Cucurbitane-type compounds from Hemsleya carnosiflora antagonize ecdysteroid action in the Drosophila melanogaster B-11 cell line

被引：19

作者：

Dinan, L ^{[1
]}

Whiting, P ^{[1
]}

Sarker, SD ^{[1
]}

Kasai, R ^{[1
]}

Yamasaki, K ^{[1
]}

机构：

[1] HIROSHIMA UNIV,SCH MED,INST PHARMACEUT SCI,MINAMI KU,HIROSHIMA 734,JAPAN

来源：

CELLULAR AND MOLECULAR LIFE SCIENCES | 1997年 / 53卷 / 03期

关键词：

antagonist; Cucurbitaceae; cucurbitane; cucurbitacin; ecdysteroid; Hemsleya carnosflora; receptor; steroid hormone;

D O I：

10.1007/PL00000603

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 B-11 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.

引用

页码：271 / 274

页数：4

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