Ethnopharmacological evaluation of some Scorzonera species: in vivo anti-inflammatory and antinociceptive effects

Ethnopharmacological relevance

Scorzonera species are mainly used against inflammation and to relieve pain in Turkish traditional medicine. Therefore, we aimed to assess in vivo anti-inflammatory and antinociceptive activities of the aerial part and root extracts of Scorzonera acuminata, Scorzonera cana var. alpina, Scorzonera cana var. jacquiniana, Scorzonera cana var. radicosa, Scorzonera cinerea, Scorzonera eriophora, Scorzonera incisa, Scorzonera laciniata ssp. laciniata, Scorzonera parviflora and Scorzonera sublanata.

Materials and methods

For the anti-inflammatory activity evaluation carrageenan, PGE₂ and serotonin-induced hind paw edema and 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema models were used. p-Benzoquinone-induced abdominal constriction test was employed in mice for the assessment of antinociceptive activity. Furthermore chemical composition of the tested extracts was investigated qualitatively and quantitatively by using RP-HPLC method. Some phenolic acids and flavonoids were used as standards.

Results

Extracts prepared from the aerial parts of Scorzonera cana var. jacquiniana, Scorzonera cinerea, Scorzonera eriophora, Scorzonera incisa and Scorzonera parviflora showed significant inhibitory effect on carrageenan and PGE₂-induced hind paw edema model as well as on p-benzoquinone-induced abdominal constriction test. The extracts did not show any remarkable activity on serotonin-induced hind paw edema and TPA-induced mouse ear edema models. Chlorogenic acid was detected as major compounds in all the species investigated. Additionally, among the tested flavonoids, luteolin-7-glucoside, hyperoside and rutin were found to be in different amounts in Scorzonera species.

Conclusion

The experimental data revealed that Scorzonera cana var. jacquiniana, Scorzonera cinerea, Scorzonera eriophora, Scorzonera incisa and Scorzonera parviflora possess significant anti-inflammatory and antinociceptive activity. It has been suggested that flavonoids and chlorogenic acid are partly responsible for mentioned activities of Scorzonera species.     

Valuation of anti-inflammatory and antinociceptive activities of Erica species native to Turkey

Erica L. species (Ericaceae) have been popularly used as antirheumatic, diuretic, astringent and treatment of urinary infections. In order to evaluate this information, anti-inflammatory and antinociceptive activities of different extracts prepared with methanol, chloroform, ethyl acetate, n-butanol and water from the aerial parts of Erica arborea L., Erica manipuliflora Salisb., Erica bocquetii (Pe?men) P.F. Stevens and Erica sicula Guss. subsp. libanotica (C.&;W. Barbey) P.F. Stevens (Ericaceae) of Turkish origin were investigated by using in vivo methods. For the anti-inflammatory activity, carrageenan-induced hind paw edema model, PGE₂-induced hind paw edema model, and 12-O-tetradecanoyl-13-acetate (TPA)-induced mouse ear edema model and for the antinociceptive activity p-benzoquinone-induced writhing test in mice were employed. The ethyl acetate extracts of Erica arborea (EAE), Erica bocquetii (EBE) and Erica manipuliflora (EME) exhibited notable inhibition against carrageenan-induced (24.1–32.3%, 23.8–36.1%, 29.2–35.1%, respectively) and PGE₂-induced (21.2–37.7%, 6.8–29.7%, and 6.2–34.1%, respectively) hind paw edema as well as TPA-induced mouse ear edema models in mice, while the ethyl acetate extract of Erica sicula subsp. libanotica (ESE) (10.7–29.7%) displayed potent anti-inflammatory activity only on the PGE₂-induced hind paw edema model. However, the remaining extracts were found to be inactive against inflammatory models. Same extracts, i.e., EAE, EBE and EME were also found to exhibit remarkable antinociceptive activity in p-benzoquinone-induced abdominal constriction test at a dose of 100 mg/kg (46.5%, 27.7% and 36.3%, respectively).     

In vivo anti-inflammatory and antinociceptive activity of the crude extract and fractions from Rosa canina L. fruits

The aqueous and ethanol extracts of Rosa canina L. (Rosaceae) fruits and the fractions prepared from the latter were investigated for their anti-inflammatory and antinociceptive activities in several in vivo experimental models. The ethanolic extract was shown to possess significant inhibitory activity against inflammatory models (i.e., carrageenan-induced and PGE(1)-induced hind paw edema models, as well as on acetic acid-induced increase in a capillary permeability model) and on a pain model based on the inhibition of p-benzoquinone-induced writhing in mice. Hexane, chloroform, ethylacetate, n-butanol and the remaining water fractions were obtained through bioassay-guided fractionation. Ethylacetate and n-butanol fractions displayed potent anti-inflammatory and antinociceptive activities at a dose of 919 mg/kg without inducing acute toxicity. Further attempts to isolate and define the active constituent(s) were inconclusive, possibly due to the synergistic interaction of components in the extract.     

Estimation of antinociceptive and anti-inflammatory activity on Geranium pratense subsp. finitimum and its phenolic compounds

To obtain experimental evidence on the therapeutic efficacy of Geranium species and its phenolic compounds for inflammatory diseases, we examined the effects of the aqueous extract of the aerial parts of Geranium pratense subsp. finitimum (Woronow) Knuth, its fractions and isolated compounds, the mixture of quercetin 3-O-alpha-arabinopyranoside, kaempferol 3-O-beta-galactopyranoside (1), the mixture of quercetin 3-O-beta-glucopyranoside, quercetin 3-O-beta-galactopyranoside (2), kaempferol 3-O-beta-glucopyranoside (3), (-)-6-chloroepicatechin (4), the mixture of quercetin 3-O-(2'-O-galloyl)-beta-glucopyranoside, quercetin 3-O-(2'-O-galloyl)-beta-galactopyranoside (5) and myricetin 3-O-(2'-O-galloyl)-beta-glucopyranoside (6), on carrageenan-, PGE(2)- and TPA-induced inflammation in mice and p-benzoquinone-induced writhing reflex to assess anti-inflammatory and antinociceptive activities. The effective dose of materials for the inhibition of carragenan-induced hind paw edema assay was determined to be 100 mg/kg, which was also used in the assays with the extract, its fractions and isolated compounds in all other experiments. The aqueous extract, 1, 2 (100 mg/kg), as well as indomethacin (10 mg/kg) inhibited significantly the formation of the carrageenan-induced hind paw edema. There was also a significant reduction in PGE(2)-induced hind paw edema and TPA-induced ear edema models with 5, in addition to the aqueous extract and the other active components 1 and 2. In the antinociceptive assay, the aqueous extract and its fractions, as well as 1, 2, and 5 diminished significantly the number of writhings. Based on the results obtained it is suggested that the aqueous extract of Geranium pratense subsp. finitimum and its phenolic compounds display anti-inflammatory activity, supporting the folkloric use.     

Investigation of the in vitro and ex vivo acetylcholinesterase and antioxidant activities of traditionally used Lycopodium species from South America on alkaloid extracts

Ethnopharmacological relevance

The study was aimed at evaluating medicinal and therapeutic potentials of two Lycopodiaceae species, Lycopodium clavatum (L.) and Lycopodium thyoides (Humb. & Bonpl. ex Willd), both used in South American folk medicine for central nervous system conditions. Alkaloid extracts were evaluated for chemical characterization, acetylcholinesterase and antioxidant activities.

Materials and methods

The alkaloid extracts obtained by alkaline extraction were determined for each species by GC/MS examination. The evaluation of the anticholinesterase and the antioxidant activities of the extracts were tested by determining in vitro and ex vivo models. Effects on acetylcholinesterase (AChE) were tested in vitro using rat brain homogenates and ex vivo after a single administration (25, 10 and 1 mg/kg i.p.) of the alkaloid extracts in mice. The in vitro antioxidant effects were tested for the 2-deoxyribose degradation, nitric oxide (NO) interaction, 2,2-diphenyl-1-picryl hydrazyl (DPPH) radical scavenging activity and total reactive antioxidant potential (TRAP). After an acute administration (25 and 10 mg/kg i.p.) of the extracts in middle-aged (12 months) mice, the antioxidant effects were estimated through the thiobarbituric acid reactive substances test (TBARS), and the antioxidant enzymes activities for catalase (CAT) and superoxide dismutase (SOD) were measured.

Results

AChE activity was inhibited in vitro by the alkaloid-enriched extracts of both Lycopodium species in a dose and time-dependent manner in rat cortex, striatum and hippocampus. A significant inhibition was also observed in areas of the brain after acute administration of extracts, as well as decreased lipid peroxidation and increased CAT activity in the cortex, hippocampus and cerebellum. A moderate antioxidant activity was observed in vitro for the extracts. Chemically, the main alkaloids found for the two species were lycopodine and acetyldihidrolycopodine.

Conclusion

This study showed that the biological properties of the folk medicinal plants Lycopodium clavatum and Lycopodium thyoides include AChE inhibitory activity and antioxidant effects, two possible mechanisms of action in Alzheimer's related processes.     

Phytosynergy in some Hypoxis species and pharmacological properties of a Hypoxis-based phytopharmaceutical formula

Ethnopharmacology relevance

Hypoxis species are used extensively in traditional medicine in southern Africa for several ailments including tuberculosis, chest infections, and nervous and urinary disorders. Several other claims have been made for extracts emanating from Hypoxis species and have led to the production of several commercial products used as immunostimulants mostly for people living with HIV/AIDS and cancer. This study was aimed at investigating the biological activity of four Hypoxis species and a commercial herbal product, ‘African potato extract’ (APE).

Materials and methods

Antibacterial, antifungal, cyclooxygenase (COX) and acetylcholineasterase (AChE) inhibitory activities of four Hypoxis species (H. acuminata, H. colchicifolia, H. hemerocallidea and H. rigidula) and a popular Hypoxis-based herbal preparation, APE were tested. The phytoconstituents of the mixture were also profiled using TLC methods. Several combinations of the Hypoxis species were prepared and their synergism, additive, autonomic and antagonism effects investigated. As a quality control measure, batch to batch comparison in the phytoconstituents and biological activity of APE was carried out.

Results

The results confirmed H. colchicifolia and H. hemerocallidea as the phytoconstituents of APE. The extracts showed a broad spectrum of activities against the bacterial and fungal strains used. Of particular interest were the activities exhibited by the APE and combinations of H. colchicifolia and H. hemerocallidea. The APE mixture exhibited good antibacterial activity (MIC values of 0.78 mg/ml each) in all the tested batches against the bacterial strains used. The water extracts of all four Hypoxis species, three batches of APE and the combination (water extracts) of H. colchicifolia and H. hemerocallidea exhibited high COX-1 and moderate COX-2 inhibitory activity except for H. acuminata which showed low activity against COX-2. All the extract, batches of APE and combinations showed low to moderate AChE inhibitory activity. These results provided some evidence of phytosynergy in some extracts of H. hemerocallidea and H. colchicifolia except for a few extracts which act as additive, autonomous and antagonistic when used to inhibit some bacterial and fungal strains. However, this was not the case for COX and AChE inhibition, as only acetone extracts acted in a synergistic way to reduce the activity of the enzyme.

Conclusion

Even though the results give an indication of a positive interaction between some extracts of H. hemerocallidea and H. colchicifolia, the study was carried out on 1:1 v/v combinations only. It is therefore important to carry out isobologram studies, which considers more than one ratio of the combinations.     

In vivo anti-nociceptive and anti-inflammatory activities of the aqueous extract of the leaves of Piper sarmentosum

Ethnopharmacological relevance

Piper sarmentosum (Piperaceae) is a medicinal plant traditionally used by the Malays to treat headaches, toothaches, coughs, asthma and fever.

Aim of the study

In order to establish the pharmacological properties of the leaf of this plant, studies were performed on anti-nociceptive and anti-inflammatory activities.

Materials and methods

The aqueous extract of Piper sarmentosum (AEPS) was prepared in the doses of 30, 100 and 300 mg/kg. Anti-nociceptive activity of AEPS was evaluated by abdominal constriction and hot-plate tests. AEPS was also pre-challenged with 5 mg/kg naloxone to determine the involvement of opioid receptors. Anti-inflammatory activity was evaluated using carrageenan-induced paw edema assay.

Results

Subcutaneous administration of AEPS exhibited anti-nociceptive activity (P < 0.05) in a dose-dependent manner in the abdominal constriction and hot-plate tests. Pre-treatment with naloxone completely (P < 0.05) diminished the extract anti-nociceptive activity in both tests. The AEPS, at all doses used, exerted significant (P < 0.05) anti-inflammatory activity in a dose-dependent manner.

Conclusions

The AEPS exhibits opioid-mediated anti-nociceptive activity at the peripheral and central levels, as well as anti-inflammatory activity, which confirmed the traditional uses of the plant in the treatment of pain- and inflammatory-related ailments.     

The anti-inflammatory activities of an extract and compounds isolated from Platycladus orientalis (Linnaeus) Franco in vitro and ex vivo

Ethnopharmacological relevance

As a Chinese traditional herbal medicine, leaves of Platycladus orientalis (Linnaeus) Franco (LPO) are used to treat coughs, excessive mucus secretion, chronic bronchitis, bronchiectasis, and asthma, etc. The experiments were carried out to investigate their anti-inflammatory properties and mechanisms, which could support the Chinese traditional uses of treating inflammatory airway diseases.

Materials and methods

The anti-inflammatory activities of the chloroform fraction (CHL) and pure compounds of LPO were evaluated for their abilities to inhibit pro-inflammatory enzymes in vitro, and production of tumor necrosis factor-α (TNF-α) and nitric oxide in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Furthermore, the arachidonic acid metabolites, stimulated by calcium ionophore A23187, were also determined by HPLC.

Results

For the first time, the assays of eicosanoids in intact cells showed that the CHL, hinokiol, and acacetin had significant inhibitory effects on 5-hydroxy-eicosa-tetra-enoic acid (5-HETE) and leukotriene B₄ (LTB4) formations. And cell-free enzyme assays (5-lipoxygenase, leukotriene A₄-hydrolase, cyclooxgenase-2) demonstrated the potent inhibitory effects of the CHL, hinokiol and acacetin on 5-lipoxygenase (5-LOX). Then, the inhibitions of the CHL, hinokiol on NO biosynthesis and the inhibitions of the CHL, 8(14),15-pimaradien-3β,18-diol, and hinokiol on TNF-α release were also confirmed in the RAW264.7 murine macrophages.

Conclusion

The data indicate that the inhibitory effects of the CHL and its components (hinokiol and acacetin) on 5-LOX contribute to the anti-inflammatory activity of LPO. Moreover, the CHL and its components also show beneficial effects on NO and TNF-α production. Consequently, these results provide a rationale for LPO's traditional applications in the treatment of inflammatory airway diseases.     

Bioactivity guided evaluation of anti-inflammatory and antinociceptive activities of Arceuthobium oxycedri (D.C.) M. Bieb.

Ethnopharmacological relevance

Arceuthobium oxycedri (D.C.) M. Bieb. (Loranthaceae) or dwarf mistletoe is a rare semi-parasitic plant that lives on the branches of Juniperus oxycedrus as the host plant. In Turkish folk medicine, the plant is prescribed as a panacea for every kind of diseases, including, against infectious and inflammatory disorders of upper respiratory system and gastro-intestinal complaints or as a hypotensive remedy.

Aim of the study

In the current study, in vivo anti-inflammatory and antinociceptive effects of Arceuthobium oxycedri have been investigated.

Material and methods

The crude ethanolic extract of the whole 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 subextract, i.e. the EtOAc subextract, was further subjected to fractionation through successive column chromatographic applications on Silica gel 60, Sephadex LH-20 and LiChropep RP-18. For the activity assessment, each extract or fraction was submitted to bioassay systems; carrageenan-induced hind paw edema model for anti-inflammatory activity and p-benzoquinone induced abdominal contraction test for antinociceptive activity assessment.

Results

Among the extracts obtained, the ethanolic extract, EtOAc and n-butanol subextracts showed significant inhibitory activity in the bioassay systems. From the EtOAc subextract, a major component was isolated and its structure was determined as (+)-catechin by means of spectral techniques.

Conclusion

Present study confirms the claimed utilization of the plant against inflammatory complaints in Turkish folk medicine.     

Evaluation of antinociceptive effects of Crassocephalum bauchiense Hutch (Asteraceae) leaf extract in rodents

Ethnopharmacological relevance

The leaves of Crassocephalum bauchiense have long been used in traditional Cameroonian medicine for the treatment of epilepsy, pain, inflammatory disorders, arthritis and intestinal pain.

Aim of the study

In this study, we attempted to identify the possible antinociceptive action of the aqueous extract and the alkaloid fraction prepared from the leaves of Crassocephalum baucheiense.

Materials and methods

Using acetic acid induced abdominal constrictions, formalin-, capsaisin- and glutamate-induced nociception, and hot plate assay procedures, the antinociceptive effects of the aqueous extract and the alkaloid fraction was assessed after oral administration in mice. Morphine sulfate was used as reference analgesic agent. Mice were submitted to the rota-rod task and open-field test in order to assess any non-specific muscle-relaxant or sedative effects of the extracts of Crassocephalum bauchiense. Male and female Swiss mice were used to assess acute toxicity of these extracts.

Results

The aqueous extract and the alkaloid fraction of Crassocephalum bauchiense produced a significant antinociceptive effects in the acetic acid, formalin, glutamate, capsaicin and hot plate tests. These antinociceptive effects of Crassocephalum bauchiense were significantly attenuated by pretreatment with naloxone. The extracts of Crassocephalum bauchiense did not alter the locomotion of animals in the open-field or rotarod tests, which suggest a lack of a central depressant effect. The animals did not exhibit any acute toxicity to the aqueous extract and the alkaloid fraction, so it was not possible to calculate the LD₅₀.

Conclusion

The results confirm the popular use of Crassocephalum bauchiense as an antinociceptive, and contribute to the pharmacological knowledge of this species because it was shown that the aqueous extract and the alkaloid fraction of Crassocephalum bauchiense produced dose related antinociception in models of chemical and thermal nociception through mechanisms that involve an interaction with opioidergic pathway.     

Evaluation of the antinociceptive, anti-inflammatory and gastric antiulcer activities of the essential oil from Piper aleyreanum C.DC in rodents

Ethnopharmacological relevance

Piper aleyreanum is a small tree that is widely distributed in tropical and subtropical regions, mostly in North and South America, and is used as an immunomodulator, analgesic and antidepressant in folk medicine.

Aim of the study

This study was designed to investigate the antinociceptive, anti-inflammatory and gastric antiulcer activities of the essential oils from the aerial parts of Piper aleyreanum (EOPa) in rodents.

Materials and methods

The antinociceptive and anti-inflammatory effects of orally administered EOPa were evaluated in mice subjected to the formalin and pleurisy models, respectively. We also pretreated the rats with EOPa before acute ethanol-induced gastric lesions and measured gastric lesion extension and mucus and glutathione (GSH) levels in the gastric mucosa. Finally, we performed a phytochemical analysis of EOPa.

Results

The chemical composition of EOPa was analyzed by gas chromatography and mass spectrometry (GC/MS), which identified 35 compounds, representing 81.7% of total oil compounds. Caryophyllene oxide (11.5%), β-pinene (9%), spathulenol (6.7%), camphene (5.2%), β-elemene (4.7%), myrtenal (4.2%), verbenone (3.3%) and pinocarvone (3.1%) were the major oil constituents. The oral administration of EOPa (10–1000 mg/kg) significantly inhibited the neurogenic and inflammatory phases of formalin-induced licking, with ID50 values of 281.2 and 70.5 mg/kg, respectively. The antinociception caused by EOPa (100 mg/kg, p.o.) was not reversed by naloxone (1 or 5 mg/kg, i.p.) in the formalin test. EOPa (100–300 mg/kg, p.o.) did not affect animal motor coordination in an open-field model. In carrageenan-induced pleurisy, EOPa (1–100 mg/kg, p.o.) significantly decreased the total cell count, neutrophils and mononuclear cells with mean ID50 values of 53.6, 21.7 and 43.5 mg/kg, respectively. In addition, EOPa (1–30 mg/kg, p.o.) protected the rats against ethanol-induced gastric lesions with an ID50 value of 1.7 mg/kg and increased the mucus and GSH levels of the gastric mucosa to levels similar to those of the non-lesioned group.

Conclusions

These data show for the first time that EOPa has significant antinociceptive and anti-inflammatory actions, which do not appear to be related to the opioid system. EOPa also has interesting gastroprotective effects related to the maintenance of protective factors, such as mucus production and GSH. These results support the widespread use of Piper aleyreanum in popular medicine and demonstrate that this plant has therapeutic potential for the development of phytomedicines with antinociceptive, anti-inflammatory and gastroprotective properties.     

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.     

Mechanisms underlying the antidiarrheal,antispasmodic and bronchodilator activities of Fumaria parviflora and involvement of tissue and species specificity

Ethnopharmacological relevance: In the Greco-Arab (Unani) traditional medicine, Fumaria parviflora Linn. is widely used in hypreractive gut and respiratory disorders including diarrhea, abdominal cramps, indigestion and asthma but scientific studies to provide rational for these medicinal uses are sparse. This study was therefore undertaken to provide ethnopharmacological basis for its medicinal use in diarrhea, abdominal cramps and asthma.     

Analgesic, anti-inflammatory and antioxidant properties of Buddleja globosa, Buddlejaceae

ETHNOPHARMACOLOGICAL RELEVANCE: Buddleja globosa, known as "matico", is employed in Chile for wound healing. AIM OF THE STUDY: To validate the traditional use of the crude drug through in vivo and in vitro evaluation of the anti-inflammatory, analgesic and antioxidant properties of its extracts. MATERIALS AND METHODS: Sequential hexane, dichloromethane, methanol and total methanol extracts were studied using bioguided fractionation. The following activities were investigated: analgesic (writhing test), oral and topic anti-inflammatory (paw- and ear-induced edema), free radical scavenging and antioxidant activities (1,1-diphenyl-2-picrylhydrazyl, DPPH, superoxide anion, lipid peroxidation and xanthine oxidase inhibition). Sodium naproxen, nimesulide, indomethacin were used as reference drugs for in vivo, quercetin and allopurinol for in vitro assays. RESULTS: A mixture of alpha- and beta-amyrins was isolated from the hexane extract that showed 41.2% of analgesic effect at 600 mg/kg, inhibited by 47.7 and 79.0% the arachidonic acid (AA) and 12-deoxyphorbol-13-decanoate (TPA)-induced inflammation at 3mg/20 microL/ear, respectively. A mixture of beta-sitosterol, stigmasterol, stigmastenol, stigmastanol and campesterol was isolated from the fraction CD4-N and beta-sitosterol-glycoside from the fraction CD5-N, reducing TPA-induced inflammation by 78.2 and 83.7% at 1mg/20 microL/ear, respectively. The fraction CD4-N at 300 mg/kg also showed analgesic activity (38.7%). The methanol extract at 600mg/kg per os showed anti-inflammatory effect (61.4%), topic anti-inflammatory (56.7% on TPA) and analgesic activity (38.5%). Verbascoside and luteolin-7-O-glucoside were the major components of the methanol extract; apigenin 7-O-glucoside was also detected. Inhibition of superoxide anion, lipoperoxidation, and DPPH bleaching effect was found in the methanol serial and global extracts. CONCLUSIONS: The present report demonstrate the analgesic and anti-inflammatory properties of Buddleja globosa and validate its use in Chilean traditional medicine.     

Evidence of anti-inflammatory effects of Passiflora edulis in an inflammation model

The popular medicine Passiflora edulis has been used as a sedative, tranquilizer, against cutaneous inflammatory diseases and intermittent fever. Most of the pharmacological investigations of Passiflora edulis have been addressed to its Central Nervous System activities, such as anxiolytic, anticonvulsant and sedative actions. Otherwise, there are few reports about the anti-inflammatory activity of the Passiflora species. The aim of this study was to investigate the mechanism of the anti-inflammatory effect of aqueous lyophilized extract obtained from leaves of Passiflora edulis var. flavicarpa Degener (Passifloraceae) in the mouse model of pleurisy induced by carrageenan (Cg), bradykinin, histamine or substance P, observing the effects upon leucocytes migration, myeloperoxidase (MPO), nitric oxide (NO) concentrations and tumor necrosis factor-alpha (TNFalpha) and interleukin-1 beta (IL-1beta) levels. RESULTS: Passiflora edulis (250mg/kg) administered by intraperitoneal route (i.p.) inhibited the leukocyte, neutrophils, myeloperoxidase, nitric oxide, TNFalpha and IL-1beta levels (P<0.01) in the pleurisy induced by carrageenan. Passiflora edulis (250-500mg/kg, i.p.) also inhibited total and differential leukocytes in the pleurisy induced by bradykinin, histamine or substance P (P<0.05). CONCLUSION: Several mechanisms, including the inhibition of pro-inflammatory cytokines (TNFalpha, IL-1beta), enzyme (myeloperoxidase) and mediators (bradykinin, histamine, substance P, nitric oxide) release and/or action, appear to account for Passiflora edulis's actions.     

The absorption characterization effects and mechanism of Radix Angelicae dahuricae extracts on baicalin in Radix Scutellariae using in vivo and in vitro absorption models

Ethnopharmacological relevance

Angelicae Dahurica(Hoffm.)Benth.&Hook.f.ex Franch.&Sav combined with Scutellaria baicalensis Georgi. has been widely used as herb-pairs in traditional Chinese medicine (TCM) to treat migraine headache and cataract, but the underlying compatibility mechanism of the two herbs remains unknown.

Aim of study

In the present work, we investigated the additive or synergistic effects of absorption behavior of Radix Angelicae dahuricae extracts on baicalin, and the absorption-enhancing mechanism of Radix Angelicae dahuricae extracts on baicalin.

Materials and methods

Total coumarins (Cou) and volatile oil (VO), as the two main components of Radix Angelicae dahuricae, were extracted by supercritical fluid extraction (SFE) further treated with liquid-liquid separation method. The absorption behavior was investigated by applying the everted gut sac technique and in situ single-pass intestinal perfusion method.

Results and conclusions

The results showed that both the Cou and the VO could improve the intestinal absorption of baicalin in vivo, and had synergistic action the enhanced absorption of baicalin. Since verapamil did not affect the P_app and K_a of baicalin significantly, we concluded that the absorption of Baicalin could not be an active transportation in dependent of P-glycoprotein-Mediated efflux systems. Based on intestinal absorption of drug studying was one of the efficacious methods to clarify the compatibility of principles of herb-pairs. The everted gut sac technique and in situ single-pass intestinal perfusion technique model were the effective methods to study the absorption of drug, the application of the animal model to investigating the absorption of herb-drug interactions or other relevant research purposes is envisioned.     

In vitro and in vivo anti-inflammatory effects of taheebo, a water extract from the inner bark of Tabebuia avellanedae

AIM OF STUDY: Tabebuia spp. (Bignoniaceae) are native to tropical rain forests throughout Central and South America and have long been used as a folk medicine to treat bacterial infection, blood coagulation, cancer and inflammatory diseases. In this study, we aimed to demonstrate the ethnopharmacological activity of Tabebuia avellanedae in various in vitro and in vivo inflammatory conditions. MATERIALS AND METHODS: To do this, LPS-stimulated macrophages and arachidonic acid or croton oil-induced mouse ear edema models were employed. RESULTS: The water extract (taheebo) of Tabebuia avellanedae significantly suppressed the production of prostaglandin (PG) E(2) and nitric oxide (NO), and blocked the mRNA expression of their catalyzing enzymes (cyclooxygenase [COX)-II] and inducible NO synthase [iNOS], respectively), in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. The blockade of inflammatory mediators by taheebo seemed to be the result of the interruption of extracellular signal-related kinase (ERK) activation, according to immunoblotting analysis and the NO assay, where LPS strongly induced the phosphorylation (a hallmark of activation) of ERK, and U0126, a selective ERK inhibitor, was found to strongly inhibit PGE(2) production. Similarly, oral administration of taheebo (100mg/kg) for 1 week completely diminished mouse ear edema induced by arachidonic acid, an activator of COX-II, but not croton oil, an activator of lipoxygenase. CONCLUSIONS: These data suggest that the ethnopharmacological action of taheebo may be due to its negative modulation of macrophage-mediated inflammatory responses by suppressing PGE(2) production. Thus, this water extract may be developed as a new therapeutic remedy for various inflammatory diseases such as arthritis and atherosclerosis.     

Pharmacological actions of the South African medicinal and functional food plant Sceletium tortuosum and its principal alkaloids

Ethnopharmacological relevance

The South African plant Sceletium tortuosum has been known for centuries for a variety of traditional uses, and, more recently, as a possible source of anti-anxiety or anti-depressant effects. A standardised extract Zembrin^® was used to test for pharmacological activities that might be relevant to the ethnopharmacological uses, and three of the main alkaloids were also tested.

Materials and methods

A standardised ethanolic extract was prepared from dried plant material, along with the purified alkaloids mesembrine, mesembrenone and mesembrenol. These were tested on a panel of receptors, enzymes and other drug targets, and for cytotoxic effects on mammalian cells.

Results

The extract was a potent blocker in 5-HT transporter binding assays (IC₅₀ 4.3 μg/ml) and had powerful inhibitory effects on phosphodiesterase 4 (PDE4) (IC₅₀ 8.5 μg/ml), but not other phosphodiesterases. There were no cytotoxic effects. Mesembrine was the most active alkaloid against the 5-HT transporter (K_i 1.4 nM), while mesembrenone was active against the 5-HT transporter and PDE4 (IC₅₀'s < 1 μM).

Conclusions

The activity of the Sceletium tortuosum extract on the 5-HT transporter and PDE4 may explain the clinical effects of preparations made from this plant. The activities relate to the presence of alkaloids, particularly mesembrine and mesembrenone.     

Comparative antioxidant and anti-inflammatory effects of [6]-gingerol, [8]-gingerol, [10]-gingerol and [6]-shogaol

Ethnopharmacological relevance

Zingiber officinale Rosc. (Zingiberaceae) has been traditionally used in Ayurvedic, Chinese and Tibb-Unani herbal medicines for the treatment of various illnesses that involve inflammation and which are caused by oxidative stress. Although gingerols and shogaols are the major bioactive compounds present in Zingiber officinale, their molecular mechanisms of actions and the relationship between their structural features and the activity have not been well studied.

Aim of the study

The aim of the present study was to examine and compare the antioxidant and anti-inflammatory activities of gingerols and their natural analogues to determine their structure–activity relationship and molecular mechanisms.

Materials and methods

The in vitro activities of the compounds [6]-gingerol, [8]-gingerol, [10]-gingerol and [6]-shogaol were evaluated for scavenging of 1,1-diphenyl-2-picyrlhydrazyl (DPPH), superoxide and hydroxyl radicals, inhibition of N-formyl-methionyl-leucyl-phenylalanine (f-MLP) induced reactive oxygen species (ROS) production in human polymorphonuclear neutrophils (PMN), inhibition of lipopolysaccharide induced nitrite and prostaglandin E₂ production in RAW 264.7 cells.

Results

In the antioxidant activity assay, [6]-gingerol, [8]-gingerol, [10]-gingerol and [6]-shogaol exhibited substantial scavenging activities with IC₅₀ values of 26.3, 19.47, 10.47 and 8.05 μM against DPPH radical, IC₅₀ values of 4.05, 2.5, 1.68 and 0.85 μM against superoxide radical and IC₅₀ values of 4.62, 1.97, 1.35 and 0.72 μM against hydroxyl radical, respectively. The free radical scavenging activity of these compounds also enhanced with increasing concentration (P < 0.05). On the other hand, all the compounds at a concentration of 6 μM have significantly inhibited (P < 0.05) f-MLP-stimulated oxidative burst in PMN. In addition, production of inflammatory mediators (NO and PGE₂) has been inhibited significantly (P < 0.05) and dose-dependently.

Conclusions

6-Shogaol has exhibited the most potent antioxidant and anti-inflammatory properties which can be attributed to the presence of α,β-unsaturated ketone moiety. The carbon chain length has also played a significant role in making 10-gingerol as the most potent among all the gingerols. This study justifies the use of dry ginger in traditional systems of medicine.