, Singh S
Reference: 
J Biomol Struct Dyn. 2021 Jan 8:1-16

Malaria infection caused by Plasmodium falciparum is majorly responsible for millions of deaths in humans every year. Moreover, a rapid increase in resistance to existing drugs has posed an urgent need for new anti-malarials. Herein, we report the highly potent anti-malarial activity of benzopyrano(4,3-b)benzopyran derivatives, inspired from naturally occurring dependensin against chloroquine (CQ) sensitive and resistant P. falciparum strains. Chemically synthesized, four dependensin analogs 85(A-D) exhibited growth inhibition at nanomolar concentrations ranging from 63.96 to 725.8 nM by blocking the parasite development at the ring and early trophozoite stages.

Breadth of humoral immune responses to the C-terminus of the circumsporozoite protein is associated with protective efficacy induced by the RTS,S malaria vaccine

January 12, 2021 - 14:36 -- Open Access
Author(s): 
Chaudhury S, MacGill RS, Early AM, Bolton JS, King CR, Locke E, Pierson T, Wirth DF, Neafsey DE, Bergmann-Leitner ES
Reference: 
Vaccine. 2021 Jan 8:S0264-410X(20)31635-2

The circumsporozoite protein (CSP) is the main surface antigen of malaria sporozoites, a prime vaccine target, and is known to have polymorphisms in the C-terminal region. Vaccines using a single allele may have lower efficacy against genotypic variants. Recent studies have found evidence suggesting the efficacy of the CSP-based RTS,S malaria vaccine may be limited against P. falciparum CSP alleles that diverge from the 3D7 vaccine allele, particularly in this polymorphic C-terminal region.

NOT Open Access | Using pastoralist community knowledge to locate and treat dry-season mosquito breeding habitats with pyriproxyfen to control Anopheles gambiae s.l. and Anopheles funestus s.l. in rural Tanzania

January 12, 2021 - 14:35 -- NOT Open Access
Author(s): 
Lupenza ET, Kihonda J, Limwagu AJ, Ngowo HS, Sumaye RD, Lwetoijera DW
Reference: 
Parasitol Res. 2021 Jan 6

Fundamentally, larviciding with pyriproxyfen (PPF) has potential to complement Long Lasting Insecticide Nets (LLINs) and indoor residual sprays (IRS) in settings where resistance to pyrethroids and residual malaria transmission exist. In this study, we evaluated the field effectiveness of larviciding using PPF to reduce dry season productivity of mosquito breeding habitats that were located by pastoralists within the study area.

Synthesis and Evaluation of 2-Hydroxy-1,4-Naphthoquinone Derivatives as Potent Antimalarial Agents

January 12, 2021 - 14:32 -- Open Access
Author(s): 
Paengsri W, Promsawan N, Baramee A
Reference: 
Chem Pharm Bull (Tokyo). 2021 Jan 8

A series of 3-substituted-2-hydroxy-1,4-naphthoquinone derivatives with a variety of side chains were successfully synthesized by Mannich reaction of 2-hydroxy-1,4-naphthoquinone (lawsone) with selected amines and aldehydes. All substances (1-16) were evaluated for in-vitro antimalarial activity against strains of Plasmodium falciparum by microculture radioisotope technique.

NOT Open Access | A Diverse Range of Hemozoin Inhibiting Scaffolds Act on Plasmodium falciparum as Heme Complexes

January 12, 2021 - 14:30 -- NOT Open Access
Author(s): 
Openshaw R, Maepa K, Benjamin SJ, Wainwright L, Combrinck JM, Hunter R, Egan TJ
Reference: 
ACS Infect Dis. 2021 Jan 12

A diverse series of hemozoin-inhibiting quinolines, benzamides, triarylimidazoles, quinazolines, benzimidazoles, benzoxazoles, and benzothiazoles have been found to lead to exchangeable heme levels in cultured Plasmodium falciparum (NF54) that ranged over an order of magnitude at the IC50. Surprisingly, less active compounds often exhibited higher levels of exchangeable heme than more active ones.

Has COVID19 derailed Bhutan’s national malaria elimination goal? A commentary

January 9, 2021 - 13:49 -- Open Access
Author(s): 
Kinley Penjor, Tobgyal, Tandin Zangpo, Archie C. A. Clements, Darren J. Gray and Kinley Wangdi
Reference: 
Malaria Journal 2021 20:20, 6 January 2021

The COVID-19 pandemic has resulted in massive global disruptions with considerable impact on the delivery of health services and national health programmes. Since the detection of the first COVID-19 case on 5th March 2020, the Royal Government of Bhutan implemented a number of containment measures including border closure and national lockdowns.

Community demand for comprehensive primary health care from malaria volunteers in South-East Myanmar: a qualitative study

January 9, 2021 - 13:48 -- Open Access
Author(s): 
Win Han Oo, Elizabeth Hoban, Lisa Gold, Kyu Kyu Than, Thazin La, Aung Thi and Freya J. I. Fowkes
Reference: 
Malaria Journal 2021 20:19, 6 January 2021

Malaria volunteers have contributed significantly to malaria control achieving a reduction of annual parasite incidence to pre-elimination levels in several townships across Myanmar. However, the volunteers’ role is changing as Myanmar transitions from a malaria control to elimination programme and towards the goal of universal health coverage. The aim of the study is to explore the perspectives of community leaders, members and malaria volunteers in South-East Myanmar on community-delivered models to inform an optimal design that targets malaria elimination in the context of primary health care in Myanmar.

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