Trypanocidal activity, cytotoxicity and histone modifications induced by malformin A1 isolated from the marine-derived fungus Aspergillus tubingensis IFM 63452

K. I. Notarte, Youichi Nakao, T. Yaguchi, M. Bungihan, K. Suganuma, T. E. dela Cruz

    Research output: Contribution to journalArticle

    2 Citations (Scopus)

    Abstract

    Malformin A1, a cyclic pentapeptide, was isolated from the marine-derived fungus Aspergillus tubingensis IFM 63452. The identity of the compound was established based on TOF-MS and 1H NMR data. Malformin A1 exhibited trypanocidal activity against Trypanosoma congolense (IC50: 15.08 ng/mL). Interestingly, the compound was selective for T. congolense rendering a selectivity index value that ranged from 3.33 to 4.67. It also demonstrated cytotoxicity against HeLa (IC50: 50.15 ng/mL) and P388 (IC50: 70.38 ng/mL) cell lines. To further identify the possible mechanism of its cytotoxic effect, immunofluorescence staining was conducted to follow the epigenetic changes induced by the compound in the amino acid lysine of histone H3 and H4 in HeLa. The compound induced repressive levels of H3K27me3, H3K27ac and H4K5ac, and enhanced levels of H3K9me2, H3K9me3 and H4K16ac supporting the compound's chemotherapeutic potential.

    Original languageEnglish
    Article number10
    JournalMycosphere
    Volume8
    Issue number1
    DOIs
    Publication statusPublished - 2017 Jan 1

    Fingerprint

    Aspergillus tubingensis
    histones
    Trypanosoma congolense
    inhibitory concentration 50
    nuclear magnetic resonance
    cytotoxicity
    amino acid
    fungus
    fungi
    rendering
    epigenetics
    fluorescent antibody technique
    lysine
    cell lines
    amino acids
    effect
    index

    Keywords

    • Bioactivities
    • Epigenetics
    • Fungal natural products
    • Marine fungi

    ASJC Scopus subject areas

    • Ecology, Evolution, Behavior and Systematics
    • Plant Science

    Cite this

    Trypanocidal activity, cytotoxicity and histone modifications induced by malformin A1 isolated from the marine-derived fungus Aspergillus tubingensis IFM 63452. / Notarte, K. I.; Nakao, Youichi; Yaguchi, T.; Bungihan, M.; Suganuma, K.; dela Cruz, T. E.

    In: Mycosphere, Vol. 8, No. 1, 10, 01.01.2017.

    Research output: Contribution to journalArticle

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