[Effect of phascoline and phascolosomine, new natural guanide derivatives, on cultured rat cardiac cells].
Two new biological guanido compounds from sipunculid worms, phascocoline [N-(3-guanidinopropionyl)-2-hydroxy-n-heptylamine] and phascolosomine [N-(3-guanidinoisobutyryl)-2-methoxy-n-heptylamine], have been tested for their effect on cultured rat heart cells. Both compounds were found to stop the beating of the cells at concentrations greater than or equal 10(-3) M, the effect being observed after 30 minutes for phascolosomine and after 24 hours for phascoline. At 10(-4) M concentration, the same compounds did not stop the beats but slowed the rhythm after 24 hours of contact. Assays performed with the hydrolysis products of phascoline and phascolosomine, beta-guanidinopropionic acid and 2-hydroxyheptylamine for the former, and beta-guanidinoisobutyric acid and 2-methoxy-n-heptylamine for the latter, have shown that the biological activity is located in the aminoalcool or aminoether moiety of the molelcule. It has been found that the effect on cultured rat heart cells was reversible at concentrations less than or equal 10(-3) M.
D000818:Animals; D002478:Cells, Cultured; D006146:Guanidines / Q000494:pharmacology*; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D009200:Myocardial Contraction / Q000187:drug effects*; D051381:Rats; D013997:Time Factors
D006146:Guanidines
Effet de la phascoline et de la phascolosomine, nouveaux dérivés guanidiques naturels, sur les cellules cardiaques de rat en culture