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Pharmaceuticals
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Pharmaceutical Applications of Lactoferrin
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Pharmaceutical Applications of Lactoferrin

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

Deadline for manuscript submissions: closed (25 August 2024) | Viewed by 14941

Special Issue Editors

Dr. Katarzyna Kaczyńska

E-Mail Website
Guest Editor
Department of Respiration Physiology, Mossakowski Medical Research Institute, Polish Academy of Sciences, Pawińskiego 5, 02-106 Warsaw, Poland
Interests: neurodegenerative disorders; breathing control; neurotransmitters; hypoxia; therapeutics
Special Issues, Collections and Topics in MDPI journals
Dr. Dorota Sulejczak

E-Mail Website
Guest Editor
Department of Experimental Pharmacology, Mossakowski Medical Research Institute, Polish Academy of Sciences, Pawińskiego 5, 02-106 Warsaw, Poland
Interests: neuroscience, immunology, oncology, pathomorphology, genetics, human diseases
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Lactoferrin is a glycoprotein capable of binding and transferring iron ions with multiple beneficial properties. It is found in significant amounts in colostrum and in smaller quantities in milk late in lactation. It can also be detected in bodily fluids such as tears, saliva and bile. Lactoferrin's antibacterial, antiviral and antifungal properties are widely known, but its ability to modulate the action of the immune system, modify gene expression and protect DNA damage is now also emphasized. There are emerging scientific reports indicating its potential use in the treatment of a wide variety of conditions such as aging-related neurodegenerative diseases, cancer, and even obesity or stress-related emotional disorders.

In this Special Issue, our goal is to present the role of lactoferrin in the prevention and support of therapy for various human diseases. We would like to present the opinions of experts in clinical, preclinical, and experimental studies in order to expand the knowledge on this topic and allow the development of new guidelines for prophylaxis or new therapeutic procedures using this versatile molecule. Both original articles and review contributions are welcome.

Dr. Katarzyna Kaczyńska
Dr. Dorota Sulejczak
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. Pharmaceuticals 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

  • lactoferrin
  • prevention
  • therapy
  • drug delivery
  • protection
  • mechanisms

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Published Papers (5 papers)

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Research

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12 pages, 1826 KiB  
Article
Lactoferrin Binds through Its N-Terminus to the Receptor-Binding Domain of the SARS-CoV-2 Spike Protein
by Patrik Babulic, Ondrej Cehlar, Gabriela Ondrovičová, Tetiana Moskalets, Rostislav Skrabana and Vladimir Leksa
Pharmaceuticals 2024, 17(8), 1021; https://doi.org/10.3390/ph17081021 - 4 Aug 2024
Viewed by 1442
Abstract
Since Coronavirus disease 2019 (COVID-19) still presents a considerable threat, it is beneficial to provide therapeutic supplements against it. In this respect, glycoprotein lactoferrin (LF) and lactoferricin (LFC), a natural bioactive peptide yielded upon digestion from the N-terminus of LF, are of utmost [...] Read more.
Since Coronavirus disease 2019 (COVID-19) still presents a considerable threat, it is beneficial to provide therapeutic supplements against it. In this respect, glycoprotein lactoferrin (LF) and lactoferricin (LFC), a natural bioactive peptide yielded upon digestion from the N-terminus of LF, are of utmost interest, since both have been shown to reduce infections of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), the virus responsible for COVID-19, in particular via blockade of the virus priming and binding. Here, we, by means of biochemical and biophysical methods, reveal that LF directly binds to the S-protein of SARS-CoV-2. We determined thermodynamic and kinetic characteristics of the complex formation and mapped the mutual binding sites involved in this interaction, namely the N-terminal region of LF and the receptor-binding domain of the S-protein (RBD). These results may not only explain many of the observed protective effects of LF and LFC in SARS-CoV-2 infection but may also be instrumental in proposing potent and cost-effective supplemental tools in the management of COVID-19. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Lactoferrin)
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Review

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31 pages, 3020 KiB  
Review
Lactoferrins in Their Interactions with Molecular Targets: A Structure-Based Overview
by Roberta Piacentini, Alberto Boffi and Edoardo Milanetti
Pharmaceuticals 2024, 17(3), 398; https://doi.org/10.3390/ph17030398 - 20 Mar 2024
Cited by 2 | Viewed by 2214
Abstract
Lactoferrins and lactoferrin-derived peptides display numerous functions linked to innate immunity in mammalians, spanning from antimicrobial to anti-inflammatory and immunomodulatory actions, and even demonstrate antitumor properties. To date, the proposed mechanisms for their biological actions are varied, although the molecular basis that governs [...] Read more.
Lactoferrins and lactoferrin-derived peptides display numerous functions linked to innate immunity in mammalians, spanning from antimicrobial to anti-inflammatory and immunomodulatory actions, and even demonstrate antitumor properties. To date, the proposed mechanisms for their biological actions are varied, although the molecular basis that governs lactoferrin interactions with molecular targets has been clarified only in a limited number of specific cases. However, key in silico methods have recently moved the topic to the fore, thus greatly expanding the possibilities of large-scale investigations on macromolecular interactions involving lactoferrins and their molecular targets. This review aims to summarize the current knowledge on the structural determinants that drive lactoferrin recognition of molecular targets, with primary focus on the mechanisms of activity against bacteria and viruses. The understanding of the structural details of lactoferrins’ interaction with their molecular partners is in fact a crucial goal for the development of novel pharmaceutical products. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Lactoferrin)
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20 pages, 1666 KiB  
Review
Lactoferrin as a Component of Pharmaceutical Preparations: An Experimental Focus
by Fabiola Guzmán-Mejía, Marycarmen Godínez-Victoria, Daniel Efrain Molotla-Torres and Maria Elisa Drago-Serrano
Pharmaceuticals 2023, 16(2), 214; https://doi.org/10.3390/ph16020214 - 31 Jan 2023
Cited by 10 | Viewed by 3817
Abstract
Lactoferrin is an 80 kDa monomeric glycoprotein that exhibits multitask activities. Lactoferrin properties are of interest in the pharmaceutical field for the design of products with therapeutic potential, including nanoparticles and liposomes, among many others. In antimicrobial preparations, lactoferrin has been included either [...] Read more.
Lactoferrin is an 80 kDa monomeric glycoprotein that exhibits multitask activities. Lactoferrin properties are of interest in the pharmaceutical field for the design of products with therapeutic potential, including nanoparticles and liposomes, among many others. In antimicrobial preparations, lactoferrin has been included either as a main bioactive component or as an enhancer of the activity and potency of first-line antibiotics. In some proposals based on nanoparticles, lactoferrin has been included in delivery systems to transport and protect drugs from enzymatic degradation in the intestine, favoring the bioavailability for the treatment of inflammatory bowel disease and colon cancer. Moreover, nanoparticles loaded with lactoferrin have been formulated as delivery systems to transport drugs for neurodegenerative diseases, which cannot cross the blood–brain barrier to enter the central nervous system. This manuscript is focused on pharmaceutical products either containing lactoferrin as the bioactive component or formulated with lactoferrin as the carrier considering its interaction with receptors expressed in tissues as targets of drugs delivered via parenteral or mucosal administration. We hope that this manuscript provides insights about the therapeutic possibilities of pharmaceutical Lf preparations with a sustainable approach that contributes to decreasing the resistance of antimicrobials and enhancing the bioavailability of first-line drugs for intestinal chronic inflammation and neurodegenerative diseases. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Lactoferrin)
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25 pages, 1640 KiB  
Review
Potential of Lactoferrin in the Treatment of Lung Diseases
by Katarzyna Kaczyńska, Monika Jampolska, Piotr Wojciechowski, Dorota Sulejczak, Kryspin Andrzejewski and Dominika Zając
Pharmaceuticals 2023, 16(2), 192; https://doi.org/10.3390/ph16020192 - 28 Jan 2023
Cited by 7 | Viewed by 5010
Abstract
Lactoferrin (LF) is a multifunctional iron-binding glycoprotein that exhibits a variety of properties, such as immunomodulatory, anti-inflammatory, antimicrobial, and anticancer, that can be used to treat numerous diseases. Lung diseases continue to be the leading cause of death and disability worldwide. Many of [...] Read more.
Lactoferrin (LF) is a multifunctional iron-binding glycoprotein that exhibits a variety of properties, such as immunomodulatory, anti-inflammatory, antimicrobial, and anticancer, that can be used to treat numerous diseases. Lung diseases continue to be the leading cause of death and disability worldwide. Many of the therapies currently used to treat these diseases have limited efficacy or are associated with side effects. Therefore, there is a constant pursuit for new drugs and therapies, and LF is frequently considered a therapeutic agent and/or adjunct to drug-based therapies for the treatment of lung diseases. This article focuses on a review of the existing and most up-to-date literature on the contribution of the beneficial effects of LF on the treatment of lung diseases, including asthma, viral infections, cystic fibrosis, or lung cancer, among others. Although in vitro and in vivo studies indicate significant potency of LF in the treatment of the listed diseases, only in the case of respiratory tract infections do human studies seem to confirm them by demonstrating the effectiveness of LF in reducing episodes of illness and shortening the recovery period. For lung cancer, COVID-19 and sepsis, the reports are conflicting, and for other diseases, there is a paucity of human studies conclusively confirming the beneficial effects of LF. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Lactoferrin)
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Other

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9 pages, 2919 KiB  
Brief Report
Inhibition of SARS-CoV-2 Infection in Vero Cells by Bovine Lactoferrin under Different Iron-Saturation States
by Nathalia S. Alves, Adriana S. Azevedo, Brenda M. Dias, Ingrid S. Horbach, Bruno P. Setatino, Caio B. Denani, Waleska D. Schwarcz, Sheila Maria B. Lima, Sotiris Missailidis, Ana Paula D. Ano Bom, Andréa M. V. Silva, Débora F. Barreto Vieira, Marcos Alexandre N. Silva, Caroline A. Barros, Carlos Alberto M. Carvalho and Rafael B. Gonçalves
Pharmaceuticals 2023, 16(10), 1352; https://doi.org/10.3390/ph16101352 - 25 Sep 2023
Cited by 3 | Viewed by 1423
Abstract
Despite the rapid mass vaccination against COVID-19, the emergence of new SARS-CoV-2 variants of concern, such as omicron, is still a great distress, and new therapeutic options are needed. Bovine lactoferrin (bLf), a multifunctional iron-binding glycoprotein available in unsaturated (apo-bLf) and saturated (holo-bLf) [...] Read more.
Despite the rapid mass vaccination against COVID-19, the emergence of new SARS-CoV-2 variants of concern, such as omicron, is still a great distress, and new therapeutic options are needed. Bovine lactoferrin (bLf), a multifunctional iron-binding glycoprotein available in unsaturated (apo-bLf) and saturated (holo-bLf) forms, has been shown to exert broad-spectrum antiviral activity against many viruses. In this study, we evaluated the efficacy of both forms of bLf at 1 mg/mL against infection of Vero cells by SARS-CoV-2. As assessed with antiviral assays, an equivalent significant reduction in virus infection by about 70% was observed when either form of bLf was present throughout the infection procedure with the SARS-CoV-2 ancestral or omicron strain. This inhibitory effect seemed to be concentrated during the early steps of virus infection, since a significant reduction in its efficiency by about 60% was observed when apo- or holo-bLf were incubated with the cells before or during virus addition, with no significant difference between the antiviral effects of the distinct iron-saturation states of the protein. However, an ultrastructural analysis of bLf treatment during the early steps of virus infection revealed that holo-bLf was somewhat more effective than apo-bLf in inhibiting virus entry. Together, these data suggest that bLf mainly acts in the early events of SARS-CoV-2 infection and is effective against the ancestral virus as well as its omicron variant. Considering that there are no effective treatments to COVID-19 with tolerable toxicity yet, bLf shows up as a promising candidate. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Lactoferrin)
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