枣味不同提取物镇静催眠作用研究

目的 研究枣味（酸枣仁、五味子）不同提取物的镇静催眠作用。方法分别制备枣味水提物、醇提物、醇水双提合并物,将小鼠随机分为空白组、对照组和实验组。观察各提取物对小鼠自主活动次数及睡眠时间的影响。结果与空白组相比,枣味醇提物高剂量组和醇水双提物中剂量组小鼠的自主活动次数明显减少;各组小鼠睡眠时间明显延长,其中醇提物和醇水双提物中、高剂量组催眠作用最显著。结论采用醇提或醇水双提方法所得的酸枣仁、五味子提取物具有明显的镇静催眠作用。     

催眠方煎剂的镇静催眠作用研究

目的:研究中药复方催眠方的镇静、催眠作用。方法:实验分为空白对照(等容生理盐水)、地西泮(0.002g/kg)与催眠方煎剂高、中、低剂量(4、2、1g/kg)组。通过小鼠自主活动实验观察其对小鼠活动的影响,通过阈上和阈下剂量戊巴比妥钠的睡眠实验观察其对小鼠入睡潜伏期和睡眠时间的协同影响作用。结果:与空白对照组比较,催眠方煎剂高、中、低剂量组小鼠自主活动次数显著减少;睡眠潜伏时间显著缩短,睡眠时间显著延长(P<0.01或P<0.05)。结论:催眠方煎剂具有一定的镇静、催眠作用。     

假杜鹃提取物对小鼠镇静催眠作用的实验研究

目的探讨假杜鹃提取物对小鼠的镇静催眠作用。方法小鼠腹腔注射给药,观察小鼠延长戊巴比妥钠的睡眠时间及自主活动次数。结果假杜鹃提取物能显著延长小鼠戊巴比妥钠睡眠时间（P〈0．01）,减少小鼠自主活动次数（P〈0．05）。结论假杜鹃提取物对小鼠有明显的镇静催眠作用。     

黄秋葵镇静催眠活性部位的筛选研究

目的黄秋葵不同极性提取部位对小鼠镇静催眠活性的研究。方法连续7 d灌胃给予小鼠不同提取部位高、低剂量(240、80 mg·kg-1)的黄秋葵,观察其对小鼠自主活动、阈下剂量戊巴比妥钠所致入睡率、阈上剂量戊巴比妥钠致入睡潜伏期与持续睡眠时间的影响。结果黄秋葵醇总提物及正丁醇层、水层和水提物可以显著抑制小鼠的自主活动,增加阈下剂量所致入睡率,缩短阈上剂量致睡眠潜伏期,延长阈上剂量致睡眠时间。结论黄秋葵醇提物正丁醇层、水层和水提物为镇静催眠活性部位。     

舒眠胶囊

［主要成分］酸枣仁、柴胡、白芍、合欢花、合欢皮、僵蚕、蝉衣、灯心草。 ［理化性状］本品为胶囊剂,内容物为棕黄色至棕色粉末,气微,味苦。 ［药理作用］小鼠自主活动实验表明（n=20）,给本药9.75,3.90,1.95g*kg-1*d-1的高、中、低3个剂量都能显著地抑制小鼠的自主活动,与空白对照组比较差异显著（P<0.001）,高剂量组与安定组无显著性差异（P>0.05）。大鼠实验表明其能显著抑制自主活动。15d给药,对小鼠阈下剂量戊巴比妥钠的镇静催眠作用有明显的协同作用,15min睡眠率空白组为10%,高、中剂量组分别为75%,60%,与空白组比较均有显著差异（P<0.001）, 而眠安宁对照组10.40mL*kg-1*d-115min睡眠率为45%,表明本品作用强度优于对照组。即使1d内给药也可对阈下剂量戊巴比妥钠致小鼠的镇静催眠作用有显著协同作用,且高剂量组的作用强度与安定相当。     

旋复花水提物与醇提物的止咳化痰作用研究

目的研究旋复花水提物和醇提物的止咳化痰作用。方法给药组小鼠连续10 d灌胃给药后,采用氨水引咳建立模型,观察其咳嗽潜伏期及咳嗽次数;采用酚红排泄试验,测定给药组小鼠气管酚红排泄吸光度值,观察其祛痰作用。结果与空白对照组相比,给药组小鼠咳嗽次数减少,咳嗽潜伏期延长,气管酚红排泄吸光度值明显升高(P0.05)。与空白对照组相比水提物高剂量组、醇提物中高剂量组气管酚红排泄吸光度值差异有统计学意义(P0.05)。结论旋复花提取物具有一定的止咳化痰作用。     

柴桂安神胶囊治疗失眠的药效学研究

目的研究柴桂安神胶囊对失眠大鼠睡眠时相变化的影响;观察柴桂安神胶囊对小鼠的镇静催眠作用;观察小鼠对催眠阈下催眠剂量戊巴比妥钠作用的影响及对小鼠自主活动的影响。方法利用电刺激诱导大鼠失眠的方法,用脑电图描记,观察给予柴桂安神胶囊后失眠大鼠睡眠时相的变化情况;将小鼠随机分为柴桂安神胶囊低、中、高剂量组(2,4和8g·kg-1),解郁安神冲剂组和空白组,观察给药后入睡潜伏期和睡眠持续时间,观察记录30min内翻正反射消失达1min以上的小鼠数以及末次给药30min后,2min内小鼠自发活动次数。结果柴桂安神胶囊可显著延长失眠大鼠的总睡眠时间(TST)、中、高剂量可明显缩短戊巴比妥钠致小鼠入睡的潜伏时间、延长睡眠持续时间、增加阈下催眠剂量戊巴比妥钠小鼠入睡率并抑制小白鼠自发活动次数。结论柴桂安神胶囊有镇静催眠作用。     

补骨脂水提物对小鼠的肝毒性及胆汁酸转运的影响

目的观察补骨脂水提物对小鼠的肝毒性及对胆汁酸转运体的影响。方法补骨脂水提物连续ig给药4周,禁食不禁水12 h,麻醉动物后取血检测血清生化,剖取肝脏称质量并进行肝脏病理组织学检查。肝脏匀浆后ELISA法检测胆盐输出泵(BSEP)和钠离子-牛磺胆酸共转运蛋白(NTCP)蛋白的表达情况。结果补骨脂水提物以大剂量ig给药,连续给药2周80 g生药/kg组小鼠体质量显著降低,给药3周3个剂量组小鼠体质量均显著降低。给药期间,80 g生药/kg组小鼠死亡10只,40 g生药/kg组小鼠死亡6只。给药4周结束补骨脂水提物80 g生药/kg和40 g生药/kg组小鼠肝系数显著大于对照组。补骨脂水提物80 g生药/kg组雄性小鼠ALT高于对照组,雌性小鼠ALP低于对照组,40 g生药/kg组雌雄小鼠ALP均低于对照组。补骨脂水提物可使小鼠肝脏出现肿胀变性。补骨脂水提物20 g生药/kg可导致肝脏BSEP和NTCP均显著降低。结论补骨脂水提物大剂量ig给药对小鼠肝毒性明显,并可影响胆汁酸转运体的表达。     

苍耳子2种提取物对正常脐带血细胞的影响及其急性毒性的比较

目的观察苍耳子水提物及醇提物对正常脐带血细胞的影响和对小鼠的急性毒性反应。方法采用细胞体外培养技术及细胞染色体标本制作技术,观察姊妹染色单体交换(SCE)频率;急性毒性试验采用小鼠ig给药测定其半数致死量(LD50)和最大耐受量(MTD)。结果苍耳子水提物对SCE频率影响不明显,其小鼠ig给药的LD50及其95%可信限为201.14g·kg-1(181.01~223.51g·kg-1生药)。醇提物能显著降低SCE频率,其小鼠ig给药的MTD大于2.4kg·kg-1生药。结论苍耳子水提物毒性较大。     

蒙药芯芭提取物的抗炎、镇痛作用研究

目的:考察蒙药芯芭提取物的抗炎、镇痛作用。方法:将96只KM小鼠或SD大鼠随机分为模型组(水),阳性对照组(阿司匹林,0.5 g/kg),芯芭醇提物(70%乙醇提取)低、中、高剂量组(0.325、0.650、1.300 g/kg,以生药计)和芯芭醇提后残渣水提物低、中、高剂量组(0.325、0.650、1.300 g/kg,以生药计),每组12只;ig给药,每天1次,连续7 d。分别采用二甲苯致小鼠耳肿胀法测定小鼠耳肿胀度和蛋清致大鼠足肿胀法测定大鼠致炎1、2、4、6 h后的足跖肿胀度,以考察芯芭提取物的抗炎作用。取96只KM小鼠同法分组、给药,采用乙酸扭体法测定小鼠20 min内扭体次数;另取64只KM小鼠,同法分组,每组8只,除阳性对照组小鼠ig盐酸曲马多(0.5 g/kg)外,其余各组小鼠同法给药,采用热板法测定小鼠给药前及给药30、45、60、90 min后的痛阈值,以考察芯芭提取物的镇痛作用。结果:与模型组比较,芯芭提取物可降低小鼠耳肿胀度和蛋清致炎6 h后大鼠足跖肿胀度,除芯芭醇提后残渣水提物高剂量组大鼠足跖肿胀度降低不显著外,其余各组差异均有统计学意义(P<0.05或P<0.01);芯芭提取物可显著减少小鼠20 min内扭体次数,延长给药30、60、90 min后的小鼠痛阈值(P<0.05)。结论:芯芭醇提物及其醇提残渣水提物均具有一定的抗炎、镇痛作用。     

Effects of Diazepam and Ethanol on Heart Rate and Galvanic Skin Responses

Abstract: Heart rate (HR), heart rate variability (HRV), and the amplitude and frequency of galvanic skin responses (GSR) were studied in nine healthy young males 2–3 hrs after oral administration of either placebo, diazepam (10 and 20 mg per 70 kg body weight), ethanol (0.78 and 1.22 ml/kg), or combined administration of diazepam (10 mg) and ethanol (0.78 ml/kg). When examinations were performed in resting subjects, ethanol produced significant increases in heart rate, as did combined administration of ethanol and diazepam. Heart rate variability, supposedly correlated to reaction time, was reduced by combined administration of the two drugs. The frequency of the GSR was reduced by both ethanol and 20 mg diazepam, while the amplitude was increased by 10 mg diazepam and reduced by 20 mg diazepam, although not significantly, and was reduced on one occasion by ethanol. Stimulation by mental arithmetic increased all parameters, and more so after drug treatment than after placebo. The results are discussed in relation to the possible effects of diazepam on the autonomic nervous system, and also in relation to the psychophysiological activation theory which presupposes that increased activation is related to increased sympathetic activity. It is concluded that the parameters used are not reliable as indicators of whether a drug is deactivating or not.     

Pharmacological evaluation of the anxiolytic-like effects of Lippia graveolens and bioactive compounds

Context: Lippia species (Verbenaceae) are widely used in Latin America and Africa as folk medicine for their tranquilizing properties.

Objective: To evaluate the anxiolytic-like effects and safety of Lippia graveolens Kunth. by exploring its aqueous and organic leaf extracts and identifying the responsible chemical constituents.

Material and methods: Aqueous and organic extracts (hexane, ethyl acetate and methanol) were pharmacologically evaluated at several doses. Chemical constituents were identified using MS, NMR and GC-MS analysis. The isolated compounds (3?mg/kg, i.p.), extracts (1, 3, 10 and 30?mg/kg, i.p.), and the reference drug diazepam (0.1?mg/kg, i.p.) were assessed in CD-1 mice using experimental behavioural models: open-field, cylinder, hole-board, plus-maze and sodium pentobarbital-induced hypnosis, as well as their acute toxicity (LD₅₀).

Results: After administration of the extracts and bioactive compounds, a significant anxiolytic-like response from 1?mg/kg, i.p. was observed, resembling the effect of diazepam. Major presence of thymol (33.40%) was observed in the hexane extract; whereas for the first time in this species a p-cymene?+?thymol mixture (9.78%), naringenin (0.18%) and cirsimaritin (1.16%) were obtained as bioactive constituents of the ethyl acetate crude extract. Acute toxicity was calculated to be LD₅₀ =?1000?mg/kg for the crude hexane extract, lower in comparison to the other extracts analyzed (LD₅₀ >?2000?mg/kg).

Discussion and conclusion: Our results suggest that L. graveolens exerts anxiolytic-like activity involving many kinds of constituents, mainly of the terpenoid and flavonoid nature. These results reinforce the potential use of this species in the therapy of anxiety.     

氟马西尼不同给药途径的催醒作用评价

目的 研究氟马西尼不同给药途径对受地西泮和唑吡坦催眠小鼠的催醒作用,评价氟马西尼口服制剂的可行性。方法 首先,昆明种小鼠分别腹腔注射生理盐水和戊巴比妥钠（S+W）、地西泮和戊巴比妥钠（D+W）、唑吡坦和戊巴比妥钠（Z+W）,观察（D+W）组和（Z+W）组能否延长戊巴比妥钠睡眠时间,验证地西泮和唑吡坦的催眠效果;然后提前腹腔注射给药氟马西尼,以小鼠睡眠时间为评价指标,评价其催醒作用;最后考察提前灌胃给药氟马西尼,观察其睡眠时间,评价氟马西尼灌胃给药的催醒作用。结果 与对照组（S+W）相比,地西泮组（D+W）和唑吡坦组（Z+W）能显著延长戊巴比妥钠诱导的小鼠睡眠时间（P<0.001,P<0.05）;提前腹腔注射或灌胃给药氟马西尼,与地西泮组（D+W）和唑吡坦组（Z+W）相比,小鼠的睡眠时间显著缩短（P<0.001,P<0.05）。结论 氟马西尼无论是腹腔注射还是灌胃给药,均能拮抗地西泮和唑吡坦的催眠作用,表明氟马西尼制成的口服制剂,同样能显著发挥药效,为研制氟马西尼口服制剂的可行性提供了依据。     

维药小枝玫瑰提取物对四氧嘧啶糖尿病小鼠血糖及糖耐量的影响

目的观察小枝玫瑰Branchlets Rosa rugosa Thunb.提取物对四氧嘧啶糖尿病小鼠血糖及糖耐量的影响。方法采用四氧嘧啶造模法建立糖尿病小鼠模型,将造模成功的小鼠分为8组,分别为模型组,小枝玫瑰水提物高、中、低剂量（3.70、1.85、0.93 g/kg）组,小枝玫瑰醇提物高、中、低剂量（2.75、1.37、0.70 g/kg）组和盐酸二甲双胍（阳性药,200 mg/kg）组,另取正常小鼠为对照组,造模成功3 d后开始给药,每天ig给药1次,共30 d。造模后0、10、20、28 d血糖试纸法测定空腹血糖;造模后30 d,进行葡萄糖耐量试验。结果各组小枝玫瑰提取物均能降低糖尿病小鼠血糖、改善其糖耐量,且呈一定量效关系,其中以醇提物高剂量效果最好,但不及阳性药盐酸二甲双胍。结论小枝玫瑰提取物可以降低糖尿病小鼠血糖,对糖尿病小鼠糖耐量有改善作用。     

复方薰衣草颗粒镇静催眠及改善认知障碍作用研究

目的 观察复方薰衣草颗粒（CLG）镇静催眠及对轻度认知功能障碍（MCI）模型小鼠的治疗作用。方法 （1）CLG镇静催眠和抗抑郁、抗疲劳作用研究：以旷场训练结果为主要条件、体质量为次要条件，随机将79只ICR小鼠分为对照组、地西泮（3 mg·kg^-1，化药阳性药）组、复方枣仁胶囊（12.3 mg·kg^-1，中药阳性药）组和CLG低、中、高剂量（2.36、4.72、9.44 g·kg^-1）组。采用戊巴比妥钠阈下剂量催眠、旷场和转棒实验，观察CLG对小鼠的一般状态、睡眠潜伏期、30 min内入睡比例和总睡眠时间以及行为学的影响。（2）CLG改善MCI作用研究：将60只昆明小鼠以Y迷宫实验训练结果为主要条件、体质量为次要条件随机分为对照组、模型组、多奈哌齐（3 mg·kg^-1，阳性药）组和CLG低、中、高剂量（2.36、4.72、9.44 g·kg^-1）组，每天1次，连续ig给药14 d，给药第9天起，给药1 h后，除对照组外，ip 3 mg·kg^-1东莨菪碱制备MCI模型。于末次给药20 min后进行Y迷宫实验；第15天进行跳台实验；解剖取脑，称取脑质量并计算脑系数；HE染色后观察脑组织病理改变；取海马，ELISA法测定乙酰胆碱（Ach）、乙酰胆碱酯酶（AchE）、超氧化物歧化酶（SOD）、丙二醛（MDA）、谷胱甘肽（GSH）水平。结果 （1）与对照组比较，CLG各剂量对体质量无明显影响；地西泮组和CLG各剂量组入睡率有增高趋势，但无显著性差异；地西泮组和CLG高剂量组入睡潜伏期明显缩短（P<0.05） ；各给药组睡眠时间均显著延长（P<0.01）。（2）与模型组比较，多奈哌齐组和CLG各剂量组跳台次数均显著减少（P<0.05）；CLG各剂量组Ach有升高趋势，多奈哌齐组和CLG中、高剂量组AchE有降低趋势；CLG各剂量组SOD显著增加，MDA显著降低（P<0.05）；CLG中、高剂量组小鼠皮层和海马病理改变明显减轻。结论 CLG具有镇静催眠作用，其改善MCI的作用可能与调节胆碱能系统和抗氧化应激有关。     

Antidiabetic activity of extracts and fraction of Zizyphus mauritiana

Various extracts, petroleum ether, chloroform, acetone, ethanol, aqueous, and crude aqueous, of fruits of Zizyphus mauritiana Lam. (Rhamnaceae) and the fractions of petroleum ether and aqueous extracts were tested for antihyperglycemic activity in glucose overloaded hyperglycemic rats. The effective antihyperglycemic extracts and fraction were tested for their hypoglycemic activity at two dose levels, 200 and 400?mg/kg, respectively. To confirm their utility in a higher model, the effective extracts and fraction of Z. mauritiana were also subjected to an antidiabetic study in the alloxan-induced diabetic model at two dose levels, 200 and 400?mg/kg. The aqueous extract and the non-polysaccharide fraction of the aqueous extract of Z. mauritiana were found to exhibit significant antihyperglycemic and hypoglycemic activities. The petroleum ether extract was found to exhibit only an antihyperglycemic effect. Treatment of diabetic rats with petroleum ether extract, aqueous extract, and non-polysaccharide fraction of this plant restored the elevated biochemical parameters, glucose, urea, creatinine, serum cholesterol, serum triglyceride, HDL, LDL, hemoglobin, and glycosylated hemoglobin significantly to the near normal level. Comparatively, the non-polysaccharide fraction of the aqueous extract was found to be more effective, followed by the aqueous extract, and the petroleum ether extract. The activity of the non-polysaccharide fraction was comparable to that of the standard drug glibenclamide.     

Effect of muscimol on ethanol-induced central nervous system depression

In male Sprague-Dawley rats acute ethanol (1.0 and 2.0 g/kg) produced impairment of motor coordination and induced hypnosis (4.0 g/kg). Muscimol (1.25 mg/kg, IP) prior to ethanol administration enhanced motor impairment as measured by the aerial righting reflex. The rate of ethanol disappearance from the blood was unaltered by muscimol. Functional tolerance to the effect of ethanol on sleep time was produced by a 24 hr ethanol inhalation procedure. Animals tested 48 hr after ethanol inhalation exhibited a reduced sleep time from ethanol (4.0 g/kg). Muscimol (1.75 mg/kg) was administered along with ethanol 48 hr following 1 day of ethanol inhalation. Although the animals exhibited tolerance to ethanol-induced hypnosis, they did not manifest tolerance to the effect of muscimol.     

Hypoglycemic and antioxidant effects of Rheum franzenbachii extract in streptozotocin-induced diabetic rats

The hypoglycemic and antioxidant effects of ethanol extract from the roots and rhizomes of Rheum franzenbachii Münt. (Polygonaceae) were evaluated in streptozotocin-induced diabetic rats. Effects of repeated oral administration of ethanol extract (125, 250, and 500?mg/kg body weight) on the plasma glucose level (PGL), oral glucose tolerance test (OGTT), malondialdehyde (MDA), reduced glutathione (GSH), superoxide dismutase (SOD), and catalase (CAT) in diabetic rats were examined. It was found that administration of ethanol extract (125, 250, and 500?mg/kg) produced a significant fall in PGL, AUC, and MDA, while elevating the GSH levels and SOD and CAT activities in diabetic rats. The dose of 500?mg/kg was identified as the most effective dose, with a decrease of 65.8 and 44.0% in PGL and MDA, and elevation of 72.6, 75.0, and 51.5% in GSH level and SOD and CAT activities, respectively, after 14 days of ERF administration in diabetic rats. Moreover, the OGTT studies showed a maximum reduction in PGL and AUC. From the active extract of Rheum franzenbachii, two stilbenes, desoxyrhapontigenin (1) and desoxyrhaponticin (2), were isolated as major constituents. The present study concludes that the ethanol extract of roots and rhizomes from Rheum franzenbachii had significant hypoglycemic and antioxidant effects.     

Antihepatotoxic and Trypanocidal Effects of the Root Bark Extract of Uvaria chamae

Antihepatotoxic and trypanocidal activities of a root bark extract derived from Uvaria chamae were tested in vivo and in vitro. The plant material was defatted with n -hexane and extracted with 70% ethanol. The ethanol extract was recovered in a 6.13% w/w yield. The LD 50 of the ethanol extract in mice at 24 hr was 166 mg/kg (i.p.). Intraperitoneal injection of the ethanol extract into mice showed no significant effect on pentobarbitone-induced hypnosis. Pentobarbitone-induced sleep in CCl 4 -poisoned rats was significantly reduced (p&lt;0.005) by oral administration of the extract (60 mg/kg). The elevation of serum GOT, GPT, alkaline phosphatase and urea induced by CCl 4 intoxication in rats was also significantly reduced (p&lt;0.005) by the ethanol extract. Uvaria chamae ethanol extract showed a significant (p&lt;0.005) trypanocidal effect which was comparable to that of diminazine aceturate (r= 0.89). Reduction of existing parasitaemia in mice experimentally infected with Trypanasoma brucei brucei was dose-dependent.     

Effects of brotizolam, a new thieno-triazolo-diazepine derivative, on the central nervous system

The effects of brotizolam, a new thieno-triazolo-diazepine derivative, on the central nervous system were analyzed in mice, rats and rabbits. Diazepam, estazolam and triazolam were used as control drugs. Brotizolam inhibited spontaneous motor activities; performances in the rotarod test, staircase test, and maximal electroshock seizure test; and pentetrazol- or bemegride-induced convulsion. Moreover, catalepsy inducing action and potentiating effect on sleep elicited by pentobarbital or ethanol were observed. Following intraperitoneal or oral administration of brotizolam to rabbits with chronically implanted electrodes, the electroencephalographic profile in spontaneous EEG was characterized by slow waves with high amplitudes in the neocortex. The arousal responses by stimulation of the midbrain reticular formation and posterior hypothalamus were slightly inhibited, but the recruiting responses induced by stimulation of the diffuse thalamic projecting system were not inhibited, and seizure discharges induced by stimulation of the dorsal hippocampus were inhibited markedly. When motor activities and pentetrazol-induced convulsions were observed as indices of tolerance for brotizolam, tolerance was not developed by repeated administration of brotizolam up to 14 days. These results suggested that brotizolam, a new thieno-triazolo-diazepine derivative, is judged to be a safer and stronger sleep inducer than diazepam and estazolam.