The effects of 15 lignan compounds, which were extracted from schisandra fruits, on the contractions of an isolated mesenteric artery of dog induced by prostaglandin F2α (PGF2α), CaCl2 or norepinephrine (NE) were examined. As a result, all lignan compounds used showed inhibitory effects on the contractions of mesenteric artery induced by PGF2α and CaCl2. However, 6 compounds such as gomisin J (GJ) also showed inhibitory effects on NE-induced contraction. We further examined the actions of GJ with much better activity. Since GJ is not soluble in water, we synthesized GJ-Na (GJN) and further used throughout the experiments. In the isolated mesenteric artery of dog, GJN showed inhibitory effects on the NE-induced contraction (ID50=131.8±0.11×10-6 M), and relaxant effects on PGF2α-induced contractions (ED50=9.72±0.36×10-6 M), and also showed inhibitory effects on CaCl2-induced contraction (ID50=6.96±0.16×10-6 M). Furthermore, GJN showed relaxant effects and an increase in coronary flow on the isolated trachea, ileum, taenia coli and heart in guinea-pigs, GJ (10-4 and 3×10-4 g, i.a.) produced an increase in coronary artery blood flow in anesthetized dog, although its effect was slightly weaker than that in diltiazem, a well known calcium antagonist. As mentioned above, it was confirmed that lignan compounds extracted from schisandra fruits had Ca antagonistic actions in varying degrees, and that GJN had a dilating effect on the coronary artery.
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Suekawa et al. (1987) studied this question.