2. Academic Validation
  3. The antiplasmodial activity of isolates from Ajuga remota

The antiplasmodial activity of isolates from Ajuga remota

  • J Nat Prod. 2002 May;65(5):789-93. doi: 10.1021/np0104626.
Kimani A M Kuria 1,  Hezekiah Chepkwony,  Cindy Govaerts,  Eugene Roets,  Roger Busson,  Peter De Witte,  Istvan Zupko,  Georges Hoornaert,  Ludo Quirynen,  Louis Maes,  Leen Janssens,  Jos Hoogmartens,  Gert Laekeman
Affiliations

Affiliation

  • 1 Faculty of Pharmacy, University of Nairobi, P.O. Box 19676, Nairobi, Kenya.
PMID: 12027771 DOI: 10.1021/np0104626
Abstract

Ajuga remota is the most frequently used medicinal herb for malaria treatment in Kenya. Its two known isolates ajugarin-1 (1) and ergosterol-5,8-endoperoxide (3) and a new isolate 8-O-acetylharpagide (2) were evaluated for their in vitro antiplasmodial activity. Ajugarin-1 was moderately active, with an IC(50) of 23.0 +/- 3.0 microM, as compared to chloroquine (IC(50) = 0.041 +/- 0.003 microM) against the chloroquine-sensitive (FCA 20/GHA) strain of Plasmodium falciparum. Ergosterol-5,8-endoperoxide was about 3x as potent (IC(50) = 8.2 +/- 1.1 microM), while 8-O-acetylharpagide, whose structure was established by spectroscopic evidence, was inactive. Both ajugarin-1 and ergosterol-5,8-endoperoxide did not exhibit cytotoxicity against A431 (skin carcinoma) cell line, but 8-O-acetylharpagide was significantly cytotoxic. This iridoid glucoside, which has been formerly isolated from Ajuga decumbens, was identified in A. remota for the first time.

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