Anti-inflammatory, Antiplatelet Aggregation, and Antiangiogenesis Polyketides from Epicoccum sorghinum: Toward an Understating of Its Biological Activities and Potential Applications

Chi Ying Li, Ching Chia Chang, Yi Hong Tsai, Mohamed El-Shazly, Chin Chung Wu, Shih Wei Wang, Tsong Long Hwang, Chien Kei Wei, Judit Hohmann, Zih Jie Yang, Yuan Bin Cheng, Yang Chang Wu, Fang Rong Chang

Research output: Contribution to journalArticle

Abstract

The ethyl acetate extract of an endophyte Epicoccum sorghinum exhibited anti-inflammatory activity at a concentration of <10 μg/mL. By bioassay-guided fractionation, one new compound, named epicorepoxydon A (1), and one unusual bioactive compound, 6-(hydroxymethyl)benzene-1,2,4-triol (6), together with six known compounds, were isolated from E. sorghinum. The structures of all isolates were established by spectroscopic analyses. The relative configuration of 1 was deduced by the NOESY spectrum and its absolute configuration was determined by X-ray single-crystal analysis. The biological activities of all isolates were evaluated using four types of bioassays including cytotoxicity, anti-inflammatory, antiplatelet aggregation, and antiangiogenesis activities. Compounds 4 and 6 showed potent anti-inflammatory activity, compound 2 possessed potent antiplatelet aggregation and antiangiogenesis activities, and compound 6 demonstrated antiangiogenesis activity. This fungal species can cause a human hemorrhagic disorder known as onyalai. In this study, we identified the active components with antiplatelet aggregation and antiangiogenesis activities, which may be related to the hemorrhagic disorder caused by this fungus. Moreover, we proposed a biosynthetic pathway of the isolated polyketide secondary metabolites and investigated their structure-activity relationship (SAR). Our results suggested that E. sorghinum is a potent source of biologically active compounds that can be developed as antiplatelet aggregation and anti-inflammatory agents.

Original languageEnglish
Pages (from-to)11092-11099
Number of pages8
JournalACS Omega
Volume5
Issue number19
DOIs
Publication statusPublished - May 19 2020

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)

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    Li, C. Y., Chang, C. C., Tsai, Y. H., El-Shazly, M., Wu, C. C., Wang, S. W., Hwang, T. L., Wei, C. K., Hohmann, J., Yang, Z. J., Cheng, Y. B., Wu, Y. C., & Chang, F. R. (2020). Anti-inflammatory, Antiplatelet Aggregation, and Antiangiogenesis Polyketides from Epicoccum sorghinum: Toward an Understating of Its Biological Activities and Potential Applications. ACS Omega, 5(19), 11092-11099. https://doi.org/10.1021/acsomega.0c01000