Suzuki T, Kobayashi Y, Uchida M K, Sakakibara I, Okuyama T, Shibata S
J Pharmacobiodyn. 1985 Apr;8(4):257-63. doi: 10.1248/bpb1978.8.257.
The effects of coumarins on anaphylactic mediator release from rat mast cells were investigated. Since Pd-Ia (3'-angeloyloxy-4'-acetoxy-3',4'-dihydroseselin) causes relaxation of smooth muscle by inhibiting calcium influx, and since mediator release is a calcium-dependent process, studies were made on whether coumarins block calcium influx into rat mast cells stimulated by concanavalin A. Pd-Ia isolated from Peucedanum praeruptorum Dunn and related compounds, named Pd-C-II, Pd-C-III and Pd-C-IV, from Peucedanum decursivum Maxim., (Angelica decursiva Fr. et Sav.) inhibited anaphylactic mediator release from purified mast cells induced by concanavalin A with phosphatidylserine; their IC50 values were 79, 100, 102 and 73 microM, respectively. Pd-III, decursidin and water-soluble analogues of Pd-Ia (Pd-Ia-OH, Pd-Ia-OCH2CH3) did not inhibit the release. Thus the inhibitory actions of coumarins on calcium influx seemed to depend on the chemical structures of these compounds; an acetoxyl residue at position 3' or 4' on the seselin or xanthyletin skeleton might be essential for an inhibitory effect. Furthermore, Pd-Ia and Pd-C-III caused more than 40% reduction in 45Ca uptake induced by concanavalin A, whereas decursidin had little effect on it. Therefore, the inhibitions of mediator release of mast cells by some of coumarins from "Qian-Hu" seem to depend on their effects in blocking calcium influx.
研究了香豆素对大鼠肥大细胞过敏介质释放的影响。由于Pd-Ia（3'-当归酰氧基-4'-乙酰氧基-3'，4'-二氢水合芹素）通过抑制钙内流引起平滑肌松弛，且介质释放是一个钙依赖性过程，因此研究了香豆素是否能阻断伴刀豆球蛋白A刺激下钙流入大鼠肥大细胞。从白花前胡中分离得到的Pd-Ia以及从紫花前胡（当归紫花变种）中得到的相关化合物Pd-C-II、Pd-C-III和Pd-C-IV，抑制了伴刀豆球蛋白A与磷脂酰丝氨酸诱导的纯化肥大细胞过敏介质的释放；它们的IC50值分别为79、100、102和73μM。Pd-III、紫花前胡素以及Pd-Ia的水溶性类似物（Pd-Ia-OH、Pd-Ia-OCH2CH3）未抑制释放。因此，香豆素对钙内流的抑制作用似乎取决于这些化合物的化学结构；水合芹素或黄嘌呤骨架上3'或4'位的乙酰氧基残基可能对抑制作用至关重要。此外，Pd-Ia和Pd-C-III使伴刀豆球蛋白A诱导的45Ca摄取减少了40%以上，而紫花前胡素对此几乎没有影响。因此，“前胡”中一些香豆素对肥大细胞介质释放的抑制作用似乎取决于它们阻断钙内流的作用。
