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Exploring natural microbial resources for the discovery of anti-malarial compounds

August 10, 2021 - 18:00 -- Open Access
Waluyo D, Prabandari EE, Nozaki T, et al.
Parasitol Int. 2021 Aug 4:102432

Microorganisms in nature are highly diverse biological resources, which can be explored for drug discovery. Some countries including Brazil, Columbia, Indonesia, China, and Mexico, which are blessed with geographical uniqueness with diverse climates display remarkable megabiodiversity, potentially provide microorganismal resources for such exploitation.

Is there evidence of anti-malarial multidrug resistance in Burkina Faso?

July 21, 2021 - 17:57 -- Open Access
Charlotte Rasmussen and Pascal Ringwald
Malaria Journal 2021 20:320, 19 July 2021

Recently, Gansané and colleagues published an article on inadequate efficacy of two different forms of artemisinin-based combination therapy (ACT) in Burkina Faso. The development of Plasmodium falciparum resistance to different ACT partner drugs at levels that could affect the efficacy of two ACT would both be startling and a cause for great concern. In reviewing the available data collected since 2008 on ACT efficacy in Burkina Faso, the analysis shows that the reported efficacy of the tested ACT varies greatly.

Broad spectrum anti-coronavirus activity of a series of anti-malaria quinoline analogues

July 6, 2021 - 13:36 -- Open Access
Persoons L, Vanderlinden E, Vangeel L, Wang X, Thuc Do ND, Caroline Foo SY, Leyssen P, Neyts J, Jochmans D, Schols D, De Jonghe S
Antiviral Res. 2021 Jul 1:105127

In this study, a series of 10 quinoline analogues was evaluated for their in vitro antiviral activity against a panel of alpha- and beta-coronaviruses, including the severe acute respiratory syndrome coronaviruses 1 and 2 (SARS-CoV-1 and SARS-CoV-2), as well as the human coronaviruses (HCoV) 229E and OC43. Chloroquine and hydroxychloroquine were the most potent with antiviral EC50 values in the range of 0.12-12 μM. Chloroquine displayed the most favorable selectivity index (i.e. ratio cytotoxic versus antiviral concentration), being 165 for HCoV-OC43 in HEL cells.

Evaluation of the effect of supervised anti-malarial treatment on recurrences of Plasmodium vivax malaria

June 16, 2021 - 13:11 -- Open Access
Kelry Mazurega Oliveira Dinelly, Sheila Vitor-Silva, Gisely Cardoso Melo, et al.
Malaria Journal 2021 20:266, 13 June 2021

Relapses in vivax malaria have posed great challenges for malaria control, and they also account for a great proportion of reported cases. Knowing the real effectiveness of a 7-day primaquine (PQ) scheme is crucial in order to evaluate not only the cost-effectiveness of implementing new anti-hypnozoite drugs, but also how health education strategies can guarantee better compliance and be reinforced. This study aimed to evaluate the effect of daily treatment with chloroquine and PQ supervised by health workers versus prescription without supervision.

2D-quantitative structure–activity relationships model using PLS method for anti-malarial activities of anti-haemozoin compounds

June 16, 2021 - 12:59 -- Open Access
Phuong Thuy Viet Nguyen, Truong Van Dat, Kenji Hirayama, et al.
Malaria Journal 2021 20:264, 11 June 2021

Emergence of cross-resistance to current anti-malarial drugs has led to an urgent need for identification of potential compounds with novel modes of action and anti-malarial activity against the resistant strains. One of the most promising therapeutic targets of anti-malarial agents related to food vacuole of malaria parasite is haemozoin, a product formed by the parasite through haemoglobin degradation.

NOT Open Access | An insight in anti-malarial potential of indole scaffold: A review

June 9, 2021 - 07:25 -- NOT Open Access
Chauhan M, Saxena A, Saha B
Eur J Med Chem. 2021 Jun 5;218:113400

Malaria is a major parasitic disease in tropical and sub-tropical regions. Pertaining to the sustaining resistance in malarial parasite against the available drugs, novel treatment options are the need of the hour. In this resolve recently, focus has shifted to finding the natural alternatives that possess anti-plasmodial activity for combatting malaria.

Malaria-Resistant Mosquitoes (Diptera: Culicidae); The Principle is Proven, But Will the Effectors Be Effective

May 25, 2021 - 13:53 -- Open Access
Adelman ZN, Kojin BB
J Med Entomol. 2021 May 21:tjab090

Over the last few decades, a substantial number of anti-malarial effector genes have been evaluated for their ability to block parasite infection in the mosquito vector. While many of these approaches have yielded significant effects on either parasite intensity or prevalence of infection, just a few have been able to completely block transmission.

Malaria and Cancer: a critical review on the established associations and new perspectives

May 19, 2021 - 13:28 -- Open Access
Ellis T, Eze E, Raimi-Abraham BT
Infect Agent Cancer. 2021 May 13;16(1):33

Cancer and malaria both have high incidence rates and are leading causes of mortality worldwide, especially in low and middle-income countries with reduced access to the quality healthcare. The objective of this critical review was to summarize key associations and new perspectives between the two diseases as is reported in existing literature.

Artemisinin combination therapy fails even in the absence of Plasmodium falciparum kelch13 gene polymorphism in Central India

May 13, 2021 - 12:39 -- Open Access
Das S, Kar A, Manna S, Mandal S, Mandal S, Das S, Saha B, Hati AK
Sci Rep. 2021 May 11;11(1):9946

Artemisinin is the frontline fast-acting anti-malarial against P. falciparum. Emergence and spread of resistant parasite in eastern-India poses a threat to national malaria control programs. Therefore, the objective of our study is to evaluate the artesunate-sulfadoxine-pyrimethamine efficacy in Central India. 180 monoclonal P. falciparum-infected patients received standard ASSP therapy during August 2015-January 2017, soon after diagnosis and monitored over next 42-days. Artemisinin-resistance was assessed through in-vivo parasite clearance half-life (PC1/2), ex-vivo ring-stage survivability (RSA), and genome analysis of kelch13 and other candidate gene (pfcrt, pfmdr1, pfatpase 6, pfdhfr and pfdhps).

NOT Open Access | Inhibition of Plasmodium falciparum Lysyl-tRNA synthetase via a piperidine-ring scaffold inspired Cladosporin analogues

May 12, 2021 - 09:26 -- NOT Open Access
Babbar P, Sato M, Manickam Y, Mishra S, Harlos K, Gupta S, Parvez S, Kikuchi H, Sharma A
Chembiochem. 2021 May 9

Plasmodium falciparum lysyl tRNA synthetase ( Pf KRS) represent a promising therapeutic anti-malarial target. Cladosporin, a tool compound was identified as a selective and potent PfKRS inhibitor but lacks metabolic stability. Here, we report chemical synthesis, biological evaluation and structural characterization of analogues where the tetrahydropyran (THP) frame of cladosporin is replaced with the piperidine ring bearing functional group variations.


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