Dinan L, Whiting P, Sarker S D, Kasai R, Yamasaki K
Department of Biological Sciences, University of Exeter, Washington Singer Laboratories, Devon, United Kingdom.
Cell Mol Life Sci. 1997 Mar;53(3):271-4. doi: 10.1007/pl00000603.
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.
在果蝇BII生物测定中，已测定了从肉花雪胆（葫芦科）中分离出的3种葫芦素、2种葫芦素糖苷和2种葫芦素的蜕皮甾类激动剂和拮抗剂活性。雪胆黄素A和C以及雪胆苷II和VI具有拮抗活性。在激动剂和拮抗剂试验中，还发现雪胆黄素A能高频诱导纺锤形细胞的形成。在10⁻³ M时，雪胆黄素B和C具有细胞毒性，23,24-二氢葫芦素F和25-乙酰氧基-23,24-二氢葫芦素F在高浓度时也具有拮抗作用。给出了这两种葫芦素、雪胆苷II和VI以及雪胆黄素C拮抗活性的浓度依赖性。结合肉花雪胆根茎中的浓度，讨论了这些结果的生物学和生态学意义。
