Bioassay-guided isolation of a diastereoisomer of kolavenol from Entada abyssinica active on Trypanosoma brucei rhodesiense.
Bioassay-guided fractionation of the dichloromethane rootbark extract of Entada abyssinica (Leguminosae), a plant used by traditional healers in Uganda for the treatment of sleeping sickness, led to the isolation of a diastereoisomer of the clerodane type diterpene kolavenol. This is the first report on this compound. It showed a trypanocidal activity with an IC50 value of 2.5 microg/ml (8.6 microM) against Trypanosoma brucei rhodesiense, the causing agent of the acute form of human African trypanosomiasis.
University of Berne, Department of Chemistry and Biochemistry, Switzerland.
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Freiburghaus
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Steck
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Pfander
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Brun
D000818:Animals; D001681:Biological Assay; D004224:Diterpenes / Q000302:isolation & purification* / Q000494:pharmacology; D007887:Fabaceae / Q000737:chemistry*; D016488:Medicine, African Traditional; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry; D010946:Plants, Medicinal; D013237:Stereoisomerism; D014344:Trypanocidal Agents / Q000302:isolation & purification* / Q000494:pharmacology; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects*
D004224:Diterpenes; D010936:Plant Extracts; D014344:Trypanocidal Agents; C114792:kolavenol