Modulation of inflammatory markers by the ethanolic extract of Leucas aspera in adjuvant arthritis

Aim of the study

To investigate the anti-inflammatory and antioxidant potential of ethanolic extract of Leucas aspera (EELA) in adjuvant arthritis.

Materials and methods

Complete Freund's adjuvant served to induce arthritis. EELA was administered in two doses along with vehicle control (0.1% carboxymethyl cellulose) and positive control (Diclofenac). Levels of tumour necrosis factor (TNF-)-α, C-reactive protein (CRP), Interleukin-2 (IL-2), Cathepsin D, activities of antioxidant enzymes superoxide dismutase (SOD), glutathione peroxidase (GPx) and catalase (CAT) were estimated in plasma/hemolysate and tissue. HPLC analysis of EELA was also performed.

Results

EELA exhibited significant anti-inflammatory (p < 0.001) and antioxidant activity (p < 0.001). It did not show mortality up to 2000 mg/kg body weight. Histopathological studies confirmed complete cartilage regeneration and near normal joint in EELA2 treated arthritic rats.

Conclusion

This study highlighted the antioxidant and anti-inflammatory potential of Leucas aspera. Three major families of compounds present in EELA may explain these activities: catechins (epicatechin, beta epicatechin), flavonoids (procyanidin), phytosterols (beta-sitosterol) apart from glycosides, phenolic compounds and tannins.     

Anti-inflammatory effect of extract and fractions from the leaves of Byrsonima intermedia A. Juss. in rats

Aim of the study

Byrsonima intermedia is commonly used for its antiseptic, antimicrobial, and anti-inflammatory properties in the treatment of diarrhea and dysentery in Brazilian folk medicine. The purpose of this study was to examine the anti-inflammatory activity of the aqueous extract and fractions of Byrsonima intermedia leaves.

Materials and methods

Rats with carrageenan-induced paw edema and fibrovascular tissue growth, which was induced by subcutaneous implantation of a cotton pellet, were used as acute and chronic animal models of inflammation to investigate the anti-inflammatory effects of the aqueous extract and the individual ethyl acetate (EtOAc) and aqueous fractions of Byrsonima intermedia and catechin. High-performance liquid chromatography (HPLC) was used to determine the fingerprint chromatogram of the aqueous extract and fractions of Byrsonima intermedia.

Results

The crude aqueous extract at test doses of 30-300 mg/kg p.o. clearly demonstrated anti-inflammatory effects by reducing carrageenan-induced paw edema, as did the ethyl acetate (100 mg/kg) and aqueous fractions (30-100 mg/kg). In the chronic inflammation rat animal model with fibrovascular tissue growth, the aqueous extract of Byrsonima intermedia (BiAE) at doses of 30-300 mg/kg and the individual EtOAc and aqueous fractions at doses of 30-100 mg/kg and catechin significantly reduced the formation of granulomatous tissue. The presence of catechin and phenolic compounds in the extract and fractions of Byrsonima intermedia was confirmed using HPLC.

Conclusion

BiAE and the individual EtOAc and aqueous fractions of Byrsonima intermedia exhibited chronic and acute anti-inflammatory efficacy in rats, which supports previous claims of its use in traditional medicine.     

Anti-inflammatory effect of Lithrea molleoides extracts and isolated active compounds

Aim of the study

In this study the anti-inflammatory activity of aqueous, dichloromethane (CH₂Cl₂) and methanolic (MeOH) extracts and two major compounds isolated from Lithrea molleoides (Vell.) Engl. (Anacardiaceae) were evaluated.

Materials and methods

Two classical experimental models were used, carrageenan-induced rat paw edema and 12-O-tetradecanoylphorbol-13 acetate (TPA) induced mouse ear edema.

Results

MeOH extracts exhibited a significant systemical anti-inflammatory effect in the carrageenan (inhibition of 46% at 3 h) and in the TPA-ear edema test (inhibition of 21%). The presence of methyl gallate (inhibition of 63% in TPA ear edema), as one of the main compounds in the active fraction from MeOH extract may be explained the effect observed. Also, 1,3-dihydroxy-(Z,Z)-5-(tridec-4′,7?dienyl) benzene obtained from CH₂Cl₂ extract showed a significant topical anti-inflammatory activity (inhibition of 68%). Furthermore, no signs of toxicity were observed with doses up to 3 g/kg in an acute toxicity assay.

Conclusions

The results of this study present evidence that Lithrea molleoides given either systemically or topically has anti-inflammatory properties.     

Analgesic and anti-inflammatory activities of 11-O-galloylbergenin

Aims of the study

Current study was designed to explore the analgesic and anti-inflammatory effects of a constituent isolated from Mallotus philippinensis, in order to validate its folk use.

Materials and methods

11-O-galloylbergenin was isolated from ethanolic extract of Mallotus philippinensis. Analgesic and anti-inflammatory activities of the test compound were assessed using formalin test and carrageenan-induced paw edema models.

Results

11-O-galloylbergenin showed significant analgesic activity at doses of 20 and 40 mg/kg against formalin test in rats. Similarly, 11-O-galloylbergenin exhibited significant anti-inflammatory activity in carrageenan-induced paw edema model at doses of 10, 20 and 30 mg/kg.

Conclusion

11-O-galloylbergenin has demonstrated its significant potential to be further investigated for its discovery as a new lead compound for management of pain and inflammation.     

Anti-inflammatory and analgesic properties of Drynaria quercifolia (L.) J. Smith

Ethnopharmacological relevance

Drynaria quercifolia (L.) J. Smith (Polypodiaceae), has been widely used by ethnic groups of India to treat inflammation, rheumatism, headache, bone fracture, jaundice, etc.

Aim of the study

To evaluate the anti-inflammatory and analgesic properties of the ethanolic extract of rhizome of Drynaria quercifolia (DQ) and its phytochemical profile.

Materials and methods

DQ was used to evaluate the anti-inflammatory and analgesic effects using carrageenan-induced paw oedema/cotton pellet-induced granuloma in Wistar rats and acetic acid-induced writhing/formalin-induced paw licking test in Swiss albino mice respectively.

Results

Oral administration of DQ produced significant inhibition of carrageenan-induced paw oedema and granuloma formation in rats, almost comparable to that caused by indomethacin. DQ significantly attenuated acute and delayed phases of formalin-induced pain and acetic acid-induced writhing episodes in mice. The analgesia was comparable to that produced by sodium salicylate and aspirin respectively. Phytochemical analysis gave positive tests for catechin, coumarins, flavonoids, phenolics, saponin, steroids, tannins, and triterpenes. The total phenolics in DQ was 244 mg/g and naringin content was 0.048%.

Conclusion

The results suggest the presence of potent anti-inflammatory and analgesic principles in DQ that justifies its use for alleviating painful inflammatory conditions.     

Characterization, anti-oxidative and anti-inflammatory effects of Costa Rican noni juice (Morinda citrifolia L.)

Aim of the study

Noni fruit (Morinda citrifolia L.) juice has been used for more than 2000 years in Polynesia as a traditional folk medicine. The aim of the present study was to finely characterize noni juice from Costa Rica and to evaluate its anti-oxidative and anti-inflammatory activities.

Materials and methods

A microfiltrated noni juice was prepared with Costarican nonis. HPLC-DAD and Electro Spray Ionization Mass Spectrometric detection (HPLC-ESI-MS) were used to identify phenolic compounds and iridoids. The anti-oxidative activity of noni juice was measured in vitro by both Oxygen Radical Absorbance Capacity (ORAC) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging methods. The anti-inflammatory effects of noni juice were investigated in vitro by: measuring its effect on nitric oxide and prostaglandin E2 production by activated macrophages, evaluating its inhibitory activities on cyclooxygenase (COX)-1 and -2 and in vivo on a carrageenan-induced paw oedema model in rats.

Results

Several polyphenols belonging to the coumarin, flavonoid and phenolic acid groups, and two iridoids were identified. Noni juice demonstrated a mean range free radical scavenging capacity. Furthermore, it also reduced carrageenan-induced paw oedema, directly inhibited cyclooxygenase COX-1 and COX-2 activities and inhibited the production of nitric oxide (NO) and prostaglandins E₂ (PGE₂) in activated J774 cells, in a dose dependent manner.

Conclusions

This study showed that noni's biological effects include: (1) anti-oxidant properties probably associated with phenolic compounds, iridoids and ascorbic acid and (2) anti-inflammatory action through NO and PGE₂ pathways that might also be strengthened by anti-oxidant effects.     

Isolation of active constituents from cherry laurel (Laurocerasus officinalis Roem.) leaves through bioassay-guided procedures

Ethnopharmacological relevance

The fresh leaves of Laurocerasus officinalis Roem. (Rosaceae) are externally used against pain and feverish symptoms in Turkish folk medicine.

Aim of the study

Effects of the extracts, fractions and isolated compounds from the leaves of L. officinalis were investigated using in vivo models of inflammation and pain in mice.

Methods

The crude ethanolic extract from the leaves of plant was sequentially fractionated into five subextracts; explicitly, n-hexane, chloroform, ethyl acetate (EtOAc), n-butanol, and remaining water extracts. Further studies were carried out on the most active EtOAc subextract was further subjected to fractionation through column chromatography. For the anti-inflammatory activity, carrageenan-induced hind paw edema and acetic acid-induced increase in capillary permeability models, and for the antinociceptive activity p-benzoquinone-induced writhing test in mice were employed.

Results

Ethanolic extract of the leaves was shown to possess significant inhibitory activity in the assay methods without inducing any gastric damage. Through bioassay-guided fractionation and isolation procedures three phenolic compounds, 2-O-β-d-glucopyranosyl-2-hydroxyphenyl-acetic acid (1), kaempferol-3-O-β-d-xylopyranosyl-(1→2)-O-β-d-glucopyranoside (2) and (+)-catechin (3) were isolated from the active fraction and their structures were elucidated by spectral techniques (1D and 2D NMR, ESIMS).

Conclusion

The experimental data verified that Laurocerasus officinalis leaves displayed remarkable anti-inflammatory and antinociceptive activity.     

Anti-inflammatory activity of Terminalia paniculata bark extract against acute and chronic inflammation in rats

Ethnopharmacological relevance

Terminalia paniculata Roxb. (Family-Combretaceae) is a wild tree commonly used in traditional ayurvedic medicine for the treatment of inflammation of parotid glands and in menstrual disorders.

Aim of the study

To explore the folk use of Terminalia paniculata on pharmacological grounds to evaluate the scientific basis of anti-inflammatory activity.

Materials and methods

The anti-inflammatory activity of Terminalia paniculata was studied against carrageenan-induced hind paw edema, air pouch inflammation and complete Freund's adjuvant (CFA)-induced arthritis in rats. The aqueous extract of Terminalia paniculata bark (TPW) was administered at the concentrations of 100, 200 and 400 mg/kg body weight.

Results

TPW showed significant (p < 0.05) anti-inflammatory activity by reducing the edema volume in carrageenan-induced paw edema in rats. Further, TPW (400 mg/kg) also reduced the carrageenan-induced leukocyte migration (50.92 ± 5.71%) and myeloperoxidase activity (49.31 ± 5.24%) in air pouch exudates. TPW (200 mg/kg) exhibits anti-rheumatic and analgesic activities by improving the altered haematological milieu (ESR, CRP, RF, WBC, RBC and Hb) and also by inhibiting the flexion scores and radiographic changes in CFA-induced arthritis. This extract also had significant (p < 0.05) effects on the occurrence of secondary lesions compared to CFA control.

Conclusions

Terminalia paniculata bark may be a potential preventive or therapeutic candidate for the treatment of chronic inflammation and arthritis.     

The analgesic and anti-inflammatory effect of WIN-34B, a new herbal formula for osteoarthritis composed of Lonicera japonica Thunb and Anemarrhena asphodeloides BUNGE in vivo

Ethnopharmacological relevance

: Lonicera japonica Thunb and Anemarrhena asphodeloides BUNGE have been used for the treatment of a variety of inflammatory diseases, cold and infective diseases in many countries, including Korea and China.

Aim of the study

: This study aimed to assess the anti-nociceptive and anti-inflammatory activities of n-butanol fraction (WIN-34B) prepared from dried flowers of Lonicera japonica and dried roots of Anemarrhena asphodeloides as potential novel treatment of osteoarthritis.

Materials and methods

: Anti-nociceptive activities of WIN-34B (100, 200 and 400 mg/kg, p.o.) were measured using acetic acid-induced writhing response, formalin-induced paw licking, hot plate, radiant heat tail-flick, carrageenan-induced paw pressure, and Hargreaves tests, respectively. Anti-inflammatory activities of WIN-34B (100, 200 and 400 mg/kg, p.o.) were assessed using acetic acid-induced vascular permeability, carrageenan-induced paw edema, and croton oil-induced ear edema. Anti-osteoarthritis effect of WIN-34B was analyzed using monosodium iodoacetate (MIA)-induced osteoarthritis animal model.

Results

: WIN-34B exhibited better anti-inflammatory activity than that of celecoxib in carrageenan at the dose of 200 mg/kg and croton oil-induced paw edema and ear edema at the doses of 200 and 400 mg/kg. WIN-34B exhibited significant anti-inflammatory effects on vascular permeability. WIN-34B also exhibited significant anti-nociceptive activities in the late phase of formalin-induced paw licking and writhing response model in mice. In radiant heat tail-flick and carrageenan-induced paw pressure tests, WIN-34B at the dose of 400 mg/kg and at the doses of 200 and 400 mg/kg presented similar activities to indomethacin and celecoxib. Compared to indomethacin WIN-34B at 400 mg/kg showed similar or better anti-nociceptive activities after 1 and 2 h of theraphy in the hot plate test and better anti-nociceptive activity than that of celecoxib in Hargreves test. In the MIA-induced osteoarthritis animal models, WIN-34B at 400 mg/kg exhibited similar or better anti-nociceptive property than that of celecoxib throughout the pain measurement periods.

Conclusion

: When compared to celecoxib, WIN-34B exhibited similar or better anti-nociceptive and anti-inflammatory activities in osteoarthritic animal models, which may become a potential novel treatment for osteoarthritis.     

Antioxidant and anti-inflammatory properties of Cardiospermum halicacabum and its reference compounds ex vivo and in vivo

Aims of the study

Cardiospermum halicacabum (CH) has been used in Chinese medicine for a long time. However, its fingerprint chromatogram, antioxidant, anti-inflammatory effects and mechanism are still needed to be explored. Therefore, the aims of this study investigated the antioxidant and anti-inflammatory effects of CH extracts and its reference compounds ex vivo and in vivo.

Materials and methods

In HPLC analysis, the fingerprint chromatogram of ethanolic extract of CH (ECH) was established. The effects of ACH (aqueous extract of CH) and ECH extracts were assessed for the antioxidant and LPS-induced NO production in RAW264.7 cells. In vivo anti-inflammatory activities of ECH were evaluated in mouse paw edema induced by λ-carrageenan (Carr). We investigate the anti-inflammatory mechanism of ECH via studies of the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) in the liver and the levels of malondialdehyde (MDA) and nitrite oxide (NO) in the edema paw. Serum NO and TNF-α were also measured.

Results

ECH had better antioxidant activity than that of ACH. In the anti-inflammatory test, ECH inhibited the development of paw edema induced by Carr and increased the activities of CAT, SOD and GPx in the liver tissue. ECH also decreased the level of NO in edematous paw tissue and in serum level, and diminished the level of serum TNF-α at the fifth hour after Carr injection.

Conclusions

ECH exerts anti-inflammatory effects by suppressing TNF-α and NO. The anti-inflammatory mechanism of ECH might be related to the decrement of the level of MDA in the edema paw via increasing the activities of CAT, SOD and GPx in the liver. The results showed that ECH might serve as a natural antioxidant and anti-inflammatory agent.     

Antioxidant, antinociceptive, and anti-inflammatory activities of Xanthii Fructus extract

Ethnopharmacological relevance

Xanthii seeds commonly called Cang-Erzi were used as a traditional Chinese medicine for treating sinusitis, headache due to rheumatism and skin pruritus.

Aim of the study

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

Materials and methods

The aqueous extract of Xanthii Fructus (AXF) was evaluated in mice for anti-inflammatory activity using carrageenan-induced hind paw edema model. The antinociceptive activity of AXF was evaluated by writhing and formalin tests. Antioxidant properties were assayed in terms of antioxidant activity by scavenging abilities on 1, 1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid (ABTS), reducing activity and liposome protection. In addition, the total phenolic content was determined with spectrophotometric method.

Results

AXF exhibited significant radical scavenging and reducing activity. And oral treatment with AXF elicited inhibitory activity on acetic acid effect and reduced the formalin effect at the late-phase. In the anti-inflammatory test, AXF inhibited the development of paw edema induced by λ-carrageenan (Carr). AXF decreased the paw edema at the fifth hour after Carr administration, and increased the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) in the liver tissue and decreased the malondialdehyde (MDA) level in the edema paw. AXF decreased the level of serum nitric oxide (NO) and tumor necrosis factor (TNF)-α after Carr injection and AXF decreased the levels of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) expressions in paw edema at the fifth hour.

Conclusions

AXF shows antioxidant, antinociceptive, and anti-inflammatory activities, supporting the folkloric usage of the plant to treat various inflammatory diseases.     

Chemical constituents from the stem bark of Symplocos paniculata Thunb. with antimicrobial, analgesic and anti-inflammatory activities

Ethnopharmacological relevance

The stem bark of Symplocos paniculata Thunb. has been used to check abortion in folk medicine in India.

Aim of the study

The present study was undertaken to isolate the phytochemicals from the plant together with the evaluation of antimicrobial, analgesic and anti-inflammatory activities of the plant extract and isolated compounds.

Materials and methods

The plant extract was subjected to column chromatography for isolation of phytochemicals. The agar diffusion method was adopted for antimicrobial activity to determine MICs. Ethanolic extract and isolated compounds were selected for investigating their analgesic activity on acetic acid-induced writhing response in mice. The anti-inflammatory activity was performed on carrageenan-induced paw edema in rats.

Results

The stem bark of the plant afforded seven compounds, 4-(8-hydroxyethyl) cyclohexan-1-oic acid (1); androst-5(6)-ene 17-one 3β-O-(β-d-glucopyranoside) (2); 9β,25-cyclo 3β-O-(β-d glucopyranosyl)-echynocystic acid (3); 9β,19-cyclo 24-methylcholan-5,22-diene 3β-O-{β-d-glucopyranosyl (1 → 6) α-l-rhamnopyranoside} (4); 30-ethyl 2α,16α-dihydroxy 3β-O-(β-d-glucopyranosyl) hopan-24-oic acid (5); 32,33,34-trimethyl-bacteriohopan-16-ene 3-O-β-d-glucopyranoside (6) and flavone 3′,4′,5′,6-tetramethoxy 7-O-β-d-glucopyranosyl (1 → 3) β-d-glucopyranoside (7). The extract and isolated compounds exhibited antimicrobial, analgesic and anti-inflammatory activities.

Conclusion

The present study concludes that ethanolic extract of the plant and its constituents having significant antimicrobial, analgesic and anti-inflammatory activities.     

Anti-inflammatory effects of methanol extract of Antrodia cinnamomea mycelia both in vitro and in vivo

Aims of the study

Antrodia cinnamomea is a folk medicinal mushroom commonly used in Taiwan for the treatment of several types of cancers and inflammatory disorders. This study aimed to explore the folk use of Antrodia cinnamomea on pharmacological grounds to characterize the scientific basis of anti-inflammatory activity.

Materials and methods

The in vitro anti-inflammatory activity of methanol extract of liquid cultured mycelia of Antrodia cinnamomea (MEMAC) was judged by the measurement of the produced levels of pro-inflammatory cytokines and mediators in lipopolysaccharide (LPS)-stimulated RAW264.7 cells and human peripheral blood mononuclear cells (PBMCs). The in vivo anti-inflammatory activity of MEMAC was evaluated using carrageenan-induced hind paw edema in mice, the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) in the liver and the levels of malondialdehyde (MDA) and nitrite oxide (NO) in the edema paw. The levels of serum NO and TNF-α were measured. The MEMAC was administered at the concentrations of 100, 200, and 400 mg/kg body weight of mouse.

Results

MEMAC inhibited the production of LPS-induced pro-inflammatory cytokines (TNF-α and IL-6) and mediators (NO and PGE2) in RAW264.7 cells and human PBMCs. Data from Western blotting showed that MEMAC decreased the levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein expression in LPS-stimulated RAW264.7 macrophages. In vivo, MEMAC showed significant (p < 0.05) anti-inflammatory activity by reducing the edema volume in carrageenan-induced paw edema in mice. MEMAC (400 mg/kg) also reduced the carrageenan-induced leukocyte migration (50.92 ± 5.71%). Further, MEMAC increased the activities of CAT, SOD, and GPx in the liver tissue and decreased the levels of serum NO and TNF-α after carrageenan administration.

Conclusions

Our results showed that MEMAC has the anti-inflammatory property both in vitro and in vivo, suggesting that it may be a potential preventive or therapeutic candidate for the treatment of inflammatory disorders.     

In vitro antioxidant, antiplatelet and anti-inflammatory activity of Carpobrotus rossii (pigface) extract

Ethnopharmacological relevance

Carpobrotus rossii (CR) has a history of use as a food and therapeutic agent by Australian indigenous peoples and early European settlers and is believed to contain a number of pharmacologically active polyphenolic compounds.

Aims of the study

Oxidation of low density lipoprotein (LDL), platelet aggregation, and inflammation contribute to the development and progression of atherosclerosis. The aim of the present study was to investigate the antioxidant, antiplatelet and anti-inflammatory activity of CR extract using human blood components.

Materials and methods

An assay employing in vitro copper-induced oxidation of serum lipids was used to assess antioxidant activity of CR extract (and tannin, flavonoid and pre- and post-flavonoid fractions). The effects of CR extract on ADP- and collagen-induced platelet aggregation, and on basal (unstimulated) and lipopolysaccharide (LPS)- and phytohaemagglutinin A (PHA)-stimulated cytokine release from peripheral blood mononuclear cells (PBMC) were also investigated.

Results

CR extract increased the lag time of serum oxidation (maximum of ∼4-fold at 20 μg/ml) in a concentration-dependent manner. The antioxidant activity resided only in the tannin and post-flavonoid fractions. CR had no effect on ADP-induced platelet aggregation, but significantly decreased collagen-induced platelet aggregation. LPS, but not PHA, significantly increased the release of IL-1β and TNF-α from PBMC. CR extract alone inhibited monocyte chemoattractant protein (MCP)-1 release and in the presence of LPS, inhibited IL-10, TNF-α and MCP-1 release compared to LPS alone.

Conclusion

CR has significant in vitro antioxidant, antiplatelet and, potentially, anti-inflammatory activity.     

In vivo study of four preparative extracts of Clematis terniflora DC. for antinociceptive activity and anti-inflammatory activity in rat model of carrageenan-induced chronic non-bacterial prostatitis

Aim of the study

The present study was conducted to evaluate the anti-inflammatory and antinociceptive activities of Clematis terniflora DC. extracts and fractions and to further support its traditional use as Chinese folk medicine in treatment of urinary infections, especially the disease of prostatitis.

Materials and methods

The antinociceptive activity of its water extract (WE), 70% ethanol extract (EE), water eluted part of EE from AB-8 macroporous resin (WEPMR) and 70% ethanol eluted part of EE from AB-8 macroporous resin (EEPMR) was conducted using mice writhing test with different doses. Then the anti-inflammatory activity of the four parts was evaluated on rat models of carrageenan-induced chronic non-bacterial prostatitis (CNP). Preliminary study was taken to determine the phytochemical compositions of the four preparative extracts.

Results

Significant writhing inhibitory effect was found with EE at small (7.5 g/kg body wt.), moderate (15 g/kg body wt.) and large (30 g/kg body wt.) doses (doses here are presented as crude herbs) as well as EEPMR at moderate and large doses by oral administration (OA) (p ≤ 0.01). Data from prostatic index, lecithin microsome density and white blood cell level showed that moderate dose of EE and EEPMR both had significant (p ≤ 0.05 or p ≤ 0.01) inhibition effect on carrageenan-induced inflammation in rat prostate. The HPLC analytical results showed that flavonoids were the main active compounds in WE, EE and EEPMR. And most flavonoids were accumulated into the part of EEPMR by AB-8 macroporous resin leaving only few compounds in WEPMR. No acute toxicity was identified in oral administration of the four parts at a dose of 100 g/kg body wt.

Conclusions

The results described here suggest that extracts of the aerial part of Clematis terniflora DC. might be of therapeutic interest in the treatment of prostatitis.     

Anti-inflammatory activity of Trichosanthes cucumerina Linn. in rats

Aim of the study

Trichosanthes cucumerina Linn. (Family: Cucurbitaceae) is one of the medicinal plants that is often used in Sri Lankan traditional systems of medicine. One of its uses is the treatment of inflammatory conditions. However, validity of the anti-inflammatory activity has not been scientifically investigated so far. Therefore, the aim of this study was to investigate the anti-inflammatory potential of Trichosanthes cucumerina hot water extract (HWE) and its fractions.

Materials and methods

The anti-inflammatory activity of Trichosanthes cucumerina was evaluated by use of the carrageenan-induced paw oedema model in Wistar rats. In addition, the mechanism/s by which Trichosanthes cucumerina is mediated the anti-inflammatory activity was assessed by determining its effects on (a) membrane stabilizing activity and (b) nitric oxide inhibitory activity.

Results

Apart from the lowest dose of the HWE, other tested doses (500, 750, 1000 mg/kg) produced a significant (P ≤ 0.05) inhibition of the inflammation, most pronounced at 5 h after the injection of carrageenan. The anti-inflammatory effect induced by 750 mg/kg, was comparable to that of the reference drug, indomethacin at 4 and 5 h. Inhibition of nitric oxide (NO) production and membrane stabilization activities are probable mechanisms by which Trichosanthes cucumerina mediates its anti-inflammatory actions. Among the tested fractions, methanol fraction (MEF) and aqueous fraction (AQF) at a dose of 75 mg/kg exhibited marked inhibition against carrageenan-induced hind paw oedema. The anti-inflammatory effect induced by MEF, was comparable to that of the reference drug, indomethacin and as well as to the 750 mg/kg of HWE at 4 and 5 h.

Conclusions

(a) These findings rationalize the traditional usage of this plant as an anti-inflammatory agent and (b) membrane stabilizing properties and NO inhibitory activity are possible mechanisms through which Trichosanthes cucumerina mediates its anti-inflammatory action.     

Studies on the anti-inflammatory properties of Plantago erosa leaf extract in rodents

Ethnopharmacological relevance

Leaves of Plantago erosa ex Roxb are used traditionally in Northeast India in different illnesses which include wounds, cuts, bruises, insect bites, poison-ivy rashes, minor sores and snakebite, etc.

Aim of the study

Plantago erosa is one of the commonly used medicinal plants in various inflammatory conditions in this region; however, due to paucity of scientific literature on its anti-inflammatory property, the present study was aimed at evaluating its anti-inflammatory activity in the leaves using in vivo models of inflammation.

Materials and methods

Different models like carageenan induced paw edema in rat and mice, formalin induced paw licking in rats and cotton pellet induced granuloma in rats were used for studying the anti-inflammatory activity in methanol extract of Plantago erosa (PEME) leaves.

Results

The PEME at the oral doses from 300 to 600 mg/kg showed anti-inflammatory activity in various models. The extract (PEME) reduced carageenan induced paw edema in rat and mice, inhibited the formation of granulomatous tissue in cotton pellet induced granuloma after treatment and also decreased the reaction time in both early and late phases in formalin induced paw licking in rats.

Conclusion

The study evidently confirmed anti-inflammatory activity of PEME and thus supported the traditional claim. The anti-inflammatory activity could be attributed to the phytoconstituent (flavonoids, alkaloids and steroid) present in the methanol extract of the plant.     

Bioassay-guided isolation of anti-inflammatory, antinociceptive and wound healer glycosides from the flowers of Verbascum mucronatum Lam.

Ethnopharmacological relevance

The leaves, flowers and whole aerial parts of Verbascum L. species have been used to treat respiratory problems, haemorrhoids and other types of inflammatory conditions in traditional Turkish medicine.

Aim of the study

In order to evaluate this traditional information, the anti-inflammatory, antinociceptive and wound healing activities of Verbascum mucronatum Lam. which is used as haemostatic in Turkish folk medicine were investigated.

Materials and methods

In vivo inhibitory effect of the extracts on the carrageenan-induced hind paw edema model in mice was studied for the assessment of anti-inflammatory activity. Moreover, the wound healing potential of the plant were evaluated by using in vivo wound healing experimental models, i.e. incision and excision models on mice and rats, were comparatively assessed with a reference ointment Madecassol^®. Skin samples were also evaluated histopathologically.

Results

The results of these experimental studies exhibited that Verbascum mucronatum displays anti-inflammatory, antinociceptive and wound healing activities. Through bioassay-guided fractionation and isolation procedures four iridoid glucosides, ajugol (1), aucubin (2), lasianthoside I (3), catalpol (4), two saponins, ilwensisaponin A (5) and C (6) and a phenylethanoid glycoside, verbascoside (7) were isolated and their structures were elucidated by spectral techniques. Verbascoside (7) was found to possess significant wound healing activity as well as antinociceptive and anti-inflammatory potentials, per os without inducing any apparent acute toxicity or gastric damage.

Conclusion

The experimental study revealed that Verbascum mucronatum displays remarkable antinociceptive, anti-inflammatory and wound healing activities.     

Anti-inflammatory effect of Ajuga bracteosa Wall Ex Benth. mediated through cyclooxygenase (COX) inhibition

Ethnopharmacological relevance

Ajuga bracteosa Wall Ex Benth. (Labiateae) is described in Ayurveda for the treatment of rheumatism, gout, palsy and amenorrhea.

Aim of the study

The aim of present investigation is to study anti-inflammatory activity of Ajuga bracteosa, to understand possible mechanism of action and to identify the constituents responsible for its activity.

Materials and methods

The anti-inflammatory activity of 70% ethanolic extract was evaluated in TPA-induced mouse ear edema assay and in vitro cyclooxygenase (COX)-1 and COX-2 inhibitory activity was determined using EIA kits employing appropriate reference standards. Aajugarin I, lupulin A, withaferin A, reptoside and 6-deoxyharpagide were isolated from the 70% ethanolic extract by silica gel column chromatography.

Results

The 70% ethanol extract of whole plants of Ajuga bracteosa showed a significant (p < 0.05) and dose-dependent anti-inflammatory activity in an acute inflammation model at the dose of 0.5 and 1.0 mg/ear. The extract also exhibited a strong in vitro COX-1 and COX-2 inhibitory activity at 25 and 50 μg/mL concentration. Among the isolated compounds 6-deoxyharpagide exhibited highest COX-2 inhibition while rest of the compounds exhibited weak to moderate COX-1 and COX-2 inhibition at 30 μM concentration.

Conclusions

The results suggest that the 70% ethanol extract of Ajuga bracteosa possesses promising anti-inflammatory activity, which is possibly mediated through inhibition of COX-1 and COX-2 enzymes. The isolated constituents could be responsible in part for its anti-inflammatory and COX inhibitory activity. The study supports traditional use of Ajuga bracteosa for inflammatory diseases.     

Anti-inflammatory activities and mechanisms of action of the petroleum ether fraction of Rosa multiflora Thunb. hips

Ethnopharmacological relevance

The hip of Rosa multiflora Thunb. has been traditionally used as a dietary supplement and a herbal remedy for the treatment of various diseases including cold, flu, inflammation, osteoarthritis, rheumatoid arthritis and chronic pain in China.

Aims of the study

To explore the anti-inflammatory ingredient of the hip of R. multiflora Thunb. and its mechanism of action.

Materials and methods

The ethanol extract of the hip of R. multiflora Thunb. was fractioned with petroleum ether, ethyl acetate and water, and each fraction was screened for anti-inflammatory activity in xylene-induced mouse ear edema model. Three more models, acetic acid-induced mouse vascular permeation, cotton pellet-induced rat granuloma, and carrageenan-induced rat hind paw edema were also employed to verify the anti-inflammatory effect of the identified fraction. To explore the mechanism of action, the activity of inducible nitric oxide synthase (iNOS) and the level of nitric oxide (NO) in sera, as well as mRNA expression level of cyclo-oxygenase-2 (COX-2) in inflammatory tissues of rats with carrageenan-induced hind paw edema were measured. GC-MS technology was applied to identify the active components in the active fraction.

Results and conclusions

The petroleum ether fraction (PEF) was identified to be the active fraction in inflammation animal models (i.e., oral administration of PEF (168.48, 42.12 and 10.53 mg/kg) evoked a significantly (P < 0.001) dose-dependent inhibition of the xylene-induced mice ear edema). Down-regulating COX-2 expression (P < 0.001) and reducing NO production (P < 0.05) through inhibiting iNOS activity (P < 0.001) may be the partial mechanism of action of PEF. GC-MS analysis indicated that unsaturated fatty acids are enriched in PEF and may be responsible for the anti-inflammatory activity of PEF and this herb. The results of this study provide pharmacological and chemical basis for the application of the hip of R. multiflora Thunb. in inflammatory disorders.