- New Derivatives of Natural Acyclic Guanidine Alkaloids with TRPV Receptor-Regulating Properties.
New Derivatives of Natural Acyclic Guanidine Alkaloids with TRPV Receptor-Regulating Properties.
Natural product communications (2015-09-29)
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
PMID26411002
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.