| Literature DB >> 12027771 |
Kimani A M Kuria1, 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.
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.Entities:
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Year: 2002 PMID： 12027771 DOI： 10.1021/np0104626
Source DB: PubMed Journal: J Nat Prod ISSN： 0163-3864 Impact factor: 4.050