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Antibiotics
Special Issues
Novel Antiprotozoal Drug Formulations and Treatments
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Novel Antiprotozoal Drug Formulations and Treatments

A special issue of Antibiotics (ISSN 2079-6382).

Deadline for manuscript submissions: closed (30 April 2023) | Viewed by 10504

Special Issue Editors

Dr. Željko Petrovski

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Guest Editor
LAQV-REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia da Universidade Nova de Lisboa, 2829-516 Caparica, Portugal
Interests: sustainable chemistry; ionic liquids; drug delivery
Special Issues, Collections and Topics in MDPI journals
Dr. Luis Cobra Branco

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Guest Editor
Departamento de Química, LAQV-REQUIMTE, Faculdade de Ciências e Tecnologia, Universidade NOVA de Lisboa, 2825-149 Caparica, Portugal
Interests: sustainable chemistry; ionic liquids; catalysis; material science; responsive materials; energy; pharmaceuticals
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Protozoan parasites such as Plasmodium spp., Trypanosoma spp. and Leishmania spp. are responsible for diseases that cause significant mortality, morbidity and economic burden, predominantly in developing countries. The life-threatening diseases they provoke, including leishmaniasis, malaria, Chagas disease and human African trypanosomiasis (HAT), are considered some of the most challenging infectious diseases due to their limited therapeutic options and high mortality rates. There are currently no effective vaccines against these diseases, and new antiprotozoals are urgently required as most existing drugs suffer from poor efficacy, drug resistance, toxicity, high costs, poor stability and solubility as well as other pharmacokinetic properties. Therefore, the treatment of malaria, human African trypanosomiasis (HAT), Chagas disease and leishmaniasis relies heavily on new drug discovery and the development of novel effective, safe and inexpensive antiprotozoal treatments. Consequently, studies on the synthesis and evaluation of new drugs with increased antiprotozoal efficiency (fewer drawbacks, better bioavailability and less long-term toxicity), mechanisms of action, drug delivery and formulation, combination and therapy delivery remain crucial for the development of new antiprotozoal treatments. Given this context, this Special Issue aims to gather review papers and original research articles dealing with the potential antiprotozoal activities of novel drug candidates, modes of action and drug formulations. We welcome contributions on the following topics: synthesis and evaluation of the antiprotozoal activity of new compounds; the preparation and evaluation of drug formulations; combination therapy of antiprotozoal drugs and other substances; in vitro and in vivo evaluation; mechanisms of action; and drug resistance.

Dr. Željko Petrovski
Dr. Luis Cobra Branco
Guest Editors

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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. Antibiotics 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 2900 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

  • antiprotozoal activity and treatment
  • drug formulations
  • mechanism of action and resistance to antiprotozoal drugs
  • combination therapy
  • malaria
  • human African trypanosomiasis (HAT)
  • Chagas disease
  • leishmaniasis

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Published Papers (4 papers)

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Research

15 pages, 1878 KiB  
Article
Evaluation of the Anti-Toxoplasma gondii Efficacy, Cytotoxicity, and GC/MS Profile of Pleopeltis crassinervata Active Subfractions
by Jhony Anacleto-Santos, Fernando Calzada, Perla Yolanda López-Camacho, Teresa de Jesús López-Pérez, Elba Carrasco-Ramírez, Brenda Casarrubias-Tabarez, Teresa I. Fortoul, Marcela Rojas-Lemus, Nelly López-Valdés and Norma Rivera-Fernández
Antibiotics 2023, 12(5), 889; https://doi.org/10.3390/antibiotics12050889 - 10 May 2023
Cited by 1 | Viewed by 2383
Abstract
Pleopeltis crassinervata (Pc) is a fern that, according to ethnobotanical records, is used in Mexican traditional medicine to treat gastrointestinal ailments. Recent reports indicate that the hexane fraction (Hf) obtained from Pc methanolic frond extract affects Toxoplasma gondii tachyzoite viability in vitro; therefore, [...] Read more.
Pleopeltis crassinervata (Pc) is a fern that, according to ethnobotanical records, is used in Mexican traditional medicine to treat gastrointestinal ailments. Recent reports indicate that the hexane fraction (Hf) obtained from Pc methanolic frond extract affects Toxoplasma gondii tachyzoite viability in vitro; therefore, in the present study, the activity of different Pc hexane subfractions (Hsf) obtained by chromatographic methods was evaluated in the same biological model. Gas chromatography/mass spectrometry (GC/MS) analysis was carried out for hexane subfraction number one (Hsf1), as it showed the highest anti-Toxoplasma activity with a half-maximal inhibitory concentration (IC50) of 23.6 µg/mL, a 50% cytotoxic concentration (CC50) of 398.7 µg/mL in Vero cells, and a selective index (SI) of 16.89. Eighteen compounds were identified by Hsf1 GC/MS analysis, with the majority being fatty acids and terpenes. Hexadecanoic acid, methyl ester was the most commonly found compound (18.05%) followed by olean-13(18)-ene, 2,2,4a,8a,9,12b,14a-octamethyl-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,12,12a,12b,13,14,14a,14b-eicosahydropicene, and 8-octadecenoid acid, methyl ester, which were detected at 16.19%, 12.53%, and 12.99%, respectively. Based on the mechanisms of action reported for these molecules, Hsf1 could exert its anti-Toxoplasma activity mainly on T. gondii lipidomes and membranes. Full article
(This article belongs to the Special Issue Novel Antiprotozoal Drug Formulations and Treatments)
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12 pages, 1536 KiB  
Communication
Phytochemical Screening, GC-MS Analysis, and Evaluating In Vivo Antitrypanosomal Effects of a Methanolic Extract of Garcinia kola Nuts on Rats
by Fatihu Ahmad Rufa’i, Daniel Baecker and Muhammad Dauda Mukhtar
Antibiotics 2023, 12(4), 713; https://doi.org/10.3390/antibiotics12040713 - 6 Apr 2023
Cited by 6 | Viewed by 2209
Abstract
Trypanosomiasis is a serious disease that affects both humans and animals, causing social and economic losses. Efforts to find new therapeutic approaches are warranted to improve treatment options. Therefore, the purpose of this communication includes the phytochemical screening of a methanolic extract of [...] Read more.
Trypanosomiasis is a serious disease that affects both humans and animals, causing social and economic losses. Efforts to find new therapeutic approaches are warranted to improve treatment options. Therefore, the purpose of this communication includes the phytochemical screening of a methanolic extract of Garcinia kola nuts and the in vivo evaluation of its biological activity against rats infected with Trypanosoma brucei brucei and treated with 4 different concentrations of the extract (0.01, 0.1, 1, and 10 mg/kg). Treatment with suramin served as a positive control, while the negative control received no drug. Since the general toxicity of the extract could be ruled out, efficacy was evaluated based on physiological changes, such as induction of trypanosome parasitemia, influence on body temperature, and body weight. Survival was assessed during this study. Physical parameters, behavioral characteristics, and various hematological indices were also monitored. Based on the (patho)physiological and behavioral parameters (e.g., no parasitemia, no increase in body temperature, an increase in body weight, no loss of condition, no alopecia, and no gangrene), the efficacy of the extract was evident, which was also confirmed by 100% survival, while in the negative control, all rats died during the observation period. Since overall very similar results were obtained as a result of treatment with the established suramin, the in vivo antitrypanosomal activity of a methanolic extract of G. kola nuts on rats can be demonstrated in this communication. This opens the way, for example, for further development of drug formulations based on this methanolic extract. Full article
(This article belongs to the Special Issue Novel Antiprotozoal Drug Formulations and Treatments)
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12 pages, 1261 KiB  
Article
Synthesis and Biological Evaluation of Amphotericin B Formulations Based on Organic Salts and Ionic Liquids against Leishmania infantum
by Ricardo Ferraz, Nuno Santarém, Andreia F. M. Santos, Manuel L. Jacinto, Anabela Cordeiro-da-Silva, Cristina Prudêncio, João Paulo Noronha, Luis C. Branco and Željko Petrovski
Antibiotics 2022, 11(12), 1841; https://doi.org/10.3390/antibiotics11121841 - 19 Dec 2022
Cited by 3 | Viewed by 2604
Abstract
Nowadays, organic salts and ionic liquids (OSILs) containing active pharmaceutical ingredients (APIs) are being explored as drug delivery systems in modern therapies (OSILs-API). In that sense, this work is focused on the development of novel OSILs-API based on amphotericin B through an innovative [...] Read more.
Nowadays, organic salts and ionic liquids (OSILs) containing active pharmaceutical ingredients (APIs) are being explored as drug delivery systems in modern therapies (OSILs-API). In that sense, this work is focused on the development of novel OSILs-API based on amphotericin B through an innovative procedure and the evaluation of the respective biological activity against Leishmania infantum. Several ammonium, methylimidazolium, pyridinium and phosphonium organic cations combined with amphotericin B as anion were synthesized in moderate to high yields and high purities by the water-reduced buffer neutralization method. All prepared compounds were characterized to confirm the desired chemical structure and the specific optical rotation ([α]D25) was also determined. The biological assays performed on L. infantum promastigotes showed increased activity against this parasitic disease when compared with the starting chloride forms and amphotericin B alone, highlighting [P6,6,6,14][AmB] as the most promising formulation. Possible synergism in the antiprotozoal activity was also evaluated for [P6,6,6,14][AmB], since it was proven to be the compound with the highest toxicity. This work reported a simple synthetic method, which can be applied to prepare other organic salts based on molecules containing fragile chemical groups, demonstrating the potential of these OSILs-AmB as possible agents against leishmaniasis. Full article
(This article belongs to the Special Issue Novel Antiprotozoal Drug Formulations and Treatments)
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23 pages, 7005 KiB  
Article
Antileishmanial Activity of 4,8-Dimethoxynaphthalenyl Chalcones on Leishmania amazonensis
by Kaio Maciel de Santiago-Silva, Bruna Taciane da Silva Bortoleti, Laudicéa do Nascimento Oliveira, Fernanda Lima de Azevedo Maia, Joyce Cristina Castro, Ivete Conchon Costa, Danielle Bidóia Lazarin, James L. Wardell, Solange M. S. V. Wardell, Magaly Girão Albuquerque, Camilo Henrique da Silva Lima, Wander Rogério Pavanelli, Marcelle de Lima Ferreira Bispo and Raoni Schroeder B. Gonçalves
Antibiotics 2022, 11(10), 1402; https://doi.org/10.3390/antibiotics11101402 - 13 Oct 2022
Cited by 8 | Viewed by 2340
Abstract
Leishmaniasis is a neglected tropical disease caused by Leishmania species. Available therapeutic options have several limitations. The drive to develop new, more potent, and selective antileishmanial agents is thus a major goal. Herein we report the synthesis and the biological activity evaluation against [...] Read more.
Leishmaniasis is a neglected tropical disease caused by Leishmania species. Available therapeutic options have several limitations. The drive to develop new, more potent, and selective antileishmanial agents is thus a major goal. Herein we report the synthesis and the biological activity evaluation against promastigote and amastigote forms of Leishmania amazonensis of nine 4,8-dimethoxynaphthalenyl chalcones. Compound ((E)-1-(4,8-dimethoxynaphthalen-1-yl)-3-(4-nitrophenyl)prop-2-en-1-one), 4f, was the most promising with an IC50 = 3.3 ± 0.34 μM (promastigotes), a low cytotoxicity profile (CC50 = 372.9 ± 0.04 μM), and a high selectivity index (SI = 112.6). Furthermore, 4f induced several morphological and ultrastructural changes in the free promastigote forms, loss of plasma membrane integrity, and increased reactive oxygen species (ROS). An in silico analysis of drug-likeness and ADME parameters suggested high oral bioavailability and intestinal absorption. Compound 4f reduced the number of infected macrophages and the number of amastigotes per macrophage, with an IC50 value of 18.5 ± 1.19 μM. Molecular docking studies with targets, ARG and TR, showed that compound 4f had more hydrogen bond interactions with the ARG enzyme, indicating a more stable protein-ligand binding. These results suggest that 4,8-dimethoxynaphthalenyl chalcones are worthy of further study as potential antileishmanial drugs. Full article
(This article belongs to the Special Issue Novel Antiprotozoal Drug Formulations and Treatments)
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