Certain withanolides from Iochroma gesnerioides antagonize ecdysteroid action in a Drosophila melanogaster cell line |
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| Authors: | Laurence Dinan, Pensri Whiting, Dorothé e Alfonso Ilias Kapetanidis |
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| Affiliation: | (1) Department of Biological Sciences, University of Exeter, Washington Singer Laboratories, Perry Road, EX4 4QG Exeter, Devon, UK;(2) Laboratoire de Pharmacognosie, Université de Genève, 30 Quai Ernest-Ansermet, CH-1211 Geneva 4, Switzerland;(3) Present address: MDCH/PCOG, School of Pharmacy, Purdue University, 47907 West Lafayette, IN, USA |
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| Abstract: | Sixteen withanolides isolated from Iochroma gesnerioides (Kunth) Miers (Solanaceae) have been assessed for their activities as ecdysteroid agonists and antagonists. None of the compounds showed any agonistic activity, but several showed significant antagonistic activity. With a 20-hydroxyecdysone concentration of 5 × 10–8 M, the ED50 values for 2,3-dihydro-3 -methoxywithaferin A, 2,3-dihydro-3-methoxywithacnistine, 2,3-dihydro-3-methoxyiochromolide and 2,3-dihydro-3-hydroxywithacnistine are 3.5 × 10-5 M, 1 × 10–5 M, 5 × 10–6 M and 2.5 × 10–6 M, respectively. |
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| Keywords: | antagonist bioassay ecdysteroid HPLC steroid hormone receptor withanolide |
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