Pharmacological and toxicological investigations on Foeniculum vulgare dried fruit extract in experimental animals

The ethanol extract of the dried ripe fruit of Foeniculum vulgare (500 mg/kg) was tested for diuretic, analgesic, antipyretic, antimicrobial, cytotoxic activities and its effect on bile secretion in rats. Also, the acute toxicity after 0.5, 1 and 3 g/kg was investigated in mice. The extract showed diuretic, analgesic, antipyretic activities and it enhanced bile secretion. As an antimicrobial agent, the extract inhibited the growth of Staphylococcus aureus and Bacillus subtilis and showed a marked mitodepressive effect. At a dose of 3 g/kg, it caused piloerection and it depressed locomotor activity but caused no deaths when administered acutely to mice.     

Analgesic and anti-inflammatory activity of Crinum glaucum aqueous extract.

The anti-inflammatory and analgesic effects of the aqueous extract of Crinum glaucum were evaluated in mice and rats using the carrageenan- and dextran-induced paw oedema, acetic acid-induced writhing, cold water tail flick and formalin pain tests. The extract (100-400 mg/kg) and acetylsalicylic acid (100 mg/kg) produced a significant (P<0.05) inhibition of the second phase response in the formalin pain model, while only the high dose (400 mg/kg) of the extract showed an antinociceptive effect in the first phase. The extract also showed a dose-dependent inhibition of acetic acid-induced abdominal writhes. The tail flick latency was dose dependently enhanced by the extract but this was significantly (P<0.05) lower than that produced by morphine (2 mg/kg). The extract (125-500 mg/kg) administered 1 h before or after carrageenan-induced paw swelling produced a dose dependent inhibition of the oedema. No effect was observed with the dextran-induced oedema model. The data obtained suggest that the anti-inflammatory and analgesic effects of the extract may be mediated via both peripheral and central mechanisms.     

Evaluation of the antinociceptive properties from Brillantaisia palisotii Lindau stems extracts

Brillantaisia palisotii Lindau is a plant belonging to Acanthaceae family and it is widely found in tropical regions. Some species of this family are used in the folk medicine to treat several disorders, mainly those that involve analgesic processes. In this work it was evaluated antinociceptive activities of dichloromethane, ethyl acetate and n-butanol extracts obtained from Brillantaisia palisotii stems in peripheral (acetic acid-induced writhing) and central (tail flick and hot plate) analgesic models. All three extracts significantly inhibited the total number of writhing in a dose dependent manner. A spinal antinociceptive effect was observed with all three extracts and with similar patterns to all doses (1-30 mg/kg). Although ethyl acetate extract did not demonstrate supra-spinal activity, the effects observed with dichloromethane extract showed analgesic effect with all doses. The n-butanolic extract had activity only with the lowest dose (1 mg/kg). Our results indicate that all extracts from Brillantaisia palisotti stems develop peripheral and spinal analgesic activity, being the dichloromethane extract the only one with supra-spinal analgesic effect.     

Pharmacological evidence favouring the folkloric use of Diospyros mespiliformis Hochst in the relief of pain and fever

The methanol extract of Diospyros mespiliformis was evaluated for its claimed folkloric usage in the relief of pain and fever. Antipyretic, analgesic and anti-inflammatory effects of the extract were evaluated in rats and mice. Studies were carried out on yeast-induced pyrexia in rats, acetic acid-induced writhing in mice, formalin test and egg albumin-induced anti-inflammatory activity in rats. The extract (50 and 100 mg/kg i.p.) gave a potent antipyretic effect for 100 mg/kg and significant activity (P<0.05) against all the analgesic and anti-inflammatory models used. The LD(50) of the extract was estimated to be 513.80+/-33.92 mg/kg i.p. in mice. These results provide support for the use of the plant in relieving pain and fever.     

Evaluation of the analgesic effect of Echium amoenum Fisch & C.A. Mey. extract in mice: possible mechanism involved

Echium amoenum Fisch & C.A. Mey. has been used in Iranian traditional medicine as demulcent and analgesic in common cold from long ago. In this investigation, the analgesic effect of the methanolic extract of the petals of this plant on male albino mice was evaluated by formalin and hot-plate test. The methanolic percolated extract with different doses 5, 10, 20 and 30 mg/kg were injected intraperitoneally to mice. The results showed that the dose of 10 mg/kg of extract had the highest analgesia in formalin (P<0.05) and hot-plate test (P<0.01) compared to the control group. The analgesic effect of extract was lower than morphine 2.5 mg/kg and ASA 300 mg/kg in the chronic phase of pain in formalin test (P<0.05) and in hot-plate test too (P<0.05). Pretreatment of animal with naloxone 4 mg/kg, s.c. 5 min before extract, decreased the analgesia induced by extract in hot-plate and acute phase of formalin tests; therefore, the opioid receptor may be involved at least partly in the analgesic effect of Echium amoenum extract. The results suggested that Echium amoenum extract has a suitable analgesic effect and further studies are required to evaluate these effects and the potential of the plant.     

Study on the antinociceptive effects of Thymus broussonetii Boiss extracts in mice and rats

In Morocco, Thymus broussonetii is widely used in folk medicine for the treatment of a variety of diseases including gastroenteric and bronchopulmonary disorders and to relieve dolorous process. The antinociceptive effect of the aqueous, butanolic and ethyl acetate extracts of this species was examined in rats and mice using chemical and thermal models. The results obtained showed that aqueous and butanolic extracts exerted an antinociceptive activity in the two phases of formalin (50-300 mg/kg), tail immersion and writhing tests. Whereas, the ethyl acetate extract reduced the nociceptive response only in the second phase of formalin (100-300 mg/kg) and writhing tests. The aqueous extract, which is the most effective, contains active analgesic principles acting both centrally and peripherally. Furthermore, this antinociceptive effect has been avoided by naloxone at a dose of 1mg/kg in the first phase of formalin and hot plate tests indicating that this extract acts partly through an opioid-mediated mechanism. The present results demonstrated that Thymus broussonetii contains active constituents which possess antinociceptive activity justifying its popular use to relieve some pains.     

Anti-inflammatory, analgesic and antipyretic effects of methanol extract from Bauhinia racemosa stem bark in animal models

In this study, the anti-inflammatory, analgesic, and antipyretic effects of 50, 100 and 200 mg/kg body weight of methanol extract obtained from Bauhinia racemosa stem bark, the so-called MEBR, were investigated. The effects of MEBR on the acute and chronic phases of inflammation were studied in carrageenan, dextran and mediators (histamine and serotonin)-induced paw oedema and cotton pellet-induced granuloma, respectively. Analgesic effect of MEBR was evaluated in acetic acid-induced writhing and hotplate tests. Antipyretic activity of MEBR was evaluated by yeast-induced hyperpyrexia in rats. The anti-oedema effect of MEBR was compared with 10 mg/kg of indomethacin orally. In acute phase of inflammation, a maximum inhibition of 44.9, 43.2, 44.8 and 45.9% (P<0.001) was noted at the dose of 200 mg/kg b.w. after 3h of treatment with MEBR in carrageenan, dextran, histamine and serotonin-induced paw oedema, respectively. Administration of MEBR (200 mg/kg b.w.) and indomethacin (10 mg/kg b.w.) significantly (P<0.05) decreased the formation of granuloma tissue induced by cotton pellet method at a rate of 50.4 and 56.2%, respectively. The extract also inhibited peritoneal leukocyte migration in mice. The MEBR also produced significant (P<0.01) analgesic activity in both models. Further, the MEBR potentiated the morphine- and aspirin-induced analgesic in mice. Treatment with MEBR showed a significant (P<0.01) dose-dependent reduction in pyrexia in rats. The results suggest that MEBR possess potent anti-inflammatory, analgesic and antipyretic activity.     

Anti-inflammatory and analgesic activity of Biebersteinia multifida DC. root extract

The root of Biebersteinia multifida DC (Geraniaceae), a native plant of Iran, has been used topically for the treatment of musculoskeletal disorders as a folk medicine. The anti-inflammatory and analgesic effects of the root extract were studied using carrageenan induced edema and formalin tests. A similar activity was seen between Biebersteinia multifida root extract (10 mg/kg; i.p.) and indomethacin (4 mg/kg; i.p.) in carrageenan test. The results of formalin test showed the analgesic activity of the root extract (50 mg/kg; i.p.) was comparable with morphine (10 mg/kg; i.p.) at the first phase of formalin test. Furthermore, the probable ulcerogenic activity of the root extract was also studied. The extract did not show any ulcerogenic effect at anti-inflammatory doses (10 mg/kg; p.o.).     

The analgesic effect of the methanolic extract of Acanthus montanus

The analgesic effect of the methanolic leaf extract of Acanthus montanus was studied in rats using the cold water tail flick assay, and in mice using the tail immersion, tail clip, acetic acid induced writhing and formalin pain tests. The results showed dose-dependent and significant (P<0.05) increases in pain threshold, at 60 min post treatment, with doses of 200 and 400 mg/kg of the extract in tail flick, tail immersion and tail clip methods. The effects of the extract were significantly (P<0.05) lower than those produced by morphine (10 mg/kg) in the same tests. The extract (100-400 mg/kg) exhibited a dose-dependent inhibition of writhing and also showed a significant (P<0.001) inhibition of both phases of the formalin pain test, but with a less intense effect on the first than on the second phase. The results indicate that the analgesic effect of Acanthus montanus methanolic extract is both centrally and peripherally mediated.     

Anti-inflammatory and analgesic activity of Peperomia pellucida (L.) HBK (Piperaceae)

An aqueous extract of the aerial part of Peperomia pellucida (L.) HBK (Piperaceae) was tested for anti-inflammatory (paw edema induced by carrageenin and arachidonic acid) and analgesic activity (abdominal writhes and hot plate) in rats and mice, respectively. Oral administration of 200 and 400 mg/kg of the aqueous extract exhibited an anti-inflammatory activity in the carrageenin test, which was based on interference with prostaglandin synthesis, as confirmed by the arachidonic acid test. In the abdominal writhing test induced by acetic acid, 400 mg/kg of the plant extract had the highest analgesic activity, whereas in the hot-plate test the best dose was 100 mg/kg. The LD(50) showed that Peperomia pellucida (5000 mg/kg) presented low toxicity.     

Evaluation of the analgesic, anti-inflammatory and anti-diabetic properties of Sclerocarya birrea (A. Rich.) Hochst. stem-bark aqueous extract in mice and rats

In order to appraise some of the ethnomedical uses of Sclerocarya birrea (A. Rich.) Hochst., subspecies caffra (Sond.) Kokwaro [family: Anacardiaceae], the present study was undertaken to investigate the analgesic, anti-inflammatory and anti-diabetic properties of the plant's stem-bark aqueous extract in experimental models of pain, inflammation and diabetes mellitus. The analgesic effect of Sclerocarya birrea stem-bark aqueous extract was evaluated in mice, while its anti-inflammatory and anti-diabetic effects were investigated in rats. Diclofenac (DIC, 100 mg/kg p. o.) and chlorpropamide (250 mg/kg p. o.) were used respectively as reference analgesic, anti-inflammatory and anti-diabetic agents for comparison. Like diclofenac (DIC, 100 mg/kg p. o.), Sclerocarya birrea stem-bark aqueous extract (SBE, 100-800 mg/kg p. o.) produced dose-dependent, significant protection (p < 0.05-0.001) against electrical heat-induced pain. The plant extract (SBE, 25-800 mg/kg p. o.) also produced dose- and time-related, sustained and significant reductions (p < 0.05-0.001) in the fresh egg albumin-induced acute inflammation of the rat hind paw oedema. However, the analgesic and anti-inflammatory effects of the plant's extract were found to be approximately 10-15 times less than that of diclofenac. In one set of experiments involving hypoglycaemic/antidiabetic evaluation of the plant's extract, graded doses of Sclerocarya birrea stem-bark aqueous extract (SBE, 25-800 mg/kg p. o.) were separately administered to groups of fasted normal and fasted diabetic rats. In another set of experiments, a single dose of the plant's aqueous extract (SBE, 800 mg/kg p. o.) was used. The hypoglycaemic effect of this single dose of Sclerocarya birrea stem-bark aqueous extract (SBE, 800 mg/kg p. o.) was compared with that of chlorpropamide (250 mg/kg p. o.) in both fasted normal and fasted streptozotocin (STZ)-treated diabetic rats. Following acute treatment, relatively moderate to high doses of Sclerocarya birrea stem-bark aqueous extract (SBE, 25-800 mg/kg p. o.) produced dose-dependent, significant reductions (p < 0.05-0.001) in the blood glucose concentrations of both fasted normal and fasted diabetic rats. Chlorpropamide (250 mg/kg p. o.) also produced significant reductions (p < 0.05-0.001) in the blood glucose concentrations of the fasted normal and fasted diabetic rats. Administration of the single dose of Sclerocarya birrea stem-bark aqueous extract (SBE, 800 mg/kg p. o.) significantly reduced (p < 0.01-0.001) the blood glucose levels of both fasted normal (normoglycaemic) and fasted STZ-treated, diabetic rats. The results of this experimental animal study indicate that Sclerocarya birrea stem-bark aqueous extract possesses analgesic, anti-inflammatory and hypoglycaemic properties. These experimental findings lend pharmacological support to the suggested folkloric uses of the plant's stem-bark in the management and/or control of pain, inflammatory conditions, and adult-onset, type-2 diabetes mellitus in some communities of South Africa.     

Antinociceptive profile of the methanolic extract of Neorautanenia mitis root in rats and mice

The antinociceptive activity of the methanolic extract of Neorautenania mitis was studied in mice and rats. Five experimental models of nociception employed were: acetic acid-induced abdominal constriction and hot-plate test in mice, formalin-induced pain, analgesy-meter and Randall-Selitto tests in rats. The antinociceptive action of the extract was tested against naloxone in the hot-plate test in a bid to further elucidate probable mechanisms of antinociception. Results showed that the extract at doses of 5, 10 and 20 mg/kg body weight caused significant (P<0.05) dose-dependent antinociceptive activity in all the nociceptive models. Naloxone (2 mg/kg), significantly (P<0.05) antagonised the antinociceptive activity at the highest dose of the extract (20 mg). The study showed that the methanolic extract of Neorautanenia mitis possesses both peripherally and centrally mediated antinociceptive activity. The peripherally mediated action may be linked partly to lipoxygenases and/or cyclo-oxygenases, while the central anti-nociception is likely to be mediated via opioid receptors in the CNS.     

Hypoglycaemic activity of Geranium core-core,Oxalis rosea and Plantago major extract in rats

The hypoglycaemic activity of ‘Core-core’ (Geranium core-core, Geraniaceae), ‘Culle’ (Oxalis rosea, Oxalidaceae) and ‘Llantén’ (Plantago major, Plantaginaceae) crude extracts was assessed in normoglycaemic rats. Furthermore, the hypoglycaemic activity of Core-core extract was evaluated in alloxan-diabetic rats. A single oral dose of 500 mg/kg Core-core extract significantly reduced glycaemia in normal rats under glucose tolerance test conditions (p < 0.01), while Culle and Llantén were devoid of activity. The effect was lower than a single oral dose of 100 mg/kg tolbutamide. After 7 days oral treatment at 250 mg extract/kg body weight, Core-core significantly reduced glycaemia (p<0.01) in normal rats under oral glucose tolerance conditions. In alloxan-diabetic rats, a single oral dose of 500 mg/kg and chronic treatment at 250 mg/kg Core-core extract significantly reduced glycaemia in glucose tolerance test conditions at p < 0.05 and p < 0.01, respectively. During the acute oral toxicity study, animals treated with Core-core extract exhibited no symptoms of drug-induced toxicity with doses up to 5 g/kg.     

CNS activity of Calotropis gigantea roots

Alcoholic extract of peeled roots of Calotropis gigantea R.Br. (Asclepiadaceae) was tested orally in albino rats at the dose level of 250 and 500 mg/kg bodyweight for CNS activity. Prominent analgesic activity was observed in Eddy's hot plate method and acetic acid induced writhings. The paw licking time was delayed and the numbers of writhings were greatly reduced. Significant anticonvulsant activity was seen as there was a delay in the onset of pentylenetetrazole induced convulsions as well as decrease in its severity. The extract treated rats spent more time in the open arm of EPM showing its antianxiety activity. There was a decrease in the locomotor activity. The fall off time (motor coordination) was also decreased. A potentiation in the pentobarbitone-induced sleep due to the sedative effect of the extract was observed. No mortality was seen upto the dose of 1 g/kg. These results show the analgesic, anticonvulsant, anxiolytic and sedative effect of the extract.     

Analgesic properties of the aqueous and ethanol extracts of the leaves of Kalanchoe crenata (Crassulaceae)

The aqueous and ethanol extracts of the dry leaves of Kalanchoe crenata (300 and 600 mg/kg) were evaluated for their analgesic properties on the pain induced by acetic acid, formalin and heat in mice and by pressure on rats. The ethanol extract of K. crenata at a dose of 600 mg/kg produced an inhibition of 61.13% on pain induced by acetic acid and 50.13% for that induced by formalin. An inhibition of 67.18% was observed on pain induced by heat 45 min after the administration of the extract. The aqueous extract administered at a dose of 600 mg/kg produced a maximum effect of 25% on pain induced by pressure. These activities were similar to those produced by a paracetamol-codeine association, while indomethacin exhibited a protective effect only against the writhing test. Our results suggest that the leaves of K. crenata could be a source of analgesic compounds.     

Antihyperglycemic Activity of Extracts from Boldoa purpurascens Leaves in Alloxan‐Induced Diabetic Rats

In order to investigate the potential use of Boldoa purpurascens against diabetes, the antihyperglycemic effect of an ethanol extract obtained from its leaves was evaluated at doses of 50, 100 and 200 mg/kg in rats after induction of hyperglycemia by alloxan. Insulin 5 IU/kg was used as positive control and NaCl 0.9% as negative control. A similar experiment was performed with the aqueous extract used at doses of 50 and 100 mg/kg using metformin at a dose of 50mg/kg as positive control. Statistical analysis was carried using the Kruskal–Wallis test with an interval of trust of 99%. The ethanolic and aqueous extract of B. purpurascens showed a significant decrease of blood glucose levels 72 h after administration. Phytochemical analysis of the ethanol extract showed the presence of D‐pinitol, a compound known for its hypoglycemic properties. In conclusion, ethanolic as well as aqueous extracts of B. purpurascens leaves show antihyperglycemic activity, possibly due to the presence of D‐pinitol and flavonoids. Copyright © 2012 John Wiley & Sons, Ltd.     

Preliminary pharmacological screening of Bixa orellana L. leaves

Preliminary pharmacological studies were performed on the methanol extract of Bixa orellana L. (Bixaceae) leaves to investigate neuropharmacological, anticonvulsant, analgesic, antidiarrhoeal activity and effect on gastrointestinal motility. All studies were conducted in mice using doses of 125, 250 and 500 mg/kg of body weight. In the pentobarbitone-induced hypnosis test, the extract statistically reduced the time for the onset of sleep at 500 mg/kg dose and (dose-dependently) increased the total sleeping time at 250 and 500 mg/kg dose. A statistically significant decrease in locomotor activity was observed at all doses in the open-field and hole-cross tests. In the strychnine-induced anticonvulsant test, the extract increased the average survival time of the test animals (statistically significant at 250 and 500 mg/kg). The extract significantly and dose-dependently reduced the writhing reflex in the acetic acid-induced writhing test. Antidiarrhoeal activity was supported by a statistically significant decrease in the total number of stools (including wet stools) in castor oil-induced diarrhoea model. A statistically significant delay in the passage of charcoal meal was observed at 500 mg/kg in the gastrointestinal motility test. The extract was further evaluated in vitro for antioxidant and antibacterial activity. It revealed radical scavenging properties in the DPPH assay (IC(50)=22.36 microg/ml) and antibacterial activity against selected causative agents of diarrhoea and dysentery, including Shigella dysenteriae.     

Pharmacological Study of Cuscuta campestris Yuncker

The dried ethanol extract of the whole plant of Cuscuta campestris Yuncker was studied for its analgesic, antipyretic, antiinflammatory as well as CNS-depressant activities. The extract was given orally at doses of 50 and 100 mg/kg. A significant protection against the p -benzoquinone-induced writhing response in mice was observed. A marked lowering of the body temperature of both hyperthermic as well as normothermic mice was produced. Therefore, the extract possesses a hypothermic rather than an antipyretic effect. A marked inhibition of the carrageenan-induced rat hind paw oedema was also obtained. Regarding its CNS action, the extract produced a decrease in the motor activity of mice placed on a rotarod. In the conditioned avoidance reaction test the percentage of failure to avoid electric shock was shown to be increased after administration of the extract without any effect on the escape behaviour of the trained rats. Therefore, the CNS-depressant activity of the extract seems to be due to a tranquillizing effect. It could be concluded that the extract possesses analgesic, hypothermic, antiinflammatory as well as CNS-depressant activities.     

Further studies on the antihepatotoxic activity of Phyllanthus maderaspatensis Linn

Phyllanthus maderaspatensis (whole plant extracts) was evaluated for its antihepatotoxic and choleretic activities in rats. The plant extracts (200 mg/kg, n-hexane, ethyl alcohol or water) showed a remarkable hepatoprotective activity against acetaminophen-induced hepatotoxicity as judged from the serum marker enzymes. The water and ethyl alcohol extracts showed moderate activity compared to the n-hexane extract, which showed activity at a dose as low as 1.5 mg/kg. The antihepatotoxicity of the hexane extract was found to be better than silymarin, a standard hepatoprotective herbal drug. The effect of n-hexane extract was found to be concentration-dependent. This extract also exhibited choleretic activity in normal rats, and in vitro hydroxyl radical scavenging activity and inhibition of lipid peroxidation.     

紫背鼠尾草总提物抗炎镇痛作用的研究

目的：研究唇形科鼠尾草属植物紫背鼠尾草的抗炎镇痛等药理活性。方法：通过二甲苯致小鼠耳肿胀、鸡蛋清致大鼠足趾肿胀、醋酸致小鼠扭体和热刺激小鼠等4种药理模型对紫背鼠尾草乙醇总提取物进行抗炎镇痛的研究。结果：在抗炎药理模型中,实验结果显示紫背鼠尾草乙醇总提取物在200mg/kg时具有显著的抗炎作用;在镇痛药理模型中,实验结果表明,紫背鼠尾草乙醇总提取物在剂量200～400mg/kg时具有较明显的镇痛作用,在100mg/kg时作用不太明显,显示出镇痛作用随剂量的增加而增强。结论：紫背鼠尾草乙醇总提取物抗炎镇痛作用显著,说明了紫背鼠尾草具有抗炎镇痛的功效,为该植物进一步的开发利用提供药效学资料。