Kobayashi S, Mimura Y, Naitoh T, Kimura I, Kimura M
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Japan.
Jpn J Pharmacol. 1993 Nov;63(3):353-9. doi: 10.1254/jjp.63.353.
Inhibitory effects of cnidium rhizome-derived phthalides on competence and progression phases of fetal bovine serum (10%)-induced proliferation were compared in primary cultures of mouse aorta smooth muscle cells (SMC). Their potencies for the competence inhibition were in the order of senkyunolide L ((Z)-6-hydroxy-7-chloro-6,7-dihydroligustilide) > senkyunolide H ((Z)-6,7-dihydroxy-6,7-dihydroligustilide) > senkyunolide J ((3S)-(E)-6,7-dihydroxy-3,6,7,8-tetrahydroligustilide) > senkyunolide I ((E)-6,7-dihydroxy-6,7-dihydroligustilide) > ligustilide = senkyunolide A ((3S)-3,8-dihydroligustilide) > butylidenephthalide. The order of their potencies for the progression inhibition was parallel with that for the competence inhibition. Senkyunolide L is considered to have been formed during the extraction of cnidium. These results demonstrate that the (Z)-6,7-dihydroxy isomer of the dihydroligustilide derivatives is essential for the anti-competent effect on proliferation of the SMC in primary culture. Senkyunolide H in cnidium rhizome may be a prototype for a new anti-atherosclerotic drug.
在小鼠主动脉平滑肌细胞（SMC）原代培养中，比较了蛇床子根茎衍生的苯酞类化合物对胎牛血清（10%）诱导增殖的起始期和进展期的抑制作用。它们对起始期抑制的效力顺序为：蛇床子内酯L（(Z)-6-羟基-7-氯-6,7-二氢藁本内酯）>蛇床子内酯H（(Z)-6,7-二羟基-6,7-二氢藁本内酯）>蛇床子内酯J（(3S)-(E)-6,7-二羟基-3,6,7,8-四氢藁本内酯）>蛇床子内酯I（(E)-6,7-二羟基-6,7-二氢藁本内酯）>藁本内酯 = 蛇床子内酯A（(3S)-3,8-二氢藁本内酯）>丁烯基苯酞。它们对进展期抑制的效力顺序与对起始期抑制的顺序平行。蛇床子内酯L被认为是在蛇床子提取过程中形成的。这些结果表明，二氢藁本内酯衍生物的(Z)-6,7-二羟基异构体对原代培养的SMC增殖的抗起始期作用至关重要。蛇床子根茎中的蛇床子内酯H可能是一种新型抗动脉粥样硬化药物的原型。
