内皮素-1对雌激素处理及妊娠小鼠子宫的作用(英文)

ET,Car和Oxy使在高钾液中的雌激素处理和早、中、晚孕的小鼠子宫产生浓度依赖性张力增加,ET对晚孕子宫的 E_(max)是早孕者的1.33倍,Car对中孕子宫的 E_(max)为晚孕者的2倍,Oxy对晚孕子宫的E_max是中孕者的3.2倍。ET对不同孕期子宫的EC_(50)无显著差别,是Car的2％—7％,为Oxy的3—15倍。表明ET对小鼠子宫的兴奋作用不同于Car和Oxy。     

Relaxing effects of Valeriana officinalis extracts on isolated human non‐pregnant uterine muscle

Objectives This study investigated the relaxing effects of Valeriana officinalis L. (Valerianaceae) on human uterine muscle. The major uses of this species in Europe are as a sedative and an anxiolytic; it is also used as a spasmolytic to treat gastrointestinal spasm. Methods We evaluated two valerian extracts (ethanolic and aqueous) in comparison with a natural mixture of valepotriates and nifedipine on spontaneous and agonist‐induced contractions in non‐pregnant human myometrium in vitro. Qualitative and quantitative chemical analysis was used to correlate the chemical composition of extracts with their spasmolytic effects. Myometrial strips were obtained from hysterectomy specimens of premenopausal women. Longitudinal muscle strips were mounted vertically in tissue baths under physiological conditions to record their isometric contraction. The responses of cumulative concentrations of valerian extracts on spontaneous contractions in the presence and absence of the β‐adrenoceptor blocker atenolol or the cyclooxygenase inhibitor indometacin, and on agonist‐induced contractions, were investigated. Key findings Valerian extracts and valepotriates inhibited uterine contra***ctility in a concentration‐dependent manner. Pretreatment with either atenolol or indometacin did not affect the uterine responses to valerian extracts. Valerian extract reduced the maximal contractile response induced by acetylcholine, phenylephrine and histamine independent of the stimulus. Conclusions Valerian extracts may have direct inhibitory effects on the contractility of the human uterus and this justifies the traditional use of this plant in the treatment of uterine cramping associated with dysmenorrhoea.     

Contractile effect of prolactin on guinea pig isolated ileum

Prolactin (PRL) at high concentrations contracted the guinea pig isolated ileum. The maximum response elicited by PRL was 44% of that of histamine-induced responses. There was no significant difference in potency between PRL preparations obtained from two different sources. PRL responses were nullified by denaturation or proteolytic digestion of the hormone. The contractile response was antagonised by atropine and potentiated by neostigmine, but unaffected by the prostaglandin antagonist SC-19220. The pA2 values of atropine against PRL and ACh were similar. Preincubation with morphine, which inhibits ACh release, produced slight inhibition of PRL-evoked contractions. Even high concentrations of PRL failed to produce any response in neostigmine-treated frog rectus muscle preparations. This suggests that PRL may produce contractions through a cholinergic mechanism involving muscarinic receptors. Enhanced gut motility reported earlier for hyperprolactinemic states may be attributed to this cholinomimetic effect of PRL on the intestinal tract.     

Isolation and evaluation of the myorelaxant effect of bergapten on isolated rat jejunum

Context: Plants of the genus Heracleum L. (Apiaceae) have a long history of being used in traditional medicines for the treatment of alimentary tract disorders, and these biological effects have been ascribed to the presence of furanocoumarins (including bergapten).

Objectives: This study aimed to develop an efficient, preparative, counter-current chromatographic separation of bergapten in order to characterize its spasmolytic activity in isolated rat jejunum strips.

Materials and methods: Successful separation of the dichloromethane extract of the fruits of Heracleum leskovii Grossh. was achieved by high-performance countercurrent chromatography (HPCCC) using a two-phase solvent system composed of n-heptane/EtOAc/MeOH/H₂O (6:5:6:5, v/v/v/v). The pharmacological assessment of bergapten (0.0001–50?μM) on jejunum smooth muscle strips isolated from rats was conducted under isotonic conditions, following up to three hours of incubation.

Results: The separation method was scaled up six-fold from analytical to semi-preparative conditions, affording bergapten of >99% purity in less than 30?min. This permitted bergapten to be available in quantity for spasmolytic tests on isolated jejunum strips from rats. Bergapten caused myorelaxation of the intestine preparations in the concentration range of 0.0001–1?μM. At higher doses, bergapten caused either relaxation or contraction of the smooth muscle.

Discussion and conclusion: Bergapten was successfully isolated by rapid HPCCC and its spasmolytic activity was confirmed, thereby providing a preliminary evidence base for the traditional medicine application. The data suggest that bergapten causes no irreversible changes to intestinal tissue.     

旱莲草水提物对戊巴比妥钠催眠作用的影响

目的研究旱莲草水提物对小鼠戊巴比妥钠催眠作用的影响.方法 100只小鼠随机分为5组,分别为旱莲草水提物低、中、高剂量组(10g.kg-1、15g.kg-1、20g.kg-1)、苯巴比妥钠(40mg.kg-1)组、生理盐水组.灌胃给药,1天1次,连续灌胃7d.第8天腹腔注射戊巴比妥钠75mg.kg-1,观察催眠潜伏期及催眠时间.结果苯巴比妥钠组,旱莲草水提物低、中、高剂量组(10g.kg-1、15g.kg-1、20g.kg-1)较生理盐水组的睡眠时间分别缩短88.9%(P<0.01)、24.8%(P<0.05)、52.7%(P<0.01)和70.5%(P<0.01).各组小鼠催眠潜伏期无显著性差异.结论旱莲草水提物能显著缩短戊巴比妥钠对小鼠的催眠时间,提示旱莲草水提物能诱导小鼠肝微粒体细胞色素P450活性.     

地菍水提物对四氧嘧啶致糖尿病小鼠的降糖作用

目的研究地菍的降血糖作用。方法以四氧嘧啶诱发糖尿病小鼠模型,将不同剂量地菍水提物（60、40、和20g生药&#183;kg^-1）灌胃给药,阳性对照组给予盐酸二甲双胍（750mg&#183;kg^-1）,连续给药10d,观察给药后的血糖值。结果地菍高剂量能明显降低四氧嘧啶致糖尿病小鼠的血糖（P〈0．01）。结论地菍对四氧嘧啶致糖尿病小鼠有一定降血糖作用。     

Metiram‐induced nephrotoxicity in albino mice: Effect of licorice aqueous extract

The present study was designed to estimate the effect of aqueous extract of licorice on metiram toxicity in mice. Treating mice with metiram at a dose level of [1/2] LD₅₀ daily for 3 weeks induced many histological changes in the kidney cortex. The renal tubules lost their characteristic appearance and their lining epithelial cells were degenerated. The glomeruli were atrophied and the renal blood vessels were congested. The intertubular spaces infiltrated by inflammatory leukocytic cells. Metiram caused an increase in proliferating cell nuclear antigen (PCNA) expression in nuclei of tubular epithelial cells. Metiram also caused marked elevation in serum creatinine and blood urea nitrogen. Treating animals with metiram and licorice aqueous extract led to an improvement, in both biochemical and histopathological alterations. These results proved that licorice had an ameliorative effect against kidney injury induced by metiram and this effect may be attributed to its antioxidant activity. © 2011 Wiley Periodicals, Inc. Environ Toxicol, 2013.     

A time course analysis of systemic administration of aqueous licorice extract on spatial memory retention in rats

In the present study, the time course of the effects of Glycyrrhiza glabra L. (Leguminosae) aqueous extract (GE), administered systemically to rats, on the spatial memory retention in the Morris water maze was investigated. The dose of glycyrrhizin (GL), i. e., 0.5, 2.5 and 5 mg/mL in daily water intake of GE was administered to three groups of rats. The first, second and third groups received GE for 1, 2 and 4 weeks, respectively (each group included 3 subgroups). Three additional control groups of animals received only tap water during the same periods of time. After terminating the treatments, all animals were trained for four days; each day included one block and each block contained four trials. Test trials were conducted 48 h after the completion of the training period. Nicotine (1 microg/side) was infused into the CA1 region of the hippocampus as a positive drug control. GE treatment decreased both escape latency and traveled distance, but not swimming speed, compared with control, suggesting significant spatial memory retention enhancement by GE. Statistical analysis did not show any significant difference between GE-treated animals and the nicotine group in escape latency and traveled distance. At the end of the testing trials plasma samples were collected and the concentrations of glycyrrhetinic acid (GA) as a major metabolite of GL were measured in the different groups of treated rats. The maximum concentration was observed after four weeks of GE administration at 5 mg/mL of GL. These results showed that the enhancement effect of GE on spatial memory retention does not correlate with GA blood levels.     

新型磷酸二酯酶Ⅳ抑制剂Ariflo对内皮素-1诱发离体人子宫平滑肌收缩的影响

目的 :研究选择性磷酸二酯酶 (phosphodies terase ,PDE)Ⅳ抑制剂Ariflo对内皮素 1(endothelin 1,ET 1)诱发的非妊娠人子宫平滑肌收缩的影响。方法 :累积给药法观察药物对离体平滑肌收缩的作用。结果 :Ariflo可降低子宫平滑肌自主收缩的收缩频率及收缩幅度 (pD2 =7.90 ) ,且对ET 1(3×10 -8mol·L-1)诱发的子宫平滑肌收缩具有浓度依赖性抑制作用 (pD2 =7.4 0 ) ,作用强度与Rolipram相似。结论 :Ariflo对ET 1诱发的离体人子宫平滑肌的收缩具有显著抑制作用 ,提示在临床上有缓解痛经的作用。     

基于解痉效应表征的香连丸多成分整合溶出度研究

目的：探讨基于解痉效应表征的香连丸多成分整合溶出度评价的可行性。方法：采用小杯法和家兔离体肠肌实验,考察不同时间点的香连丸溶出液对乙酰胆碱、氯化钡引起肠肌收缩的解痉作用,测定药物对肠肌收缩张力与频率的抑制率,并计算基于肠肌收缩抑制率的生物效应溶出度,并以f₂相似因子法,与高效液相色谱法测定木香烃内酯、去氢木香内酯及两者加权整合后的溶出曲线进行相关性评价。结果：整合溶出曲线与木香烃内酯、去氢木香内酯、生物效应溶出曲线的f₂值分别为77.7、94.8、55.2,均大于50,表明整合溶出曲线与生物效应及单体成分的溶出曲线均相似。结论：多成分加权整合的溶出度能反映香连丸拮抗肠肌痉挛性收缩的生物效应,建立基于生物效应为导向的中药制剂多成分整合溶出度评价方法具有可行性。     

甘草提取物对大鼠体内环孢素药代动力学的影响

目的:研究甘草连续给药7 d对环孢素在大鼠体内的药代动力学影响。方法:12只大鼠随机分为生理盐水对照组和甘草实验组,甘草实验组予甘草提取物(0.5 g/kg,1次/d)连续给药7 d,第8天晨两组均予环孢素灌胃给药后按时间点连续采样,采用荧光偏振免疫分析法测定环孢素的血药浓度,计算并比较主要药动学参数。结果:对照组和实验组的环孢素主要药动学参数Cmax、tmax、t1/2、AUC0-48 h、AUC0-∞、平均滞留时间(MRT)、药物清除率(CL/F)、表观分布面积(V/F)差异均无统计学意义(P>0.05)。结论:甘草连续给药7 d后不影响环孢素在大鼠体内的药代动力学。     

益母草水提物对子宫收缩活动的影响

目的:益母草水提物对大鼠离体子宫平滑肌收缩功能的影响。方法:实验前两日雌性未孕大鼠每日肌肉注射苯甲酸雌二醇1 mg.kg-1,于第3日颈椎脱臼处死动物,迅速剖取子宫,用BL-420E生物机能系统记录子宫收缩曲线;加入水提物药液20、20、40μL,采用累加给药方式,每次给药后记录10 min收缩曲线,比较给药前后收缩张力、频率和活动力的变化。结果:益母草水提物对未孕大鼠子宫均具有促进收缩作用,使子宫活动力、收缩张力均值和最小值均明显增加(P0.05或P0.01),且呈一定量效关系;同时,水提物可抑制缩宫素对子宫的收缩作用,使子宫活动力、收缩张力的均值和最大值均显著降低(P0.05或P0.01)。结论:益母草水提物对子宫活动具有双向调节作用,对未孕大鼠正常子宫具有兴奋作用,对痉挛子宫具有舒张作用。     

Oxytocin inhibiting effect of the aqueous leaf extract of Ficus exasperata (Moraceae) on the isolated rat uterus

The leaves of Ficus exasperata Vahl Enum. Pl. vahl (Moraceae) are used by traditional healers in Southern Nigeria and some parts of Africa to avoid preterm births. However, previous reports showed that the plant also exhibited uterine contractions at specific concentrations. This study is therefore aimed at investigating the purported uterine inhibitory aspect of the plant on the isolated rat uterus. The aqueous extract (AET) was tested on rhythmic spontaneous uterine contractions. Concentration-response relationships were obtained for oxytocin (OT), acetylcholine (ACh) and ergometrine (EGM), in the presence or absence of fixed concentrations of AET. Salbutamol (SBL) and verapamil (VER) were used as positive controls. AET, at 1.0 x 10(-2) mg/mL, significantly increased (p < 0.05) the EC50 of oxytocin-induced contractions but had no significant effect on ACh, EGM and spontaneous uterine contractions. However, SBL and VER significantly increased (p < 0.01) the EC50, of OT, ACh and EGM and significantly inhibited (p < 0.01) the frequency and amplitude of spontaneous uterine contractions. The aqueous leaf extract of F. exasperata inhibits oxytocin-induced uterine contractions at the concentration shown in this study. This observation may explain its folkloric use in counteracting preterm contractions and alleviating dysmenorrhoea.     

Relaxant effect induced by wogonin from Scutellaria baicalensis on rat isolated uterine smooth muscle

Context: Wogonin is a flavone derivative isolated from Scutellaria baicalensis Georgi (Labiatae) root, which is a traditional Chinese drug used as an anti-inflammatory and for management of dysmenorrhea.

Objective: The effect of wogonin on the uterus has not yet been examined. We investigated the relaxant effects of wogonin on contractile activity of isolated uterine strips of rats.

Materials and methods: The effect of wogonin on spontaneous uterine contraction, and uterine contraction induced by agonists, K⁺-depolarization and oxytocin in Ca²⁺-free solution was observed. To clarify the type of potassium channel, we tested the effects of 4-aminopyridine, tetraethylammonium and glibenclamide.

Results: Wogonin reduced the contractile amplitude of uterine strip smooth muscle of rats in a dose-dependent manner. The concentration of wogonin for reducing the contraction amplitude by 50% (IC₅₀) on spontaneous contractions was 60.5 μM. Wogonin also inhibited the contraction induced by three agonists (oxytocin, prostaglandin F_2α and acetylcholine). For the uterine strips pretreated with oxytocin in Ca²⁺-free solution or K⁺-depolarization, wogonin showed relaxant effect on the induced uterine contractions. In addition, whereas the inhibitive effect of wogonin on the contraction of uterine smooth muscle in rats could be partly blocked by 4-aminopyridine and tetraethylammonium, it was not influenced by glibenclamide.

Discussion and conclusion: Wogonin significantly inhibited the contraction of rat uterine smooth muscle probably through the inhibition of the inflow of extracellular calcium into cells via cell membrane, and intracellular release of calcium ions. In addition, the relaxant effect induced by wogonin might be due in part to the opening of voltage-dependent and large conductance Ca²⁺-activated K⁺ channels.     

Immunostimulatory activity of aqueous extract isolated from Prunella vulgaris

Prunella vulgaris (P. vulgaris) has been used as a traditional medicine in the clinical treatment of herpetic keratitis and for its antioxidative and antimicrobial activities. In this study, we examined the immunostimulatory and antitumor activity of P. vulgaris in murine macrophage RAW 264.7 cells. Thus, we investigated the effects of an aqueous extract of P. vulgaris (PVAE) on macrophage function. We found that PVAE stimulated macrophage phagocytic activity, nitric oxide (NO) production and cytostatic activity. In addition, PVAE induced gene expression and production of macrophage-related cytokines such as TNF-α, IL-1β and IL-6. Transient transfection revealed that NF-κB mediated the PVAE-induced increases in macrophage-related cytokine expression levels. Mitogen-activated protein kinases (MAP Kinase) were also significantly activated by the PVAE-induced NF-κB activation. Pretreatment with NF-κB inhibitor and MAP Kinase inhibitors inhibited the NO production and the phagocytic activity induced by PVAE. This demonstrates that PVAE stimulates macrophage activation via NF-κB transactivation and MAP kinase activation.     

Anti-aging effect of aqueous extract from Astragalus membranaceus on Drosophila melanogaster

OBJECTIVE To study the anti-aging effect of aqueous extract from Astragalus membranaceus on Drosophila melanogaster. METHODS Drosophila(male and female) were collected within 3 d in adult stage.Drosophila were randomly divided into control group and aqueous extract from Astragalus groups(0.625, 1.25,2.5, 5 and 10 g·L~(-1)). The pharmacodynamics experiment of aqueous extract from Astragalus was investigated by using lifespan experiment, crawling assay, hydrogen peroxide stress assay, paraquat stress assay. To evaluate the antioxidant effect of aqueous extract from Astragalus,the enzyme activity of superoxide dismutase(SOD), catalase(CAT) were conducted. RESULTS The results of lifespan showed that 1.25 g·L~(-1) of aqueous extract from Astragalus could significantly prolong the life span of both male and female Drosophila(P<0.05). The 0.625 g·L~(-1) of aqueous extract from Astragalus could significantly extend the life span of female Drosophila(P<0.01). The1.25 g·L~(-1) of aqueous extract from Astragalus could significantly improve the crawling ability of male Drosophila at 25 d age(P<0.05). The 1.25 g·L~(-1) of aqueous extract from Astragalus significantly extended the life span of male Drosophila after hydrogen peroxide exposure(P<0.01). The 0.625 g·L~(-1) of aqueous extract from Astragalus could significantly prolong the life span of female Drosophila after hydrogen peroxide exposure(P<0.05). The 1.25 g·L~(-1) of aqueous extract from Astragalus could significantly prolong the life span of male and female Drosophila after paraquat exposure(P<0.01). The 1.25 g·L~(-1) of aqueous extract from Astragalus significantly increased SOD and CAT activity in fruit flies at 25 d age(P<0.01). CONCLUSION The aqueous extract from Astragalus prolongs the life span of Drosophila by improving the activity of SOD,CAT and alleviating the damage of free radicals caused by aging.     

茉莉根提取物抗实验性心律失常的研究

目的研究茉莉根提取物的抗实验性心律失常作用。方法取茉莉根提取物分别注入由氯仿诱发心室颤动的小鼠、乌头碱诱发心律失常的大鼠、氯化钙诱发心室颤动的大鼠和肾上腺素诱发心律失常的家兔体内,观察其对实验动物心律失常的影响。结果①茉莉根提取物(腹腔注射2.0mg/kg、3.0mg/kg)对氯仿诱发的小鼠心室颤动有明显的预防作用;②茉莉根提取物(静脉注射1.0mg/kg、1.5mg/kg)对乌头碱诱发的大鼠心律失常有明显的治疗效果;③茉莉根提取物(静脉注射2.0mg/kg、3.0mg/kg)对氯化钙诱发的大鼠心室颤动具有预防作用,且能明显地降低大鼠的死亡率;④茉莉根提取物(静脉注射2.0mg/kg、3.0mg/kg)还能对抗肾上腺素诱发的家兔心律失常。以上作用具有明显的剂量依赖性。结论茉莉根提取物有明显的抗心律失常作用,可能与其抑制Na+内流、Ca2+内流及与阻断β-肾上腺素受体有关。     

乌药水提取物抗心律失常作用的研究

目的研究乌药水提取物的抗心律失常作用。方法采用常规抗心律失常方法,将三氯甲烷诱发小鼠室颤试验和氯化钙诱发大鼠室颤试验分为生理盐水组、维拉帕米组、10．0mg／kg乌药水提取物组和30．0mg／kg乌药水提取物组：将肾上腺素诱发家兔心律失常试验分为给药前后组;蟾蜍离体坐骨神经动作电位试验分为任氏液组、1．0％盐酸普鲁卡因溶液组、0．5g/ml和1．0/md乌药水提取物组。结果乌药水提取物对三氯甲烷诱发的小鼠室颤具有明显的治疗作用（P〈0．05）,对氯化钙诱发的大鼠室颤具有明显的预防效果（P〈0．05）,能明显对抗肾上腺素诱发的家兔心律失常（P〈0．01）,可明显降低蟾蜍离体坐骨神经动作电位振幅（P〈O．05）。结论乌药水提取物具有明显的抗试验性心律失常作用,能对抗由三氯甲烷、氯化钙、肾上腺素等诱发的心律失常,其抗心律失常作用可能与其抑制Na＋内流及与阻断β一肾上腺素受体有关。     

壳聚糖在黄芪水提取液中的澄清效果

目的 考察壳聚糖絮凝剂澄清黄芪水提液的效果.方法 单因素试验考察了壳聚糖用量、絮凝pH、温度对絮凝效果的影响,将最佳絮凝工艺与醇沉工艺进行比较.结果 絮凝最佳工艺与醇沉工艺具有相似的澄清效果,且黄芪甲苷和总多糖保留率优于醇沉工艺.结论 壳聚糖可以用于黄芪水提液的澄清处理.