复方酸枣安神胶囊催眠作用实验研究

目的研究复方酸枣安神胶囊对小鼠的镇静催眠作用。方法采用小鼠自主活动记数法研究复方酸枣安神胶囊的镇静作用,通过直接诱导小鼠睡眠,观察阈上、阈下剂量戊巴比妥钠对小鼠睡眠的协同作用。结果复方酸枣安神胶囊能明显降低小鼠的自主活动次数,延长阈上剂量戊巴比妥钠小鼠的睡眠时间,减少睡眠潜伏期;未见对小鼠有明显直接诱导睡眠作用,但与阈下剂量戊巴比妥钠对小鼠睡眠具有明显的协同作用,使入睡小鼠个数显著增加。结论复方酸枣安神胶囊具有一定的镇静催眠作用。     

Hypnotic effects of total aqueous extracts of Vervain hastata (Verbenaceae) in rats

The in vivo sedative property of the total aqueous extract of the aerial portion of Vervain hastata (Verbenaceae) (TAEV) was studied in male rats to establish its scientific basis in herbal medicine. The investigation was conducted using electroencephalogram (EEG) analysis, and the barbituric-hypnosis test. The results showed that TAEV potentiated the pentobarbital-induced hypnosis significantly by reducing sleep latency and increased sleeping time in a dose-dependent manner that was reversed by flumazenil. The EEG data demonstrated that extract administration augmented total sleep time, rapid eye movement (REM) sleep and non-REM sleep at the expense of wakefulness. The study's results clearly showed the scientific validity for the use of this plant as a sedative and possibly as a nerve tonic substance.     

应用脑电非线性分析监测镇静下异丙酚的脑区作用

目的:采用脑电非线性分析监测方法,研究围术期硬膜外复合镇静下异丙酚对不同脑区的作用,探讨其临床价值。方法:20例患者,随机分为异丙酚5mg·kg1·h1、异丙酚6mg·kg1·h1两组(每组10例),麻醉采用硬膜外麻醉复合异丙酚镇静。监测患者围术期的脑电非线性参数—近似熵(ApEn)及关联维数(D2),常规监测BP,HR,SpO2。结果:与入室后相比,镇静下患者均表现为额叶与颞叶区的脑电抑制程度较高。两组患者入室后与镇静下相比较,关联维数、近似熵明显降低,差异有统计学意义(P<0.05);术中与复苏、觉醒相比较,差异有统计学意义(P<0.05),组间比较无明显差异。在复苏与觉醒后,各个脑区的脑电变化表现为:额叶与颞叶区的脑电活动度较高。结论:硬膜外麻醉复合异丙酚镇静下,各个脑区在异丙酚作用下抑制程度是不同的,以额叶和颞叶的抑制程度较高,额叶和颞叶区在复苏觉醒时兴奋程度较高。     

缬草挥发油对中枢神经系统药理作用的研究

观察了缬草挥发油对中枢神经系统的影响，结果表明，缬草挥发油具有良好的镇静与抗惊厥作用。     

VISUAL EVOKED POTENTIALS AS A MEASURE OF DRUG EFFECTS ON AROUSAL IN THE RABBIT

SUMMARY 1. Averaged evoked potentials in response to light flashes were recorded from the scalp in conscious, restrained rabbits. Six sedative and three stimulant drugs were administered intravenously and their effects on the evoked potential were measured
2. All six sedative drugs reduced the amplitude of the surface-negative wave occurring 150–200 ms after the stimulus, whereas all three stimulants increased the size of this component. No such consistency was found in drug effects on the early surface-positive wave.
3. The results obtained support the hypothesis that the size of certain components of sensory averaged evoked potentials is related to the level of behavioural arousal.     

Stress-induced insomnia treated with kava and valerian: singly and in combination

Kava and valerian are herbal remedies that are claimed to have anxiolytic and sedative properties respectively, without dependence potential or any appreciable side effects. In this pilot study, 24 patients suffering from stress-induced insomnia were treated for 6 weeks with kava (LI-150), 120 mg daily. This was followed by a 2-week 'wash-out' period off treatment, and then, five patients having dropped out, 19 received valerian (LI-156), 600 mg daily, for another 6 weeks. Then there was a further 2-week period off treatment, and a final 6 weeks of treatment of these 19 patients with the two compounds combined (kava + valerian). Stress was measured in three areas: social, personal and life events; insomnia in three areas also: time to fall asleep, hours slept and waking mood. Total stress severity was significantly relieved by both compounds individually (p < 0.01), with no significant differences between them; and there was also improvement with the combination, significant in the case of insomnia (p < 0.05). On direct questioning, 16 patients (67%) reported no side effects on kava, 10 (53%) on valerian and 10 (53%) on the combination. The 'commonest' effect was vivid dreams with kava + valerian (4 cases (21%)) and with valerian alone (3 cases (16%)), followed by gastric discomfort and dizziness with kava (3 cases each (3 %)). These results are considered to be extremely promising but further studies may be required to determine the relative roles of the two compounds for such indications. Copyright 2001 John Wiley & Sons, Ltd.     

Neurophysiological effects of an extract of Eschscholzia californica Cham. (Papaveraceae)

An aqueous alcohol extract of Eschscholzia californica (Ec) has been evaluated for benzodiazepine, neuroleptic, antidepressant, antihistaminic and analgesic properties, in order to complete the study of the sedative and anxiolytic effects previously demonstrated. The plant extract did not protect mice against the convulsant effects of pentylenetetrazol, and did not cause muscle relaxant effects but appeared to possess an affinity for the benzodiazepine receptor: thus, flumazenil, an antagonist of these receptors, suppressed the sedative and anxiolytic effects of the extract. The Ec extract induced peripheral analgesic effects in mice but did not possess antidepressant, neuroleptic or antihistaminic effects.     

苏州产淡水珍珠生物活性评价及镇静活性物质基础研究

目的对苏州产淡水珍珠的镇静、养阴、抗氧化及酪氨酸酶抑制等生物活性进行评价,并针对其镇静活性的物质基础开展研究。方法采用小鼠在黑箱中自发活动计数的方法考察其镇静作用;利用Sephadex G-100对珍珠热提液进行分离,并评价不同相对分子质量段部位的镇静活性,探讨镇静活性的物质基础。建立甲状腺素小鼠阴虚模型考察养阴作用;通过使用改进的邻苯三酚自氧化法及测定SOD、MDA含量考察抗氧化作用。结果珍珠热提液中大、小相对分子质量段部位均有显著的镇静活性;热提液能够明显增强阴虚状态下小鼠的抗疲劳、耐缺氧的能力,有效抑制阴虚状态下各脏器功能的衰减;冷浸液能显著提高小鼠血清SOD含量、降低MDA含量。结论珍珠具有良好的镇静、养阴和抗氧化作用;珍珠的镇静活性源于多组分物质共同作用的结果。     

生栀子、焦栀子50%和95%乙醇洗脱部位药效学比较研究

目的:对炮制前后变化明显的组分50%和95%乙醇洗脱部位(简称部位)进行药效学比较研究,为阐明栀子的炮制原理和栀子饮片的合理应用提供科学依据。方法:采用抗炎、镇静、凝血及化学性肝损伤等指标,观察生栀子、焦栀子50%和95%部位作用的差别。结果:生栀子、焦栀子50%和95%部位对小鼠炎症反应有较好的抑制作用,对小鼠镇静作用不明显,对四氯化碳造成的肝损伤没有保护作用,焦栀子95%部位有明显的促进血液凝固的作用。结论:生栀子、焦栀子两个洗脱部位抗炎作用较好,对镇静和肝损伤作用不明显。焦栀子95%部位凝血作用明显,有较好的止血功效。     

α-Subunit selective modulators of GABAA receptor function as CNS therapeutics

γ-Aminobutyric acid (GABA) is the major inhibitory neurotransmitter within the CNS. Many drugs, including the benzodiazepines, exert their effects by modulating the GABA_A receptor complex, but side effects are common and reflect, in part, poor subunit selectivity. The subunits are arranged into heteropentamers and this produces a rich diversity of GABA_A receptor subtypes, which are potential targets for treating a variety of CNS disorders including epilepsy, anxiety and insomnia, as well as for ameliorating deficiencies arising from neurodegeneration, such as cognitive impairment. The identification of new ligands with improved subunit selectivity should reduce or abolish some of the side effects observed with current drugs, such as tolerance, dependence and withdrawal. This article focuses on new ligands that are reported to selectively recognise particular α-subunits of GABA_A receptors and may thereby offer improved treatments for CNS disorders. Only patents and literature since 1998 are necessarily included, although some earlier reports and reviews are also cited. Several publications and patent applications since 1998 disclose new compounds that modulate GABA_A receptor function without mentioning whether they have α-subunit selectivity; these compounds, like those known to interact with sites on other GABA_A subunits (particularly β), are not within the scope of this review.