School of Chemistry and Chemical Engineering, Jiangsu University, Zhenjiang 212013, China.
J Ethnopharmacol. 2011 May 17;135(2):325-9. doi: 10.1016/j.jep.2011.03.016. Epub 2011 Mar 21.
Rhizoma Pinelliae Praeparatum is the product of raw Rhizoma Pinellia processed with alkaline solution and Licorice, which had been widely used for treatment of insomnia in traditional Chinese medicine. The present study aimed to investigate the sedative, hypnotic and anticonvulsant activities of ethanol fraction from Rhizoma Pinelliae Praeparatum (EFRP) and to determine whether these effects were related to GABAergic mechanism.
The sedative, hypnotic and anticonvulsant activities of EFRP were investigated with locomotion activity, pentobarbital-induced sleeping and nikethamide (NKTM)-induced convulsion tests, respectively. Additionally, the effects of flumazenil (an antagonist of GABA(A) receptor) and L-malic acid (blocker of synthetic enzyme for GABA) on the hypnotic activity of EFRP were evaluated.
EFRP at dose of 12 g/kg significantly inhibited the locomotion activity of mice. EFRP showed synergic effect on pentobarbital-induced sleeping by increased numbers of mice falling asleep, reduced the sleep latency and prolonged the sleeping time. L-malic acid and flumazenil inhibited the augment effects of EFRP on pentobarbital-induced sleeping. EFRP promoted a significant protection to NKTM-induced convulsion, by prolonged the death latency and decreased mortality.
EFRP possessed sedative, hypnotic and anticonvulsant activities and these activities may be related to the GABAergic system.
制半夏是由生半夏经碱性溶液和甘草加工而成的产物，在中医中被广泛用于治疗失眠。本研究旨在探讨制半夏乙醇提取物（EFRP）的镇静、催眠和抗惊厥活性，并确定这些作用是否与 GABA 能机制有关。
采用运动活性、戊巴比妥钠诱导睡眠和烟酰胺（NKTM）诱导惊厥试验分别研究 EFRP 的镇静、催眠和抗惊厥活性。此外，还评估了氟马西尼（GABA A 受体拮抗剂）和 L-苹果酸（GABA 合成酶抑制剂）对 EFRP 催眠活性的影响。
EFRP 剂量为 12 g/kg 时，显著抑制小鼠的运动活性。EFRP 通过增加入睡小鼠的数量、缩短睡眠潜伏期和延长睡眠时间对戊巴比妥钠诱导的睡眠产生协同作用。L-苹果酸和氟马西尼抑制了 EFRP 对戊巴比妥钠诱导睡眠的增强作用。EFRP 对 NKTM 诱导的惊厥有显著的保护作用，延长了死亡潜伏期，降低了死亡率。
EFRP 具有镇静、催眠和抗惊厥活性，这些活性可能与 GABA 能系统有关。
