Special Issue "Antiprotozoal Activity of Natural Products"

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Plant-Derived Antibiotics".

Deadline for manuscript submissions: 31 October 2021.

Special Issue Editors

Prof. Dr. Riccardo Petrelli
E-Mail Website
Guest Editor
School of Pharmacy, University of Camerino, 62032 Camerino, Italy
Interests: medicinal chemistry; small-molecules; essential oils; naturally-occurring compounds, NAD-dependent enzymes; plant secondary metabolites; bioactive-active fractionation, phytochemicals; ethnopharmacology; biological activity of natural compounds
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Special Issue Information

Dear Colleagues,

Neglected tropical diseases (NTDs), caused by protozoan parasites, are the leading cause of morbidity and mortality among the world’s low-income populations. They affect more than 1 billion people worldwide, causing around 500000 deaths each year and social discrimination and physical suffering. Of the 17 major NTDs, the life-threatening diseases Leishmaniasis, Malaria, Chagas disease, and human African Trypanosomiasis (HAT) are considered the most challenging due to their limited therapeutic options and high mortality rates. The absence of eagerly desired vaccines and the availability of limited chemotherapeutics, some with reduced efficacy and considerable drawbacks, hinder the efficient treatment of these diseases. Therefore, the discovery and development of novel effective, safe, and inexpensive antiprotozoal agents remain an urgent need. In this scenario, natural products can play an important role as potential lead compounds as they might have advantages over conventional chemical-based drugs (e.g., fewer drawbacks, better bioavailability, and less long-term toxicity). On this basis, this Special Issue is designed to gather review papers and original articles dealing with the potential antiprotozoal activities of plant secondary metabolites, including different classes such as terpenoids, alkaloids and phenolics. The Special Issue welcomes contributions on the following topics:

  • Phytochemical analysis and biological evaluation (in vitro and/or in vivo studies) of plant extracts/essential oils and isolated compounds.
  • Mode of action studies of natural products.
  • Structure-activity relationships studies including hemi-synthesized molecules.
  • Synergistic and antagonistic studies of mixtures of natural products
  • Development of new anti-protozoal agent formulations

Prof. Dr. Filippo Maggi
Prof. Dr.  Riccardo Petrelli
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 papers will be 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. 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 1800 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

  • Botanicals
  • Secondary metabolites
  • Isolation
  • Structural elucidation
  • Anti-protozoal activity

Published Papers (2 papers)

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Research

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Article
Antiprotozoal Nor-Triterpene Alkaloids from Buxus sempervirens L.
Antibiotics 2021, 10(6), 696; https://doi.org/10.3390/antibiotics10060696 - 10 Jun 2021
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Abstract
Malaria and human African trypanosomiasis (HAT; sleeping sickness) are life-threatening tropical diseases caused by protozoan parasites. Due to limited therapeutic options, there is a compelling need for new antiprotozoal agents. In a previous study, O-tigloylcyclovirobuxeine-B was recovered from a B. sempervirens L. [...] Read more.
Malaria and human African trypanosomiasis (HAT; sleeping sickness) are life-threatening tropical diseases caused by protozoan parasites. Due to limited therapeutic options, there is a compelling need for new antiprotozoal agents. In a previous study, O-tigloylcyclovirobuxeine-B was recovered from a B. sempervirens L. (common box; Buxaceae) leaf extract by bioactivity-guided isolation. This nor-cycloartane alkaloid was identified as possessing strong and selective in vitro activity against the causative agent of malaria tropica, Plasmodium falciparum (Pf). The purpose of this study is the isolation of additional alkaloids from B. sempervirens L. to search for further related compounds with strong antiprotozoal activity. In conclusion, 25 alkaloids were obtained from B. sempervirens L., including eight new natural products and one compound first described for this plant. The structure elucidation was accomplished by UHPLC/+ESI-QqTOF-MS/MS and NMR spectroscopy. The isolated alkaloids were tested against Pf and Trypanosoma brucei rhodesiense (Tbr), the causative agent of East African sleeping sickness. To assess their selectivity, cytotoxicity against mammalian cells (L6 cell line) was tested as well. Several of the compounds displayed promising in vitro activity against the pathogens in a sub-micromolar range with concurrent high selectivity indices (SI). Consequently, various alkaloids from B. sempervirens L. have the potential to serve as a novel antiprotozoal lead structure. Full article
(This article belongs to the Special Issue Antiprotozoal Activity of Natural Products)
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Review

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Review
Next-Generation Human Liver Models for Antimalarial Drug Assays
Antibiotics 2021, 10(6), 642; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics10060642 - 27 May 2021
Viewed by 816
Abstract
Advances in malaria prevention and treatment have significantly reduced the related morbidity and mortality worldwide, however, malaria continues to be a major threat to global public health. Because Plasmodium parasites reside in the liver prior to the appearance of clinical manifestations caused by [...] Read more.
Advances in malaria prevention and treatment have significantly reduced the related morbidity and mortality worldwide, however, malaria continues to be a major threat to global public health. Because Plasmodium parasites reside in the liver prior to the appearance of clinical manifestations caused by intraerythrocytic development, the Plasmodium liver stage represents a vulnerable therapeutic target to prevent progression. Currently, a small number of drugs targeting liver-stage parasites are available, but all cause lethal side effects in glucose-6-phosphate dehydrogenase-deficient individuals, emphasizing the necessity for new drug development. Nevertheless, a longstanding hurdle to developing new drugs is the availability of appropriate in vitro cultures, the crucial conventional platform for evaluating the efficacy and toxicity of drugs in the preclinical phase. Most current cell culture systems rely primarily on growing immortalized or cancerous cells in the form of a two-dimensional monolayer, which is not very physiologically relevant to the complex cellular architecture of the human body. Although primary human cells are more relevant to human physiology, they are mainly hindered by batch-to-batch variation, limited supplies, and ethical issues. Advances in stem cell technologies and multidimensional culture have allowed the modelling of human infectious diseases. Here, current in vitro hepatic models and toolboxes for assaying the antimalarial drug activity are summarized. Given the physiological potential of pluripotent and adult stem cells to model liver-stage malaria, the opportunities and challenges in drug development against liver-stage malaria is highlighted, paving the way to assess the efficacy of hepatic plasmodicidal activity. Full article
(This article belongs to the Special Issue Antiprotozoal Activity of Natural Products)
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