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Xiaoqin Yu1, Werner E G Müller2, Zhiyong Guo3

  • 1Institute of Pharmaceutical Biology and Biotechnology, Heinrich-Heine-University Düsseldorf, Universitätsstrasse 1, 40225 Düsseldorf, Germany; Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, People's Republic of China.

Fitoterapia
|May 11, 2019
PubMed
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Researchers discovered five new indole alkaloids, okaramines V-Z, from the fungus Aphanoascus fulvescens. Some compounds exhibited significant cytotoxicity against mouse lymphoma cells, suggesting potential therapeutic applications.

Area of Science:

  • Mycology
  • Natural Product Chemistry
  • Pharmacology

Background:

  • The Ascomycete fungus Aphanoascus fulvescens, found in goose dung, is a source of biologically active secondary metabolites.
  • Indole alkaloids represent a diverse class of natural products with a wide range of pharmacological activities.

Purpose of the Study:

  • To isolate and characterize new secondary metabolites from Aphanoascus fulvescens.
  • To evaluate the cytotoxic potential of the isolated compounds against a mouse lymphoma cell line.

Main Methods:

  • Chemical investigation of the fungal extract using chromatographic techniques.
  • Structure elucidation of new compounds employing 1D and 2D Nuclear Magnetic Resonance (NMR) spectroscopy and High-Resolution Mass Spectrometry (HRMS).
  • Cytotoxicity assays using the L5178Y mouse lymphoma cell line to determine IC50 values.
Keywords:
Aphanoascus fulvescensCytotoxicityIndole alkaloidsOkaramine

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Main Results:

  • Five new indole alkaloids, designated okaramines V-Z (1-5), along with eleven known derivatives (6-16), were identified.
  • Compounds 6, 8, 11, and 12 demonstrated significant to moderate cytotoxicity against L5178Y cells, with IC50 values ranging from 4.0 to 14.7 μM.
  • Preliminary structure-activity relationship (SAR) analysis was performed.

Conclusions:

  • Aphanoascus fulvescens produces a variety of indole alkaloids with notable cytotoxic properties.
  • The identified compounds, particularly okaramines 6, 8, 11, and 12, warrant further investigation for their potential as anticancer agents.
  • This study expands the knowledge of secondary metabolites from fungal sources and their biological activities.