Spongian diterpenes with thyrotropin releasing hormone receptor 2 binding affinity from Spongia sp.

Authors

Anthony R. Carroll
Jasmine Lamb, University of Notre Dame AustraliaFollow
Roger Moni
John N A Hooper
Ronald J. Quinn

Publication Details

Carroll, A. R., Lamb, J., Moni, R., Hooper, J. N. A., & Quinn, R. J. (2008). Spongian diterpenes with thyrotropin releasing hormone receptor 2 binding affinity from Spongia sp. Journal of Natural Products, 71(5), 884–886. doi:10.1021/np070658r

Abstract

High-throughput screening of a plant and marine invertebrate extract library to find natural products with rat thyrotropin releasing hormorne (TRH) receptor 2 binding affinity led to the isolation of four new (1−4) and one known (5) spongian diterpene from the sponge Spongia sp. The structures were assigned from interpretation of 2D NMR and high-resolution ESIMS data. The absolute configurations of 1−4 were proposed on the basis of analysis of their CD spectra. Diterpenes 1−5 showed rat TRH receptor 2 binding affinity with IC₅₀ values of 23 μM, 70 μM, 400 μM, 600 μM, and 1 mM, respectively.

Keywords

peer-reviewed