Synthesis and anti- <i>Candida albicans</i> activity of oleanolic acid derivatives

With the increase incidence of <i>Candida albicans</i> infections and the widespread use of azole drugs, particularly fluconazole, the emergence of drug-resistant strains has become a significant concern. In this study, the derivatives were prepared by nucleophilic substitution at the 3-OH position of oleanolic acid, utilizing the reactivity of triphosgene, and by electrophilic coupling at the 28-COOH position through photoredox reactions. The antifungal activity of all compounds was evaluated, revealing that most derivatives exhibited good synergistic antifungal activity with fluconazole against the drug-resistant <i>Candida albicans</i> strain ATCC14053, with FICI values ranging from 0.45 to 0.14.

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Publication Details

Journal
Journal of Asian Natural Products Research
Published
2025-10-27
DOI
https://doi.org/10.1080/10286020.2025.2572087
Primary Topic
Natural product bioactivities and synthesis
Type
article
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article

Synthesis and anti- Candida albicans activity of oleanolic acid derivatives

Guanghui Ni, Fei Chen, Zefei Fan, Ruirui Wang et al.
Journal of Asian Natural Products Research
Natural product bioactivities and synthesis
article

Synthesis and anti- Candida albicans activity of oleanolic acid derivatives

Guanghui Ni, Fei Chen, Zefei Fan, Ruirui Wang, Fei Zou, Tian-Yu Zhang, Luyi Jiang, Tian-Yue Yang
article en

Abstract

With the increase incidence of <i>Candida albicans</i> infections and the widespread use of azole drugs, particularly fluconazole, the emergence of drug-resistant strains has become a significant concern. In this study, the derivatives were prepared by nucleophilic substitution at the 3-OH position of oleanolic acid, utilizing the reactivity of triphosgene, and by electrophilic coupling at the 28-COOH position through photoredox reactions. The antifungal activity of all compounds was evaluated, revealing that most derivatives exhibited good synergistic antifungal activity with fluconazole against the drug-resistant <i>Candida albicans</i> strain ATCC14053, with FICI values ranging from 0.45 to 0.14.

Journal of Asian Natural Products Research
Minzu University of China (CN), State Ethnic Affairs Commission (CN), Yunnan University of Traditional Chinese Medicine (CN)
Openalex Percentile: Top 72%
Natural product bioactivities and synthesis
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Synthesis and anti- <i>Candida albicans</i> activity of oleanolic acid derivatives — Guanghui Ni, Fei Chen, et al. · Journal of Asian Natural Products Research (2025) | TGRS Research Map | TGRS