The bioactivity of novel furanoterpenoids isolated from Siphonochilus aethiopicus.
OBJECTIVE
This study investigated the medicinal plant Siphonochilus aethiopicus (Zingiberaceae) for antiplasmodial activity.


METHODS
The ethyl acetate extract of Siphonochilus aethiopicus rhizomes was fractionated using solid phase extraction (SPE) and purified by high performance liquid chromatography. Structure elucidation was performed with nuclear magnetic resonance and mass spectrometry. The in vitro cytotoxicity and antiplasmodial activity was determined. In vivo schizontocidal activity was performed in a malaria mouse-model. Additional in vitro testing was done against Staphylococcus aureus, Klebsiella pneumoniae and Mycobacterium tuberculosis.


CONCLUSIONS
The ethyl acetate extract showed in vitro activity against the chloroquine-sensitive (CQS) and chloroquine-resistant (CQR) strains of Plasmodium falciparum with IC(50)-values of 2.9 microg/ml and 1.4 microg/ml, respectively. Bioassay-guided fractionation led to the isolation of three novel furanoterpenoids with moderate in vitro antiplasmodial activity. The crude extract showed very good in vivo activity. The compounds and crude extract were more active against the CQR strain than the CQS strain of Plasmodium falciparum. The SPE fractions were more active than the isolated compounds. The compounds did not show good activity against the micro-organisms tested. No in vitro cytotoxicity was observed.


CONCLUSIONS
This study provides evidence of antiplasmodial compounds present in Siphonochilus aethiopicus.
Lategan
Carmen A
CA
Division of Pharmacology, Department of Medicine, University of Cape Town, K-45 OMB GSH, Observatory 7925, South Africa.
Campbell
William E
WE
Seaman
Tracy
T
Smith
Peter J
PJ
D000818:Animals; D000900:Anti-Bacterial Agents / Q000302:isolation & purification / Q000494:pharmacology; D000935:Antifungal Agents / Q000302:isolation & purification / Q000494:pharmacology; D000962:Antimalarials / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D016466:CHO Cells; D002738:Chloroquine / Q000494:pharmacology; D006224:Cricetinae; D003412:Cricetulus; D005663:Furans / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D020128:Inhibitory Concentration 50; D016778:Malaria, Falciparum / Q000188:drug therapy*; D051379:Mice; D008810:Mice, Inbred C57BL; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry; D018517:Plant Roots / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects; D013729:Terpenes / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D030521:Zingiberaceae / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000962:Antimalarials; D005663:Furans; D010936:Plant Extracts; D013729:Terpenes; D002738:Chloroquine