New Derivatives of Natural Acyclic Guanidine Alkaloids with TRPV Receptor-Regulating Properties.

Ekaterina K Ogurtsova, Tatyana N Makarieva, Yuliya V Korolkova, Yaroslav A Andreev, Irina V Mosharova, Vladimir A Denisenko, Pavel S Dmitrenok, Yeon-Ju Lee, Eugene V Grishin, Valentin A Stonik

Index: Nat. Prod. Commun. 10 , 1171-3, (2015)

Full Text: HTML

Abstract

The guanidine alkaloids, dihydropulchranin A (2), prepared from pulchranin A from the sponge Monanchora pulchra, and hexadecylguanidine (3), a synthetic analog of pulchranins, were studied for their TRPV channel-regulating activities. Compound 2 was active as an inhibitor of rTRPV1 and hTRPV3 receptors with EC50 values of 24.3 and 59.1 μM, respectively. Hexadecylguanidine (3) was not active against these receptors.