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Antibiotics
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Plant-Derived Natural Products in Antibacterial and Antifungal Drug Discovery
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Plant-Derived Natural Products in Antibacterial and Antifungal Drug Discovery

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

Deadline for manuscript submissions: closed (30 June 2023) | Viewed by 14579

Special Issue Editors

Prof. Dr. Jaime Ribeiro-Filho

E-Mail Website
Guest Editor
Oswaldo Cruz Foundation (FIOCRUZ), Eusébio, CE, Brazil
Interests: natural products; preclinical research; pharmacology; drug development; inflammatory diseases; antibiotic resistance; antifungals; ethnopharmacology; public health
Special Issues, Collections and Topics in MDPI journals
Dr. Juliana Moura Mendes Arrua

E-Mail Website
Guest Editor
Centro Multidisciplinario de Investigaciones Tecnológicas (CEMIT), Universidad Nacional de Asunción (UNA), San Lorenzo, Paraguay
Interests: antifungal; fungicide; antibacterial; antimicrobial; mycotoxins; aflatoxins; Aspergillus; medicinal plants; essential oil; food safety
Prof. Dr. Fillipe De Oliveira Pereira

E-Mail Website
Guest Editor
Education and Health Center, Federal University of Campina Grande, Cuité, Brazil
Interests: antifungals; natural products; spoilage fungi; pathogenic fungi; dermatophytes; virulence; resistance; biofilms

Special Issue Information

Dear Colleagues,

Antimicrobial resistance has become a global public health concern. As the number of multidrug-resistant bacterial and fungal strains has become increasingly higher, the effectiveness of conventional antibiotics has decreased significantly, impacting the proper treatment of various infectious diseases. Moreover, the discovery of new antimicrobials occurs slower than the rise of new MDR strains, which points to the need to search for urgent and effective alternatives to combat microbial resistance.

Ethnopharmacological studies have long described medical plants' use in treating infectious diseases, many of which are currently described as etiologically identified as bacterial and fungal diseases. In addition, consistent evidence has demonstrated that plant-derived natural products, including extracts, fractions, essential oils, and isolated secondary metabolites, have significant antimicrobial activity, in addition to inhibiting microbial virulence, and potentiate the action of antimicrobial drugs against resistant strains.

This Special Issue intends to gather manuscripts of all article types demonstrating the pharmacological effects and preferably mechanism of action of fully characterized plant-derived natural products with the potential to be used in antibacterial and antifungal drug discovery in the context of preclinical research, through in vivo, ex vivo in vitro, and in silico testing

Prof. Dr. Jaime Ribeiro-Filho
Dr. Juliana Moura Mendes Arrua
Prof. Dr. Fillipe De Oliveira Pereira
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. 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

  • plants
  • natural products
  • antibacterial
  • antifungal
  • antimicrobial resistance
  • drug discovery
  • preclinical research

Published Papers (5 papers)

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Research

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25 pages, 2122 KiB  
Article
Antifungal Activity of Guiera senegalensis: From the Chemical Composition to the Mitochondrial Toxic Effects and Tyrosinase Inhibition
by Rute Moreira, Federico Ferreres, Ángel Gil-Izquierdo, Nelson G. M. Gomes, Luísa Araújo, Eugénia Pinto, Paula B. Andrade and Romeu A. Videira
Antibiotics 2023, 12(5), 869; https://doi.org/10.3390/antibiotics12050869 - 08 May 2023
Cited by 1 | Viewed by 1593
Abstract
Pest resistance against fungicides is a widespread and increasing problem, with impact on crop production and public health, making the development of new fungicides an urgent need. Chemical analyses of a crude methanol extract (CME) of Guiera senegalensis leaves revealed the presence of [...] Read more.
Pest resistance against fungicides is a widespread and increasing problem, with impact on crop production and public health, making the development of new fungicides an urgent need. Chemical analyses of a crude methanol extract (CME) of Guiera senegalensis leaves revealed the presence of sugars, phospholipids, phytosterols, guieranone A, porphyrin-containing compounds, and phenolics. To connect chemical composition with biological effects, solid-phase extraction was used to discard water-soluble compounds with low affinity for the C18 matrix and obtain an ethyl acetate fraction (EAF) that concentrates guieranone A and chlorophylls, and a methanol fraction (MF) dominated by phenolics. While the CME and MF exhibited poor antifungal activity against Aspergillus fumigatus, Fusarium oxysporum and Colletotrichum gloeosporioides, the EAF demonstrated antifungal activity against these filamentous fungi, particularly against C. gloeosporioides. Studies with yeasts revealed that the EAF has strong effectiveness against Saccharomyces cerevisiae, Cryptococcus neoformans and Candida krusei with MICs of 8, 8 and 16 μg/mL, respectively. A combination of in vivo and in vitro studies shows that the EAF can function as a mitochondrial toxin, compromising complexes I and II activities, and as a strong inhibitor of fungal tyrosinase (Ki = 14.40 ± 4.49 µg/mL). Thus, EAF appears to be a promising candidate for the development of new multi-target fungicides. Full article
(This article belongs to the Special Issue Plant-Derived Natural Products in Antibacterial and Antifungal Drug Discovery)
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30 pages, 1900 KiB  
Article
Phytochemistry and Biological Activities of Essential Oils from Six Aromatic Medicinal Plants with Cosmetic Properties
by Atika Ailli, Nadia Handaq, Hanane Touijer, Aman Allah Gourich, Aziz Drioiche, Khalid Zibouh, Brahim Eddamsyry, Fadoua El Makhoukhi, Aicha Mouradi, Yousef A. Bin Jardan, Mohammed Bourhia, Abdelhakim Elomri and Touriya Zair
Antibiotics 2023, 12(4), 721; https://doi.org/10.3390/antibiotics12040721 - 07 Apr 2023
Cited by 7 | Viewed by 2804
Abstract
In this work, the chemical composition and antioxidant and antimicrobial activities of the essential oils (EOs) of six species—Laurus nobilis, Chamaemelum nobile, Citrus aurantium, Pistacia lentiscus, Cedrus atlantica, and Rosa damascena—have been studied. Phytochemical screening of [...] Read more.
In this work, the chemical composition and antioxidant and antimicrobial activities of the essential oils (EOs) of six species—Laurus nobilis, Chamaemelum nobile, Citrus aurantium, Pistacia lentiscus, Cedrus atlantica, and Rosa damascena—have been studied. Phytochemical screening of these plants revealed the presence of primary metabolites, namely, lipids, proteins, reducing sugars, and polysaccharides, and also secondary metabolites such as tannins, flavonoids, and mucilages. The essential oils were extracted by hydrodistillation in a Clevenger-type apparatus. The yields are between 0.06 and 4.78% (mL/100 g). The analysis of the chemical composition carried out by GC-MS showed the presence of 30 to 35 compounds and represent between 99.97% and 100% of the total composition of EOs, with a variation in the chemical composition detected at the level of the majority compounds between these species. Indeed, in the EO of Laurus nobilis, 1,8-cineole (36.58%) is the major component. In Chamaemelum nobile EO, the most abundant compound is angelylangelate (41.79%). The EO of Citrus aurantium is rich in linalool (29.01%). The EO of Pistacia lentiscus is dominated by 3-methylpentylangelate (27.83%). The main compound of Cedrus atlantica is β-himachalene (40.19%), while the EO of Rosa damascenaa flowers is rich in n-nonadecane (44.89%). The analysis of the similarity between the EOs of the plants studied by ACH and ACP showed that the chemical composition of the EOs makes it possible to separate these plants into three groups: the first represented by Chamaemelum nobile, because it is rich in oxygenated monoterpenes, the second defined Cedrus atlantica and Rosa damascena, which are rich in sesquiterpenes, and the third gathers Pistacia lentiscus, Laurus nobilis and Citrus aurantium, which are composed of oxygenated sesquiterpenes and monoterpenes (these three species are very close). The study of the antioxidant activity showed that all the EOs tested have a high capacity for scavenging free radicals from DPPH. The EOs of Laurus nobilis and Pistacia lentiscus showed the highest activity, 76.84% and 71.53%, respectively, followed by Cedrus atlantica EO (62.38%) and Chamaemelum nobile (47.98%) then Citrus aurantium EO (14.70%). Antimicrobial activity EO was tested against eight bacterial strains and eight fungal strains; the results showed that EOs exhibit significant bactericidal and fungicidal activities against all the microorganisms tested, of which the MICs of the bacterial strains start with 5 mg/mL, while the MICs of the fungal strains are between 0.60 mg/mL and 5 mg/mL. Thus, these EOs rich in antimicrobial and antioxidant components can serve as a natural alternative; this confirms their use as additives in cosmetics. Full article
(This article belongs to the Special Issue Plant-Derived Natural Products in Antibacterial and Antifungal Drug Discovery)
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11 pages, 2651 KiB  
Article
α-Pinene: Docking Study, Cytotoxicity, Mechanism of Action, and Anti-Biofilm Effect against Candida albicans
by Daniela Bomfim de Barros, Luanna de Oliveira e Lima, Larissa Alves da Silva, Mariana Cavalcante Fonseca, Rafael Carlos Ferreira, Hermes Diniz Neto, Danielle da Nóbrega Alves, Walicyranison Plinio da Silva Rocha, Luciana Scotti, Edeltrudes de Oliveira Lima, Marianna Vieira Sobral, Lúcio Roberto Cançado Castellano, Juliana Moura-Mendes, Felipe Queiroga Sarmento Guerra and Márcia Vanusa da Silva
Antibiotics 2023, 12(3), 480; https://doi.org/10.3390/antibiotics12030480 - 28 Feb 2023
Cited by 8 | Viewed by 1871
Abstract
Candida albicans is associated with serious infections in immunocompromised patients. Terpenes are natural-product derivatives, widely studied as antifungal alternatives. In a previous study reported by our group, the antifungal activity of α-pinene against C. albicans was verified; α-pinene presented an MIC between 128–512 [...] Read more.
Candida albicans is associated with serious infections in immunocompromised patients. Terpenes are natural-product derivatives, widely studied as antifungal alternatives. In a previous study reported by our group, the antifungal activity of α-pinene against C. albicans was verified; α-pinene presented an MIC between 128–512 µg/mL. In this study, we evaluate time-kill, a mechanism of action using in silico and in vitro tests, anti-biofilm activity against the Candida albicans, and toxicity against human cells (HaCaT). Results from the molecular-docking simulation demonstrated that thymidylate synthase (−52 kcal mol−1), and δ-14-sterol reductase (−44 kcal mol−1) presented the best interactions. Our in vitro results suggest that α-pinene’s antifungal activity involves binding to ergosterol in the cellular membrane. In the time-kill assay, the antifungal activity was not time-dependent, and also inhibited biofilm formation, while rupturing up to 88% of existing biofilm. It was non-cytotoxic to human keratinocytes. Our study supports α-pinene as a candidate to treat fungal infections caused by C. albicans. Full article
(This article belongs to the Special Issue Plant-Derived Natural Products in Antibacterial and Antifungal Drug Discovery)
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Review

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26 pages, 2963 KiB  
Review
Natural Medicine a Promising Candidate in Combating Microbial Biofilm
by Athar Shamim, Asgar Ali, Zeenat Iqbal, Mohd Aamir Mirza, Mohd Aqil, S. M. Kawish, Ayesha Siddiqui, Vijay Kumar, Punnoth Poonkuzhi Naseef, Abdulkhaliq Ali F. Alshadidi and Mohamed Saheer Kuruniyan
Antibiotics 2023, 12(2), 299; https://doi.org/10.3390/antibiotics12020299 - 02 Feb 2023
Cited by 9 | Viewed by 3601
Abstract
Studies on biofilm-related infections are gaining prominence owing to their involvement in most clinical infections and seriously threatening global public health. A biofilm is a natural form of bacterial growth ubiquitous in ecological niches, considered to be a generic survival mechanism adopted by [...] Read more.
Studies on biofilm-related infections are gaining prominence owing to their involvement in most clinical infections and seriously threatening global public health. A biofilm is a natural form of bacterial growth ubiquitous in ecological niches, considered to be a generic survival mechanism adopted by both pathogenic and non-pathogenic microorganisms and entailing heterogeneous cell development within the matrix. In the ecological niche, quorum sensing is a communication channel that is crucial to developing biofilms. Biofilm formation leads to increased resistance to unfavourable ecological effects, comprising resistance to antibiotics and antimicrobial agents. Biofilms are frequently combated with modern conventional medicines such as antibiotics, but at present, they are considered inadequate for the treatment of multi-drug resistance; therefore, it is vital to discover some new antimicrobial agents that can prevent the production and growth of biofilm, in addition to minimizing the side effects of such therapies. In the search for some alternative and safe therapies, natural plant-derived phytomedicines are gaining popularity among the research community. Phytomedicines are natural agents derived from natural plants. These plant-derived agents may include flavonoids, terpenoids, lectins, alkaloids, polypeptides, polyacetylenes, phenolics, and essential oils. Since they are natural agents, they cause minimal side effects, so could be administered with dose flexibility. It is vital to discover some new antimicrobial agents that can control the production and growth of biofilms. This review summarizes and analyzes the efficacy characteristics and corresponding mechanisms of natural-product-based antibiofilm agents, i.e., phytochemicals, biosurfactants, antimicrobial peptides, and their sources, along with their mechanism, quorum sensing signalling pathways, disrupting extracellular matrix adhesion. The review also provides some other strategies to inhibit biofilm-related illness. The prepared list of newly discovered natural antibiofilm agents could help in devising novel strategies for biofilm-associated infections. Full article
(This article belongs to the Special Issue Plant-Derived Natural Products in Antibacterial and Antifungal Drug Discovery)
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38 pages, 1529 KiB  
Review
Antibacterial and Antifungal Alkaloids from Asian Angiosperms: Distribution, Mechanisms of Action, Structure-Activity, and Clinical Potentials
by Mazdida Sulaiman, Khoshnur Jannat, Veeranoot Nissapatorn, Mohammed Rahmatullah, Alok K. Paul, Maria de Lourdes Pereira, Mogana Rajagopal, Monica Suleiman, Mark S. Butler, Mohammed Khaled Bin Break, Jean-Frédéric Weber, Polrat Wilairatana and Christophe Wiart
Antibiotics 2022, 11(9), 1146; https://doi.org/10.3390/antibiotics11091146 - 24 Aug 2022
Cited by 7 | Viewed by 3256
Abstract
The emergence of multidrug-resistant bacteria and fungi requires the development of antibiotics and antifungal agents. This review identified natural products isolated from Asian angiosperms with antibacterial and/or antifungal activities and analyzed their distribution, molecular weights, solubility, and modes of action. All data in [...] Read more.
The emergence of multidrug-resistant bacteria and fungi requires the development of antibiotics and antifungal agents. This review identified natural products isolated from Asian angiosperms with antibacterial and/or antifungal activities and analyzed their distribution, molecular weights, solubility, and modes of action. All data in this review were compiled from Google Scholar, PubMed, Science Direct, Web of Science, ChemSpider, PubChem, and a library search from 1979 to 2022. One hundred and forty-one antibacterial and/or antifungal alkaloids were identified during this period, mainly from basal angiosperms. The most active alkaloids are mainly planar, amphiphilic, with a molecular mass between 200 and 400 g/mol, and a polar surface area of about 50 Å2, and target DNA and/or topoisomerase as well as the cytoplasmic membrane. 8-Acetylnorchelerythrine, cryptolepine, 8-hydroxydihydrochelerythrine, 6-methoxydihydrosanguinarine, 2′-nortiliacorinine, pendulamine A and B, rhetsisine, sampangine, tiliacorine, tryptanthrin, tylophorinine, vallesamine, and viroallosecurinine yielded MIC ≤ 1 µg/mL and are candidates for the development of lead molecules. Full article
(This article belongs to the Special Issue Plant-Derived Natural Products in Antibacterial and Antifungal Drug Discovery)
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