DEFAR - Departamento de Farmácia
URI permanente desta comunidadehttp://www.hml.repositorio.ufop.br/handle/123456789/530
Navegar
9 resultados
Resultados da Pesquisa
Item Chromatographic profile of xanthones and flavonoids in the anti-dengue extracts of Fridericia samydoides (Cham.) L.G. Lohmann (Bignoniaceae).(2022) Fonseca, Juliane Morais da; Reis, Adriana Cotta Cardoso; Pereira, Guilherme Rocha; Moura, Hélia Maria Marques de; Souza Filho, José Dias de; Silva, Breno de Mello; Brandão, Geraldo CélioThe flavonoids and xanthones present in the ethanol extracts of leaves and stems of Fridericia samydoides showed that anti-dengue activities in vitro were investigated qualitatively by liquid chromatography–ultraviolet-mass spectrometry in series. Nineteen flavones and fifteen xanthones were detected and characterized on the basis of their fragmentation pattern in the positive and negative ion mode tandem mass spectrometry spectra and ultraviolet bands. Acacetin, chrysin, vitexin, isovitexin, orientin, isoorientin, mangiferin, 2’-O-trans-caffeoylmangiferin, 2’-O-trans-coumaroylmangiferin and 2’-O-trans-cinnamoylmangiferin were identified by comparison with authentic samples. The other compounds detected were tentatively assigned by analysis of the spectral data and by comparison with literature reports. In addition, it performed the fractionation of the leaves extract leading to the isolation of mangiferin, isovitexin and isoorientin. All extracts and isolated compounds inhibited the Dengue virus replication cycle with EC50 less than 25.0 μg/mL for extracts and 272.5, 85.6 and 79.3 μg/mL for mangiferin, isovitexin and isoorientin, respectively.Item Cytotoxic activity of extracts from Tecoma species and isolated lignans.(2022) Reis, Adriana Cotta Cardoso; Silva, Breno de Mello; Souza Filho, José Dias de; Pereira, Guilherme Rocha; Brandão, Geraldo CélioA phytochemical study of Tecoma genus (Bignoniaceae) was accomplished by antitumor activity of ethanolic extracts. Species of this genus are composed of small shrubs often used as ornamental plants. The Tecoma stans species is used in folk medicine for different purposes. Recent work shows in vitro anticancer activity against human breast cancer. The ethanolic extracts from leaves and trunks of Tecoma casneifolia, T. garrocha, T. stans var. angustata and T. stans var. stans were tested in vitro. The assays used were against line tumor cells by the MTT method and the most active extracts were further studied. In this way, the ethanolic extract from T. stans var. stans trunks presented the higher cytotoxicity against the tumor cell lines studied (CC50 0.02 to 0.55 μg/ml) when compared to the other extracts tested (CC50 0.08 to 200.0 μg/ml). Accordingly, this extract was selected for chromatographic fractionation from which five known lignans were isolated. Further, paulownin, paulownin acetate, sesamin, olivil and cycloolivil were identified using 13C and 1 H NMR, IR, UV and spectroscopy and spectrometric MS techniques. These isolated compounds were tested and exhibited CC50 ranging from 13.01 to100.0 μg/ml which is superior to the ethanolic extract of trunk of T. stans.Item Chemical analysis of Eruca sativa ethanolic extract and its effects on hyperuricaemia.(2022) Teixeira, Arthur Ferrari; Souza, Jacqueline de; Dophine, Douglas Daniel; Souza Filho, José Dias de; Guimarães, Dênia Antunes SaúdeIn vivo assays and chemical analyses were performed on the ethanolic extract from leaves of Eruca sativa. UHPLC-ESI-QTOF analysis confirmed the presence of glucosinolates and flavonol glucosides. The major flavonoid of the ethanolic extract, kaempferol-3,40 -di-O-β-glucoside, was isolated, a HPLC-DAD method developed and validated to quantify its content in the extract. In vivo experiments were carried out on Wistar rats with hyperuricaemia induced by potassium oxonate and uric acid. A hypouricaemic effect was observed in hyperuricaemic Wistar rats treated with ethanolic extract at dose of 125 mg/kg and kaempferol-3,40 -di-O-β-glucoside at dose of 10 mg/kg. The main anti-hyperuricaemic mechanism observed in the extract was uricosuric. Kaempferol-3,40 -di-O-β- glucoside was identified as an important component responsible for the total activity of the ethanolic extract and was considered as a good chemical and biological marker of the ethanolic extract of E. sativa. The obtained results indicated the potential of E. sativa in the treatment of hyperuricaemia and its comorbidities.Item Synthesis by click reactions and antiplasmodial activity of Lupeol 1,2,3-Triazole derivatives.(2017) Borgati, Tatiane Freitas; Pereira, Guilherme Rocha; Brandão, Geraldo Célio; Santos, Juliana de Oliveira; Fernandes, Dayane Aparecida Morais; Paula, Renata Cristina de; Nascimento, Maria Fernanda Alves do; Soares, Luciana Ferreira; Lopes, Júlio César Dias; Souza Filho, José Dias de; Oliveira, Alaíde Braga deLupeol, a triterpene frequently found in Asteraceae plant species, showed moderate to low activity in different strains of Plasmodium falciparum, the most virulent malaria etiological agents. In this work, lupeol was isolated from Parahancornia fasciculata, a plant that is used to treat malaria in the Amazonia region. In the search of more activity lupeol derivatives, five new 1,2,3-triazole hybrid molecules were synthetized by copper-catalyzed azide-alkyne cycloaddition. The antiplasmodial activity of the semi-synthetic compounds were evaluated by the lactate dehydrogenase assay; the lupeol propargyl ether was the only one to disclosing increased activity (half maximal inhibitory concentration-IC50-62.0 ± 1.92 μmol L-1) in relation to lupeol (IC50 117.00 μmol L-1). Therefore, this work revealed a new class of interesting lupeol derivatives that can be obtained by linking electron donors to the hydroxy group at C-3.Item Antiviral activity of Fridericia formosa (Bureau) L. G. Lohmann (Bignoniaceae) extracts and constituents.(2017) Brandão, Geraldo Célio; Kroon, Erna Geessien; Souza Filho, José Dias de; Oliveira, Alaíde Braga deA phytochemical study of Fridericia formosa (Bignoniaceae) ethanol extracts of leaves, stems, and fruits was guided by in vitro assays against vaccinia virus Western Reserve (VACV-WR), human herpes virus 1 (HSV-1), murine encephalomyocarditis virus (EMCV), and dengue virus type 2 (DENV-2) by the MTT method. All the ethanol extracts were active against DENV-2, HSV-1, and VACV-WRwith best results for the fruits extract against DENV-2 (SI > 38.2). For VACV-WRand HSV-1, EC50 values > 200 𝜇g mL−1 were determined, while no inhibition of the cytopathic effect was observed with EMCV. Five compounds were isolated and identified as the C-glucosylxanthones mangiferin (1), 2-O-trans-caffeoylmangiferin (2), 2-O-trans-coumaroylmangiferin (3), 2- O-trans-cinnamoylmangiferin (5), and the flavonoid chrysin (4). The most active compound was 2-O-trans-coumaroylmangiferin (3) with SI > 121.9 against DENV-2 and 108.7 for HSV-1. These results indicate that mangiferin cinnamoyl esters might be potential antiviral drugs.Item Anti-inflammatory and antinociceptive activities of Campomanesia adamantium.(2013) Ferreira, Lidiane Cristina; Guimarães, Andrea Grabe; Paula, Carmem Aparecida de; Michel, Marcela Carolina de Paula; Guimarães, Raquel Gomes; Rezende, Simone Aparecida; Souza Filho, José Dias de; Guimarães, Dênia Antunes SaúdeEthnopharmacological relevance: Campomanesia species are used in folk medicine as anti-inflammatory, anti-rheumatic, anti-diarrheal and hypocholesterolemic. Aim of the study: The present study investigated the in vivo anti-inflammatory and antinociceptive properties of ethyl acetate (AE) and aqueous (Aq) extracts from leaves of Campomanesia adamantium and in vitro anti-inflammatory activity of AE and its isolated flavonols, myricitrin and myricetin. Materials and methods: The antinociceptive activity of AE and Aq was evaluated using acetic acid- induced writhing and formalin methods. The in vivo anti-inflammatory effect of AE and Aq was evaluated using carrageenan-induced paw oedema in mice. AE, myricitrin and myricetin were evaluated for their abilities to modulate the production of NO, TNF-a and IL-10 in LPS/IFN-g stimulated J774.A1 macrophages. Results: It was found that orally administrated AE and Aq (125 and 250 mg/kg) inhibited carrageenan- induced paw oedema in mice. AE (125 and 250 mg/kg) and Aq (125 mg/kg) reduced the time to licking at the second phase of the formalin method in vivo in mice. AE (250 mg/kg) and Aq (125 mg/kg) also reduced the number of writhes. AE, myricitrin and myricetin inhibited NO (320 mg/mL and 6.25–100 mM, respectively) and TNF-a production by macrophages (320 mg/mL for AE, 100 mM for myricitrin and 25–100 mM for myricetin). AE (160 and 320 mg/mL), myricitrin (50 and 100 mM) and myricetin (25–100 mM) increased IL-10 production by macrophages. Conclusions: The ethyl acetate and aqueous extracts from Campomanesia adamantium showed anti- nociceptive and anti-inflammatory effects supporting the use of the plant in folk medicine. The results suggest that anti-oedematogenic effect promoted by aqueous extract involves several anti- inflammatory mechanisms of action. The antinociceptive effect shown by aqueous extract can be due to the modulation of release of inflammatory mediators involved in nociception. The anti-inflammatory effects of AE and of its isolated flavonols may be attributed to inhibition of pro-inflammatory cytokines production, TNF-a and NO and to the increased of IL-10 production.Item Chemical constituents of Distictella elongata (Vahl) Urb. (Bignoniaceae).(2013) Simões, Leandro R.; Maciel, Glauber M.; Brandão, Geraldo Célio; Souza Filho, José Dias de; Oliveira, Alaíde Braga de; Castilho, Rachel OliveiraPectolinarina, uma flavona heterosídica, foi isolada do extrato etanólico das folhas de Distictella elongata (Vahl) Urb., além de uma mistura de ácidos ursólico, pomólico e oleanólico, além de β-sitosterol. Suas estruturas foram estabelecidas com base em análise espectral (RMN de 1H e 13C 1D e 2D) em comparação com a literatura. Esta é a primeira vez em que se relata a ocorrência deste flavonoide em uma espécies da família Bignoniaceae.Item Chemistry and antiviral activity of Arrabidaea pulchra (Bignoniaceae).(2013) Brandão, Geraldo Célio; Kroon, Erna Geessien; Souza, Danielle E. R.; Souza Filho, José Dias de; Oliveira, Alaíde Braga deThe aim of the present work was to carry out a bioguided isolation of antiviral chemical constituents from an ethanol extract of leaves from Arrabidaea pulchra (Cham.) Sandwith (EEAPL) that had shown in vitro activity in a previous screening using DNA and RNA viruses. The activity of EEPAL was evaluated against the DNA viruses Human herpesvirus 1 (HSV-1) and Vaccinia virus Western Reserve (VACV-WR) as well as against the RNA viruses Murine encephalomyocarditis virus (EMCV), and Dengue virus 2 (DENV-2) by the 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) colorimetric assay. Cytotoxicity was determined in LLCMK2 and Vero cells and the Selectivity Indexes (SI) were calculated. The most potent effect was observed against DENV-2 (EC50 46.8 ± 1.6 μg mL−1; SI 2.7). For HSV-1 and VACV-WR EC50 values > 200 μg mL−1 were determined, while no inhibition of the cytopathic effect was observed with EMCV. Bioguided fractionation of EEAPL by partition between immiscible solvents followed by chromatography over a Sephadex LH20 column afforded two arylpropanoid glycosides, verbascoside (AP 1) and caffeoylcalleryanin (AP 2), along with a terpenoid, ursolic acid (AP 3). AP 1 and AP 3 exhibited similar anti-DENV-2 profiles, with SI values of 3.8 and 3.1, respectively, while AP 2 was the most effective anti-DENV-2 constituent, with a SI of 20.0. Our results show that A. pulchra leaves ethanol extract (EEAPL) affords compounds with antiviral activity, mainly against DENV-2.Item Pharmacological basis for use of Lychnophora trichocarpha in gouty arthritis : anti-hyperuricemic and anti-inflammatory effects of its extract, fraction and constituents.(2012) Souza, Maíra Ribeiro de; Paula, Carmem Aparecida de; Resende, Michelle Luciane Pereira de; Guimarães, Andrea Grabe; Souza Filho, José Dias de; Guimarães, Dênia Antunes SaúdeEthnopharmacological relevance: The ethanolic extract of Lychnophoratrichocarpha Spreng. is used in Brazilian folk medicine to treat bruise, pain and inflammatory diseases. Aim of the study: The present study aimed at investigating whether ethanolic extract of L. trichocarpha, its ethyl acetate fraction and its main bioactive compounds could be useful to treat gouty arthritis by countering hyperuricemia and inflammation. Materials and methods: L. trichocarpha ethanolic extract (LTE), ethyl acetate fraction from ethanolic extract (LTA) and isolated compounds were evaluated for urate-lowering activity and liver xanthine oxidase (XOD) inhibition in oxonate-induced hyperuricemic mice. Anti-inflammatory activity in monosodium urate crystal-induced paw oedema, an experimental model of gouty arthritis, was also investigated. Results: Crude ethanolic extract and its ethyl acetate fraction showed significant urate-lowering effects. LTE was also able to significantly inhibit liver xantine oxidase (XOD) activity in vivo at the dose of 250 mg/kg. Luteolin, apigenin, lupeol, lychnopholide and eremantholide C showed the anti-hyperuricemic activities among tested compounds. Apigenin also showed XOD inhibitory activity in vivo. Luteolin, lychnopholide, lupeol and eremantholide C, in turn, did not shown significant inhibitory activity towards this enzyme, indicating that this mechanism is not likely to be involved in urate-lowering effects of those compounds. LTE, LTA, lupeol, β-sitosterol, lychnopholide, eremantholide, luteolin and apigenin were also found to inhibit monosodium urate crystals-induced paw oedema in mice. Conclusions: Ethanolic extract of Lychnophoratrichocarpha and some of its bioactive compounds may be promising agents for the treatment of gouty arthritis since they possesses both anti-hiperuricemic and anti-inflammatory properties.