Article Title

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


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.



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