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Staurosporine as an Antifungal Agent

Summary

Staurosporine is a natural compound from soil bacteria that can kill fungal infections. While originally known for its anti-cancer properties, scientists have recently rediscovered its strong antifungal activity, especially against dangerous drug-resistant fungi. The challenge is that it also damages human cells, but researchers are developing improved versions and combination treatments to make it safer and more effective.

Background

Staurosporine (STS) is an indolocarbazole alkaloid discovered in 1977 from the soil bacterium Streptomyces staurosporeus. Originally recognized for antifungal activity, STS became widely studied for its potent protein kinase inhibitory properties and anticancer potential. Recent discoveries of STS-induced apoptosis in filamentous fungi have renewed interest in developing STS-based antifungal therapies.

Objective

This review critically examines the antifungal properties of staurosporine and its natural and synthetic derivatives against diverse fungal species since its discovery. The authors aim to highlight advantages, limitations, conceivable mechanisms of action, and potential of STS and its analogues as antifungal chemotherapeutic agents to address growing antifungal drug resistance.

Results

STS demonstrates broad-spectrum antifungal activity against both phytopathogens and human pathogens with MIC values ranging from 0.02-50 μg/mL depending on fungal species. STS acts through multiple mechanisms including protein kinase inhibition, apoptosis induction, and membrane targeting. Natural analogues like UCN-01, K-252a, K-252d, Holyrine A, and RK-286c show varied antifungal potency, with some exhibiting superior activity to STS.

Conclusion

STS represents a promising scaffold for antifungal drug development, particularly when used in combination therapies or as modified derivatives. While non-selective protein kinase inhibition and cytotoxicity remain challenges, strategies including drug delivery systems, combination therapies, and rational chemical modifications can overcome these limitations and develop effective antifungal agents against resistant fungal infections.
  • Published in:International Journal of Molecular Sciences,
  • Study Type:Review,
  • Source: 41096950
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