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Pathogens
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Emerging Treatment Options to Fight Malaria: New Compounds and Drug...
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Emerging Treatment Options to Fight Malaria: New Compounds and Drug Combinations

A special issue of Pathogens (ISSN 2076-0817). This special issue belongs to the section "Parasitic Pathogens".

Deadline for manuscript submissions: closed (28 September 2023) | Viewed by 3414

Special Issue Editors

Dr. Nicolò Musso

E-Mail Website
Guest Editor
Bio-Nanotech Research and Innovation Tower (BRIT), University of Catania, 95125 Catania, Italy
Interests: Malaria
Special Issues, Collections and Topics in MDPI journals
Dr. Andrea Marino

E-Mail Website
Guest Editor
Department of Clinical and Experimental Medicine, University of Catania, Catania, Italy
Interests: infectious diseases; bacterial infections; viral infections; antibiotic stewardship
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Despite unsuccessful eradication attempts, control efforts to avoid infections, and artemisinin-based therapies, the global burden of malaria remains high, with 430,000 deaths every year and 200 million cases. Unfortunately, children represent a high proportion of new diagnoses.

Over the last few years, renewed attempts to control the disease have reduced the prevalence of malaria by over 50%, raising the prospect that elimination and perhaps eradication may be a long-term possibility.

Achievement of this goal requires the development of new tools, including efficacious vaccines as well as a precise understanding of the pathophysiology and biology of the parasite, and especially novel antimalarial drugs and combinations which could safely ensure the rapid clearance of infection as well as a durable cure without recurrence. In addition, the development of resistance to past and present anti-malarial drugs, especially artemisinin-based regimes, highlights the need for continued research to stay one step ahead, specifically to treat severe complications such as cerebral malaria.

Multiple approaches to develop new antimalarial medications, ranging from modifications of existing agents to the design of novel agents targeting novel targets, already exist.

Modern advances in parasite biology knowledge, along with the availability of various genomic techniques, represent several novel targets for the elaboration of new therapies.

This Special Issue aims to collect original articles, literature reviews, and case reports/case series on emerging treatment options against malaria, with particular interest on new compounds, either experimental or under research, and drug combinations.

Dr. Nicolò Musso
Dr. Andrea Marino
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pathogens is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Malaria
  • antimalarial drugs
  • severe malaria
  • resistant malaria
  • treatment

Published Papers (2 papers)

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Research

17 pages, 11110 KiB  
Article
Novel Baicalein-Derived Inhibitors of Plasmodium falciparum
by Chandra Sekhar Gudla, Vignesh Selvam, Siva Shanmugam Selvaraj, Renu Tripathi, Prince Joshi, Salique Hassan Shaham, Mayas Singh, Radha Krishan Shandil, Saman Habib and Shridhar Narayanan
Pathogens 2023, 12(10), 1242; https://doi.org/10.3390/pathogens12101242 - 13 Oct 2023
Cited by 1 | Viewed by 1286
Abstract
Malaria, a life-threatening mosquito-borne disease caused by Plasmodium parasites, continues to pose a significant global health burden. Despite notable progress in combating the disease in recent years, malaria remains prevalent in many regions, particularly in Southeast Asia and most of sub-Saharan Africa, where [...] Read more.
Malaria, a life-threatening mosquito-borne disease caused by Plasmodium parasites, continues to pose a significant global health burden. Despite notable progress in combating the disease in recent years, malaria remains prevalent in many regions, particularly in Southeast Asia and most of sub-Saharan Africa, where it claims hundreds of thousands of lives annually. Flavonoids, such as the baicalein class of compounds, are known to have antimalarial properties. In this study, we rationally designed and synthesized a series of baicalein derivatives and identified a lead compound, FNDR-10132, that displayed potent in vitro antimalarial activity against Plasmodium falciparum (P. falciparum), both chloroquine-sensitive (60 nM) and chloroquine-resistant (177 nM) parasites. FNDR-10132 was evaluated for its antimalarial activity in vivo against the chloroquine-resistant strain Plasmodium yoelii N67 in Swiss mice. The oral administration of 100 mg/kg of FNDR-10132 showed 44% parasite suppression on day 4, with a mean survival time of 13.5 ± 2.3 days vs. 8.4 ± 2.3 days of control. Also, FNDR-10132 displayed equivalent activity against the resistant strains of P. falciparum in the 200–300 nM range. This study offers a novel series of antimalarial compounds that could be developed into potent drugs against chloroquine-resistant malarial parasites through further chemistry and DMPK optimization. Full article
(This article belongs to the Special Issue Emerging Treatment Options to Fight Malaria: New Compounds and Drug Combinations)
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20 pages, 2570 KiB  
Article
Rational-Based Discovery of Novel β-Carboline Derivatives as Potential Antimalarials: From In Silico Identification of Novel Targets to Inhibition of Experimental Cerebral Malaria
by Fernanda de Moura Alves, Jessica Correa Bezerra Bellei, Camila de Souza Barbosa, Caíque Lopes Duarte, Amanda Luisa da Fonseca, Ana Claudia de Souza Pinto, Felipe Oliveira Raimundo, Bárbara Albuquerque Carpinter, Ari Sérgio de Oliveira Lemos, Elaine Soares Coimbra, Alex Gutterres Taranto, Vinícius Novaes Rocha, Fernando de Pilla Varotti, Gustavo Henrique Ribeiro Viana and Kézia K. G. Scopel
Pathogens 2022, 11(12), 1529; https://doi.org/10.3390/pathogens11121529 - 13 Dec 2022
Viewed by 1613
Abstract
Malaria is an infectious disease widespread in underdeveloped tropical regions. The most severe form of infection is caused by Plasmodium falciparum, which can lead to development of cerebral malaria (CM) and is responsible for deaths and significant neurocognitive sequelae throughout life. In [...] Read more.
Malaria is an infectious disease widespread in underdeveloped tropical regions. The most severe form of infection is caused by Plasmodium falciparum, which can lead to development of cerebral malaria (CM) and is responsible for deaths and significant neurocognitive sequelae throughout life. In this context and considering the emergence and spread of drug-resistant P. falciparum isolates, the search for new antimalarial candidates becomes urgent. β-carbolines alkaloids are good candidates since a wide range of biological activity for these compounds has been reported. Herein, we designed 20 chemical entities and performed an in silico virtual screening against a pool of P. falciparum molecular targets, the Brazilian Malaria Molecular Targets (BRAMMT). Seven structures showed potential to interact with PfFNR, PfPK7, PfGrx1, and PfATP6, being synthesized and evaluated for in vitro antiplasmodial activity. Among them, compounds 3–6 and 10 inhibited the growth of the W2 strain at µM concentrations, with low cytotoxicity against the human cell line. In silico physicochemical and pharmacokinetic properties were found to be favorable for oral administration. The compound 10 provided the best results against CM, with important values of parasite growth inhibition on the 5th day post-infection for both curative (67.9%) and suppressive (82%) assays. Furthermore, this compound was able to elongate mice survival and protect them against the development of the experimental model of CM (>65%). Compound 10 also induced reduction of the NO level, possibly by interaction with iNOS. Therefore, this alkaloid showed promising activity for the treatment of malaria and was able to prevent the development of experimental cerebral malaria (ECM), probably by reducing NO synthesis. Full article
(This article belongs to the Special Issue Emerging Treatment Options to Fight Malaria: New Compounds and Drug Combinations)
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