Dinan L, Bourne P C, Meng Y, Sarker S D, Tolentino R B, Whiting P
Department of Biological Sciences, University of Exeter, Devon, UK.
Cell Mol Life Sci. 2001 Feb;58(2):321-42. doi: 10.1007/PL00000859.
Ecdysteroid agonist and antagonist activities can be detected and quantified with the Drosophila melanogaster B(II) cell bioassay. This bioassay is convenient, sensitive and robust. We report the assessment with this bioassay of the activities of a wide range of compounds representing a number of classes of natural products. Many compounds were inactive over a wide concentration range (10(-8) to 10(-4) or 10(-3) M) or cytotoxic at high concentrations. However, antagonisitic activity was associated with several classes of compounds: cucurbitacins and withanolides (extending previous findings) and phenylalkanoids and certain alkaloids (described for the first time). A withanolide (withaperuvin D) is identified which possesses agonistic activity. Brassinosteroids, which have been ascribed (ant)agonistic properties in the past, were not found to be active in the B(II) bioassay, either as agonists or antagonists. Possible reasons for the prevalence of antagonists and for the low potency of the majority of them are discussed.
蜕皮甾类激动剂和拮抗剂活性可用黑腹果蝇B(II)细胞生物测定法进行检测和定量。这种生物测定法方便、灵敏且可靠。我们报告了用这种生物测定法对代表多种天然产物类别的一系列化合物的活性进行的评估。许多化合物在很宽的浓度范围（10^(-8)至10^(-4)或10^(-3) M）内无活性，或在高浓度下具有细胞毒性。然而，拮抗活性与几类化合物有关：葫芦素和醉茄内酯（扩展了先前的发现）以及苯烷类化合物和某些生物碱（首次描述）。鉴定出一种具有激动活性的醉茄内酯（withaperuvin D）。过去被认为具有（抗）激动特性的油菜素甾醇类化合物，在B(II)生物测定法中未发现有活性，无论是作为激动剂还是拮抗剂。讨论了拮抗剂普遍存在以及大多数拮抗剂效力较低的可能原因。
