Activity of extracts and naphthoquinones from Kigelia pinnata against Trypanosoma brucei brucei and Trypanosoma brucei rhodesiense

S. V K Moideen, P. J. Houghton, P. Rock, S. L. Croft, F. Aboagye-Nyame

Research output: Contribution to journalArticle

48 Citations (Scopus)

Abstract

Dichloromethane extracts of the root bark and stern bark of Kigelia pinnata collected from Zimbabwe exhibited antitrypanosomal activity against Trypanosoma brucei brucei in vitro. Activity-guided fractionation led to the isolation of four naphthoquinones from both the root and stem bark of the plant. The compounds were identified as 2-(1-hydroxyethyl)naphtho[2,3- b]furan-4,9-quinone (1), isopinnatal (2), kigelinol (3), and isokigelinol (4). Subsequently, the compounds were assessed for antitrypanosomal activity against T. brucei brucei and T. brucei rhodesiense bloodstream form trypomastigotes in vitro. Compound 1 with a furanonaphthoquinone structure was found to possess pronounced activity against both parasites with IC50 values of 0.12 and 0.045 μM, respectively, although it was less active than the standard drug pentamidine. Compounds 2, 3, and 4 also exhibited activity against the parasites, although to a lesser extent. The activities of the compounds were further assessed by comparison with the cytotoxic activities obtained against KB cell lines.

Original languageEnglish
Pages (from-to)536-540
Number of pages5
JournalPlanta Medica
Volume65
Issue number6
DOIs
Publication statusPublished - 1999
Externally publishedYes

Fingerprint

Trypanosoma rhodesiense
Trypanosoma brucei rhodesiense
Trypanosoma brucei brucei
Naphthoquinones
naphthoquinones
bark
Pentamidine
Methylene Chloride
extracts
Parasites
Fractionation
Plant Bark
bloodstream forms
Plant Stems
trypomastigotes
KB Cells
parasites
Zimbabwe
furans
Cells

Keywords

  • 2-(1-hydroxyethyl)naphtho[2,3-b]furan-4,9- quinone
  • Antitrypanosomal activity
  • Bignoniaceae
  • Cytotoxicity assay
  • Isokigelinol
  • Isopinnatal
  • Kigelia pinnata
  • Kigelinol
  • Naphthoquinones

ASJC Scopus subject areas

  • Plant Science
  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

Cite this

Activity of extracts and naphthoquinones from Kigelia pinnata against Trypanosoma brucei brucei and Trypanosoma brucei rhodesiense. / Moideen, S. V K; Houghton, P. J.; Rock, P.; Croft, S. L.; Aboagye-Nyame, F.

In: Planta Medica, Vol. 65, No. 6, 1999, p. 536-540.

Research output: Contribution to journalArticle

Moideen, S. V K ; Houghton, P. J. ; Rock, P. ; Croft, S. L. ; Aboagye-Nyame, F. / Activity of extracts and naphthoquinones from Kigelia pinnata against Trypanosoma brucei brucei and Trypanosoma brucei rhodesiense. In: Planta Medica. 1999 ; Vol. 65, No. 6. pp. 536-540.
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