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Luiz Carlos Klein-Júnior,
José Roberto Santin,
Marivane Lemos,
Alessandro Conrado de Oliveira Silveira,
Jady Alice Rodrigues Rocha,
Ana Paula Beber,
Theodoro Marcel Wagner,
Tania Mari Bellé Bresolin,
Alexandre Bella-Cruz, Valdir Cechinel-Filho,
Sérgio Faloni de Andrade
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ABSTRACT: This study has aimed to assess the mechanisms of action for the gastroprotective effect of the acetone extract (PCAE) and methanol fraction (PCMF) of Polygala cyparissias, as well as to evaluate the activity of 1,3,6,8-tetrahydroxy-2,7-dimethoxyxanthone (1), 1,7-dihydroxy-2,3-dimethoxyxanthone (2) and astragalin (3).
Gastric secretion and mucus content were determined by pylorus ligation in mice. Nitric oxide (NO) and sulfhydryl group participation were observed by the pretreatment of mice with L-NAME or NEM. Acute ulcer was induced by ethanol/HCl and chronic ulcer by acetic acid. Anti-Helicobacter pylori activity was evaluated by the agar solid dilution assay.
Neither PCAE nor PCMF had the ability to reduce H(+) concentration. However, both of them enhanced mucus secretion. PCAE demonstrated its gastroprotection in a NO-dependent manner, while PCMF exerted the activity depending on the sulfhydryl group. In chronic ulcer, the curative ratios for the PCAE and PCMF were 67.5 and 58.4%, respectively. No effect over H. pylori was detected. Compounds 1, 2 and 3 were able to reduce lesions in the order of 79.6, 73.8 and 67.6%, respectively.
The data suggested that PCAE and PCMF displayed antiulcer activity due to different mechanisms and with the participation of phenolic compounds obtained from the plant.
The Journal of pharmacy and pharmacology. 05/2013; 65(5):767-76.
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ABSTRACT: This paper evaluates CHCl3 and CH3OH extracts of the stem bark, branches and leaves of Drimys brasiliensis and drimane sesquiterpenes isolated from the stem bark against strains of Leishmania amazonensis and Leishmania braziliensis promastigotes and Plasmodium falciparum trophozoites. All of the extracts and compounds were tested in cell lines in comparison with reference standards and cell viability was determined by the XTT method. The CHCl3 and CH3OH extracts from the stem bark and branches yielded promising results against two strains of Leishmania, with 50% inhibitory concentrations (IC50 ) values ranging from 39-100 µg/mL. The CHCl3 extract of the stem bark returned IC50 values of 39 and 40.6 µg/mL for L. amazonensis and L. braziliensis, respectively. The drimanes were relatively effective: 1-β-(p-coumaroyloxy)-polygodial produced IC50 values of 5.55 and 2.52 µM for L. amazonensis and L. braziliensis, respectively, compared with 1-β-(p-methoxycinnamoyl)-polygodial, which produced respective IC50 values of 15.85 and 17.80 µM. The CHCl3 extract demonstrated activity (IC50 of 3.0 µg/mL) against P. falciparum. The IC50 values of 1-β-(p-cumaroyloxyl)-polygodial and 1-β-(p-methoxycinnamoyl)-polygodial were 1.01 and 4.87 µM, respectively, for the trophozoite strain. Therefore, the results suggest that D. brasiliensis is a promising plant from which to obtain new and effective antiparasitic agents.
Memórias do Instituto Oswaldo Cruz 04/2013; 108(2):140-4. · 2.15 Impact Factor
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ABSTRACT: ETHNOPHARMACOLOGICAL RELEVANCE: Corilagin (β-1-O-galloyl-3,6-(R)-hexahydroxydiphenoyl-D-glucose) is a tannin isolated from Phyllanthus niruri (Euphorbiaceae). This plant is well known for their therapeutic purposes to treat several diseases associated with dolorous process and are used in several ethno-medicines in tropical and subtropical countries. AIM OF THE STUDY: This study was designed to evaluate the anti-hyperalgesic activity of corilagin using chemically and thermally based nociception models in mice. MATERIALS AND METHODS: Corilagin was isolated from Phyllanthus niruri (Euphorbiaceae) by extraction and chromatographic procedures and the anti-hyperalgesic activity was evaluated by using writhing, formalin, capsaicin, glutamate and hot plate tests in mice. RESULTS: Corilagin presented activity in acetic acid model with the ID(50) calculated value of 6.46 (3.09-13.51) being about 20.6 fold more potent than acetylsalicylic acid. It also exhibited activity against the first phase of formalin test with ID(50) value of 18.38 (15.15-22.59) μmol/kg. In the capsaicin and glutamate models, corilagin demonstrated significantly activity at the 3mg/kg. CONCLUSION: The experimental data demonstrated that corilagin exhibits anti-hyperalgesic activity that may be due to interaction with the glutamatergic system.
Journal of ethnopharmacology 01/2013; · 2.32 Impact Factor
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ABSTRACT: Background: Kavalactones are pharmacologically active compounds present in preparations of the root trunk of Piper methysticum Forst, known as kava. This work describes the analgesic activity of some synthesized analogues of synthetic kavain, which is the main component of kava. Methods: The essays were initially performed against the writhing test in mice, and the most promising compound was analyzed using other classical models of nociception, including formalin-, capsaicin-, glutamate-induced nociception, the hot plate test, and measurement of motor performance. Results: The results indicated that compound 6-(4-fluorophenyl)-4-methoxy-5,6-dihydropyran-2-one (2d) exerts potent and dose-dependent analgesic activity, inhibiting abdominal constrictions caused by acetic acid in mice, and being more active than some reference drugs. It also presented activity in the other models of pain, with the exception of the hot plate test and the measurement of motor performance. Conclusions: Although compound 2d exerts antinociceptive activity, the mechanism of action remains uncertain, but it does not involve the opioid system and does not appear to be associated with non-specific effects such as changes in locomotor activity or motor coordination.
Pharmacological reports: PR 11/2012; 64(6):1419-26. · 2.44 Impact Factor
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ABSTRACT: This study was undertaken to evaluate the gastroprotective properties of seed, leaf, and branch methanolic extracts and guttiferone A obtained from Garcinia achachairu (Clusiaceae). Mice were used in all the models, and treatments were administered orally only in pylorus-ligated model of the extracts, and drugs were administered intraduodenally. Treatment with different extracts (500 mg/kg) significantly reduced the ulcerative lesions in the ethanol/HCl-induced model; however, the seed extract was most active. When tested in different doses (50, 250, or 500 mg/kg), the seed extract of G. achaicharu showed a dose-dependent effect with a percentage of inhibition of gastric lesions of 41, 49, and 85 %, respectively. The seed extract also significantly reduced the ulcerative lesions in the indomethacin/bethanechol-induced ulcer. In this model, the percentage of inhibition of ulcer was 24, 58, and 90 %, respectively. Regarding the model of gastric secretion, a reduction of gastric juice volume and total acidity was observed, as well as an increase in gastric pH. Considering that the seed extract was the most active, it was subjected to silica gel column chromatography, leading to the isolation of guttiferone A. The isolated compound and omeprazole were evaluated in the HCl/ethanol-induced ulcer model. In this assay, both compounds at a dose of 30 mg/kg reduced the ulcerative lesions by about 75 %. These results demonstrate, for the first time, that extracts obtained from G. achachairu and guttiferone A produce gastroprotective effects, corroborating ethnomedicinal use of this plant.
Archiv für Experimentelle Pathologie und Pharmakologie 08/2012; 385(11):1103-9. · 2.65 Impact Factor
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ABSTRACT: This work evaluates the antinociceptive properties of benzofuranones using chemically induced models of pain and the hot plate test. All the compounds exhibited significant antinociceptive activity, with 3-[2-(4-chlorophenyl)-2-oxoetil]-2-benzofuran-1(3H)-one (3d) being the most active. According to the application of the Topliss method, the 2π-π(2) parameter was the preponderant one, indicating that the hydrophobicity (π) seems to be more involved in the antinociceptive activity. Based on the table of other possible substituents proposed by Topliss, three derived from compound 3d were tested. 3-[2-(3-methoxyphenyl)-2-oxoetil]-2-benzofuran-1(3H)-one (3g) showed greater antinociceptive activity with better pharmacokinetic properties predicted. These results show the efficiency of the Topliss Method as a research tool for the discovery of potential candidate molecules for a new antinociceptive drug.
European journal of medicinal chemistry 08/2012; 56:120-6. · 3.27 Impact Factor
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ABSTRACT: This study investigated the antinociceptive effect of Aleurites moluccana dried extract (DE; 125 to 500 mg/kg, p.o.) and the isolated flavonoid 2″-O-rhamnosylswertisin (5 to 50.6 μmol/kg, p.o.) using different models of long-lasting inflammatory and neuropathic pain in mice. Attempts were made to analyse the mechanisms through which A. moluccana exerted its effects. A. moluccana DE inhibited complete Freund's adjuvant (CFA)-induced mechanical nociception. It was also evidenced by a reduction of sensitization in the contralateral hindpaw. The extract reversed the mechanical hypersensitivity of partial ligation of sciatic nerve (PLSN)-treated animals, similar to gabapentin. In PLSN model, the opioid, dopaminergic and oxidonitrergic pathways were involved in the A. moluccana DE antinociceptive effects. A single dose of 2″-O-rhamnosylswertisin inhibited the carrageenan- and CFA-induced mechanical nociception. Furthermore, the compound caused expressive antinociception in PLSN-mice, with inhibition value greater than obtained with gabapentin. Oral treatment with the extract or the isolated compound attenuated the neutrophil migration and IL-1β levels following carrageenan injection. Of note, A. moluccana DE did not interfere with thermal sensitivity in healthy mice. The absence of side effects, including interference in locomotor activity, motor performance in animals treated with the extract, showed excellent potential for the therapeutic use of this medicinal plant in treating persistent pain in humans.
Pharmacology Biochemistry and Behavior 05/2012; 102(2):302-11. · 2.53 Impact Factor
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ABSTRACT: Chitosan was modified with lauroyl chloride to prepare a solid support for the application of matrix solid-phase dispersion
(MSPD) for the extraction of flavonoids from the medicinal plant Aleurites moluccana. The laurylchitosan prepared by the homogenous and heterogeneous method, was characterized using analytical methods such
as potentiometric titration and infrared spectroscopy. The hydrophobic properties were studied by naphthalene incorporation.
The MSPD performance was evaluated by extraction of swertisin and 2″-O-rhamnosylswertisin from the leaves of A. moluccana.
Chromatographia 04/2012; 69:183-187. · 1.20 Impact Factor
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ABSTRACT: The hexane, chloroform, ethyl acetate and aqueous-soluble fractions from leaves of Maytenus robusta (Celastraceae) were evaluated for their protective actions against ethanol-induced gastric lesions in rats. The treatment
with all fractions (150 mg/kg) and omeprazol (30 mg/kg) significantly reduced the lesion index, the total lesion area, and
the percentage of lesion, in comparison with the control group (p<0.05). Since the ethyl acetate-soluble fraction was found
to be most active in the pylorus ligated model, this fraction was further investigated and resulted in the isolation of triterpene
3,15-dioxo-21α-hydroxy friedelane. The triterpene was evaluated in the HCl/ethanol-induced ulcer model in mice. In this assay,
both the groups treated with 3,15-dioxo-21α-hydroxy friedelane and omeprazol, at a dose of 30 mg/kg, presented a significant
reduction in lesion index, total lesion area, and in the percentage of the lesion, when compared with the control group (p<0.05).
The result suggests that the antiulcer effect observed in the extract and fractions may be attributed, at least in part, to
this compound. Further experiments are underway to determine which antiulcer mechanisms involved in gastroprotection.
Archives of Pharmacal Research 04/2012; 31(1):41-46. · 1.59 Impact Factor
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ABSTRACT: In a search for new and effective analgesic substances from the Brazilian biodiversity, the present study evaluates the chemical composition and antinociceptive potential of the methanol extract and a pure compound obtained from the seeds of Garcinia achachairu Rusby (Clusiaceae). The methanolic seed extract was directly subjected to purification by column chromatography and the purification was monitored by thin-layer chromatography. The main isolated compound was identified as Guttiferone A by comparison of conventional spectroscopic data (IR, NMR-(1)H and (13)C) to the literature data which was isolated for the first time from this plant. When evaluated in the acetic acid-induced nociception model in mice, the methanolic seed extract had an ID(50) (Inhibitory dose) of 13.1 (11.23-14.91) mg/kg and a maximal inhibition of 72 ± 4%. In the same model, Guttiferone A had an ID(50) of 4.54 (3.29-6.24) mg/kg and a maximal inhibition of 73 ± 5%. The methanolic seed extract and Guttiferone A were also active in pain models induced by formalin, capsaicin, glutamate and carrageenan. These data suggest that the antinociceptive effect of Guttiferone A partly depends on its interference with the synthesis or activity of the cytokine TNF-α, the keratinocyte-derived chemokine KC, and/or PGE(2). These data support, at least in part, the use of G. achachairu in folk medicine and suggest that this plant is an important source of compounds with a suitable profile for development as new and effective medicinal agents to treat pain processes.
Archives of Pharmacal Research 03/2012; 35(4):623-31. · 1.59 Impact Factor
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ABSTRACT: Polygala cyparissias, used in folk medicine as an anaesthetic, has already demonstrated antinociceptive activity against acute pain. In this study, we investigated the antihyperalgesic activity of the P. cyparissias methanol extract (PCME) from which the following compounds were isolated: α-spinasterol (PC1), 1,3-dihydroxy-7-methoxyxanthone (PC2), 1,7-dihydroxy-2,3-methylenedioxyxanthone (PC3) and 1,3,6,8-tetrahydroxy-2,7-dimethoxyxanthone (PC4). The antihyperalgesic effect was evaluated using experimental models of persistent pain induced by carrageenan, lipopolysaccharide (LPS), Freund's Complete Adjuvant (CFA), PGE(2) or epinephrine. The partial ligation of the sciatic nerve (PLSN) model was also used. In inflammatory hyperalgesia induced by carrageenan, LPS, CFA or PGE(2), the inhibition values obtained with the PCME treatment were 68 ± 3%, 89 ± 5%, 43 ± 3% and 40 ± 4%, respectively. In epinephrine-induced hyperalgesia, the extract was effective, reducing 99 ± 11% of response frequency, while in PLSN, 54 ± 4% of inhibition was obtained. These results allow to suggest that the antihyperalgesic activity of PCME is, at least in part, related to its capability to inhibit the hypersensitization induced by pro-inflammatory mediators, such as LPS, carrageenan and CFA, without interfering with locomotor activity or motor performance. Furthermore, compounds PC1, PC3 and PC4 inhibited the carrageenan-induced hyperalgesia with inhibition of 42 ± 6%, 48 ± 5% and 64 ± 4%, respectively. In summary, our data demonstrate that PCME has relevant antihyperalgesic activity and that the isolated PC1, PC3 and PC4 seem to be responsible, at least in part, for this important effect.
Basic & Clinical Pharmacology & Toxicology 03/2012; 111(3):145-53. · 2.18 Impact Factor
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ABSTRACT: Two regioisomeric meroterpenoids, Eugenial A and B, have been isolated from the fruits of Eugenia multiflora and their structures established on the basis of NMR evidences. They possess a phloroglucinol-monoterpene structure similar to the euglobals occurring in the sister genus Eucaliptus. A simple method to distinguish between regioisomeric pairs was pointed.
Natural product research 02/2012; · 1.01 Impact Factor
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Chemistry & Biodiversity 02/2012; 9(2):181-209. · 1.80 Impact Factor
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ABSTRACT: The purpose of this study was to assess the gastroprotective properties of the methanol extract and the diterpene marrubiin obtained from the leaves of M. vulgare.
Assays were performed using different protocols in mice. Studies focusing on mechanisms of gastroprotection were also undertaken.
In the model of ethanol-induced ulcers, we observed a significant reduction in all the parameters analysed; the curative ratios obtained were 49.31±0.57, 74.31±0.91 and 79.86±0.59 for the groups treated with 50 and 100mg/kg of extract of M. vulgare and omeprazole (30mg/kg), respectively. For indomethacin-induced ulcers, the percentages of ulcer inhibition were 50.32±5.60, 66.24±4.30, 82.17±04.09 and 67.52±4.38, for the groups treated with 25, 50 and 100mg/kg M. vulgare and positive control (cimetidine), respectively. In both models, the marrubiin (25mg/kg) produced a significant reduction in all the parameters when compared with the control group (P<0.01). There was also a significant increase in pH and mucus production in the groups treated with M. vulgare extract and marubiin. The results also demonstrated that the gastroprotection induced by the extract and marubiin is related to the activity of nitric oxide and endogenous sulfhydryls, which are important gastroprotective factors.
The results of this study show that the extract of M. vulgare and marrubiin displays antiulcer activity and that this effect can be partly attributed to the isolated diterpene.
The Journal of pharmacy and pharmacology. 09/2011; 63(9):1230-7.
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ABSTRACT: Cariniana rubra Miers (Lecythidaceae), popularly known as "jequitibá-vermelho'', is a large Brazilian tree whose bark is used in infusion and decoction for the treatment of inflammatory conditions. This study aims to assess the anti-inflammatory, antinociceptive, and antipyretic effects of Cariniana rubra methanolic stem bark extract (EM Cr) using experimental animals. Anti-inflammatory activity of EM Cr was tested on carrageenan and dextran-induced rat paw edema, carrageenan-induced pleurisy in rats and acetic acid-increase vascular permeability in mice. Antinociceptive and antipyretic activities were evaluated using acetic acid-induced writhing, formalin and hot-plate tests in mice, as well as brewer's yeast-induced pyrexia in rats. The extract inhibitied carrageenan and dextran-induced edema, reduced exudate volume and leukocyte migration on the carrageenan-induced pleurisy and on the vascular permeability increase induced by acetic acid. The EM Cr inhibited nociception on the acetic acid-induced writhing and in the second phase of formalin test, and decreased rectal temperature. It was, however, inactive against thermal nociception.Phytochemical analysis with EM Cr showed the occurrence of saponins, triterpenes, sterols and phenolic compounds. Phytosterols (β-sitosterol, stigmasterol), pentacyclic triterpenes (α- and β-amyrin as a mixture), arjunolic acid, a phytosterol glycoside (sitosterol 3-O-β-D-glucopyranoside), and triterpenoid saponins (28-β-glucopyranosyl-23-O-acetyl arjunolic acid; 3-O-β-glucopyranosyl arjunolic acid and 28-O-[α-L-Rhamnopyranosyl-(1→2)-β-glucopyranosyl]-23- O-acetyl arjunolic acid) were the main identified compounds. It can be presumed that EM Cr caused their effects by inhibiting the liberation and/or action of different inflammatory mediators. These findings support the traditional use of Cariniana rubra preparations to treat inflammation.
Anais da Academia Brasileira de Ciências 06/2011; 83(2):557-66. · 1.09 Impact Factor
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ABSTRACT: Plants belonging to the genus Maytenus (Celastraceae) are routinely used in folk medicine in Brazil and other countries to treat a variety of illnesses, the most common of which are gastric disorders. Several studies have reported on the importance of these biological effects, and the chemical substances, mostly terpenoids and flavonoid glycosides, responsible for them. This review summarizes the ethnopharmacological, chemical and pharmacological knowledge of plants of the Maytenus genus, with particular emphasis on those growing in Brazil.
Current pharmaceutical design 05/2011; 17(18):1851-71. · 4.41 Impact Factor
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Michel F Otuki,
Camila A Bernardi,
Arthur S Prudente,
Kerly Laskoski,
Franciane Gomig,
Cintia D S Horinouchi,
Claudio L Guimarães,
Juliano Ferreira,
Franco Delle-Monache, Valdir Cechinel-Filho,
Daniela A Cabrini
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ABSTRACT: Garcinia gardneriana is popularly used in skin disorders; therefore, this article investigated the effect of G. gardneriana extracts from leaves, bark and seeds and two isolated compounds in ear oedema and leucocytes migration caused by croton oil. The topical application of the extract of G. gardneriana leaves was able to reduce (70 ± 3%, and ID(50) 0.33 mg/ear) ear oedema, while the seeds (51 ± 5%) and the wood (60 ± 12%) extracts were less effective. In a time-course evaluation, the leaf extract (1 mg/ear) was effective when applied 2 hr before and until 3 hr after the stimulation, presenting a higher effectiveness when applied right after croton oil (83 ± 7% inhibition). In addition, the leaf extract was able to diminish the myeloperoxidase (MPO) activity in 64 ± 13%, which suggests the inhibition of leucocyte infiltration that was confirmed by histological analysis. Also, both biflavonoids isolated from the leaves of G. gardneriana, fukugetin (or morelloflavone) and 13-naringenin-II 8-eriodictyol (GB-2a), were able to reduce ear oedema, with ID(50) values of 0.18 (0.10-0.28) and 0.22 (0.15-0.31) mg/ear, respectively, besides the inhibition of MPO activity of 52 ± 6% and 64 ± 5%, respectively. Using the fluorescent probe 2',7'-dichlorodihydrofluorescein diacetate, the leaf extract, fukugetin and GB-2a topically applied to the ear treated with croton oil reduced 52 ± 15%, 63 ± 17% and 83 ± 4%, respectively, the production of reactive oxygen species of the skin. Thus, these results reveal the anti-inflammatory effect of G. gardneriana leaves for topical usage, and both biflavonoids are responsible for this effect.
Basic & Clinical Pharmacology & Toxicology 03/2011; 109(1):56-62. · 2.18 Impact Factor
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ABSTRACT: Simaba ferruginea A. St-Hil. (Simaroubaceae) is a subshrub typical of the Brazilian Cerrado, whose rhizomes are popularly used as infusion or decoction for the treatment of gastric ulcers, diarrhea and fever.
To evaluate the pharmacological mechanism(s) of action of the antiulcer effects of the methanol extract of Simaba ferruginea and its alkaloid canthin-6-one.
Rhizome of Simaba ferruginea was macerated with methanol to obtain the methanol extract (MESf) from which was obtained, the chloroform fraction. Canthin-6-one alkaloid (Cant) was purified and then isolated from the chloroform fraction (CFSf). The isolated Cant was identified by HPLC. Anti-ulcer assays were determined using ethanol and indomethacin-induced ulcer models in mice and rats respectively. In order to determine the probable mechanisms of actions of MESf and Cant animals were pretreated with l-NAME prior to anti-ulcer agent treatments and ulcer induction and nitric oxide (NO) level determined in order to assess NO involvement in the gastroprotective effects. Assays of malondialdehyde (MDA), myeloperoxidase (MPO), pro-inflammatory cytokines: interleukin 8 (IL-8) and tumor necrosis factor-alpha (TNF-α) and prostaglandin E(2) (PGE(2)) were also carried out according to previously described methods.
The results indicate that the antiulcerogenic effects of MESf and Cant in ethanol-induced ulcer is mediated in part through increase in the production of protective endogenous NO as the antiulcerogenic activity of MESf and Cant was reduced in animals pre-treated with l-NAME. In indomethacin-induced ulcer pre-treatment with MESf and Cant showed reduction in the levels of MPO and MDA in the gastric tissue, thus indicating the participation of the antioxidant mechanisms on the gastroprotective effects. The plasma levels of IL-8 in ulcerated rats with indomethacin were also reduced by Cant, but not by MESf, indicating that inhibition of this cytokine contributes to the gastroprotective effect of Cant. However MESf and Cant had no effect on the mucosal membrane levels of PGE(2), indicating that the gastroprotective effects of these agents is independent of PGE(2) modulation.
The results obtained in this study with MESf and Cant added insights into the pharmacological mechanisms involved in their mode of antiulcer action. The results indicate that Cant is one of the compounds responsible for these effects. Such findings are of extreme importance in the strive for future development of potent, safer and effective antiulcer agent. The efficacy of MESf and Cant in gastroprotection shows that Simaba ferruginea might be a promising antiulcer herbal medicine, in addition to confirming the popular use of this plant against gastric ulcer models utilised in this study.
Journal of ethnopharmacology 01/2011; 134(3):630-6. · 2.32 Impact Factor
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ABSTRACT: Cipura paludosa (Iridaceae) is a plant that is distributed in the north region of Brazil. Its bulbs are used in folk medicine to treat inflammation and pain. Four naphthalene derivatives have been isolated from the bulbs of this plant. Three of them have been identified as the known naphthalene derivatives, eleutherine, iso-eleutherine, and hongkonin. The structure of the fourth and new component was determined as 11-hydroxyeleutherine by extensive NMR study. In addition, the IN VIVO effect of the two major compounds, eleutherine and iso-eleutherine, was evaluated in carrageenan-induced hypernociception and inflammation in mice. Eleutherine and iso-eleutherine (1.04-34.92 µmol/kg), dosed intraperitoneally (i.p.) or orally (p.o.), decreased the carrageenan-induced paw oedema (i.p. - inhibitions of 36 ± 7 % and 58 ± 14 %, respectively; p.o. - inhibitions of 36 ± 7 % and 58 ± 14 %, respectively). Iso-eleutherine, but not eleutherine, significantly reduced (inhibitions of 39 ± 4 %) the plasma extravasation induced by intradermal (i.d.) injection of carrageenan. Likewise, eleutherine and iso-eleutherine (1.04-34.92 µmol/kg, i.p. or p.o.) were also effective in preventing the carrageenan-induced hypernociceptive response (i.p. - inhibition of 59 ± 4 % and 63 ± 1 %, respectively; p.o. - inhibitions of 36 ± 7 % and 58 ± 14 %, respectively). It was also suggested that the anti-inflammatory and anti-hypernociceptive effects of eleutherine or iso-eleutherine partly depend on the interference with the synthesis or activity of mast cell products, kinins, cytokine, chemokines, prostanoids, or sympathetic amines. Our findings show that two major compounds of C. paludosa contain pharmacologically active constituents that possess antinociceptive and anti-inflammatory activity, justifying, at least in part, its popular therapeutic use for treating conditions associated with pain.
Planta Medica 01/2011; 77(10):1035-43. · 2.15 Impact Factor
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ABSTRACT: There are few studies on the pharmacological properties of Valeriana prionophylla Standl. (VP), known as "Valeriana del monte", and used in Mesoamerican folk medicine to treat sleep disorders. This study examines the pharmacological effects of the hydroalcoholic extract of the dry rhizome using the open field, rota rod, elevated plus-maze (EPM), forced swimming (FST), strychnine- and pentobarbital-induced sleeping time, PTZ-induced seizures, and the inhibitory avoidance tests. VP did not show any protective effect against PTZ-induced convulsions. In the EPM, exhibited an anxiolytic-like effect through the effective enhancement of the entries (38.5%) and time spent (44.7%) in the open arms, when compared with control group. Time spent and the numbers of entrances into the enclosed arms were decreased, similar to those effects observed with diazepam. In the FST, acute treatment with VP, produced a dose-dependent decrease in immobility time, similarly to imipramine. VP also produced a significant dose-dependent decrease in the latency of sleeping time, while producing an increase in total duration of sleep; influenced memory consolidation of the animals only at lower doses, unlike those that produced anti-depressant and anxiolytic effects. In summary, the results suggest that VP presents several psychopharmacological activities, including anxiolytic, antidepressant, and hypno-sedative effects.
Evidence-based Complementary and Alternative Medicine 01/2011; 2011:312320. · 4.77 Impact Factor
