Discovery of deguelin derivatives in combination with fluconazole against drug-resistant Candida albicans

Liu, Biaoqi; Wu, Youwei; Qin, Dingmei; Wang, Hairong; Chen, Hongjie; Zhang, Yi; Xiao, Wei‐Lie; Liu, Yuanyuan; Wang, Ruirui; Zhang, R S

doi:10.1007/s00044-023-03118-7

Cited by 3 publications

(1 citation statement)

References 15 publications

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“…C. albicans was nurtured at 37 °C for 24 h, and Filamentous fungi were nurtured at 25 °C for 5 days, and the absorbance value at 625 nm was measured by an enzyme marker. The experiment was set up with a medium blank control, a fungal control [ 32 ], and positive drug controls for amphotericin B and terbinafine hydrochloride.…”

Section: Discussionmentioning

confidence: 99%

The antifungal properties of terpenoids from the endophytic fungus Bipolaris eleusines

Fan,

Tian,

Tong

et al. 2023

Nat. Prod. Bioprospect.

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A series of terpenoids (1–17), comprising six new compounds designated bipolariterpenes A-F (1–6) and eleven recognized compounds (7–17), were isolated from the wheat culture of the potato endophytic fungus Bipolariseleusines. Their structures and stereochemistry were clarified by HRESIMS, NMR, DP4 + probability analyses, and computations for electronic circular dichroism (ECD). All compounds are made up of six meroterpenoids, four sesterterpenes and seven sesquiterpenes. Among them, four sesterterpenes (4, 5, 10, 11) were investigated for their antifungal, antibacterial and cytotoxic properties, and six meroterpenoids (1–3, 7–9) were evaluated for their antifungal properties. The compounds 7, 9, and 10 had substantial antifungal activity against Epidermophytonfloccosum at a concentration of 100 µM. No antibacterial and cytotoxic activities were observed. Graphical Abstract

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Section: Discussionmentioning

confidence: 99%

The antifungal properties of terpenoids from the endophytic fungus Bipolaris eleusines

Fan,

Tian,

Tong

et al. 2023

Nat. Prod. Bioprospect.

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Design, synthesis and biological evaluation of novel benzocoumarin derivatives as potent inhibitors of MAO-B activity

Meletli,

Gündüz,

Alparslan

et al. 2024

Bioorganic & Medicinal Chemistry Letters

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Inhibitory Effects of B-, C-, and E-Ring-Truncated Deguelin Derivatives Against A549, HCT116, and MCF-7 Cancer Cells

Francisco,

Paderes

2023

ACS Omega

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Deguelin has been extensively studied for its anticancer properties; however, its clinical application has been hindered by concerns about in vivo toxicity. Structural modifications of deguelin including ring truncation have been explored to enhance its pharmacological properties. In this study, the design and straightforward synthesis of a series of B, C, and E (BCE)-ringtruncated deguelin analogues with deoxybenzoin backbone were described. The structure−activity relationships (SARs) were established by evaluation of their inhibitory activities against three cancer cell lines, A549 (adenocarcinomic human alveolar basal epithelial cells), HCT116 (human colorectal cancer cells), and MCF-7 (breast cancer cells). Six derivatives demonstrated significant and selective inhibitory activities. The ketone derivative 3a showed potency against A549 (IC 50 = 6.62 μM) while the oxime analogue 6a and D-ring-benzylated ketone analogue 8d exhibited activity against HCT116 (IC 50 = 3.43 and 6.96 μM, respectively). Moreover, the D-ring alkylated derivatives 8c and 8e−f were active against MCF-7 cells (IC 50 < 10 μM). The potential suitability of the BCE-ring-truncated deguelin derivatives for drug development was further supported by the favorable in silico prediction of their physicochemical properties, druglikeness, and toxicity. This study could provide valuable insights for the further development of novel anticancer agents.

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Discovery of deguelin derivatives in combination with fluconazole against drug-resistant Candida albicans

Cited by 3 publications

References 15 publications

The antifungal properties of terpenoids from the endophytic fungus Bipolaris eleusines

The antifungal properties of terpenoids from the endophytic fungus Bipolaris eleusines

Design, synthesis and biological evaluation of novel benzocoumarin derivatives as potent inhibitors of MAO-B activity

Inhibitory Effects of B-, C-, and E-Ring-Truncated Deguelin Derivatives Against A549, HCT116, and MCF-7 Cancer Cells

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