Antispasmodic effect of Bersama abyssinica aqueous extract on guinea-pig ileum

The present study deals with the effect of one of the traditionally used Ethiopian medicinal plants, Bersama abyssinica, on gut motility. The experiment was carried out on isolated guinea-pig ileum with a standard spasmogen, histamine, in the absence and presence of the water extract of the medicinal plant. The spasmogenic effect of histamine was found to be antagonized by the extract in a nonreversible manner, indicating that B. abyssinica has a spasmolytic activity.     

Effect of Extract of Leaf and Seed of Piper guineense on Some Smooth Muscle Activity in Rat,Guinea-pig and Rabbit

Extracts of the leaf and seed of Piper guineense were separately prepared and their pharmacological effects screened using smooth muscle of the gastrointestinal tract and uterus. The leaf extract enhanced both the frequency and tone of spontaneous contractions of rabbit jejunum and induced contraction of guinea-pig ileum, which were blocked by atropine. The seed extract had the opposite effect on rabbit jejunum, an inhibition which was antagonized by prazocin, and little or no effect on guinea-pig ileum. Both extracts had a stimulant effect on rat uterine muscle, the seed extract to a lesser extent.     

Spasmolytic activity of Toddalia asiatica Var. floribunda

The spasmolytic activity of the aerial parts of Toddalia asiatica var. floribunda (family Rutaceae) was evaluated. The ethanol extract exhibited significant spasmolytic activity and was then partitioned into five fractions. The activity was found to be concentrated only in the hexane and chloroform fractions. This activity was shown not to be due to the coumarins, toddalolactone and toddanone, as was previously thought.     

Antispasmodic property of the aqueous extract of Aristolochia albida Duch

The antispasmodic property of the underground parts of Aristolochia albida Duch (family: Aristolochiaceae) was evaluated. The evidence was provided by the aqueous extract of the plant's rhizome which exhibited significant relaxation of the spontaneous pendular contraction of isolated rabbit duodenum. The extract at moderate doses abolished acetylcholine (Ach), histamine and 5-hydroxytryptamine (5-HT) induced contractions on isolated rabbit duodenum and guinea-pig ileum. The effects of the extract mimicked antagonists (atropine, mepyramine and methysergide). Therefore, the extract evoked its antispasmodic actions by antagonism via muscarinic, histaminic and 5-HT receptors. © 1997 John Wiley & Sons, Ltd.     

Inhibitory effects of quercetin on guinea-pig ileum contractions

The inhibitory effect of quercetin on the guinea-pig ileum contractile responses was examined to further clarify its mechanism of action. Quercetin inhibited, from doses of 5 μM , the spontaneous phasic contractions of the guinea-pig ileum, as well as the phasic and tonic components of either acetylcholine- or KCl-elicited contractions, in a dose-dependent way. The former effect was reversible and was unaffected by nicotinic blockade. The tonic component of the contractions was more responsive to quercetin than the phasic component. The inhibition of the tonic contraction was, at least partially, due to the blockade of calcium channels by quercetin, since increasing calcium concentration in the tissue bath reversed the inhibition when the organ was contracted by KCl. Quercetin may also interfere with calcium release from intracellular stores, since it inhibited acetylcholine-elicited phasic contraction even in a calcium-free solution. Finally, quercetin shifted the concentration-response curves to carbachol downwards, without modifying the ED₅₀ of the agonist, whereas the concentration-response curves to CaCl₂ were shifted downwards and to the right. In conclusion, quercetin inhibits the contractile responses of guinea-pig ileum, decreasing the calcium concentration available for contractile machinery.     

Mechanism of action of the aqueous seed extract of Mucuna pruriens on the guinea-pig ileum

The hot water extract (HWE) of the seed of Mucuna pruriens dose-dependently contracted the guinea-pig ileum. The ED₅₀ and pD₂ values for the HWE was lower than those of ACh and histamine. Cyproheptadine and promethazine (10 ng/mL) significantly antagonized the effects of histamine, 5-hydroxytryptamine (5-HT) and HWE. Atropine blocked the effect of ACh and partially blocked the HWE. The calcium channel blockers nifedipine and verapamil both blocked the effects of all the agonists including HWE. These results suggest that the HWE contains potent histamine receptor stimulants or principles as it was blocked by low doses of H₁ receptor blockers. It appears that stimulation of the receptors leads to influx of calcium since the effect was also blocked by nifedipine and verapamil. It is likely that it also stimulates muscarinic receptors. © 1997 John Wiley & Sons, Ltd.     

Studies on spasmogenic and spasmolytic activities of Calendula officinalis flowers

The aqueous-ethanol extract of Calendula officinalis flowers (Co.Cr) was studied for its possible spasmolytic and spasmogenic effects in isolated gut preparations. In rabbit jejunum, Co.Cr caused a dose-dependent (0.03-3.0 mg/mL) relaxation of spontaneous and K+-induced contractions, suggestive of calcium channel blockade (CCB). In a few preparations, a mild non-reproducible spasmogenic effect was observed at lower doses, followed by relaxation. The CCB effect was confirmed when pretreatment of the jejunum preparations with Co.Cr produced a dose-dependent rightward shift in the Ca(++) dose-response curves, similar to that of verapamil. Activity-directed fractionation revealed that the spasmolytic activity of the plant was concentrated in its organic fractions. The aqueous fraction exhibited a marked atropine sensitive spasmogenic effect but was found to be devoid of any spasmolytic effect. These data indicate that the crude extract of Calendula officinalis flowers contains both spasmolytic and spasmogenic constituents, exhibiting these effects through calcium channel blocking and cholinergic activities and this study provides a scientific base for its traditional use in abdominal cramps and constipation.     

The spasmolytic activity of the essential oils of scented Pelargoniums (Geraniaceae)

A selection of essential oils obtained by steam distillation from scented-leaf Pelargonium species, hybrids and cultivars were assessed for their pharmacological activity using guinea-pig ileum in vitro. All the essential oils tested were spasmolytic. Their relative spasmolytic activity was related to the yield obtained from the leaves. The pharmacological activity was comparable to that of commercial geranium oils. The mechanism of action was postsynaptic and not atropine-like. Different Pelargonium oils could be exploited for their antispasmodic and possibly other functions. © 1997 John Wiley & Sons, Ltd.     

银杏叶提取物(EGB 761)抗心律失常的实验研究

研究银杏叶提取物EGB 761抗心律失常的作用与机制。以静脉给乌头碱、氯化钡造动物心律失常的模型，观察EGB 761对心律失常与对乳头肌动作电位各项电生理参数影响。结果：EGB 761使乌头碱、氯化钡诱发的室早、室速、室颤及停搏的剂量增加（P＜0．05－P＜0．001）；与对照组相比较，本实验用25mg/L、50mg/L和75mg/L三种不同浓度EGB 761分别使APD50缩短5．8％、9．4％和13．6％；APD90则分别缩短4．4％、8．4％和12．0％（P＜0．05－P＜0．01），呈剂量依赖性，这一效应无被无EGB 761的正常台氏液洗回。提示银杏叶提取物EGB 761有缩短心肌APD，对乌头碱，氯化钡致动物实验性心律失常有良好的对抗作用。     

黑鳗藤中三萜皂苷的分离与鉴定

目的：研究黑鳗藤Stephanotis mucronata根正丁醇部位化学成分。方法：采用色谱法分离，运用多种波谱技术鉴定结构。结果：从黑鳗藤中分离得到4个三萜皂苷，分别为sitakisoside Ⅶ(1)，sitakisoside Ⅵ(2)，sitakisoside Ⅱ(3)和sitakisoside Ⅰ(4)。结论：4个三萜皂苷均为首次从黑鳗藤中分离得到。     

Hypolipidaemic Activity of Ficus carica Leaf Extract in Streptozotocin-diabetic Rats

A decoction of Ficus carica significantly lowered plasma triglyceride levels in rats with insulin-dependent diabetes (streptozotocin 80 mg/kg body weight) when it was administered orally (357±206 mg/dL before administration and 81±81 mg/dL 3 weeks after administration, p< 0.01, n =11). The plasma triglyceride levels in diabetic rats were also lower when the Gicus carica extract was administered intraperitoneally (608±391 mg/dL before administration; 444±310 mg/dL 90 min after administration; and 106±129 mg/dL 48 h after administration; p< 0.005, n =7). The cholesterolaemia remained unchanged.     

银杏叶提取物对早期糖尿病肾病的影响

目的探讨银杏叶提取物（脑恩,extract of Ginkgo bilboa leaf,EGB）对早期糖尿病肾病（diabetic nephropathy,DN）的影响。方法将68例早期DN患者,分为对照组和治疗组。对照组给予常规治疗;治疗组在常规治疗的基础上加用EGB9．6mg,每天3次口服;两组均治疗3个月。比较两组治疗前后尿中微量白蛋白（microalbumin,mALB）、α1-微球蛋白（α—microglobulin,α1-MG）、免疫球蛋白G（IgG）、转铁蛋白（transferrin,TF）、视黄醇结合蛋白（retinal binding protein,RBP）、N-乙酰-β-D-氨基葡萄糖苷酶（N—acety—beta—D—glucosaminidase,NAG）等检测指标。结果与治疗前比较,治疗组治疗后尿mALB、α1—MG、IgG、TF、RBP、NAG明显下降,差异有显著性（P〈0．05）,而对照组上述指标下降不明显（P〉0．05）。结论EGB对早期糖尿病肾病具有保护作用。     

山楂叶提取物分离纯化工艺的优化＊

目的 优化《中华人民共和国药典》2015年版山楂叶提取物工艺的分离纯化条件，提高山楂叶提取物制备的达标率。在现有的针对总黄酮研究的基础上，提高牡荆素鼠李糖苷的含量，符合山楂叶提取物用药要求。方法 以牡荆素鼠李糖苷含量为指标，考察了山楂叶提取参数、分离纯化过程中的树脂型号、洗脱体系等。结果 选用LX158树脂替代药典规定的D101树脂，采用3BV水洗除杂后，3BV 10%乙醇洗脱除杂，洗脱剂为6BV 30％乙醇。结论 优化后的工艺总黄酮含量≥80%，牡荆素鼠李糖苷含量≥8.8%，满足药典相关要求且较比药典工艺收率高7.07%，为中国药典山楂叶提取物制备工艺的补充和修订提供科学依据。     

Spasmolytic activity of Thymus membranaceus essential oil

The spasmolytic activity of Thymus membranaceus essential oil in the duodenum isolated from rat has been investigated. The qualitative and quantitative composition of the essential oil was studied. The essential oil affects the duodenum in two ways, showing a spasmogenic action (due to 1,8-cineole) and, on the other hand, an antagonistic non-competitive effect against the contractions by acetylcholine (due to the phenols and hydrocarbons).     

银杏达莫注射液治疗糖尿病周围神经病变的临床研究

目的:通过对100例糖尿病周围神经病变(DPN)患者的临床研究,探讨银杏达莫针对DPN的临床治疗效果。方法:对照组患者口服甲钴胺片,研究组采用银杏达莫注射液联合甲钴胺片治疗。结果:研究组治疗总有效率明显高于对照组,数据经统计学比较具有显著差异(P0.05);两组患者治疗后正中神经、腓总神经的SNCV和MNCV均明显升高(P0.05),研究组治疗后SNCV和MNCV均明显高于对照组(P0.05);研究组不良反应发生率明显高于对照组,数据经统计学比较具有显著差异(P0.05)。结论:银杏达莫注射液与甲钴胺片联合应用对于DPN的临床治疗具有更好的疗效,且对神经传导速度的改善效果更加明显。     

痹祺胶囊水提取物及其单体成分抗炎活性比较

目的:考察痹祺胶囊水提取物及其单体成分对脂多糖(LPS)诱导小鼠单核/巨噬细胞株RAW 264.7炎症反应的保护作用,以确定痹祺胶囊中抗炎的主要活性成分,为质量控制标准升级提供依据。方法:利用LPS诱导RAW 264.7细胞建立体外急性炎症模型,给予痹祺胶囊水提取物及6种单体成分马钱子碱,士的宁,隐丹参酮,丹酚酸B,甘草苷,甘草酸治疗,痹祺胶囊水提取物质量浓度分别为0.25,0.5,1 mg·L^-1,各单体成分浓度分别为1×10^-7,1×10^-6,1×10^-5 mol·L^-1,治疗24 h后,采用Griess试剂法和酶联免疫吸附测定法(ELISA)分别检测痹祺胶囊水提取物及各单体成分对LPS诱导RAW 264.7细胞分泌一氧化氮(NO)以及白细胞介素-6(IL-6)的影响。结果:与正常组比较,模型组RAW 264.7细胞NO,IL-6表达显著升高。与模型组比较,痹祺胶囊水提取物与隐丹参酮均能抑制NO和IL-6分泌;马钱子碱,士的宁,甘草苷和甘草酸均可抑制RAW 264.7细胞NO分泌。结论:痹褀胶囊水提取物中的主要抗炎成分是隐丹参酮,马钱子碱,士的宁。     

番茄叶水提物对急性炎症氧化应激的拮抗作用

目的:探讨番茄叶水提物对脂多糖(lipopolysaccharide,LPS)诱导的急性炎症所致氧化应激的拮抗作用。方法:50只SD大鼠随机分为正常组、模型组与番茄叶水提物3.19,1.59,0.80g·kg-1·d-1组,连续灌胃给药10d,每天1次。末次给药后以腹腔注射LPS(4mg·kg-1)建立急性炎症模型。酶联免疫吸附法(ELISA)测定血清铜锌超氧化物歧化酶(CuZn-SOD),谷胱甘肽过氧化物酶1(GSH-Px-1)和肿瘤坏死因子α(TNF-α),白细胞介素-6(IL-6),以逆转录聚合酶链式反应(RT-PCR)检测外周血白细胞CuZn-SOD,GSH-Px-1基因表达水平。结果:3.19,1.59g·kg-1·d-1番茄叶水提物可明显提高急性炎症大鼠外周血白细胞CuZn-SOD,GSH-Px-1基因表达以及血清CuZn-SOD,GSH-Px-1水平,显著降低血清TNF-α,IL-6水平。结论:番茄叶水提物可显著抑制LPS诱导的大鼠急性炎症及其所致氧化应激。     

不同来源黄芩醇提物与水提物抗炎作用比较研究

目的：探讨不同产地（河北、山西、大连）黄芩醇提物与水提物抗炎药效差异。方法：建立干酵母致大鼠足跖肿胀动物模型和二甲苯致小鼠耳肿胀动物模型,观察不同产地黄芩醇提物与水提物对炎症模型肿胀度的影响。结果：小鼠耳肿实验,大连水提物抑制小鼠耳廓炎症优于醇提物（P〈0.05）,山西、河北醇提物抗炎药效优于水提物（P〈0.05）,且山西、河北醇提物在所有提取物中表现出较好的抑制耳廓炎症作用。大鼠足肿实验总体抗炎疗效比较,各个产地的黄芩醇提物均较同产地的水提物表现出较优的抑制肿胀作用（P〈0.05）,河北醇提物具有较好抑制炎症作用（P〈0.01）。结论：3个产地黄芩醇提物和水提物均有一定的抑制炎症作用,产地为河北的黄芩醇提液在3种产地中具有较强的抑制急性炎症作用。     

Ca++ channel blocking activity of Artemisia scoparia extract

Intravenous administration of a hydro-methanolic extract of Artemisia scoparia (3–30 mg/kg) produced hypotensive and bradycardiac effects. These effects remained unaltered in atropine treated animals and the presence of the extract did not modify the vasoconstrictor response of norepinephrine, indicating that cardiovascular effects of the plant extract are not mediated through activation of muscarinic receptors or adrenoceptor blockade. In the in vitro studies, it suppressed the spontaneous movements of rabbit jejunum in a concentration-dependent (0.1-1 mg/mL) manner. The plant extract inhibited K⁺-induced tonic contraction in a manner similar to that of verapamil. Exposure of tissue to Ca⁺⁺-free Kreb's solution abolished the spontaneous movements which were restored on addition of Ca⁺⁺. In tissue pretreated with plant extract or verapamil, addition of Ca⁺⁺ (50 μM) failed to restore spontaneous contractions. These data indicate that Artemisia scoparia cntains Ca⁺⁺ channel blocker-like constituent(s) which may explain the hypotensive effect observed in vivo and the traditional use of the plant as a spasmolytic.     

Relaxant effect of essential oil and hydro-alcoholic extract of Pycnocycla spinosa Decne. exBoiss. on ileum contractions

Pycnocycla spinosa is an essential oil from a wild plant growing in central Iran. However, so far its pharmacological effects have not been studied. The aim of this study was to look for relaxant effects of the essential oil and hydro-alcoholic extract of P. spinosa on rat isolated ileum contractions induced by KCl and acetylcholine (ACh). P. spinosa essential oil (PSEO) and the hydro-alcoholic extract inhibited the response to 80 mM KCl in a concentration-dependent manner and attenuated the maximum attainable response of ACh concentration-response curve. Furthermore, in caster oil induced diarrhoea, the hydro-alcoholic extract had a dose-dependent anti-diarrhoeal effect. This study showed that P. spinosa essential oil and its hydro-alcoholic extract act as a relaxant of rat isolated ileum. As the inhibition of contractile over-activity of the ileum is the basis for the treatment of gastro-intestinal disorders such as diarrhoea, P. spinosa may have clinical bene fi ts for treatment of this condition.