Anti-malarial drug targets: Screening for inhibitors of 2C-methyl-d-erythritol 4-phosphate synthase (IspC protein) in Mediterranean plants

J. Kaiser, M. Yassin, S. Prakash, N. Safi, M. Agami, S. Lauw, E. Ostrozhenkova, A. Bacher, F. Rohdich, W. Eisenreich, J. Safi, A. Golan-Goldhirsh

    Research output: Contribution to journalArticlepeer-review

    19 Scopus citations

    Abstract

    The recently discovered non-mevalonate pathway of isoprenoid biosynthesis serves as the unique source of terpenoids in numerous pathogenic eubacteria and in apicoplast-type protozoa, most notably Plasmodium, but is absent in mammalian cells. It is therefore an attractive target for anti-infective chemotherapy. The first committed step of the non-mevalonate pathway is catalyzed by 2C-methyl-d-erythritol 4-phosphate synthase (IspC). Using photometric and NMR spectroscopic assays, we screened extracts of Mediterranean plants for inhibitors of the enzyme. Strongest inhibitory activity was found in leaf extracts of Cercis siliquastrum.

    Original languageEnglish
    Pages (from-to)242-249
    Number of pages8
    JournalPhytomedicine
    Volume14
    Issue number4
    DOIs
    StatePublished - 10 Apr 2007

    Keywords

    • Antibiotic
    • Cercis siliquastrum
    • Deoxyxylulose inhibitors of 2C-methyl-D-erythritol 4-phosphate sythase (IspCprotein)
    • Malaria
    • Terpene

    ASJC Scopus subject areas

    • Molecular Medicine
    • Pharmacology
    • Pharmaceutical Science
    • Drug Discovery
    • Complementary and alternative medicine

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