Lu Yu-Cheng, Chen Hwei-Hsien, Ko Chien-Hsin, Lin Yi-Ruu, Chan Ming-Huan
Department of Pharmacy, Buddhist Dalin Tzu Chi General Hospital, Chia Yi, Taiwan.
Naunyn Schmiedebergs Arch Pharmacol. 2003 Oct;368(4):262-9. doi: 10.1007/s00210-003-0802-8. Epub 2003 Sep 18.
The effects of honokiol and magnolol extracted from the Magnolia officinalis on muscular contractile responses and intracellular Ca(2+) mobilization were investigated in the non-pregnant rat uterus. Honokiol and magnolol (1-100 micromol/l) were observed to inhibit spontaneous and uterotonic agonists (carbachol, PGF(2alpha), and oxytocin)-, high K(+)-, and Ca(2+) channel activator (Bay K 8644)-induced uterine contractions in a concentration-dependent manner. The inhibition rate of honokiol on spontaneous contractions appeared to be slower than that of magnolol-induced response. The time periods that were required for honokiol and magnolol, at 100 micromol/l, to abolish 50% spontaneous contractions were approximately 6 min. Furthermore, honokiol and magnolol at 10 micromol/l also blocked the Ca(2+)-dependent oscillatory contractions. Consistently, the increases in intracellular Ca(2+) concentrations (Ca(2+)) induced by PGF(2alpha) and high K(+) were suppressed by both honokiol and magnolol at 10 micromol/l. After washout of these treatments, the rise in Ca(2+) induced by PGF(2alpha) and high K(+) was still partially abolished. In conclusion, the inhibitory effects of honokiol and magnolol on uterine contraction may be mediated by blockade of external Ca(2+) influx, leading to a decrease in Ca(2+). Honokiol and magnolol may be considered as putative Ca(2+) channel blockers and be of potential value in the treatment of gynecological dysfunctions associated with uterine muscular spasm and dysmenorrhea.
研究了从厚朴中提取的和厚朴酚与厚朴酚对未孕大鼠子宫肌肉收缩反应及细胞内钙离子动员的影响。观察到和厚朴酚与厚朴酚（1 - 100微摩尔/升）以浓度依赖的方式抑制自发的以及子宫收缩剂（卡巴胆碱、前列腺素F2α和催产素）、高钾和钙离子通道激活剂（Bay K 8644）诱导的子宫收缩。和厚朴酚对自发收缩的抑制率似乎比厚朴酚诱导的反应要慢。100微摩尔/升的和厚朴酚与厚朴酚消除50%自发收缩所需的时间约为6分钟。此外，10微摩尔/升的和厚朴酚与厚朴酚也阻断了钙离子依赖性振荡收缩。同样，10微摩尔/升的和厚朴酚与厚朴酚均抑制了由前列腺素F2α和高钾诱导的细胞内钙离子浓度（[Ca2+]i）升高。在洗脱这些处理后，由前列腺素F2α和高钾诱导的[Ca2+]i升高仍部分被消除。总之，和厚朴酚与厚朴酚对子宫收缩的抑制作用可能是通过阻断细胞外钙离子内流介导的，导致[Ca2+]i降低。和厚朴酚与厚朴酚可被视为假定的钙离子通道阻滞剂，在治疗与子宫肌肉痉挛和痛经相关的妇科功能障碍方面可能具有潜在价值。
