RESUMO

BACKGROUND: Chronic orofacial pain is a serious public health problem with a prevalence of 7-11% in the population. This disorder has different etiologies and characteristics that make pharmacological treatment difficult. Natural products have been shown to be a promising source of treatments for the management of chronic pain, as an example the terpenes. PURPOSE: The aim of this study was to evaluate the anti-nociceptive and anti-inflammatory effects of one of these terpenes, d-limonene (LIM - a common monoterpene found in citrus fruits) alone and complexed with hydroxypropyl-ß-cyclodextrin (LIM/HPßCD) in preclinical animal models. METHODS: Orofacial pain was induced by the administration of hypertonic saline on the corneal surface, the injection of formalin into the temporomandibular joint (TMJ), or chronic constriction injury of the infraorbital nerve (CCI-IoN). The study used male Wistar rats and Swiss mice treated with LIM (50 mg/kg), LIM/HPßCD (50 mg/kg), vehicle (control), gabapentin or morphine, and eyes wiping (induced by hypertonic saline), face rubbing (formalin-induced in TMJ) or mechanical hyperalgesia (provoked by CCI-IoN) were assessed. Additionally, ELISA was used to measure TNF-α, and western blot analysis to assess levels of PKAcα, NFκB, p38MAPK and phosphorylated PKC substrates. Serum levels of aspartate aminotransferase (AST) and alanine transferase (ALT) were also evaluated. RESULTS: LIM and LIM/HPßCD significantly reduced (p < 0.001) corneal nociception and formalin-induced TMJ nociception. In addition, both substances attenuated (p < 0.001) mechanical hyperalgesia in the CCI-IoN model. The antinociceptive effect induced by LIM and HPßCD/LIM was associated with decreased TNF-α levels, downregulation of the NFκB and p38MAPK signalling pathways and reduced PKC substrate phosphorylation and PKA immunocontent. Moreover, the results demonstrated that complexation with HPßCD was able to decrease the therapeutic dose of LIM. CONCLUSION: LIM was found to be a promising molecule for the treatment of orofacial pain due to its capacity to modulate some important mediators essential to the establishment of pain, and HPßCD can be a key tool to improve the profile of LIM.

Assuntos

Citrus , Nociceptividade , 2-Hidroxipropil-beta-Ciclodextrina , Animais , Dor Facial/tratamento farmacológico , Hiperalgesia/tratamento farmacológico , Limoneno , Masculino , Camundongos , Monoterpenos/farmacologia , Ratos , Ratos Wistar , Roedores

RESUMO

BACKGROUND: Plant lectins have shown promising biological activities in the central nervous system (CNS). OBJECTIVE: This study evaluated the effect of DAL, a lectin isolated from the seeds of the Dioclea altissima species, having binding affinity to D-glucose or D-mannose residues, on mice behavior. METHODS: Mice (n=6/group) were treated (i.p.) with DAL (0.25, 0.5 or 1 mg/kg) or vehicle and subjected to several tests (open field/OFT, marble-burying/MBT, hole-board/HBT, elevated plus maze/PMT, tail suspension/ TST, forced swimming/FST or rotarod/RRT). Pizotifen, cyproheptadine, flumazenil, L-NAME, 7-NI, Larginine or yohimbine were administered 15 min before DAL (0.5 mg/kg) and the animals were evaluated on PMT. It was also verified whether the DAL effect depended on its structural integrity and ability to interact with carbohydrates. RESULTS: The results showed there were no neurobehavioral changes in the mice at the RRT, FST and locomotion in the OFT. DAL (0.25, 0.5 or 1 mg/kg) increased the behavior of grooming and rearing in the OFT, head dips in the HBT, pedalling in the TST and decreased the number of marbles hidden in the MBT. In the PMT, DAL (0.25, 0.5 and 1 mg/kg) and Diazepam increased the frequency of entries in the open arms and the time of permanence in the open arms without affecting the locomotor activity. The effect of DAL was dependent on carbohydrate interaction and protein structure integrity and it prevented by pizotifen, cyproheptadine, flumazenil, L-NAME and 7-NI, but not by L-arginine or yohimbine. CONCLUSION: DAL was found to have an anxiolytic-like effect mediated by the 5-HT and GABAergic receptors and NO pathway.

Assuntos

Ansiolíticos , Dioclea , Animais , Ansiolíticos/farmacologia , Antidepressivos , Comportamento Animal , Lectinas , Camundongos , Extratos Vegetais , Sementes

RESUMO

Schinus terebinthifolius Raddi (Anacardiaceae) is popularly known in Brazil as aroeira-da-praia and has pharmacological use as an astringent, antidiarrheal, anti-inflammatory, depurative, diuretic, and antifebrile agent. Although the neuropathic antinociceptive potential of S. terebinthifolius fruits has already been investigated, this study is the first one to analyze the acute antinociceptive effect of the essential oil of S. terebinthifolius (female) leaves (EOFSt) on adult zebrafish. EOFSt was submitted to antioxidant activity evaluation by two methods (ferrous ion-chelating capacity [FIC] and ß-carotene). The animals (n = 6/group) were treated orally (20 µL) with EOFSt (0.1, 0.5, or 1.0 mg/mL) or vehicle (0.9% sodium chloride [NaCl]; 20 µL), and submitted to nociception (formalin, cinnamaldehyde, capsaicin, glutamate, acidic saline, and hypertonic saline). Possible neuromodulation mechanisms, as well motor alterations and toxicity were also evaluated. In the FIC assay, EOFSt showed ferrous ion-chelating capacity in ∼40% to 90%. Regarding the ß-carotene bleaching assay, EOFSt showed inhibition in a 58% to 80% range. Oral administration of EOFSt showed no acute toxicity and did not alter the locomotor system of aZF, and reduced the nociceptive behavior in all tested models. These effects of EOFSt were significantly similar to those of morphine, used as a positive control. The antinociceptive effect of EOFSt was inhibited by naloxone, L-NAME, ketamine, camphor, ruthenium red, and amiloride. The antinociceptive effect of the EOFSt cornea was inhibited by capsazepine. EOFSt has the pharmacological potential for acute pain treatment and this effect is modulated by the opioid system, NMDA receptors, and transient receptor potential ankyrin 1 (TRPA1), transient receptor potential vanilloid 1 (TRPV1), and acid-sensing ion channels. The EOFSt also has the pharmacological potential for corneal pain treatment and this effect is modulated by the TRPV1 channel.

Assuntos

Anacardiaceae/química , Analgésicos/farmacologia , Óleos Voláteis/farmacologia , Peixe-Zebra/fisiologia , Administração Oral , Analgésicos/química , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Antioxidantes/metabolismo , Feminino , Masculino , Óleos Voláteis/química , Folhas de Planta/química

RESUMO

A new mannose/N-acetyl-dglucosamine-specific lectin, named MaL, was purified from seeds of Machaerium acutifolium by precipitation with ammonium sulfate, followed by affinity and ion-exchange chromatography. MaL haemagglutinates either native rabbit erythrocytes or those treated with proteolytic enzymes. MaL is highly stable by the ability to maintain its haemagglutinating activity after exposure to temperatures up to 50 °C. The lectin haemagglutinating activity was optimum between pH 6.0 and 7.0 and inhibited after incubation with d-mannose and N-acetyl-d-glucosamine and α-methyl-d-mannopyranoside. MaL is a glycoprotein with relative molecular mass of 29 kDa (α-chain), 13 kDa (ß-chain) and 8 kDa (γ-chain) with secondary structure composed of 3% α-helix, 44% ß-sheet, 21% ß-turn, and 32% coil. The orofacial antinociceptive activity of the lectin was also evaluated. MaL (0.03 mg mL-1) reduced orofacial nociception induced by capsaicin, an effect that occurred via carbohydrate recognition domain interaction, suggesting an interaction of MaL with the transient receptor potential cation channel subfamily V member 1 (TRPV1) receptor. Our results confirm the potential pharmacological relevance of MaL as an inhibitor of acute orofacial mediated by TRPV1.

Assuntos

Acetilglucosamina/química , Fabaceae/química , Dor Facial/tratamento farmacológico , Lectinas/isolamento & purificação , Lectinas/uso terapêutico , Manose/química , Canais de Cátion TRPV/metabolismo , Sequência de Aminoácidos , Animais , Fenômenos Biofísicos , Cromatografia de Afinidade , Eletroforese em Gel de Poliacrilamida , Feminino , Lectinas/química , Masculino , Estrutura Secundária de Proteína , Coelhos , Espectrometria de Massas em Tandem , Peixe-Zebra

RESUMO

This study aimed to evaluate the antinociceptive effect of oleanolic acid using adult zebrafish models of orofacial pain. Acute nociception was induced by formalin, capsaicin, cinnamaldehyde, menthol, acidified saline or glutamate (cutaneous modes) and hypertonic saline (corneal model). In another set of experiments, animals were pre-treated with naloxone, L-NAME, methylene blue, ketamine, camphor, HC-030031, mefenamic acid, ruthenium red or amiloride to investigate the mechanism of antinociception. The involvement of central afferent C-fibers was also investigated. A molecular docking was performed using the TRPV1 channel. Motor activity was evaluated with the open field test. Pre-treatment with oleanolic acid significantly reduced nociceptive behavior associated with acute pain. Antinociception was effectively inhibited by ruthenium red and capsaicin-induced desensitization. Presence of trpv1 was confirmed by RT-PCR in cerebral tissue of zebrafish. In line with in vivo experiments, docking studies indicated that oleanolic acid may interact with TRPV1. Results confirm the potential pharmacological relevance of oleanolic acid as an inhibitor of orofacial nociception mediated by TRPV1.

Assuntos

Analgésicos/farmacologia , Comportamento Animal/efeitos dos fármacos , Ácido Oleanólico/farmacologia , Canais de Cátion TRPV/metabolismo , Proteínas de Peixe-Zebra/metabolismo , Acetanilidas/farmacologia , Analgésicos/uso terapêutico , Animais , Sítios de Ligação , Capsaicina/farmacologia , Dor Facial/tratamento farmacológico , Dor Facial/etiologia , Formaldeído/farmacologia , Simulação de Acoplamento Molecular , Ácido Oleanólico/química , Ácido Oleanólico/uso terapêutico , Estrutura Terciária de Proteína , Purinas/farmacologia , Rutênio Vermelho/química , Rutênio Vermelho/metabolismo , Canais de Cátion TRPV/química , Canais de Cátion TRPV/genética , Termodinâmica , Peixe-Zebra

RESUMO

Neem fruit (Azadirachta indica A. Juss.) are popularly used to treat infections, diarrhea, fever, bronchitis, skin diseases, infected burns and hypertension. Although the antinociceptive and anti-inflammatory potential of A. indica has already been investigated in experimental models of pain and inflammation in mice, the current research is the first to report the evaluation of the capacity of A. indica fruit ethanolic extract (EtFrNeem) in acute pain attenuation using the adult zebrafish (Danio rerio) as an alternative model to the use in rodents. EtFrNeem was submitted to antioxidant action, preliminary chemical prospecting, FT-IR and determination of phenol and flavonoid content tests. Subsequently, EtFrNeem was tested for acute nociception and abdominal inflammation, locomotor activity, and acute toxicity in adult zebrafish. Possible neuromodulation mechanisms were also evaluated. EtFrNeem showed low antioxidant activity, but was shown to be rich in flavonoids. EtFrNeem showed no anti-inflammatory action, did not alter the locomotor system, and it was not toxic. However, EtFrNeem significantly reduced the nociceptive behavior induced by formalin, glutamate and acidic saline, when compared to the control group. These effects of EtFrNeem were significantly similar to those of morphine, used as a positive control. The antinociceptive effect of EtFrNeem was inhibited by naloxone, ketamine and amiloride. EtFrNeem has the pharmacological potential for acute pain treatment and this effect is modulated by the opioid system, NMDA receptors and ASICs channels. These results lead us to studies of isolation and characterization of EtFrNeem bioactive principles, using adult zebrafish as an experimental model.

Assuntos

Analgésicos Opioides/farmacologia , Analgésicos/farmacologia , Azadirachta/química , Fármacos Atuantes sobre Aminoácidos Excitatórios/farmacologia , Frutas/química , Meliaceae/química , Extratos Vegetais/farmacologia , Canais Iônicos Sensíveis a Ácido/metabolismo , Animais , Antioxidantes/metabolismo , Modelos Animais de Doenças , Etanol , Flavonoides/farmacologia , Locomoção/efeitos dos fármacos , Morfina/farmacologia , Dor/tratamento farmacológico , Dor/metabolismo , Receptores de N-Metil-D-Aspartato/metabolismo , Peixe-Zebra

RESUMO

Orofacial pain is a highly prevalent clinical condition, yet difficult to control effectively with available drugs. Much attention is currently focused on the anti-inflammatory and antinociceptive properties of lectins. The purpose of this study was to evaluate the antinociceptive effect of frutalin (FTL) using rodent models of inflammatory and neuropathic orofacial pain. Acute pain was induced by formalin, glutamate or capsaicin (orofacial model) and hypertonic saline (corneal model). In one experiment, animals were pretreated with l-NAME and naloxone to investigate the mechanism of antinociception. The involvement of the lectin domain in the antinociceptive effect of FTL was verified by allowing the lectin to bind to its specific ligand. In another experiment, animals pretreated with FTL or saline were submitted to the temporomandibular joint formalin test. In yet another, animals were submitted to infraorbital nerve transection to induce chronic pain, followed by induction of thermal hypersensitivity using acetone. Motor activity was evaluated with the rotarod test. A molecular docking was performed using the TRPV1 channel. Pretreatment with FTL significantly reduced nociceptive behaviour associated with acute and neuropathic pain, especially at 0.5 mg/kg. Antinociception was effectively inhibited by l-NAME and d-galactose. In line with in vivo experiments, docking studies indicated that FTL may interact with TRPV1. Our results confirm the potential pharmacological relevance of FTL as an inhibitor of orofacial nociception in acute and chronic pain mediated by TRPA1, TRPV1 and TRPM8 receptor.

Assuntos

Analgésicos/uso terapêutico , Dor Facial/tratamento farmacológico , Galectinas/uso terapêutico , Dor Aguda/tratamento farmacológico , Dor Aguda/metabolismo , Analgésicos/isolamento & purificação , Animais , Artocarpus/química , Modelos Animais de Doenças , Dor Facial/metabolismo , Galectinas/isolamento & purificação , Camundongos , Simulação de Acoplamento Molecular , Neuralgia , Ratos Wistar , Canais de Cátion TRPM/metabolismo , Canais de Cátion TRPV/metabolismo , Canais de Potencial de Receptor Transitório/metabolismo

RESUMO

Tropidurus hispidus has been used in traditional medicine in several regions of Northeastern Region of Brazil. Its medicinal use involves the treatment of diseases such as warts, sore throat, tonsillitis, chicken pox, varicella, measles, asthma, alcoholism, and dermatomycosis. The present study evaluated the topical anti-inflammatory activity of Tropidurus hispidus fat in treating ear edema in an animal model. Oil from T. hispidus (OTH) was evaluated on its effect against experimental inflammation in mice. OTH was extracted from body fat located in the ventral region of Tropidurus hispidus using hexane as a solvent. We used the model of mouse ear edema induced by phlogistic agents, croton oil (single and multiple applications), arachidonic acid, phenol, capsaicin, and histamine, applied into the right ears of animals pretreated with acetone (control), dexamethasone, or OTH. OTH inhibited the dermatitis induced by all noxious agents, except capsaicin. This effect may be related to the fatty acids present in OTH.

RESUMO

BACKGROUND: Cordia verbenacea is a Brazilian coastal shrub popularly known as "erva baleeira". The essential oil from fresh leaves was obtained by hydrodistillation and analyzed by CG/MS. The main components were identified as ß-caryophyllene (25.4%), bicyclogermacrene (11.3%), δ-cadinene (9.%) and α-pinene (9.5%). In this study, the antimicrobial activity of Cordia verbenacea was evaluated. MATERIALS AND METHODS: The minimal inhibitory concentration (MIC) of the essential oil was obtained using the broth microdilution assay (from 512 to 8 µg/ml). RESULTS: The results showed that the essential oil presented fungistatic activity against Candida albicans and Candida krusei and antibacterial activity against Gram-positive strains (Staphylococcus aureus and Bacillus cereus) and against multiresistant Gram-negative (Escherichia coli 27), in all tests the MIC was 64 µg/ml. When the essential oil was associated to aminoglycosides (subinhibitory concentrations, MIC/8), a synergic and antagonic activity was verified. The synergic effect was observed to the amikacin association (MIC reduction from 256 mlto 64 µg/ml) in all strains tested. CONCLUSION: The essential oil of Cordia verbenacea influences the activity of antibiotics and may be used as an adjuvant in antibiotic therapy against respiratory tract bacterial pathogens.

RESUMO

BACKGROUND: The use and investigation of natural products with antimicrobial activity from vegeral source have been reported by several researchers. Cajanus cajan (Fabaceae) is a multiple use specie mainly as human food. In popular medicine, diverse parts of the plant are used as sedative and to treat cough, hepatitis, and diabetes. MATERIALS AND METHODS: This study shows the characterization of secondary metabolites present in ehtanolic extracts from leaves and roots of Cajanus cajan by phytochemical prospection. The evaluation of the antifungal activity was performed by the microdilution method, and from the subinhibitory concentrations (MIC 1/8) the modulatory activity of antifungical (fluconazole and ketoconazole) was analyzed by the direct contact assay against C. albicans ATCC40006, Candida krusei ATCC 6538 and Candida tropicalis ATCC 40042. RESULTS: The results showed the presence of tannins, flavonoids, and alkaloids in both extracts as the clinically relevant antifungal activity. The modulatory potential is presented by the antifungal tested against yeasts. CONCLUSION: The extracts studied here have demonstrated to be a new therapeutic source to treat these microorganism-associated diseases.

RESUMO

Compounds with dual action on cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) may be a treatment option for erectile dysfunction, as they not only promote penile erection but also prevent the upregulation of phosphodiesterase-5. In this study, we examined the possible relaxant effect and mechanism of 17-nor-subincanadine E (SEC, 0.2-200 µmol l⁻¹), a plant-derived alkaloid, in rabbit corpus cavernosum (RbCC) strips that had been precontracted by exposure to phenylephrine (10 µmol l⁻¹) or a high concentration of K(+) (60 mmol l⁻¹) in vitro. In addition to SEC's effect on cAMP and cGMP levels, electrical field stimulation (EFS) in phenylephrine-precontracted RbCC and calcium chloride (1-100 mmol l⁻¹) evoked responses in depolarized RbCC were analysed. SEC relaxed the phenylephrine-precontracted RbCCs in a concentration-dependent manner. Atropine, guanethidine and N-ω-nitro-l-arginine methyl ester (L-NAME) did not have any effect on the relaxation of RBCCs. When 1H-(1, 2, 4)oxadiazole[4,3-a] quinoxalin-1-one (ODQ) was added, it effectively blocked the relaxant response of SEC. Although SEC enhanced the maximal relaxation produced by sodium nitroprusside (SNP) and forskolin in phenylephrine-precontracted cavernosal smooth muscle, it caused a decrease in the maximal contractile response induced by calcium chloride in depolarized RbCCs. The relaxant effect of SEC was paralleled by an increase in the tissue levels of the cyclic nucleotides cAMP and cGMP. We conclude that SEC promotes the relaxation of RbCC, possibly favouring cAMP and cGMP accumulation and calcium blockade. This novel mechanism could be useful for patients who do not benefit from phosphodiesterase inhibitors and for those with endothelial and nitrergic dysfunction, such as patients with diabetes, hypertension and dyslipidaemias.

Assuntos

Vasos Sanguíneos/efeitos dos fármacos , Alcaloides Indólicos/farmacologia , Pênis/irrigação sanguínea , Vasodilatadores/farmacologia , Animais , Masculino , Coelhos

RESUMO

OBJECTIVE: In this work, we report the antibacterial and modulatory activity of Lantana montevidensis Briq. MATERIALS AND METHODS: The antibacterial activities of leaf (LELm) and root (RELm) extracts alone or in association with aminoglycosides were determined by a microdilution test. Multiresistant strains of Escherichia coli (Ec 27) and Staphylococcus aureus (Sa 358) were used. RESULTS: The results show the inhibitory activity of LELm against E. coli (minimal inhibitory concentration [MIC] 16 µg/mL) and S. aureus (MIC 128 µg/mL). The synergistic effect of the extracts and aminoglycosides was verified too. The maximum effects were obtained with RELm with gentamicin against E. coli with MIC reduction (312 to 2 µL). CONCLUSION: The data from this study are indicative of the activity antibacterial of extracts of L. montevidensis and its potential in modifying the resistance of aminoglycosides.

RESUMO

The study examined the antiinflammatory and antinociceptive effects of the sesquiterpene (-)-α-bisabolol (BISA). The antiinflammatory effect was evaluated on acute models of dermatitis induced by Croton oil, arachidonic acid, phenol and capsaicin, respectively, in mouse ear. BISA inhibited the dermatitis induced by all noxious agents, except capsaicin. BISA was assessed in two established mouse models of visceral nociception. Mice were pretreated orally with BISA, and the pain-related behavioral responses to intraperitoneal cyclophosphamide or to intracolonic mustard oil were analyzed. BISA showed a dose-unrelated significant antinociception. Collectively, the results suggest that BISA may be an topical antiinflammatory and visceral antinociceptive agent.

Assuntos

Dor Abdominal/tratamento farmacológico , Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Comportamento Animal/efeitos dos fármacos , Dermatite/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Sesquiterpenos/uso terapêutico , Dor Abdominal/induzido quimicamente , Doença Aguda , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Colo/efeitos dos fármacos , Ciclofosfamida , Modelos Animais de Doenças , Orelha , Masculino , Camundongos , Sesquiterpenos Monocíclicos , Mostardeira , Óleos Voláteis/química , Peritônio/efeitos dos fármacos , Extratos Vegetais/farmacologia , Óleos de Plantas , Sesquiterpenos/farmacologia , Pele/efeitos dos fármacos

RESUMO

AIM OF THE STUDY: Caryocar coriaceum Wittm. fruit pulp fixed oil (CCFO) has been widely employed by communities from Brazil Northeastern in the treatment of skin inflammation, respiratory affections, wound healing and muscle pain. In this study, we evaluated the topical effect of CCFO against different irritant agents in vivo, in order to verify its antiedematous effect as well to unravel its tentative mechanisms of action. MATERIALS AND METHODS: CCFO was obtained from Caryocar coriaceum fruits using ethyl acetate as solvent. Ear edema provoked by the application of Croton oil (single and multiple applications), arachidonic acid (AA), capsaicin, phenol and histamine to Swiss mice was used to evaluate the topical anti-inflammatory effect of CCFO. Histological analysis from mice ears sensitized with Croton oil and AA single application was also performed. RESULTS: Crude CCFO (20µL/ear) demonstrated significant topical antiedematous effect against Croton oil single (inhibition of 32.0%; P<0.05) and multiple (41.4% after 9 days, P<0.001) applications, AA (inhibition of 49.7%; P<0.01) and phenol (inhibition of 38.8%; P<0.001). In contrast, CCFO did not antagonize the edema caused by topical treatment with capsaicin and histamine when compared to control group (P>0.05). Histological analysis also revealed that CCFO was able to reduce the edema and the influx of inflammatory cells in mice ears sensitized with Croton oil and AA. CONCLUSIONS: CCFO exhibited a similar profile of topical anti-inflammatory activity to that of drugs that classically modulate the production of arachidonic acid metabolites. The study also indicates the potential application of CCFO as an important herbal medicine to be used against skin inflammatory diseases.

Assuntos

Anti-Inflamatórios/uso terapêutico , Edema/tratamento farmacológico , Ericales , Inflamação/tratamento farmacológico , Fitoterapia , Óleos de Plantas/uso terapêutico , Pele/efeitos dos fármacos , Administração Tópica , Animais , Anti-Inflamatórios/farmacologia , Orelha , Feminino , Frutas , Sistema Imunitário/citologia , Sistema Imunitário/efeitos dos fármacos , Inflamação/induzido quimicamente , Inflamação/imunologia , Masculino , Camundongos , Camundongos Endogâmicos , Óleos de Plantas/farmacologia , Pele/imunologia , Pele/patologia

RESUMO

BACKGROUND: Many medicinal plant species from the Araripe Basin are widely known and used in folk medicine and for commercial manufacturing of phytotherapeutic products. Few ethnobotanical and pharmacological studies have been undertaken in this region, however, in spite of the great cultural and biological diversity found there. MATERIALS AND METHODS: Extracts of 11 plant species collected from Ceará state, Brazil, were subjected to the brine shrimp lethality test in order to detect potential sources of novel cytotoxic, antitumor compounds. The larvicidal activity, based on the percentage of larval mortality, was evaluated after 24 h exposure to the treatments. RESULTS: All species tested showed good larvicidal activity as compared to a reference compound and literature data. The extract from Vanillosmopsis arborea was the most active with an LC(50) of 3.9 µg/ml. Best results were shown by Lantana montevidensis against Pseudomonas aeruginosa [minimum inhibitory concentration (MIC) 8µg/ml] and Escherichia coli (MIC 32 µg/ml), Zanthoxylum rhoifolium against E. coli (MIC, 256 µg/ml) and Staphylococcus aureus (MIC 64 µg/ml) and Croton zenhtneri against S. aureus (MIC 64 µg/ml). CONCLUSION: Chemical tests indicated that a wide variety of natural product classes was present in those extracts that showed significant activities in the bioassays.

RESUMO

In this work, the chemical constituents, antibacterial and modulatory activities of the essential oil of Lantana camara Linn were studied. The essential oil was extracted from the leaves of L. camara by hydrodistillation method using Clevenger's apparatus and its chemical constituents were separated and identified by GC-MS, and the relative content of each constituent was determined by area normalization. Among the 25 identified components, bicyclogermacrene (19.42%), isocaryophyllene (16.70%), valecene (12.94%) and germacrene D (12.34%) were the main constituents. The oil was examined to antibacterial and modulatory activities against the multiresistant strains of Escherichia coli and Staphylococcus aureus by microdilution test. The results show an inhibitory activity to E. coli (MIC 512 mug/ml) and S. aureus (MIC 256 mug/ml). The synergism of the essential oil and aminoglycosides was verified too, with significant reduction of MICs (7 x, 1250-5 mug/ml) against E. coli. It is suggested that the essential oil of Lantana camara Linn could be used as a source of plant-derived natural products with resistance-modifying activity.

RESUMO

Momordica charantia L. belongs to the family Curcubitaceae and it is very common in many Brazilian regions. The plant is a liana with flowers and yellow fruits that present red seeds when are ripe. Popularly known as "melão-de-sãocaetano", "melão amargo" or "cabaço-amargo", it possesses many uses: antidiabetic, antihelmintic, antmicrobial, anticancerigenous and antioxidant. The phytochemical prospection of the fresh and dried leaves extracts showed the presence of different classes of secondary metabolites, as flavonoids, alkaloids and tannins, that have demonstrated antimicrobial action. Fresh and dried leaves presented significantly antimicrobial activity against all bacterial strains tested, specially Escherichia coli. Ethyl acetate fractions were effective against Escherichia coli and Bacillus cereus. The modulatory activity was significative too.

RESUMO

This study was aimed to clarify the mechanism of gastroprotection by Vanillosmopsis arborea Baker essential oil (EOVA) using ethanol-induced gastric mucosal damage in mice. Gastric lesions were significantly reduced by EOVA (200 and 400 mg/kg). Chemical analysis showed that the major compound of EOVA was alpha-bisabolol. Pretreatment of mice with yohimbine, the alpha2-antagonist, greatly suppressed the gastroprotective effect of OEVA. Furthermore, OEVA gastroprotection was not attenuated in mice pretreated with indomethacin, L-NAME or glibenclamide, the respective inhibitors of cyclooxygenase, nitric oxide synthase and K(+)(ATP) channel activation. These data suggest that OEVA affords gastroprotection most possibly by alpha2-receptor activation.

Assuntos

Antagonistas Adrenérgicos alfa/farmacologia , Antiulcerosos/farmacologia , Asteraceae , Mucosa Gástrica/efeitos dos fármacos , Óleos Voláteis/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Animais , Antiulcerosos/antagonistas & inibidores , Antiulcerosos/uso terapêutico , Asteraceae/química , Inibidores Enzimáticos/farmacologia , Etanol , Glibureto/farmacologia , Indometacina/farmacologia , Masculino , Camundongos , Modelos Animais , Sesquiterpenos Monocíclicos , NG-Nitroarginina Metil Éster/farmacologia , Óleos Voláteis/química , Óleos Voláteis/uso terapêutico , Casca de Planta , Sesquiterpenos/análise , Úlcera Gástrica/prevenção & controle , Ioimbina/farmacologia

RESUMO

The anti-inflammatory pentacyclic triterpene, oleanolic acid (OA) was examined on acute nociception induced by intraplantar injection of capsaicin in mice. OA administered orally to mice at 10, 30 and 100 mgkg(-1), significantly attenuated the paw-licking response to capsaicin (1.6 microg/paw) by 53%, 68.5% and 36.6%, respectively. Ruthenium red (3 mgkg(-1), s.c.), a non-competitive vanilloid receptor (V1, TRPV1)-antagonist also suppressed the capsaicin nociception by 38.6%. The maximal antinociception produced by 30 mgkg(-1) OA was significantly blocked in animals pre-treated with naloxone (2 mgkg(-1), i.p.), the opioid antagonist; l-arginine (600 mgkg(-1), i.p.), the substrate for nitric oxide synthase; or glibenclamide (2 mgkg(-1), i.p.), the K(ATP)-channel blocker, but was unaffected by yohimbine (2 mgkg(-1), i.p.), an alpha(2)-adrenoceptor antagonist. In open-field and rota-rod tests that detect motor deficits, mice received 30 mgkg(-1) OA did not manifest any effect per se, indicating that the observed antinociception is not a consequence of motor abnormality. These data suggest that OA inhibits capsaicin-evoked acute nociception due to mechanisms possibly involving endogenous opioids, nitric oxide, and K(ATP)-channel opening.

Assuntos

Capsaicina/antagonistas & inibidores , Ácido Oleanólico/farmacologia , Dor/induzido quimicamente , Dor/tratamento farmacológico , Antagonistas Adrenérgicos alfa/farmacologia , Analgésicos Opioides/farmacologia , Animais , Capsaicina/farmacologia , Corantes , Inibidores Enzimáticos/farmacologia , Glibureto/farmacologia , Hipoglicemiantes/farmacologia , Canais KATP , Lamiaceae/química , Masculino , Camundongos , Morfina/farmacologia , Atividade Motora/efeitos dos fármacos , NG-Nitroarginina Metil Éster/farmacologia , Naloxona/farmacologia , Antagonistas de Entorpecentes/farmacologia , Medição da Dor/efeitos dos fármacos , Equilíbrio Postural/efeitos dos fármacos , Canais de Potássio Corretores do Fluxo de Internalização/efeitos dos fármacos , Canais de Potássio Corretores do Fluxo de Internalização/metabolismo , Rutênio Vermelho , Ioimbina/farmacologia

RESUMO

In recent years, there has been a renewed interest in the search for novel natural substances active against erectile dysfunction. Plants that belong to the genus Aspidosperma (Apocyanaceae) are known to be very rich in indole alkaloids and have an ethnomedical history of use as traditional remedies for erectile dysfunction. This study examined whether the indole alkaloidal rich fraction (F(3-5)) from Aspidosperma ulei Markgr. root bark could manifest penile erection-related behavioral responses (penile erection, erection-like and genital grooming) in mice. Intraperitoneal injection of F(3-5) (25 and 50mg/kg) elicited all the three different behavioral responses in a manner similar to yohimbine (2mg/kg, i.p.), a known indole alkaloid. Seventy-five percent of mice treated with yohimbine or F(3-5) showed penile erections, which were completely blocked by clonidine, an alpha-2-adrenoceptor agonist and haloperidol, a dopaminergic antagonist and as well as by l-NAME, a nitric oxide synthase inhibitor. These results point out that F(3-5) facilitates penile erection in mice possibly through the activation of central dopamine and blockade of presynaptic alpha-2 adrenoceptors with a subsequent enhancement in nitric oxide release from the penile nerves and arteries. This study further supports the traditional use of extracts from Aspidosperma species in erectile dysfunction.

Assuntos

Aspidosperma , Ereção Peniana/efeitos dos fármacos , Animais , Masculino , Camundongos , Ereção Peniana/fisiologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Raízes de Plantas