ArticleAntimicrobial agents and chemotherapy2014
Histatin 5-spermidine conjugates have enhanced fungicidal activity and efficacy as a topical therapeutic for oral candidiasis.
Article in Antimicrobial agents and chemotherapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 34 citations in OpenAlex.
- Protective effect of histatin 5 and amphotericin B conjugated nanostructures in C. albicans challenged Swiss albino mice.Naunyn-Schmiedeberg's archives of pharmacology · 2025Article
- Reducing Functional Domain of Histatin 5 Improves Antifungal Activity and Prevents Proteolytic Degradation.Microorganisms · 2025Article
- High iron-mediated increased oral fungal burden, oral-to-gut transmission, and changes to pathogenicity ofJournal of oral microbiology · 2022Article
- Histatin 5 Metallopeptides and Their Potential againstBiomolecules · 2021Review
- Zinc Binding by Histatin 5 Promotes Fungicidal Membrane Disruption inJournal of fungi (Basel, Switzerland) · 2020Article
- Chemokine CCL28 Is a Potent Therapeutic Agent for Oropharyngeal Candidiasis.Antimicrobial agents and chemotherapy · 2020Article
- Bio- and Nanotechnology as the Key for Clinical Application of Salivary Peptide Histatin: A Necessary Advance.Microorganisms · 2020Review
- Iron Chelator Deferasirox ReducesAntimicrobial agents and chemotherapy · 2019Article
- Bioactive Peptides Against Fungal Biofilms.Frontiers in microbiology · 2019Review
- Methodologies forMicrobial cell (Graz, Austria) · 2018Review
- Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds.Journal of visualized experiments : JoVE · 2018Article
- Specific Histidine Residues Confer Histatin Peptides with Copper-Dependent Activity against Candida albicans.Biochemistry · 2017Article
- Structural Characterization of Histatin 5-Spermidine Conjugates: A Combined Experimental and Theoretical Study.Journal of chemical information and modeling · 2017Article
- Human Salivary Protein Histatin 5 Has Potent Bactericidal Activity against ESKAPE Pathogens.Frontiers in cellular and infection microbiology · 2017Article
- Histatin peptides: Pharmacological functions and their applications in dentistry.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2017Review
- pH Dependent Antimicrobial Peptides and Proteins, Their Mechanisms of Action and Potential as Therapeutic Agents.Pharmaceuticals (Basel, Switzerland) · 2016Review
- Design and Application of Antimicrobial Peptide Conjugates.International journal of molecular sciences · 2016Review
- Candida glabrata Binding to Candida albicans Hyphae Enables Its Development in Oropharyngeal Candidiasis.PLoS pathogens · 2016Article
- Development and In Vivo Evaluation of a Novel Histatin-5 Bioadhesive Hydrogel Formulation against Oral Candidiasis.Antimicrobial agents and chemotherapy · 2016Article
- Inhibition of Candida albicans Biofilm Formation by the Synthetic Lactoferricin Derived Peptide hLF1-11.PloS one · 2016Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Oropharyngeal candidiasis (OPC) is caused by the opportunistic fungi Candida albicans and is prevalent in immunocompromised patients, individuals with dry mouth, or patients with prolonged antibiotic therapies that reduce oral commensal bacteria. Human salivary histatins, including histatin 5 (Hst 5), are small cationic proteins that are the major source of fungicidal activity of saliva. However, Hsts are rapidly degraded in vivo, limiting their usefulness as therapeutic agents despite their lack of toxicity. We constructed a conjugate peptide using spermidine (Spd) linked to the active fragment of Hst 5 (Hst 54-15), based upon our findings that C. albicans spermidine transporters are required for Hst 5 uptake and fungicidal activity. We found that Hst 54-15-Spd was significantly more effective in killing C. albicans and Candida glabrata than Hst 5 alone in both planktonic and biofilm growth and that Hst 54-15-Spd retained high activity in both serum and saliva. Hst 54-15-Spd was not bactericidal against streptococcal oral commensal bacteria and had no hemolytic activity. We tested the effectiveness of Hst 54-15-Spd in vivo by topical application to tongue surfaces of immunocompromised mice with OPC. Mice treated with Hst 54-15-Spd had significant clearance of candidal tongue lesions macroscopically, which was confirmed by a 3- to 5-log fold reduction of C. albicans colonies recovered from tongue tissues. Hst 54-15-Spd conjugates are a new class of peptide-based drugs with high selectivity for fungi and potential as topical therapeutic agents for oral candidiasis.
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