Auclair M C, Adolphe M, Guillou Y, Robin Y
C R Seances Soc Biol Fil. 1976;170(1):65-70.
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.
从星虫中提取的两种新型生物胍类化合物，phascoline [N-(3-胍基丙酰基)-2-羟基正庚胺] 和phascolosomine [N-(3-胍基异丁酰基)-2-甲氧基正庚胺]，已对其对培养的大鼠心脏细胞的作用进行了测试。发现两种化合物在浓度大于或等于10(-3) M时会使细胞停止跳动，phascolosomine在30分钟后观察到这种作用，phascoline在24小时后观察到这种作用。在10(-4) M浓度下，相同的化合物不会使心跳停止，但在接触24小时后会使节律减慢。用phascoline和phascolosomine的水解产物进行的测定，前者为β-胍基丙酸和2-羟基庚胺，后者为β-胍基异丁酸和2-甲氧基正庚胺，结果表明生物活性位于分子的氨基醇或氨基醚部分。已发现，在浓度小于或等于10(-3) M时，对培养的大鼠心脏细胞的作用是可逆的。
