title: Cucurbitane-type compounds from Hemsleya carnosiflora antagonize ecdysteroid action in the Drosophila melanogaster BII cell line.
abstract: The ecdysteroid agonist and antagonist activities of 3 cucurbitanes, 2 cucurbitane glycosides and 2 cucurbitacins isolated from Hemsleya carnosiflora (Cucurbitaceae) have been determined in the Drosophila melanogaster BII bioassay. Carnosiflogenins A and C and carnosiflosides II and VI possess antagonistic activity. Carnosiflogenin A was also found to induce the formation of spindle-shaped cells with high frequency in both the agonist and antagonist assays. At 10(-3) M, carnosiflogenins B and C were cytotoxic, 23,24-Dihydrocucurbitacin F and 25-acetoxy-23,24-dihydrocucurbitacin F are also antagonistic at high concentrations. The concentration dependencies of the antagonistic activities of these two cucurbitacins, carnosiflosides II and VI and carnosiflogenin C are presented. The biological and ecological significance of these results are discussed in relationship to the concentrations present in the rhizomes of H. carnosiflora.
authors.affiliation: Department of Biological Sciences, University of Exeter, Washington Singer Laboratories, Devon, United Kingdom. l.n.dinan@exeter.ac.uk
authors.forename: L
authors.initials: L
authors.lastname: Dinan
authors.forename: P
authors.initials: P
authors.lastname: Whiting
authors.forename: S D
authors.initials: SD
authors.lastname: Sarker
authors.forename: R
authors.initials: R
authors.lastname: Kasai
authors.forename: K
authors.initials: K
authors.lastname: Yamasaki
mesh_terms: D000818:Animals; D001681:Biological Assay; D002460:Cell Line; D004331:Drosophila melanogaster; D026461:Ecdysteroids; D010936:Plant Extracts; D010944:Plants / Q000378:metabolism*; D013256:Steroids / Q000037:antagonists & inhibitors*; D014315:Triterpenes / Q000302:isolation & purification* / Q000494:pharmacology
chemical_list: D026461:Ecdysteroids; D010936:Plant Extracts; D013256:Steroids; D014315:Triterpenes