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A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (25 October 2023) | Viewed by 25112

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Special Issue Editor

Prof. Dr. Francisco Jaime Bezerra Mendonça Júnior

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Laboratory of Synthesis and Drug Delivery, State University of Paraíba, João Pessoa 58020-540, PB, Brazil
Interests: drug design; neglected diseases; antimicrobial; anti-cancer
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Dear Colleagues,

Protozoan diseases continue to be a serious worldwide health problem, causing serious social and economic impacts, especially in developing countries. Protozooses such as malaria, leishmaniasis, trypanosomiasis, toxoplasmosis, trichomoniasis, giardiasis and amoebiasis are responsible for high mortality and morbidity rates, with the potential to affect more than 1 billion people worldwide.

Globally, the endemicity of these diseases has increased due to several factors, including: low investment in research in the search for new drugs with novel mechanisms of action; lack of effective drugs with low adverse effects and low toxicity, as well as to the increase in drug resistance, the increasing appearance of cross resistance, which has made the few therapeutic options ineffective in many cases.

This problem has led many researchers to seek new antiprotozoal drugs, through different scientific approaches, based mainly on two axes: 1) isolation and identification of drug candidates through bioprospection of natural resources (plants, animals, microorganisms); 2) drug design based on the use of medicinal chemistry tools, involving synthetic chemistry procedures, associated or not with computational approaches (structure-based drug discovery and ligand-based drug discovery)

In this special Issue, authors are invited to submit review and original articles related to the recent research in drug design and discovery, synthesis, and pharmacological properties (in vitro and in vivo) of natural products and/or synthetic compounds that have the potential to become drug candidates for protozoan diseases. As well as presenting the latest advances in the search for pharmacological targets for protozoan diseases, with the aim to provide researchers with the most up-to-date information in this field.

Potential topics include but are not limited to:

Bioprospecting of natural products;
Drug Design & Discovery;
Synthesis;
Computational methods (ADMET, CADD, LBDD, SBDD, QSAR, VS);
In vitro, and in vivo evaluations;
Recent advances in antiprotozoal drugs;

Prof. Dr. Francisco Jaime Bezerra Mendonça Júnior
Guest Editor

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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. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

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Keywords

antiprotozoal agents
drug discovery
medicinal chemistry
natural products
in vitro and in vivo studies
ADMET
computer-aided drug design
chemoinformatics
molecular docking
virtual screening

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Drug Discovery of Antiprotozoal Agents 2024 in Pharmaceuticals (1 article)

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Editorial

Jump to: Research, Review

4 pages, 173 KiB

Open AccessEditorial

Special Issue “Drug Discovery of Antiprotozoal Agents”

by Francisco Jaime Bezerra Mendonça-Junior

Pharmaceuticals 2024, 17(2), 176; https://doi.org/10.3390/ph17020176 - 30 Jan 2024

Viewed by 1082

Abstract

Protozoal diseases, such as leishmaniasis, malaria, African sleeping sickness, Chagas disease, amoebiasis, giardiasis, cryptococcosis, and toxoplasmosis (among others), affect and/or have the potential to infect more than one billion people worldwide [...] Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

Research

Jump to: Editorial, Review

16 pages, 1331 KiB

Open AccessArticle

Eugenol-Rich Essential Oil from Pimenta dioica: In Vitro and In Vivo Potentialities against Leishmania amazonensis

by Lianet Monzote, Laura Machín, Adiel González, Ramón Scull, Yamilet I. Gutiérrez, Prabodh Satyal, Lars Gille and William N. Setzer

Pharmaceuticals 2024, 17(1), 64; https://doi.org/10.3390/ph17010064 - 29 Dec 2023

Cited by 2 | Viewed by 1553

Abstract

Pimenta dioica L. is one the most recognized species with diverse biological activities. In this study, in vitro activity and in vivo efficacy of essential oil from P. dioica (EO-Pd) was evaluated. The main compound was also included in the animal studies and its in silico prediction related to biological activities, molecular ligands, drug likeness, and ADME (absorption, distribution, metabolism, and excretion) properties are listed. The chemical composition analyzed by GC-MS retrieved 45 components, which the most abundant compound was the eugenol (80.1%). The EO-Pd was able to inhibit the growth of L. amazonensis (IC₅₀ = 9.7 ± 0.7 and 11.3 ± 2.1 µg/mL, promastigotes and amastigotes, respectively). The cytotoxicity assay showed a CC₅₀ of 104.5 ± 0.9 µg/mL and a selectivity index of 9. In the model of cutaneous leishmaniasis in BALB/c mice, the effect of EO-Pd and eugenol was observed after treatment at 30 mg/kg by intralesional route with 5 administrations every 4 days. In the in silico predictions, some targets that justified the antileishmanial activity of eugenol and good drug like properties for this compound, were obtained. This study showed for first time the potential of EO-Pd to inhibit L. amazonensis, which could be linked to the activity of major compound eugenol. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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15 pages, 2170 KiB

Open AccessArticle

Immunomodulatory, Antioxidant, and Anti-Inflammatory Activities of Green Synthesized Copper Nanoparticles for Treatment of Chronic Toxoplasma gondii Infection

by Abdullah D. Alanazi and Sultan F. Alnomasy

Pharmaceuticals 2023, 16(11), 1574; https://doi.org/10.3390/ph16111574 - 7 Nov 2023

Cited by 5 | Viewed by 1357

Abstract

Background: Nowadays, interest in the use of nanotechnology for medical purposes is increasing. The current experimental investigation is planned for the green synthesis, characterization, and efficacy of copper nanoparticles (CLN) against chronic Toxoplasma gondii infection. Methods: Green synthesis of CNP was performed using the Lupinus arcticus extract via the precipitation method. The effects of CNP on tachyzoites, infectivity rate, parasites inside THP-1 cells, nitric oxide (NO) triggering, iNOS, and IFN-γ expression genes were evaluated. Following toxoplasmosis in BALB/c mice via the T. gondii ME49 strain, mice received CNP at 5 and 10 mg/kg/day alone and combined with pyrimethamine (PYM) at 5 mg/kg for two weeks. CNP’s in vivo effects were evaluated by analyzing the load and size of cysts, oxidant/antioxidant enzymes, and bradyzoite surface antigen 1 (BAG1) expression gene levels. Results: CNP displayed a circular shape ranging from 10 to 85 nm. The IC50 value of CNP and PYM against tachyzoites was 37.2 and 25.7 µg/mL, respectively, whereas the CC50 value of CNP and pyrimethamine against THP-1 cells was 491.4 μg/mL and 269.5 μg/mL, respectively. The rate of infectivity and parasite load among THP-1 cells exposed to CNP was obviously reduced (p < 0.05). CNP at the doses of 5 and 10 mg/kg predominantly along with PYM evidently (p < 0.05) reduced the number and size of the T. gondii cysts in the infected mice. The levels of NO, iNOS, and IFN-γ genes were remarkably (p < 0.001) boosted compared with the cells without treatment. CNP at the doses of 10 and 20 mg/kg drastically (p < 0.05) reduced the oxidative stress markers in the infected mice, whereas CNP significantly elevated the level of antioxidant factors. CNP also revealed no toxicity in the liver and kidney at the tested doses in healthy mice. Conclusions: Our experimental study reported the beneficial effects of CNP principally along with existing chemical drugs against latent toxoplasmosis in mice, whereas the possible action mechanisms of CNP are controlling oxidative stress, refining antioxidant enzymes, and increasing the production of immunomodulatory cytokines with no toxicity to the function of vital organs. But, additional trials are required to confirm these results, as well as to clarify the accurate mechanisms and their toxicity. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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17 pages, 6268 KiB

Open AccessArticle

Repurposing Terfenadine as a Novel Antigiardial Compound

by Daniel Osmar Suárez-Rico, Francisco Javier Munguía-Huizar, Rafael Cortés-Zárate, José Manuel Hernández-Hernández, Sirenia González-Pozos, Armando Perez-Rangel and Araceli Castillo-Romero

Pharmaceuticals 2023, 16(9), 1332; https://doi.org/10.3390/ph16091332 - 21 Sep 2023

Viewed by 1527

Abstract

Giardia lamblia is a highly infectious protozoan that causes giardiasis, a gastrointestinal disease with short-term and long-lasting symptoms. The currently available drugs for giardiasis treatment have limitations such as side effects and drug resistance, requiring the search for new antigiardial compounds. Drug repurposing has emerged as a promising strategy to expedite the drug development process. In this study, we evaluated the cytotoxic effect of terfenadine on Giardia lamblia trophozoites. Our results showed that terfenadine inhibited the growth and cell viability of Giardia trophozoites in a time–dose-dependent manner. In addition, using scanning electron microscopy, we identified morphological damage; interestingly, an increased number of protrusions on membranes and tubulin dysregulation with concomitant dysregulation of Giardia GiK were observed. Importantly, terfenadine showed low toxicity for Caco-2 cells, a human intestinal cell line. These findings highlight the potential of terfenadine as a repurposed drug for the treatment of giardiasis and warrant further investigation to elucidate its precise mechanism of action and evaluate its efficacy in future research. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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10 pages, 1528 KiB

Open AccessArticle

Design and Synthesis of New Anthranyl Phenylhydrazides: Antileishmanial Activity and Structure–Activity Relationship

by Claudia do Carmo Maquiaveli, Edson Roberto da Silva, Barbara Hild de Jesus, Caio Eduardo Oliveira Monteiro, Tiago Rodrigues Navarro, Luiz Octavio Pereira Branco, Isabela Souza dos Santos, Nanashara Figueiredo Reis, Arieli Bernardo Portugal, João Luiz Mendes Wanderley, André Borges Farias, Nelilma Correia Romeiro and Evanoel Crizanto de Lima

Pharmaceuticals 2023, 16(8), 1120; https://doi.org/10.3390/ph16081120 - 9 Aug 2023

Viewed by 1506

Abstract

Leishmaniasis is a neglected tropical disease affecting millions of people worldwide. A centenary approach to antimonial-based drugs was first initiated with the synthesis of urea stibamine by Upendranath Brahmachari in 1922. The need for new drug development led to resistance toward antimoniates. New drug development to treat leishmaniasis is urgently needed. In this way, searching for new substances with antileishmanial activity, we synthesized ten anthranyl phenylhydrazide and three quinazolinone derivatives and evaluated them against promastigotes and the intracellular amastigotes of Leishmania amazonensis. Three compounds showed good activity against promastigotes 1b, 1d, and 1g, with IC₅₀ between 1 and 5 μM. These new phenylhydrazides were tested against Leishmania arginase, but they all failed to inhibit this parasite enzyme, as we have shown in a previous study. To explain the possible mechanism of action, we proposed the enzyme PTR1 as a new target for these compounds based on in silico analysis. In conclusion, the new anthranyl hydrazide derivatives can be a promising scaffold for developing new substances against the protozoa parasite. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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19 pages, 4309 KiB

Open AccessArticle

Riluzole, a Derivative of Benzothiazole as a Potential Anti-Amoebic Agent against Entamoeba histolytica

by Maritza Velásquez-Torres, José Guadalupe Trujillo-Ferrara, Marycarmen Godínez-Victoria, Rosa Adriana Jarillo-Luna, Víctor Tsutsumi, Virginia Sánchez-Monroy, Araceli Posadas-Mondragón, Roberto Issac Cuevas-Hernández, José Angel Santiago-Cruz and Judith Pacheco-Yépez

Pharmaceuticals 2023, 16(6), 896; https://doi.org/10.3390/ph16060896 - 19 Jun 2023

Cited by 5 | Viewed by 2154

Abstract

Amoebiasis is produced by the parasite Entamoeba histolytica; this disease affects millions of people throughout the world who may suffer from amoebic colitis or amoebic liver abscess. Metronidazole is used to treat this protozoan, but it causes important adverse effects that limit its use. Studies have shown that riluzole has demonstrated activity against some parasites. Thus, the present study aimed, for the first time, to demonstrate the in vitro and in silico anti-amoebic activity of riluzole. In vitro, the results of Entamoeba histolytica trophozoites treated with IC₅₀ (319.5 μM) of riluzole for 5 h showed (i) a decrease of 48.1% in amoeba viability, (ii) ultrastructural changes such as a loss of plasma membrane continuity and alterations in the nuclei followed by lysis, (iii) apoptosis-like cell death, (iv) the triggering of the production of reactive oxygen species and nitric oxide, and (v) the downregulation of amoebic antioxidant enzyme gene expression. Interestingly, docking studies have indicated that riluzole presented a higher affinity than metronidazole for the antioxidant enzymes thioredoxin, thioredoxin reductase, rubrerythrin, and peroxiredoxin of Entamoeba histolytica, which are considered as possible candidates of molecular targets. Our results suggest that riluzole could be an alternative treatment against Entamoeba histolytica. Future studies should be conducted to analyze the in vivo riluzole anti-amoebic effect on the resolution of amebic liver abscess in a susceptible model, as this will contribute to developing new therapeutic agents with anti-amoebic activity. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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15 pages, 12226 KiB

Open AccessArticle

Annona muricata Leaf as an Anti-Cryptosporidial Agent: An In Silico Molecular Docking Analysis and In Vivo Studies

by Eman S. El-Wakil, Hagar F. Abdelmaksoud, Majed H. Wakid, Muslimah N. Alsulami, Olfat Hammam, Haleema H. Albohiri and Marwa M. I. Ghallab

Pharmaceuticals 2023, 16(6), 878; https://doi.org/10.3390/ph16060878 - 14 Jun 2023

Cited by 3 | Viewed by 1732

Abstract

Cryptosporidiosis is a serious parasitic diarrheal disease linked to the occurrence of colorectal cancer in immunocompromised patients. The FDA-approved drug nitazoxanide (NTZ) achieved a temporary effect, and relapses occur. Annona muricata leaf is widely used in traditional medicine to treat a wide range of disorders, including antiparasitic and anticancer effects. So, this study aimed to investigate Annona muricata leaf antiparasitic and anticancer properties compared to NTZ in Cryptosporidium parvum (C. parvum) acutely and chronically infected immunosuppressed mice. A molecular docking analysis was performed to evaluate the effectiveness of some biologically active compounds that represented the pharmacological properties of Annona muricata leaf-rich extract toward C. parvum lactate dehydrogenase compared to NTZ. For the in vivo study, eighty immunosuppressed albino mice were classified into four groups as follows: group I: infected and treated with A. muricata; group II: infected and treated with nitazoxanide; group III: infected and received no treatment; and group IV: were neither infected nor treated. Furthermore, half of the mice in groups I and II received the drugs on the 10th day post-infection (dpi), and the other half received treatment on the 90th day post-infection. Parasitological, histopathological, and immunohistochemical evaluations were performed. The docking analysis showed that the lowest estimated free energy of binding of annonacin, casuarine, L-epigallocatechin, P-coumaric acid, and ellagic acid toward C. parvum LDH, were −6.11, −6.32, −7.51, −7.81, and −9.64 kcal/mol, respectively, while NTZ was −7.03 kcal/mol. Parasitological examination displayed a significantly high difference in C. parvum oocyst mean counts in groups I and II compared to group III (p-value < 0.001), with group I demonstrating the highest efficacy. The analyses of histopathological and immunohistochemical results revealed that group I showed restoration of the normal villous pattern without evidence of dysplasia or malignancy. A. muricata leaf has proved to be a reliable agent for Cryptosporidium treatment. This paper argues for its promising use as an antiparasitic agent and for the prevention of neoplastic sequels of Cryptosporidium infection. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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14 pages, 3272 KiB

Open AccessArticle

Nitazoxanide: A Drug Repositioning Compound with Potential Use in Chagas Disease in a Murine Model

by Minerva Arce-Fonseca, Rodolfo Andrés Gutiérrez-Ocejo, José Luis Rosales-Encina, Alberto Aranda-Fraustro, Juan José Cabrera-Mata and Olivia Rodríguez-Morales

Pharmaceuticals 2023, 16(6), 826; https://doi.org/10.3390/ph16060826 - 1 Jun 2023

Cited by 2 | Viewed by 1962

Abstract

Chagas disease (ChD), caused by Trypanosoma cruzi, is the most serious parasitosis in the western hemisphere. Benznidazole and nifurtimox, the only two trypanocidal drugs, are expensive, difficult to obtain, and have severe side effects. Nitazoxanide has shown to be effective against protozoa, bacteria, and viruses. This study aimed to evaluate the nitazoxanide efficacy against the Mexican T. cruzi Ninoa strain in mice. Infected animals were orally treated for 30 days with nitazoxanide (100 mg/kg) or benznidazole (10 mg/kg). The clinical, immunological, and histopathological conditions of the mice were evaluated. Nitazoxanide- or benznidazole-treated mice had longer survival and less parasitemia than those without treatment. Antibody production in the nitazoxanide-treated mice was of the IgG1-type and not of the IgG2-type as in the benznidazole-treated mice. Nitazoxanide-treated mice had significantly high IFN-γ levels compared to the other infected groups. Serious histological damage could be prevented with nitazoxanide treatment compared to without treatment. In conclusion, nitazoxanide decreased parasitemia levels, indirectly induced the production of IgG antibodies, and partially prevented histopathological damage; however, it did not show therapeutic superiority compared to benznidazole in any of the evaluated aspects. Therefore, the repositioning of nitazoxanide as an alternative treatment against ChD could be considered, since it did not trigger adverse effects that worsened the pathological condition of the infected mice. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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16 pages, 10757 KiB

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Virtual Screening of Benzimidazole Derivatives as Potential Triose Phosphate Isomerase Inhibitors with Biological Activity against Leishmania mexicana

by Lenci K. Vázquez-Jiménez, Alfredo Juárez-Saldivar, Manuel J. Chan-Bacab, Timoteo Delgado-Maldonado, Luis D. González-Morales, Isidro Palos, Eyra Ortiz-Pérez, Edgar E. Lara-Ramírez, Esther Ramírez-Moreno and Gildardo Rivera

Pharmaceuticals 2023, 16(3), 390; https://doi.org/10.3390/ph16030390 - 3 Mar 2023

Cited by 3 | Viewed by 2693

Abstract

Leishmania mexicana (L. mexicana) is a causal agent of cutaneous leishmaniasis (CL), a “Neglected disease”, for which the search for new drugs is a priority. Benzimidazole is a scaffold used to develop antiparasitic drugs; therefore, it is interesting molecule against L. mexicana. In this work, a ligand-based virtual screening (LBVS) of the ZINC15 database was performed. Subsequently, molecular docking was used to predict the compounds with potential binding at the dimer interface of triosephosphate isomerase (TIM) of L. mexicana (LmTIM). Compounds were selected on binding patterns, cost, and commercial availability for in vitro assays against L. mexicana blood promastigotes. The compounds were analyzed by molecular dynamics simulation on LmTIM and its homologous human TIM. Finally, the physicochemical and pharmacokinetic properties were determined in silico. A total of 175 molecules with docking scores between −10.8 and −9.0 Kcal/mol were obtained. Compound E2 showed the best leishmanicidal activity (IC₅₀ = 4.04 µM) with a value similar to the reference drug pentamidine (IC₅₀ = 2.23 µM). Molecular dynamics analysis predicted low affinity for human TIM. Furthermore, the pharmacokinetic and toxicological properties of the compounds were suitable for developing new leishmanicidal agents. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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25 pages, 4848 KiB

Open AccessArticle

ACW-02 an Acridine Triazolidine Derivative Presents Antileishmanial Activity Mediated by DNA Interaction and Immunomodulation

by Sonaly Lima Albino, Willian Charles da Silva Moura, Malu Maria Lucas dos Reis, Gleyton Leonel Silva Sousa, Pablo Rayff da Silva, Mayara Gabriele Carvalho de Oliveira, Tatiana Karla dos Santos Borges, Lucas Fraga Friaça Albuquerque, Sinara Mônica Vitalino de Almeida, Maria do Carmo Alves de Lima, Selma Aparecida Souza Kuckelhaus, Igor José dos Santos Nascimento, Francisco Jaime Bezerra Mendonca Junior, Teresinha Gonçalves da Silva and Ricardo Olímpio de Moura

Pharmaceuticals 2023, 16(2), 204; https://doi.org/10.3390/ph16020204 - 29 Jan 2023

Cited by 5 | Viewed by 2395

Abstract

The present study proposed the synthesis of a novel acridine derivative not yet described in the literature, chemical characterization by NMR, MS, and IR, followed by investigations of its antileishmanial potential. In vitro assays were performed to assess its antileishmanial activity against L. amazonensis strains and cytotoxicity against macrophages through MTT assay and annexin V-FITC/PI, and the ability to perform an immunomodulatory action using CBA. To investigate possible molecular targets, its interaction with DNA in vitro and in silico targets were evaluated. As results, the compound showed good antileishmanial activity, with IC₅₀ of 6.57 (amastigotes) and 94.97 (promastigotes) µg mL⁻¹, associated with non-cytotoxicity to macrophages (CC₅₀ > 256.00 µg mL⁻¹). When assessed by flow cytometry, 99.8% of macrophages remained viable. The compound induced an antileishmanial effect in infected macrophages and altered TNF-α, IL-10 and IL-6 expression, suggesting a slight immunomodulatory activity. DNA assay showed an interaction with the minor grooves due to the hyperchromic effect of 47.53% and Kb 1.17 × 10⁶ M⁻¹, and was sustained by docking studies. Molecular dynamics simulations and MM-PBSA calculations propose cysteine protease B as a possible target. Therefore, this study demonstrates that the new compound is a promising molecule and contributes as a model for future works. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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Review

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13 pages, 3476 KiB

Open AccessReview

Analysis of Giardia lamblia Nucleolus as Drug Target: A Review

by Carlos Gaona-López, Ana Verónica Martínez-Vázquez, Juan Carlos Villalobos-Rocha, Karina Janett Juárez-Rendón and Gildardo Rivera

Pharmaceuticals 2023, 16(8), 1168; https://doi.org/10.3390/ph16081168 - 16 Aug 2023

Cited by 2 | Viewed by 2741

Abstract

Giardia lamblia (G. lamblia) is the main causative agent of diarrhea worldwide, affecting children and adults alike; in the former, it can be lethal, and in the latter a strong cause of morbidity. Despite being considered a predominant disease in low-income and developing countries, current migratory flows have caused an increase in giardiasis cases in high-income countries. Currently, there is a wide variety of chemotherapeutic treatments to combat this parasitosis, most of which have potentially serious side effects, such as genotoxic, carcinogenic, and teratogenic. The necessity to create novel treatments and discover new therapeutic targets to fight against this illness is evident. The current review centers around the controversial nucleolus of G. lamblia, providing a historical perspective that traces its apparent absence to the present evidence supporting its existence as a subnuclear compartment in this organism. Additionally, possible examples of ncRNAs and proteins ubiquitous to the nucleolus that can be used as targets of different therapeutic strategies are discussed. Finally, some examples of drugs under research that could be effective against G. lamblia are described. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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39 pages, 6887 KiB

Open AccessReview

Advances in Protozoan Epigenetic Targets and Their Inhibitors for the Development of New Potential Drugs

by Carlos Gaona-López, Lenci K. Vazquez-Jimenez, Alonzo Gonzalez-Gonzalez, Timoteo Delgado-Maldonado, Eyrá Ortiz-Pérez, Benjamín Nogueda-Torres, Adriana Moreno-Rodríguez, Karina Vázquez, Emma Saavedra and Gildardo Rivera

Pharmaceuticals 2023, 16(4), 543; https://doi.org/10.3390/ph16040543 - 4 Apr 2023

Cited by 3 | Viewed by 2966

Abstract

Protozoan parasite diseases cause significant mortality and morbidity worldwide. Factors such as climate change, extreme poverty, migration, and a lack of life opportunities lead to the propagation of diseases classified as tropical or non-endemic. Although there are several drugs to combat parasitic diseases, strains resistant to routinely used drugs have been reported. In addition, many first-line drugs have adverse effects ranging from mild to severe, including potential carcinogenic effects. Therefore, new lead compounds are needed to combat these parasites. Although little has been studied regarding the epigenetic mechanisms in lower eukaryotes, it is believed that epigenetics plays an essential role in vital aspects of the organism, from controlling the life cycle to the expression of genes involved in pathogenicity. Therefore, using epigenetic targets to combat these parasites is foreseen as an area with great potential for development. This review summarizes the main known epigenetic mechanisms and their potential as therapeutics for a group of medically important protozoal parasites. Different epigenetic mechanisms are discussed, highlighting those that can be used for drug repositioning, such as histone post-translational modifications (HPTMs). Exclusive parasite targets are also emphasized, including the base J and DNA 6 mA. These two categories have the greatest potential for developing drugs to treat or eradicate these diseases. Full article

(This article belongs to the Special Issue Drug Discovery of Antiprotozoal Agents)

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