New Derivatives of Natural Acyclic Guanidine Alkaloids with TRPV Receptor-Regulating Properties.
NATURAL PRODUCT COMMUNICATIONS(2015)
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 mu M, respectively. Hexadecylguanidine (3) was not active against these receptors.
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Key words
Acyclic guanidine alkaloids,Structure-activity relationships,Sponge,Monanchora pulchra,rTRPV1,hTRPV3,rTRPA1
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