Abstract

During a screening for antifungal secondary metabolites, six new mono-/bis-alkenoic acid derivatives (2–7) and one known alkenoic acid derivative (1) were isolated from an endophytic fungi Scopulariopsis candelabrum. Their chemical structures were identified by 1H-NMR, 13C-NMR, 2D NMR, and high-resolution mass spectrometry, as well as comparisons with previously reported literatures. Among them, fusariumesters C‒F (2–5) are bis-alkenoic acid derivatives dimerized by an ester bond, while acetylfusaridioic acid A (6) and fusaridioic acid D (7) are alkenoic acid monomers. All the isolates were submitted to an antifungal assay against Candida albicans and the corn pathogen Exserohilum turcicum using the filter paper agar diffusion method. As a result, only compound 1 decorating with β-lactone ring turned out to be active against these two tested fungi. The broth microdilution assay against Candida albicans showed the minimum inhibitory concentration (MIC) value of 1 to be 20 μg/ml, while the minimum inhibitory concentration value of the positive control (naystatin) was 10 μg/ml. And the half maximal inhibitory concentration (IC50) value (21.23 μg/ml) of 1 against Exserohilum turcicum was determined by analyzing its inhibition effect on the mycelial growth, using cycloheximide (IC50 = 46.70 μg/ml) as the positive control.

Highlights

  • Candida albicans, as an opportunistic pathogenic fungus, normally maintain symbiosis with the human body in the skin, oral cavity, and gastrointestinal tract (Mishra and Koh, 2021)

  • Four hundred thousand people are infected with C, albicans every year, and 75% of women suffer from vulvovaginal candidiasis at least once in their lives (Fidel et al, 2004; Yang et al, 2014; Rajendran et al, 2016)

  • Most of the alkenoic acid derivatives are acyclic, and seven of them are decorating with terminal lactone rings, including β-lactone, c-lactone, and δ-lactone

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Summary

Introduction

As an opportunistic pathogenic fungus, normally maintain symbiosis with the human body in the skin, oral cavity, and gastrointestinal tract (Mishra and Koh, 2021). The fatality rate of invasive C. albicans infection is still close to 40% (Lohse et al, 2018; Whitesell et al, 2019). Among immunocompromised people such as chemotherapy and organ transplantation, the mortality rate of Fungal Mono-/Bis-Alkenoic Acid Derivatives fungal diseases caused by C. albicans is 33–50% (Krcmery et al, 2000; Winston, 1999; Levesque et al, 2015). Infections caused by C. albicans are still nonnegligible threats to human health

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