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Baicalein as a potent antifungal agent against Candida albicans: synergy with fluconazole and sustainable production through probiotic-mediated bioconversion

Summary

Baicalein, a natural compound from a traditional medicinal plant, is significantly more effective at fighting Candida albicans infections than its parent compound baicalin. When combined with the common antifungal drug fluconazole, baicalein creates a powerful synergistic effect that is especially useful against drug-resistant fungal strains. Scientists discovered that a beneficial probiotic bacterium, Lactobacillus rhamnosus, can efficiently convert the abundant baicalin into baicalein, providing a sustainable and safe way to produce this potent antifungal compound at scale.

Background

Fungal infections caused by Candida albicans represent a significant global health challenge, with increasing drug resistance and biofilm formation limiting treatment effectiveness. Baicalein, a flavonoid derived from Scutellaria baicalensis, has demonstrated considerable antifungal efficacy but is limited by its low natural abundance. Lactobacillus rhamnosus has been identified as a potential biocatalyst for converting baicalin to baicalein through whole-cell catalysis.

Objective

To evaluate the antifungal efficacy of baicalein versus baicalin against C. albicans, investigate synergistic effects with fluconazole, and develop a sustainable production method using L. rhamnosus-mediated biotransformation of baicalin to baicalein.

Results

Baicalein demonstrated 6.4-fold greater antifungal activity than baicalin against C. albicans, with MIC values of 80 μg/mL (sensitive) and 160 μg/mL (resistant strains). When combined with fluconazole, baicalein showed strong synergy with FICI of 0.07, resulting in a 1,280-fold reduction in fluconazole MIC. L. rhamnosus achieved a 66% molar yield at 4 g/L baicalin substrate concentration under optimized conditions, a 4.07-fold improvement. The transformation solution exhibited enhanced antifungal effects compared to L. rhamnosus or baicalein alone.

Conclusion

Baicalein is a potent antifungal agent showing superior activity compared to baicalin and demonstrating strong synergistic effects with fluconazole against resistant C. albicans strains. L. rhamnosus provides a safe, scalable, and sustainable method for producing baicalein from baicalin through probiotic-mediated bioconversion. The combination of L. rhamnosus and baicalein offers a promising novel approach for treating resistant fungal infections, particularly in intestinal candidiasis.
  • Published in:Frontiers in Microbiology,
  • Study Type:Experimental/Laboratory Study,
  • Source: PMID: 40071210
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