Some pharmacological effects of the ethanol extract of leaves of Annona diversifolia on the central nervous system in mice

In the present study we investigated some neuropharmacological effects of the ethanol extract of the leaves of Annona diversifolia (Annonaceae). Intraperitoneal administration of the extract delayed the onset of clonic seizures induced by pentylenetetrazole and delayed the time in the ‘rota-rod’ and ‘swimming’ test. In addition, the extract augmented the duration of sleeping time induced by sodium pentobarbital. These results indicate that the ethanol extract of the leaves of A. diversifolia has depressant activity on the central nervous system. Copyright © 1998 John Wiley & Sons, Ltd.     

The pharmacological properties of the ethanolic root extract of Combretum dolichopetalum

The pharmacological actions of the crude ethanolic extract and the active fractions of the roots of Combretum dolichopetalum were tested on guinea-pig isolated ileum and in intact rats. The extract relaxed guinea-pig ileum in a concentration-dependent manner. Two active fractions (R_f 0.96 and 0.84) which also relaxed the guinea-pig ileum were isolated using column chromatography and TLC respectively. Both the crude extract and the active fractions inhibited the contractions induced by acetylcholine and histamine concentration-dependently in the guinea-pig ileum. The crude extract inhibited ulcers and gastric secretions induced in rats by pyloric ligation together with histamine 100 mg/kg, i.p. (p<0.05). The extract also delayed gastric emptying in rats in a dose-dependent manner. The effects of the extract were compared with cimetidine at each stage of the study.     

Evaluation of pharmacological activity of a crude hydroalcoholic extract from Jatropha elliptica

The pharmacological effect of the hydroalcoholic extract of Jatropha elliptica was analysed in in vivo and in vitro models. When given orally in mice, the extract showed a low acute toxicity (LD₅₀ 5 g/kg). In a dose of 0.5 or 1 g/kg p.o. the extract did not interfere with diuresis in the rat, but was found to be effective in blocking rat paw oedema induced by carrageenan and partially, serotonin-induced oedema. In the same dose, the extract failed to inhibit rat paw oedema induced by dextran and the increase of rat cutaneous vascular permeability caused by Bothrops Jararaca venom, dextran, histamine, PAF-acether and serotonin. Pre-incubation of the isolated rat uterus and guinea-pig ileum with the extract (0.2–0.8 mg/mL), produced a concentration-related and non-competitive inhibition of contractions induced by acetylcholine and bradykinin. However, the extract was about 2-fold more potent in inhibiting the contraction of both agonists in guinea-pig ileum than in rat uterine muscle. In rat aorta, the extract (50–100 μg/mL) caused a concentration-dependent inhibition of noradrenaline-evoked contractions, being about 5-fold more potent when compared to the IC₅₀ values obtained in rat uterus.     

白屈菜提取物中生物碱的镇痛抗炎作用研究

目的:研究白屈菜提取物的镇痛抗炎作用.方法:小鼠分别ig给予白屈菜提取物低、中、高剂量(0.1,0.2,0.4g·kg-1)1次,采用扭体法、热板法、福尔马林致痛模型,观察白屈菜提取物的镇痛作用.按以上剂量连续7d,采用小鼠二甲苯耳肿胀模型和小鼠腹腔毛细血管通透性实验,观察其抗炎作用;通过纳洛酮拮抗实验,初步验证其镇痛机制.结果:白屈菜提取物可明显抑制冰醋酸引起的小鼠扭体反应次数和扭体反应鼠数(P＜0.05),提高小鼠光热辐射致疼痛反应的痛阈值;高剂量组对二甲苯引起的小鼠耳廓肿胀有显著的抑制作用(P＜0.01).结论:白屈菜提取物具有显著镇痛抗炎作用,其镇痛作用不受纳洛酮拮抗,主要是外周性的.     

龙利叶根急性毒性和抗炎作用的研究

目的:研究龙利叶根水煎液的急性毒性和抗炎作用。方法:采用改良寇氏法对急性毒性进行研究,采用二甲苯所致小鼠耳廓肿胀、醋酸所致小鼠腹腔毛细血管通透性等急性炎症模型,小鼠棉球肉芽肿的慢性炎症模型,评价龙利叶根的抗炎效果。结果:龙利叶根水煎液的LD50为152.24 g.kg-1,其高、中、低剂量(20,10,5 g.kg-1)能降低二甲苯所致小鼠耳肿胀程度,降低醋酸所致小鼠腹腔毛细血管通透性和降低小鼠棉球肉芽肿的湿重(P<0.05或P<0.01)。结论:龙利叶根水煎液毒性较小,具有较好的抗炎作用,为龙利叶的开发和利用提供了科学依据。     

穿心莲提取物的药效学研究

目的:研究穿心莲提取物的药效学作用。方法:通过解热、抗炎、镇咳、祛痰、抗病毒和免疫调节等相关试验,研究了穿心莲提取物的药效作用。结果:穿心莲提取物对酵母菌引起的大鼠发热有明显的对抗作用,作用长达6h。对冰醋酸诱导的腹腔毛细血管通透性增高有明显的抑制作用;可明显减轻角叉菜胶诱导的大鼠足肿胀;显著抑制棉球肉芽肿增生;明显抑制浓氨水诱导的小鼠咳嗽和枸橼酸钠诱导的豚鼠咳嗽;可使流感杆菌感染小鼠的肺脏炎症明显减轻;对环磷酰胺造成的小鼠溶血素抗体分泌低下具有明显的促进作用;增强巨噬细胞的吞噬功能。结论:穿心莲提取物有明显的解热、抗炎、镇咳、抗病毒和免疫调节作用。     

Pharmacological studies of the antiinflammatory profile of Mikania cordata (Burm) B. L. robinson root extract in rodents

The methanolic fraction of the root extract of Mikania cordata was found to possess an inhibitory effect on carrageenin and other mediator—induced oedema; there was a significant inhibition of protein exudation, an increase in peritoneal capillary permeability and leucocyte migration in inflammatory conditions. The extract significantly inhibited both cotton pellet and carrageenin—induced granuloma formation, was effective in experimentally induced arthritic conditions and turpentine—induced joint oedema. The extract also possessed inhibitory effects on sodium urate-induced experimental gout. A significant reduction of pyrexia was also found to occur when rats were treated with the extract. Thus it may be concluded that the methanolic fraction of M. cordata root extract possessed significant antiinflammatory effects in exudative, proliferative and chronic phases of inflammation and demonstrated an antipyretic activity.     

Blood–Brain Barrier Permeability of Bioactive Withanamides Present in Withania somnifera Fruit Extract

The neuroprotective effect of Withania somnifera L. Dunal fruit extract, in rodent models, is known. Withanamides, the primary active constituents in W. somnifera fruit extract exhibited neuroprotective effects against β‐amyloid‐induced cytotoxicity in neuronal cell culture studies. Therefore, we investigated the blood–brain barrier permeability of withanamides in W. somnifera fruit extract in mice using HPLC coupled with high resolution quadrupole time of flight mass spectrometer (Q‐TOF/MS) detection. Mice were administered with 250 mg/kg of W. somnifera extract by intraperitoneal injection, and the blood and brain samples analyzed by Q‐TOF/MS detection. Four major withanamides were detected in brain and blood of mice administered with W. somnifera extract. The results suggested that the withanamides crossed the blood–brain barrier. These results may help to develop W. somnifera fruit extract as a preventive or therapeutic botanical drug for stress‐induced neurological disorders. Copyright © 2014 John Wiley & Sons, Ltd.     

Anti‐Inflammatory and Antinociceptive Activity of Urera aurantiaca

Urera aurantiaca Wedd. (Urticaceae) is a medicinal plant commonly used in traditional medicine to relieve pain in inflammatory processes. In the present study, the in vivo anti‐inflammatory and antinociceptive effects of U. aurantiaca methanolic extract and its possible mechanisms of action were investigated. The extract showed anti‐inflammatory activity in the ear edema in mice test (34.3% inhibition), myeloperoxidase (MPO) activity was markedly reduced in animals administered with the extract: within 49.6% and 68.5%. In the histological analysis, intense dermal edema and intense cellular infiltration of inflammatory cells were markedly reduced in the ear tissue of the animals treated with the extract. In the carrageenan‐induced hind paw edema in rats assay the extract provoked a significant inhibition of the inflammation (45.5%, 5 h after the treatment) and the MPO activity was markedly reduced (maximum inhibition 71.7%), The extract also exhibited significant and dose‐dependent inhibitory effect on the increased vascular permeability induced by acetic acid. The extract presented antioxidant activity in both 2,2‐diphenyl‐1‐picrylhydrazyl and 2,2′‐azinobis 3‐ethylbenzothiazoline 6‐sulfonic acid tests and its total phenol content was 35.4 ± 0.06 mg GAE/g of extract. Also, the extract produced significant inhibition on nociception induced by acetic acid (ED₅₀: 8.7 mg/kg, i.p.) administered intraperitoneally and orally. Naloxone significantly prevented this activity. Copyright © 2014 John Wiley & Sons, Ltd.     

Relaxant effect of ethanol extract of Bacopa monniera on trachea,pulmonary artery and aorta from rabbit and guinea-pig

The relaxant action of an ethanol extract of Bacopa monniera was examined on ring segments of pulmonary arteries (guinea-pig and rabbit), aorta (rabbit) and tracheal preparations (guinea-pig). The plant extract induced relaxation in all the tissues in a dose-dependent manner. Guinea-pig main pulmonary artery was found to be the most responsive to the plant extract, however, complete relaxation was obtained in the tracheal preparations. The relaxant response to the plant extract was unaffected by pretreatment of the blood vessels with either atropine or propranolol, whereas in the tracheal preparations propranolol partially blocked the response. Indomethacin reduced the plant extract-induced relaxation in all the tissues. In blood vessels relaxation induced by the plant extract was not modified in the presence or absence of the endothelial layer. These results suggest that relaxation induced by Bacopa monniera possibly involves prostacyclin compounds (in all the tissues) and β-adrenoceptors (in tracheal preparations). Furthermore, this relaxation is independent of endothelium and muscarinic receptors activation. © 1997 John Wiley & Sons, Ltd.     

Terminalia arjuna extract modulates the contraction of rat aorta induced by KCl and norepinephrine

The bark of Terminalia arjuna is in clinical use for the management of cardiovascular disorders in India. The objective of this study was to investigate the contractile response induced by the extract on rat aorta, a vascular smooth muscle. Terminalia arjuna relaxed the contraction, induced by both KCl (60 mM ) and norepinephrine (NE, 3 μM ). Inhibition was more prominent (80%) in the NE induced contraction than the KCl induced contraction (30%). Under similar conditions diltiazem, a calcium channel blocker (Dz, 1.0 μM ), inhibited 68% of the KCl induced and 30% of NE induced contraction. Thus it appears that the action of Terminalia arjuna extract differs from that of diltiazem in that it is more specific for alpha-adrenergic receptor agonists. It indirectly inhibited the contraction induced by norepinephrine by acting on K (Ca) channel by hyperpolarizing the smooth muscle membrane.     

Ethanol Extract of Magnolia officinalis Prevents Lipopolysaccharide‐Induced Memory Deficiency via Its Antineuroinflammatory and Antiamyloidogenic Effects

Magnolia bark contains several compounds such as magnolol, honokiol, 4‐O‐methylhonokiol, obovatol, and other neolignan compounds. These compounds have been reported to have various beneficial effects in various diseases. There is sufficient possibility that ethanol extract of Magnolia officinalis is more effective in amyloidogenesis via synergism of these ingredients. Neuroinflammation has been known to play a critical role in the pathogenesis of Alzheimer's disease (AD). We investigated whether the ethanol extract of M. officinalis (10 mg/ kg in 0.05% ethanol) prevents memory dysfunction and amyloidogenesis in AD mouse model by intraperitoneal lipopolysaccharide (LPS, 250 µg/ kg/day for seven times) injection. We found that ethanol extract of M. officinalis prevented LPS‐induced memory deficiency as well as inhibited the LPS‐induced elevation of inflammatory proteins, such as inducible nitric oxide synthase and cyclooxygenase 2, and activation of astrocytes and microglia. In particular, administration of M. officinalis ethanol extract inhibited LPS‐induced amyloidogenesis, which resulted in the inhibition of amyloid precursor protein, beta‐site amyloid‐precursor‐protein‐cleaving enzyme 1 and C99. Thus, this study shows that ethanol extract of M. officinalis prevents LPS‐induced memory impairment as well as amyloidogenesis via inhibition of neuroinflammation and suggests that ethanol extract of M. officinalis might be a useful intervention for neuroinflammation‐associated diseases such as AD. Copyright © 2012 John Wiley & Sons, Ltd.     

Anticonvulsant and Sedative Effects of Crude Extracts of Ternstroemia pringlei and Ruta chalepensis

Ternstroemia pringlei Rose (Theaceae) and Ruta chalepensis L. (Rutaceae) have been used frequently for many years in Mexican traditional medicine as sedative and anticonvulsant remedies. In order to evaluate the attributed properties of these species on the CNS, some neuropharmacological tests were done. The methanol extract of T. pringlei flowers signifcantly delayed the onset of tonic seizures induced by strychnine; it diminished mortality totally and the number of animals that exhibited convulsions. R. chapepensis leaf and stem extract extended sleeping time induced by sodium pentobarbital; in addition, it showed protection against pentylenetetrazol-induced convulsions by increasing the latency period and diminishing the death rate. Extracts of both species inhibited electrically induced contraction in guinea-pig ileum; in each case, the effect was concentration-dependent.     

Suppression of ovalbumin‐induced airway inflammatory responses in a mouse model of asthma by Mimosa pudica extract

Asthma is an inflammatory airway disease. The pathogenic mechanisms of asthma include the infiltration of leukocytes and release of cytokines. Mimosa pudica (Mp) has been used traditionally for the treatment of insomnia, diarrhea and inflammatory diseases. Although Mp extract has various therapeutic properties, the effect of this extract on asthma has not yet been reported. This study investigated the suppressive effects of Mp extract on asthmatic responses both in vitro and in vivo. Mp extract was acquired from dried and powdered whole plants of M. pudica using 80% ethanol. BALB/c mice were used for the mouse model of asthma induced by ovalbumin. Mp extract significantly inhibited the HMC‐1 cell migration induced by stem cell factor and blocked the release of monocyte chemotactic protein‐1 (MCP‐1) and interleukin‐6 (IL‐6) in EoL‐1 cells. Leukocytosis, eosinophilia and mucus hypersecretion in asthmatic lung were significantly suppressed by Mp extract. The release of ovalbumin‐specific IgE in bronchoalveolar lavage fluid and serum was also decreased. Mp extract treatment resulted in no liver cytotoxicity. The Mp extract has inhibitory properties on asthma and may be used as a potent therapeutic agent for allergic lung inflammation. Copyright © 2010 John Wiley & Sons, Ltd.     

Antioedema and analgesic actions of Diodia scandens extract in rats and mice

An extract of Diodia scandens obtained by petroleum ether extraction of the leaves was screened for pharmacological actions. The extract evinced a marked antiinflammatory effect in rats, causing a dose-related and sustained inhibition of the increase in rat paw circumference caused by subplantar injection of a phlogistic agent. In addition, the extract increased the threshold of pain stimulus in mice. The extract significantly protected rats from aspirin, indomethacin and reserpine induced ulcers. These results revealed that the plant, Diodia scandens has potential medicinal value.     

Effects of Hypericum montbretti Extract on the Central Nervous System and Involvement of GABA (A)/Benzodiazepine Receptors in its Pharmacological Activity

The present study was undertaken to investigate the putative activity of a methanol extract of Hypericum montbretti (Guttiferae) on the central nervous system. Rutin (1519 ppm) and quercitrin (784 ppm) were identified as the major phenolic compounds in the extract. When administered at 25, 50 and 100 mg/kg doses, the extract decreased the total number of head‐dipping behaviours performed by mice during a hole‐board test. Administration of both the extract and diazepam (2 mg/kg) reduced spontaneous locomotory activity, potentiated hexobarbital (60 mg/kg)‐induced sleeping parameters and prevented pentylenetetrazole (80 mg/kg)‐induced seizures relative to the controls. These findings are the first to indicate the sedative and anticonvulsant activities of H. montbretti extract. Atropine (2 mg/kg) and naloxone (5 mg/kg) pre‐treatment did not reverse the sedative effect, indicating that muscarinic and opioidergic mechanisms did not contribute to the pharmacological action. However, pre‐treatment with flumazenil (a benzodiazepine receptor antagonist) reversed both the sedative and anticonvulsant effects induced by a 100 mg/kg dose of the extract, indicating the involvement of the GABA(A)‐benzodiazepine receptor complex. In conclusion, H. montbretti extract is a novel candidate as a sedative and anticonvulsant drug for the treatment of sleep disorders and for the prevention of epileptic seizures. Copyright © 2012 John Wiley & Sons, Ltd.     

羌活水溶部分的抗心律失常作用

实验表明羌活水溶部分对乌头碱引起的小白鼠、大白鼠实验性心律失常及氯仿-肾上腺素所致家兔实验性心律失常均有明显的对抗作用。其抗心律失常作用为羌活溶液的非无机盐部分。     

Hypoglycaemic activity of Anthocleista vogelii (Planch) aqueous extract in rodents

The hypoglycaemic effect of Anthocleista vogelii was studied in mice, rats and rabbits. Aqueous extract of the plant obtained by infusion from finely pulverized root was used. The extract (100, 400 and 800 mg/kg) induced significant hypoglycaemic activity in a dose-related fashion at 2 h after oral administration in mice and rats with ED₂₅ of 250 mg/kg and 350 mg/kg respectively. The extract (800 mg/kg, orally) similarly induced statistically significant lowering of blood glucose levels at 8 h in normoglycaemic rabbits. The extract (400 mg/kg and 800 mg/kg, orally) also caused reduction of blood glucose levels in alloxan-induced diabetic animals. The results of this study indicate that the aqueous extract of the roots of Anthocleista vogelii possess favourable hypoglycaemic activity both in normo and hyperglycaemic animals compared to chlorpropamide as a standard.     

Anticonvulsant effects of Searsia dentata (Anacardiaceae) leaf extract in rats

Searsia species are used in South Africa to treat epilepsy. Previous studies have demonstrated an in vitro N‐methyl‐D‐aspartic acid (NMDA) receptor antagonistic effect of the ethanolic leaf extract. The aim of this study was to evaluate the potential anticonvulsant properties of the ethanolic extract of S. dentata in various animal models of epilepsy. The extract was submitted to a screening in anticonvulsant assays including NMDA‐, kainic acid (KA)‐, pentylenetetrazol (PTZ)‐ and bicuculline (BIC)‐induced seizures in rats. The extract protected 47% of the PN 18 Wistar pups (postnatal day 18, date of birth PN 0) (p < 0.05, n > 10) against NMDA‐induced seizures and significantly delayed the onset of PTZ‐induced seizures (p < 0.05, n > 8) at a dose of 250 mg/kg. A dose optimum was detected at 500 mg/kg for protection against KA‐(63% protection, p < 0.05, n > 8) and BIC‐induced seizures (50% protection, p < 0.05, n > 8) in young adult and PN 18 rats, respectively. The ethanolic extract of S. dentata showed anticonvulsive properties in several models of epilepsy. These results are compatible with previous findings of NMDA receptor antagonism. Due to the complex composition of the extract, the effect might be caused by more than one compound. Copyright © 2009 John Wiley & Sons, Ltd.     

Pharmacological screening of the methanol and dichloromethanol extracts of Genista patens

The pharmacological effects of the dichloromethanol and methanol extracts obtained from leaves and stems of Genista patens DC were analysed in in vitro and in vivo models. Both extracts showed low acute toxicity (LD₅₀ > 3 g/kg), CNS depressor and antiinflammatory activity, and similar analgesic effect in models of chemical and thermal stimulation. Furthermore, the dichloromethanol extract (1–20 mg/kg) induced a pronounced dose-dependent decrease on blood pressure. On isolated organs, the dichloromethanol extract (1, 10, 100 μg/mL) shifted the concentration-effect curve to the right for ACh and reduced the E_max induced by histamine without modifying responses induced by noradrenaline and serotonin.