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 IC(50) values of 23 microM, 70 microM, 400 microM, 600 microM, and 1 mM, respectively.
Carroll
Anthony R
AR
Eskitis Institute, Griffith University, Brisbane, Queensland, Australia.
Lamb
Jasmine
J
Moni
Roger
R
Hooper
John N A
JN
Quinn
Ronald J
RJ
D000818:Animals; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009792:Oceans and Seas; D011161:Porifera / Q000737:chemistry*; D051381:Rats; D018025:Receptors, Thyrotropin-Releasing Hormone / Q000819:agonists*
D004224:Diterpenes; D018025:Receptors, Thyrotropin-Releasing Hormone