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Guanidine-Functionalized Pillar[5]arene Exhibits Antifungal Activity for Fungal Keratitis
Xinyu Gu1, Xiwen Geng2, Chiyin Zhang1
1School of Materials Science and Engineering, Henan Key Laboratory of Advanced Nylon Materials and Application, Zhengzhou University, Zhengzhou 450001, China.
Abstract:
Fungal keratitis (FK) represents a severe infectious disease of the cornea, characterized by high incidence rates and a significant risk of vision loss, creating a substantial clinical need for novel therapeutic strategies. Addressing this challenge, we developed a water-soluble macromolecule, guanidine-linked pillar[5]arene (P5A-Gu), via click chemistry. P5A-Gu exhibited potent antifungal activity in vitro, characterized by rapid membrane penetration and complete fungicidal efficacy within 30 min at a low concentration of 1 μg/mL, alongside excellent biocompatibility. In murine FK models, P5A-Gu treatment significantly outperformed the clinical standard, voriconazole (Vor), in fungal clearance. Moreover, P5A-Gu effectively reduced corneal inflammation levels and accelerated the restoration of ocular surface tissue integrity. In summary, the macromolecule P5A-Gu shows highly effective antifungal properties and biocompatibility, positioning it as a promising candidate material for the treatment of FK.
Insights
A novel guanidine-linked pillar[5]arene (P5A-Gu) shows potent antifungal activity against fungal keratitis (FK). This macromolecule effectively clears fungi and reduces inflammation, offering a promising new treatment for this serious eye infection.
Area of Science:
- Ophthalmology
- Mycology
- Materials Science
Background:
- Fungal keratitis (FK) is a severe corneal infection with a high risk of vision loss.
- Existing treatments for FK present limitations, necessitating novel therapeutic approaches.
- Developing effective and safe antifungal agents is crucial for managing FK.
Purpose of the Study:
- To synthesize and evaluate a novel water-soluble macromolecule, guanidine-linked pillar[5]arene (P5A-Gu), as a potential treatment for fungal keratitis.
- To assess the in vitro antifungal efficacy and biocompatibility of P5A-Gu.
- To compare the in vivo therapeutic effect of P5A-Gu with voriconazole in a murine model of FK.
Main Methods:
- P5A-Gu was synthesized using click chemistry.
- In vitro antifungal activity was determined by assessing membrane penetration and fungicidal efficacy.
- Murine models of fungal keratitis were used to evaluate in vivo efficacy, including fungal clearance, inflammation reduction, and tissue repair.
Main Results:
- P5A-Gu demonstrated rapid membrane penetration and complete fungicidal activity within 30 minutes at 1 μg/mL in vitro.
- The synthesized macromolecule exhibited excellent biocompatibility.
- In vivo studies showed P5A-Gu significantly outperformed voriconazole in fungal clearance, reduced corneal inflammation, and accelerated ocular surface healing.
Conclusions:
- The macromolecule P5A-Gu possesses potent antifungal properties and good biocompatibility.
- P5A-Gu shows significant therapeutic potential for treating fungal keratitis.
- This novel compound represents a promising candidate for developing advanced FK treatments.
