Daleformis, a new phytoalexin from the roots fo Dalea filiciformis: an inhibitor of endothelin converting enzyme.
As part of a search for novel inhibitors of endothelin converting enzyme (ECE), the MeOH-CH2Cl2 extract of the roots of Dalea filiciformis was shown to be active. Bioassay-guided fractionation of the extract yielded a novel phytoalexin, daleformis (1), whose structure was determined by interpretation of spectral data and X-ray analysis. Daleformis (1) inhibited ECE with an IC50 of 9 microM.
Patil
A D
AD
Department of Biomolecular Discovery and Analytical Sciences, SmithKline Beecham Pharmaceuticals, Research and Development, King of Prussia, Pennsylvania 19406-0939.
Freyer
A J
AJ
Eggleston
D S
DS
Haltiwanger
R C
RC
Tomcowicz
B
B
Breen
A
A
Johnson
R K
RK
D000107:Acetylation; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D001572:Benzofurans / Q000302:isolation & purification* / Q000494:pharmacology; D001578:Benzopyrans / Q000302:isolation & purification* / Q000494:pharmacology; D002855:Chromatography, Thin Layer; D018360:Crystallography, X-Ray; D000072396:Endothelin-Converting Enzymes; D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors*; D008968:Molecular Conformation; D018517:Plant Roots / Q000737:chemistry*; D010946:Plants, Medicinal / Q000737:chemistry*; D013055:Spectrophotometry, Infrared
D001572:Benzofurans; D001578:Benzopyrans; D004791:Enzyme Inhibitors; C105641:daleformis; D016282:Aspartic Acid Endopeptidases; D008666:Metalloendopeptidases; D000072396:Endothelin-Converting Enzymes