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Cellular and Molecular Life Sciences CMLS

, Volume 58, Issue 2, pp 321–342 | Cite as

Assessment of natural products in the Drosophila melanogaster BII cell bioassay for ecdysteroid agonist and antagonist activities

  • L. Dinan*
  • P. C. Bourne
  • Y. Meng
  • S. D. Sarker**
  • R. B. Tolentino
  • P. Whiting

Abstract.

Ecdysteroid agonist and antagonist activities can be detected and quantified with the Drosophila melanogaster BII 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 BII 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.

Key words. Agonist; alkaloid; antagonist; bioassay; brassinosteroid; cucurbitacin; ecdysteroid; limonoid; phenylalkanoid; receptor; steroid hormone; triterpenoid; withanolide. 

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Copyright information

© Birkhäuser Verlag Basel, 2001

Authors and Affiliations

  • L. Dinan*
    • 1
  • P. C. Bourne
    • 1
  • Y. Meng
    • 1
  • S. D. Sarker**
    • 1
  • R. B. Tolentino
    • 1
  • P. Whiting
    • 1
  1. 1.Department of Biological Sciences, University of Exeter, Hatherly Laboratories, Prince of Wales Road, Exeter, Devon, EX4 4PS (UK), Fax +44 1392 263700, e-mail: l.n.dinan@exeter.ac.uk GB

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