Abstract

Endophytes, living inside plant tissues, play an essential role in plant growth and development, whilst producing unique bioactive secondary metabolites. In the current study, the endophytic fungus Bipolaris sorokiniana LK12 was isolated from the leaves of ethno-medicinal and alkaloidal rich Rhazya stricta. The bulk amount of ethyl acetate extract of fungus was subjected to advance column chromatographic techniques, which resulted in the isolation of a new radicinol derivative, bipolarisenol (1). It was found to be a derivative of radicinol. The structure elucidation was carried out by the combined use of 1D and 2D nuclear magnetic resonance, infrared spectroscopy, mass, and UV spectrometric analyses. The bipolarisenol was assessed for its potential role in enzyme inhibition of urease and acetyl cholinesterase (AChE). Results showed that bipolarisenol significantly inhibited the AChE activity with low IC50 (67.23 ± 5.12 µg·mL−1). Bipolarisenol inhibited urease in a dose-dependent manner with high IC50 (81.62 ± 4.61 µg·mL−1). The new compound also showed a moderate anti-lipid peroxidation potential (IC50 = 168.91 ± 4.23 µg·mL−1). In conclusion, endophytes isolated from medicinal plants possess a unique potential to be considered for future drug discovery.

Highlights

  • Endophytic microbes live inside plant tissues without causing any symptoms of disease to the host

  • Since the host R. stricta was found rich in diverse kinds of secondary metabolites, we aimed to explore its symbiotic endophytic fungi for similar potentials

  • Initial screening results showed that the extract (100 ppm) possessed significantly higher anti-lipid peroxidation potential (51.28% ± 0.97%)

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Summary

Introduction

Endophytic microbes (bacteria and fungi) live inside plant tissues without causing any symptoms of disease to the host. Endophytic fungal association extends benefits to the plants by changing the endogenous mineral nutrients and metabolites levels [1]. During symbiosis, these endophytes produce metabolites inside plant tissues to help in the improvement of plant defenses against environmental stresses [2,3,4,5]. A previous study by Schulz et al [6] showed that about 51% of biologically active metabolites originate from endophytes compared to only 38% of novel substances originating from other soil microflora. In the past two decades, many novel bioactive compounds with antimicrobial, insecticidal, cytotoxic, and anticancer properties have been successfully isolated and characterized from endophytic fungi [4,7]

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