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One of the major disadvantages of the current cancer therapy is the suppression of the immune system. Brazilian flora is considered one of the most diverse in the world and many plants were found to contain active constituents that can be valuable sources of new drugs. The plant Indigofera suffruticosa was studied to determine its potential to stimulate the immune system and also to be effective against tumour cells. We investigated the effects of the alkaloidal fraction and the pure alkaloid indigo obtained from I. suffruticosa on macrophage activation by measuring nitric oxide (NO) and tumour necrosis factor-α (TNF-α) production. Cytotoxic activity was also evaluated against the two tumour murine cells lines, LM2 (breast adenocarcinoma) and LP07 (lung adenocarcinoma). The alkaloidal fraction induced a high NO production and a moderated TNF-α release. The pure indigo demonstrated an elevated NO and TNF-α production. The fraction and the pure compound also exhibited cytotoxic activity against both adenocarcinoma cell lines and indigo showed the strongest cytotoxic activity with IC₅₀ value of 0.89 µg mL⁻¹ against LM2 and 1.44 µg mL⁻¹ against LP07. Our results presented the immunostimulatory and cytotoxic activity of I. suffruticosa, enhancing macrophage function and therefore contributing to the host defence against tumours.

Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-27T11:26:07Z No. of bitstreams: 0Bitstream added on 2014-05-27T14:36:26Z : No. of bitstreams: 1 2-s2.0-80455131271.pdf: 3278875 bytes, checksum: cd7d0c653950fdc25c8feb76e6844ea4 (MD5) Made available in DSpace on 2014-05-27T11:26:07Z (GMT). No. of bitstreams: 0 Previous issue date: 2011-11-09 Alchornea triplinervia (Spreng.) Muell. Arg (Euphorbiaceae) is a medicinal plant commonly used by people living in the Cerrado region of Brazil to treat gastrointestinal ulcers. We previously described the gastroprotective action of methanolic extract (ME) of Alchornea triplinervia and the ethyl acetate fraction (EAF) in increasing of prostaglandin E 2 (PGE 2) gastric levels in the mucosa. In this work we evaluated the effect of EAF in promoting the healing process in rats with acetic acid-induced gastric ulcers. In addition, toxicity was investigated during treatment with EAF. After 14 days of treatment with EAF, the potent stimulator of gastric cell proliferation contributed to the acceleration of gastric ulcer healing. Upon immunohistochemical analysis, we observed a pronounced expression of COX-2, mainly in the submucosal layer. The 14-day EAF treatment also significantly increased the number of neutrophils in the gastric mucosa regeneration area. The EAF induced angiogenesis on gastric mucosa, observed as an increase of the number of blood vessels supplying the stomach in rats treated with EAF. Oral administration for 14 days of the ethyl acetate fraction from Alchornea triplinervia accelerated the healing of gastric ulcers in rats by promoting epithelial cell proliferation, increasing the number of neutrophils and stimulation of mucus production. This fraction, which contained mainly phenolic compounds, contributed to gastric mucosa healing. © 2011 by the authors; licensee MDPI, Basel, Switzerland. Department of Physiology Univ. Estadual Paulista-UNESP, Rubião Junior, cp 510, CEP 18618-000, Botucatu, São Paulo Institute of Chemistry Univ. Estadual Paulista-UNESP, cp 355, CEP 14801-970, Araraquara, São Paulo Department of Morphology Univ. Estadual Paulista-UNESP, cp 610, CEP 18618-000, UNESP, Botucatu, São Paulo Department of Physiology Univ. Estadual Paulista-UNESP, Rubião Junior, cp 510, CEP 18618-000, Botucatu, São Paulo Institute of Chemistry Univ. Estadual Paulista-UNESP, cp 355, CEP 14801-970, Araraquara, São Paulo Department of Morphology Univ. Estadual Paulista-UNESP, cp 610, CEP 18618-000, UNESP, Botucatu, São Paulo

Made available in DSpace on 2013-09-27T14:53:42Z (GMT). No. of bitstreams: 1 WOS000297896500005.pdf: 678984 bytes, checksum: 248d5de1a91ef6e61afbcc9dc03582ab (MD5) Previous issue date: 2011-10-31 Made available in DSpace on 2013-09-30T18:37:23Z (GMT). No. of bitstreams: 1 WOS000297896500005.pdf: 678984 bytes, checksum: 248d5de1a91ef6e61afbcc9dc03582ab (MD5) Previous issue date: 2011-10-31 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T13:49:42Z No. of bitstreams: 1 WOS000297896500005.pdf: 678984 bytes, checksum: 248d5de1a91ef6e61afbcc9dc03582ab (MD5) Made available in DSpace on 2014-05-20T13:49:42Z (GMT). No. of bitstreams: 1 WOS000297896500005.pdf: 678984 bytes, checksum: 248d5de1a91ef6e61afbcc9dc03582ab (MD5) Previous issue date: 2011-10-31 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Ethnopharmacological relevance: Strychnos pseudoquina St. Hil. (Loganiaceae) is one Brazilian native medicinal species described in the first edition of the Brazilian Official Pharmacopoeia in 1929. This medicinal plant, popularly known as quina-quina, quina-branca or casca aromatica was very commonly used in folk medicine in tea form obtained from the bark and/or leaves as tonic, antipyretic, antimalarial and mainly against diseases of the liver, spleen and stomach.Aim of the study: Previous study already characterized the gastroprotective action of this species The aim of the present study is to elucidate the mechanism of the healing process mediated by the methanolic extract (ME) and their enriched alkaloid fraction (EAF) from Strychnos pseudoquina in chronic gastric ulceration induced by 5% acetic acid in rats, an experimental model that accurately reflects human gastrointestinal disease.Material and methods: The ME and EAF was administered orally in a single dose (based on previously study of dose-response curve) for 14 days after chronic ulceration was induced in rats. The healing effect of ME and EAF was evaluated by macroscopic and morphometric analyses, immunohistochemical assay (PCNA and SOD) and anti-Helicobacter pylori effect was evaluated by in vitro assay.Results: Our results demonstrated that EAF significantly reduced border internal (42%) and external (38%) lesion area (mm(2)) by macroscopic analyses (P

Ethnopharmacological relevance The species Qualea grandiflora and Qualea multiflora , which belong to the Vochysiaceae family, are common in the Brazilian savannah (Cerrado biome), and the local inhabitants use these species to treat external ulcers and gastric diseases and as an anti-inflammatory agent. Studies have demonstrated that these plants contain compounds that exhibit pharmacological activities; however, the risks associated with their consumption are not known. Material and methods In the present study, the mutagenicity of polar and apolar extracts from Qualea grandiflora and Qualea multiflora were assessed by employing the Ames assay with and without metabolic activation. Additionally, phytochemical analyses (HPLC–ESI-IT-MS, HPLC–UV-PDA and GC–IT-MS) were performed to identify the chemical constituents present in these species, including the evaluation of physico-chemical properties, such as polarity or apolarity of the organic compounds, which are related to each fraction obtained. These studies provide important information regarding the biochemical behaviour of these compounds. Results All extracts exhibited mutagenicity, inducing frameshift mutations and base substitutions in DNA. Phytochemical analysis identified terpenes, ellagic acid derivatives and phytosteroids. Conclusions The mutagenicity observed might be due to the presence of pentacyclic triterpenes and polyphenols, which are able to generate reactive oxygen species (ROS) and result in the potential to cause DNA damage. The genetic risk identified in this present work shows that special attention should be considered for the use of compounds obtained from these plant species in medicinal treatments. Further studies must be conducted to identify safe therapeutic doses.

Made available in DSpace on 2013-09-27T14:54:28Z (GMT). No. of bitstreams: 1 WOS000295236700022.pdf: 1054917 bytes, checksum: ade3c93db496ae9bfef43fc129742e42 (MD5) Previous issue date: 2011-09-01 Made available in DSpace on 2013-09-30T18:37:23Z (GMT). No. of bitstreams: 1 WOS000295236700022.pdf: 1054917 bytes, checksum: ade3c93db496ae9bfef43fc129742e42 (MD5) Previous issue date: 2011-09-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T13:49:42Z No. of bitstreams: 1 WOS000295236700022.pdf: 1054917 bytes, checksum: ade3c93db496ae9bfef43fc129742e42 (MD5) Made available in DSpace on 2014-05-20T13:49:42Z (GMT). No. of bitstreams: 1 WOS000295236700022.pdf: 1054917 bytes, checksum: ade3c93db496ae9bfef43fc129742e42 (MD5) Previous issue date: 2011-09-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Ethnopharmacological relevance: Indigofera suffruticosa is specie typical of the Cerrado or Brazilian savannah; it is a member of the Fabaceae family - in folkmedicine is used for gastric disorders, infection and inflammation.Aim of the study: Ethyl acetate fraction (AcF) and aqueous fraction (AqF) of the methanolic extract of I. suffruticosa leaves were evaluated against acute gastric ulcer. The AcF fraction was selected to assess its activity in ulcer healing and its gastroprotective effects via mucus and gastric secretion.Materials and methods: The gastroprotective action of AcF and AqF fractions were evaluated in a rodent experimental model. The action mechanisms, involvements of the antisecretory action, mucus and prostaglandin production, toxicological and healing activity of the AcF (100 mg/kg, p.o.) were evaluated. We also used histological analysis (HE and PAS) and immunohistochemical (PCNA and HSP-70) assays to evaluate the effects of I. suffruticosa.Results: AcF significantly inhibited the gastric mucosal damage caused by ethanol. This effect was statistically significant in 100 mg/kg group compared vehicle. AcF did not interfered with gastric secretion, significantly increased the PGE(2) and mucus production (validated in PAS technique). The gastroprotection was attenuated by pretreatment with N-ethylmaleimide, but not L-NAME. In acid-acetic-induced ulcer model AcF accelerated ulcer healing. Immunohistochemistry analysis showed induction of proliferating cell (PCNA) and heat shock protein (HSP 70).Conclusions: These results showed that AcF acted as gastroprotective agent stimulating prostaglandin, mucus and HSP70. (C) 2011 Elsevier B.V. All rights reserved. Univ Estadual Campinas, Dept Anat Biol Celular Fisiol & Biofis, Inst Biol, BR-13083970 Campinas, SP, Brazil Univ Estadual Campinas, Fac Ciencias Med, Dept Farmacol, BR-13083970 Campinas, SP, Brazil Univ Estadual Paulista, Inst Quim, Dept Quim Organ, Araraquara, SP, Brazil Univ Estadual Paulista, Dept Morfol, Inst Biociencias, Botucatu, SP, Brazil Univ Estadual Paulista, Inst Biociencias, Dept Fisiol, Botucaru, SP, Brazil Univ Estadual Paulista, Inst Quim, Dept Quim Organ, Araraquara, SP, Brazil Univ Estadual Paulista, Dept Morfol, Inst Biociencias, Botucatu, SP, Brazil Univ Estadual Paulista, Inst Biociencias, Dept Fisiol, Botucaru, SP, Brazil

Made available in DSpace on 2013-08-12T18:58:28Z (GMT). No. of bitstreams: 0 Previous issue date: 2011-11-01 Made available in DSpace on 2013-09-30T18:05:40Z (GMT). No. of bitstreams: 0 Previous issue date: 2011-11-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T13:24:00Z No. of bitstreams: 1 S0102-695X2011005000153.pdf: 1244113 bytes, checksum: add8d2f58588d0d15e2cc8d36f5ceeef (MD5) Made available in DSpace on 2014-05-20T13:24:00Z (GMT). No. of bitstreams: 1 S0102-695X2011005000153.pdf: 1244113 bytes, checksum: add8d2f58588d0d15e2cc8d36f5ceeef (MD5) Previous issue date: 2011-11-01 Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) 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 mu M respectively. The structure-activity relationship suggests that rings A and B containing an alpha, beta-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. Univ Estadual Paulista, Fac Ciencias Farmaceut, São Paulo, Brazil Univ Granada, E-18071 Granada, Spain Univ Estadual Paulista, Inst Quim, São Paulo, Brazil Univ Estadual Paulista, Fac Ciencias Farmaceut, São Paulo, Brazil Univ Estadual Paulista, Inst Quim, São Paulo, Brazil

The species Astronium urundeuva (Allemao) Engl. and Astronium graveolens Jacq., which are used in Brazilian folk medicine to treat allergies, inflammation, diarrhea and ulcers, were investigated for their composition. The aim of this study was to define a rapid and reliable analytical approach, based on the flow-injection analysis–electrospray ionization–ion trap–tandem mass spectrometry (FIA-ESI-IT-MS-MS) and matrix-assisted laser desorption/ionization-time-of-flight mass spectrometry (MALDI-ToF-MS), to investigate the full range of hydrolyzable tannins present in the extracts of these Astronium species. The MALDI-ToF-MS analysis allowed us to ascertain the presence of hydrolysable tannins in both Astronium species as a series of gallotannins with degrees of polymerization of 7 to 13 galloyl units. Moreover, the analysis by FIA-ESI-IT-MS-MS, as well as confirming this result and chemically defining gallotannins as galloylglucose compounds, highlighted the presence of further classes of hydrolysable tannins, such as hexahydrodiphenoyl esters of glucose and some gallic acid derivatives, providing information about their structure by a careful study of their fragmentation patterns. Finally, the evaluation of the number of positional isomers of gallotannins occurring in both Astronium species was obtained by high-performance liquid chromatography–electrospray ionization–ion trap mass spectrometry (HPLC/ESI-IT-MS). This is the first mass spectrometric evidence relating to the existence of gallotannins in Astronium genus.

Submitted by Guilherme Lemeszenski (guilherme@nead.unesp.br) on 2013-08-22T18:57:50Z No. of bitstreams: 1 S0102-695X2011000400018.pdf: 1891682 bytes, checksum: 91505f18ac41ecc497ea641ed01878b6 (MD5) Made available in DSpace on 2013-08-22T18:57:50Z (GMT). No. of bitstreams: 1 S0102-695X2011000400018.pdf: 1891682 bytes, checksum: 91505f18ac41ecc497ea641ed01878b6 (MD5) Previous issue date: 2011-08-01 Made available in DSpace on 2013-09-30T19:10:53Z (GMT). No. of bitstreams: 2 S0102-695X2011000400018.pdf: 1891682 bytes, checksum: 91505f18ac41ecc497ea641ed01878b6 (MD5) S0102-695X2011000400018.pdf.txt: 48488 bytes, checksum: 6935d5e60a685433422400fdbc922278 (MD5) Previous issue date: 2011-08-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T14:21:23Z No. of bitstreams: 2 S0102-695X2011000400018.pdf: 1891682 bytes, checksum: 91505f18ac41ecc497ea641ed01878b6 (MD5) S0102-695X2011000400018.pdf.txt: 48488 bytes, checksum: 6935d5e60a685433422400fdbc922278 (MD5) Made available in DSpace on 2014-05-20T14:21:23Z (GMT). No. of bitstreams: 2 S0102-695X2011000400018.pdf: 1891682 bytes, checksum: 91505f18ac41ecc497ea641ed01878b6 (MD5) S0102-695X2011000400018.pdf.txt: 48488 bytes, checksum: 6935d5e60a685433422400fdbc922278 (MD5) Previous issue date: 2011-08-01 Inflammatory bowel diseases are characterized by a chronic clinical course of relapse and remission associated with self-destructive inflammation of the gastrointestinal tract. Active extracts from plants have emerged as natural potential candidates for its treatment. Abarema cochliacarpos (Gomes) Barneby & Grimes, Fabaceae (Barbatimão), is a native medicinal plant in to Brazil. Previously we have demonstrated in an acute colitis model a marked protective effect of a butanolic extract, so we decided to assess its anti-inflammatory effect in a chronic ulcerative colitis model induced by trinitrobenzensulfonic acid (TNBS). Abarema cochliacarpos (150 mg/day, v.o.) was administered for fourteen consecutive days. This treatment decreased significantly macroscopic damage as compared with TNBS. Histological analysis showed that the extract improved the microscopic structure. Myeloperoxidase activity (MPO) was significantly decreased. Study of cytokines showed that TNF-α was diminished and IL-10 level was increased after Abarema cochliacarpos treatment. In order to elucidate inflammatory mechanisms, expression of cyclooxygenase (COX)-2 and nitric oxide synthase (iNOS) were studied showing a significant downregulation. In addition, there was reduction in the JNK and p-38 activation. Finally, IκB degradation was blocked by Abarema cochliacarpos treatment being consistent with an up-regulation of the NF-kappaB-binding activity. These results reinforce the anti-inflammatory effects described previously suggesting that Abarema cochliacarpos could provide a source for the search for new anti-inflammatory compounds useful in ulcerative colitis treatment. Universidade Estadual de Campinas Departamento de Anatomia, Biologia Celular e Fisiologia e Biofísica University of Seville Facultad de Farmacia Departamento de Farmacología Universidade Estadual de São Paulo Instituto de Química Departamento de Química Orgânica

Gaudichaudianic acid, a prenylated chromene isolated from Piper gaudichaudianum, has been described as a potent trypanocidal compound against the Y-strain of Trypanosoma cruzi. We herein describe its isolation as a racemic mixture followed by enantiomeric resolution using chiral HPLC and determination of the absolute configuration of the enantiomers as (+)-S and (-)-R by means of a combination of electronic and vibrational circular dichroism using density functional theory calculations. Investigation of the EtOAc extract of the roots, stems, and leaves from both adult specimens and seedlings of P. gaudichaudianum revealed that gaudichaudianic acid is biosynthesized as a racemic mixture from the seedling stage onward. Moreover, gaudichaudianic acid was found exclusively in the roots of seedlings, while it is present in all organs of the adult plant. Trypanocidal assays indicated that the (+)-enantiomer was more active than its antipode. Interestingly, mixtures of enantiomers showed a synergistic effect, with the racemic mixture being the most active.

Syngonanthus nitens is a grass-like species, whose flower stems assume a beautiful golden colour when dried, hence their common name “capim dourado”. This plant represents an important source of income for rural communities, especially in Jalapao region, being the scapes used in the craft industry to make, together with buriti palm strips, traditional handcrafts from their coils. Therefore, considering that scapes and not flowerheads are used, we carried out an analytical study to define the metabolite fingerprint of both S. nitens parts, with the aim, on one hand, to identify the molecules responsible for the characteristic golden colour of the capim dourado herb and, on the other hand, to identify the occurrence of interesting constituents in S. nitens flowerheads to increase the value of this part of the plant, considered a waste matter of golden grass handcrafts. Therefore an HPLC–ESI-MS n method, based on high-performance liquid chromatography coupled to electrospray negative ionization multistage ion trap mass spectrometry, was developed to rapidly identify and guide the isolation of the secondary metabolites occurring in flowers and scapes. On the basis of the on-line HPLC–ESI-MS n screening, 17 compounds, including 6 new molecules, were isolated, and their structures were unambiguously elucidated by NMR spectroscopic data.

Previous analysis of the ECD spectra of two prenylated benzopyrans isolated from Peperomia obtusifolia, by means of the helicity rule for the chromane chromophore, resulted in the incorrect assignment of their absolute configuration, (S) instead of (R) for a deduced P-helicity of the chromane ring for the (+)-enantiomers. This was discovered by the application of DFT calculations and VCD spectroscopy. Experimental and calculated (B3LYP/6-31G(d)) VCD and IR spectra were compared, and a definitive absolute configuration of (+)-1 and (+)-2 is reassigned directly in solution as (R). The assumption of equatorial positioning of bulky groups, shown here to be invalid for the title molecules, is the underlying cause of the previous incorrect assignment of absolute configuration. Moreover, TDDFT (B3LYP/6-311++G(2d,2p)//B3LYP/6-31G(d)) calculations of ECD spectra have shown that both P- and M-helicity of the heterocyclic ring, for a given absolute configuration, lead to the same sign for the 1Lb ECD band, thus bringing into question the validity of the empirical ECD helicity rule for chromane molecules.

Ethnopharmacological relevance Abarema cochliacarpos (Gomes) Barneby & Grimes (Mimosaceae) is a species – in folk medicine of Lagarto city, Sergipe state, northeastern Brazil – reputed to heal gastric ulcer and gastritis. Aim of the study Chloroform (CE) and methanolic (ME) extracts as well as ethyl acetate fraction (AF), butanolic fraction (AC) and aqueous fraction (AQF) of the methanolic extract of Abarema cochliacarpos bark were evaluated against acute gastric ulcer. The AC fraction was selected to assess its activity in ulcer healing and its gastroprotective effects via mucus and gastric secretion. Material and methods The gastroprotective action of CE and ME extracts and the fractions of the latter were evaluated in a rodent experimental model. The action mechanisms, involvements of the antisecretory action and mucus production, toxicological and healing activity of the AC (150 mg/kg, p.o.) were evaluated. We also used histological analysis (HE and PAS) and immunohistochemical (PCNA, COX-2, VEGF and HSP-70) assays to evaluate the effects of Abarema cochliacarpos . Results CE (200 and 400 mg/kg, p.o.) and ME (100, 200 and 400 mg/kg, p.o.) extracts were able to protect gastric mucosa against absolute ethanol. Respective inhibitions produced were: 65.31% and 83.80% by the first; 91.69%, 96.75% and 99.80% by the second; and 74.24% by the AC fraction. Antisecretory and mucus production effects were exhibited by the AC fraction, which also accelerated the healing of ulcerated gastric mucosa by stimulating proliferation factors (PCNA) and induced healing factors including COX-2, VEGF and HSP-70. Conclusion All these results suggest that Abarema cochliacarpos (Gomes) Barneby & Grimes presents gastroprotective effects and wound-healing properties.

Context: Alchornea triplinervia (Spreng.) Mull. Arg. (Euphorbiaceae) is a tree widespread in many Brazilian states. This plant naturally occurs in different ecosystems including tropical Atlantic forest, Amazon rain forest, moist tropical mixed forest, savanna forest, among others. Local populations traditionally use it in tea form to treat gastric disturbances.Objective: The objective of this research was to evaluate the plant A. triplinervia as a potential inhibitor of some macrophage functions involved in the inflammatory process.Materials and methods: The effects of Alchornea triplinervia ethyl acetate fraction (AtF) on hydrogen peroxide (H2O2), nitric oxide (NO) and tumor necrosis factor-α (TNF-α) production in peritoneal macrophages were investigated using phenol red, Griess reagent and a sandwich immunoassay, respectively.Results: AtF chromatographic analyses indicate the presence of flavonoids as majority compounds. The fraction also showed an intense inhibition of H2O2 and NO production. The inhi...

Mouriri pusa, popularly known as "manapuçá" or "jaboticaba do mato", is a plant from Brazilian cerrado that has been found to be commonly used in the treatment of gastrointestinal disturbs in its native region. The present work was carried out to investigate the effect of tannins (TF) and flavonoids (FF) fractions from Mouriri pusa leaves methanolic extract on the prevention and cicatrisation process of gastric ulcers, and also evaluate possible toxic effects.The following protocols were taken in rats: acute assay, in which ulcers were induced by oral ethanol after pre-treatment with the fractions; and 14 days treatment assay, in which ulcers were treated for 14 days after induction by local injection of acetic acid.In the acute model, treatment with either, TF (25mg/kg) or FF (50mg/kg), was able to reduce lesion area, showing gastroprotective effect. In addition, FF proved itself anti-inflammatory by reducing COX-2 levels. In acetic acid model, both fractions exhibited larger ulcers' regenerative mucosa, indicating cicatrisation enhancement. FF group also showed augmented cell proliferation, anti-inflammatory action and enhanced angiogenesis as well as increased mucus secretion. Moreover, concerning the toxicity parameters analyzed, no alteration in the fractions groups was observed.Tannins and flavonoids from Mouriri pusa provide beneficial effects against gastric ulcers with relative safety.

Mycobacterium tuberculosis is responsible for over 8 million cases of tuberculosis (TB) annually. Natural products may play important roles in the chemotherapy of TB. The antimycobacterial activity and the innate immune response of methanol (METH) and dichloromethane (DCM) extracts of Indigofera suffruticosa Miller (Fabaceae) were evaluated. We observed that the minimum inhibitory concentrations (MICs) for METH and DCM extracts were 125 and 1000 microg/mL, respectively. However, they were able to induce the innate immune response through the production of high levels of NO and TNF-alpha (p < 0.001) by peritoneal exudate cells (PECs). These results suggest that I. suffruticosa extracts may have an important immunological role in the control of TB once macrophage activity is induced by them.

Background: Leishmaniasis is a complex protozoa disease caused by Leishmania genus (Trypanosomatidae family). Currently, there have been renewed interests worldwide in plants as pharmaceutical agents. In this study, the in vivo efficacy of Solanum spp. is assessed in an L. amazonensis BALB/c mice model for experimental cutaneous leishmaniasis. Methods: Animals were infected with 5 &times, 106 metacyclic promastigotes and 30-day post-infection, a treatment with 30 mg/kg of Solanum extracts or Glucantime&reg, (GTM) was applied intralesionally every four days to complete 5 doses. Results: Neither death nor loss of weight higher than 10% was observed. All the tested extracts were able to control the infection, compared with the infected and untreated group. Solanum havanense Jacq. extract showed the highest efficacy and was superior (p &lt, 0.05) to GTM. Solanum myriacanthum Dunal., S. nudum Dunal. and S. seaforthianum Andr. extracts demonstrated a similar effect (p &gt, 0.05) to GTM. An increase of IFN-&gamma, (p &lt, 0.05) was displayed only by animals treated with S. nudum compared to the group treated with a vehicle, while no differences (p &gt, 0.05) were observed for IL-12. Conclusions: In vivo effects of Solanum extracts were demonstrated, suggesting that this genus could be further explored as a new antileishmanial alternative.

Two new saponins, 3-O-[β-D-xylopyranosyl-(13)-β-D-galactopyranosyl-(13)-β-glucuronopyranosyl]oleanolic acid 28-O-β-D-glucopyranosyl ester (1) and the corresponding monodesmoside, 3-O-[β-D-xylopyranosyl-(13)-β-D-galactopyranosyl-(13)-β-glucuronopyranosyl]oleanolic acid (2), have been isolated from the leaves of Guapira graciliflora (Nyctaginaceae), together with two further oleanane saponins, 3 and 4, daucosterol (5), and two known glycerogalactolipids, 6 and 7. The structures of the new compounds were established by extensive NMR and MS experiments, in conjunction with acid hydrolysis and sugar analysis. This is the first report on the phytochemistry of plants of the genus Guapira.

Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-27T11:24:35Z No. of bitstreams: 0Bitstream added on 2014-05-27T14:30:38Z : No. of bitstreams: 1 2-s2.0-77953750965.pdf: 2006883 bytes, checksum: e94e8c96aac3715b88438cc2a403101e (MD5) Made available in DSpace on 2014-05-27T11:24:35Z (GMT). No. of bitstreams: 0 Previous issue date: 2010-01-01 Considering the quality of the phytotherapic agents, it is important to point out that it includes rigorous attendance of the different steps of the development and production of these products, from the collection of the vegetable to the availability of the final product. In this work the quality control of the Operculina macrocarpa (Linn) Urb. roots, popularly known as 'batata-de-purga', was carried out. Pharmacopoeic and no pharmacopoeic methodologies were employed to physico-chemical and microbiological quality control. The obtained results showed that the roots presents a content of resin of 9,85%, The microbiological analysis did not present pathogenic growth among the other accomplished tests. The work stands out the importance of the establishment of norms for the quality control for the plants, so that they are found able to be used for phytotherapic reasons. Faculdade de Ciências Farmacêuticas Departamento de Fármacos e Medicamentos Universidade Estadual Paulista 'Julio de Mesquita Filho', Rodovia Araraquara-Jaú km 1, 14801-902 Araraquara-SP Faculdade de Ciências Farmacêuticas Departamento de Princípios Ativos Naturais e Toxicologia Universidade Estadual Paulista 'Julio de Mesquita Filho', Rodovia Araraquara-Jaú km 1, 14801-902 Araraquara-SP Instituto de Química Departamento de Química Orgânica Universidade Estadual Paulista 'Julio de Mesquita Filho', Rua Francisco Degni s/n, 14800-900, Araraquara-SP Faculdade de Ciências Farmacêuticas Departamento de Fármacos e Medicamentos Universidade Estadual Paulista 'Julio de Mesquita Filho', Rodovia Araraquara-Jaú km 1, 14801-902 Araraquara-SP Faculdade de Ciências Farmacêuticas Departamento de Princípios Ativos Naturais e Toxicologia Universidade Estadual Paulista 'Julio de Mesquita Filho', Rodovia Araraquara-Jaú km 1, 14801-902 Araraquara-SP Instituto de Química Departamento de Química Orgânica Universidade Estadual Paulista 'Julio de Mesquita Filho', Rua Francisco Degni s/n, 14800-900, Araraquara-SP

Ailanthus excelsa (Roxb), an Egyptian medicinal species highly important for treating numerous diseases, was investigated against experimentally induced gastric ulcer in rodents. We evaluated the gastroprotective effect of four extracts (petroleum ether, diethyl ether, chloroform, and methanol) of A. excelsa bark by using the ethanol-induced gastric lesion model. The pretreatment of animals with methanolic, petroleum ether, and chloroformic extracts (100 mg/kg, oral (p.o.)) from A. excelsa significantly reduced gastric lesion induced by ulcerogenic agent (56, 47, and 70%, respectively) when compared with animals pretreated with vehicle. However, the diethyl ether pretreatment led to the least gastric lesion damage (83%), similar to the standard antiulcer drug, cimetidine, at the same dose (100 mg/kg, p.o.). The lower effective dose of diethyl ether extract, as well as cimetidine, given by intraduodenal route, significantly increased the pH values and reduced the acid output of gastric juice. Sterols, triterpenes, and quassinoids are present in the diethyl ether extract of A. excelsa stem bark, which presented the best gastroprotective action among the studied extracts. Our study confirmed the traditional indications of A. excelsa for the treatment of gastric ulcer.

Ethnopharmacological relevance Mouriri elliptica Martius (Melastomataceae) is species reputed in folk medicine to heal gastric ulcer and gastritis. Aim of the study Methanolic extract (ME) and ethyl acetate fraction (EAF) from leaves of Mouriri elliptica were evaluated for their gastroprotective, healing, immunological, toxicological and anti- Helicobacter pylori activities. Material and methods The gastroprotective action of ME and EAF was evaluated in rodent experimental models and to elucidate mechanisms of action, the antisecretory action, involvements of NO, SH, PGE 2 , anti- Helicobacter pylori action of ME was evaluated. We also used immunohistochemical (PCNA and COX-2) and immunomodulatory (murine peritoneal macrophages) assays to evaluate Mouriri elliptica effects. Results ME present gastroprotective action without antisecretory effect. Otherwise, ME showed anti- Helicobacter pylori action (MIC = 0.025 μg/mL) and was able to inhibit NO production by macrophages. This species also accelerate the healing of ulcerated gastric mucosa by stimulating proliferation factors (PCNA), COX-2 and maintained basal PGE 2 level independent action of NSAID in gastric mucosa. The phytochemical investigation showed that this species possesses phenolic acid derivatives, acylglycoflavonoids and condensed tannins which probably influenced their pharmacological action. Conclusion All these results suggest the efficacy and safety of Mouriri elliptica in combating and healing gastric ulcer.

Ethnopharmacological relevance Davilla elliptica and Davilla nitida are species commonly found in the Brazilian Cerrado biome. Aim of the study Based on ethnopharmacological and phytochemical analyses, methanolic extracts from leaves of Davilla elliptica (EDE) and Davilla nitida (EDN) were evaluated for their anti-ulcer, anti-inflammatory, immunological and anti- Helicobacter pylori activities. Materials and methods The gastroprotective action of both extracts was evaluated in rodent experimental models (HCl/ethanol, ethanol or NSAID). We also evaluated anti-inflammatory (carrageenin-induced rat hind paw edema), immunomodulatory (murine peritoneal macrophages) and antibacterial action of both extracts against a standard strain of Helicobacter pylori . Results EDE and EDN (500 mg/kg) were able to protect gastric mucosa against HCl/ethanol solution (EDE 63%; EDN 59%), absolute ethanol (EDE 95%; EDN 88%), and also against injurious effect of NSAID (EDE 77%; EDN 67%). When EDE and EDN were challenged with sulfhydryl depleter compound, the gastroprotective action of both extracts was completely abolished. EDE had gastroprotective effect related to increase of glutathione bioavailability and stimulated higher levels of NO, H 2 O 2 and TNF-α production. Otherwise EDN showed better anti- Helicobacter pylori action than EDE. Neither extracts presented anti-inflammatory activity by oral route. Conclusion The phytochemical investigation showed that both extracts possess phenolic acid derivatives, acylglycoflavonoids and condensed tannins with evident quantitative variations that probably influenced the pharmacological differences between extracts.

Made available in DSpace on 2013-08-28T14:10:24Z (GMT). No. of bitstreams: 1 WOS000264565000016.pdf: 201886 bytes, checksum: 6efe2d3a2a366e500e8c1457192fe7c2 (MD5) Made available in DSpace on 2013-09-30T19:10:41Z (GMT). No. of bitstreams: 2 WOS000264565000016.pdf: 201886 bytes, checksum: 6efe2d3a2a366e500e8c1457192fe7c2 (MD5) WOS000264565000016.pdf.txt: 38476 bytes, checksum: 39dc3708d7052c783d2d9238d5605939 (MD5) Previous issue date: 2009-03-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T13:49:52Z No. of bitstreams: 2 WOS000264565000016.pdf: 201886 bytes, checksum: 6efe2d3a2a366e500e8c1457192fe7c2 (MD5) WOS000264565000016.pdf.txt: 38476 bytes, checksum: 39dc3708d7052c783d2d9238d5605939 (MD5) Made available in DSpace on 2014-05-20T13:49:52Z (GMT). No. of bitstreams: 2 WOS000264565000016.pdf: 201886 bytes, checksum: 6efe2d3a2a366e500e8c1457192fe7c2 (MD5) WOS000264565000016.pdf.txt: 38476 bytes, checksum: 39dc3708d7052c783d2d9238d5605939 (MD5) Previous issue date: 2009-03-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) This study was designed to determine the gastroprotective effect of a Mangifera indica leaf decoction (AD), on different experimental models in rodents. The administration of AD up to a dose of 5 g/kg (p.o.) did not produce any signs or symptoms of toxicity in the treated animals, while significantly decreasing the severity of gastric damage induced by several gastroprotective models. Oral pre-treatment with AD ( 250, 500 or 1000 mg/kg) in mice and rats with gastric lesions induced by HCl/ethanol, absolute ethanol, non-steroidal anti-inflammatory drug (NSAID) or stress-induced gastric lesions resulted in a significant decrease of said lesions. Phytochemical analyses of AD composition demonstrated the presence of bioactive phenolic compounds that represent 57.3% of total phenolic content in this extract. Two main phenolic compounds were isolated, specifically mangiferin (C-glucopyranoside of 1,3,6,7-tetrahydroxyxanthone) and C-glucosylbenzophenone (3-C-beta-D-glucopyranosyl-4',2,4,6-tetrahydroxybenzophenone). These findings indicate the potential gastroprotective properties of aqueous decoction from M. indica leaves. São Paulo State Univ, UNESP, Biosci Inst, Dept Physiol, BR-18618000 Botucatu, SP, Brazil São Paulo State Univ, UNESP, Fac Pharmaceut Sci, Pharmacos & Drugs Dept, BR-14801902 Araraquara, SP, Brazil Univ Estadual Campinas, UNICAMP, Inst Biol, Dept Physiol & Biophys, BR-13083970 Campinas, SP, Brazil São Paulo State Univ, UNESP, Inst Chem, Dept Organ Chem, BR-14800900 Araraquara, SP, Brazil São Paulo State Univ, UNESP, Biosci Inst, Dept Physiol, BR-18618000 Botucatu, SP, Brazil São Paulo State Univ, UNESP, Fac Pharmaceut Sci, Pharmacos & Drugs Dept, BR-14801902 Araraquara, SP, Brazil São Paulo State Univ, UNESP, Inst Chem, Dept Organ Chem, BR-14800900 Araraquara, SP, Brazil

Aim of the study Vochysia tucanorum is an important medicinal plant used in the Cerrado of Brazil against gastric disorders and this study reveals the pharmacological action of this traditional medicine use. Materials and methods The methanolic extract (E-MeOH) and buthanolic fraction (Fr-Bu) obtained from V. tucanorum were challenged by different necrotizing agents in rodents. NO-synthase inhibitor (L-NAME) and SH blocker (NEM) were used to evaluate the participation of cytoprotective factors in E-MeOH and Fr-Bu gastroprotection. Antiulcerogenic action of V. tucanorum was evaluated in rats and mice at doses 250, 500 or 1000 mg/kg (E-MeOH) and 37.5, 75 or 150 mg/kg (Fr-Bu). Results Both E-MeOH and Fr-Bu present elevated gastroprotective action in all in vivo experimental models, without signs of acute toxicity. The mechanisms involved in the gastroprotective action of E-MeOH and Fr-Bu are related to the antioxidant activity and protection to gastric mucosa NO levels. Phytochemical investigations of Fr-Bu identified different pentacyclic triterpenoids such as betulinic acid, erythrodiol, epi-betulinic acid and mixtures of ursolic acid and oleanolic acid derivatives as the major constituents. The presence of such triterpenoids in Fr-Bu is probably related to the potent gastroprotective action of this medicinal plant species. Conclusion Effectiveness in gastroprotection and the absence of acute toxicity indicate this species as a promising herbal drug that is in accordance with ethnopharmacological use against gastric disorders.

Submitted by Guilherme Lemeszenski (guilherme@nead.unesp.br) on 2013-08-22T18:49:20Z No. of bitstreams: 1 S0100-46702008000400007.pdf: 168880 bytes, checksum: da5ada541ce6515696ae3ba24c0fda07 (MD5) Made available in DSpace on 2013-08-22T18:49:20Z (GMT). No. of bitstreams: 1 S0100-46702008000400007.pdf: 168880 bytes, checksum: da5ada541ce6515696ae3ba24c0fda07 (MD5) Previous issue date: 2008-12-01 Made available in DSpace on 2013-09-30T19:39:41Z (GMT). No. of bitstreams: 2 S0100-46702008000400007.pdf: 168880 bytes, checksum: da5ada541ce6515696ae3ba24c0fda07 (MD5) S0100-46702008000400007.pdf.txt: 30580 bytes, checksum: e008149f1624175e40ffe118656f4c3d (MD5) Previous issue date: 2008-12-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T15:10:33Z No. of bitstreams: 2 S0100-46702008000400007.pdf: 168880 bytes, checksum: da5ada541ce6515696ae3ba24c0fda07 (MD5) S0100-46702008000400007.pdf.txt: 30580 bytes, checksum: e008149f1624175e40ffe118656f4c3d (MD5) Made available in DSpace on 2014-05-20T15:10:33Z (GMT). No. of bitstreams: 2 S0100-46702008000400007.pdf: 168880 bytes, checksum: da5ada541ce6515696ae3ba24c0fda07 (MD5) S0100-46702008000400007.pdf.txt: 30580 bytes, checksum: e008149f1624175e40ffe118656f4c3d (MD5) Previous issue date: 2008-12-01 Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Cinco flavanonas e três chalconas foram isoladas das folhas de Campomanesia adamantium Berg. (Myrtaceae). O teor desses compostos foram determinados por CLAE. O teor de compostos fenólicos também foi determinado. O monitoramento da atividade antioxidante foi feito pela inibição da peroxidação usando o sistema do ácido linoleico e método do radical livre 2,2-difenil-1-picrilhidrazila - DPPH . As espécies vegetais foram coletadas em 4 cidades diferentes do estado de Mato Grosso do Sul, Brasil. As diferentes amostras exibiram uma variação de 4,67-232,35 mg/g chalconas e 15,62-50,71 mg/g flavanonas e teor de compostos fenólicos de 7,24-21,19 mg/g ácido gálico. Todos os extratos exibiram alta atividade antioxidante com uma variação do efeito radical livre (DPPH) de 52,0-92,2 % e da inibição da oxidação do ácido linoleico de 14,6-94,2%. Five flavanones and three chalcones were isolated from Campomanesia adamantium Berg. (Myrtaceae) leaves. The contents of these compounds were determined by HPLC. The phenolic contents were also determined. The monitoring of the antioxidant activity was carried out by inhibition of peroxidation using the linoleic acid system and radical-scavenging (DPPH). The plants were collected from 4 distinct cities of the Mato Grosso do Sul State, Brazil. The different samples exhibited a range of 4.67-232.35 mg/g chalcones and 15.62-50.71 mg/g flavanones and phenolic contents of the 7.24-21.19 mg/g gallic acid. All extracts showed high antioxidant activity with a wide range of the radical-scavenging (DPPH) from 52.0 to 92.2 % and inhibition oxidation of linoleic acid from 14.6 to 94.2%. Universidade Federal de Mato Grosso do Sul Departamento de Química Universidade Estadual de Mato Grosso do Sul (UEMS) Universidade Estadual Paulista Departamento de Química Orgânica Universidade Estadual Paulista Departamento de Química Orgânica

The interaction of ascorbic acid with 5-methoxy-3,4-dehydroxanthomegnin, an 1,4-naphthoquinone, was investigated using the cytotoxic index for McCoy cells by neutral red assay. The synergstic effect was observed when such compounds were added simultaneously, most probably due to hydrogen peroxide being generated by ascorbate – driven 5-methoxy-3,4-dehydroxanthomegnin redox cycling. Incubation of cells in the presence of 5-methoxy-3,4-dehydroxanthomegnin/ascorbic acid/catalase, an enzyme that destroys H 2 O 2 , resulted in an increase of cell survival, reinforcing the involvement of hydrogen peroxide generated as an important oxidizing agent that kills McCoy cells.

Aim of the study Cissus sicyoides L. is a medicinal plant popularly known in Brazil against various diseases and the research interest in this plant is justifiable because of its potential medicinal value in stomachache and gastric ulcer. Materials and methods The methanolic extract obtained from the leaves of Cissus sicyoides (Cc) was evaluated for the ability to protect the gastric mucosa against injuries caused by necrotizing agents (0.3 M HCl/60% EtOH, absolute ethanol, piroxicam and pylorus ligature) in rodents. We also evaluated microcirculation, antioxidant action and participation of NO (nitric oxide) and sulfhydryls (SH) groups in the Cc gastroprotective action. Results Administration of Cc significantly reduced gastric lesions induced by different ulcerogenic agents in rodents. This extract administered by oral route significantly increased gastric volume without exerting antisecretory effect. The Cc effect involved an increase of the defense mechanism of the gastrointestinal mucosa such as NO and SH groups that prevent and attenuate the ulcer process. The Cc also has antioxidant property against oxidative stress but does not modify microcirculation response in gastric mucosa. Conclusions These results confirmed the traditional use of Cissus sicyoides for the treatment of gastric ulcer.

The chemical interaction between plants is known as allelopathy and it is related to the release of substances into the environment. The present study aimed at the evaluation of the allelopathic activity of the leaves of Leonurus sibiricus against the germination and initial growth of Raphanus sativus, Lactuca sativa, and Lepidium sativum. Chemical analyses showed the presence in the leaves of four major flavonoids (quercetin-3-O-α-L-rhamnopyranosyl-(1>6)-β-D-galactopyranoside; rutin; hyperin, and isoquercetrin) and of three minor flavonoidic compounds (genkwanin, 3′-hydroxy genkwanin, and quercetin). Extracts, their chromatographic fractions and pure isolated flavonoids showed different biological activities. A methanol extract of leaves of Leonurus sibiricus caused significant reduction only in the germination of Lactuca sativa, with no effects on the germinative processes of Raphanus sativus and Lepidium sativum. Some chromatographic fractions, containing the flavonoids, showed inhibitory acti...

Ethnopharmacological Relevance Mouriri pusa Gardn. (Melastomataceae) is a medicinal plant commonly used by people living in the Cerrado to treat gastrointestinal disturbances. This medicinal plant has shown intense gastroprotective action in rodent gastric lesion, but still there are no data about its healing effect on gastric mucosa. Aim of the Study To evaluate the methanolic extract (MeOH) obtained from Mouriri pusa leaves for its effect on the cicatrisation process of gastric ulcer. Mterials and Methods The healing effects on gastric ulcers inducted by subserosal injection of acetic acid were evaluated by macroscopic and microscopic measures, imunohistochemistry and cell counting in rats treated with MeOH extract of Mouriri pusa (250 mg/kg, p.o./daily) for 14 or 30 days. The toxicity of Mouriri pusa was also evaluated by body and organ weight measure and clinical biochemical parameters. Results Mouriri pusa treatments lasting 14 and 30 days showed elevated mucus secretion (PAS) and thicker regenerative gastric mucosa, denoting increased cell proliferation, which was confirmed by PCNA immunohistochemical analysis. Moreover, there was important cell recruitment (neutrophils and mast cells) to the site of the ulcer, which is an important factor in ulcer healing. No toxic effect was observed in all parameters evaluated. Phenolic compounds present in the MeOH extract like tannins, flavonoids and epicatechin are the probable agents involved in the healing effects of this medicinal plant. Conclusions These findings showed a potential effect of Mouriri pusa in increasing regeneration of damaged gastric mucosa with safety for human use.

Methanolic (VPME) and chloroformic (VPCL) extracts, obtained from the aerial parts of Vernonia polyanthes, were investigated for its antiulcerogenic properties. Administration of VPME (250 mg/kg) and VPCL (50 mg/kg) significantly inhibited the gastric mucosa damage (64% and 90%, respectively) caused by absolute ethanol (p.o.). Otherwise, in NSAID-induced gastric damage, their gastroprotective effects have decreased. Since the VPCL extract resulted to be more effective than the VPME we focused our efforts over VPCL action mechanism of action.

Ethanol-induced oxidative damage is commonly associated with the generation of reactive oxygen molecules, leading to oxidative stress. Considering that antioxidant activity is an important mechanism of action involved in cytoprotection, the aim of this work was to evaluate the antioxidant properties of the alkaloid indigo (1) (2 mg/kg, P. O.), obtained from the leaves of Indigofera truxillensis Kunth (Fabaceae), on rat gastric mucosa submitted to ethanol-induced (100%, 1 mL, P. O.) gastric ulcer. Enzymatic assays and DNA fragmentation analysis were performed. When ethanol was administered to the control group, the sulfhydryl content (SH) and the glutathione peroxidase (GPx) activity decreased by 41% and 50%, respectively; in contrast, superoxide dismutase (SOD) and glutathione reductase (GR) activities increased by 56% and 67%, respectively. Additionally, myeloperoxidase (MPO) activity, a marker for free radical generation caused by polymorphonuclear neutrophil (PMN) tissue infiltration, also increased 4.5-fold after ethanol treatment. Rat gastric mucosa exposed to ethanol showed DNA fragmentation. Indigo alkaloid pretreatment protected rats from ethanol-induced gastric lesions. This effect was determined by the ulcerative lesion area (ULA), indicating an inhibition of around 80% at 2 mg/kg. This alkaloid also diminished GPx activity, which was higher than that observed with ethanol alone. However, this effect was counterbalanced by increased GR activity. Indigo was unable to restore alterations in SOD activity promoted by ethanol. After indigo pretreatment, SH levels and MPO activity remained normal and gastric mucosa DNA damage caused by ethanol was also partially prevented by indigo. These results suggest that the gastroprotective mechanisms of indigo include non-enzymatic antioxidant effects and the inhibition of PMN infiltration which, in combination, partially protect the gastric mucosa against ethanol-induced DNA damage.

The isocoumarins (1-50 microM) paepalantine (9,10-dihydroxy-5,7-dimethoxy-1H-naptho(2,3c)pyran-1-one), 8,8'-paepalantine dimer, and vioxanthin isolated from Paepalanthus bromelioides, were assessed for antioxidant activity using isolated rat liver mitochondria and non-mitochondrial systems, and compared with the flavonoid quercetin. The paepalantine and paepalantine dimers, but not vioxanthin, were effective at scavenging both 1,1-diphenyl-2-picrylhydrazyl (DPPH(*)) and superoxide (O(2)(-)) radicals in non-mitochondrial systems, and protected mitochondria from tert-butylhydroperoxide-induced H(2)O(2) accumulation and Fe(2+)-citrate-mediated mitochondrial membrane lipid peroxidation, with almost the same potency as quercetin. These results point towards paepalantine, followed by paepalantine dimer, as being a powerful agent affording protection, apparently via O(2)(-) scavenging, from oxidative stress conditions imposed on mitochondria, the main intracellular source and target of those reactive oxygen species. This strong antioxidant action of paepalantine was reproduced in HepG2 cells exposed to oxidative stress condition induced by H(2)O(2).

A rapid analytical approach suitable to achieve a comprehensive characterization of the compounds present in the infusion prepared from the leaves of Byrsonima fagifolia Niedenzu (Malpighiaceae), a Brazilian plant used as an infusion to treat gastric disorders, was developed. The method was based on high-performance liquid chromatography coupled to electrospray negative ionisation multistage ion trap mass spectrometry (HPLC/ESI-ITMSn). The main ions in the ESI-ITMS spectra were attributed to a quinic acid core containing from one to five galloyl units. Quercetin derivatives containing one and two sugar moieties as well as galloyl esterification were also detected. These results indicated that HPLC/ESI-ITMSn is easily applicable to infusions of this plant and allows the rapid and direct identification of these compounds in crude plant extracts. Copyright (C) 2007 John Wiley & Sons, Ltd.

Made available in DSpace on 2015-12-07T15:39:58Z (GMT). No. of bitstreams: 0 Previous issue date: 2015-10-29. Added 1 bitstream(s) on 2015-12-07T15:54:28Z : No. of bitstreams: 1 PMC4625929.pdf: 472777 bytes, checksum: dedcb2fb4fdcef28e5613e423b621389 (MD5) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Syngonanthus arthrotrichus and Syngonanthus bisulcatus, currently known for Comanthera aciphylla (Bong.) L.R.Parra & Giul. and Comanthera bisulcata (Koern.) L.R. Parra & Giul, popularly known in Brazil as sempre-vivas, are plants from the family Eriocaulaceae. They are found in the states of Minas Gerais and Bahia. The species are known to be rich in flavonoids to which their gastroprotective activity has been attributed. In this research, experimental protocols were performed to elucidate the associated mechanisms of action. The activity was evaluated using induced gastric ulcer models (acetic acid and ethanol-induced gastric lesions in NEM or L-NAME pre-treated mice, and by ischemia/reperfusion). Antioxidant enzymes, serum somatostatin, and gastrin were also evaluated. In chronic gastric ulcers, a single daily oral dose of Sa-FRF or Sb-FRF (100 mg/kg body wt.) for 14 consecutive days accelerated ulcer healing to an extent similar to that seen with an equal dose of cimetidine. The pre-treatment of mice with NEM (N-ethylmaleimide) or L-NAME (N-nitro-L-arginine) abolished the protective activity of Sa-FRF, Sa-FDF, Sb-FDF and Sb-FRF or Sa-FRF and Sb-FRF, respectively, which indicates that antioxidant compounds and nitric oxide synthase activity are involved in the gastroprotective. Sa-FRF and Sb-FRF (100 mg/kg p.o) protected the gastric mucosa against ulceration that was induced by ischemia/reperfusion (72 and 76 %, respectively). It also decreased lipid peroxidation and restored total thiols in the gastric wall of mice that had been treated with ethanol. When administered to rats submitted to ethanol-induced gastric lesions, Sa-FRF and Sb-FRF (100 mg/kg, p.o.) increased the somatostatin serum levels, while the gastrin serum levels were proportionally decreased. The results indicate significant healing effects and gastroprotective activity for the Sa-FRF and Sb-FRF, which probably involves the participation of SH groups, nitric oxide (NO), the antioxidant system, somatostatin, and gastrin. All are integral parts of the gastrointestinal mucosa's cytoprotective mechanisms against aggressive factors. Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Laboratório de Farmacologia do Trato Gastrintestinal, Universidade Federal da Paraíba (UFPB), João Pessoa, PB, Brasil Departamento de Fisiologia e Biofísica, Instituto de Biologia, Universidade Estadual de Campinas (UNICAMP), Campinas, SP, Brasil Departamento de Morfologia, Instituto de Biociências de Botucatu (IBB), Universidade Estadual Paulista (UNESP), Botucatu, SP, Brasil Departamento de Fisiologia, Instituto de Biociências de Botucatu (IBB), Universidade Estadual Paulista (UNESP), Botucatu, SP, Brasil Departamento de Botânica, Instituto de Biociências, Universidade de São Paulo (USP), São Paulo, SP, Brasil Universidade Estadual Paulista, Departamento de Morfologia, Instituto de Biociências de Botucatu Universidade Estadual Paulista, Departamento de Fisiologia, Instituto de Biociências de Botucatu

Made available in DSpace on 2015-12-07T15:34:37Z (GMT). No. of bitstreams: 0 Previous issue date: 2015. Added 1 bitstream(s) on 2015-12-07T15:54:19Z : No. of bitstreams: 1 PMC4536841.pdf: 1159237 bytes, checksum: 5d62bb3d5bc2b343d38c60e292cb8188 (MD5) The genus Astronium (Anacardiaceae) includes species, such as Astronium fraxinifolium, Astronium graveolens, and Astronium urundeuva, which possess anti-inflammatory, anti-ulcerogenic, healing, and antimicrobial properties. Nanostructured lipid systems are able to potentiate the action of plant extracts, reducing the required dose and side effects and improving antimicrobial activity. This work aims to evaluate a nanostructured lipid system that was developed as a strategy to improve the anti-Candida albicans activity of hydroethanolic extracts of stems and leaves from Astronium sp. The antifungal activity against C. albicans (ATCC 18804) was evaluated in vitro by a microdilution technique. In addition to the in vitro assays, the Astronium sp. that showed the best antifungal activity and selectivity index was submitted to an in vivo assay using a model of vulvovaginal candidiasis infection. In these assays, the extracts were either used alone or were incorporated into the nanostructured lipid system (comprising 10% oil phase, 10% surfactant, and 80% aqueous phase). The results indicated a minimal inhibitory concentration of 125.00 µg/mL before incorporation into the nanostructured system; this activity was even more enhanced when this extract presented a minimal inhibitory concentration of 15.62 µg/mL after its incorporation. In vivo assay dates showed that the nanostructure-incorporated extract of A. urundeuva leaves was more effective than both the unincorporated extract and the antifungal positive control (amphotericin B). These results suggest that this nanostructured lipid system can be used in a strategy to improve the in vitro and in vivo anti-C. albicans activity of hydroethanolic extracts of Astronium sp. Department of Biological Sciences, School of Pharmaceutical Sciences, UNESP - Univ Estadual Paulista, Araraquara, São Paulo, Brazil. Department of Drugs and Medicines, School of Pharmaceutical Sciences, UNESP - Univ Estadual Paulista, Araraquara, São Paulo, Brazil. Department of Organic Chemistry, Chemistry Institute, UNESP - Univ Estadual Paulista, Araraquara, São Paulo, Brazil. Coastal Campus of São Vicente, UNESP - Univ Estadual Paulista, São Vicente, São Paulo, Brazil. Department of Biological Sciences, School of Pharmaceutical Sciences, UNESP - Univ Estadual Paulista, Araraquara, São Paulo, Brazil. Department of Drugs and Medicines, School of Pharmaceutical Sciences, UNESP - Univ Estadual Paulista, Araraquara, São Paulo, Brazil. Department of Organic Chemistry, Chemistry Institute, UNESP - Univ Estadual Paulista, Araraquara, São Paulo, Brazil. Coastal Campus of São Vicente, UNESP - Univ Estadual Paulista, São Vicente, São Paulo, Brazil.

Made available in DSpace on 2018-12-11T16:59:16Z (GMT). No. of bitstreams: 0 Previous issue date: 2015-12-24 Ethnopharmacological relevance The Brazilian Cerrado is an important source of natural products, such as Myrcia bella Cambess (MB, also known as mercurinho). MB leaves are popularly used for the treatment of diabetes and gastrointestinal disorders; however, only its hypoglycemic activity has been experimentally described. Aim of the study Because MB is used to treat gastrointestinal disorders, the present study characterized biological activities of hydroalcoholic MB extract in human normal and tumor gastric cells. Materials and methods Cytotoxic, antiproliferative, genotoxic and protective effects were evaluated, as well as the effects of the MB extract on gene expression. Results The MB extract induced cytotoxicity in tumor cells at lower concentrations compared with normal cells as assessed by the MTT assay. Moreover, the MB extract induced necrosis based on acridine orange/ethidium bromide staining. An antiproliferative effect was evidenced through an arrest in the G2/M phase detected by flow cytometry and a decrease in the nuclear division index using the cytokinesis-block micronucleus cytome assay. Cells treated with MB extract combined with doxorubicin (DXR) showed increased NUBDs, which may be related to the gene amplification of CCND1. Antimutagenic effects were also observed and may be associated with the antioxidant activities detected using the CM-H2DCFDA probe. Conclusions Our findings showed the following: (a) high concentrations of MB induced cytotoxicity and cell death by necrosis; (b) its antiproliferative effect was associated with G2/M arrest; and (c) its antioxidant activity could be responsible for the observed antimutagenic effects and for protective effects against gastrointestinal disorders previously described to MB. Although these effects are not specific to normal or tumor cells, they provide a panel of biological activities for further exploration. Department of Biological Sciences Faculty of Pharmaceutical Sciences São Paulo State University (UNESP) Department of General Biology Center of Biological Sciences State University of Londrina (UEL) Experimental Campus of São Vicente São Paulo State University (UNESP) Instituto de Investigaciones Biológicas Clemente Estable Department of Biological Sciences Faculty of Sciences São Paulo State University (UNESP) Department of Botany Institute of Bioscience São Paulo State University (UNESP) Department of Biological Sciences Faculty of Pharmaceutical Sciences São Paulo State University (UNESP) Experimental Campus of São Vicente São Paulo State University (UNESP) Department of Biological Sciences Faculty of Sciences São Paulo State University (UNESP) Department of Botany Institute of Bioscience São Paulo State University (UNESP)

Inflammation and haemorrhage are the main characteristics of tissue injury in botropic envenomation. Although some studies have shown that anti-venom prevents systemic reactions, it is not efficient in preventing tissue injury at the site of the bite. Therefore, this work was undertaken to investigate the anti-inflammatory effects of the methanolic extract and fractions from D. elliptica and to evaluate the role of matrix metalloproteinases (MMPs) in this process. Effects of the extract and fractions from D. elliptica were evaluated using a carrageenan-induced paw oedema model in rats, and leukocyte rolling was visualized by intravital. The quantification of MMPs activities (MMP-2 and MMP-9) extracted from the dermis of mice treated with extract and fractions alone or incubated with venom was determined by zymographic analyses. Our results show that intraperitoneal (i.p.) injection of fractions significantly reduced paw oedema after the carrageenan challenge. Treatment with the tannins fraction also resulted in considerable inhibition of the rolling of leukocytes and this fraction was able to decrease the activation of MMP-9. These results confirmed the anti-inflammatory activity of the methanolic extract and tannins fraction of D. elliptica and showed that the dermonecrosis properties of B. jararaca venom might be mediated through the inhibition of MMP-9 activity.

Made available in DSpace on 2018-12-11T17:00:27Z (GMT). No. of bitstreams: 0 Previous issue date: 2016-04-01 Crack cocaine is a very toxic product derived from cocaine. The aim of this study was to evaluate genetic damage in multiple organs of rats following acute exposure to crack cocaine. A total of 20 Wistar rats were distributed into four groups (n = 5), as follows: 0, 4.5, 9, and 18 mg/kg body weight (b.w.) of crack cocaine administered by intraperitoneal route (i.p.). All animals were killed 24 h after intraperitoneal (i.p.) injection. The results showed that crack cocaine increased the number of micronucleated cells in bone marrow cells exposed to 18 mg/kg crack cocaine (p < 0.05). Peripheral blood and liver cells presented genetic damage as depicted by single cell gel (comet) assay at 9 and 18 mg/kg doses (p < 0.05). Immunohistochemistry data revealed significant increase in 8-hydroxy-20-deoxyguanosine (8-OHdG) immunoexpression in hepatocytes of animals exposed to crack cocaine at 9 and 18 mg/kg (p < 0.05) when compared with negative controls. Taken together, our results demonstrate that crack cocaine is able to induce genomic damage in multiple organs of Wistar rats. Departamento de Biociências Universidade Federal de São Paulo-UNIFESP, Av. Ana Costa 95 Department of Pathology Federal University of Sao Paulo UNIFESP Sao Paulo State University UNESP, Campus Litoral Paulista Department of Sea Sciences Federal University of Sao Paulo UNIFESP Sao Paulo State University UNESP, Campus Litoral Paulista

Made available in DSpace on 2015-10-21T13:11:49Z (GMT). No. of bitstreams: 0 Previous issue date: 2015-01-01. Added 1 bitstream(s) on 2015-10-22T09:52:15Z : No. of bitstreams: 1 WOS000355473600001.pdf: 3508222 bytes, checksum: 585c6d6123ab9cb7c0936e3b651ffaff (MD5) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) PROPE Several species of Bauhinia are used in traditional medicine for the treatment of gastrointestinal diseases, diabetes, and inflammation, among other conditions. The aim of this study was to investigate the antiulcer effect of a hydroalcoholic extract from the leaves of B. holophylla. The chemical profile of the extract was determined by HPLC-PAD-ESI-IT-MS. A dose-effect relation was constructed using the ethanol-induced gastric ulcer model in male Wistar rats. Histological analyses and studies of antioxidant and anti-inflammatory activities were performed in stomach samples. The involvement of SH compounds, NO, K-ATP(+) channels, and alpha(2)-adrenergic receptors in the gastroprotective effect was evaluated. A toxicity study was performed with a single oral dose of 5000 mg/kg. The extract was composed mainly of cyanoglucoside and flavonol-O-glycosides derivatives of quercetin and myricetin. SH compounds, NO release, K-ATP(+) channel activation, and presynaptic alpha(2)-adrenergic receptor stimulation each proved to be involved in the antiulcer effect. The levels of GSH and activity of GR and GPx were increased, and the levels of TNF-alpha, IL-6 and IL-10 were modulated. There was an antidiarrheal effect and there were no signs of toxicity. B. holophylla presents antiulcer activity mainly by decreasing oxidative stress and attenuating the inflammatory response, without inducing side effects. Department of Structural and Functional Biology, Institute of Biology, University of Campinas (Unicamp), 13083-862 Campinas, SP, Brazil Laboratory of Experimentation of Natural Products, Morphology Department, Institute of Biosciences, Universidade Estadual Paulista (UNESP), 18618-970 Botucatu, SP, Brazil Botany Department, Institute of Biosciences, Universidade Estadual Paulista (UNESP), 18618-970 Botucatu, SP, Brazil Biological Science Department, Science Faculty, Universidade Estadual Paulista (UNESP), 17033-360 Bauru, SP, Brazil Experimental Campus of the Paulista Coast, Universidade Estadual Paulista (UNESP), 11330-900 São Vicente, SP, Brazil Clinics Veterinary Department, School of Veterinary Medicine and Animal Science, Universidade Estadual Paulista (UNESP), 18618-970 Botucatu, SP, Brazil. FAPESP: 09/52237-9 FAPESP: 12/05323-0

Turnera ulmifolia is a plant popularly known in Brazil and South America as chanana. Some species of Turnera are widely used in folk medicine for different types of inflammatory diseases. In this study, the preventive intestinal antiinflammatory activity of a lyophilized infusion obtained from the aerial parts of T. ulmifolia was tested in the trinitrobenzenesulphonic acid (TNBS) model of rat colitis. The results obtained revealed that pretreatment to colitic rats with the extract, at 250 and 500 mg/kg, significantly attenuated the colonic damage induced by TNBS. This beneficial effect was associated with an improvement in the colonic oxidative status, since the infusion prevented the glutathione depletion that occurred as a consequence of the colonic inflammation. On the other hand, this antioxidant activity was confirmed in in vitro studies. In conclusion, the preventive effect exerted by the lyophilized infusion of T. ulmifolia in the TNBS model of rat colitis is probably related to its antioxidant properties, due to its flavonoids content.

The methanolic extract of the bark of the medicinal plant Qualea parviflora (Vochysiaceae) contains new nor-seco-triterpene and pentacyclic triterpenoids. They were separated in a preparative scale using droplet counter-current chromatography. The optimum solvent used was composed of a mixture of CHCl3/MeOH/H2O (43:37:20, v/v) in the descending mode and led to a successful separation of the new compound 28-nor-17, 22-seco-2α, 3β, 19, 22, 23-pentahydroxy-Δ12-oleanane, besides the known triterpenoids bellericagenin B, bellericaside B and arjunglucoside I . Identification was performed by ESI-MS, 1H NMR and 13C NMR analyses.

Several plants are used in folk medicine to treat gastrointestinal disorders. Mouriri pusa Gardn. (Melastomataceae) is a medicinal plant commonly used in the central region of Brazil against gastric ulcer. Two organic extracts methanolic (MeOH) and dichloromethane (DCM) obtained by sequential extraction from the leaves of Mouriri pusa were evaluated for their ability to protect the gastric mucosa against injuries caused by necrotizing agents (0.3 M HCl/60% EtOH, absolute ethanol, non-steroidal anti-inflammatory drug, stress and pylorus ligature) in mice and rats. The best results were obtained after pretreatment with MeOH extract whereas the DCM extract did not show the same significant antiulcerogenic activity. No acute toxicity was observed in animals treated with 5 g/kg, p.o. of MeOH extract. The mechanism involving the antiulcerogenic action of MeOH extract seemed to be related to NO generation and also suggested the effective participation of endogenous sulfhydryl group in the gastroprotective action. Phytochemical investigation of the MeOH extract of Mouriri pusa yielded tannins, flavonoids and (-)-epicatechin. The presence of these phenolic compounds probably would explain the antiulcerogenic effect of the polar extract of Mouriri pusa leaves.

From the ethanol extract of the capitula and scapes of Syngonanthus bisulcatus (Koern) Ruhland the flavonoids 5-hydroxy-7,4'-dimethoxy-6-C-beta-D-glucopyranosylflavone, isovitexin (5,7,4'-trihydroxy-6-C-beta-D-glucopyranosylflavone), luteolin (5,7,3',4'-tetrahydroxyflavone), lutonarin (5,3',4'-trihydroxy-6-C-7-O-beta-D-glucopyranosylflavone) and 5,6,3',4'-tetrahydroxy-7-O-beta-D-glucopyrade were isolated. The structure of the compounds were characterized by spectroscopic methods, mainly 1D and 2D NMR experiments, as well as ESMS spectrometry. In addition we examined the effect of the ethanol extract of capitulae and scapes in the ulcer model ethanol/HCl-induced gastric mucosal lesions.Do extrato etanólico dos capítulos e dos escapos de Syngonanthus bisulcatus (Koern) Ruhland foram isolados os flavonóides: 5-hidroxi-7,4'-dimetoxi-6-C-beta-D-glicopiranosilflavona, isovitexina (5,7,4'-triidróxi-6-C-beta-D-glicopiranosilflavona, luteolina (5,7,3',4'- tetraidroxiflavona), lutonarina (5,3',4'-triidroxi-6-C-7-O-beta-D-glicopiranosilflavona) e 5,6,3',4'-tetraidroxi-7-O-beta-D-glicopiranosilflavona. As estruturas dos compostos foram caracterizadas por espectroscopia (RMN mono e bi-dimensionais) e por espectrometria de massas Electrospray. Adicionalmente foram examinados os efeitos dos extratos etanólicos dos capítulos e dos escapos pelo modelo de úlcera induzida por etanol/HCl

Byrsonima crassa is a plant pertaining to the Brazilian central savannah-like belt of vegetation and popularly used for the treatment of gastric dysfunctions and diarrhoea. The methanol extract contains catechin, tannins, terpenes and flavonoids; both mutagenic potential and antioxidant properties have been ascribed to flavonoids. The mutagenicity of some flavonoids is believed to be associated with the formation of reactive oxygen species and seems to depend on the number and position of hydroxyl groups. In the present study the mutagenic activity of the methanol, chloroform and 80% aqueous methanol extracts, as well as acetate and aqueous sub-fractions, of this medicinal plant were evaluated by Salmonella typhimurium assay, using strains TA100, TA98, TA102 and TA97a, and in mouse reticulocytes. The results showed mutagenic activity of the methanolic extract in the TA98 strain without S9, but no mutagenicity to mouse cells in any of the extracts. The acetate fraction showed strong signs of mutagenicity without S9, suggesting that in this enriched fraction were concentrated the compounds that induced mutagenic activity. The aqueous fraction showed no mutagenic activity. The TLC and HSCCC analyses of the acetate fraction with some standard compounds permitted the isolation of the quercetin-3-O-beta-D-galactopyranoside, quercetin-3-O-alpha-L-arabinopyranoside, amentoflavone, methyl gallate and (+)-catechin, of which only the amentoflavone exhibited positive mutagenicity to TA98 (+S9, -S9).

A naphthopyranone dimer, named planifolin, was isolated from a methylene chloride extract of the capitula of Paepalanthus planifolius Koern. The molecule (C(31)H(26)O(10)) appeared to be made up of two monomeric portions, semi-vioxanthin and paepalantine (an isocoumarin), linked by an ether bond, and it may possess several kinds of biological activity that can be related to its polyphenolic structure. Short-term tests that detect genetic damage can afford the information needed to evaluate carcinogenic risks of chemicals to humans. The Ames test, recommended for testing the mutagenicity of chemical compounds with potential pharmacological application, was used in the present study. The mutagenic activity was evaluated in Salmonella typhimurium strains TA100, TA98, TA102 and TA97a and the cytotoxic effect in McCoy cells. The in vitro cytotoxicity of planifolin to McCoy cells, tested in microculture with neutral red, showed a significant cytotoxic index (CI(50)) of 12.83 microg/mL. Planifolin showed mutagenic activity for TA100, TA98 and TA97a. The results indicate that this new naphthopyranone dimer causes mutations by substitution and by addition and deletion of bases in the sequence of DNA. Moreover, its mutagenic potential was increased by metabolic activation.

This study was designed to determine the effect of Mangifera indica flowers decoction, on the acute and subacute models of induced ulcer in mice and rats. A single oral administration of the aqueous decoction (AD) from M. indica up to a dose of 5 g/kg, p.o. did not produce any signs or symptom of toxicity in the treated animals. The oral pre-treatment with AD (250, 500 and 1000 mg/kg) in rats with gastric lesions induced by ethanol, decreased the gastric lesions from 89.0 ± 6.71 (control group) to 9.25 ± 2.75, 4.50 ± 3.30 and 0, respectively. Pretreatment with AD (250, 500 and 1000 mg/kg) to mice with HCl/ethanol- or stress-induced gastric lesions resulted in a dose-dependent significant decrease of lesion index. In the piroxicam-induced gastric lesions, the gastroprotective effect of AD was reducing with the increase of the AD dose. In the pylorus-ligature, AD (p.o.) significantly decreased the acid output indicating the antisecretory property involved in the gastroprotective effect of M. indica . Treatment with AD during 14 consecutive days significantly accelerated the healing process in subacute gastric ulcer induced by acetic acid in rats. Pretreatment with N -nitro- l -arginine methyl ester ( l -NAME), an inhibitor of NO-synthase, did not abolish the gastroprotective effects (99% with saline versus 80% with l -NAME) of AD against ethanol-induced gastric lesions. Pretreatment with N -ethylmaleimide (NEM), a blocker of endogenous sulphydryl group, significantly abolished the protective effects of AD against ethanol-induced gastric ulcers (95% with saline versus 47% with NEM). Phytochemical screening showed the presence of steroids, triterpenes, phenolic compounds and flavonoids. Estimation of the global polyphenol content in the AD was performed by Folin–Ciocalteu method and showed approximately 53% of total phenolic on this extract. These findings indicate the potential gastroprotective and ulcer-healing properties of aqueous decoction of M. indica flowers and further support its popular use in gastrointestinal disorders in Caribbean.

Qualea grandiflora is one of the species widely used in folk medicine to treat gastric ulcers in Cerrado of the central region of Brazil. The hydroalcoholic extract of bark (HE) of Qualea grandiflora was investigated for their ability to prevent and heal lesions in the gastric mucosa. The oral administration of HE exhibited antiulcer activity decreasing the ulcerative index induced by HCl/ethanol solution, indomethacin/bethanechol and stress. In the Shay model, results showed that HE (p.o.) only reduced the severity of gastric lesions without effects on pH, gastric acidity or volume. When given by intraduodenal route, HE changed the pH, but did not modify the other parameters of the gastric juice. These data were in accordance with those obtained when HE was administered orally for 14 days after gastric ulcers were induced by acetic acid in rats. HE presented healing process in subacute gastric ulcer induced by acetic acid in rats. Moreover, histological examinations showed the simple columnar epithelium, lamina propria with simple branched tubular glandules with dilated lumen and large amounts of mucus secretion. Phytochemical investigation of HE led to the detection of terpenes, steroids, saponins, phenolic compounds and tannins in this extract, which may be involved in the observed activity.

The stem-bark extract of Carpolobia lutea (Polygalaceae), used in ethno-medicine as anti-diarrhea was pharmacologically evaluated. This was the first report of assessment of the ethanolic stem extract (ESE), of C. lutea as anti-diarrhoeal agent in rats. The anti-diarrhoeal effects, acute toxicity and ionic profile are investigated and reported.The acute toxicity was established using Lock's method. The anti-diarrhoeal effects were demonstrated using castor oil-induced diarrheal and fluid accumulation and its effect on normal intestinal transit. The mechanism elucidated using yohimbine, isosorbide dinitrate, and diphenoxylate. The elemental and ionic profile of ESE was established using inductively coupled argon-plasma emission spectrometer and potentiometric titration respectively. The finger print of ESE was revealed by Jasco (Tokyo, Japan), HPLC and active compounds by phytochemical screening using standard procedure.The LD50 obtained is 866.025 mg/kg (i.p). The doses of 43.3, 86.6, and 173.2 mg/kg of ESE showed inhibition of castor oil-induced diarrheal (p0.05 -0.001). The most abundant cations in the extract are potassium and phosphorus (1.00 ±0.01 and 0.80 ± 0.030 mg/g respectively); while the most abundant anions are phosphate and sulphate (33.50±7.09 and 7.19±3.29 mg/g respectively). The HPLC fingerprint of ESE revealed UV spectra of biomolecules. Phytochemical screening revealed presence of saponins, polyphenols and glycosides.These investigations indicate presence of bioactive and elemental substances which could play major role in diarrheal management. This investigation justifies the use of stem-bark of C. lutea in illicit gin (akpatashi), among the Effiks in Nigeria as antidiarrheal.

Submitted by Guilherme Lemeszenski (guilherme@nead.unesp.br) on 2013-08-22T18:57:17Z No. of bitstreams: 1 S0102-33062005000400007.pdf: 79717 bytes, checksum: da28e9037eecb4f69b401e9dd3222a9b (MD5) Made available in DSpace on 2013-08-22T18:57:17Z (GMT). No. of bitstreams: 1 S0102-33062005000400007.pdf: 79717 bytes, checksum: da28e9037eecb4f69b401e9dd3222a9b (MD5) Previous issue date: 2005-12-01 Made available in DSpace on 2013-09-30T19:51:55Z (GMT). No. of bitstreams: 2 S0102-33062005000400007.pdf: 79717 bytes, checksum: da28e9037eecb4f69b401e9dd3222a9b (MD5) S0102-33062005000400007.pdf.txt: 19741 bytes, checksum: 61a52a8233cfb4fab2713eeef960d425 (MD5) Previous issue date: 2005-12-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T15:13:31Z No. of bitstreams: 2 S0102-33062005000400007.pdf: 79717 bytes, checksum: da28e9037eecb4f69b401e9dd3222a9b (MD5) S0102-33062005000400007.pdf.txt: 19741 bytes, checksum: 61a52a8233cfb4fab2713eeef960d425 (MD5) Made available in DSpace on 2014-05-20T15:13:31Z (GMT). No. of bitstreams: 2 S0102-33062005000400007.pdf: 79717 bytes, checksum: da28e9037eecb4f69b401e9dd3222a9b (MD5) S0102-33062005000400007.pdf.txt: 19741 bytes, checksum: 61a52a8233cfb4fab2713eeef960d425 (MD5) Previous issue date: 2005-12-01 Este trabalho apresenta o estudo de substâncias apolares obtidas a partir de plantas pertencentes ao gênero Paepalanthus Mart. (Eriocaulaceae). Hidrocarbonetos alifáticos de cadeias longas lineares foram identificados por CG-DIC e CG-EM. Os resultados indicam que as espécies de Paepalanthus subg. Platycaulon apresentam perfil homogêneo, com cadeias carbônicas de n-alcanos variando de C25 a C31, com a maioria das amostras apresentando freqüências maiores dos homólogos C27 e C29. As espécies do subgênero Paepalocephalus podem ser diferenciadas pela distribuição dos n-alcanos principais. P. macrocephalus, uma espécie da subseção Aphorocaulon, apresenta perfil com alcanos de cadeia ímpar, enquanto P. denudatus e P. polyanthus, espécies da seção Actinocephalus, apresentam perfil bem distinto, com grande número de cadeias mais curtas e alta freqüência de cadeias com número par de carbonos, especialmente P. polyanthus. Os resultados obtidos indicam que a distribuição de nalcanos pode ser útil como caráter taxonômico, assim como as substâncias mais polares, como os flavonóides glicosilados. This work presents the study of nonpolar compounds from plants belonging to the genus Paepalanthus Mart. (Eriocaulaceae). Long-chain linear aliphatic hydrocarbons were identified by GC-FID and GC-MS. The results indicate that Paepalanthus subg. Platycaulon species present a very homogenous profile, with carbon chains of n-alkanes ranging from C25 to C31, most samples presenting higher frequencies of C27 and C29 homologues. Paepalanthus subg. Paepalocephalus species may be distinguished from one another by the distribution of main n-alkanes. P. macrocephalus, subsect. Aphorocaulon species, presents alkanes with odd-carbon numbers and P. denudatus and P. polyanthus, Actinocephalus species, present alkanes with quite distinctive profiles, with many shorter chains and a high frequency of even-carbon number, especially P. polyanthus. The results obtained indicate that the distribution of alkanes can be a useful taxonomic character, as do polar compounds like flavonoid glycosides. Universidade Estadual Paulista Instituto de Química Departamento de Química Orgânica Universidade Estadual Paulista Faculdade de Ciências Departamento de Ciências Biológicas Universidade Estadual Paulista Instituto de Química Departamento de Química Orgânica Universidade Estadual Paulista Faculdade de Ciências Departamento de Ciências Biológicas

Two new and six known flavonoids and two known naphthopyranones have been isolated by chromatographic methods and spectrometrically identified in capitulae and scapes of Eriocaulon ligulatum (Vell.) L.B. Smith (Eriocaulaceae). The presence of naphthopyranones suggests approximation between Eriocaulon and Paepalanthus genus.