Genotoxicity testing of Cecropia obtusifolia extracts in two in vivo assays: the wing somatic mutation and recombination test of Drosophila and the human cytokinesis-block micronucleus test

Cecropia obtusifolia Bertol. (Cecropiaceae) is a tree that grows in secondary vegetation in the tropical rain forest along both coasts of Mexico. Its leaves are used in folk medicine for the treatment of diabetes mellitus type 2. The aim of the present studies was the evaluation of possible genotoxic effects of the aqueous extract from the leaves of Cecropia obtusifolia by means of two different experimental assay models: the wing somatic mutation and recombination test in flies and the micronucleus test from lymphocytes obtained from patients treated with the extract. No toxicity was found to be induced by the leaves of Cecropia obtusifolia. The Drosophila wing somatic mutation and recombination test (SMART) was applied in the standard version with basal biotransformation activity as well as in a variant version with increased cytochrome P450-dependent bioactivation capacity. The ranges of exposure concentrations for these genotoxicity experiments were between 0.82 and 13.32 mg/ml. The extract did not produce any genotoxic effect; however it showed a non significant antigenotoxic effect. The human micronucleus assay in vivo was performed with cultured lymphocytes obtained from six diagnosed type 2 diabetic patients treated daily with 13.5 g of the aqueous extract between 32 and 85 days. No statistically significant increases in cytotoxicity and/or genotoxicity between control and diabetic blood samples were observed.     

狭叶荨麻根、茎、叶的抗炎镇痛作用

目的研究狭叶荨麻Urticaangustifolia根、茎、叶70%乙醇提取物及狭叶荨麻根水提取物的抗炎、镇痛作用。方法二甲苯致小鼠耳廓肿胀实验;冰醋酸致小鼠扭体反应实验。结果狭叶荨麻根、茎、叶70%乙醇提取物及狭叶荨麻根水提取物能明显对抗二甲苯致小鼠耳廓肿胀,并显著抑制0.5%醋酸致小鼠扭体反应。结论狭叶荨麻根、茎、叶70%乙醇提取物及狭叶荨麻根水提取物具有显著的抗炎、镇痛活性。     

Analgesic and anti-inflammatory activity of the ethanolic extract from Spiranthera odoratissima A. St. Hillaire (Manacá) roots

Acetic acid-induced abdominal writhing, the tail flick test and carrageenan-induced peritonitis were used to study the analgesic and anti-inflammatory activity of the crude ethanolic extract from Spiranthera odoratissima roots. Pentobarbital-induced sleeping time was used to study the central depressant effect of the extract. The ethanolic extract caused a dose dependent inhibition of acetic acid-induced abdominal writhing and leukocyte migration, and produced a significant, dose-related increase in the duration of sleep. The results suggest that Spiranthera odoratissima roots contain compounds with anti-inflammatory and central depressant actions.     

Anti-inflammatory and analgesic activities of mature fresh leaves of Vitex negundo

This study confirmed the oral anti-inflammatory, analgesic and antihistamine properties of mature fresh leaves (MFL) of Vitex negundo L. (Verbenaceae) claimed in the Ayurveda medicine by orally treating a water extract of the leaves to rats. The early phase (2h) of carrageenan-induced rat paw oedema was significantly (P<0.01) suppressed in an inversely does-dependent (r(2)=1, P<0.01) manner by MFL. The EC(50) was 2g/kg of MFL. In the formaldehyde-induced rat paw oedema test, the 2.5 and 5g/kg leaves significantly (P<0.05) suppressed the inflammation on days 4-6 of the test. In the hot plate test, 2.5 and 5g/kg of MFL showed a significant (P<0.05) and directly dose-dependent analgesic activity at 1h of treatment while the activity was absent in the tail flick test in rats. The EC(50) for the analgesic activity was 4.1g/kg. In the formalin test, 1.25, 2.5 and 5g/kg of MFL significantly (P<0.05) suppressed the pain in both the phases of the test like aspirin. The leaves showed an inversely dose-dependent in vivo antihistamine and in vitro prostaglandin (PG) synthesis inhibition, membrane stabilising and antioxidant activities. Naloxone did not abolish the analgesic activity in the hot plate test. A 5g/kg of MFL did not impair muscle strength and co-ordination and did not induce sedation. The treatment of 5g/kg of MFL did not show signs of acute toxicity or stress. Fourteen-day oral treatment of 5g/kg of MFL significantly increased the serum activity of AST. Flowering of the tree did not abolish the analgesic and anti-inflammatory activities of the leaves. These observations revealed that the fresh leaves of Vitex negundo have anti-inflammatory and pain suppressing activities possibly mediated via PG synthesis inhibition, antihistamine, membrane stabilising and antioxidant activities. The antihistamine activity can produce the anti-itching effect claimed in Ayurveda medicine.     

Studies on Ruta chalepensis, an ancient medicinal herb still used in traditional medicine

An ethanolic extract of the aerial parts of Ruta chalepensis was studied for its anti-inflammatory, antipyretic, analgesic and CNS depressant activities. The extract produced a significant inhibition of carrageenan-induced paw oedema and cotton pellet granuloma in rats. The studies on spontaneous motor activity in mice and conditioned avoidance responding (CAR) in rats showed a dose-dependent depression of the central nervous system in treated animals. Reduction of yeast-induced hyperthermia in mice confirmed its reputed antipyretic activity. The extract did not produce any significant changes in prothrombin time and fibrinogen level. It also failed to produce any analgesic activity in the hot plate reaction-time test in mice. Phytochemical screening of the aerial parts of the plant showed the presence of alkaloids, flavonoids, coumarins, tannins, volatile oil, sterols and/or triterpenes.     

Analgesic and anti-inflammatory properties of Nelsonia canescens leaf extract

An ethanolic extract of the dried leaves of Nelsonia canescens was investigated for anti-inflammatory and analgesic activities in rat. In the test for anti-inflammatory activity, the extract at the doses of 50-200 mg/kg significantly (P<0.05) inhibited carrageenan-induced paw oedema and cotton pellet granuloma. Likewise, at the same doses the extract exhibited analgesic activity in both the hot plate latency assay (hot plate maintained at 55 degrees C) and on the early and late phases of formalin-induced paw licking in rats. The result of the present study confirm that Nelsonia canescens has analgesic and anti-inflammatory activities. These findings also justify the traditional use of the plant for treating pain.     

Evaluation of Antinociceptive Activity of Methanol Extract from Cleome rutidosperma in Mice

Objective Cleome rutidosperma (Capparidaceae), commonly known as “Fringed Spider Flower”, is a medicinal plant found in Southeast Asia. C. rutidosperma is used in folk medicine for diuretic, laxative, analgesic, anti-inflammatory, antipyretic, antimicrobial, anti-oxidant, hypoglycemic, and anthelmintic activities. We have evaluated the anti-nociceptive properties of methanol extract from C. rutidosperma (MECR) in vivo. Methods Thermal method (hot plate test and tail flick test) was induced to judge the anti-inflammatory effect and couple of chemical method also used (formalin induced licking test; writhing test carried by acetic acid) to evaluate analgesic effect. Both of these tests were made over animal models, like mice and rats. Two different doses (100 and 200 mg/kg) were used for each case of test, while morphine sulphate (5mg/kg, ip) was used as reference drug. Results MECR demonstrated the significantly anti-nociceptive activity in the analgesic and anti-inflammatory tests by reducing nociception in mice models (P < 0.001). In the hot-plate and tail-flick tests, MECR significantly elongated the time to response to the thermal stimuli (100 and 200 mg/kg with P < 0.05, 0.001). The remarkable increase in the latency was observed at 90 and 120 min. In acetic acid-induced writhing test and formalin induced licking test for anti-inflammatory activity, MECR at 100 and 200 mg/kg doses exhibited significant (P < 0.001) reduction of writhing and licking response. Conclusion The anti-inflammatory and analgesic effects of C. rutidosperma propose that this effect may be a result of both peripheral and central mechanisms. Further study is required to ensure the proper mechanism of action as well as the active ingredient.     

Anti-inflammatory and analgesic activities of ethanolic extract and two limonoids from Melia toosendan fruit

AIM OF STUDY: The fruit of Melia toosendan Sieb. et Zucc. (MTF) is a traditional Chinese herbal medicine in the treatment of stomachache and many acute or chronic inflammations, as well as ascariasis. This paper aimed to investigate the anti-inflammatory and analgesic activities of the MTF extract and two main limonoid-type triterpenoids isolated from MTF. MATERIALS AND METHODS: The ethanolic extract of MTF and two limonoids, isotoosendanin (1) and 1-O-tigloyl-1-O-debenzoylohchinal (2) were evaluated for their anti-inflammatory and analgesic activities. Acetic acid-induced vascular permeability and lambda-carrageenan-induced hind paw edema tests in mice were used to investigate anti-inflammatory activity; and acetic acid-induced writhing and hot-plate tests in mice were used to determine analgesic effect. RESULTS: Both the ethanolic extract and two limonoids displayed significant anti-inflammatory effects. Although the ethanolic extract showed remarkable analgesic effects in both writhing and hot-plate tests, the two limonoids had analgesic effects just in writhing test. CONCLUSION: The results suggested that the ethanolic extract of MTF had obvious anti-inflammatory and analgesic activities, and the two limonoids were the active constituents contributing to the anti-inflammatory and analgesic effects of MTF.     

Pharmacological properties of the methanol extract from Mentha suaveolens Ehrh

The present study analyses the pharmacological activity in in vivo and in vitro models of the methanol extract obtained from the leaves and steams of Menta suaveolens Ehrh. This extract lacked toxicity, but exhibited a central nervous system depressant action; an analgesic effect in models of chemical and mechanical stimulation suggesting the induction of a peripheral analgesic response. The extract also exhibited an antiinflammatory action inhibiting the rat paw oedema induced by carrageenin. Moreover, the in vitro studies showed a significant diminution in the contractile effects induced by histamine, serotonin and acetylcholine.     

Hypoglycemic effect and chlorogenic acid content in two Cecropia species

The hypoglycemic effect of methanol leaf extracts from Cecropia obtusifolia and C. peltata was evaluated in healthy mice. A significant decrease (p < 0.05) in plasma glucose levels was recorded 2 and 4 h after a single oral administration of methanol extracts (1 g/kg). This effect was correlated with the chlorogenic acid contents in both species; C. peltata, containing 19.84 +/- 1.64 mg of chlorogenic acid/g of dried leaves produced the highest decrease (D(alpha 2,60) = 20.18, p < 0.05) of plasma glucose levels (52.8%). The extracts of C. obtusifolia from Tabasco and Veracruz, showed similar hypoglycemic effects (33.3% and 35.7%, respectively) and chlorogenic acid contents (Tukey(0.05) = 1.8859) (13.3 +/- 3.2 mg/g and 13.1 +/- 1.6 mg/g, respectively). The hypoglycemic effect produced by different doses (0.1, 0.25, 0.50, 0.75 and 1 g/kg body wt, p.o.) of C. peltata showed a lineal relationship with chlorogenic acid content, reaching an ED(50) = 0.540 g/kg body wt for extract, and an ED(50) = 10.8 mg/kg body wt for chlorogenic acid. These results suggest that C. peltata is a better hypoglycemic agent than C. obtusifolia, and it could be considered for developing a phytomedicinal product to carry out clinical trials.     

Evaluation of the analgesic and topical anti-inflammatory effects of Hypericum reflexum L. fil

The present study investigates the analgesic and topical anti-inflammatory effects of the infusion, methanol extract and fractions of the aerial part in blossom of Hypericum reflexum L. fil. in mice. The acetic acid-induced writhing test, formalin test, tail flick test and the tetradecanoylphorbol acetate (TPA)-induced ear inflammation model in mice were used to determine these effects. Our findings show that oral administration of all extracts tested from this species significantly inhibit acetic acid-induced writhing in mice. Only the methanol extract and chloroform fraction were significantly active in both phases of formalin-induced pain and in the tail flick assays, suggesting that they may have central analgesic properties. On the other hand, the topical treatment of methanol extract, butanol and chloroform fractions of this species significantly reduced the TPA-induced ear oedema. In conclusion, the results indicate analgesic and topical anti-inflammatory activities in mice for the Hypericum species studied.     

牛白藤抗炎镇痛作用有效部位的筛选

目的比较研究牛白藤的不同溶剂提取物的抗炎镇痛作用,为牛白藤的临床应用以及筛选分离活性成分提供实验依据。方法采用二甲苯致小鼠耳廓肿胀和醋酸致小鼠毛细血管通透模型评价药物的抗炎作用,采用小鼠热刺激致痛和醋酸扭体模型评价镇痛作用,比较牛白藤水提物、醇提物及不同溶剂萃取物的抗炎镇痛作用。结果牛白藤水提物、醇提物均具有抗炎镇痛作用,同剂量之间比较以醇提物活性较强;牛白藤石油醚、乙酸乙酯萃取物能明显减轻二甲苯诱导的小鼠耳肿胀程度,抑制热刺激和醋酸引起的小鼠疼痛反应。结论牛白藤具有明显的抗炎镇痛活性,石油醚萃取物和乙酸乙酯萃取物可能是其主要有效部位。     

Antinociceptive and anti-inflammatory activities of Acacia pennata wild (Mimosaceae)

The butanolic fraction of dried leaves of Acacia pennata (Mimosaceae) was tested for analgesic and anti-inflammatory activities in animal models. It showed significant protective effects against chemical stimuli (acetic acid and formalin) in the mouse. It also produced a significant increase of the threshold of sensitivity to pressure-induced pain in the rats. The extract revealed an inhibitory effect in carrageenin-induced rat paw oedema in the late phase. The results suggested that a peripheral mechanism is involved in the analgesic, associated to anti-inflammatory effect (NSAIDs-like). Among the class of compounds characterized in this fraction, flavonoids may be mainly responsible for the pharmacological activities.     

Anti-inflammatory and anti-nociceptive activities of Platanus orientalis Linn. and its ulcerogenic risk evaluation

Ethnopharmacological relevance

Leaves of Platanus orientalis Linn. are used in folk medicine as a wound-healer and ophthalmologic agent. Phytol derivatives from the leaves of plane-tree show anti-ulcer activity. Its analgesic and anti-inflammatory effects for knee pain were known to Persian scientists and hakims.

Materials and methods

The ethanolic extract of Platanus orientalis Linn. and its various fractions were given at a dose of 100 mg/kg po and 200 mg/kg po for testing their anti-inflammatory activity by carrageenan induced hind paw edema. The analgesic activity of the ethanolic extract and its fractions has been carried out by tail-flick method and writhing test at a dosage of 200 mg/kg po. Gastric ulceration studies have been further carried out to study the ulcerogenic risk evaluation of the ethanolic extract and its various fractions at a dose of 600 mg/kg body weight.

Results

Among the tested fractions, chloroform fraction exhibited better inhibition (68.33%) at 200 mg/kg po dosage when compared to the standard drug Ibuprofen (66.66%) after 3 h in the carrageenan induced hind paw edema. The ethanolic extract and all its fractions especially the chloroform (p<0.01) showed significant analgesic activity with insignificant ulceration as compared to the standard drug i.e. Ibuprofen. The histopathological study of ethanolic extract and its fractions revealed that none of them cause ulcer.

Conclusion

The present study indicates that Platanus orientalis Linn. has significant anti-inflammatory and analgesic effect.     

Anti-inflammatory and anti-nociceptive activities of Smilax china L. aqueous extract

The aqueous extract of the tuber of Smilax china L., popularly known in China as "jin gang ten", was tested for its anti-inflammatory activities in rats by egg-albumin-induced edema and anti-nociceptive effects in mice using hot-plate test and acetic acid-induced abdominal constriction test, respectively. The aqueous extract in the dose of 1000 mg/kg (i.g.) had a significant anti-nociceptive and anti-inflammatory effect compared to physiological saline. The anti-inflammatory effects are similar to acetylsalicylic acid (200 mg/kg, i.g.). We also evaluated the aqueous extract for the inhibition of prostaglandin production (for COX-2 inhibitions) in lipopolysaccharide (LPS)-induced mouse macrophage cells. The result showed that both COX-2 activity and COX expression were inhibited by the extract. These active extracts suppressing activities warranted further studies of active principles and development of new anti-inflammatory and analgesic agents. Studies to determine correlation between chemical composition and pharmacological activity are underway.     

Anti-inflammatory effects of crude methanolic extract and fractions of Alchornea cordifolia leaves

The leaves of Alchornea cordifolia were collected, identified, dried, and reduced to coarse powder and extracted with aqueous methanol. Using various solvent treatments, the powdered dried leaf was fractionated into five fractions, A1, A2, B, C, D and E. The fractions were subjected to phytochemical analysis to identify the biologically active constituents. The anti-inflammatory effects of crude methanolic extract (ME) of Alchornea cordifolia leaves and the five fractions were evaluated using egg-albumen-induced rat hind paw oedema as a model of inflammation. The crude extract was also subjected to acute toxicity test. Fraction A2, which exhibited the most promising anti-inflammatory effect, was also subjected to analgesic and ulcerogenic tests. Phytochemical analysis of the extracts showed the presence of terpenes, sterols, flavonoids, tannins, carbohydrates, glycosides, saponins and traces of alkaloids. The LD(50) of the aqueous ME was found to be 1131.4 mg/kg. The crude ME (50 mg/kg) gave anti-inflammatory activity which was significant (P<0.05) at all the observation times (1-3h). The different solvent fractions exhibited varying degrees of anti-inflammatory activities, with terpenoid fraction (A2) and the tannin-containing multi-component fraction (D) showing very high and significant (P<0.01) activity at 100mg/kg, with percentage inhibition of oedema value of 87.69 each. In conclusion, the aqueous ME of Alchornea cordifolia leaves could be beneficial in the management of different inflammatory disease states. Its anti-inflammatory activity may not be attributed only to the terpenoid content.     

The analgesic and anti-inflammatory effects of Portulaca oleracea L. subsp. Sativa (Haw.) Celak

Many ethnic groups have used different species of Portulaca oleracea L., a member of the Family Portulacaceae, as vegetable and also herbal medicine against several diseases for many centuries. A review of the records in both folkloric and scientific literature indicates that Portulaca has many medicinal uses. After our previous preliminary screening of three species of the family for analgesic and anti-inflammatory properties, Portulaca oleracea L. subsp. sativa (Haw.) Celak. (a cultivar) was chosen for further work due to its abundant availability from reliable sources. The 10% ethanolic extract of the aerial parts (dried leaves and stem) showed significant anti-inflammatory and analgesic after intraperitoneal and topical but not oral administration when compared with the synthetic drug, diclofenac sodium as the active control. Results indicate this cultivar species of Portulaca also possesses some of the claimed traditional uses of the wild species in the relief of pain and inflammation.     

Anti-inflammatory and antipyretic effects of Trigonella foenum-graecum leaves extract in the rat

Anti-inflammatory and antipyretic effects of the Trigonella foenum-graecum (TFG) leaves extract, an Iranian medicinal plant, were examined. For anti-inflammatory activity, the formalin-induced edema model was used. Hyperthermia was induced by intraperitoneal injection of 20% (w/v) aqueous suspension of brewer's yeast. Sodium salicylate (SS) was used as a positive control. Both TFG and SS significantly reduced formalin-induced edema in single dose (TFG 1000 and 2000 mg/kg, SS 300 mg/kg) and chronic administration (TFG 1000 mg/kg and SS 300 mg/kg). TFG and SS also significantly reduced hyperthermia induced by brewer's yeast in 1 and 2 h after their administration. The results indicate that the TFG leaves extract possess anti-inflammatory as well as antipyretic properties in both i.p. and p.o. administration. Phytochemical studies indicate that alkaloids, cardiac glycosides, and phenols are the major component in the extract. Although existence of three anti-inflammatory, analgesic and antipyretic effects in this extract suggest a NSAID-like mechanism for it, but the presence of alkaloids, the absence of other effective compounds such as flavonoids, saponins, steroids, etc., and also its analgesic effect on tail-flick test that usually is not produced by NSAIDs, suggest another mechanism for the extract. So the possibility of alkaloids as effective compounds, in this extract, increases.     

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.     

Antinociceptive and anti-inflammatory effects of Elaeagnus angustifolia fruit extract

In this study, probable antinociceptive and anti-inflammatory effects of Elaeagnus angustifolia fruit components, were evaluated. For evaluation of antinociceptive effects, the chronic (formalin test) and acute (tail-flick) pain models of rats were used. For the anti-inflammatory effects, the paw inflammation model was used through subcutaneous injection of 5% formalin to the paw of male rats. Water extracts of the fruit and its components in the single dose were assessed through comparison with the antinociceptive and anti-inflammatory effects of sodium salicylate (SS) as a positive control. Administration of 300 mg/kg of SS (i.p.) had no effect on tail flick latency, while 1000 mg/kg of total (i.p. and p.o.) and endocarp (i.p.) extract, increased this latency (P<0.01, P<0.001, respectively), which was not reversed by naloxone (2 mg/kg). In the formalin test, SS (300 mg/kg, i.p.) and the extract (1000 mg/kg, p.o. ) alleviated the animals nociception in the second phase, while in the first phase they were not effective. The total and endocarp extracts (1000 mg/kg, i.p.) showed a significant effect on both phases (P<0.01, P<0.001, respectively) which was also not reversed by naloxone (2 mg/kg, i.p.). In the acute anti-inflammatory test, the total extract and the aqueous extract of individual fruit components showed a significant effect (P<0.001). This anti-inflammatory effect was not significant compared with the anti-inflammatory effect of SS. Because of the extract effect on the tail-flick latency and both phases of the formalin test, the site of its analgesic action is probably central, and the mechanism of antinociceptive action of the extract are not related to the opioid system. Our phytochemical studies indicated that aqueous extract of E. angustifolia fruit contains flavonoids, terpenoids and cardiac glycosides.