Scielo RSS <![CDATA[Revista Brasileira de Farmacognosia]]> vol. 21 num. 6 lang. en <![CDATA[SciELO Logo]]> <![CDATA[<b>The last issue of 2011</b>]]> <![CDATA[<b>Contribution for the phytochemical studies of <i>Ageratum fastigiatum</i></b>]]> Organic extracts from leaves plus branches plus inflorescences of Ageratum fastigiatum (Gardner) R. M. King & H. Rob., Asteraceae, were fractionated through classic chromatography. The steroids stigmasterol, chondrillasterol and campesterol were isolated from hexane extract. The triterpenes lupeol, taraxasterol, α-amyrin, β-amyrin, pseudotaraxasterol, lupeol acetate and α-amyrin acetate were isolated from ethyl acetate extract. Steroids and triterpenes were identified by GC-MS. The coumarin ayapin was isolated from ethanol extract and identified by NMR. Essential oils of the fresh leaves and fresh inflorescences were obtained by hydrodistillation and analyzed for GC-MS. The main components in both essential oils were α-pinene, limonene and germacrene D. <![CDATA[<b>Composition, antioxidant and chemotherapeutic properties of the essential oils from two <em>Origanum</em> species growing in Pakistan</b>]]> The GC-MS analyses of Origanum majorana L. (OME) and Origanum vulgare L. (OVE), Lamiaceae, essential oils helped identification of 39 (96.4% of the total oils) and 43 (92.9% of the total oils) components, respectively. The major constituents of OME were terpinene-4-ol (20.9%), linalool (15.7%), linalyl-acetate (13.9%), limonene (13.4%) and α-terpineol (8.57%), whereas, thymol (21.6%), carvacrol (18.8%), o-cymene (13.5%) and α-terpineol (8.57%) were the main components of OVE. In the disc diffusion and the resazurin microtitre assays, OME showed better antibacterial activity than OVE with larger zones of inhibition (16.5-27.0 mm) and smaller MIC (40.9-1250.3 μg/mL) against the tested bacterial strains. Only OVE displayed anti-heme biocrystallization activity with an IC50 at 0.04 mg/mL. In the DPPH assay, OVE showed better radical-scavenging activity than OME (IC50=65.5 versus 89.2 μg/mL) and both OME and OVE inhibited lionleic acid oxidation. However, in the bleaching β-carotene assay, OVE exhibited better antioxidant activity than OME. In the MTT assay, OME was more cytotoxic than OVE against different cancer cell types, such as MCF-7, LNCaP and NIH-3T3, with IC50s of 70.0, 85.3 and 300.5 μg/mL, respectively. Overall, some components of OME and OVE may have antiparasitic and chemotherapeutic activity. <![CDATA[<b>Chalcones from <i>Myracrodruon urundeuva</i> are efficacious in guinea pig ovalbumin-induced allergic conjunctivitis</b>]]> The objective of the study was to verify the effects of dimeric chalcones (urundeuvines A, B, and C) from Myracrodruon urundeuva Allemão, Anacardiaceae (a Brazilian anti-inflammatory species), on an allergic conjunctivitis model. Male guinea-pigs were sensitized with two intraperitoneal injections of ovalbumin (10 μg dissolved in 0.5 mL saline and emulsified in 0.5 mL Freund's adjuvant), at days 0 and 7. At day 24, the animals were submitted to an ocular instillation (right eyes) with ovalbumin. At the next day, the animals were treated with chalcones (0.5 mg, three times a day for 7 days), 0.1% fluormetalone acetate (0.05 mg, as the reference drug) or saline. After anesthesia of the animals, enucleations of their corneas and conjunctivas were carried out for morphometric and histological analyses, at days 1, 3 and 7. Their radical scavenging activity and action on myeloperoxidase were also determined. We demonstrated that chalcones from M. urundeuva stem barks presented anti-inflammatory and antioxidant effects, and drastically inhibited the MPO activity, pointing them as candidates for the treatment of allergic conjunctivitis and other inflammatory conditions. <![CDATA[<b>Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin</b>]]> Cancer constitutes the second main mortality cause in the world, after cardiovascular diseases. In spite of the progresses in the chemotherapeutics treatments, many patients fail chemotherapy, mainly because of side effects or multi-drugs resistance, proving the need and importance of the research for new molecules with anticancer activity, more effective and with smaller adverse effects. Various compounds derived from plant secondary metabolites are commonly used in the chemotherapy against cancer and the natural products play an important role in the research for new molecules. Among several molecules of natural origin evaluated by MTT assay in murine tumor cell lines [breast (LM3) and lung (LP07)] the quinona-methide triterpenes tingenone and pristimerin showed marked cytotoxic activity presenting IC50 around 2 and 5 µM respectively. The structure-activity relationship suggests that rings A and B containing an α, ß-unsaturated carbonyl group are essential for the observed cytotoxic activity. The interaction between these positions and acetylcisteyne residues suggests a probable mechanism of action. The in vitro mutagenic activity was also evaluated by the Salmonella microsome assay (Ames test) for pristimerin and tingenone with and without metabolic activation (S9) in the strains TA98, TA97a, TA100 and TA102, none of which showed mutagenic potential in any strains. Estrogenic and anti-estrogenic activities were also studied by the e-screen assay in MCF-7 cells with negative results. The present data point to the importance of pristimerin and tingenone as representative of an emerging class of potential anticancer chemicals. <![CDATA[<b>Constituents and antiproliferative activity of extracts from leaves of <i>Croton macrobothrys</i></b>]]> Croton macrobothrys Baill, Euphorbiaceae, is a tree from the Atlantic Forest in Southern Brazil, used in traditional medicine and popularly known as "dragon's blood" and "pau-sangue". Leaf n-hexane, dichloromethane and methanol extracts were analyzed by GC/MS and evaluated for their in vitro antiproliferative activity on cell lines 786-0 (kidney), HT-29 (colon), K562 (leukemia), NCI-ADR/RES (drug resistant ovary), NCI-H460 (lung), MCF-7 (mammary), PC-3 (prostate), OVCAR-3 (ovary), U251 (glioma) and UACC-62 (melanoma). The dicloromethane extract exhibited activity against all cell lines at the concentration 25 µg/mL, in particular on cell lines NCI-H460 (GI50 0.33 μg/mL) and K5662 (GI50 0.91 μg/mL). Relevant constituents in dichloromethane extract are the alkaloids corydine and salutaridine, as well as the diterpenes geranylgeraniol and crotonin-derived clerodanes. <![CDATA[<b>Anti-oxidative and anti-ulcerogenic activity of <i>Ipomoea imperati</i></b>]]> Ipomoea imperati (Vahl) Griseb., Convolvulaceae, is used in traditional medicine for the treatment of inflammation, swelling and wounds, as well as to treat pains and stomach problems. This work evaluates the anti-oxidative activity by ESR (Electron Spin Resonance spectroscopy) and the preventive and curative actions of I. imperati in gastric ulcer animal model. Ipomoea imperati (200 mg/kg, p.o.) prevented the formation of gastric lesions in 78% (p<0.05) when compared with the negative control tween 80. Lanzoprazole, prevented in 85% the gastric lesions formation induced by ethanol (p<0.05). Therefore, the oral administration of I. imperati one hour before the ulcerogenic agent prevented the ulcer formation, conserving the citoprotection characteristics of the gastric mucosa and assuring the integrity of gastric glands and gastric fossets. The healing activity of I. imperati (200 mg/kg, p.o.) evaluated in chronic ulcer experiments induced by the acetic acid, was 72% (p<0.05). The positive control, ranitidine, healed 78% of the gastric lesions (p<0.05). The histological analysis confirmed the recovery of the mucosal layer and the muscle mucosal layer harmed by the acetic acid. Experiments in vitro with DPPH (2.2-diphenyl-1-picrylhydrazyl) of anti-oxidative activity demonstrated that I. imperati presents an IC50 of 0.73±0.01 mg/mL. <![CDATA[<b>Evaluation of antimalarial, free-radical-scavenging and insecticidal activities of <i>Artemisia scoparia</i> and <i>A. Spicigera</i>, Asteraceae</b>]]> Artemisia species (Asteraceae), widespread throughout the world, are a group of important medicinal plants. The extracts of two medicinal plants of this genus, Artemisia scoparia Waldst. & Kit. and A. spicigera C. Koch, were evaluated for potential antimalarial, free-radical-scavenging and insecticidal properties, using the heme biocrystallisation and inhibition assay, the DPPH assay and the contact toxicity bioassay using the pest Tribolium castaneum, respectively. The methanol extracts of both species showed strong free-radical-scavenging activity and the RC50 values were 0.0317 and 0.0458 mg/mL, respectively, for A. scoparia and A. spicigera. The dichloromethane extracts of both species displayed a moderate level of potential antimalarial activity providing IC50 at 0.778 and 0.999 mg/mL for A. scoparia and A. spicigera, respectively. Both species of Artemisia showed insecticidal properties. However, A. spicigera was more effective than A. scoparia. <![CDATA[<b><i>Pentaclethra macroloba</i></b><b> tannins fractions active against methicillin-resistant staphylococcal and Gram-negative strains showing selective toxicity</b>]]> The ethanol extract of the vegetal species Pentaclethra macroloba (Willd.) Kuntze, Fabaceae, was fractioned and the antibacterial activity was determined. The active ethyl acetate (ea) fraction showed activity against Gram-positive (Staphylococcus spp. and Enterococcus spp.) and Gram-negative (Pseudomonas aeruginosa, Acinetobacter spp. and Klebsiella pneumoniae) multiresistant bacteria. Gallic acid derivatives were identified as the main compounds in inactive subfractions from the ea fraction, while the active one afforded ellagic acid as the major constituent when submitted to acid hydrolysis reaction, which suggests the presence of hydrolysable tannins. The minimum bactericidal concentration analysis showed a bactericide mechanism of action for the tannin subfraction found. The antibacterial mechanism of action of the active tannin subfraction against S. aureus reference strains (ATCC 29213 e 33591) was proposed adopting an in vitro assay of protein synthesis inhibition. For this, bacterial cells were labeled with [35S] methionine in the presence of the subfraction. The protein synthesis inhibition was observed at 256 µg/mL of this subfraction. At this concentration it did not present cytotoxicity in eukaryotic cells by the neutral red technique, suggesting selective toxicity. The present study is the first in vitro investigation of the antibacterial properties of tannin fractions obtained from a polar extract of P. macroloba. <![CDATA[<b>Protective action against chemical-induced genotoxicity and free radical scavenging activities of Stryphnodendron adstringens ("barbatimão") leaf extracts</b>]]> The present study describes for the first time the antigenotoxic and antioxidant properties of Stryphnodendron adstringens (Mart.) Coville, Fabaceae ("barbatimão") leaves. The aqueous (AEB), water fraction (WFB) and ethanolic (EEB) extracts of leaves were obtained and they presented high content of phenolic compounds, flavonoids and proanthocyanidins. WFB and EEB inhibited the genotoxicity induced by cyclophosphamide. WFB inhibited the DNA lesion formation and both WFB and EEB decreased significantly (p<0.05) micronucleus formation. All extracts also showed high DPPH radical scavenging activity and reducing power. In conclusion all extracts presented antioxidant activity and WFB and EEB protected cells from genotoxicity induced by cyclophosphamide in rat bone marrow cells. Thus, our results support the beneficial effects of the barbatimão extracts as an anticarcinogenic agent. <![CDATA[<b>Effect of ethyl acetate extract from husk fiber water of <i>Cocos nucifera</i> in <i>Leishmania braziliensis</i> infected hamsters</b>]]> The objective of this study was to evaluate the treatment with ethyl acetate extract (EAE) from husk fiber water of Cocos nucifera L., Arecaceae, in L. braziliensis (Lb) infected hamsters. Twelve male hamsters were randomly allocated in three groups (n=4): G1 received only EAE; G2 was infected with Lb only and G3 received EAE after Lb infection. The infection was carried 28 days prior to the treatment with EAE, which was administrated (0.2 mL, 300 for 21 consecutive days. Infection was evaluated through skin lesions and infected footpad edema. Haematological evaluation was done on -28th, 0 and 21st days. Imprint footpad and lymph node weight were evaluated on 21st day. Lb infection significantly inhibited the peripheral leukocytes blood. However, neutrophils and lymphocytes values did not have significant alterations. G3 presented eosinophilia in relation to G2. The treatment with EAE did not reduce edema of infected footpad neither weight of drainage lymph node. Infected footpad imprints revealed amastigotes forms and cellular infiltration. Animals from G3 presented skin lesions on 7th day, shown a reduction of these lesions in day 14. Therefore, the treatment with EAE did not alter the etiological agent elimination in these conditions. However, EAE presents a healing activity in this experimental model. <![CDATA[<b>Antimicrobial activity, cytotoxicity and intracellular growth inhibition of Portuguese <i>Thymus</i> essential oils</b>]]> Thyme essential oils are well recognized by their excellent biological activities and the antimicrobial activity of Portuguese thyme essential oils has been investigated with promising results, particularly against food borne pathogens. In this study the potential antimicrobial activity of the essential oils of five species of Thymus (Lamiaceae), namely Th. caespititius Brot., Th. camphoratus Hoffmanns. & Link, Th. capitellatus Hoffmanns. & Link., Th. carnosus Boiss. and Th. zygis L. was evaluated against Candida albicans, Haemophilus influenza, Helicobacter pylori, Listeria monocytogenes, Salmonella enterica and Streptococcus pneumoniae. H. pylori strains were the most susceptible bacteria, particularly to the essential oils of Th. caespititius (Planalto Central), Th. zygis (Rebordãos) and Th. caespititius (Pico) which minimum inhibitory concentration (MIC) values ranged from 0.05 to 0.08 mg.mL-1. Th. caespititius essential oil from Planalto Central or its main component, carvacrol significantly (p<0.05) inhibited the intracellular growth of H. pylori, and showed no citotoxicity to the gastric cell line. Our results suggest the potential of this essential oil and its main component as a promising tool as anti-Helicobacter agent potentiating the eradication of this important gastroduodenal pathogen. <![CDATA[<b>Antitumorigenicity of xanthones-rich extract from <em>Garcinia mangostana</em> fruit rinds on HCT 116 human colorectal carcinoma cells</b>]]> This study aimed to investigate the antitumorigenicity of xanthones-rich extract from Garcinia mangostana L., Clusiaceae, fruit rinds which was obtained by a simple recrystallization of 75% ethanolic extract. α-Mangostin content of the extract was determined qualitatively by TLC and quantitatively by HPLC, and total xanthones content was quantified by UV spectrophotometry. The extract was evaluated for cytotoxicity, apoptosis and antitumorigenicity on HCT 116 human colorectal carcinoma cells. α-Mangostin was found to be the main constituent of the extract which was 71.2±0.1%, and the total xanthones content was 95±4.8% (wt/wt). The extract showed potent dose dependent cytotoxicity with IC50 value 9.2 μg/mL. Apoptosis studies revealed activation of caspases 3 and 7, DNA fragmentation, chromatin condensation and loss of mitochondrial membrane potential. Studies on cell migration and colony formation indicate reduced cell migration ability and clonogenicity of treated HCT 116 cells at sub-inhibitory concentrations. Taken together, the cytotoxic effect of the xanthones extract is mediated through the mitochondrial pathway of apoptosis. The reduced cell migration and clonogenicity of HCT 116 cells might prevent both primary and metastatic tumor growth in vivo which will be the topic of our future work using the metastatic orthotopic colon cancer model. <![CDATA[<b>Xylodiol from <i>Xylopia langsdorfiana </i> induces apoptosis in HL60 cells</b>]]> An atisane diterpene was isolated from Xylopia langsdorfiana St. Hilaire & Tulasne, Annonaceae, leaves, ent-atisane-7α,16α-diol (xylodiol). Preliminary study showed that xylodiol was cytotoxic and induced differentiation on human leukemia cell lines. However, the molecular mechanisms of xylodiol-mediated cytotoxicity have not been fully defined. Thus, we investigated the anti-tumor effect of xylodiol in human leukemia HL60 cell line. Xylodiol induced apoptosis and necrosis. HL60 cells treated with xylodiol showed biochemical changes characteristic of apoptosis, including caspases-8, -9 and -3 activation and loss of mitochondrial transmembrane potential (∆ Ψm). However, there was a condensation rather than swelling of mitochondria. Moreover, the formation of condensed mitochondria and the loss of ∆ Ψm occurred downstream of caspase activation. Cyclosporine A did not protect HL60 cells from the cytotoxic effects of xylodiol, suggesting that the loss of ∆ Ψm is a late event in xylodiol-induced apoptosis. Oxidative stress was involved in xylodiol-induced apoptosis. Thus, we conclude that activated caspases cleave cellular proteins resulting in mitochondrial damage leading to mitochondrial condensation, loss of ∆ Ψm and ROS release from the mitochondria. ROS can further induce and maintain a collapse of ∆ Ψm leading to cellular damage through oxidation of lipids and proteins resulting in apoptotic cell death. <![CDATA[<b><i>Ocimum basilicum</i></b><b> leaf essential oil and (-)-linalool reduce orofacial nociception in rodents</b>: <b>a behavioral and electrophysiological approach</b>]]> The present study investigated the antinociceptive effects of Ocimum basilicum L. (Lamiaceae) leaf essential oil (LEO) and (-)-linalool (LIN) in formalin (2%)-, glutamate (25 µM)- and capsaicin (2.5 µg)- induced orofacial nociception models in mice. The involvement of these substances was further evaluated on the neuronal excitability of the hippocampal dentate gyrus. Male mice (n=8/group) were pretreated separately with LEO and by LIN (50, 100, and 200 mg/kg, i.p.), morphine (5 mg/kg, i.p.) and vehicle (saline + Tween 80 0.2%), before injection of nociceptive agent into the right upper lip (perinasal area). The LEO and LIN reduced the nociceptive face-rubbing behaviour in both phases on formalin test. LEO and LIN, at high doses, produced significantly antinociceptive effect in the capsaicin and glutamate tests. In hippocampal slices, LEO inhibited the population spike generated by stimulation of the hylus (antidromic stimulation), with an IC50 of 0.1±0.05 mg/mL. This response was reversibly blocked by lidocaine (0.5 mg/mL), a known voltage-dependent sodium channel antagonist and by LIN (0.5 mg/mL). Our results suggest that LEO and LIN modulate neurogenic and inflammatory pain in the tests of orofacial nociception induced by formalin, capsaicin and glutamate. Part of these effects may be associated with decreased peripheral and central neuronal excitability. <![CDATA[<b>Further studies on membrane stabilizing, anti-inflammatory and FCA induced arthritic activity of various fractions of bark of <i>Machilus macrantha</i> in rats</b>]]> Machilus macrantha Nees, Lauraceae, bark is traditionally used in the treatment of asthma, tuberculosis and rheumatoid arthritis. In order to validate, mechanism based anti-inflammatory activity of fractions M. macrantha bark are investigated for first time. Test materials viz. petroleum ether (PE), alkaloidal fraction (CH), acetone extracts (TAN) and mucilage (MM) (250 and 500 mg/kg, p.o.) obtained from M. macrantha bark were tested for membrane stabilizing, anti-nociceptive; anti inflammatory and Freund's complete adjuvant (FCA) induced arthritis activity. Diclofenac sodium and morphine were used as the reference standards in pharmacological assay. Test materials have significantly (p<0.01) inhibited paw edema after Carrageenan and histamine induction at higher doses. Administration of test materials of M. macrantha (250 and 500 mg/kg b.w.) significantly reduced abdominal writhing, formalin nociception, cotton pellet granuloma and vascular permeability in experimental animal. In addition to this, bark of M. macrantha showed chronic anti-rheumatic effect by suppressing the swelling volume, arthritis index, hematological and biochemical parameters (ESR, RA factor, CRP, liver transferase enzyme) in FCA-induced arthritis. It also significantly inhibited protein denaturation, heat-induced haemolysis of RBC and reduction in total leukocyte migration. Bioassay guided fractionation of the pet. ether extract of bark of M. macrantha led to isolation and characterization of β-sitosterol and stigma sterol confirmed by its HPLC, NMR and GC-MS study. In conclusion, extracts of M. macrantha bark can be explored as a therapeutic agent for the treatment of acute and chronic arthritis. <![CDATA[<b>Neurobehavioral, reflexological and physical development of Wistar rat offspring exposed to ayahuasca during pregnancy and lactation</b>]]> Ayahuasca is a hallucinogenic beverage prepared by the decoction of plants native to the Amazon Basin region. The beverage has been used throughout the world by members of some syncretic religious movements. Despite the recent legalization of ayahuasca in Brazil for religious purposes, there is little pre-clinical and clinical information attesting to its safety, particularly in relation to the use during pregnancy. The aim of the current work was to determine the effects of perinatal exposure to ayahuasca (from the 6th day of pregnancy to the 10th day of lactation) on physical, reflexology and neurobehavioral parameters of the Wistar rat offspring. The offspring showed no statistically significant changes in the physical and reflexology parameters evaluated. However, in adult rats, perinatally exposed to ayahuasca, an increase in frequency of entries in open arms in elevated plus-maze test, a decrease in total time of interaction in social interaction test, a decrease in time of latency for the animal to start swimming and a decrease of the minimum convulsant dose induced by pentylenetetrazol were observed. In conclusion, our results showed that the use of ayahuasca by mothers during pregnancy and lactation reduced the general anxiety and social motivation of the rat offspring. Besides, it promoted a higher sensitivity for initiation and spread of seizure activity. <![CDATA[<b>Antinociceptive and anti-inflammatory effects of <i>Caesalpinia pyramidalis</i> in rodents</b>]]> Caesalpinia pyramidalis Tul., Fabaceae, is a plant with an anti-inflammatory activity that is used in folk medicine. To evaluate the mechanism of action of this plant, studies were performed on its antinociceptive and anti-inflammatory properties using an ethanol extract (EE) made from the inner bark. Oral treatment of mice with the EE (100, 200, and 400 mg/kg) decreased their acetic acid-induced abdominal writhes (p<0.001) and their formalin-induced paw licking in both the first and second phases (p<0.001). This treatment increased the reaction time of mice on the hot-plate test (400 mg/kg, p<0.05); however, it did not alter their performance on the Rotarod performance test. The carrageenan-induced paw edema in the rats and the leukocyte migration into the peritoneal cavity of the mice were also reduced by the EE given at a dose of 400 mg/kg (p<0.05). In addition, the EE (100-400 mg/kg, v.o.) did not alter the arterial pressure of non-anesthetized rats. In conclusion, the EE of C. pyramidalis shows antinociceptive and anti-inflammatory activities in rodents, supporting the usage of this plant to treat various inflammatory diseases for which it has traditionally been used. <![CDATA[<b>Antitumor and immunomodulatory effects of the naphthoquinone 5-methoxy-3,4-dehydroxanthomegnin</b>]]> Large number of quinones has been associated with antitumor, antibacterial, antimalarial and antifungal activities. In this work we describe the effect of the naphthoquinone, 5-methoxy-3,4-dehydroxanthomegnin, on murine tumor cells (LP07 and LM2) and its immunomodulatory effect on nitric oxide (NO) production on LPS-stimulated macrophages. The results have shown that 5-methoxy-3,4-dehydroxanthomegnin was a significant inhibitor of LPS-stimulated NO generation from macrophage (inhibition percentage ranged from 97.4 to 98.9%) and a strong cytotoxic agent against both tumor cells LP07 and LM2 (CI50 6.2±0.36 µM and 74.6±1.9 µM, respectively). These results indicate that the 5-methoxy-3,4-dehydroxanthomegnin may show promising activity in the treatment of murine breast and lung cancer by immunomodulatory and antiproliferative activities. <![CDATA[<b>Antiulcerogenic activity of the extracts of <i>Struthanthus marginatus</i></b>]]> The gastroprotective action of the aqueous extract (AE) and the hydroalcoholic extract obtained from the leaves of Struthanthus marginatus (Desr.) Blume, Loranthaceae, were performed with in vivo models in rodents using: ethanol, indomethacin or stress-induced ulcers, determination of gastric secretion and the mucus production. The scavenger activity of AE in vitro was tested by the DPPH method. The treatment with the extracts (125-1000 mg/kg) significantly inhibited ulcerative lesions in comparison with the negative control groups in all the models evaluated and demonstrated greater effectiveness of the aqueous extract. Regarding the model of gastric secretion, a reduction in volume of gastric juice and total acidity was observed, as well as an increase in the gastric pH. The treatment of rats raised the gastric mucus production. Significant DPPH scavenging activity was evident in the AE. No sign of toxicity was observed. These results show that S. marginatus possesses gastroprotective activity. There are indications that the mechanisms involved in anti-ulcer activity are related to a decrease in acid secretion and an increase in gastric mucus content. Also, there is evidence for the involvement of antioxidant activity in the gastroprotective mechanism. <![CDATA[<b>Pharmacognostical, antioxidant and antiulcer screening of <i>Cyclea peltata</i> roots</b>]]> Cyclea peltata Hook. f. & Thomson, belongs to the family Menispermaceae commonly known as "paatha", is a climbing shrub found throughout South and East India. In Indian traditional medicine the tuberous roots are also used to treat jaundice, stomachache, fever and asthma. This study deals with the microscopic study of leafs and roots of C. peltata, along with the physico-chemical, preliminary phytochemical analyses and antioxidant properties. Acute oral toxicity study was conducted as per OECD-423 guidelines and the extract was found to be devoid of any conspicuous acute toxicity in extract treated animals and no mortality upto 2 g/kg by oral route. Hydroalcoholic extract of C. peltata in a dose dependant manner (125 and 250 mg/kg. p.o.) showed significant gastric protection against the ethanol-induced gastric ulcer model in rats. <![CDATA[<b>Evaluation of effects of dichloromethane fraction from <em>Platonia insignis</em> on pilocarpine-induced seizures</b>]]> The objective of present study was to evaluate the antioxidant and anticonvulsant activities of dichloromethane fraction (DMF) from Platonia insignis Mart., Clusiaceae. The DMF from P. insignis (2 mg/kg) was tested by intraperitoneal (i.p.) to evaluate effects on lipid peroxidation level, nitrite formation, as well as on locomotor and anticonvulsant activities. Wistar rats were treated with, (saline/Tween 80 0.5%, i.p., control group), DMF (2 mg/kg, i.p., DMF group), pilocarpine (400 mg/kg, i.p., P400 group), or the combination of DMF (2 mg/kg, i.p.) and pilocarpine (400 mg/kg, i.p., DMF plus P400). After the treatments all groups were observed for 24 h. In P400 group rats there was a decrease in the motor activity when compared with control group. In DMF plus P400 co-administered rats was observed an increase in motor activity when compared with P400 group. In P400 group rats there was a significant increase in lipid peroxidation and nitrite levels. In DMF plus P400 co-administered rats, antioxidant treatment significantly reduced the lipid peroxidation level and nitrite content after seizures. Previous findings strongly support the hypothesis that oxidative stress occurs in rat striatum during pilocarpine-induced seizures, and our results imply that strong neuprotective effect on this brain region could be achieved using DMF from P. insignis. <![CDATA[<b>Report of cases in patients with acute herpetic neuralgia using a <i>Mangifera indica</i> extract</b>]]> It has been accepted that neuroinflammation, oxidative stress and glial activation are involved in the central sensitization underlying neuropathic and inflammatory pain. Vimang® is the brand name of an aqueous extract of Mangifera indica L., Anacardiaceae, traditionally used in Cuba for its antioxidant, antiinflammatory, analgesic, and immunomodulatory properties. In the present study, we determined the possible effects of Vimang formulations in acute herpes zoster (n=12) patients, that received a daily dose of 1800 mg of extract (two coated Vimang tablets, 300 mg each, three times daily before meals) associated to low doses of amitriptyline (10-25 mg/d). In addition to the tablets, they utilized compresses containing Vimang dissolution at 2% on skin lesions for thirty days. The average daily pain score using a Likert scale and variations in concomitant drug daily dosage were determined. The analgesic effect was observed from week 1 (p<0.001) with respect to baseline data and none showed post-herpetic neuralgia. Significant reduction of antidepressant medication (p<0.01) and analgesic rescue dosages (p=0.0035) with respect to the initial daily dosage were showed. No adverse events were reported. The results obtained in this report of cases suggest that Vimang supplementation might be beneficial to prevent and treat neuropathic pain. <![CDATA[<b>Gastric antiulcer and antiinflammatory activities of <i>Calotropis procera</i> stem bark</b>]]> In recent years, a widespread search has been launched to identify new antiinflammatory and antiulcer-drugs from natural sources. The study was aimed at evaluating the antiinflammatory and antiulcer activity of chloroform extract (CH) and hydroalcoholic extract (HE) of the stem bark of Calotropis procera (Aiton) W.T. Aiton, Apocynaceae, obtained successively by cold maceration. The antiinflammatory effect of the CH and HE extracts of the stem bark of the C. procera against carrageenan-induced paw oedema and also its antiulcer activity by using two acute models: Aspirin (100 mg/kg, p.o.) and ethanol (96%, 1 mL/200 g) in albino rats have been studied and found to be significant at 200 and 400 mg/kg when compared to the standard drugs. As a part of investigations to obtain compounds with antiinflammatory and antiulcer activity in this work, a bioassay was carried out with fractions obtained from chloroform extract with n-hexane (NF1), 1-butanol (BF1), ethyl acetate (EF1) and chloroform (CF1). The hydroalcoholic extract (HE) of the stem bark was fractionated with n-hexane (NF2), 1-butanol (BF2), ethyl acetate (EF2), chloroform (CF2) and water (WF2). The fractions were freeze-dried and evaluated for its antiinflammatory and antiulcer activity. Fractions NF1, CF1, BF2 and EF2 (20 mg/kg) showed significant antiinflammatory and antiulcer activity. The results obtained for antiulcer activity were also supported well by the histopathological examination of the open excised rat stomach. Further experiments are underway to determine which phytoconstituents are involved in antiinflammatory and antiulcer activities as well as mechanisms involved in gastroprotection. <![CDATA[<b>Influence of environmental factors on the concentration of phenolic compounds in leaves of <i>Lafoensia pacari</i></b>]]> Lafoensia pacari A. St.-Hil., Lythraceae, a plant from the Cerrado known as pacari or dedaleiro, is widely used as an antipyretic, wound healing, anti-inflammatory, antidiarrheal and in the treatment of gastritis and cancer. Notable among the metabolite groups identified in leaves of L. pacari are the polyphenols, such as tannins and flavonoids, related to the pharmacological activities of pacari. Studies on the influence of environmental factors over production of major groups of secondary metabolites in pacari are important because they contribute data for its cultivation and harvest, and establish quantitative parameters of secondary metabolites in the plant drug. The objective of this study was to evaluate the influence of environmental factors on concentrations of phenolic metabolites in the leaves of L. pacari. Compounds quantified in the leaves were: total phenols, tannins by protein precipitation, hydrolysable tannins, total flavonoids, ellagic acid and mineral nutrients, while soil fertility was also analyzed, all over a period of one year. The data were analyzed using multivariate analysis, and the results suggest that metabolite concentrations in the leaves of this plant are influenced by seasonal factors, in particular the temperature and foliar micronutrients (Cu, Fe, Mn, Zn). <![CDATA[<b><i>p</i>-Cymene reduces orofacial nociceptive response in mice</b>]]> This study investigated the possible antinociceptive effect of p-cymene in different tests of orofacial nociception. The animals (mice) were pretreated (i.p.) with p-cymene (25, 50, 100 mg/kg), morphine (5 mg/kg), or vehicle (0.2% Tween 80+saline), and were then subsequently administered, subcutaneously into their upper lip: formalin, capsaicin, and glutamate. The nociceptive behavior response was characterized by the time in s that the mice remained rubbing the orofacial region, for a period of 40 min in the formalin test (first phase, 0-6 min; and second phase, 21-40 min), and for 42 and 15 min in the capsaicin and glutamate tests, respectively. To verify the possible opioid involvement in the antinociceptive effects, naloxone (i.p.) was administered into the mice 15 min prior to the pretreatment with p-cymene (100 mg/kg). Finally, whether or not the p-cymene evoked any change in motor performance in the Rota-rod test was evaluated. The results showed that the treatment with p-cymene, at all doses, reduced (p<0.001) the nociceptive behavior in all nociception tests. The antinociceptive effect of p-cymene was antagonized by naloxone (1.5 mg/kg). Additionally, mice treated with p-cymene did not show any change in motor performance. In conclusion, p-cymene attenuated orofacial nociception, suggesting an involvement of the opioid system in this effect. Thus, p-cymene might represent an important biomolecule for management and/or treatment of orofacial pain. <![CDATA[<b>Evaluation of macro and microminerals in crude drugs and infusions of five herbs widely used as sedatives</b>]]> It has been determined the concentration of fourteen micro and macrominerals (Al, Ca, Co, Cr, Cu, Fe, K, Li, Mg, Mn, Na, P, Se, and Zn) in both crude drugs and infusions of Melissa officinalis L., Lamiaceae, Nepeta cataria L., Lamiaceae, Passiflora caerulea L., Passifloraceae, Tilia x moltkei Späth ex C.K. Schneid., Tiliaceae, and Valeriana officinalis L., Caprifoliaceae. These herbs are widely consumed by its sedative properties, either alone or in herb mixtures. All measurements were performed using an inductively coupled plasma optical emission spectrometer (ICP-OES). The products were obtained from regional markets, mainly in San Luis province (Argentina). The estimated daily intake was compared with current recommendations. All products and its infusions were included within the upper tolerable limits for minerals, in trace elements such as toxic elements present at low levels. <![CDATA[<b>Scent analysis of <i>Rosa laevigata</i> through metal oxide sensor array electronic nose</b>]]> The scent fingerprint of Rosa laevigata Michx., Rosaceae, samples harvested at different periods was investigated. Principal component analysis (PCA) and discriminant factor analysis (DFA) were done on the scent response values measured by an electronic nose (EN) sensor. Statistical quality control (SQC) analysis was also conducted. The R. laevigata samples were clustered into two categories after being analyzed by PCA and DFA. One cluster consisted of samples No. 1 to No. 6, and the other consisted of samples No. 7 to No. 10. The combination of EN, PCA, and DFA for scent analysis can be used for the quality control of traditional Chinese medicines. <![CDATA[<b>Anti-inflammatory activities of the hydroalcoholic extracts from <i>Erythrina velutina</i> and <i>E. mulungu</i> in mice</b>]]> This work studied the anti-inflammatory activities of the hydroalcoholic extracts (HAEs) from Erythrina velutina Willd. (Ev) and E. mulungu Mart. ex Benth. (Em) in the carrageenan- and dextran-induced mice hind paw edema models. These medicinal plants belonging to the Fabaceae family are used in some Brazilian communities to treat pain, inflammation, insomnia and disorders of the central nervous system. In the present work, the extracts were administered orally in male mice at the doses of 200 or 400 mg/kg. In the carrageenan-induced test, only Em showed anti-inflammatory activity, decreasing the paw edema, at the doses of 200 and 400 mg/kg. No effect was observed with Ev in this model. On the other hand, in the dextran model, Ev demonstrated anti-inflammatory effect, showing decrease of the paw edema at the 1, 2, 3, 4 and 24th h. Em (200 or 400 mg/kg) presented anti-inflammatory effect at the 2, 3 and 4th h after administration of dextran, as compared to control. In conclusion, the work showed that Ev and Em present anti-edematous actions, which possibly occurs by distinct mechanisms. While Ev seems to interfere especially in inflammatory processes in which mast cells have an important role, Em exerts greater activity in the inflammatory process that depends mainly on polymorphonuclear leucocytes. However, further studies are needed to determine the exact mechanism of action of the species investigated. <![CDATA[<b>Flavonoids and fatty acids of <i>Camellia japonica </i>leaves extract</b>]]> The ethanol extract from the leaves of Camellia japonica L., Theaceae, showed antiradical potential in the DPPH test using TLC plates (SiO2). Aiming the isolation of active compounds, this extract was partitioned between BuOH:H2O (1:1) and the two obtained phases were also evaluated to detection of antiradical activity. The active BuOH phase was fractionated in Sephadex LH-20 and silica (normal or reverse phase) to afford three aglycone flavonoids (quercetin, kaempferol and apigenin), which have been described in the C. japonica at first time, two glycosilated flavonoids (rutin and quercetrin), and a mixture of saturated fatty acids. The structures of isolated compounds were defined by NMR and GC/MS analyses. <![CDATA[<b>Herbs of interest to the Brazilian Federal Government</b>: <b>female reproductive and developmental toxicity studies</b>]]> In 2009 the Brazilian Ministry of Health published a document named RENISUS that lists 71 herbs traditionally used in Brazil that could result in phytomedicines to be dispensed by the governmental health care program. This manuscript reviews female reproductive and/or developmental toxicity information of these herbs. More than half (35) of the herbs lack information regarding female reproductive and/or developmental effects. From the fourteen herbs used traditionally to disturb female reproduction, five present experimental data corroborating their actions as abortifacients (Maytenus ilicifolia, Momordica charantia, Plectranthus barbatus, Ruta graveolens) or labour facilitator (Bidens pilosa). For 23 of the herbs evaluated experimentally for any type of female reproductive endpoint, only a single study was retrieved and at least twelve of these studies were conducted with a single dose. This scenario suggests that the scientific power of the published information is very low and that a scientifically-based risk/benefit analysis about the use of these herbs during pregnancy is not possible. Considering the appeal that phytomedicines have for pregnant women, usually aware and afraid of the risks that synthetic drugs may have in their pregnancy and progeny, well designed studies evaluating reproductive and/or developmental toxicity of these herbs urge. <![CDATA[<b>Embryotoxicity <i>in vitro</i> of <i>Indigofera suffruticosa</i> leaves extract on <i>Aedes aegypti</i></b>]]> In 2009 the Brazilian Ministry of Health published a document named RENISUS that lists 71 herbs traditionally used in Brazil that could result in phytomedicines to be dispensed by the governmental health care program. This manuscript reviews female reproductive and/or developmental toxicity information of these herbs. More than half (35) of the herbs lack information regarding female reproductive and/or developmental effects. From the fourteen herbs used traditionally to disturb female reproduction, five present experimental data corroborating their actions as abortifacients (Maytenus ilicifolia, Momordica charantia, Plectranthus barbatus, Ruta graveolens) or labour facilitator (Bidens pilosa). For 23 of the herbs evaluated experimentally for any type of female reproductive endpoint, only a single study was retrieved and at least twelve of these studies were conducted with a single dose. This scenario suggests that the scientific power of the published information is very low and that a scientifically-based risk/benefit analysis about the use of these herbs during pregnancy is not possible. Considering the appeal that phytomedicines have for pregnant women, usually aware and afraid of the risks that synthetic drugs may have in their pregnancy and progeny, well designed studies evaluating reproductive and/or developmental toxicity of these herbs urge.