Histamine-induced Rat Paw Edema Research Articles

Viscum monoicum: A New Source of Polyphenolic Compounds Responsible for Antioxidant and Anti-Inflammatory Activities

ABSTRACT Viscum monoicum has been used as a traditional medicinal plant for the treatment of many ailments that include pain, neuropharmacological disorders as well as various types of tumors. This study was designed to investigate the polyphenolic compound, antioxidant, and anti-inflammatory activities of the ethanolic extract of Viscum monoicum (EVM). The extract was subjected to HPLC-DAD analysis for the quantification of polyphenols. In addition, DPPH, ABTS free radical scavenging, reducing power, total antioxidant capacity, phenolic, and flavonoid content was measured for antioxidant activities of EVM. Besides, the anti-inflammatory activity of EVM was studied using carrageenan and histamine-induced rat paw edema at different doses. High levels of ellagic acid and (+)-catechin hydrate (410.15 and 340.88 mg/100 g extract, respectively) were determined for the first time through HPLC in EVM. IC50 of EVM was significant in DPPH and ABTS scavenging assay compared to that of ascorbic acid. The total antioxidant capacity, total phenolic, and total flavonoid contents were estimated and found significant amount equivalent to standard. At a dose of 400 mg kg−1, a significant anti-inflammatory activity (P<0.01) was observed in rats at both carrageenan and histamine-induced edema test models with a reduction in the paw volume; in comparison to indomethacin. Therefore, the results suggest that polyphenolic compounds might be responsible for the antioxidant and anti-inflammatory activities of EVM.

Denatonium benzoate decreases the effect of histamine in vitro and in rats

Purpose: To evaluate the effect of denatonium benzoate (DB) in histamine-induced model of inflammation and the effect of the selective H1 receptor agonist (2-(2-Pyridyl) ethylamine) on rat gastric smooth muscle strips pretreated with DB.Methods: The anti-inflammatory effect of DB was evaluated in vivo on histamine-induced rat paw edema. In vitro studies on spontaneous muscle contraction were performed on smooth muscle strips isolated from rat gastric corpus.Results: The results showed a well-defined anti-inflammatory effect of DB (15 mg/kg) during the early stage of rat paw edema at the 15th (p &lt; 0.001), 30th (p &lt; 0.01) and 60th min (p &lt; 0.001) compared to control. In vitro experiments indicated reduced spontaneous contractile activity of smooth muscle strips to H1 receptor agonist in the presence of DB (0.5 μM). The vascular effects of histamine are mediated by H1 receptors. Substances, which reduce the effect of histamine on the H1 receptors could influence the early stage of histamine-induced inflammation.Conclusion: The results show that the anti-inflammatory activity of DB probably is related to its antagonistic activity on histamine H1 receptors. The results would contribute to the search for new antiinflammatory drugs.&#x0D; Keywords: Denatonium benzoate, Inflammation, Histamine, Muscle contraction

Nano formulated proanthocyanidins as an effective wound healing component

Proanthocyanidins (PCs), a component of grape seed extract (GSE), have recently being used for the treatment of wounds. However, poor absorption, poor stability and rapid elimination from the systemic circulation limit its acceptance. In addressing these problems, we herein report the development of PCs based nanoformulations (PCs/SOLU) for the first time based on 1% GSE and assessed its wound healing potential in-vivo on the wistar rats. GSE and PCs/SOLU nanodispersions 1% were prepared by incorporating them into the ointment base via uniform mixing to form ointment which could be easily applied topically to wounds. The antibacterial activity of PCs/SOLU against gram positive and gram-negative bacteria strains proved that the cell membranes became more permeable with disrupted cell structure. While carrageenan and histamine induced rat paw edema analyses show there was no inflammatory signs in animals treated with 1 wt% of PCs/SOLU nanodispersion. Excision wound measuring about 3 cm in depth was created on the wistar rats. The ointment was applied topically on the wounded site and the wound contraction was measured daily. Grape seed extract (GSE) ointment, ointment base and povidone‑iodine (Povi-Iod) ointment of about 1% was used as the control, positive and negative standards. PCs/SOLU nanodispersion heals the wound by mobilising the fibroblasts in the wound site and inhibits the inflammatory response through decreased expression of monocyte. The macroscopical, immunological and histopathological assessments revealed that PCs/SOLU nanodispersion ointment usage improves the cell adhesion and proliferation.

The effect of Elsholtzia densa methanolic extract modulates inflammation in vitro and in vivo

Inflammatory diseases being one of the back bending global burden are alarming the world. Established anti-inflammatory drugs exert side-effects, demanding for the development of alternative drugs, likely from natural source because of their diverse chemical nature. The anti-inflammatory activity of aerial part methanol extract of Elsholtzia densa collected from the natural forest of Naranag area of Kashmir valley was evaluated both in vitro and in vivo model systems using Macrophages RAW 264.7 cells and acute (carrageenan and histamine-induced rat paw edema) and chronic model (formaldehyde induced arthritis) respectively. The EDM extract exhibited a significant decline in the paw volume being at par with the standard drug Diclofenac (10 mg/kg) as compared with the control group. The reduction was observed in dose dependent manner with 300 mg/kg resulting in 27.27% and 100 mg/kg in 16.88% inhibition at 3rd h. A statistically significant (p < 0.05) decline in the secretion of serum pro-inflammatory cytokines like TNF-α, IL-1 β and IL-6 was found with 80.93%, 75.33% and 67.09%, and 83.25%, 62.11% and 66.69% in EDM-300 as compared with the carrageenan and histamine group respectively. The pro-inflammatory cytokines levels showed clampdown in LPS stimulated RAW264.7 by the extract treatments. The LC–MS data revealed the presence of Quercetin 3-glycosides, Apigenin 7-(2″-acetyl-6″-methylglucuronide) and betulinic acid as major compounds present in EDM extract. Results obtained from in vivo experiments demonstrate that oral administration of EDM extract significantly attenuated inflammation in carrageenan and histamine-induced paw edema, and improved chronic models (formaldehyde induced arthritis).

Evaluation on Analgesic and Anti-Inflammatory Activities of Total Flavonoids from Juniperus sabina.

The leaves of Juniperus sabina (Cupressaceae) are used in traditional Uygur medicine for the treatment of rheumatism and arthritic pain. This study aimed to investigate the analgesic and anti-inflammatory effects of total flavonoids from leaves of Juniperus sabina (JSTF) on rodents. The anti-inflammatory activity was investigated using the carrageenan, egg albumin, or histamine-induced rat paw edema as well as xylene-induced ear edema, capillary permeability, and cotton pellet granuloma while the antinociceptive activity was evaluated using the mouse writhing, formalin, and hot-plate tests. JSTF (125, 250, 500 mg/kg) significantly inhibited xylene-induced ear edema in mice (inhibition ratio as 16.22%, 40.67%, and 51.78%, respectively) and also significantly ameliorated acetic acid increased vascular permeability in mice (inhibition ratio as 11.63%, 32.56%, and 53.49%, respectively). JSTF (250 and 500 mg/kg) gave significant reduction of carrageenin-induced paw oedema at the interval of 1 h and 5 h. Administration of JSTF (500 mg/kg) caused a significant anti-inflammatory effect against oedema induced by egg albumin or histamine at the interval of 0.5 h and 4 h, and both which induced the paw oedema were also inhibited by JSTF (250 mg/kg) at a point in 1, 2, or 3 h after the inflammation. Furthermore, JSTF (125, 250, and 500 mg/kg) produced time-course increase in pain threshold in hot-plate test also. JSTF produced concentration-dependent inhibition on cyclooxygenase-2 (COX-2) or 5-lipoxygenase (5-LO) activities in vitro, and their IC50 values were 31.92 and 129.26 μg/mL, respectively. Moreover, JSTF significantly caused a significant dose-dependent inhibition on acetic acid induced writhing response in mice (inhibition ratio as 23.27%, 36.91%, and 50.76%, respectively). JSTF also significantly ameliorated formalin-induced pain in mice in the late phase on dose-dependent way. These results confirms the clinical use of J. sabina for treatment of rheumatoid arthritis in ethnomedicine, and its effective mechanism will be further studied in the future.

Preliminary screening of &lt;em&gt;Waltheria indica&lt;/em&gt; (L.) plant for its anti-inflammatory activity

&lt;p dir="ltr"&gt;&lt;span&gt;The investigation on anti-inflammatory activity of the various extract of &lt;/span&gt;&lt;span&gt;Waltheria indica &lt;/span&gt;&lt;span&gt;L. &lt;/span&gt;&lt;span&gt;was reported to find out the pharmacological basis for its ethnomedical use. &lt;/span&gt;&lt;span&gt;The anti-inflammatory activity of the pet ether (PEW) and methanol (MEW) extracts of the leaves of &lt;/span&gt;&lt;span&gt;Waltheria indica &lt;/span&gt;&lt;span&gt;L. (&lt;/span&gt;&lt;span&gt;Malvaceae&lt;/span&gt;&lt;span&gt;)&lt;/span&gt;&lt;span&gt;were evaluated by using in vivo (Carrageenan &amp;amp; histamine induced rat paw edema, cotton pellet granuloma test) models. It was observed that, all the extracts showed significant activity in the in-vivo model at the dose of 500 mg/kg b.w. orally, when compared with control and standard drugs. Of the two extracts tested, methanol extract MEW showed most significant activity well in comparison to the standard drug. Therefore, present study suggests, potential of leaves of &lt;/span&gt;&lt;span&gt;Waltheria indica &lt;/span&gt;&lt;span&gt;L. in both models of acute and chronic inflammation.&lt;/span&gt;&lt;/p&gt;&lt;p dir="ltr"&gt; &lt;/p&gt;

Anti-Inflammatory and Antioxidant Activity of Acalypha hispida Leaf and Analysis of its Major Bioactive Polyphenols by HPLC.

Inflammation and oxidative stress can lead to different chronic diseases including cancer and atherosclerosis. Many medicinal plants have the potential to show as anti-inflammatory activity. Present investigation was performed to investigate anti-inflammatory, antioxidant activity, and quantification of selected bioactive plant polyphenols of the ethanol (EAH) and aqueous (AAH) extracts of Acalypha hispida (Euphorbiaceae) leaves. Anti-inflammatory activity was evaluated by carragenan and histamine induced rat paw edema models while antioxidant capacity was evaluated by DPPH free radical scavenging, Fe+2 chelating ability, reducing power, NO scavenging, total phenolic and total flavonoid content assay. Identification and quantification of bioactive polyphenols was done by HPLC. At the doses of 200 and 400 mg/kg, both EAH and AAH showed statistically significant inhibition of paw volume in the anti-inflammatory activity test. Both the extracts showed DPPH scavenging (IC50: 14 and 17 µg/ml, respectively), Fe+2 ion chelating (IC50: 40 and 46 µg/ml, respectively), NO scavenging activity (65.49 and 60.66% inhibition at 100 µg/ml), and concentration dependent reducing power ability. For EAH and AAH, flavonoid content was 126.30 and 149.72 mg QE/g dry extract, while phenolic content was 130.51 and 173.80 mg GAE/g dry extract, respectively. HPLC analysis of EAH and AAH indicated the presence of high content of ellagic acid along with other phenolic constituents. High content of ellagic acid along with other phenolic constituents might have played an important role in the observed anti-inflammatory and antioxidant activity.

Dual effects of a lectin from the green seaweed Caulerpa cupressoides var. lycopodium on inflammatory mediators in classical models of inflammation.

Wide biotechnological investigations of only a limited number of seaweed lectins have been performed. We previously demonstrated the anti-nociceptive and anti-inflammatory effects of a lectin isolated from the green seaweed Caulerpa cupressoides var. lycopodium (CcL). Herein, we further studied the mechanisms of action of CcL. Classical acute inflammation models induced by different flogistic agents were used to evaluate the anti-inflammatory action of CcL. CcL was injected locally into the rat paw to verify a possible pro-inflammatory outcome. CcL (0.1, 1 or 10mg/kg; i.v.) reduced the carrageenan-induced rat paw edema and neutrophilic infiltration, which was not altered by either mucin (inhibitor of CcL carbohydrate-binding site) or ZnPP-IX (specific HO-1 inhibitor). Immunohistochemical analyses showed that CcL (1mg/kg) reduced the expression of the cytokines IL-1β, TNF-α, IL-6 and COX-2. CcL (0.1, 1 or 10mg/kg) inhibited dextran, and CcL (1mg/kg) inhibited histamine-induced rat paw edema. Both effects were reversed by mucin inhibition. CcL (1mg/kg) was ineffective for the treatment of serotonin- and bradykinin-induced rat paw edema. When injected via the i.pl. route, CcL (10mg/kg) elicited rat paw edema involving a wide range of mediators. The anti-inflammatory action of CcL involves the inhibition of IL-1β, TNF-α, IL-6 and COX-2 expression and histamine H1 receptors. When locally administered, CcL exerts pro-inflammatory actions.

Anti-inflammatory and antioxidant activities of ethanolic extract of aerial parts of Vernonia patula (Dryand.) Merr.

ObjectiveTo investigate the inflammatory and antioxidant activities of ethanolic extract of aerial part of Vernonia patula (Dryand.) Merr (EAV). MethodsThe anti-inflammatory activity of EAV was studied using carrageenan and histamine-induced rat paw edema test at different doses (100, 200 and 400 mg/kg body weight). DPPH free radical scavenging, nitric oxide scavenging, reducing power and Fe2+ ion chelating ability were used for determining antioxidant activities. ResultsThe EAV, at the dose of 400 mg/kg, showed a significant anti-inflammatory activity (P<0.01) both in the carrageenan and histamine-induced oedema test models in rats, showing 62.86% and 64.42% reduction in the paw volume comparable to that produced by the standard drug indomethacin (67.26% and 66.01%) at 5 h respectively. In DPPH free radical scavenging test, IC50 value for EAV was found fairly significant 36.59 μg/mL when compared to the IC50 value of the reference standards ascorbic acid 8.97 μg/mL. The IC50 values of the extract and ascorbic acid were 47.72 and 12.39 μg/mL, respectively in nitric oxide scavenging assay. The IC50 value of the EAV (33.59 μg/mL) as percentage of Fe2+ ion chelating ability was also found significant compared to that of EDTA (9.16 μg/mL). The maximum absorbance for reducing power assay was found to be 1.928 at 100 μg/mL when compared to 2.449 for standard ascorbic acid. The total phenolic content was 198.81 mg/g of gallic acid equivalent. Acute toxicity test showed that the plant might be safe for pharmacological uses up to a dose level of 3 200 mg/kg of body weight in rats. ConclusionsTherefore, the obtained results suggest the acute anti-inflammatory and antioxidant activities of the EAV and thus provide the scientific basis for the traditional uses of this plant part as a remedy for inflammations.

Anti-inflammatory and antioxidant activities of ethanolic leaf extract of Brownlowia tersa (L.) Kosterm

The present study was designed to investigate the inflammatory and antioxidant activities of ethanolic leaf extract of Brownlowia tersa (L.) Kosterm. The anti-inflammatory activity of leaf extract was studied using carrageenan and histamine-induced rat paw edema test at different doses (200 and 400 mg/kg body weight). DPPH free radical scavenging, nitric oxide scavenging, reducing power, Fe++ ion chelating ability and total phenolic content were used for determining antioxidant activities. The extract, at the dose of 400 mg/kg, showed a significant anti-inflammatory activity (P < 0.01) both in the carrageenan and histamine-induced edema test models in rats showing 54.76 % and 56.96 % reduction in the paw volume comparable to that produced by the standard drug indomethacin (64.88 % and 67.09 %) at 4 h respectively. In DPPH free radical scavenging test, IC50 value for ethanolic extract was found fairly significant 39.33 μg/ml when compared to the IC50 value of the reference standards ascorbic acid and Butylated Hydroxy Anisole (BHA) (3.16 and 5.81 μg/ml) respectively. The IC50 values of the extract and ascorbic acid were 99.06 and 39.35 μg/ml, respectively in nitric oxide scavenging assay. The maximum absorbance for reducing power assay was found to be 1.276 at 100 μg/ml when compared to 2.821 and 1.231 for standard ascorbic acid and BHA respectively. The IC50 value of the extract as percentage of Fe++ ion chelating ability was also found significant compared to that of EDTA. The total phenolic content was 211.82 mg/g of gallic acid equivalent. Acute toxicity test showed that the plant might be safe for pharmacological uses up to a dose level of 3,200 mg/kg of body weight in rats. Therefore, the obtained results suggest the acute anti-inflammatory and antioxidant activities of the ethanolic extract of Brownlowia tersa leaves and thus provide the scientific basis for the traditional uses of this plant part as a remedy for pain and inflammations.

Evaluation of anti-inflammatory activity of Solanum xanthocarpum Schrad and Wendl (Kaṇṭakāri) extract in laboratory animals.

Context:Solanum xanthocarpum Schrad and Wendl (Kaṇṭakāri) is a diffuse herb with prickly stem, traditionally used for the treatment of inflammation and one in the group of daśamūla (group of ten herbs) herbs commonly used drug in Ayurveda.Aims:In continuation of search for potent natural anti-inflammatory agents, the present research work was planned to evaluate the anti-inflammatory activity of ethanol extract of S. xanthocarpum whole plant.Settings and Design:The ethanol extract was evaluated at dose 10, 30 and 100 mg/kg p.o. in rats.Materials and Methods:Using pharmacological screening models carrageenan induced rat paw edema, histamine induced rat paw edema and cotton pellet granuloma in rats.Statistical Analysis Used:Data obtained was analyzed statistically using analysis of variance followed by post-hoc Dunnett test, P < 0.05 is considered as statistically significant.Results:Acute treatment didn’t show anti-inflammatory activity against carrageenan and histamine induced paw edema. However, administration of 100 mg/kg p.o for 7 day reduced the granuloma formation in cotton pellet granuloma model.Conclusions:Present results support the traditional use of plant for anti-inflammatory activity. In brief, the results provide scientific pharmacological basis for the therapeutic use of S. xanthocarpum.

Anti-inflammatory, wound healing and in-vivo antioxidant properties of the leaves of Ficus amplissima Smith

Ethno pharmacological relevanceFicus amplissima, commonly known as kal-itchchi, being used in folklore medicine, leaves juice is applied externally on old chronic wounds and the latex is applied on the wound. AimThere was no scientific evidence justifying the medicinal use of Ficus amplissima, therefore the present study was aimed at evaluation of anti-inflammatory, wound healing and in-vivo antioxidant activity of the plant. Materials and methodsIn the present study the acetone extract of Ficus amplissima leaves were studied for enzymatic antioxidant activity through different assays, anti-inflammatory by using carrageenan and histamine induced rat paw edema models (50mg, 100mg acetone extract) and wound healing activity by incorporating the two doses (1% (w/w) and 2% (w/w)) of acetone extract and simple ointment base B.P. in concentration of 0.5% (w/w) using excision and incision wound models in rats. In case of the excision wound model wound contraction and period of epithelization was studied while incision wound model was evaluated by determining tensile strength. ResultsFicus amplissima leaves expressed the potent anti-inflammatory and in-vivo antioxidant activity where 100mg acetone extract showed high activity. Treatment of wound with ointment containing 2% (w/w) acetone extract exhibited significant (P<0.001) wound healing activity. ConclusionThe acetone extract of Ficus amplissima leaves exhibited better anti-inflammatory, wound healing and in-vivo antioxidant activity probably due to phenols constituents.

Synthesis and Anti-inflammatory Performance of Newly Cyclizine Derivatives on Adult Male Wistar Rats.

Cyclizine (1-benzhydryl-4-methyl-piperazine, CAS 82-92-8, CYC, I), a piperazine derivative, belongs to H1 antihistamine group of drugs that shows such pharmacological properties as anti-inflammatory, anti-allergic and anti-platelet effects, similar to other H1-receptor antagonists. In this study, two new tolyl and cumene derivatives of I (1-ethyl- 4-[(p-isopropylphenyl) (p-tolyl) methyl]-piperazine, II and 1-[3, 4-dichlorophenyl]-4-[[p-isopropylphenyl] [p-tolyl] methyl]-piperazine, III) were synthesized to investigate their acute and chronic anti-inflammatory activities in formalin and histamine-induced rat paw edema. In addition, the vascular permeability in formalin and histamine-induced paw edema, xylene-induced ear edema, and peritonitis due to acetic acid application into peritoneal cavity were measured. The cotton pellet-induced granuloma model was chosen for inducing chronic inflammation in rats. Findings proved reduction in formalin-induced rat paw edema and vascular permeability (acute inflammation) by I and II at 30 min after the injection. In addition, results in histamine-induced rat paw edema showed anti-inflammatory effects of all drugs started 60 min after the injection as these effects continued for a longer period by II and III comparing to I, as discussed above. In addition, the data on vascular permeability in xylene-induced ear edema and acetic acid-induced to peritoneal cavity confirmed that substitutions on cyclizine molecule were more effective and could decrease the vascular permeability and acute inflammation. However, the results from the cotton pellet-induced granuloma formation in rats revealed that none of the drugs (I-III) were effective to reduce the reactions and intermediates of chronic inflammation.

Anti-inflammatory effects of two new methyl and morpholine derivatives of diphenhydramine on rats

Diphenhydramines are one of the first-generation histamine H1-receptor antagonists of the ethanolamine class that demonstrate many pharmacological properties including anti-inflammatory effects. In this research, bromo (II) and two new tolyl derivatives of I, (Di [p-tolyl] [dimethylaminoethoxy] methane, III) and (Di [p-tolyl] [2-morpholinoethoxy] methane, IV) were synthesized. Their acute and chronic anti-inflammatory activities were evaluated with the formalin and histamine-induced rat paw edema. The vascular permeability in formalin and histamine-induced paw edema, in xylene-induced ear edema, and in peritonitis after acetic acid application into peritoneal cavity were also measured and compared to II. Cotton pellet-induced granuloma model was selected for inducing chronic inflammations in rats. The newly synthesized analogs of diphenhydramine seemed effective to decrease acute inflammations. It was concluded that the prominent anti-phlogistic effects of the new drugs could be related to its reduction vascular permeability mechanism(s) or to its antagonistic effects on H1 histamine receptors.

Anti-inflammatory effect of Stereospermum suaveolens ethanol extract in rats

The anti-inflammatory effect of the ethanol extract of Stereospermum suaveolens (Roxb.) DC (Bignoniaceae) bark given orally at the dose of 200 and 400 mg/kg body weight was studied in rats using the carrageenan-, dextran-, and histamine-induced hind paw edema, and cotton pellet-induced granuloma formation models. Indomethcin at the dose of 10 mg/kg body weight was used as a standard drug. The extract (400 mg/kg body weight per os) showed maximum inhibition of edema 64.6, 53.48, and 50.06% at the end of 3 h with carrageenan-, dextran-, and histamine-induced rat paw edema, respectively. The extract (400 mg/kg) exhibited significant reduction (34.77%) in granuloma weight in the cotton pellet-induced granuloma model. From these results it could be concluded that, the ethanol extract of Stereospermum suaveolens possesses maximum anti-inflammatory activity in a dose-dependent manner, in various experimental models.

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.