Cucurbitacins, cell adhesion inhibitors from Conobea scoparioides.
In the course of screening natural products for antagonists of CD18-mediated cell adhesion, an extract with inhibitory activity was identified from the stem and leaves of Conobea scoparioides. Bioassay-guided fractionation led to a pure compound, identified by spectroscopy as cucurbitacin E [1]. Although many biological activities have been reported for the cucurbitacins, this is the first report of cell adhesion inhibition. Furthermore, closely related cucurbitacin analogues had different potencies, pointing to substructural features that are important for the activity.
Sterling Winthrop Pharmaceuticals Research Division, Malvern, Pennsylvania 19355.
L L
LL
Musza
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P
Speight
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McElhiney
C J
CJ
Barrow
A M
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Gillum
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Cooper
L M
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Killar
D000199:Actins / Q000187:drug effects / Q000378:metabolism; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D002448:Cell Adhesion / Q000187:drug effects*; D002455:Cell Division / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002634:Chemotaxis, Leukocyte / Q000187:drug effects; D054728:Cucurbitacins; D006367:HeLa Cells; D006801:Humans; D066298:In Vitro Techniques; D018799:Intercellular Adhesion Molecule-1 / Q000494:pharmacology; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000494:pharmacology; D009504:Neutrophils / Q000187:drug effects / Q000502:physiology; D010936:Plant Extracts / Q000494:pharmacology*; D013936:Thymidine / Q000378:metabolism; D014197:Trees; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*
D000199:Actins; D000972:Antineoplastic Agents, Phytogenic; D010936:Plant Extracts; D014315:Triterpenes; D018799:Intercellular Adhesion Molecule-1; D009240:N-Formylmethionine Leucyl-Phenylalanine; D054728:Cucurbitacins; D013936:Thymidine