Title of article :
Pulchranin A, isolated from the Far-Eastern marine sponge, Monanchora pulchra: the first marine non-peptide inhibitor of TRPV-1 channels
Author/Authors :
Guzii، نويسنده , , Alla G. and Makarieva، نويسنده , , Tatyana N. and Korolkova، نويسنده , , Yuliya V. and Andreev، نويسنده , , Yaroslav A. and Mosharova، نويسنده , , Irina V. and Tabakmaher، نويسنده , , Ksenya M. and Denisenko، نويسنده , , Vladimir A. and Dmitrenok، نويسنده , , Pavel S. and Ogurtsova، نويسنده , , Ekaterina K. and Antonov، نويسنده , , Alexandr S. and Lee، نويسنده , , H، نويسنده ,
Abstract :
A new marine guanidine-containing compound, pulchranin A (1) was isolated from the marine sponge Monanchora pulchra. Its structure was elucidated by detailed NMR and MS analyses. The Mosher’s method did not allow determination of the absolute configuration of the carbinol center in 1, but after conversion of 1 into the bis-MTPA esters of 1,3-diol 2, the same method was successfully used to solve the problem. Compound 1 was active as an inhibitor of the TRPV1 receptor with an EC50 value of 41.2 μM.
Keywords :
Guanidine alkaloids , Sponge , absolute configuration , Monanchora pulchra , Inhibitor , TRPV1 channel
