The antiplasmodial activity of isolates from Ajuga remota.

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.

• Authors: Kimani A M Kuria, 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
• Journal: Journal of natural products (J Nat Prod) Vol. 65 Issue 5 Pg. 789-93 (May 2002) ISSN: 0163-3864 [Print] United States
• PMID: 12027771 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antimalarials
• Antineoplastic Agents
• Diterpenes
• ajugarin I
• Chloroquine
• L-Lactate Dehydrogenase
• Fluorouracil
• ergosterol-5,8-peroxide
• Ergosterol

Topics

• Animals
• Antimalarials (chemistry, isolation & purification, pharmacology)
• Antineoplastic Agents (chemistry, isolation & purification, pharmacology)
• Chloroquine (pharmacology)
• Chromatography, Thin Layer
• Diterpenes (chemistry, isolation & purification, pharmacology)
• Drug Resistance, Microbial (physiology)
• Drug Screening Assays, Antitumor
• Ergosterol (analogs & derivatives, chemical synthesis)
• Fluorouracil (pharmacology)
• Humans
• In Vitro Techniques
• Inhibitory Concentration 50
• Kenya
• L-Lactate Dehydrogenase (metabolism)
• Lamiaceae (chemistry)
• Plants, Medicinal (chemistry)
• Plasmodium falciparum (drug effects, enzymology, metabolism)
• Skin Neoplasms
• Tumor Cells, Cultured (drug effects)