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Published on: February 14, 2018
Antifungal activity of maytenin and pristimerin
Fernanda P Gullo1, Janaina C O Sardi, Vânia A F F M Santos
1Laboratory of Clinical Mycology, Department of Clinical Analysis, Faculty of Pharmaceutical Sciences, UNESP, Rua Expedicionários do Brasil 1621, 14801-902 Araraquara, SP, Brazil.
Abstract:
Fungal infections in humans have increased alarmingly in recent years, particularly in immunocompromised individuals. Among the infections systemic candidiasis, aspergillosis, cryptococcosis, paracoccidioidomycosis, and histoplasmosis mortality are more prevalent and more severe in humans. The current high incidence of dermatophytosis is in humans, especially as the main etiologic agents Trichophyton rubrum and Trichophyton mentagrophytes. Molecules pristimerin and maytenin obtained from the plant Maytenus ilicifolia (Celastraceae) are known to show various pharmacological activities. This study aimed to evaluate the spectrum of antifungal activity of maytenin and pristimerin and their cytotoxicity in human keratinocytes (NOK cells of the oral mucosa). It was concluded that the best spectrum of antifungal activity has been shown to maytenin with MIC varying from 0.12 to 125 mg/L, although it is also active with pristimerin MIC ranging between 0.12 and 250 mg/L. Regarding the toxicity, both showed to have high IC(50). The SI showed high pristimerin against some species of fungi, but SI maytenin was above 1.0 for all fungi tested, showing a selective action of fungi. However, when comparing the two substances, maytenin also showed better results. The two molecules can be a possible prototype with a broad spectrum of action for the development of new antifungal agents.
Insights
Maytenin and pristimerin, derived from Maytenus ilicifolia, show broad-spectrum antifungal activity. Maytenin demonstrates greater efficacy and selectivity against fungi, suggesting potential for new antifungal drug development.
Area of Science:
- Pharmacology
- Mycology
- Natural Products Chemistry
Background:
- Human fungal infections are rising, especially in immunocompromised individuals.
- Systemic infections like candidiasis and aspergillosis pose significant mortality risks.
- Dermatophytosis, caused by Trichophyton species, is also highly prevalent.
Purpose of the Study:
- To evaluate the antifungal activity spectrum of maytenin and pristimerin.
- To assess the cytotoxicity of these compounds in human keratinocytes.
- To identify potential new antifungal agents from Maytenus ilicifolia.
Main Methods:
- Minimum Inhibitory Concentration (MIC) assays were performed for antifungal activity.
- Cytotoxicity was assessed using IC50 values in human oral keratinocytes (NOK cells).
- Selectivity Index (SI) was calculated to determine safety and efficacy.
Main Results:
- Maytenin exhibited potent antifungal activity with MICs ranging from 0.12 to 125 mg/L.
- Pristimerin also showed antifungal activity, with MICs between 0.12 and 250 mg/L.
- Both compounds displayed high IC50 values, indicating cytotoxicity, but maytenin showed a better Selectivity Index, suggesting selective action against fungi.
Conclusions:
- Maytenin and pristimerin possess broad-spectrum antifungal properties.
- Maytenin demonstrates superior antifungal efficacy and selectivity compared to pristimerin.
- These molecules represent promising prototypes for developing novel antifungal therapeutics.
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