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Molecules
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Natural Antimicrobial Agents: Design, Synthesis, and Evaluation
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Natural Antimicrobial Agents: Design, Synthesis, and Evaluation

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 January 2022) | Viewed by 6989

Special Issue Editors

Prof. Dr. Naresh Kumar

E-Mail Website
Guest Editor
School of Chemistry, University of New South Wales, Sydney, NSW 2052, Australia
Interests: biologically active molecules; medicinal chemistry; organic chemical synthesis; peptidomimetics; novel antimicrobials; biomaterials
Special Issues, Collections and Topics in MDPI journals
Dr. Renxun Chen

E-Mail Website
Guest Editor
School of Chemistry, University of New South Wales, UNSW, Sydney, Australia
Interests: antimicrobial peptides and mimics; antimicrobial biomaterials; disinfection; surface coatings; functional materials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The emergence of multi-drug resistance in common human pathogens has highlighted the need to develop novel classes of antimicrobials for the treatment of human disease. Antibiotics are no longer the magic bullets they were once thought to be, and therefore there is an urgent need for the development of alternative therapeutic strategies to combat infections without inducing drug resistance. Naturally produced chemicals are of fundamental importance in biological systems. Such chemicals are used to mediate interactions across all levels of biological hierarchy, and have tremendous potential for the discovery of new antimicrobial entities. Natural antimicrobial scaffolds can also act as inspiration for the design and synthesis of new antimicrobial agents.

Several topics in this research area are discussed:

  1. Isolation and structure elucidation of natural products with antimicrobial activities;
  2. Synthesis of antimicrobial natural product analogues;
  3. Synthesis of new classes of natural antimicrobial agents with anti-virulence and anti-biofilm properties;
  4. Rational design of antimicrobial agents based on natural products;
  5. Structure–activity relationship studies of natural antimicrobial agents;
  6. Applications and targeted delivery of natural antimicrobial agents;
  7. Synergistic activities of natural antimicrobial agents.

Molecules will publish a Special Issue focusing on “Natural Antimicrobial Agents: Design, Synthesis, and Evaluation”. It is my pleasure to invite submissions of high-quality research-based papers related to the topics mentioned above.

Prof. Dr. Naresh Kumar
Dr. Renxun Chen
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. Molecules is an international peer-reviewed open access semimonthly 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

  • Discovery of new natural antimicrobial agents
  • Design and synthesis of natural products with antimicrobial activity
  • Rational design of antimicrobial agents based on natural product leads
  • Evaluation of natural products and their analogues for antimicrobial activity including antifouling, anti-biofilm, and anti-viral activity
  • Synergistic effects of natural products with other antimicrobial agents

Published Papers (3 papers)

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Research

15 pages, 4636 KiB  
Article
Rationalisation of Antifungal Properties of α-Helical Pore-Forming Peptide, Mastoparan B
by Edward Jianyang Lim, Eunice Goh Tze Leng, Nhan Dai Thien Tram, Mercy Halleluyah Periayah, Pui Lai Rachel Ee, Timothy Mark Sebastian Barkham, Zhi Sheng Poh, Navin Kumar Verma and Rajamani Lakshminarayanan
Molecules 2022, 27(4), 1438; https://doi.org/10.3390/molecules27041438 - 21 Feb 2022
Cited by 2 | Viewed by 2008
Abstract
The high mortality associated with invasive fungal infections, narrow spectrum of available antifungals, and increasing evolution of antifungal resistance necessitate the development of alternative therapies. Host defense peptides are regarded as the first line of defense against microbial invasion in both vertebrates and [...] Read more.
The high mortality associated with invasive fungal infections, narrow spectrum of available antifungals, and increasing evolution of antifungal resistance necessitate the development of alternative therapies. Host defense peptides are regarded as the first line of defense against microbial invasion in both vertebrates and invertebrates. In this work, we investigated the effectiveness of four naturally occurring pore-forming antimicrobial peptides (melittin, magainin 2, cecropin A, and mastoparan B) against a panel of clinically relevant pathogens, including Candida albicans, Candida parapsilosis, Candida tropicalis, and Candida glabrata. We present data on the antifungal activities of the four pore-forming peptides, assessed with descriptive statistics, and their cytocompatibility with cultured human cells. Among the four peptides, mastoparan B (MB) displayed potent antifungal activity, whereas cecropin A was the least potent. We show that MB susceptibility of phylogenetically distant non-candida albicans can vary and be described by different intrinsic physicochemical parameters of pore-forming α-helical peptides. These findings have potential therapeutic implications for the design and development of safe antifungal peptide-based drugs. Full article
(This article belongs to the Special Issue Natural Antimicrobial Agents: Design, Synthesis, and Evaluation)
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14 pages, 6346 KiB  
Article
Halogenated Dihydropyrrol-2-One Molecules Inhibit Pyocyanin Biosynthesis by Blocking the Pseudomonas Quinolone Signaling System
by Theerthankar Das, Shekh Sabir, Ren Chen, Jessica Farrell, Frederik H. Kriel, Gregory S. Whiteley, Trevor O. Glasbey, Jim Manos, Mark D. P. Willcox and Naresh Kumar
Molecules 2022, 27(4), 1169; https://doi.org/10.3390/molecules27041169 - 09 Feb 2022
Cited by 9 | Viewed by 2285
Abstract
Quorum-sensing (QS) systems of Pseudomonas aeruginosa are involved in the control of biofilm formation and virulence factor production. The current study evaluated the ability of halogenated dihydropyrrol-2-ones (DHP) (Br (4a), Cl (4b), and F (4c)) and a non-halogenated version (4d) to inhibit the [...] Read more.
Quorum-sensing (QS) systems of Pseudomonas aeruginosa are involved in the control of biofilm formation and virulence factor production. The current study evaluated the ability of halogenated dihydropyrrol-2-ones (DHP) (Br (4a), Cl (4b), and F (4c)) and a non-halogenated version (4d) to inhibit the QS receptor proteins LasR and PqsR. The DHP molecules exhibited concentration-dependent inhibition of LasR and PqsR receptor proteins. For LasR, all compounds showed similar inhibition levels. However, compound 4a (Br) showed the highest decrease (two-fold) for PqsR, even at the lowest concentration (12.5 µg/mL). Inhibition of QS decreased pyocyanin production amongst P. aeruginosa PAO1, MH602, ATCC 25619, and two clinical isolates (DFU-53 and 364707). In the presence of DHP, P. aeruginosa ATCC 25619 showed the highest decrease in pyocyanin production, whereas clinical isolate DFU-53 showed the lowest decrease. All three halogenated DHPs also reduced biofilm formation by between 31 and 34%. The non-halogenated compound 4d exhibited complete inhibition of LasR and had some inhibition of PqsR, pyocyanin, and biofilm formation, but comparatively less than halogenated DHPs. Full article
(This article belongs to the Special Issue Natural Antimicrobial Agents: Design, Synthesis, and Evaluation)
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14 pages, 3318 KiB  
Article
Leucine-Rich, Potent Anti-Bacterial Protein against Vibrio cholerae, Staphylococcus aureus from Solanum trilobatum Leaves
by Manohar Radhakrishnan, Malathy Palayam, Ammar B. Altemimi, Lakshminarayanan Karthik, Gunasekaran Krishnasamy, Francesco Cacciola and Lakshmanan Govindan
Molecules 2022, 27(4), 1167; https://doi.org/10.3390/molecules27041167 - 09 Feb 2022
Cited by 2 | Viewed by 1970
Abstract
A 24 kDa leucine-rich protein from ion exchange fractions of Solanum trilobatum, which has anti-bacterial activity against both the Gram-negative Vibrio cholerae and Gram-positive Staphylococcus aureus bacteria has been purified. In this study, mass spectrometry analysis identified the leucine richness and found [...] Read more.
A 24 kDa leucine-rich protein from ion exchange fractions of Solanum trilobatum, which has anti-bacterial activity against both the Gram-negative Vibrio cholerae and Gram-positive Staphylococcus aureus bacteria has been purified. In this study, mass spectrometry analysis identified the leucine richness and found a luminal binding protein (LBP). Circular dichroism suggests that the protein was predominantly composed of α- helical contents of its secondary structure. Scanning electron microscopy visualized the characteristics and morphological and structural changes in LBP-treated bacterium. Further in vitro studies confirmed that mannose-, trehalose- and raffinose-treated LBP completely inhibited the hemagglutination ability towards rat red blood cells. Altogether, these studies suggest that LBP could bind to sugar moieties which are abundantly distributed on bacterial surface which are essential for maintaining the structural integrity of bacteria. Considering that Solanum triolbatum is a well-known medicinal and edible plant, in order to shed light on its ancient usage in this work, an efficient anti-microbial protein was isolated, characterized and its in vitro functional study against human pathogenic bacteria was evaluated. Full article
(This article belongs to the Special Issue Natural Antimicrobial Agents: Design, Synthesis, and Evaluation)
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