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Updated: Mar 21, 2026

Immunofluorescence to Monitor the Cellular Uptake of Human Lactoferrin and its Associated Antiviral Activity Against the Hepatitis C Virus
Published on: October 1, 2015
Anti-infective efficacy of the lactoferrin-derived antimicrobial peptide HLR1r
Camilla Björn1, Margit Mahlapuu2, Inger Mattsby-Baltzer3
1Pergamum AB, Karolinska Institutet Science Park, Fogdevreten 2, SE-171 65 Solna, Sweden; SP Technical Research Institute of Sweden, Medical Device Technology, Box 857, SE-501 15 Borås, Sweden; The Lundberg Laboratory for Diabetes Research, Department of Molecular and Clinical Medicine, The Sahlgrenska Academy at University of Gothenburg, Blå stråket 5, SE-413 45 Gothenburg, Sweden.
Abstract:
Antimicrobial peptides (AMPs) have emerged as a new class of drug candidates for the treatment of infectious diseases. Here we describe a novel AMP, HLR1r, which is structurally derived from the human milk protein lactoferrin and demonstrates a broad spectrum microbicidal action in vitro. The minimum concentration of HLR1r needed for killing ≥99% of microorganisms in vitro, was in the range of 3-50μg/ml for common Gram-negative and Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), and for the yeast Candida albicans, when assessed in diluted brain-heart infusion medium. We found that HLR1r also possesses anti-inflammatory properties as evidenced by inhibition of tumor necrosis factor alpha (TNF-α) secretion from human monocyte-derived macrophages and by repression of interleukin-6 (IL-6) and plasminogen activator inhibitor-1 (PAI-1) secretion from human mesothelial cells, without any cytotoxic effect observed at the concentration range tested (up to 400μg/ml). HLR1r demonstrated pronounced anti-infectious effect in in vivo experimental models of cutaneous candidiasis in mice and of excision wounds infected with MRSA in rats as well as in an ex vivo model of pig skin infected with S. aureus. In conclusion, HLR1r may constitute a new therapeutic alternative for local treatment of skin infections.
Insights
A novel antimicrobial peptide (AMP), HLR1r, derived from lactoferrin, shows broad-spectrum microbicidal and anti-inflammatory effects. This peptide holds promise as a new therapeutic option for treating skin infections caused by bacteria and fungi.
Area of Science:
- Biochemistry
- Microbiology
- Pharmacology
Background:
- Antimicrobial peptides (AMPs) are a promising class of therapeutics for infectious diseases.
- Novel AMPs are needed to combat resistant microbial strains.
- HLR1r, derived from human lactoferrin, is investigated for its therapeutic potential.
Purpose of the Study:
- To characterize the novel antimicrobial peptide HLR1r.
- To evaluate its efficacy against Gram-negative and Gram-positive bacteria, including MRSA, and Candida albicans.
- To assess its anti-inflammatory properties and safety profile.
Main Methods:
- In vitro microbicidal assays were performed to determine the minimum inhibitory concentration (MIC) of HLR1r.
- Inhibition of pro-inflammatory cytokine secretion (TNF-α, IL-6, PAI-1) was measured in human cell lines.
- In vivo efficacy was tested in murine models of cutaneous candidiasis and rat models of MRSA-infected wounds, along with ex vivo pig skin models.
Main Results:
- HLR1r exhibited broad-spectrum microbicidal activity against bacteria and yeast, with MICs ranging from 3-50μg/ml.
- The peptide demonstrated significant anti-inflammatory effects by inhibiting TNF-α, IL-6, and PAI-1 secretion without cytotoxicity.
- HLR1r showed pronounced anti-infective effects in experimental models of candidiasis and MRSA-infected wounds.
Conclusions:
- HLR1r possesses potent antimicrobial and anti-inflammatory properties.
- It is effective in both in vitro and in vivo models of infection.
- HLR1r represents a potential new therapeutic agent for the local treatment of skin infections.
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