Pharmacological studies on hypotensive and spasmolytic activities of pure compounds from Moringa oleifera

Bioassay directed fractionation of an ethanolic extract of Moringa oleifera (MO) leaves resulted in the isolation of four pure compounds, niazinin A (1), niazinin B (2), niazimicin (3) and niaziminin A + B (4 + 5). Intravenous administration of either one of the compounds (1–10 mg/kg) produced hypotensive and bradycardiac effects in anaesthetized rats. Pretreatment of the animals with atropine (1 mg/kg) completely abolished the hypotensive and bradycardiac effects of acetylcholine (ACh), whereas cardiovascular responses to the test compounds remained unaltered, ruling out the possible involvement of muscarinic receptor activation. In isolated guinea-pig atria all the compounds (50–150 μg/mL) produced negative inotropic and chronotropic effects. Each compound inhibited K⁺ -induced contractions in rabbit aorta as well as ileal contractions induced by ACh or histamine at similar concentrations. Spontaneous contractions of rat uterus were also inhibited equally by all compounds. These data indicate that the direct depressant action of these compounds exhibited on all the isolated preparations tested is probably responsible for its hypotensive and bradycardiac effects observed in vivo. Moreover, spasmolytic activity exhibited by the constituents of the plant provides a scientific basis for the traditional uses of the plant in gastrointestinal motility disorders.     

Presence of blood‐pressure lowering and spasmolytic constituents in Buddleja crispa

This aim of this study was to investigate the crude extract of Buddleja crispa (Bc.Cr) and its active constituent(s) for their antihypertensive and antispasmodic activities. The Bc.Cr caused a dose‐dependent (3–10 mg/kg) fall in mean arterial pressure in rats under anesthesia. In rabbit aorta preparations, Bc.Cr (0.03–1 mg/mL) caused inhibition of high K⁺ (80 mM) precontractions. The Bc.Cr (0.03–1 mg/mL) also inhibited spontaneous and high K⁺ precontractions in rabbit jejunum preparations, suggestive of calcium channel blocking (CCB) activity. CCB activity was further confirmed when pretreatment of the tissues with Bc.Cr (0.03–0.10 mg/mL) caused a rightward shift in Ca⁺⁺ concentration response curves, similar to verapamil. Among the pure compounds, BdI‐H3 was more potent against the high K⁺ than spontaneous contractions and was around eight times more potent than Bc.Cr against the spontaneous contractions while the other two compounds, BdI‐2 and BH‐3 were inactive. Activity‐directed fractionation revealed that the hexane fraction was more potent against K⁺ precontractions. These data indicate that Bc.Cr possesses a blood‐pressure lowering effect, mediated possibly through CCB, though additional mechanism(s) cannot be ruled out. Among the pure compounds, Bdl‐H3 is likely to be the active compound involved in the spasmolytic and possibly BP lowering effect of the parent crude extract. Copyright © 2008 John Wiley & Sons, Ltd.     

Investigation for anti-inflammatory and anti-thrombotic activities of methanol extract of Capparis ovata buds and fruits

Ethnopharmacological relevance

Capparis ovata Desf. has wide natural distribution in Turkey and it is consumed in pickled form. Flower buds, root bark, and fruits of the plant are used traditionally due to their analgesic, anti-inflammatory, wound healing, anti-rheumatismal, tonic, and diuretic effects.

Aim of the study

The aim of this study was to investigate the possible anti-inflammatory and anti-thrombotic effects of methanol extracts prepared from flower buds (CBE) and fruits (CFE) of C. ovata.

Materials and methods

Anti-inflammatory effects of CBE and CFE were assessed using carrageenan-induced and prostaglandin E₂-induced mouse paw edema models. For the anti-thrombotic effect evaluation, carrageenan-induced tail thrombosis model was performed in mice. The extracts were administered intraperitonally (i.p.) at the doses of 100, 200, and 300 mg/kg. The anti-inflammatory effect of Capparis extracts were tested in comparison to 10 mg/kg diclofenac and anti-thrombotic activity to 10 and 100 IU heparin.

Results

CBE at the doses of 200, and 300 mg/kg and CFE at the doses of 100, 200, and 300 mg/kg showed significant anti-inflammatory activity and CFE reached therapeutic concentration early than CBE in carrageenan inflammation model. In prostaglandin E₂ inflammation model, CBE and CFE exhibited significant inhibitory effects. The C. ovata extracts did not show remarkable anti-thrombotic effect.

Conclusions

Based on the results obtained, it can be concluded that fruits of C. ovata have more potent anti-inflammatory effect than flower buds. It has been suggested that inhibition of cyclooxygenase pathway is one of the mechanisms of the activity. C. ovata may be potentially used as therapeutic agents for inflammatory diseases.     

Hypotensive activity of Thymus orospedanus alcoholic extract

The hypotensive effects of the alcoholic extract of Thymus orospedanus were investigated in both in vivo and in vitro assays. Our results indicate that the extract reduced rat blood pressure and modified the dose–response curve to epinephrine in the rat vas deferens and the rabbit artery, indicative of a competitive antagonism.     

Enhancing oral moisture using an extract of Capparis masaikai Levl

The purpose of this study was to examine the effect of a Capparis masaikai Levl. extract on enhancing oral moisture. Solutions of Capparis masaikai extract, citric acid, sodium chloride, and sucrose were dropped on the tongue dorsum of 20 healthy subjects aged 23-34 years. After swallowing each solution, the oral moisture was measured for 60 min using a saliva wetness tester and a moisture checker. The subjects recorded the degree of taste using a visual analog scale to examine the stimulating effect of each solution on salivation. The Capparis masaikai extract had a long-lasting moistening effect on both the tongue dorsum and buccal mucosa for up to 60 min. The weakly bittersweet taste of the extract was perceived stronger than the other taste elements. The results suggest that the Capparis masaikai extract is useful for enhancing oral moisture.     

刺山柑化学成分及其药理活性研究进展

刺山柑是一种山柑属植物,在多个国家药用。传统用作驱虫药、泥敖剂、利尿剂、通便剂、止痛剂和滋补剂。在我国新疆、西藏地区被广泛用于治疗痛风、类风湿性关节炎等。现代研究发现该植物含有挥发油、芥子油苷类、生物碱、萜类、黄酮类等多种成分,具有保肝、抗炎、抗病毒、抗氧化、免疫调节、降血糖、降血脂等多种生物活性。现对该植物化学成分和研究进展进行综述,以利于该植物的研究、开发与利用。     

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.     

刺山柑的化学成分、药理活性与临床应用研究进展

对刺山柑的化学成分、药理活性和临床应用的研究进展进行综述。刺山柑中的化学成分主要为糖和苷类、黄酮类、生物碱类、萜类和挥发油、脂肪酸类以及甾体类等。刺山柑具有广泛的药理作用，包括抗炎止痛、抗真菌作用、保肝作用、降血糖作用、降高血脂作用、抗氧化作用、抗凝血作用、兴奋平滑肌作用、抗应激反应、改善记忆等。国内临床上主要用于痛风和风湿性关节炎、皮肤病等的治疗，应用前景广阔。     

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.     

Hypotensive Activity of Lannea coromandelica Bark Extract

An ethanol extract of Lannea coromandelica bark (ELC) showed hypotensive activity in anaesthetized dogs and rats. On intravenous administration (i.v.) at a dose range of 5–100 mg/kg in dogs and 1–25 mg/kg in rats it produced a mild to marked decrease in the arterial blood pressure in a dose dependent manner. The effect did not alter after cholingergic, histaminergic, adrenergic and ganglion receptor blockade. The hypotension was also unchanged in vagotomized and eviscerated dogs, whereas there was a slight increase in hypotension in the spinal preparation. It produced dose related decreases in heart rate, without any effect on respiratory rate.     

Tyrosinase inhibitory pentacyclic triterpenes and analgesic and spasmolytic activities of methanol extracts of Rhododendron collettianum

During the course of screening of medicinal plants of Pakistan for the isolation and structure elucidation of bioactive natural products, it was found that the methanol extract of the Rhododendron collettianum showed analgesic and spasmolytic activities. The methanol extract was then extracted with chloroform. Nine pentacyclic triterpenes were isolated from the chloroform extract and their structures were elucidated as erythrodiol (1), betulinic acid (2), maslinic acid (3), 2alpha,3alpha,23-trihydroxyolean-12-en-28-oic acid (4), bayogenin (5), arjunilic acid (6), methyl arjunolate (7), arjungenin (8) and 3beta, 23, 24-trihydroxyolean-12-en-28-oic acid (9). Among the triterpenes (1-9) tested, arjunilic acid (6) was found to be most potent. Their structure-activity relationship (SAR) showed that if the configuration of the -OH group at C-2 is changed from alpha to beta the potency is decreased. In most of the compounds the position and configuration of the -OH group was found to be important for the inhibitory potency against the enzyme tyrosinase. For the comparison, the standard tyrosinase inhibitors kojic acid (IC50=16.67 microm) and L-mimosine (IC50=3.68 microm) were used as controls.     

刺山柑提取物的体外抗脂质过氧化作用

目的:研究刺山柑提取物对正常小鼠脂质过氧化的影响。方法:小鼠肝匀浆与刺山柑提取物共浴后,以自发产生脂质过氧化或者分别以自由基诱导剂CCl4、H2O2和铁离子-抗坏血酸(Fe2+-VitC)激发脂质过氧化作用,以MDA产生量作为脂质过氧化作用指标。结果:刺山柑提取物0.1 mg/ml组可明显降低小鼠肝组织自发性MDA的生成,减轻Fe2+-VitC诱导所致的肝脏脂质过氧化反应;刺山柑提取物0.5 mg/ml组可减轻CCl4、H2O2诱导所致的肝脏脂质过氧化反应。结论 :刺山柑提取物具有良好的抗脂质过氧化作用。     

Hypotensive action of Solanum melongena on normotensive rats

The cardiovascular action of Solanum melongena extract (SME) was investigated using in vivo and in vitro preparations. SME produced dose-dependent hypotensive responses in normotensive albino rats. The duration of response was also dose dependent. In pharmacological antagonist studies, the hypotensive action of SME was proved not to be mediated through the autonomic ganglion, the α-adrenoceptor or the histaminergic receptor. SME worked via the β-adrenoceptor and cholinergic (muscarinic) receptor inducing the hypotensive response. A dose-related attenuation of hypotension with increasing dosages of the β-adrenoceptor blocker, propranolol, and the cholinergic receptor blocker, atropine was observed. In vitro studies indicated that the vasorelaxing and negative inotropic effect of SME might be implicated in the hypotensive response. The activities of the β-adrenergic and acetylcholine receptors mediated by SME in turn promoted vasodilation of the resistant vessels and a reduction in cardiac activity respectively. It is also possible that the hypotensive effect of SME could be accounted for by its influence on the activity of the renin-angiotensin system, since a significant difference of the hypotensive response of SME was obtained with captopril. Furthermore, SME induced diuresis in water-loaded rats which might also account for the hypotensive effect observed. SME could be a very potent hypotensive agent.     

Pharmacological Effects of Capparis spinosa L.

Medicinal plants have been known as one of the most important therapeutic agents since ancient times. During the last two decades, much attention has been paid to the health‐promoting effects of edible medicinal plants, because of multiple beneficial effects and negligible adverse effects. Capparis spinosa L. is one of the most common medicinal plants, used widely in different parts of the world to treat numerous human diseases. This paper aims to critically review the available scientific literature regarding the health‐promoting effects of C. spinosa, its traditional uses, cultivation protocols and phytochemical constituents. Recently, a wide range of evidence has shown that this plant possesses different biological effects, including antioxidant, anticancer and antibacterial effects. Phytochemical analysis shows that C. spinosa has high quantities of bioactive constituents, including polyphenolic compounds, which are responsible for its health‐promoting effects, although many of these substances are present in low concentrations and significant changes in their content occur during processing. In addition, there is negligible scientific evidence regarding any adverse effects. Different health promotion activities, as well as tremendous diversity of active constituents, make C. spinosa a good candidate for discovering new drugs. However these findings are still in its infancy and future experimental and clinical studies are needed. Copyright © 2016 John Wiley & Sons, Ltd.     

Hypotensive action of syringin from Syringa vulgaris

Naturally occurring syringin was isolated from the bark of Syringa vulgaris (Oleaceae), and its pharmacological action examined on anaesthetized Wistar rats. When the drug was introduced intravenously, it caused a dose dependent fall in systolic, diastolic and mean arterial blood pressure, whereas heart rate also decreased at a slightly higher dose. The hypotensive activity was not inhibited by antihistamine or antimuscarinic agents. Syringin has no effect on the pressor effect induced by norepinephrine or carotid occlusion.     

槌果藤对进行性系统性硬化症患者成纤维细胞增殖和Ⅰ型胶原产生的影响

目的:探讨槌果藤乙醇提取物对进行性系统性硬化症(PSS)患者及正常人成纤维细胞增殖、Ⅰ型胶原产生的影响。方法:MTT比色法观察槌果藤提取物对成纤维细胞增殖活性的影响及其抗氧化作用,流式细胞仪检测提取物对细胞凋亡的影响,RT-PCR及Western blot检测提取物对PSS患者Ⅰ型胶原mRNA表达及蛋白合成的影响。结果:槌果藤提取物可抑制PSS患者成纤维细胞的增殖、Ⅰ型胶原mRNA表达及蛋白合成,呈剂量和时间依赖性,但无细胞毒性或诱导凋亡作用。该提取物对正常人成纤维细胞的增殖及胶原合成无影响,对过氧化氢造成的成纤维细胞损伤有一定保护作用。结论:槌果藤乙醇提取物可抑制PSS患者成纤维细胞增殖及Ⅰ型胶原的合成,并有抗氧化作用。     

正交设计法优选维药老鼠瓜生物碱提取工艺的研究

目的优选老鼠瓜中总生物碱的提取工艺。方法以总生物碱的得率为指标,采用正交设计的方法考察离子交换树脂的上样液浓度、pH值、流速对总生物碱提取率的影响。结果最佳提取工艺为A1B1C1,即上样液浓度为2.589μg/ml,pH值为2.5,流速为1 ml/min。结论优选得到的工艺使生物碱的提取效率高,稳定性好。     

The spasmolytic activity of the essential oil of Thymus baeticus boiss in rats

Gas chromatography and GC/MS studies of Thymus baeticus Boiss essential oil showed its major component to be 1,8-cineole. The essential oil was found to present a marked spasmolytic activity in rat duodenum against acetylcholine via a non-competitive type of inhibition. This action was not related to its major component, 1,8-cineole.     

地龙中降压的类血小板活化因子物质

静注地龙煎剂引起大鼠血压明显下降。预先使用特异性血小板活化因子受体阻断剂CV6209显著抑制地龙的降压作用。从地龙脂质中分离得到一种类血小板活化因子物质,用生物检定法测得含量约90～130ng/g。     

Anticonvulsant activities of ethanolic extract and aqueous fraction isolated from Delphinium denudatum

Dried roots of Delphinium denudatum Wall. are a popular folk remedy for the treatment of epilepsy in the traditional Unani system of medicine in the sub-continent. We carried out anticonvulsant screening of the ethanolic extract (EE) and aqueous fraction (AF) of this plant utilising the maximal electroshock (MEST) and subcutaneous pentylenetetrazole (scPTZ), bicuculline (scBIC), picrotoxin (scPTX) and strychnine (scSTN) tests for anticonvulsant activity. EE had weak dose-dependent anticonvulsant effects on seizures induced by PTZ and BIC. AF exhibited dose-dependent activity against hind limb tonic extension phase (HLTE) of MEST and comparatively stronger anticonvulsant activity against seizures induced by PTZ and BIC. The results suggest the presence of potent anticonvulsant compounds in AF of D. denudatum and deserve further investigation for isolation of active compounds and elucidation of the mechanism of anticonvulsant action.