Antinociceptive effect of Lecythis pisonis Camb. (Lecythidaceae) in models of acute pain in mice

Ethnopharmacological relevance

Lecythis pisonis Camb., also known in Brazil as sapucaia, is used in folk medicine against pruritus, muscle pain and gastric ulcer.

Aim of the study

To investigate the antinociceptive effect of ethanol extract from Lecythis pisonis leaves (LPEE), fractions (hexane-LPHF, ether-LPEF and ethyl acetate-LPEAF) and mixture of triterpenes [ursolic and oleanolic acids (MT)] in mice.

Materials and methods

LPEE and LPEF were evaluated on the acetic acid induced writhings and formalin, capsaicin and glutamate tests. In addition, MT was investigated on the writhings induced by acetic acid, capsaicin and glutamate tests. In the study of some possible mechanisms involved on the antinociceptive effect of LPEF, it was investigated the participation of opioid system, K⁺_ATP channels and l-arginine-nitric oxide pathway.

Results

LPEE (12.5 and 25 mg/kg, p.o.), LPEF and MT (6.25, 12.5 and 25 mg/kg, p.o.) reduced the writhings in comparison to saline. LPEE (100 mg/kg, p.o.) and LPEF (50 mg/kg, p.o.) were effective in inhibiting both phases of formalin test. In capsaicin test, LPEE (100 and 200 mg/kg, p.o.), LPEF (12.5–50 mg/kg, p.o) and MT (6.25–25 mg/kg, p.o.) showed a significant antinociceptive effect compared to the control. LPEE (25 and 50 mg/kg, p.o.), LPEF (50 and 100 mg/kg, p.o.) and MT (12.5 and 25 mg/kg, p.o.) reduced the glutamate-evoked nociceptive response. Treatment with naloxone, l-arginine and glibenclamide reversed the effect of LPEF in glutamate test.

Conclusions

These results indicate the antinociceptive effect of Lecythis pisonis leaves and suggest that this effect may be related to opioid pathway, K⁺_ATP channels, and l-arginine-nitric oxide modulation. Furthermore, these data support the ethnomedical use of this plant.     

Evaluation of antidiabetic and antihyperlipidemic activity of Artemisia indica linn (aeriel parts) in Streptozotocin induced diabetic rats

Ethnopharmacological relevance

Diabetes mellitus is a major metabolic disorder affecting a huge population all over the world. Artemisia species have been extensively used for the management of diabetes in folkloric medicine. The present study is designed to investigate the antidiabetic and antihyperlipidemic effects of aeriel parts of Artemisia indica.

Materials and methods

Hydromethanolic crude extracts, chloroform, ethyl acetate and n-butanol fractions of aerial parts of Artemisia indica were tested for their antidiabetic potential in Streptozotocin (STZ) (50 mg/kg, i.p.) induced diabetic Sprague-Dawley rats. Blood glucose level, body weight, serum lipid profile and activities of liver enzymes were determined. The extracts were further subjected to preliminary phytochemical analysis.

Results

A daily oral dose of hydromethanolic crude extracts (200 and 400 mg/kg b.w.) and chloroform fraction (200 mg/kg b.w.) of Artemisia indica for 15 days showed a significant reduction in blood glucose level which was comparable to that of the standard antidiabetic drug, glibenclamide (500 μg/kg, p.o.). Artemisia indica extracts also showed reduction in total cholesterol, triglycerides and low density lipoproteins as well as serum creatinine level, serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT) and alkaline phosphatase (ALP) in diabetic rats.

Conclusion

According to the results Artemisia indica possesses hypoglycemic, antihyperlipidemic and valuable effects on liver and renal functions in diabetic rats, which seems to validate its traditional usage.     

Analgesic and anti-inflammatory effects of Pistacia integerrima extracts in mice

Aim of study

Extracts of Pistacia integerrima galls have been dispensed by Traditional Practitioners of Subcontinent for chest diseases as well as for aches and pains in the body. This study was planned to evaluate the possible analgesic and antiinflammatory effects of Pistacia integerrima extracts.

Materials and methods

Analgesia was determined using acetic acid induced abdominal constriction and formalin induced paw licking in mice. Antinociceptive effect was observed by thermally induced algesia in mice.

Results

Pistacia integerrima leaves extracts showed significant response against chemically induced pain (P < 0.001) whereas galls extracts had highly significant protection (P < 0.0001) in a dose dependent manner. In thermally induced algesia, Pistacia integerrima galls extracts 200 mg/kg (p.o.), showed significant (P < 0.05) response but less than pentazocine and diclofenac, positive references. The extracts of Pistacia integerrima 50–200 mg/kg (p.o.) had modest activity against hind paw acute and chronic inflammation induced by formalin (P < 0.01).

Conclusion

These results demonstrate that Pistacia integerrima extracts have antinociceptive and analgesic effects and no apparent acute toxicity on oral administration.     

Antinociceptive and anti-inflammatory activities of Bowdichia virgilioides (sucupira)

Ethnopharmacological relevance

Bowdichia virgilioides Kunth (Leguminosae Papilonoideae) is a plant with anti-inflammatory activity used in folk medicine. The importance of this plant promoted its inclusion in Brazilian Pharmacopoeia.

Aim of the study

In order to evaluate the actions of this plant, studies were performed on antinociceptive and anti-inflammatory activities.

Materials and methods

The aqueous extracts (AE) of Bowdichia virgilioides inner bark and leaves were used at 100, 200, and 400 mg/kg. Antinociceptive activity of plant extract was evaluated by writhing, hot-plate and formalin tests. Anti-inflammatory activity was evaluated using paw oedema and peritonitis methods.

Results

Oral treatment with the AE of inner bark or leaves elicited inhibitory activity (P < 0.01) on acetic acid effect at 200 and 400 mg/kg, and reduced the formalin effect at the second-phase (200 and 400 mg/kg, P < 0.01), however it did not elicit any inhibitory effect on hot-plate test. The indomethacin inhibited the acetic acid-induced writhing and the formalin effect at the second-phase (P < 0.001), and the morphine reduced the both phases of formalin test (P < 0.001). Carrageenan-induced oedema formation and neutrophil migration into the peritoneal cavity were reduced with the AE of inner bark or leaves at 100, 200, and 400 mg/kg (P < 0.05), and by the reference compounds aspirin (P < 0.001) and dexamethasone (P < 0.001), respectively.

Conclusions

The AE of Bowdichia virgilioides shows antinociceptive and anti-inflammatory activities, supporting the folkloric usage of the plant to treat various inflammatory diseases.     

Evaluation of mechanisms involved in the antinociception of the ethanol extract from the inner bark of Caesalpinia pyramidalis in mice

Ethnopharmacological relevance

Caesalpinia pyramidalis Tul. (Fabaceae) is an endemic tree of the Northeast region of Brazil, mainly in the Caatinga region. More commonly, inner bark or flowers are traditionally used to treat many painful and inflammatory processes. A common use of this plant is made by macerating a handful of its stem bark in a liter of wine or sugarcane brandy. It is drunk against stomachache, dysenteries, and diarrheas.

Materials and methods

The ethanol extract of Caesalpinia pyramidalis inner bark was used in mice via oral route, at the doses of 10, 30, and 100 mg/kg, in behavioral models of nociception and investigates some of the mechanisms underlying this effect.

Results

The ethanol extract (30 and 100 mg/kg, P<0.001), given orally, produced dose dependent inhibition of acetic acid-induced visceral pain. The ethanol extract also caused significant and dose-dependent inhibition of capsaicin-(100 mg/kg, P<0.001) and glutamate-(10, 30, and 100 mg/kg, P<0.01) induced pain. The antinociception caused by the ethanol extract (30 mg/kg) in the abdominal constriction test was significantly attenuated (P<0.001) by intraperitoneal treatment of mice with l-arginine (600 mg/kg).

Conclusions

Collectively, the present results suggest that the ethanol extract of Caesalpinia pyramidalis produced dose-related antinociception in several models of pain through mechanisms that involved both glutamatergic system and/or the l-arginine–nitric oxide pathway, supporting the folkloric usage of the plant to treat various painful processes.     

Aqueous extract of Artemisia capillaris exerts hepatoprotective action in alcohol–pyrazole-fed rat model

Ethnopharmacologic relevance

Artemisia capillaris, also called “InJin” in Korean, has been widely used to treat various hepatic disorders in traditional Oriental medicine.

Aims

The purpose of this study is to evaluate the hepatoprotective effect of Artemisia capillaris (aqueous extract, WAC) on alcoholic liver injury.

Materials and methods

Liver injury was induced by oral administration of 30% alcohol (10 mL/kg, twice per day) plus pyrazole (PRZ, 30 mg/kg) with/without WAC (50, 100 mg/kg, orally once per day) or silymarin (50 mg/kg) for 10 days. The hepatoprotective effects were assessed by observing histopathological changes, hepatic transaminase enzymes, hepatic oxidation and antioxidant parameters, inflammatory cytokines, and alcohol metabolic enzymes in serum and hepatic gene expression level, respectively.

Results

Alcohol–PRZ treatment drastically increased the serum levels of aspartate transaminase (AST), alanine transaminase (ALT), and malondialdehyde (MDA) levels in serum and liver tissues while these changes were significantly ameliorated by WAC administration (p<0.05 or 0.01). The prominent microvesicular steatosis and mild necrosis in hepatic histopathology were induced by alcohol–PRZ treatment, but notably attenuated by WAC administration. Moreover, the alcohol–PRZ treatment-induced depletions of the antioxidant components including glutathione content, total antioxidant capacity (TAC), activities of glutathione peroxidase (GSH-Px), reductase (GSH-Rd), catalase, and superoxide dismutase (SOD) were significantly ameliorated by WAC administration (p<0.05, except GSH-Rd). These results were in accordance with the modulation of NF-E2-related factor (Nrf2) and heme oxygenase-1 (HO-1) gene expression. Alcohol–PRZ treatment increased the levels of tumor necrosis factor-alpha (TNF-α) and transforming growth factor-beta (TGF-β) in hepatic tissues. However they were significantly normalized by WAC administration (p<0.05 or 0.01). In addition, WAC administration significantly attenuated the alterations of aldehyde dehydrogenase (ALDH) level in serum and hepatic gene expressions of ALDH and alcohol dehydrogenase (ADH).

Conclusions

These results support the relevance in clinical use of Artemisia capillaris for alcohol-associated hepatic disorders. The underlying mechanisms may involve both enhancement of antioxidant activities and modulation of proinflammatory cytokines.     

Evaluation of the diuretic and analgesic activities of the rhizomes of Rumex abyssinicus Jacq in mice

Aim of the study

Rumex abyssinicus Jacq (Polygonaceae) has been used traditionally for treatment of hypertension, inflammatory and painful conditions in Ethiopia. The present study aimed to evaluate the diuretic and analgesic activities of extracts of Rumex abyssinicus at different doses in mice.

Materials and methods

The effect on urine volume and urinary electrolyte (Na⁺, K⁺ and Cl⁻) was assessed for a period of 5 h following oral administration of aqueous (500 mg/kg, 750 mg/kg or 1000 mg/kg) or 80% methanolic (250 mg/kg, 500 mg/kg or 750 mg/kg) extract or furosemide (10 mg/kg). Acetic acid-induced writhing and hot-plate tests were employed to study the analgesic effect of 80% methanolic extracts (250 mg/kg, 500 mg/kg or 1000 mg/kg, P.O.) and compared with that of aspirin (100 mg/kg, P.O.) or morphine (10 mg/kg, sc).

Results

The extracts displayed dose-dependent diuretic and analgesic effects. The highest doses of both extracts markedly and significantly increased (P < 0.001) urine volume and urinary electrolytes, qualitatively similar to that of furosemide. 1000 mg/kg of the extract reduced the number of writhing by 67.6% (P < 0.001) and conferred more than 70% protection against thermally induced pain stimuli after 45 min of treatment comparable to that of aspirin and morphine, respectively.

Conclusion

These findings collectively indicate that the extracts exhibited significant diuretic and analgesic activities, providing evidence, at least in part, for its folkloric use.     

Further evaluation of antihyperglycaemic activity of Hunteria umbellata (K. Schum) Hallier f. seed extract in experimental diabetes

Ethnopharmacological relevance

In African traditional medicine, water decoction made from the dry seeds of Hunteria umbellata (K. Schum) Hallier f. is highly valued in the management of diabetes mellitus.

Aim

In the present study, the antihyperglycaemic activity of the seed aqueous extract of Hunteria umbellate (K. Schum) Hallier f. (HU) was investigated in alloxan-induced, high fructose- and dexamethasone-induced hyperglycaemic rats.

Materials and methods

Alloxan-induced, dexamethasone-induced and high fructose-induced hyperglycaemic rats were treated with single, daily oral administration of 1 mg/kg of glibenclamide, 50 mg/kg, 100 mg/kg and 200 mg/kg of HU in Groups III, IV, V and VI, for 14 days, 21 days and 8 weeks, respectively. The effects of these drugs on FBG, free plasma insulin levels, HbA_1c, serum TG and TC, and insulin resistance indices were investigated.

Results

Data generated in the current study showed that glibenclamide and graded oral doses of HU caused significant dose related (p < 0.05, <0.01 and <0.001) reductions in FBG when compared to the values obtained for the model control (Group II) rats. Similarly, daily oral administration of 66.7 g/kg fructose to rats for 8 weeks was associated with significant (p < 0.001) hyperglycaemia, elevations in plasma HbA_1c, free insulin, fasting insulin resistance indices, serum TG, and cholesterol. However, concomitant oral treatments with 1 mg/kg of glibenclamide, 50 mg/kg, 100 mg/kg, and 200 mg/kg of HU extract significantly and dose dependently (p < 0.05, <0.01 and <0.001) attenuated development of hyperglycaemia, decreased levels of plasma HbA_1c, free insulin, and serum triglyceride and cholesterol, in the Groups III, IV, V and VI rats, respectively, when compared to fructose-induced hyperglycaemic (Group II) rats. Similar effect was also recorded in the dexamethasone-induced hyperglycaemic rats.

Conclusion

Results of this study suggest that the hypoglycaemic and antihyperlipidaemic effects of HU are mediated via enhanced peripheral glucose uptake and improvements in hyperinsulinaemia.     

Antipyretic and anti-inflammatory properties of the ethanolic extract,dichloromethane fraction and costunolide from Magnolia ovata (Magnoliaceae)

Aim of the study

Magnolia ovata (A.St.-Hil.) Spreng (formerly Talauma ovata), known as “pinha-do-brejo” or “baguaçu”, is a large tree widely distributed in Brazil. Its trunk bark has been used in folk medicine against fever. However, no data have been published to support the antipyretic ethnopharmacological use. This study investigated the antipyretic and anti-inflammatory effects of the ethanolic extract (EEMO), dichloromethane fraction (DCM), and the isolated compound costunolide.

Materials and methods

The antipyretic and anti-inflammatory activities were evaluated in experimental models of fever and inflammation in mice.

Results

The oral administration of EEMO, DCM and costunolide inhibited carrageenan (Cg)-induced paw oedema (ID₅₀ 72.35 (38.64–135.46) mg/kg, 5.8 (2.41–14.04) mg/kg and 0.18 (0.12–0.27) mg/kg, respectively) and was effective in abolishing lipopolysaccharide (LPS)-induced fever (30 mg/kg, 4.5 mg/kg and 0.15 mg/kg, respectively). EEMO was also effective in reducing cell migration in the pleurisy model. Intraplantar injection of costunolide also reduced the paw oedema, myeloperoxidase and N-acetyl-glucosaminidase activity induced by Cg in mice.

Conclusions

Collectively, these results show, for the first time, that extracts obtained from Magnolia ovata possess antipyretic and anti-inflammatory properties, and costunolide appears to be the compound responsible for these effects.     

Antidiabetic and antioxidant effect of various fractions of Phyllanthus simplex in alloxan diabetic rats

Aim of the study

To evaluate the antidiabetic and antioxidant effects of various fractions of Phyllanthus simplex on alloxan induced diabetes in rats.

Materials and methods

Hypoglycemic effect of Phyllanthus simplex fractions was evaluated in normal and diabetic rats. Diabetes was induced by intraperitoneal injection of alloxan monohydrate (120 mg/kg). Normal and diabetic rats were divided into different groups (six rats each group) and orally administered with petroleum ether (P.E.) (200 and 400 mg/kg), ethyl acetate (EtOAc) (100 and 200 mg/kg), methanol (125 and 250 mg/kg), water fraction (150 and 300 mg/kg) and glibenclamide (10 mg/kg) for 21 days. Blood samples were collected from overnight fasted normal rats on day 21, from overnight fasted diabetic rats at 7, 14 and 21 days of treatment and analyzed for blood glucose level. On day 22 blood samples were collected from diabetic rats to estimate biochemical parameters, rats were sacrificed by single stunning and tissues were excised to measure their antioxidant and glycogen status.

Results

In the normoglycemic rats, MeOH (125 and 250 mg/kg) and aqueous fractions (150 and 300 mg/kg) showed a significant (P < 0.05) hypoglycemic effect on day 21. In diabetic control rats, MeOH (125 and 250 mg/kg) and aqueous fractions (150 and 300 mg/kg) showed significant antihyperglycemic effect (P < 0.001). The active fractions (MeOH and aqueous) of Phyllanthus simplex also increased the body weight of diabetic rats significantly compared to the control group. The active fractions were able to normalize the marked alterations in antioxidant enzymes and antioxidant parameters levels in liver and kidney. Treatment with the active fractions also normalized the diabetic induced hyperlipidemia and liver glycogen.

Conclusions

These results demonstrate the antidiabetic and antioxidant potential of fractions of Phyllanthus simplex and suggests that the plant may have therapeutic value in diabetes and related complications.     

Anti-inflammatory activity of flavonoids from Cayaponia tayuya roots

Ethnopharmacological relevance

Taiuiá or tayuya (Cayaponia tayuya, Cucurbitaceae) is a climbing, lignified plant with a large swollen root that has traditionally been used as an anti-inflammatory and anti-rheumatic agent in the folk medicine of Brazil, Peru, and Colombia.

The aim of the study

We have assayed the pharmacological properties of a flavonoid fraction obtained from the butanol extract of Cayaponia tayuya roots using two models of topical mouse ear oedema, paying special attention to its influence on the induction on pro-inflammatory enzymes and peptidic mediators.

Material and methods

The in vivo experiments involved both the acute oedema induced by a single application of TPA and the subchronic inflammation brought on by repeated applications of TPA. The effects on the induction of pro-inflammatory enzymes and peptidic mediators in RAW 264.7 macrophages were analyzed with the aid of Western blot analysis.

Results

The extract was identified as a mixture of flavonoids in which vicenin-2, spinosin, isovitexin, and a mixture of swertisin and isoswertisin were found. In acute TPA-induced oedema in mouse ears, the flavonoid-enriched fraction (at a dose of 0.5 mg/ear) inhibited the oedema by 66% (4.2 ± 0.6 mg vs. 12.3 ± 1.4 mg, P < 0.01) while in the subchronic model, the inhibition reached 37% at a dose of 0.5 mg/ear × 7 applications (7.5 ± 0.6 mg vs. 11.9 ± 1.3 mg, P < 0.05). When assayed in vitro, the flavonoid showed no toxicity at 33.45 μg/mL on RAW 264.7 macrophages. Although the nitric oxide production in these cells was moderately reduced (42%) at 33.45 μg/mL, the flavonoid-enriched fraction had no effect on TNF-α production. In addition, at 22.30 μg/mL, the test sample inhibited both iNOS and COX-2 expression by 98% and 49%, respectively.

Conclusion

These results indicate that the anti-inflammatory activity of flavonoids from tayuya roots most likely stems from their inhibition of the induction of the enzymes COX-2 and iNOS.     

Ethanol extracts of Saururus chinensis suppress ovalbumin-sensitization airway inflammation

Aim of the study

The aerial part of Saururus chinensis has been used in folk medicine to treat several inflammatory diseases in China and Korea. Previously, our group reported that anti-asthmatic activity of an ethanol extract of Saururus chinensis (ESC) might occur, in part, via the inhibition of prostaglandin D₂ (PGD₂) and leukotriene C₄ (LTC₄) production, and degranulation reaction in vitro, as well as through the down-regulation of interleukin (IL)-4 and eotaxin mRNA expression in an in vivo ovalbumin-sensitization animal model. However, the effects of Saururus chinensis on eicosanoid generation, as well as Th2 cytokines and eotaxin production in an in vivo asthma model, have not been fully investigated. Moreover, it has not been determined whether ESC can ameliorate airway inflammation in vivo. In the present study, we investigated the therapeutic activity of Saururus chinensis on ovalbumin (OVA)-sensitized airway inflammation and its major phytochemical compositions.

Materials and methods

Asthma was induced in BALB/c mice by ovalbumin-sensitization and inhalation. ESC (10-100 mg/kg) or dexamethasone (5 mg/kg), a positive control, was administered 7 times orally every 12 h from one day before the first challenge to 1 h before the second challenge. The recruitment of inflammatory cells and hyperplasia of goblet cells were evaluated by H&E and PAS staining. Levels of Th2 cytokines, eotaxin, PGD₂ and LTC₄ were measured to evaluate the anti-inflammatory activity of ESC in OVA-sensitized mice. Contents of major components were analyzed by HPLC using a reversed-phase C18 column.

Results

ESC (10 mg/kg) suppressed allergic airway inflammation by inhibition of the production of IL-4 (P < 0.001), IL-5 (P < 0.05), IL-13 (P < 0.001), eotaxin (P < 0.001), PGE₂ (P < 0.001), LTC₄ (P < 0.001) in lung extract and IgE level (P < 0.001) in the serum. In addition, ESC (50 mg/kg) reduced the infiltration of inflammatory cells and hyperplasia of goblet cells in the lung tissues. The anti-inflammatory effect of ESC was comparable to that of the positive control drug, dexamethasone. Its major phytochemical composition includes manassantin A, B and sauchinone.

Conclusions

These results suggest that ESC decreased inflammation and mucus secretion in the OVA-induced bronchial asthma model, and its anti-asthmatic activity may occur in part via the inhibition of Th2 cytokines and eotaxin protein expression, as well as through prostaglandin E₂ (PGE₂) and leukotriene C₄ (LTC₄) generation. This effects may be attributed particularly to the presence of manassantin A, B and sauchinone major component evidenced by a HPLC analysis.     

Emblica officinalis and hepatocarcinogenesis: A chemopreventive study in Wistar rats

Introduction

Emblica officinalis L. commonly known as gooseberry, Phyllanthus emblica, Emblica, Indian gooseberry, amla is used in Indian system of medicine for the treatment of liver ailments.

Aim and Objectives

In the present study, we report that it ameliorates the carcinogenic response as it reverses the histopathological changes and reduces the number of γ-GT-positive foci induced by Solt Farber protocol in the liver of Wistar rats.

Materials and Methods

Tumors were induced by initiation with diethylnitrosoamine (DEN) (200 mg/kg body wt., i.p.) followed by promotion with 2-acetylaminoflourine (2-AAF) (0.02%, w/w in diet) for continuous 6 weeks and the animals were subjected to partial hepatectomy on day 21 of initiation.

Results

Pretreatment with defatted methanolic fruit extract (100 and 200 mg/kg b.w.) of Emblica officinalis showed significant partial recovery of pathological manifestations as compared to DEN and 2-AAF-treated group animals (p < 0.001) and suppressed the tumor forming potential of 2-AAF (p < 0.05) at both the doses.

Conclusion

Emblica officinalis has the potential to suppress carcinogen-induced response in rat liver.     

Evaluation of the analgesic and anti-inflammatory effects of the essential oil of Lippia gracilis leaves

Aim of the study

The aim of the present study is to investigate the antinociceptive, anti-inflammatory, and antioxidant activities of essential oil (EO) of Lippia gracilis Schauer (Verbenaceae) leaves to support the medicinal uses claimed by folklore practitioners in the caatinga region (semi-arid) of Northeastern Brazil.

Materials and methods

The chemical composition and antinociceptive and anti-inflammatory activities of the EO of Lippia gracilis leaves (50–200 mg/kg) were investigated. Antinociceptive activity of the EO was evaluated by writhing test. Anti-inflammatory activity of the EO was evaluated using paw oedema and peritonitis methods.

Results

Oral treatment with the EO of Lippia gracilis leaves elicited inhibitory activity on acetic acid effect at 50, 100, and 200 mg/kg (30.33 ± 2.36, 25.20 ± 1.48, and 21.00 ± 1.54 abdominal writhes, respectively, P < 0.05), as compared with the control group (36.73 ± 1.92 writhes). The compound acetylsalicylic acid (ASA, 300 mg/kg) inhibited the acetic acid-induced writhing (12.67 ± 0.50 abdominal writhes, P < 0.001). Carrageenan-induced oedema formation was reduced with the EO of Lippia gracilis leaves at 200 mg/kg (0.72 ± 0.06 mL h, P < 0.001) and by the reference compound ASA (300 mg/kg, 0.85 ± 0.04 mL h, P < 0.001), as compared with the control group (1.76 ± 0.06 mL h). Leukocyte migration into the peritoneal cavity induced by carrageenan was reduced with the EO of Lippia gracilis leaves at 50, 100, and 200 mg/kg (13.81 ± 0.61, 11.77 ± 0.91, and 10.30 ± 0.60 leukocytes × 10⁶/mL, respectively, P < 0.01), and by the compound dexamethasone (2 mg/kg, 5.34 ± 0.33 leukocytes × 10⁶/mL, P < 0.001), as compared with the control group (16.71 ± 0.54 leukocytes × 10⁶/mL). The analyses of the essential oil allowed the identification of Lippia gracilis as a thymol-p-cymene chemotype (32.68% and 17.82%, respectively).

Conclusions

The EO of Lippia gracilis leaves shows antinociceptive and anti-inflammatory activities.     

Anticonvulsant,anxiolytic and sedative activities of the aqueous root extract of Securidaca longepedunculata Fresen.

Aim of the study

The objective of this study is to investigate the anticonvulsant, anxiolytic and sedative activities of the aqueous root extract of Securidaca longepedunculata.

Materials and methods

The anticonvulsant effect of the aqueous root extract (100, 200 and 400 mg/kg) was evaluated in mice using the strychnine- and picrotoxin-induced seizure models. Its anxiolytic activity was evaluated using the elevated plus maze (EPM) and the Y maze (YM) methods (14 and 32) while the hexobarbitone induced sleep and the hole board models were used to evaluate the sedative and exploratory activities in mice respectively. The acute toxicity studies and phytochemical analysis of the extract were also carried out.

Results

The extract (100–400 mg/kg) produced a significant (P < 0.01) dose dependent increase in onset of convulsion compared to the control for strychnine- and picrotoxin-induced seizures. It also produced a significant (P < 0.01) dose dependent prolongation of the cumulative time spent in the open arms of the elevated plus maze and Y maze compared with the control. The extract (100–400 mg/kg) produced significant (P < 0.01) reduction in the time of onset of sleep induced by hexobarbitone. The prolongation of hexobarbitone sleeping time by the extract (200 mg/kg) was comparable to that produced by diazepam (3 mg/kg). At doses of 100–400 mg/kg, the extract produced a dose dependent decrease in exploratory activity of the mice. The reduction in exploratory activity produced by the extract (400 mg/kg) was greater than that of chlorpromazine (1 mg/kg). The results obtained from the experiments indicate that the extract has central nervous system depressant and anxiolytic activities. The LD₅₀ obtained for the acute toxicity studies using both oral and intraperitoneal routes of administration were 1.74 g/kg and 19.95 mg/kg respectively.

Conclusion

These findings justify the use of Securidaca longepedunculata in traditional medicine for the management of convulsion and psychosis.     

Analgesic and antimalarial activities of crude leaf extract and fractions of Acalypha wilkensiana

Aim of the study

Antiplasmodial and analgesic activities of leaf extract and fractions of Acalypha wilkensiana were evaluated to ascertain the folkloric claim of its antimalarial and analgesic activities.

Materials and methods

The crude leaf extract (220–659 mg/kg) and fractions (chloroform and aqueous; 440 mg/kg) of Acalypha wilkensiana were investigated for antiplasmodial activity against chloroquine sensitive Plasmodium berghei infections in mice and for analgesic activity against chemical and heat-induced pains. The antiplasmodial activity during early and established infections as well as prophylactic activity were investigated. Chloroquine (5 mg/kg) and pyrimethamine (1.2 mg/kg) were used as positive controls. Thin films made from tail blood of each mouse were used to assess the level of parasitaemia of the mice. Analgesic activity of the crude extract was also evaluated against acetic acid, formalin and heat-induced pains.

Results

The extract and its fractions dose-dependently reduced parasitaemia induced by chloroquine sensitive Plasmodium berghei infection in prophylactic, suppressive and curative models in mice. These reductions were statistically significant (p < 0.001). They also improved the mean survival time (MST) from 16 to 22 days relative to control (p < 0.01–0.001). The activities of extract/fractions were incomparable to that of the standard drugs used (chloroquine and pyrimethamine). On chemically and thermally induced pains, the extract inhibited acetic acid and formalin-induced inflammation as well as hot plate-induced pain in mice. These inhibitions were statistically significant (p < 0.001) and in a dose-dependent fashion.

Conclusion

The antiparasitaemic and analgesic effects may in part be mediated through the chemical constituents of the plant.     

The anti-ulcer activities of bisabolangelone from Angelica polymorpha

Aim of the study

Evaluate the anti-ulcer effects of bisabolangelone from Angelica polymorpha Maxim and provide the basic data to further study for the Angelica polymorpha and bisabolangelone.

Materials and methods

Bisabolangelone was isolated from Angelica polymorpha Maxim collected from Shennongjia Forest District of China. The structure of bisabolangelone was elucidated by NMR and MS spectrums. The anti-ulcer effects were evaluated with length of lesion (mm) and activity of H⁺/K⁺-ATPase in two models induced by ethanol and Pylorus ligation. Experimental groups were administered with different doses of bisabolangelone (3.8, 7.6 and 15.3 mg/kg). The positive control group was administered omeprazole with a dose of 3.3 mg/kg.

Results

Bisabolangelone significantly reduced the length of lesion (3.8, 7.6 and 15.3 mg/kg, P < 0.01), inhibited the activity of H⁺/K⁺-ATPase (3.8, 7.6 and 15.3 mg/kg, P < 0.01), decreased the volume of gastric juice (7.6 and 15.3 mg/kg, P < 0.05), and increased the pH value of gastric juice (7.6 and 15.3 mg/kg, P < 0.01, 3.8 mg/kg, P < 0.05).

Conclusions

Bisabolangelone is the main anti-ulcer active compound of Angelica polymorpha, and remarkably preventive and therapeutic action on gastric ulcer. It is possible that bisabolangelone inhibited the activity of the H⁺/K⁺-ATPase, then reducing the secretion of H⁺, and the anti-ulcer mechanism of bisabolangelone was deserved to be further studied.     

In vivo hepatoprotective activity of the aqueous extract of Artemisia absinthium L. against chemically and immunologically induced liver injuries in mice

Aim of the study

This study aimed to evaluate in vivo hepatoprotective activity of the aqueous extract of Artemisia absinthium L. (AEAA), which has been used for the treatment of liver disorders in Traditional Uighur Medicine.

Materials and methods

Qualitative and quantitative phytochemical analysis of the AEAA was performed by means of thin layer chromatography and spectrophometric assays. Aqueous extract (50, 100 or 200 mg/kg body weight/day) was administered orally to experimental mice. Liver injury was induced chemically, by a single CCl₄ administration (0.1% in olive oil, 10 ml/kg, i.v.), or immunologically, by injection of endotoxin (LPS, 10 μg, i.v.) in BCG-primed mice. The levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), tumor necrosis factor-α (TNF-α) and interleukin-1 (IL-1) in mouse sera, as well as superoxide dismutase (SOD), glutathione peroxidase (GPx) and malondialdehyde (MDA) in mouse liver tissues were measured. The biochemical observations were supplemented by histopathological examination.

Results

Obtained results demonstrated that the pretreatment with AEAA significantly (P < 0.001) and dose-dependently prevented chemically or immunologically induced increase in serum levels of hepatic enzymes. Furthermore, AEAA significantly (P < 0.05) reduced the lipid peroxidation in the liver tissue and restored activities of defense antioxidant enzymes SOD and GPx towards normal levels. In the BCG/LPS model, increase of the levels of important pro-inflammatory mediators TNF-α and IL-1 was significantly (P < 0.01) suppressed by AEAA pretreatment. Histopathology of the liver tissue showed that AEAA attenuated the hepatocellular necrosis and led to reduction of inflammatory cells infiltration. Phytochemical analyses revealed the presence of sesquiterpene lactones, flavonoids, phenolic acids and tannins in the AEAA.

Conclusions

The results of this study strongly indicate the protective efect of AEAA against acute liver injury which may be attributed to its antioxidative and/or immunomodulatory activity, and thereby scientifically support its traditional use.     

Beneficial effects of Anadenanthera colubrina (Vell.) Brenan extract on the inflammatory and nociceptive responses in rodent models

Ethnopharmacological relevance

Anadenanthera colubrina (Vell.) Brenan, popularly known as “angico”, is a plant that has been widely used in folk medicine due to its anti-inflammatory property. To evaluate the pharmacological activities of this plant, studies were performed on its antinociceptive and anti-inflammatory properties.

Materials and methods

The AE of Anadenanthera colubrina, made from the bark, was used in rodents via oral route (p.o.), at 100, 200, and 400 mg/kg in classical models of nociception (acetic acid-induced writhing and hot-plate test) and inflammation evoked by carrageenan (e.g., paw edema, peritonitis, and synovitis).

Results

The acetic acid-induced abdominal writhes in mice were significantly reduced (P<0.001) by oral treatment with the extract (100, 200, and 400 mg/kg), but the extract did not significantly increase the latency in the nociceptive hot-plate test. Anadenanthera colubrina aqueous extract reduced significantly the edema and, besides, diminished the mieloperoxidase activity (200 and 400 mg/kg, P<0.01). The carrageenan-induced peritonitis was significantly reduced (P<0.05) by the aqueous extract at 100, 200, and 400 mg/kg. The aqueous extract (200 mg/kg) reduces the synovial leukocyte infiltration on carrageenan-induced synovitis in rats (P<0.01), but failed to significantly affect joint swelling and impaired mobility.

Conclusions

We show for the first time that the anti-inflammatory and peripheral antinociceptive activities of Anadenanthera colubrina are consistent, at least in part, with the use of this plant in popular medicine practices.     

Orofacial antinociceptive effect and antioxidant properties of the hydroethanol extract of Hyptis fruticosa salmz ex Benth

Ethnopharmacological relevance

Hyptis fruticosa is a plant native to Brazil with antinociceptive and antiinflamatory properties. This study evaluated the antinociceptive activity of the hydroethanol extract of the plant leaves (CHEE) against orofacial pain as well as its in vitro effect against lipid peroxidation.

Materials and methods

The antinociceptive activity was investigated in mice orally treated with different doses of the CHEE (50, 100, and 200 mg/kg) and morphine (5 mg/kg) using formalin, glutamate, and capsaicin orofacial pain models using. Lipoperoxidation was induced in egg yolk by AAPH and FeSO₄ in the absence and presence of the CHEE (5, 50, 100, and 150 μg/mL).

Results

CHEE (200 mg/kg) significantly reduced (ρ<0.001) the pain response in the first (69.6%) and second (81.8%) phases of the formalin test, while the nociception caused by capsaicin was significantly (ρ<0.001) reduced by up to 62% at 200 mg/kg of extract. When glutamate was used as algogen, a significant (ρ<0.001) nociception reduction of up to 85% at 200 mg/kg extract was observed. CHEE showed a higher protection against lipoperoxidation caused by FeSO₄ (82.3% TBARS inhibition) than AAPH (35.7% TBARS inhibition) at 150 μg/mL.

Conclusion

Hyptis fruticosa leaf CHEE is of pharmacological interest because it was able to inhibit the peripheral and central transmission of orofacial pain, while reducing the spreading of the inflammatory processes by neutralizing reactive oxygen species, which are by-products in the biosynthesis of pain mediators.