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Antifungal compounds of Chinese prickly ash against drug-resistant Candida albicans.

ABSTRACT: The leaf of Chinese prickly ash, a unique spice having typical pungent sensation, is a popular food in Southwest China with antipruritic, insecticidal and fungicidal functions, but its bioactive constituents of fungistatic capacity remain unknown. In present investigation, twenty-nine compounds were isolated from leaf of Chinese prickly ash, and their antifungal bioactivity against drug-resistant Candida albicans were evaluated in vitro and in vivo. As a result, three compounds 3, 10, 29 showed antifungal bioactivity by damage of the fungal biofilm, and they might recover sensitive of drug resistant C. albicans to Fluconazole. Then Chinese prickly ash leaf was proved to be a functional food against fungus for the first time in experiment.

SUBMITTER: Ma DY

PROVIDER: S-EPMC9532736 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature

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Antifungal compounds of Chinese prickly ash against drug-resistant Candida albicans.

Ma Dan-Yu DY Wang Zhao-Jie ZJ Chen Yi-Chi YC Qi Zi-Heng ZH Wang Huan H Zhu Yan-Yan YY Luo Xiao-Dong XD

Food chemistry: X 20220725

The leaf of Chinese prickly ash, a unique spice having typical pungent sensation, is a popular food in Southwest China with antipruritic, insecticidal and fungicidal functions, but its bioactive constituents of fungistatic capacity remain unknown. In present investigation, twenty-nine compounds were isolated from leaf of Chinese prickly ash, and their antifungal bioactivity against drug-resistant Candida albicans were evaluated in vitro and in vivo. As a result, three compou ...[more]

PMID: 36211763

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Project description:Recently, the occurrence of candidiasis has increased dramatically, especially in immunocompromised patients. Additionally, their treatment is often ineffective due to the resistance of yeasts to antimycotics. Therefore, there is a need to search for new antifungals. A series of nine newly synthesized thiazole derivatives containing the cyclopropane system, showing promising activity against Candida spp., has been further investigated. We decided to verify their antifungal activity towards clinical Candida albicans isolated from the oral cavity of patients with hematological malignancies and investigate the mode of action on fungal cell, the effect of combination with the selected antimycotics, toxicity to erythrocytes, and lipophilicity. These studies were performed by the broth microdilution method, test with sorbitol and ergosterol, checkerboard technique, erythrocyte lysis assay, and reversed phase thin-layer chromatography, respectively. All derivatives showed very strong activity (similar and even higher than nystatin) against all C. albicans isolates with minimal inhibitory concentration (MIC) = 0.008-7.81 µg/mL Their mechanism of action may be related to action within the fungal cell wall structure and/or within the cell membrane. The interactions between the derivatives and the selected antimycotics (nystatin, chlorhexidine, and thymol) showed additive effect only in the case of combination some of them and thymol. The erythrocyte lysis assay confirmed the low cytotoxicity of these compounds as compared to nystatin. The high lipophilicity of the derivatives was related with their high antifungal activity. The present studies confirm that the studied thiazole derivatives containing the cyclopropane system appear to be a very promising group of compounds in treatment of infections caused by C. albicans. However, this requires further studies in vivo. KEY POINTS: • The newly thiazoles showed high antifungal activity and some of them - additive effect in combination with thymol. • Their mode of action may be related with the influence on the structure of the fungal cell wall and/or the cell membrane. • The low cytotoxicity against erythrocytes and high lipophilicity of these derivatives are their additional good properties.

Dataset Information

Antifungal compounds of Chinese prickly ash against drug-resistant Candida albicans.

Publications

Antifungal compounds of Chinese prickly ash against drug-resistant <i>Candida albicans</i>.

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