Anti-Candida Activity of Cysteine-Modified Amidated Decoralin in the Presence of Engineered Nanomaterials

半胱氨酸修饰的酰胺化去甲肾上腺素在工程纳米材料存在下的抗念珠菌活性

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Abstract

Background: Candidiasis remains a chief concern in global healthcare. Drug safety issues and increasing resistance make it urgent to develop alternative antifungal agents, namely antimicrobial peptides. Amidated decoralin (Dec-CONH(2)) possesses considerable anti-Candida activity, and its association with nanocarriers could help in enhancing efficacy while reducing intrinsic toxicity to the host. Methods: We studied an N-terminal cysteine-modified version of the peptide (Cys-Dec-CONH(2)) and screened the effects of different nanosystems (polymeric nanoparticles (NPs), liposomes and gold NPs) on its activity against azole-sensitive and azole-resistant Candida species using a clinically relevant in vitro assay. Results: The antifungal activity of Cys-Dec-CONH(2) was maintained (minimum inhibitory concentration (MIC) = 16-64 µg/mL), but the presence of poly(d,l-lactic-co-glycolic acid) (PLGA)- and polycaprolactone-based NPs impaired the antifungal effect of the peptide (MIC > 256 µg/mL). This effect was milder for polystyrene-based NPs, liposomes, and gold NPs (MIC ≤ 128 µg/mL). Additionally, the covalent surface functionalization of PLGA-based NPs with Cys-Dec-CONH(2) or the presence of relevant biomolecules (albumin and mucin) resulted in complete inhibition of antifungal activity. Conclusions: Our data suggest that Cys-Dec-CONH(2) is able to establish strong interfacial interactions with different nanomaterials, which need to be considered when developing nanomedicines based on this peptide for the management of candidiasis.

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