Effect of a Garcinia gardneriana (Planchon and Triana) Zappi hydroalcoholic extract on melanogenesis in B16F10 melanoma cells

Ethnopharmacology relevance

Garcinia gardneriana (Planchon and Triana) Zappi (Clusiaceae) is popularly called “bacopari” in southern Brazil. The leaves of this plant are traditionally used to treat skin disorders.

Aim of study

This study evaluated the effects of a hydroalcoholic extract of Garcinia gardneriana leaves (HEGG) on B16F10 murine melanoma cells in order to search for new depigmenting agents.

Materials and methods

The effects of HEGG were assessed in melanin content assays in B16F10 melanoma cells compared with the reference drug kojic acid (500 mM). Melanin content was measured after spontaneous melanogenesis, UVB-induced melanogenesis and melanogenesis induced by α-MSH. At the same time, cell viability assays were conducted. Intracellular and mushroom tyrosinase activity assays were employed to evaluate the effect of HEGG on tyrosinase activity.

Results

HEGG decreased the level of melanin under all three experimental conditions of melanin content evaluation without reducing cell viability. In intracellular tyrosinase assays, the enzyme's activity was reduced about 19% with extract concentrations ranging 0.1–10 µg/mL. In the mushroom tyrosinase activity assay a maximal inhibition of 35% (1000 µg/mL) was observed.

Conclusion

These results suggest that HEGG inhibition relates to its tyrosinase activity. Therefore, the hydroalcoholic extract of Garcinia gardneriana shows great potential for use as a depigmenting agent in hyperpigmentation disorders.     

Anti-inflammatory, analgesic and antipyretic activities of the extract of gamboge from Garcinia hanburyi Hook f

In Thai folklore medicine, gamboge, the yellow gum-resin secreted from Garcinia hanburyi, is used for infected wound, pain and edema The ethyl acetate extract from Garcinia hanburyi (GH5763) was assessed for anti-inflammatory, analgesic and antipyretic activities using experimental animal models. It was found that GH5763 possessed inhibitory activity on acute phase of inflammation as seen in ethyl phenylpropiolate-induced ear edema and carrageenin-induced hind paw edema in rats. However, GH5763 did not elicit any inhibitory effect on arachidonic acid-induced hind paw edema. In subchronic inflammatory model, GH5763 provoked a significant reduction of both transudative and proliferative phase when tested on cotton pellet-induced granuloma model. GH5763 also reduced the alkaline phosphatase activity in serum of rats in this animal model. In the analgesic test, GH5763 elicited inhibitory activity on acetic acid-induced writhing response and on both the early and the late phase of formalin test. Moreover, GH5763 also possessed an excellent antipyretic effect when tested in yeast-induced hyperthermic rats. It is postulated that the anti-inflammatory, analgesic and antipyretic activities of GH5763 are caused by the inhibition of the prostaglandin biosynthesis.     

Flavonoids with anti-inflammatory and antinociceptive activity from Cistus laurifolius L. leaves through bioassay-guided procedures

Extracts obtained from the leaves and branches of various Cistus species have been used worldwide as folk remedy for the treatment of various inflammatory ailments including rheumatism and renal inflammations. Effects of the extracts and fractions from the leaves with non-woody branches of Cistus laurifolius L. (Cistaceae) were studied using two in vivo models of inflammation in mice. Model one was based on observed potent inhibitory activity against carrageenan-induced hind paw oedema and the second model used was acetic acid-induced, increased vascular permeability model. Through bioassay-guided fractionation and isolation procedures three flavonoids; 3-O-methylquercetin (1), 3,7-O-dimethylquercetin (2) and 3,7-O-dimethylkaempferol (3) were isolated as the main active ingredients from the ethanol extract. Later on, these flavonoids were shown to possess potent antinociceptive activity, which was assessed through inhibition of p-benzoquinone-induced writhing reflex. Results of the present study have clearly supported the utilization of Cistus laurifolius in Turkish traditional medicine. Subsequently, three flavonoids were shown to have strong antinociceptive and anti-inflammatory activities, per os without inducing any apparent acute toxicity as well as gastric damage.     

Anti-inflammatory and anti-allergic properties of the essential oil and active compounds from Cordia verbenacea

The anti-inflammatory and anti-allergic effects of the essential oil of Cordia verbenacea (Boraginaceae) and some of its active compounds were evaluated. Systemic treatment with the essential oil of Cordia verbenacea (300-600mg/kg, p.o.) reduced carrageenan-induced rat paw oedema, myeloperoxidase activity and the mouse oedema elicited by carrageenan, bradykinin, substance P, histamine and platelet-activating factor. It also prevented carrageenan-evoked exudation and the neutrophil influx to the rat pleura and the neutrophil migration into carrageenan-stimulated mouse air pouches. Moreover, Cordia verbenacea oil inhibited the oedema caused by Apis mellifera venom or ovalbumin in sensitized rats and ovalbumin-evoked allergic pleurisy. The essential oil significantly decreased TNFalpha, without affecting IL-1beta production, in carrageenan-injected rat paws. Neither the PGE(2) formation after intrapleural injection of carrageenan nor the COX-1 or COX-2 activities in vitro were affected by the essential oil. Of high interest, the paw edema induced by carrageenan in mice was markedly inhibited by both sesquiterpenic compounds obtained from the essential oil: alpha-humulene and trans-caryophyllene (50mg/kg, p.o.). Collectively, the present results showed marked anti-inflammatory effects for the essential oil of Cordia verbenacea and some active compounds, probably by interfering with TNFalpha production. Cordia verbenacea essential oil or its constituents might represent new therapeutic options for the treatment of inflammatory diseases.     

Molecular mechanism of anti-inflammatory activity of Pluchea indica leaves in macrophages RAW 264.7 and its action in animal models ofinflammation

Ethnopharmacological relevance: Pluchea indica Less.

(Asteraceae) is a Thai medicinal plant used in traditional medicine for the treatment of hemorrhoids, lumbago, leucorrhoea and inflammation. This study investigated the molecular mechanism of anti-inflammatory activity of Pluchea indica leaf extract in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages and also determined its action in acute inflammation animal models.

Materials and methods

The inhibitory effect of Pluchea indica leaf extract on LPS-induced nitric oxide (NO) production was evaluated by Griess reaction. Protein and mRNA expressions were determined by real time RT-PCR and Western blotting analysis, respectively. Inducible nitric oxide synthase (iNOS) promoter activity was evaluated by iNOS promoter based reporter gene assay. In vivo anti-inflammatory effect was examined in ethylphenylpropiolate (EPP)-induced ear edema and carrageenan-induced paw edema in rat models.

Results

Ethyl acetate fraction of ethanol extract of Pluchea indica leaves (EFPI) exhibited the potent inhibitory effect on NO production in LPS-induced macrophages and also inhibited PGE₂ release. EFPI reduced iNOS mRNA and protein expression through suppressed iNOS promoter activity and nuclear translocation of subunit p65 of nuclear factor-κB, but did not inhibit phosphorylation of the mitogen-activated protein kinases (MAPKs). Moreover, EFPI possessed anti-inflammatory activities on acute phase of inflammation as seen in EPP-induced ear edema and carrageenan-induced paw edema inrats.

Conclusions

These data support the pharmacological basis of Pluchea indica plant as a traditional herbal medicine for treatment of inflammation.     

Anti-inflammatory activity of Markhamia tomentosa (Benth.) K. Schum. Ex Engl. ethanolic leaf extract

Ethnopharmacological relevance

The leaves of Markhamia tomentosa (Benth.) K. Schum (Bignoniaceae) are used traditionally for the treatment of oedema and rheumatoid arthritis in Nigeria.

Aim of the study

The aim of the work was to investigate the anti-inflammatory activity of the ethanolic leaf extract of Markhamia tomentosa.

Materials and methods

The extract was screened using the carrageenan-induced paw oedema in rats, xylene-induced oedema in mice and the formalin-induced oedema in mice at 50, 100, 200 mg/kg doses p.o respectively. The mechanism by which the extract mediated the anti-inflammatory activity was assessed using the histamine-induced rat paw oedema and serotonin-induced rat paw oedema at the highest dose (200 mg/kg).

Results

The results showed that the extract produced a significant dose-dependent inhibition in carrageenan-induced, xylene-induced and the formalin tests. The extract exerted a significant inhibition of 54.55% (P<0.0001) and 42.11% (P<0.01) at 90 min in the histamine-induced and serotonin-induced rat paw oedema models respectively.

Conclusions

These findings suggest that the ethanolic leaf extract of Markhamia tomentosa possesses anti-inflammatory activity possibly mediated by histamine. The results justify the use of the plant in the preparation of ethno medicines used in the treatment of ailments associated with inflammation.     

Anti-inflammatory and anti-nociceptive activities of the stem bark extracts from Allanblackia monticola STANER L.C. (Guttiferae)

THE AIM OF THIS STUDY: was to assess the anti-inflammatory and mechanism of action of Allanblackia monticola (Guttiferae). The anti-inflammatory activity "in vivo" of the methylene chloride/methanol extract, methanol and methylene chloride fractions of stem barks of Allanblackia monticola, administered orally at doses of 37.5; 75; 150 and 300 mg/kg, was evaluated on carrageenan-induced oedema in rats to determine the most active fraction. Indomethacin, inhibitor of cyclo-oxygenase was used as reference drug. The effects of the most active fraction were then examined on the rat paw oedema caused by histamine, serotonin, arachidonic acid and dextran followed by its ulcerogenic effect. The results showed that the methylene chloride fraction of Allanblackia monticola was more effective on the oedema caused by the carrageenan. The anti-nociceptive activity of the methylene chloride fraction was assessed using the acetic acid-induced abdominal constriction model, formalin test and hot plate test. At 150 mg/kg, Allanblackia monticola caused maximum inhibitions of inflammation induced by carrageenan (83.33%), by histamine (42.10%), by dextran (40.29%) and by arachidonic acid (64.28%). Allanblackia monticola (75-300 mg/kg) did not cause significant modification of the oedema induced by serotonin. Concerning the anti-nociceptive properties of the plant, the methylene chloride fraction (75-300 mg/kg) caused a dose-dependent inhibition on abdominal contractions induced by acetic acid (32.34-77.37%) and significantly inhibited the inflammatory pain caused by formalin (40.71-64.78%). Allanblackia monticola did not increase the latency time in the hot plate test. Like indomethacin (10mg/kg), the fraction at the dose of 150 mg/kg caused ulceration of the gastric mucous membrane in treated rats. These results show that Allanblackia monticola has an anti-inflammatory and analgesic activities with gastric ulcerative side effects.     

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.     

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.     

The latex obtained from Hancornia speciosa Gomes possesses anti-inflammatory activity

Aim of the study

Hancornia speciosa Gomes (Apocynaceae) is a tree that is widely distributed throughout Brazil. Its latex is collected and used extensively to treat acne, warts, diseases related to bursitis, and inflammation. In this work, we describe the anti-inflammatory effects of the latex.

Materials and methods

The latex from Hancornia speciosa (0.06-1.3 mg/kg, p.o.) and the reference drug acetylsalicylic acid (ASA, 200 mg/kg, p.o.) were evaluated in analgesia (formalin-induced licking, acetic acid-induced contortions, and hot plate) and inflammation models (formalin-induced licking, paw oedema, and subcutaneous air pouch, with measurement of cell migration, exudate volume, protein extravasations, nitric oxide, prostaglandin E2, TNF-α, and IL-6, and expression of the enzymes inducible nitric oxide synthase and cyclooxygenase 2).

Results

The latex from Hancornia speciosa significantly inhibited the number of writhings and the time that the animal spent licking the formalin-injected paw (second phase). Doses of 0.1-1.3 mg/kg latex reduced carrageenan-induced rat paw oedema. However, only the highest doses (0.6 and/or 1.3 mg/kg) reduced the oedema induced by bradykinin, histamine, and serotonin. The latex also inhibited inflammation induced by subcutaneous carrageenan injection, cell migration, exudate volume, protein extravasations, increased levels of inflammatory mediators (nitric oxide, prostaglandin E2, TNF-α, and IL-6) produced in the pouch, and increased expression of the enzymes nitric oxide synthase and cyclooxygenase 2.

Conclusions

Our results indicate that the latex obtained from Hancornia speciosa demonstrates significant anti-inflammatory activity through the inhibition of nitric oxide, PGE2, and cytokine production, thus confirming the popular use of this plant as an anti-inflammatory agent.     

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-ulcer, anti-inflammatory and antioxidant activities of the n-butanol fraction from Pteleopsis suberosa stem bark

Pteleopsis suberosa Engl. et Diels (Combretaceae) is a tree distributed in many African countries. The decoction from the stem bark is orally administered for the treatment of gastric ulcers in traditional medicine. Previous pharmacological studies reported the anti-ulcer activity of extracts from P. suberosa stem bark. In the present study, the anti-ulcer and anti-inflammatory effects of the n-butanol fraction (RBuOH) obtained from a methanol extract of P. suberosa bark were investigated on ethanol-induced gastric ulcers in rats and carrageenan-induced paw oedema in mice. Misoprostol (0.50 mg/kg, p.o.) and indomethacin (8.00 mg/kg, p.o.) were used as positive controls for anti-ulcer and anti-inflammatory activities, respectively. Results showed that RBuOH treatment significantly reduced the incidence of gastric lesions (50 mg/kg, P<0.05; 100 and 200 mg/kg, P<0.01) and restored the decreased levels of total sulfhydryl groups (T-SH) and non-protein sulfhydryl groups (NP-SH) (50, 100 mg/kg, P<0.05; 200 mg/kg, P<0.01) in the stomach homogenate. Moreover, RBuOH treatment attenuated MDA levels as index of lipid peroxidation in gastric mucosa. Administration of RBuOH at the same dosage (50, 100 and 200 mg/kg) reduced significantly (P<0.01) carrageenan-induced paw oedema in dose-dependent manner (from 42.81% to 87.81% inhibition, 5h after carrageenan injection). The anti-inflammatory effect of RBuOH at 200 mg/kg was comparable with that of indomethacin. Finally, RBuOH proved to possess elevated free radical scavenger capacity on 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay (IC(50) 23.48 microg/ml) which may contribute to the observed anti-ulcer and anti-inflammatory activities.     

The effect of the aqueous extract of Helietta parvifolia A. Gray (Rutaceae) stem bark on carrageenan-induced paw oedema and granuloma tissue formation in mice

Aims of study

Despite the ethnopharmacological relevance of Helietta parvifolia A. Gray (Rutaceae) in Mexico, we found no significant pharmacological studies of this plant in the scientific literature. The aim of the present study was to establish the anti-inflammatory effect of an aqueous extract of the stem bark of Helietta parvifolia in mice.

Materials and methods

The anti-inflammatory activity of the aqueous extract of the stem bark of Helietta parvifolia was evaluated using carrageenan-induced paw oedema in mice, and the cotton pellet granuloma method.

Results

An extract dose ranging from 20 to 80 mg/kg p.o. showed a non-significant effect over the initial phase of carrageenan-induced oedema. However, it showed a significant inhibition of oedema after 3 h, which can be related to the inhibition of the release of kinin-like substances. An ID₅₀ value of 47.4 mg/kg was obtained for the plant extract. The extract also suppressed granulomatous tissue formation during chronic inflammation. The inhibitory values were 19.2, and 22.2, corresponding to 40 and 80 mg/kg doses of extract respectively.

Conclusions

Aqueous extract showed a statistically significant anti-inflammatory effect in mice during the late phase of acute inflammation and during chronic inflammation. However, the exact mechanism(s) of anti-inflammatory effects of Helietta parvifolia observed in this study remains unclear.     

Preliminary study of the anti-inflammatory activity of hexane extract and fractions from Bursera simaruba (Linneo) Sarg. (Burseraceae) leaves

Bursera simaruba (L.) Sarg. leaves hexane extracts display anti-inflammatory activity on the adjuvant-carrageenan-induced inflammation in rats. In order to isolate and identify the active compounds of the hexane extract, we performed a preliminary phytochemical study and a bioassay-directed fractionation using the carrageenan-induced paw oedema test in mice. From the nine fractions (A-I) obtained, of an initial chromatographic separation, fractions A and E (doses equivalents to 1.50 g dry plant/kg body weight) showed the strongest anti-inflammatory activity comparable to that of the reference drug phenylbutazone (80 mg/kg). The isolation and characterization of 3-methylene-7,11,15-trimethylhexadec-1-ene (neophytadiene) (1), ergost-5-en-3beta-ol (2), 24S-stigmast-5,22E-dien-3beta-ol (3), 24S-stigmast-5-en-3beta-ol (4) and alpha-amyrin (5), from these fractions is reported.     

Inhibitory effect of eupatilin and jaceosidin isolated from Artemisia princeps on carrageenan-induced inflammation in mice

Ethnopharmacological relevance

Artemisia princeps Pampanini (family Asteraceae) is an herbal medicine widely used as a hepatoprotective, antioxidative, anti-inflammatory, and antibacterial agent in Korea, China, and Japan.

Aim of the study

This study aimed to elucidate the anti-inflammatory effect of the main constituents, eupatilin and jaceosidin, isolated from Artemisia princeps.

Materials and methods

We used carrageenan-induced inflammation in an air pouch on the back of mice and carrageenan-induced hind paw edema in rats to determine the anti-inflammatory effects of eupatilin and jaceosidin. Inflammatory makers, such as expression of pro-inflammatory cytokines and cyclooxygenase (COX)-2, and activation of nuclear factor-kappa B (NF-κB), were measured by enzyme-linked immunosorbent assays and immunoblot analyses.

Results

Eupatilin and jaceosidin blocked carrageenan-induced increase in leukocyte number and protein levels in air pouch exudates. Eupatilin and jaceosidin inhibited COX-2 expression and NF-κB activation, and markedly reduced TNF-α, IL-1β, and prostaglandin E2 (PGE₂) levels. They also inhibited hind paw edema induced by carrageenan. Eupatilin and jaceosidin had similar activity.

Conclusions

These findings suggest that eupatilin and jaceosidin may reduce inflammation by inhibiting NF-κB activation, and that Artemisia princeps inhibits inflammation because of these constituents.     

Anti-inflammatory and analgesic activity of aqueous extract of Flos populi

Ethnopharmacological relevance

Flos populi is an important traditional Chinese medicine prepared from the male inflorescence of Populus tomentosa Carr. or Populus canadensis Moench (Salicaceae family). Flos populi is mainly used for the treatment of various inflammatory diseases and anti diarrhea in East Asian countries. The objective of this study was to investigate the anti-inflammatory and analgesic properties of the aqueous extract of Flos populi (FPAE).

Materials and methods

Cotton pellets-induced granuloma, carrageenan-induced paw oedema, arachidonic acid-induced right ear oedema and xylene-induced ear oedema were used to assess anti-inflammatory activity of FPAE and analgesic activity was evaluated by hot plate test, acetic acid-induced abdominal writhing test and formalin test.

Results

FPAE produced significant dose–response anti-inflammatory activity against cotton pellets-induced granuloma. FPAE at dosages of 50, 100 and 200 mg/kg b w. significantly reduced carrageenan-induced paw edema by 48.84% (P<0.05), 54.95% (P<0.05), and 62.05% (P<0.05) at 5 h after carrageenan injection, respectively. FPAE significantly (P<0.05) reduced the ear oedema induced by arachidonic acid and peaked at the dose of 200 mg/kg b w. (40.78%). A significant (P<0.05) dose dependent inhibition of xylene-induced oedema was produced by FPAE and peaked at the highest dose of 200 mg/kg b w. (23.95%). FPAE (50, 100 and 200 mg/kg b w.) produced significant dose–response analgesic activity in the hot-plate test. However, the low percentage inhibition (<50%) suggests that it is not a centrally acting analgesic. Extract at dosages of 50, 100 and 200 mg/kg b w., p.o. significantly reduced acetic acid-induced writhing by 39.6% (P<0.05), 45.4% (P<0.05), and 51.8% (P<0.05), respectively. The extract also caused marked dose-dependent inhibition of formalin-induced pain in the second phase (P<0.05).

Conclusion

The findings in this study suggest that the aqueous extract of Flos populi possesses anti-inflammatory and analgesic activities. These results may support the fact that this plant is used traditionally to cure inflammatory diseases.     

In vivo anti-inflammatory and antinociceptive actions of some Lamium species

ETHNOPHARMACOLOGICAL RELEVANCE: Several Lamium species have been used to relieve pain in arthritic ailments in Turkish folk medicine. AIM OF THE STUDY: To evaluate the anti-inflammatory and antinociceptive activities of different extracts prepared with methanol, dichloromethane, n-butanol and water from the aerial parts of some Lamium species of Turkish origin. MATERIALS AND METHODS: Lamium eriocephalum subsp. eriocephalum, Lamium garganicum subsp. laevigatum, Lamium garganicum subsp. pulchrum and Lamium purpureum var. purpureum (Lamiaceae); for the anti-inflammatory activity, carrageenan-induced hind paw edema model, PGE(2)-induced hind paw edema model, and 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema model and for the antinociceptive activity p-benzoquinone (PBQ)-induced writhing test in mice were employed. RESULTS: The n-butanol extracts of Lamium garganicum subsp. laevigatum (LGL-BuOH), Lamium garganicum subsp. pulchrum (LGP-BuOH), and Lamium purpureum var. purpureum (LPP-BuOH) exhibited notable inhibition (16.5-28.9, 14.5-26.9, 12.3-21.5%, resp.) in carrageenan-induced hind paw edema model at doses of 200mg/kg without inducing any gastric damage. The LGL-BuOH (7.1-30.4%) and LGP-BuOH (5.9-24.1%) extracts also displayed potent anti-inflammatory activity against PGE(2)-induced hind paw edema model. LGL-BuOH and LGP-BuOH were also found to exhibit remarkable antinociceptive activity in p-benzoquinone-induced abdominal constriction test at a dose of 200 mg/kg (25.0 and 24.3%, respectively). CONCLUSION: The experimental data demonstrated that Lamium garganicum subsp. laevigatum and Lamium garganicum subsp. pulchrum displayed remarkable anti-inflammatory and antinociceptive activities.     

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.     

β Mangostin suppress LPS-induced inflammatory response in RAW 264.7 macrophages in vitro and carrageenan-induced peritonitis in vivo

Ethnopharmacological relevance

The fruit hull of Garcinia mangostana Linn. has been used in traditional medicine for treatment of various inflammatory diseases. Hence, this study aims to investigate the in vitro and in vivo anti-inflammatory effect of β mangostin (βM), a major compound present in Garcinia mangostana.

Materials and methods

The in silico analysis of inflammatory mediators such as cyclooxygenase (COX) and nuclear factor-kappa B (NF-kB) were performed via molecular docking. Further evaluation of anti-inflammatory effect was conducted in lipopolysaccharide (LPS) induced RAW 264.7 macrophages. Suppression of activated NF-kB was analyzed by high content screening. βM triggered inhibition of COX-1 and COX-2 in vitro were studied using biochemical kit. The in vivo model used in this study was carrageenan-induced peritonitis model, where reduction in carrageenan-induced peritonitis is measured by leukocyte migration and vascular permeability. In addition, the evaluation of βM?s effect on carrageenan induced TNF-α and IL-1β release on peritoneal fluid was also carried out.

Results

Treatment with βM could inhibit the LPS-induced NO production but not the viability of RAW 264.7. Similarly, βM inhibited PGE₂ production and the cytokines: TNF-α and IL-6. The COX catalyzed prostaglandin biosynthesis assay had showed selective COX-2 inhibition with a 53.0±6.01% inhibition at 20 µg/ml. Apart from this, βM was capable in repressing translocation of NF-kB into the nucleus. These results were concurrent with molecular docking which revealed COX-2 selectivity and NF-kB inhibition. The in vivo analysis showed that after four hours of peritonitis, βM was unable to reduce vascular permeability, yet could decrease the total leukocyte migration; particularly, neutrophils. Meanwhile, dexamethasone 0.5 mg/kg, successfully reduced vascular permeability. The levels of TNF-α and IL-1β in peritoneal fluid was reduced significantly by βM treatment.

Conclusion

The current study supports the traditional use of Garcinia mangostana fruit hull for treatment of inflammatory conditions. In addition, it is clear that the anti-inflammatory efficacy of this plant is not limited to the presence of α and γ, but β also with significant activity.     

Anti-inflammatory and antinociceptive activities of extract, fractions and populnoic acid from bark wood of Austroplenckia populnea

Austroplenckia populnea (Reiss) Lund is a Brazilian plant from "cerrado", which belongs to Celastraceae family, popularity know as "marmelinho-do campo, mangabeira-brava, mangabarana, vime and maria-mole". This plant is used in folk medicine to treat dysenteries and inflammatory disorders, such as rheumatism. Austroplenckia populnea bark hydroalcoholic crude extract, and its hexane, chloroform and ethyl acetate fractions, obtained by partition, as well as the isolated populnoic acid were investigated for their anti-inflammatory (carrageenan, dextran and histamine-induced rat paw oedema, histamine-induced increase in vascular permeability, and granulomatous tissue induction) and analgesic activities (writhing and hot plate tests). The ED(50) (oral) of the crude extract for the inhibition of carragenan-induced rat paw oedema assay was determined to be 200 mg/kg, which was also used in the assays with the extract and its fractions in all other experiments. Populnoic acid was administered in the dose of 50 mg/kg. Crude extract, hexane and chloroform fractions (200 mg/kg), and indomethacin (10 mg/kg) inhibited significantly (p<0.05) the formation of the carrageenan-induced rat paw oedema, measured in third hour of experiment (peak of oedema formation) by 43.2%, 37.3%, 31.1% and 59.3%, respectively. There was a significant reduction (p<0.05) in dextran-induced rat paw oedema in all groups, while in the assay using histamine as the oedematogenic agent, only the groups treated with populnoic acid (50 mg/kg) and cyproheptadine (10 mg/kg) displayed significant reduction (p<0.05). The populnoic acid and cyproheptadine reduced the peak of oedema formation (1st hour) by 41.3% and 34.7%, respectively. Only for the groups treated with populnoic acid (50 mg/kg) and cyproheptadine (10 mg/kg) it was observed a significant (p<0.05) reduction in histamine-induced increase in vascular permeability (44.8% and 80.3%, respectively). Granulomatous tissue formation was significantly inhibited (p<0.05) by both hexane fraction (46.0%) and dexamethasone (66.2%). In the analgesic assays, the crude extract and its hexane and chloroform fractions, as well as indomethacin diminished significantly the number of writhings (p<0.05) by 69.6%, 47.2%, 44.8% and 62.8%, respectively. On the other hand, none assayed sample displayed significant result in the hot plate test. Based on the obtained results it is suggested that extracts of Austroplenckia populnea bark and populnoic acid display anti-inflammatory activity, supporting its folkloric use to treat inflammatory disorders.