Anti-inflammatory and antinociceptive activity of Thymus pubescens extract

Thymus pubescens is an aromatic and medicinal plant, which has been widely distributed in Iran. The anti-inflammatory and analgesic effects of the T. pubescens aerial parts methanol extract were studied at doses of 50-400 mg/kg i.p. using carrageenan-induced edema, formalin, hot plate and writhing tests. The extract produced a significant decrease in the degree of swelling, 3 h after carrageenan injection and caused graded inhibition of both phases of formalin-induced pain. Moreover, in the hot plate test, it significantly raised the pain threshold. While in the writhing test produced a significant decrease in the number of writhing in comparison with the control group (P<0.001). The results of pharmacological tests performed in the present study suggest that the extract of T. pubescens presents analgesic and anti-inflammatory effects.     

Evaluation of analgesic effect of Datura fastuosa leaves and seed extracts

The aqueous extracts of Datura fastuosa leaves and seeds were evaluated for the analgesic effect on acetic acid-induced writhing and hot plate reaction in mice. According to the results, D. fastuosa leaves and seeds extracts at oral doses of 400 and 800 mg/kg are effective as analgesic. The analgesic activity of leaf extract is reduced by naloxone but not that of seed extract.     

Analgesic properties of Capraria biflora leaves aqueous extract

The analgesic properties of dried leaves of Capraria biflora were investigated. The aqueous extract (50-200 mg kg(-1)) produced moderate inhibition of acetic acid-induced writhing in mice. At the same doses, a better analgesic effect was observed on the hot plate test.     

Analgesic activity of Calotropis gigantea flower

The alcoholic extract of the flowers of Calotropis gigantea was administered orally and explored for its analgesic activity in chemical and thermal models in mice. In acetic acid induced writhing test, an inhibition of 20.97% and 43.0% in the number of writhes was observed at the doses of 250 and 500 mg/kg, respectively. In the hot plate method the paw licking time was delayed. The analgesic effect was observed after 30 min of dose administration which reached its maximum after 90 min.     

Chemical composition and pharmacological activity of essential oil of Canarium schweinfurthii

The essential oil obtained by hydrodistillation of the resin of Canarium schweinfurthii growing in Central African Republic, was analysed by GC and GC/MS and its analgesic and antiinflammatory effects were studied. The major constituents of the essential oil were octylacetate (60%) and nerolidol (14%). At the doses of 1, 2 and 3 ml/kg i.p. essential oil shows a significant analgesic effect using acetic acid-induced writhing and hot plate methods. However, its was unable to reduce inflammatory process in cotton pellet induced granuloma method.     

Preliminary analysis of the antinociceptive activity of zerumbone

We have investigated the antinociceptive activity of zerumbone (1), a natural cyclic sesquiterpene isolated from Zingiber zerumbet Smith, in acetic acid-induced abdominal writhing test and hot plate test in mice. 1 given by intraperitoneal route produced significant dose-dependent antinociceptive effect in all the test models used. In addition, the antinociceptive effect of 1 in the hot plate test was reversed by the non-selective opioid receptor antagonist naloxone, suggesting that the opioid system is involved in its analgesic mechanism of action.     

Study of anti-inflammatory,analgesic and antipyretic activities of seeds of Hyoscyamus niger and isolation of a new coumarinolignan

A chemical and biological validation of the traditional use of Hyoscyamus niger seeds as anti-inflammatory drug has been established. The methanolic extract of seeds of H. niger (MHN) was evaluated for its analgesic, anti-inflammatory and antipyretic activities in experimental animal models at different doses. MHN produced significant increase in hot plate reaction time, while decreasing writhing response in a dose-dependent manner indicating its analgesic activity. It was also effective in both acute and chronic inflammation evaluated through carrageenin-induced paw oedema and cotton pellet granuloma methods. In addition to its analgesic and anti-inflammatory activity, it also exhibited antipyretic activity in yeast-induced pyrexia model. Furthermore, the bioactive MHN under chemical investigation showed the presence of coumarinolignans as major chemical constituent and yielded a new coumarinolignan, cleomiscosin A methyl ether (1) along with four known coumarinolignans, cleomiscosin A (2), cleomiscosin B (3), cleomiscosin A-9′-acetate (4) and cleomiscosin B-9′-acetate (5). The structure elucidation of 1 was done by spectroscopic data interpretation and comparative HPLC analysis. Cleomiscosin A, but not its isomer cleomiscosin B, reduced dry and wet weight of cotton pellet granuloma in mice. This suggests that cleomiscosin A is an important constituent of MHN responsible for anti-inflammatory activity.     

Evaluation of the antinociceptive activity of Ficus deltoidea aqueous extract

The aqueous extract of Ficus deltoidea leaves was evaluated for possible antinociceptive activity in three models of nociception, namely, acetic acid-induced abdominal writhing, formalin and hot plate test. The results of the present study showed that intraperitoneal administration of the F. deltoidea leaves aqueous extract at the dose of 1, 50 and 100 mg/kg, 30 min prior to pain induction produced significant dose-dependent antinociceptive effect in all the models used, which indicating the presence of both central and peripherally mediated activities. Furthermore, the antinociceptive effect of the extract in the formalin and hot plate test was reversed by the non-selective opioid receptor antagonist naloxone suggesting that the endogenous opioid system is involved in its analgesic mechanism of action. Thus, the present results demonstrated that F. deltoidea leaves aqueous extract contains pharmacologically active constituents which possess antinociceptive activity justifying its popular therapeutic use in treating conditions associated with the painful conditions.     

Anti-inflammatory and analgesic activity of the topical preparation of Glaucium grandiflorum

The species of Glaucium have been used in Iranian herbal medicine in the treatment of dermatitis. Due to anti-inflammatory and analgesic activity of Glaucium grandiflorum methanolic extract in i.p. administration, these effects in topical administration were studied using carrageenan-induced edema and formalin test. Several formulations were prepared and the best cream was chosen as vehicle. Piroxicam gel and methyl salicylate ointment were studied as positive control for anti-inflammatory and analgesic activity, respectively. The edema inhibition of preparations containing extract at the doses of 1-5% w/w were significantly different from control group. The anti-inflammatory effect of MS4-5% was similar to the effect of piroxicam gel at 3 h after carrageenan injection. Topical preparation containing G. grandiflorum methanolic extract showed analgesic effect in concentrations more than 4% w/w in early phase in formalin test. This activity was observed in concentrations more than 3% w/w in late phase. The topical analgesic activity of extract was less than the analgesic activity of methyl salicylate ointment.     

Activity study of a hydroxynaphthoquinone fraction from Arnebia euchroma in experimental arthritis

Although various drugs for the treatment of rheumatoid arthritis (RA) have been used in clinics, RA is not completely curable to date. Thus, to seek new drugs for the treatment of RA has been a hotspot. Hydroxynaphthoquinones are the major anti-inflammatory active constituents in Arnebia euchroma (Royle) Johnst. The present study aims to evaluate the anti-arthritic activity of a hydroxynaphthoquinone mixture (HM) of A. euchroma (Royle) Johnst, including its anti-inflammatory and analgesic effects. The anti-arthritic efficacy of HM was examined using complete Freund's adjuvant- and bovine type II collagen-induced arthritic models. The paw edema, polyarthritis index and histopathological change were evaluated. The analgesic effect was assessed using the chemical and thermal models of nociception. Results found that HM administered prophylactically and curatively showed marked anti-arthritic activity by suppressing the paw swelling and development of inflammation, lowering the levels of TNF-α and IL-1β and protecting cartilage and bone from damage. The protection of HM was superior to that of reference drugs such as prednisone acetate or etanercept, and showed no direct deleterious effect. Similarly, HM showed significant analgesic effects. In summary, HM possessed potent anti-arthritic activity. It could relieve inflammatory symptoms and protect against joint destruction. These findings indicate that HM would be a potential therapeutic agent for arthritic disease, which provide pharmacological evidence for its clinical application.     

Anti-inflammatory and analgesic potential of a novel steroidal derivative from Bryophyllum pinnatum

A new steroidal derivative, urs Stigmast-4, 20 (21), 23-trien-3-one and other four compounds were isolated from the leaves of Bryophyllum pinnatum. The structure of this new steroid was elucidated and established by standard spectroscopic methods. Carrageenan induced paw edema model was used for anti-inflammatory and acetic acid induced model used for analgesic activity. This new steroidal compound was found to be active in reducing inflammation (% inhibition 87.29 and 84.45 respectively) when compared with diclofenac. Further, it showed 75.72% protection in analgesic activity in acetic acid induced writhing test in mice. In conclusion the % inhibition against carrageenan induced rat paw edema and % protection against acetic acid induced writhings showed by new compound revealed that the anti-inflammatory and analgesic activity of aqueous extract B. pinnatum are mainly due to the presence of this steroidal compound.     

Studies on antidepressant and antinociceptive effects of ethyl acetate extract from Piper laetispicum and structure-activity relationship of its amide alkaloids

Piper laetispicum C.DC. (Piperaceae), is an endemic climbing, glabrous plant distributed in the southern part of China. A novel alkaloid amide, Laetispicine, from it has been proven to possess antidepressant activity. In this present study, antidepressant and antinociceptive effects of the ethyl acetate extract (EAE) of P. laetispicum have been studied in forced swimming, open field, acetic acid writhing and formalin tests in KM mice. A significantly antidepressant-like effect was showing at doses of higher than 60 mg/kg, which was not due to an increase in locomotive activity. The EAE also presented an analgesic effect, in our studies. At lower doses (30 mg/kg) the antinociceptive effect was likely mediated via peripheral inflammation and changes in central processing, and at higher doses (120 mg/kg) that was due to both central and peripheral pathways. We also quantitatively analyzed the major components of EAE by HPLC and approached the structure–activity relationship between structure of amide alkaloids and its antidepressant activities. The antidepressant effective components of EAE might be Leatispiamide A and Laetispicine. In their molecular structures, the isolated double bond from benzene ring and conjugated double bond located at 2–3 and 4–5 were necessary for its antidepressant activity.     

Antinociceptive activity of Eupatorium buniifolium aqueous extract

The antinociceptive properties of the aqueous extract of Eupatorium buniifolium aerial parts were investigated in chemical and thermal models of nociception in mice. Oral doses of 250 and 500 mg/kg produced an inhibition of 42.3% and 73.9%, respectively, of the abdominal writhes induced by acetic acid in mice. This antinociceptive effect was not reversed by pretreatment with naloxone. In the formalin test, the administration of 500 and 1000 mg/kg p.o. had no effects in the first phase (0-5 min) but produced a dose-dependent analgesic effect on the second phase (15-30 min) with inhibitions of the licking time of 38.9% and 57.3%, respectively. In the hot plate test, no effect was seen at the dose of 500 mg/kg p.o.     

Theacrine,a purine alkaloid with anti-inflammatory and analgesic activities

The anti-inflammatory and analgesic effects of theacrine (1, 3, 7, 9-tetramethyluric acid), a purine alkaloid which is abundantly present in Camellia kucha, were investigated. Xylene-induced ear edema, acetic acid-induced vascular permeability and λ-carrageenan-induced paw edema were used to investigate anti-inflammatory activity, and acetic acid-induced writhing and hot-plate tests were used to determine analgesic effect. Oral administration of theacrine (8–32 mg/kg) induced dose-related anti-inflammatory and analgesic effects. On the other hand, oral caffeine administration (8–32 mg/kg) did not show an inhibitory effect on the inhibition of inflammatory response or cause analgesia. Additionally, the result of the acute toxicity test showed that the LD₅₀ of theacrine was 810.6 mg/kg (769.5–858.0 mg/kg). The data obtained suggest theacrine possessed analgesic and anti-inflammatory activities.     

Antinociceptive activity of Zizyphus spina-christi root bark extract

The antinociceptive effect of the aqueous extract of Zizyphus spina-christi root bark was investigated in mice and rats. Acetic acid-induced writhing, formalin and thermal (hot plate) tests were used. The extract (50 and 100 mg/kg, i.p.) showed a dose-dependent analgesic effect in all the tests used. Its i.p. LD50 in mice was 2236.07 mg/kg.     

Analgesic and anti-inflammatory effects of the aqueous extract of leaves of Persea americana mill (lauraceae)

The aqueous extract of Persea americana leaves produced a dose-dependent inhibition of both phases of formalin pain test in mice, a reduction in mouse writhing induced by acetic acid and an elevation of pain threshold in the hot plate test in mice. The extract also produced a dose-dependent inhibition of carrageenan-induced rat paw oedema. The results obtained indicate that the extract possesses analgesic and anti-inflammatory effects.     

Anti-inflammatory activity of Butea monosperma flowers

Methanolic extract of Butea monosperma flowers (MEBM) was studied for anti-inflammatory activity against carrageenin induced paw edema and cotton pellet granuloma in albino rats. In carrageenin induced paw edema, MEBM at oral doses of 600 mg/kg and 800 mg/kg, dose-dependently inhibited the paw edema. In cotton pellet induced granuloma, MEBM at the same doses was found to significantly inhibit granuloma tissue formation, including significant reduction in levels of serum lysosomal enzymes (SGOT, SGPT and ALP) and lipid peroxides as compared to control.     

Antinociceptive and anti-inflammatory activities of Phlomis umbrosa Turcz extract

Phlomis umbrosa Turcz has been used as the traditional medicine for thousands of years in China. In this paper, the acetic acid-induced writhing test, the hot plate test, the carrageenan-induced paw edema test, the xylene-induced ear swelling test, and the acetic acid-induced Evans blue leakage and leukocyte infiltration test were used to investigate the antinociceptive and anti-inflammatory activities of the aqueous extract of this plant (25, 50 and 100 mg/kg i.p.). Good dose-dependent effects were obtained in most of these tests, except in the hot plate test and the acetic acid-induced Evans blue leakage test. TLC and HPLC analyses showed iridoid glucosides were the main compositions of this extract. These findings suggested that the aqueous extract of P. umbrosa has significant antinociceptive and anti-inflammatory activities.     

Analgesic activity of Peperomia pellucida aerial parts in mice

The methanol extract of Peperomia pellucida aerial parts, given orally at doses ranging from 70 to 210 mg/kg, showed a significant analgesic activity on acetic acid-induced writhing in mice.     

Transdermal behaviors comparisons among Evodia rutaecarpa extracts with different purity of evodiamine and rutaecarpine and the effect of topical formulation in vivo

Aim

Evodiamine (EVO) and rutaecapine (RUT), the major active components from Evodia rutaecarpa extract (EE), are recognized as a depended analgesic agent. This study was designed to investigate the effect of purity and chemical enhancers on the transdermal behavior of EVO and RUT, and the pharmacological effect of their topical cream in vivo.

Material and methods

Transdermal delivery across a full thickness pig abdominal skin was detected in vitro by Franz-type diffusion cell, with HPLC for quantification of the permeation of EVO and RUT. The activity of topical cream in vivo was evaluated by a mice pain model induced by formalin and hot plate.

Results

Transdermal characters of EVO and RUT showed a low transdermal rate, long lag time and low cumulative amount. The transdermal rate and cumulative amount could be promoted by lipophilic enhancers, whereas lag time was shortened by hydrophilic surfactant, but these permeation parameters were not markedly influenced by purity of EE (p > 0.05). The effect in vivo was confirmed by analgesic models in topical cream of EE, which produced a significant (p < 0.05) inhibitory effects on pain response in dose-dependent manner.

Conclusion

The purity of EVO and RUT from EE has no significant effect on their permeation through porcine skin, but oleic acid or nerolidol can markedly elevate the transdermal rate of EVO and RUT. High purity of EE is the best choice for topical preparation to increase the drug loading. The effect of EE in vivo is verified by formalin model and hot plate test.