Calcium antagonistic activity of Bacopa monniera on vascular and intestinal smooth muscles of rabbit and guinea-pig.

The present study demonstrates the calcium antagonistic activity in ethanol extract of Bacopa monniera. The plant extract inhibited the spontaneous movements of both guinea-pig ileum (IC50 = 24+/-4 microg/ml) and rabbit jejunum (IC50 = 136+/-9 microg/ml). A marked reduction in acetylcholine- and histamine-induced responses (0.0001-10 microM) in the ileum was evident in the presence of extract (260 microg/ml). The acetylcholine (1 microM)-induced contraction in the ileum was also inhibited by the extract (100-700 microg/ml) in a concentration dependent way (IC50 = 285+/-56 microg/ml). All these results indicate a direct action of the extract on smooth muscles. Calcium chloride-induced responses in the rabbit blood vessels and jejunum were attenuated in the presence of plant extract (10-700 microg/ml) implying a direct interference of plant extract with influx of calcium ions in the cells. However, the lack of modification of either noradrenaline- or caffeine-induced contractions in the presence of extract suggests that extract has no detectable effect on mobilization of intracellular calcium. These results indicate that spasmolytic effect of the B. monniera extract in smooth muscles is predominantly due to inhibition of calcium influx via both voltage and receptor operated calcium channels of the cell membrane.     

Ligustilide inhibits spontaneous and agonists- or K+ depolarization-induced contraction of rat uterus

In the present study, the effects of ligustilide (LIG) on uterine contraction in vitro were investigated. In isolated rat uterine, LIG (2-8 microg/ml) inhibited the spontaneous periodic contraction in a concentration-dependent manner (EC(50)=4.4 microg/ml, 95% confidence interval 2.7-6.1 microg/ml), and attenuated prostaglandin F2alpha (PGF(2)alpha)- or acetylcholine chloride (Ach)-induced uterine contractions. At 8 microg/ml, LIG nearly completely blocked the PGF(2)alpha-induced contractions (95.3%). In the case of Ach-induced contraction, about 73.9% was inhibited by LIG at this dosage. It was also observed that LIG affected significantly oxytocin-induced increase in the contraction of uterine horns that were incubated not only in the Locke solution but also in a Ca(2+)-free solution. In addition, LIG caused concentration-dependent inhibition of uterine contraction induced by K(+) (56.3 Mm) depolarization, reaching the significant level at 2 microg/ml (EC(50)=3.3 microg/ml, 95% confidence interval 2.5-4.1 microg/ml). The findings clearly show that LIG has multiple effects on the uterine smooth muscles, suggesting that LIG possesses a non-specific antispasmodic function. The data also imply strongly that LIG is one of active ingredients of Danggui and has the potential to be developed into an effective drug for the prevention and treatment of primary dysmenorrhoea.     

Species Differences in the Antidiarrheal and Antispasmodic Activities of Lepidium sativum and Insight into Underlying Mechanisms

The aim of this study was to see if the crude extract of Lepidium sativum (Ls.Cr) exhibits species specificity in its antidiarrheal and antispasmodic activities along with insight into the underlying mechanisms using the in‐vivo and in‐vitro experiments. Ls.Cr inhibited castor oil‐induced diarrhea in mice at doses (300 and 1000 mg/kg) three times higher dose than for rats. In isolated rat ileum and jejunum, Ls.Cr completely inhibited carbachol (CCh), low K⁺ (25 mM) and high K⁺ (80 mM)‐induced contractions, while in guinea‐pig tissues, Ls.Cr caused complete inhibition of only CCh‐induced contraction. In rabbit tissues, Ls.Cr completely inhibited CCh and low K⁺‐induced contractions sensitive to K⁺ channel antagonists. Pretreatment of guinea‐pig and rat tissues with Ls.Cr caused a rightward shift in CCh‐induced contractions in a pattern similar to dicyclomine, while in rabbit and rat tissues, Ls.Cr shifted isoprenaline curves to the left similar to papaverine. These data indicate that the antidiarrheal and antispasmodic activities of L. sativum are species dependent, mediating its antispasmodic effect through combinations of multiple pathways including activation of K⁺ channels, and inhibition of muscarinic receptors, Ca⁺⁺ channels and PDE enzyme. Rat tissues showed the highest potency. Based on the results, we recommend using multiple species to know the real pharmacological profile of medicinal products. Copyright © 2012 John Wiley & Sons, Ltd.     

甘草体外抑制呼吸道合胞病毒作用研究

目的:开发安全有效的抗呼吸道合胞病毒的新药.方法:采用细胞病变抑制实验观察甘草在Hela细胞中对呼吸道合胞病毒的抑制作用.结果:甘草半数中毒浓度(TC50)为3.43g/L;抑制呼吸道合胞病毒的半数有效浓度(EC50)为0.2535g/L,治疗指数(TI)为13.53;甘草对呼吸道合胞病毒的抑制作用存在量效反应关系;在感染后0 h、2 h、4 h、6 h、8 h,甘草均有抑制呼吸道合胞病毒的作用.结论:甘草在Hela细胞中对呼吸道合胞病毒有明显的抑制作用,其作用机制是多途径的.     

The aqueous extract of Radix Glycyrrhizae stimulates mitogen-activated protein kinases and nuclear factor-kappaB in Jurkat T-cells and THP-1 monocytic cells

Radix Glycyrrhizae (RG) is a medicinal herb extensively utilized in numerous Chinese medical formulae for coordinating the actions of various components in the recipes and strengthening the body functions. In this report, we demonstrate that the aqueous extract of Radix Glycyrrhizae is capable of stimulating the c-Jun N-terminal kinase and p38 subgroups of mitogen-activated protein kinases (MAPKs), and the nuclear factor-kappaB (NFkappaB) in Jurkat T-lymphocytes. The activation magnitudes of MAPKs and NFkappaB were dose-dependent (EC(50) approximately 1 mg/ml) and time-dependent (maximal around 15-30 minutes). Stimulations of MAPKs and NFkappaB were not associated with changes in intracellular Ca(2+) mobilization. Similar activation profiles of MAPK and NFkappaB were obtained from THP-1 monocytes treated with the extract. In terms of chemotactic activity, the SDF-induced chemotaxis of Jurkat cells and THP-1 cells were inhibited by RG extract at 1-10 mg/ml, while a lower RG concentration (0.1-0.3 mg/ml) potentiated the SDF-induced chemotaxis for the former, but not the latter cell type. Given the fact that MAPKs and NFkappaB are important signaling intermediates for lymphocyte activities, our results suggest that Radix Glycyrrhizae may contain active constituents capable of modulating immuno-responses through various intracellular signaling pathways.     

从蛋白质自组装的角度探析甘草附子配伍减毒机制

甘草与附子配伍有减毒增效的作用。该研究从中药汤剂甘草和附子混煎过程中蛋白质自组装的现象入手,以甘草蛋白和附子主要毒性物质——乌头碱为研究对象,探析甘草附子配伍减毒机制。研究发现经分离纯化后的甘草蛋白在p H 5时可通过自组装形成粒径为(206.2±2.02)nm的稳定颗粒,且可与乌头碱形成平均粒径为(238.20±1.23)nm的甘草蛋白-乌头碱稳定颗粒。通过小鼠急性毒性实验发现注射乌头碱单体的小鼠全部死亡,而注射相同乌头碱含量的甘草蛋白-乌头碱颗粒的小鼠全部存活。对甘草蛋白-乌头碱胶体颗粒的稳定性的调查显示,该胶体颗粒在室温下较稳定,具有成为候选药物载体的可能性。综上所述,甘草蛋白可通过与乌头碱自组装而达到减毒效果。     

不同比例海藻与甘草配伍对大鼠的毒性研究

目的：研究不同比例海藻与甘草配伍对大鼠的毒性作用。方法：32只Wistar大鼠,体重(123±15.3) g,随机分为4组,每组各8只,分别为 正常组(A)和配伍用药组(B,C,D)。正常组用蒸馏水灌胃,B,C,D组用海藻-甘草(1∶1)、海藻-甘草(2∶1)、甘草-海藻(3∶1)灌胃,给药剂量为生 药20 mg·g^-1体重,共35 d,期间观察大鼠的毛色、进食、活动等情况。第36天处死大鼠,对大鼠体重,脏器系数,血常规,血液生化指 标及肝药酶进行检测。结果：海藻与甘草配伍对大鼠毛色、进食、活动、体重、脏器系数无影响,对血液系统、肝功能、心肌酶、肾功能、肝药 酶会产生一定的影响,且与配伍比例有关。结论：海藻甘草不同比例配伍后,对大鼠脏器具有选择毒性作用,并与配伍比例有关。     

Protective effect of jakyak-gamcho-tang extract and its constituents against t-BHP-induced oxidative damage in HT22 cells

The present study investigated whether Jakyak-Gamcho-Tang (JGT, Shaoyao-Gancao-tang) and its constituents have the protective effect against tert-butyl hydroperoxide (t-BHP)-induced cytotoxicity on hippocampal HT22 cell line. JGT consists of two medicinal herbs, Paeoniae Radix (PR) and Glycyrrhizae Radix (GR). In contrast to treating with t-BHP alone, pre-treatment of HT22 cells with JGT, PR and GR (50-400 microg/ml) for 3 hours significantly increased the cell viability in a concentration-dependent manner. In addition, JGT, PR and GR exhibited the scavenging activity in both 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and superoxide anion assays. Among the tested extracts, PR showed the most potent protective and antioxidative activities. These results suggest that PR acts as an antioxidant and this property may contribute to the neuroprotective activity of JGT extract.     

Ethnopharmacological evaluation of the anticonvulsant, sedative and antispasmodic activities of Lavandula stoechas L

Lavandula stoechas L. (Lamiaceae) has been used for a long time in traditional medicine as an anticonvulsant and antispasmodic. The aqueous-methanolic extract of L. stoechas flowers (LS) was studied for its possible anticonvulsant and antispasmodic activities. When tested in mice, LS (600 mg/kg) significantly reduced the severity and increased the latency of convulsions induced by pentylene tetrazole (PTZ). LS likewise reduced PTZ's lethality. LS up to a dose of 600 mg/kg was found devoid of any hypnotic effect in mice, however, animals were found to be dull, calm and relaxed. The sedative effect of the plant extract was confirmed, as it prolonged the pentobarbital sleeping time in mice similar to that of diazepam. In isolated rabbit jejunum preparations, LS caused a dose-dependent (0.1-1.0 mg/ml) relaxation of spontaneous contractions. LS also inhibited K(+)-induced contractions in a similar dose range, thereby suggesting calcium channel blockade. This effect was confirmed when pretreatment of the jejunum preparation with LS produced a dose-dependent shift of the Ca(2+) dose-response curve to the right, similar to the effect of verapamil, a standard calcium channel blocker. These data indicate that the plant extract exhibits anticonvulsant and antispasmodic activities. Its calcium channel blocking property may be mechanistically related to these activities. Its usefulness in folk medicine appears thus to be based on a sound mechanistic background.     

Effect of quercetin on tachykinin-induced plasma extravasation in rat urinary bladder

The effect of quercetin on substance P-induced plasma extravasation in rat urinary bladder and its modulation by endogenous peptidases in conscious rats was studied. Plasma protein extravasation (PE) was assayed by measurement of extravasated Evans blue dye (microg/g dry tissue). Intravenous injection of substance P (SP, 10 nmol/kg) significantly increased PE in the urinary bladder. PE evoked by SP was increased significantly by quercetin (20 mg/kg, p.o.) pretreatment in the urinary bladder (73.5 +/- 4.9 to 152.2 +/- 9.9). Pretreatment with captopril, an angiotensin-converting enzyme (ACE) inhibitor (10 nmol/kg, i.v.), or with phosphoramidon, a neutral endopeptidase (NEP) inhibitor (2.5 micromol/kg, i.v.) also potentiated the SP-induced PE in urinary bladder, 286.2 +/- 20.4 and 323.3 +/- 34.0, respectively. Quercetin did not show any effect on neurokinin-A (NKA, 10 nmol/kg, i.v.) -induced plasma extravasation. The present study demonstrates that quercetin potentiates the PE induced by substance P in the urinary bladder. These effects suggest that this flavonoid might cause inhibition of NEP and/or ACE.     

附子与甘草不同配伍比例配伍减毒的实验研究

目的:通过平行比较附子及附子与甘草不同配伍比例对附子毒性的影响,观察甘草对附子的解毒作用,并对减毒机制进行探索性的研究。方法:平行比较了附子和附子配伍不同比例甘草对附子小鼠急性毒性,测定其半数致死剂量LD50;平行比较附子和附子配伍甘草对大鼠的心脏毒性,测定其半数中毒剂量TD50;以无血清DMEM将附子、附子-甘草3∶1、附子-甘草1∶1、附子-甘草1∶3的含药血清分别按5%,10%,20%稀释成3个浓度,观察各给药组不同浓度的含药血清对原代乳大鼠心肌细胞搏动节律、细胞存活率以及细胞内乳酸脱氢酶(LDH)含量的影响。结果:附子配伍甘草后能够提高附子的LD50和TD50。同空白血清对照组比较附子含药血清能够明显增加心肌细胞搏动节律和LDH的含量(P<0.05),附子配伍不同比例甘草含药血清能够明显降低附子导致心机搏动节律的加快,降低LDH含量。随着甘草比例的增加,作用加强。但不同浓度的附子以及附子配伍甘草含药血清对细胞存活没有明显影响。结论:甘草能够通过提高附子中毒剂量,从而达到减毒作用。甘草对于附子减毒作用是通过抑制心肌细胞节律的增加,保护心肌细胞从而达到减毒作用。     

药物炮制后对黄芩汤止痛作用的影响

目的：探讨蜜炙甘草和醋制白芍在复方中是否也同单味药炮制药理研究一样具有止痛作用。方法：用热板法、扭体法和电刺激法对小鼠进行止痛研究。结果：白芍和甘草不经过炮制在黄芩汤中的止痛作用不明显,两药经过炮制后,黄芩汤才具有止痛作用,甘草蜜炙比白芍醋制后的止痛作用更好。结论：蜜炙甘草和醋制白芍在复方中也同单味药炮制药理研究一样具有止痛作用。     

复方降脂胶囊质量标准研究

目的　建立复方降脂胶囊的质量标准。方法　采用薄层色谱法对方中丹参、山楂、甘草进行定性鉴别 ,采用比色法测定方中主药绞股蓝总皂苷的含量。结果　处方中丹参、山楂、甘草所含主要成分与其它成分分离良好。比色法测定方中主药绞股蓝总皂苷的测定波长为 4 96 nm,工作曲线在 0 .0 7～ 0 .5 2 m g/ml的范围内呈线性关系 ,平均回收率为 99.4 %。RSD=0 .78%。结论　本法操作简便、结果准确 ,重现性好 ,可用于复方降脂胶囊的质量控制     

煎煮时间及甘草配伍剂量对附子中酯型生物碱含量的影响

目的研究煎煮时间及甘草剂量对附子中酯型生物碱含量的影响。方法采用紫外分光光度法测定附子中的酯型生物总碱含量;采用高效液相法比较乌头碱和次乌头碱的含量。结果酯型生物碱含量的降低,与煎煮时间和甘草剂量有较高的相关性;煎煮时间超过30 min,100 g制附子煎煮液所含的乌头碱和次乌头碱含量低于2 mg/ml。结论大剂量附子用药必须通过合理煎煮和配伍以降低毒性,发挥其特长。     

1949-2009年海藻、甘草同方配伍临床应用文献分析

探讨近60年(1949-2009年)的现代文献中海藻、甘草反药同方配伍在临床中的应用特点.利用关联规则对其组方配伍特点进行挖掘,并对剂量、疾病等进行统计分析.海藻、甘草同方配伍的复方中核心药物为昆布、当归、柴胡、夏枯草、牡蛎、陈皮等;核心药对为昆布-甘草,昆布-海藻,当归-海藻,当归-甘草,柴胡-甘草,夏枯草-海藻等;主要治疗的疾病是乳腺和甲状腺疾病等;海藻、甘草的用量分别集中在10～15 g和3～9g;复方中海藻、甘草用药比例在7∶3 ～8∶2.海藻、甘草反药同用常配伍活血化痰药;主要治疗乳腺和甲状腺疾病等;甘草用量小于海藻.     

The inhibitory effect of herbal medicine -Dai Kenchu To (DKT)- on the colonic motility in rats in vitro

Dai-Kenchu-To (DKT) is a herbal medicine and is currently used as the treatment of paralytic ileus in Japan. We investigated the mechanism of beneficial effects of DKT in vitro. DKT-extract powder (DKT-EP; 30-300 microg/ml) caused a significant inhibition on carbachol (CCH: 10(-6))-induced contraction in a concentration dependent manner of the rat distal colon. DKT-EP (100 microg/ml) consists of 20 microg/ml of Zanthoxylum Fruit, 30 microg/ml of Ginseng Root and 50 microg/ml of Ginger Rhizome. Although each of them had no effect on CCH-induced muscle contraction, the combination of three ingredients caused a significant inhibition on CCH-induced contraction.     

Cirsium japonicum elicits endothelium-dependent relaxation via histamine H(1)-receptor in rat thoracic aorta

Cirsium japonicum De Candole is widely used in traditional herbal medicine for the treatment of hemorrhage, hypertension or blood circulation in Korea. In this work, we investigated the vasorelaxant activity of an aqueous extract of C. japonicum whole plant (CjEx) and its possible mechanism in isolated rat thoracic aortic rings constricted with norepinephrine (NE; 300 nmol/l). CjEx elicited an acute relaxation in endothelium-intact rings in a concentration-dependent manner (0.1-1.0 mg/ml). This relaxation was eliminated by the removal of the endothelium and pretreatment with N(G)-nitro-L-arginine (10 micromol/l), methylene blue (1 micromol/l) or diphenylhydramine (10 micromol/l), but indomethacin (10 micromol/l) atropine (100 nmol/l), [D-Pro(2), D-Trp(7,9)] substance P (5 micromol/l) or HOE-140 (10 nmol/l) did not affect the relaxation. The results indicate that the response to CjEx involves enhancement of the nitric oxide-cyclic guanosine monophosphate system, and that it occurs via histamine H(1)-receptor. Our findings may contribute to better understanding of the potential link between the clinical use and its beneficial effects on vascular health.     

三个不同品种甘草多糖的含量测定

[目的]建立甘草多糖含量定量的测定方法,为评估甘草药材的质量提供方法.[方法]甘草样品经95％乙醇除去小极性的杂质后,采用水提醇沉的方法,再通过多步除杂质得精制多糖.采用苯酚-硫酸法测定甘草多糖与葡萄糖的换算因子,并以此测定不同品种甘草药材中多糖的含量.[结果]三个不同品种间甘草生药中甘草多糖的含量为光果＞胀果＞乌拉尔.乌拉尔甘草多糖平均加样回收率为98.23％,RSD为1.63％.[结论]此方法简便可行,甘草多糖供试液在4h内显色稳定,重复性较好,平均加样回收率高,可作为甘草多糖的含量测定方法.