木香超临界水提液对豚鼠离体肠和小鼠肠推动的作用研究

目的观察木香超临界后水提液对小鼠小肠推进运动和豚鼠离体回肠平滑肌收缩的影响。方法以正常、新斯的明负荷和肾上腺素负荷为研究模型,采用碳末推动法和离体肠实验方法。结果木香Ⅰ组、木香Ⅱ组和木香Ⅲ组碳末推进率均高于正常对照组,差异有统计学意义（P〈0.05和P〈0.01）。肾上腺素组碳末推进率明显低于正常对照组,差异有统计学意义（P〈0.01）;木香Ⅰ组、木香Ⅱ组和木香Ⅲ组碳末推进率明显高于肾上腺素组,差异有统计学意义（P〈0.01）。新斯的明组碳末推进率明显高于正常对照组,差异有统计学意义（P〈0.01）;木香Ⅰ组、木香Ⅱ组和木香Ⅲ组碳末推进率均低于新斯的明组,差异有统计学意义（P〈0.05和P〈0.01）。给药后豚鼠自发收缩活动频率和振幅均高于给药前,差异有统计学意义（P〈0.05和P〈0·01）,且振幅随着木香超临界水提液剂量的增加而增大。结论木香超临界水提液有促进小鼠小肠运动的作用,对肾上腺素所致小鼠小肠推进抑制有显著的促进作用,对新斯的明所致的小鼠小肠推进亢进有拮抗作用,对豚鼠离体回肠自发活动有兴奋作用。     

太子参保健酒对小鼠离体肠平滑肌的研究

目的：观察太子参保健酒对小鼠离体肠平滑肌收缩活动的影响,并探讨其可能的作用机制。方法通过小鼠离体肠段实验,观察不同浓度的太子参保健酒对小鼠正常离体肠收缩活动的影响和对乙酰胆碱（ Ach）引起离体肠兴奋以及阿托品（ Atr）致肠管抑制等方面来考察太子参保健酒对小鼠离体小肠平滑肌的影响。结果与空白组比较,太子参保健酒增加正常小鼠小肠的张力、频率、活力;协同性作用于Ach 致小鼠离体小肠平滑肌;拮抗Atr 致小鼠离体小肠平滑肌抑制作用。结论提示太子参保健酒对肠管有一定的兴奋作用。     

花椒不同炮制品水提液的传导麻醉作用研究

目的 比较花椒不同炮制品水提液对大鼠离体坐骨神经传导电位的影响,从而揭示花椒不同炮制品传导麻醉作用的差异.方法 按照体重将Wistar大鼠随机分为空白组、溶剂组(水);花椒生品、清炒品、醋制品、盐制品、酒制品水回流提取液高、低2个剂量组(药物浓度0.2,0.1 g·mL-1);阳性对照组(利多卡因20 mg·mL-1)...     

木香茎叶提取物成分类别的初步检识及其对小鼠肠推进和胃排空的影响

目的 对木香茎叶提取物化学成分进行初步检识,研究其对小鼠肠推进和胃排空的影响。方法 制备木香茎叶水、乙醇、乙醚提取物,化学反应检识木香茎叶化学成分;以小鼠为研究对象,新斯的明和阿托品诱导小鼠胃肠亢进和抑制状态,ig给予0.5 g/kg木香茎叶水提物、醇提物,用改良的酚红法测定其对胃肠正常、亢进、抑制状态小鼠胃排空率和小肠推进率的影响。结果 木香茎叶醇提物、水提物均能够显著提高正常小鼠小肠酚红推进率（P<0.05、0.01）,显著降低新斯的明所致胃肠亢进状态下的小鼠小肠酚红推进率（P<0.05）,且醇提物的作用较强;两提取物使阿托品所致抑制状态下小鼠小肠推进率进一步降低,且差异显著（P<0.05）,两提取物之间无明显差异;两种提取物对三种状态下的胃排空都发挥显著抑制作用（P<0.05、0.01）。化学成分检识表明,木香茎叶中含蛋白、糖、挥发油、黄酮、内酯、皂苷、生物碱和鞣质等多种成分,但何种成分与小肠推进和胃排空有关尚不确定。结论 木香茎叶提取物对正常小鼠的小肠推进功能具有一定的促进作用,对新斯的明所致小肠推进亢进有抑制作用,对阿托品所致小肠推进抑制有加剧作用,其对肠道的促进作用可能与M胆碱受体有关;对正常和亢进小鼠的胃排空有抑制作用,对阿托品所致胃排空抑制有加剧作用。     

四季青水提液和乙醇提取液对小鼠急性炎症的影响

四季青为冬青科常绿乔木冬青Ilexchinestssims的叶，具有清热解毒、凉血止血、敛疮的功效。临床上可用于风热感冒、肺热咳嗽、咽喉肿痛、热淋涩痛及水火烫伤等症。如抗感灵片、急支糖浆中均含有四季青。叶中主要含挥发油、鞭质、黄酮类成份。有抑菌、抗感染、防止渗出等作用[1]。我省资源丰富，主要用于治疗烧烫伤[2]。临床上既有水煎入药，也有油炸入膏的，其抗急性炎症的有效部位究竟是水溶性成份还是酸溶性成份，尚未见报道。为此，本文比较了水溶性成份和醇溶性成份对小鼠急性炎症的影响，为临床用药提供科学依据。1实验材料四季青叶采…     

薏苡仁水提液对免疫抑制小鼠免疫功能的影响

目的探讨薏苡仁水提液对免疫功能低下小鼠的免疫调节作用。方法先给予小鼠腹腔注射环磷酰胺以建立小鼠免疫功能低下模型,然后将薏苡仁水提液按10、5和2.5 g.kg-1三种剂量连续给三组小鼠灌胃10 d,观察薏苡仁水提液对免疫低下小鼠免疫器官重量指数、白细胞数量、腹腔巨噬细胞吞噬率与吞噬指数、T淋巴细胞酯酶阳性率和血清溶血素HC50值等实验指标的影响。结果薏苡仁水提液能显著拮抗环磷酰胺所致免疫功能低下小鼠的免疫器官重量减轻和白细胞数量减少,明显增加小鼠腹腔巨噬细胞的吞噬百分率及吞噬指数,显著增加血清溶血素含量,且能明显促进T淋巴细胞酯酶阳性率。结论薏苡仁水提液对机体免疫功能具有较好的增强作用。表现为体液免疫、细胞免疫和非特异免疫功能的改变。     

桔梗水提液的镇咳、祛痰作用研究

目的:研究桔梗水提液的镇咳、祛痰作用。方法:通过氨水引咳,观察小鼠咳嗽潜伏期和咳嗽次数,实验分为5组,即模型(等容生理盐水)、右美沙芬(0.03g·kg-1)和桔梗水提液高、中、低剂量(16、8、4g·kg-1)组,ig给药,每12h1次,连续6次。通过测定小鼠气管酚红排泌量来评定小鼠气管黏液分泌量,实验分为5组,即空白对照(等容生理盐水)、盐酸氨溴索(0.03g·kg-1)和桔梗水提液高、中、低剂量(16、8、4g·kg-1)组,ig给药,每12h1次,连续6次。结果:与模型组比较,桔梗水提液高、中剂量组咳嗽潜伏期显著延长(P<0.01或P<0.05),咳嗽次数显著减少(P<0.01或P<0.05)。与空白对照组比较,桔梗水提液高、中剂量组小鼠气管酚红排泌量显著增加(P<0.01或P<0.05)。结论:桔梗水提液在镇咳、祛痰方面效果较好,本研究可为临床用药提供理论依据。     

老龙七水提液对兔离体肠平滑肌收缩的影响

目的:研究老龙七水提液对兔离体肠平滑肌收缩的影响。方法:以0.25、0.50、0.75、1.00、1.25 g(生药)/L老龙七水提液、0.003 125 g/L乙酰胆碱(先加入)+1.25 g(生药)/L老龙七水提液(后加入)、0.003 125 g/L阿托品(先加入)+1.25 g(生药)/L老龙七水提液(后加入)作用于兔离体肠平滑肌,记录兔离体肠平滑肌收缩频率、振幅和张力。结果:0.75~1.25 g(生药)/L老龙七水提液可明显增强兔离体肠平滑肌自发性收缩的振幅和张力(P<0.01),且呈浓度依赖性,但对频率无影响;1.25 g(生药)/L老龙七水提液可明显增强乙酰胆碱诱导的兔离体肠平滑肌收缩的振幅和张力(P<0.05),并且可明显增强阿托品诱导的兔离体肠平滑肌舒张后的振幅和张力(P<0.05)。结论:老龙七水提液可增强乙酰胆碱诱导的兔离体肠平滑肌的收缩,可对抗阿托品诱导的兔离体肠平滑肌舒张。     

山楂水提物对大鼠离体胃、肠平滑肌条收缩性的影响研究

目的:研究山楂水提物对大鼠离体胃、肠平滑肌条收缩性的影响。方法:以大鼠离体胃、肠平滑肌条为研究对象,观察在正常克氏液条件下加入山楂水提物后大鼠胃、肠平滑肌条的收缩状况及在乙酰胆碱、阿托品作用下加入山楂水提物后大鼠肠平滑肌条的收缩状况。结果:山楂水提物在5～20mg·mL-1浓度范围内可显著增强大鼠胃、肠平滑肌条的运动,且具有显著剂量依赖性。山楂水提物(20mg·mL-1)可加强乙酰胆碱引起的肠平滑肌的强烈收缩,对抗阿托品引起的肠平滑肌的舒张作用。结论:山楂水提物对大鼠胃、肠平滑肌条的收缩具有显著的刺激作用。     

飞廉水提液对兔心血管系统的作用

报道飞廉水提液对兔心血管系统的作用：显著提高离体心脏冠脉流量，减弱垂体后叶素致T波、S－T波升高程度。     

The effect of GABA antagonism on propulsive activity of the guinea-pig large intestine

Possible involvement of γ-aminobutyric acid (GABA) in intestinal motility of the guinea-pig has been investigated using the speed of propulsion of faecal pellets along isolated segments of guinea-pig distal colon, and the rate of pellet expulsion from freshly excised colon. GABA antagonism, by bicuculline or by tachyphylaxis to GABA, substantially reduced intestinal motility and generally reduced the amplitude of the reflex contraction associated with pellet propulsion. These results support the view that GABAergic mechanisms may be involved in the propulsive activity of the guinea-pig distal colon.     

Differences in the effects (in vitro) of ethylenediamine on the guinea-pig and rat intestine

The effects of ethylenediamine in different regions of the rat and guinea-pig small intestine were investigated pharmacologically using isolated gut-bath preparations. In the guinea-pig, ethylenediamine caused concentration-dependent neurally mediated contractions or biphasic responses (contraction followed by relaxation). The contractions could be prevented by muscarinic and GABAA receptor antagonists. Ethylenediamine-evoked relaxations and depression of electrically evoked cholinergic twitch responses were blocked by desensitization to baclofen. However, in the rat intestine, the primary response to applied ethylenediamine was a concentration-dependent, non-desensitizing relaxation, evidently due to a direct action of ethylenediamine on the muscularis since it was unaffected by tetrodotoxin or GABAergic blockade.     

白芍水提物及芍药苷改善环磷酰胺致白细胞减少的对比研究

目的对比观察白芍水提物及芍药苷对环磷酰胺(CTX)致小鼠白细胞减少症的影响。方法给小鼠连续灌胃10d,第6和第7天腹腔注射高剂量CTX造成外周血白细胞减少。比较各给药组和模型组小鼠体质量、外周血白细胞数量、股骨中骨髓有核细胞数及肝、脾、胸腺造血免疫器官脏器系数。结果连续2d腹腔注射CTX 100mg.kg-1,可见小鼠外周血白细胞数、骨髓有核细胞数均显著减少(P<0.01),肝脏、脾脏和胸腺系数均明显降低(P<0.01)。白芍水提物及芍药苷均使小鼠外周血白细胞数、骨髓有核细胞数显著增多,脾脏系数明显升高。用药期间各组小鼠体质量无明显差异。结论白芍水提物及芍药苷对CTX所致小鼠白细胞减少和骨髓细胞减少均有升高作用,可提高CTX减少的小鼠脾脏系数。     

干酪菌发酵产物对小鼠小肠推进功能的影响

目的观察干酪菌发酵产物对小鼠小肠推进功能的影响。方法采用小鼠小肠推进实验观察经胃给予干酪菌发酵产物前后小肠推进百分比的变化以及腹腔注射几种受体阻断剂后对其药效的影响。结果干酪菌发酵产物 ( 1 50、30 0、6 0 0mg kg)能提高小鼠小肠推进百分比 ,且呈剂量 效应依赖关系 ;苯海拉明 ( 1 0mg kg)能抑制其对小肠运动的促进作用 ;阿托品 ( 1 0mg kg)能部分对抗其药效。结论干酪菌发酵产物能提高小鼠小肠推进功能 ;其作用途径与H1 受体有关 ,可能与M受体有间接关系。     

Effects of Heliopsis longipes ethanolic extract on mouse spermatozoa in vitro

Context: Heliopsis longipes (A. Gray) Blake (Asteraceae), a plant native to Mexico, is used in traditional medicine as analgesic and microbicide. The main component in the H. longipes ethanolic extract (HLEE) is affinin, as determined by HPLC/UV–visible and NMR measurement. To date, there is no documented evidence on the spermicidal activity of this extract.

Objective: The objective of this study was to assess in vitro the effectiveness of HLEE as spermicide.

Materials and methods: The spermicidal activity of HLEE was evaluated by the Sander–Cramer assay. Spermatozoa were incubated for 20 s with HLEE in concentrations ranging from 75 to 2000 µg/mL to determine the minimum effective concentration (MEC) value. The 50% effective concentration (EC₅₀) of HLEE was estimated by assaying serial dilutions from the MEC. Additionally, sperms were incubated with 125, 250, or 500?µg/mL of HLEE to evaluate the viability and the integrity of sperm membrane. Lipid peroxidation was assessed by the thiobarbituric acid reactive substances assay.

Results: HLEE caused an inhibition of 100% in spermatozoa motility at a MEC value of 2000?µg/mL; the EC₅₀ value was 125?µg/mL. Additionally, exposure to HLEE at 125, 250, or 500?µg/mL for 30?min decreased sperm viability to 27%, 8%, and 2% of the control value, respectively, and significantly increased the percentage of sperms with structurally disorganized membrane. HLEE also increased significantly the level of lipid peroxidation in sperms with respect to controls.

Discussion and conclusion: The results demonstrate the spermicidal activity of HLEE in vitro and suggest that this action is caused by oxidative damage and alterations in the spermatozoal membrane.     

Relaxative effect of core licorice aqueous extract on mouse isolated uterine horns

Abstract

Context: Primary dysmenorrhea is one of the most frequent gynecological disorders in young women. Chinese herbal medicine has the advantage in terms of multi-targeting efficacy, lower toxicity, as well as lower cost. Core licorice is the hard and atropurpureus heart part in root and rootstock of Glycyrrhiza uralensis Fisch (Leguminosae), having a therapeutic effect on dysmenorrhea.

Objective: This experiment indicated the spasmolytic effect of core licorice aqueous extract (CLE) on spontaneous rhythmic contractions and spasmogen-provoked contractions of stilbestrol primed, estrogen-dominated, non-pregnant mouse isolated uterine horns and its spasmolytic mechanism.

Materials and methods: We investigated the spasmolytic effect of CLE (0.025–0.1?mg/mL) on spontaneous contractions and potassium chloride (KCl, 40?mM), acetylcholine (ACh, 5?μg/mL), carbachol (CCh, 5?μg/mL), oxytocin (OT, 2 U/L) or bradykinin (5?ng/mL)-provoked contractions of mouse isolated uterine horns. Contractions were recorded by tension force transducers using Biolap 420F software on a PC.

Results: Our present study showed that graded, escalated concentrations of CLE (0.025–0.1?mg/mL) significantly inhibited the amplitude of spontaneous phasic contractions (15.03–55.10%), as well as the contractions produced by KCl (40?mM; 20.16–53.99%), ACh (5?μg/mL; 14.65–48.32%), CCh (5?μg/mL; 38.40–76.70%), OT (2 U/L; 21.53–58.49%) or bradykinin (5?ng/mL; 58.01–79.44%) of the estrogen-dominated isolated mice uterine horn preparations in a concentration-related manner.

Discussion and conclusion: The spasmolytic effect of CLE observed in the present study lends pharmacological support to the traditional use of core licorice in the management, control and treatment of primary dysmenorrhea.     

Effects of the benzodiazepine receptor agonist midazolam and antagonist flumazenil on 5-hydroxytryptamine release from guinea-pig intestine in vitro

Summary Isolated segments of the guinea-pig small intestine and the guinea-pig stomach were vascularly perfused and the release of 5-hydroxytryptamine (5-HT) and 5-hydroxy-indoleacetic acid into the portal venous effluent determined by high pressure liquid chromatography with electrochemical detection. Test substances were applied intraarterially.The benzodiazepine receptor agonist, midazolam, concentration-dependently increased (by 58%, at 1 nmol/l) and decreased (by 32%, at 100 nmol/l) the release of 5-HT from small intestine preparations. Both effects were blocked by the benzodiazepine receptor antagonist flumazenil (10 nmol/l) The stimulatory effect of midazolam was also abolished in the presence of tetrodotoxin (1 mol/l) or scopolamine (100 nmol/l). In the absence of tetrodotoxin, flumazenil (10 nmol/l) alone decreased the release of 5-HT from the small intestine by 41%, but it increased the release of 5-HT by 50% in the presence of tetrodotoxin. Both effects of flumazenil were abolished in the presence of bicuculline (50 mol/l). In the absence of tetrodotoxin, flumazenil (10 nmol/l) decreased also the release of 5-HT and its metabolite from the perfused stomach by about 40%, whereas midazolam (1 nmol/l) caused an increase by about 60%. In conclusion, benzodiazepine receptors modulate the previously described intrinsic GABAergic regulation of 5-HT release from enterochromaffm cells in the guinea-pig intestine. It is suggested that an endogenous benzodiazepine-like substance of non-neuronal origin is present in the small intestine and stomach of the guinea-pig. Send offprint requests to K. Racke at the above address     

Antioxidant effects of aqueous extract of Terminalia chebula in vivo and in vitro

The ripe fruit of Terminalia chebula RETZIUS (T. chebula RETZ) (Combretsceae), which is a native plant in India and Southeast Asia, has traditionally been used as a popular folk medicine for homeostatic, antitussive, laxative, diuretic, and cardiotonic treatments. The objective of this study was to evaluate the protective effects of an aqueous extract of fruit of T. chebula on the tert-butyl hydroperoxide (t-BHP)-induced oxidative injury observed in cultured rat primary hepatocytes and rat liver. Both treatment and pretreatment of the hepatocytes with the T. chebula extract (TCE) significantly reversed the t-BHP-induced cell cytotoxicity and lactate dehydrogenase leakage. In addition, TCE exhibited in vitro ferric-reducing antioxidant activity and 2,2-diphenyl-1-picryhydrazyl free radical-scavenging activities. The in vivo study showed that pretreatment with TCE (500 or 1000 mg/kg) by gavage for 5 d before a single dose of t-BHP (0.1 mmol/kg i.p.) significantly lowered the serum levels of the hepatic enzyme markers aspartate aminotransferase and alanine aminotransferase and reduced the indicators of oxidative stress in the liver, such as the glutathine disulfide content and lipid peroxidation, in a dose-dependent manner. Histopathologic examination of the rat livers showed that TCE reduced the incidence of liver lesions, including hepatocyte swelling and neutrophilic infiltration, and repaired necrosis induced by t-BHP. Based on the results described above, we speculate that TCE has the potential to play a role in the hepatic prevention of oxidative damage in living systems.     

In vitro degradation of the stereoisomers of soman in guinea-pig, mouse and human skin

The fate of the four stereoisomers of soman [C(-)P(+), C(+)P(+), C(+)P(-) and C(-)P(-)] was studied by incubating 10 microM C(+/-)P(+/-)-soman at pH 7.4 and 37 degrees for various periods in the presence or absence of homogenates (1:10 and 1:20 w/v) of guinea-pig, mouse or human skin. The remaining concentrations of the soman isomers were determined gas chromatographically. Similar rates of spontaneous (non-enzymatic) hydrolysis (K = 0.005 min-1) were found for the four isomers of soman. Hydrolysis of the toxic (C(+/-)P(-)-isomers is not accelerated in the presence of the skin homogenates. In contrast, the non-toxic C(+/-)P(+)-isomers are enzymatically hydrolysed. As the amount of proteins present in the homogenates varied the rate constants for enzyme hydrolysis per protein concentration were calculated. Except for the high hydrolysis rate constant of greater than 0.127/min.g.l for C(+)P(+) in human skin, these values were almost similar (0.031-0.045/min.g.l) for the skin homogenates tested. Irreversible binding sites for the four soman-stereoisomers are only found in homogenates of mouse skin; 122-195 pmol soman-isomer are bound per mg protein. After preincubation of mouse homogenate with 10 microM soman during 18 hr at 0-4 degrees no further binding of the isomers was detected. It is concluded that skin of the three species tested does not contain enzymes that degrade the toxic C(+/-)P(-)-isomers of soman, whereas phosphorylphosphatase activity for the C(+/-)P(+)-isomers is present in the skin of all three species. Binding sites for all four soman isomers are only present in mouse skin.