Topical Anti‐inflammatory Potential of Standardized Pomegranate Rind Extract and Ellagic Acid in Contact Dermatitis

The present study evaluated the topical anti‐inflammatory potential of a standardized pomegranate rind extracts (SPRE) in parallel with its marker compound ellagic acid (EA, 13% w/w) against a mouse model of contact dermatitis. In the phenol‐induced mouse ear edema, topical application of SPRE (5, 2.5, and 1 mg/ear) and EA (0.65, 0.325, and 0.13 mg/ear, equivalent to its content in SPRE) dose‐dependently reduced the ear edema with the maximal inhibition of 79.12% and 73.63%, respectively. Triamcinolone (0.1 mg/ear) and diclofenac (1 mg/ear) as reference drugs inhibited the edema by 73.63% and 37.91%. Myeloperoxidase (MPO) activity in the mouse ear was also decreased by SPRE and EA up to 69.68% and 68.79%, respectively. Triamcinolone and diclofenac decreased the MPO activity by 76.66% and 80.14% similarly. The results indicated that topical application of SPRE and EA is promising for use in the treatment of inflammatory skin disorders. Copyright © 2013 John Wiley & Sons, Ltd.     

Assessment of anti-inflammatory and antinociceptive activities of Daphne pontica L. (Thymelaeaceae)

The n-hexane, diethylether, ethyl acetate and methanol extracts from roots, leaves, stems and flowers with young leaves of Daphne pontica L. (Thymelaeaceae) were investigated for their in vivo anti-inflammatory and antinociceptive activities. For the anti-inflammatory activity assessment, carrageenan-induced hind paw edema, PGE(2)-induced hind paw edema and 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema models and for the antinociceptive activity, p-benzoquinone-induced abdominal constriction test were used. Only ethyl acetate extracts of the roots showed significant anti-inflammatory activity on carrageenan-induced (22.7-32.0% inhibition) and PGE(2)-induced hind paw edema (3.2-27.3% inhibition) as well as 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema (47.8-43.3% inhibition) models at 50 mg/kg dose without inducing any apparent gastric lesion or acute toxicity, whereas the other extracts were shown to be ineffective. In addition to roots, ethyl acetate extracts of the stems exhibited 19.5-29.9%; 5.3-23.9%; 36.6-28.1% inhibition on carrageenan-induced and PGE(2)-induced hind paw edema as well as 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema models, respectively. On the other hand, none of the extracts showed any significant antinociceptive activity.     

Anti-venom potential of butanolic extract of Eclipta prostrata against Malayan pit viper venom

The butanolic and purified butanolic extracts (PBEs) of Eclipta prostrata were evaluated for their anti-venom potential. Inhibition of lethal, hemorrhagic, proteolytic, and phospholipase A₂ activities of Calloselasma rhodostoma (Malayan pit viper (MPV)) venom by these extracts were determined. Demethylwedelolactone was identified as their major constituent. The butanolic extract, at 2.5 mg per mouse, was able to completely neutralize the lethal activity of 2LD₅₀ of MPV venom, but increasing the dose diminished the effect. The PBE, at 1.5–4.5 mg per mouse, was able to neutralize the lethality of the venom at around 50–58%. Both extracts partially inhibited the hemorrhagic activity but displayed very low anti-phospholipase A₂ activity and did not inhibit proteolytic activity of MPV venom.     

Evaluation of anti-inflammatory activity of Cissampelos pareira root in rats

In the present study, 50% ethanolic extract of Cissampelos pareira roots (CPE) in acute, subacute and chronic models of inflammation was assessed in rats. Per os (p.o.) administration of CPE (200, 400 mg/kg) exhibited significant anti-inflammatory activity. In acute inflammation as produced by carrageenin 59.55% and 64.04%, by histamine 15.38% and 30.77%, by 5-hydroxytryptamine 17.78% and 31.11% and by prostaglandin E₂-induced hind paw edema 19.23% and 30.77% protection was observed. While in subacute anti-inflammatory models using formaldehyde-induced hind paw edema (after 1.5 h) 38.36% and 47.95% and in chronic anti-inflammatory model using cotton pellet granuloma 15.02% and 19.19% protection from inflammation was observed. CPE did not show any sign of toxicity and mortality up to a dose level of 1000 mg/kg, p.o. in rats. Both acute as well as chronic administration of CPE (100, 200 and 400 mg/kg, p.o.) did not produce any gastric lesion in rats. These data indicate that CPE possesses significant anti-inflammatory activity without ulcerogenic activity suggesting its potential as an anti-inflammatory agent for use in the treatment of various inflammatory diseases.     

Anti-inflammatory activity of hexane leaf extract of Aspilia africana C.D. Adams

The anti-inflammatory activity of hexane leaf extract of Aspilia africana C.D. Adams (Compositae) was evaluated in rodents using the xylene-induced ear edema, egg albumin- and agar-induced paw edema, formaldehyde-induced arthritis, cotton pellet granuloma, gastric ulcerogenic, acetic acid-induced vascular permeability and dextran-induced in vivo leukocyte migration tests. Results showed that the extract (5mg/ear) inhibited topical edema in the mouse ear and at 200 and 400mg/kg (i.p.), it significantly (P<0.05) suppressed the development of egg albumin- and agar-induced paw edema, and the global edematous response to arthritis induced by formaldehyde in rats. Oral administration of the extract (200 or 400mg/kg) evoked a significant (P<0.05) dose-related ulceration of the rat gastric mucosa and inhibition of vascular permeability induced by acetic acid in mice. The extract also significantly (P<0.05) reduced total leukocyte and neutrophils counts in a non-dose-related manner. However, it significantly (P<0.05) increased lymphocyte counts and stimulated the growth of granuloma tissues induced by subcutaneously implanted cotton pellets in rats. Phytochemical tests showed that the extract contained sterols and terpenoids. These findings suggest that the leaves of Aspilia africana possess anti-inflammatory activity in acute and certain aspects of chronic inflammation, which may derive from inhibition of prostaglandins synthesis, inhibition of increased vascular permeability, inhibition of neutrophil migration into inflamed tissues, and stimulation of lymphocyte accumulation, which may enhance tissue repair and healing. The terpenoids present in the leaves may account for the anti-inflammatory activity.     

In vitro and in vivo anthelmintic activity of crude extracts of Coriandrum sativum against Haemonchus contortus

In vitro anthelmintic activities of crude aqueous and hydro-alcoholic extracts of the seeds of Coriandrum sativum (Apiaceae) were investigated on the egg and adult nematode parasite Haemonchus contortus. The aqueous extract of Coriandrum sativum was also investigated for in vivo anthelmintic activity in sheep infected with Haemonchus contortus. Both extract types of Coriandrum sativum inhibited hatching of eggs completely at a concentration less than 0.5 mg/ml. ED₅₀ of aqueous extract of Coriandrum sativum was 0.12 mg/ml while that of hydro-alcoholic extract was 0.18 mg/ml. There was no statistically significant difference between aqueous and hydro-alcoholic extracts (p > 0.05). The hydro-alcoholic extract showed better in vitro activity against adult parasites than the aqueous one. For the in vivo study, 24 sheep artificially infected with Haemonchus contortus were randomly divided into four groups of six animals each. The first two groups were treated with crude aqueous extract of Coriandrum sativum at 0.45 and 0.9 g/kg dose levels, the third group with albendazole at 3.8 mg/kg and the last group was left untreated. Efficacy was tested by faecal egg count reduction (FECR) and total worm count reduction (TWCR). On day 2 post treatment, significant FECR was detected in groups treated with higher dose of Coriandrum sativum (p < 0.05) and albendazole (p < 0.001). On days 7 and 14 post treatment, significant FECR was not detected for both doses of Coriandrum sativum (p > 0.05). Significant (p < 0.05) TWCR was detected only for higher dose of Coriandrum sativum compared to the untreated group. Reduction in male worms was higher than female worms. Treatment with both doses of Coriandrum sativum did not help the animals improve or maintain their PCV while those treated with albendazole showed significant increase in PCV (p < 0.05).     

Anti-inflammatory,analgesic activity and acute toxicity of Glaucium grandiflorum extract

The species of Glaucium have been used in Iranian herbal medicine as laxative, hypnotic, antidiabetic agents and also in the treatment of dermatitis. The anti-inflammatory and analgesic effects of the aerial parts of Glaucium grandiflorum Boiss & Huet (Papaveraceae), a native plant of Iran, were studied using carrageenan induced edema, formalin and hot plate tests. The G. grandiflorum extract at the dose of 200 mg/kg had more edema inhibition than indomethacin at the doses of 10 (P<0.01) and 8 mg/kg (P<0.001) in the carrageenan test. The ED₅₀ (i.p.) in the edema induced by carrageenan was 13.59 mg/kg. In formalin test, the extract (60–90 mg/kg, i.p.) caused graded inhibition of both phases of formalin-induced pain. In hot plate test, the i.p. administration of the extract at the doses of 60, 70, 80 and 90 mg/kg significantly raised the pain threshold at a observation time of 45 min in comparison with control (P<0.001). The extract, at the antinociceptive doses, did not affect motor coordination of animals when assessed in the rotarod model. The 72 h acute LD₅₀ value of this extract after i.p. administration in mice was 797.94 mg/kg.     

Anti‐Inflammatory,Antinociceptive and Cytotoxic Effects of the Methanol Extract of Cecropia pachystachya Trécul

Cecropia pachystachya is widely used in the traditional medicine as anti‐inflammatory, antitusive, expectorant, antiasthmatic and hypoglycemic. It is also commercially available to treat skin cancer. To validate some of the popular uses of this species, its methanol leaves extract (CPM) was tested for anti‐inflammatory, antinociceptive and cytotoxic effects. The anti‐inflammatory activity was evaluated by croton oil‐induced ear edema test. When used orally, the anti‐inflammatory effect of CPM at 300 mg/kg was similar to that of indomethacin with 53% inhibition of the ear edema. Also, results on topical treatment were similar to that of dexamethasone with 83% inhibition of the edema. To evaluate the antinociceptive activity, acetic acid‐induced writhing and formalin‐induced pain tests were employed. CPM (100 and 300 mg/kg) reduced the number of writhing by 61% and 67%, respectively. In both doses, the activity was comparable to the reference drug, indomethacin. The oral administration of CPM was ineffective in the first phase of formalin test but exhibited great effects on the second phase decreasing the licking time by 85% at 300 mg/kg. The cytotoxic potential of CPM was also investigated against HL60, HL60.bcl2 and Jurkat tumor cell lines and showed an inhibition of more than 50% of cell proliferation. The flavones orientin and isoorientin were detected in CPM. Copyright © 2012 John Wiley & Sons, Ltd.     

Clematis vitalba L. aerial part exhibits potent anti-inflammatory, antinociceptive and antipyretic effects

Extracts obtained from the dried aerial parts of Clematis species are used as folk remedy worldwide for the treatment of various inflammatory ailments such as rheumatism and to reduce fever. In order to test the effectiveness of extracts, fractions and subfractions from dried Clematis vitalba L. (Ranunculaceae) aerial parts were studied on mice. Extracts are shown to have a potent effect on carrageenan-induced hind paw edema and acetic acid-induced increased vascular permeability models. Through bioassay-guided fractionation procedures a new C-glycosylflavon, 4′-O-coumaroyl-isovitexine (vitalboside) was isolated as the main active ingredient of the aerial parts. Vitalboside showed a potent and dose-dependent (in 75 and 150 mg/kg does, per os) in vivo anti-inflammatory activity against acute (carrageenan-, serotonin- and PGE₂-induced hind paw edema model, castor oil-induced diarrhea), subacute (subcutaneous air-pouch) and chronic (Freund's complete adjuvant-induced arthritis) models of inflammation. The same compound was also isolated as the main antinociceptive principle which was assessed by using the models based on the inhibition of p-benzoquinone-induced writhings, as well as antipyretic activity against Freund's complete adjuvant-induced increased body temperature. Acute and subchronic toxicity studies were also performed.     

Isolation and anticomplement activity of compounds from Dendropanax morbifera

Dendropanax morbifera Leveille (Araliaceae) is used in Korea for a variety of disease, such as migraine headache and dysmenorrheal. A new polyacetylene (1) and six known compounds (2–7) were isolated from the leaves of this plant by conventional chromatographic techniques. The structure of the new polyacetylene (1) was determined as (9Z,16S)-16-hydroxy-9,17-octadecadiene-12,14-diynoic acid by spectroscopic means including 2D NMR, which comprised the determination of a chiral by modified Mosher’s ester method. Compounds 1–7 were investigated in vitro for their anticomplement activity against the classical pathway of the complement system. Of these, compound 1 showed significant anticomplement activity with 50% inhibitory concentration (IC₅₀) value of 56.98 μM, whereas compounds 2–7 were inactive.     

Topical anti-inflammatory activity of Serjania erecta Radlk (Sapindaceae) extracts

Serjania erecta Radlk (Sapindaceae), commonly called cinco-folhas or cipó-cinco-folhas in Brazil, is thought to be effective for treating several inflammatory diseases. In order to verify the topical anti-inflammatory effect of Serjania erecta, hydroalcoholic extract and fractions were obtained by extraction in solvents of increasing polarity and were tested in mouse models using croton-oil-induced inflammation. Our findings showed that topical application of Serjania erecta hydroalcoholic extract (0.01-3.0 mg/ear), and the dichloromethane (0.03-1.0 mg/ear), ethyl acetate (0.03-1.0 mg/ear), and hexane (0.003-1.0 mg/ear) fractions revealed significant activity, causing a dose-dependent reduction of croton-oil ear edema (ID(50)=0.14 mg/ear, 0.23 mg/ear, 0.14 mg/ear, 0.04 mg/ear, respectively). The extract and all tested fractions also decreased tissue myeloperoxidase activity (indicative of polymorphonuclear leukocytes influx) in mouse-ears treated with croton oil with a maximum inhibition of 72% at 3.0 mg/ear for the hydroalcoholic extract and 81%, 78%, and 83% at 1.0mg/ear for dichloromethane, ethyl acetate and hexane fractions, respectively. As expected, dexamethasone (0.05 mg/ear) was effective in inhibiting both edema and myeloperoxidase activity (99% and 82%, respectively). In conclusion, our results indicate a topical anti-inflammatory effect for the species of Serjania studied.     

Inhibition of the pro-inflammatory mediators' production and anti-inflammatory effect of the iridoid scrovalentinoside

We have studied scrovalentinoside, an iridoid with anti-inflammatory properties isolated from Scrophularia auriculata ssp. pseudoauriculata, as an anti-inflammatory agent in different experimental models of delayed-type hypersensitivity. We found that scrovalentinoside reduced the edema induced by oxazolone at 0.5 mg/ear and sheep red blood cells at 10 mg/kg. The observed effect occurred during the last phase or inflammatory response; during the earlier phase or induction of the delayed-type hypersensitivity reaction, no significant activity was noted. Thus, scrovalentinoside reduced both the edema and cell infiltration in vivo and reduced lymphocyte proliferation in vitro, affecting the cycle principally during the first 48 h. Whereas cells stimulated with phytohemagglutinin changed from the G₀/G₁ phase to the S and G₂/M phases, when these same cells were treated with scrovalentinoside (100 μM), they remained in the G₀/G₁ phase. Finally, scrovalentinoside inhibited the production of the pro-inflammatory mediators’ TNF-, IFN-γ, IL-1β, IL-2, IL-4, LTB₄, and NO, but had no effect on the production of the anti-inflammatory cytokine IL-10.     

Studies on the anti-inflammatory and analgesic properties of Tithonia diversifolia leaf extract

A methanol extract of the dried leaves of Tithonia diversifolia was investigated for anti-inflammatory and analgesic activities. The extract (50–200 mg/kg, p.o.) produced dose-related inhibition of carrageenan-induced paw oedema and cotton pellet-induced granuloma in rats. At the same doses, analgesic effect was also observed with hot plate latency assays maintained at (55 °C) as well as on the early and late phases of formalin-induced paw licking in rats. The results of the present study further confirm the use of Tithonia diversifolia traditionally for the treatment of painful inflammatory conditions.     

Toxicological study on Glinus lotoides: a traditionally used taenicidal herb in Ethiopia

Extracts of five medicinal plants: Boscia angustifolia, Cissus quadrangularis, Securidaca longipedunculata, Stylosanthes erecta and Trichilia emetica, used traditionally in Malian traditional medicine were screened for in vitro antiplasmodial activity and GABA_A–benzodiazepine receptor binding activity. Four extracts showed significant antiplasmodial activities, with the dichloromethane extract of leaf of Securidaca longipedunculata being the most active (IC₅₀ of 7 μg/ml [95% CI: 5–9]). The dichloromethane extract of leaf of Trichilia emetica, in addition to its antiplasmodial activity (IC₅₀: 12 μg/ml [95% CI: 12–14]), exhibited a good binding activity to the GABA_A–benzodiazepine receptor, while water and methanol extracts of the same plant did not show any activity. A strong GABA_A-receptor complex binding activity was observed in the methanol extract of aerial part of Stylosanthes erecta. The results in this study justify some of the traditional indications of the plants investigated and may thus be candidates for Improved Traditional Medicines in Mali.     

Inhibition of chemically induced inflammation and pain by orally and topically administered leaf extract of Manihot esculenta Crantz in rodents

The aqueous leaf extract of Manihot esculenta Crantz (MELE) is being used orally and topically in traditional African medicine for the treatment of inflammation and pain, and claimed to be safe. The anti-inflammatory effects of MELE (100-400mg/kg, p.o. or 1-4%, w/w in petroleum jelly, topically) were tested against carrageenan-induced paw oedema in rats as well as against xylene-induced ear oedema in mice. The analgesic effect of MELE (100-400mg/kg, p.o. or 1-4%, w/w in petroleum jelly, topically) was tested against acetic acid-induced (20mul, 0.6%, v/v in normal saline, i.p.) and acetylcholine-induced (8.3mg/kg, i.p.) mouse writhing models. At 100-400mg/kg, p.o. and 1-4% (w/w), topically, MELE produced significant inhibitions of carrageenan-induced rat paw oedema and xylene-induced ear swelling in mice. Effects produced by MELE were significantly higher than those produced by indomethacin (10mg/kg, s.c. or 1%, w/w in petroleum jelly) in the anti-inflammatory models. For the analgesic effect, MELE (100-400mg/kg, orally) and (1-4%, w/w, topically), like aspirin (100mg/kg, i.p.) exhibited significant (P<0.05) inhibition of acetic acid- and acetylcholine-induced mouse writhing tests, compared to untreated control. Effects produced by MELE were significantly lower than those produced by aspirin (100mg/kg, i.p.) in the analgesic models, except for the topically administered extract on acetylcholine-induced pain. Acute oral administration up to 10g/kg did not cause death within 14 days, but mortalities were produced in i.p. administered extract with LD(50) of 2.5+/-0.3g/kg. Based on these, the extract may contain orally safe, topically and orally effective anti-inflammatory and analgesic principles, which justify its use in traditional African medicine.     

Cytotoxicity of plants from Malaysia and Thailand used traditionally to treat cancer

The SRB cytotoxicity assay was used to screen extracts and isolated constituents of some traditional medicinal plants from Malaysia and Thailand against two human cancer cell lines, COR L23 lung cancer cell line and MCF7 breast cancer cell line and the non-cancer MCF5 cell line. Five out of the seven species tested, i.e. Thai Alpinia galanga, Alpinia officinarum, Cayratia japonica, Physalis minima, Tabernaemontana divaricata, exhibited interesting cytotoxicity activity and this is the first report of cytotoxicity from any Cayratia species. Following bioassay-guided fractionation, 1′-acetoxychavicol acetate (48 h exposure against COR L23 cells, IC₅₀ 7.8 μM against MCF7 cells, IC₅₀ 23.9 μM) was isolated as the major cytotoxic component of the Alpinia species, physalin F as the major cytotoxic component of Physalis minima (48 h exposure against COR L23 cells IC₅₀ 0.4 μM against MCF7 cells, IC₅₀ 0.59 μM). The Malaysian Alpinia galanga showed weak activity compared with the Thai sample and this was shown to be due to the relatively high amounts of 1′-acetoxychavicol acetate present in the Thai sample.     

Analgesic and anti-inflammatory effects of the dry matter of culture broth of Termitomyces albuminosus and its extracts

Aim of the study

The objectives of this study were to investigate the analgesic and anti-inflammatory effects of the dry matter of culture broth (DMCB) of Termitomyces albuminosus in submerged culture and its crude saponin extract (CSE) and crude polysaccharide extract (CPE).

Materials and methods

The analgesic effects of DMCB, CSE and CPE were evaluated with models of acetic acid-induced writhing response and formalin test in mouse. The anti-inflammatory effects of DMCB, CSE and CPE were evaluated by using models of xylene-induced mouse ear swelling and carrageen-induced mouse paw edema.

Results

The DMCB, CSE and CPE significantly decreased the acetic acid-induced writhing response and the licking time on the late phase in the formalin test. Treatment of DMCB (1000 mg/kg), CSE (200 mg/kg) or CPE (200 mg/kg) inhibited the mouse ear swelling by 61.8%, 79.0% and 81.6%, respectively. In the carrageen-induced mouse paw edema test, the group treated with indomethacin showed the strongest inhibition of edema formation by 77.8% in the third hour after carrageenan administration, while DMCB (1000 mg/kg), CSE (200 mg/kg) and CPE (200 mg/kg) showed 48.4%, 55.6% and 40.5%, respectively.

Conclusions

The results suggested that DMCB of Termitomyces albuminosus possessed the analgesic and anti-inflammatory activities. Saponins and polysaccharides were proposed to be the major active constituents of Termitomyces albuminosus in submerged culture.     

Antitrypanosomal and antiplasmodial activity of medicinal plants from Côte d'Ivoire

The antitrypanosomal activity of 101 crude ethanol extracts derived from 88 medicinal plants from Côte d’Ivoire was determined in vitro using Trypanosoma brucei rhodesiense. Of those extracts 8 showed good activity (IC₅₀ values ≤8 μg/ml), 37 revealed a weak activity (IC₅₀ values between 25 and 8.1 μg/ml) and 56 did not show any activity at all (IC₅₀ values>25 μg/ml). The extracts of Enantia polycarpa (Annonaceae) and Trichilia emetica (Meliaceae) were the most promising ones. Their IC₅₀ values were 0.5 and 0.04 μg/ml, respectively, and the selectivity index 616 and 209, respectively. This is the first report of in vitro antitrypanosomal activity of these two plants. Their high activities render them candidates for the isolation of compounds which could develop into new lead structures for drug development programs against African trypanosomiasis. Seven of the tested extracts exhibited an antiplasmodial activity against K1 strain of Plasmodium falciparum with IC₅₀ values below 4 μg/ml. The highest activity was found for Enantia polycarpa stem bark with an IC₅₀ value of 0.126 μg/ml.     

Antiinflammatory activity of Synurus deltoides

Synurus deltoides Aiton, Nakai, is an edible plant that has been used as a folk medicine for treating inflammatory disorders. This investigation was carried out to establish the antiinflammatory activity of this plant material using a 75% ethanol extract from the aerial part of S. deltoides. Against the acute inflammatory animal model of mouse croton oil-induced ear oedema assay, the extract did not show significant inhibition at 100-800 mg/kg by oral administration. On the other hand, the extract showed considerable inhibition against the chronic inflammatory animal model of rat adjuvant-induced arthritis (25% inhibition at 100 mg/kg/day) while prednisolone exerted 40% inhibition at 10 mg/kg/day. In addition, S. deltoides possessed strong analgesic activity (IC50 = 50 mg/kg) in the acetic acid-induced writhing test. From the extract, ursolic acid and scopoletin were successfully isolated and their contents were found to be 0.31% and 0.37% (w/w), respectively, based on the dried extract by HPLC analysis. All the results obtained indicate that this plant material may be used beneficially as an antiinflammatory agent having analgesic action.     

Investigation of anti-inflammatory and antinociceptive activities of Lantana trifolia

The anti-inflammatory activity of Lantana trifolia (Verbenaceae) was determined by carrageenan, serotonin and histamine-induced rat paw edema and the analgesic activity of this plant was studied by acetic acid-induced writhings and tail flick tests in mice. Lantana trifolia extracts (at 30 mg/kg) inhibited carrageenan and histamine-induced rat paw edema. Although the extracts did not produce any effect on acetic acid-induced writhings, they all develop a significant increase on tail flick antinociceptive index (doses varying between 1 and 30 mg/kg), indicating a spinal antinociceptive effect. These results provide support for the use of Lantana trifolia in relieving inflammatory pain.