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Trypanocidal Activity of Limonoids and Triterpenes from Cedrela fissilis

LEITE, Ana Cristina; AMBROZIN, Alessandra Regina Pepe; FERNANDES, Joao Batista; VIEIRA, Paulo Cezar; SILVA, Maria Fatima das Gracas Fernandes da; ALBUQUERQUE, Sergio de
Fonte: GEORG THIEME VERLAG KG Publicador: GEORG THIEME VERLAG KG
Tipo: Artigo de Revista Científica
ENG
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Chagas` disease is an illness that affects millions of people in Central and South America, The search for both a prophylactic drug to be added to human blood as well as a safe and reliable therapeutic drug are greatly needed to control such disease. Herein, we report the trypanocidal activity of 15 crude extracts and 14 Compounds (limonoids and triterpenes) as well as the isolation of 25 known compounds (6 limonoids, 12 triterpenes, 1 sesquiterpene, 5 steroids, and 1 flavonoid) from Cedrela fissilis. The present study shows that this plant is a Promising Source of active compounds for the control of Chagas` disease. The inhibitory activity found for odoratol indicates that it is potentially useful as an alternative for the chemoprophylactic gentian violet.; Fundacao de Amparo A Pesquisa do Estado de Sao Paulo (FAPESP); Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq); Coordenacao de Aperfeicoamento de Pessoal de Ensino Superior (CAPES); Financiadora de Estudos e Projetos (FINEP)

Desenvolvimento e validação de um método bioanalítico para avaliação farmacocinética de uma mistura binária de triterpenos pentacíclicos e de seus metabólitos in vivo.; Developmnet and validation of bioanalytical method for pharmacokinetic disposition of a binary mixture of pentacyclic triterpenes and their metabolites in vivo

Rodrigues, Ivanildes Vasconcelos
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Tese de Doutorado Formato: application/pdf
Publicado em 11/08/2014 PT
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A mistura triterpênica ¤ e ß- amirinas é comumente encontrada em quantidades significativas em espécies do gênero Protium (Burseraceae) e possuem reconhecidas atividades anti-inflamatória, hepatoprotetora, gastroprotetora e analgésica, dentre outras. Entretanto, pouco se sabe sobre sua farmacocinética e metabolismo. Neste sentido, esta tese teve o objetivo de desenvolver metodologias bioanalíticas para determinar a farmacocinética e a eliminação de ? e ?-amirinas isoladas de P. spruceanum bem como avaliar o metabolismo in vitro destes triterpenos. A mistura de ¤ e ß-amirinas foi isolada em grau de pureza cromatográfica acima de 99%. Foi desenvolvida e caracterizada uma nanoemulsão do tipo O/A contendo ¤ e ß-amirinas a fim de viabilizar a administração por vias oral e endovenosa e realizar os estudos de disposição cinética dessas substâncias em camundongos. O tamanho médio das partículas da nanoemulsão foi de 103,5 ± 0,44 nm, com porcentagem de encapsulação de acima de 99%. Os estudos de liberação in vitro mostraram baixa taxa de liberação após 24 horas. A avaliação da disposição cinética de ? e ?-amirinas em camundongos mostrou que após administração oral a suspensão de CMC não foi absorvida...

Triterpenos de Alibertia edulis A. rich (Rubiaceae); Triterpenes Alibertia edulis A. Rich (Rubiaceae)

Brochini, Cláudia Barbosa
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 10/05/1993 PT
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A família Rubiaceae se caracteriza por produzir uma grande variedade de metabólitos secundários. Alcalóides, triterpenos iridóides e antraquinonas destacam-se entre os produtos naturais de maior ocorrência nas rubiaceas. Espécies desta família ocorrem com frequência no cerrado brasileiro, sendo que o gênero Alibertia, não havia sido estudado até recentemente. O presente trabalho, que é o primeiro com a espécie Alibertia edulis A. Rich, descreve o isolamento, identificação e determinação estrutural de triterpenos presentes nas folhas de um espécimen coletado nas proximidades de Campo Grande, Mato Grosso do Sul. O estudo da fração clorofórmica do extrato etanólico mostrou a ocorrência predominante de triterpenos. Foram isolados através dos métodos cromatográficos usuais (coluna e placa preparativa), os pares oleanano-ursano urs-12-en-3β,28-diol e olean-12-en-3β,28-diol; 3β-hidroxiurs-12-en-28-óico e 3β-hidroxiolean-12-en-28-óico; 3β,23-diidroxiurs-12-en-28-óico e 3β,23-diidroxiolean-12-en-28-óico, que foram identificados através dos espectros de RMN de 13C e 1H. A mistura dos ésteres metílicos dos ácidos 3β, 19α,23,24-tetraidroxiurs-12-en-28-óico e 3β, 19α...

Triterpenes and antitubercular activity of Byrsonima crassa

Higuchi, Célio Takashi; Pavan, Fernando Rogério; Leite, Clarice Queico Fujimura; Sannomiya, Miriam; Vilegas, Wagner; Leite, Sergio Roberto de Andrade; Sacramento, Luis Vitor S.; Sato, Daisy Nakamura
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: 1719-1721
ENG
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP); We evaluated the potential antitubercular activity of triterpenes obtained from leaves and bark of Byrsonima crassa. From chloroform extracts of the leaves, by bioassay-guided fractionation, we obtained mixtures of known triterpenes: α-amyrin, β-amyrin and their acetates, lupeol, oleanolic acid, ursolic acid and α-amyrinone. Tested against Mycobacterium tuberculosis, the triterpenes exhibited minimum inhibitory concentrations (MICs) of 31.25 - 312.25 µg/mL. β-amyrin and friedelin, isolated from the chloroform extract of bark, showed MICs of 312.25 and 125 µg/mL respectively. This is the first report of the identification and determination of the activity of B. crassa triterpenes against M. tuberculosis.

Identification of triterpenes and sterols from pterogyne nitens (fabaceae-caesalpinioideae) using high-resolution gas chromatography

Regasini, Luis Octavio; Vieira-Junior, Gerardo Magela; Fernandes, Daniara Cristina; Bolzani, Vanderlan da Silva; Cavalheiro, Alberto José; Siqueira Silva, Dulce Helena
Fonte: Soc Chilena Quimica Publicador: Soc Chilena Quimica
Tipo: Artigo de Revista Científica Formato: 218-221
ENG
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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); Processo FAPESP: 04/07932-7; As part of our ongoing bioprospecting studies on secondary metabolites in plants of Cerrado and Atlantic Rain Forest of São Paulo State (Brazil), we describe the identification of triterpenes and sterols present in the hexane extracts and foliar epicuticular wax of Pterogyne nitens Tulasne (Fabaccae-Caesalpinioideae) using high resolution gas chromatography. Compounds detected in these extracts include beta-amyrin (1), taraxerol acetate (2), lupenone (3), beta-amlyrenone (4), germanicone (5), campesterol (6), stigmasterol (7), and beta-sitosterol (8). The method reported herein is shown to be a rapid, sensitive and reproducible tool for describing triterpenes and sterols present in non-polar extracts.

Antioxidant phenolic and quinonemethide triterpenes from Cheiloclinium cognatum

Jeller, A. H.; Silva, DHS; Liao, L. M.; Bolzani, Vanderlan da Silva; Furlan, Maysa
Fonte: Elsevier B.V. Publicador: Elsevier B.V.
Tipo: Artigo de Revista Científica Formato: 1977-1982
ENG
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The triterpenes, 22beta-hydroxypristimerin and cognatine, were isolated together with the known compounds pristimerin, maytenin, 20alpha-hydroxymaytenin, 22beta-hydroxymaytenin, netzahualcoyol, netzahualcoyondiol and netzahualcoyone from root bark of Chei-Ioclinium cognatum. The structures of the isolated compounds were elucidated by interpretation of their spectral data, including gHMQC and gHMBC experiments. The isolates were investigated for their radical scavenging abilities through a spectrophotometric assay involving reduction of 2,2-diphenyl-picryl hydrazyl (DPPH). (C) 2004 Elsevier Ltd. All rights reserved.

Triterpenes from Maytenus macrocarpa and evaluation of their anti-HIV activity

Piacente, Sonia; Dos Santos, Lourdes Campaner; Mahmood, Naheed; Pizza, Cosimo
Fonte: Natural Products Inc Publicador: Natural Products Inc
Tipo: Artigo de Revista Científica Formato: 1073-1078
ENG
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A set of pentacyclic triterpenes has been isolated from the bark of Maytenus macrocarpa (Celastraceae). It includes two new olean-12-ene derivatives, namely 3 beta, 22(alpha-dihydroxy-olean-12-en-30-oic acid (1) and 22 alpha-hydroxy-olean-12-en-3-oxo-30-oic acid (2), and the new urs-12-ene derivative 3-(E)-coumaroyluvaol (7), along with 10 known compounds possessing olean-12ene, urs-12-ene, lupane and friedelane skeletons. The structures have been elucidated by extensive spectroscopic methods including ID- and 2D-NMR experiments, as well as ESI-MS analysis. All isolated compounds were tested for anti-HIV activity in C8166 cells infected with HIV-1(MN), the most active compound was 22(alpha-hydroxy-12-en-3-oxo-29-oic acid (triterpenonic acid A, 4), with an EC50 value of I mu g/mL and a selectivity index of 35.

Triterpenes and saponins from Rudgea viburnioides

Young, M. Claudia M.; Araújo, Angela R.; Da Silva, Cristhiane A.; Lopes, Marcia N.; Trevisan, Ligia M. V.; Bolzani, Vanderlan da Silva
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 936-938
ENG
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A novel triterpene; viburgenin (1), has been isolated from an extract of the ripe fruit rinds of Rudgea viburnioides, together with the known saponins, arjunglucoside I and trachelosperosides B-1 and E-l, and the triterpenes trachelosperogenin B (2) and arjungenin. Compound 2 was previously obtained as a product from enzymatic hydrolysis, and it is reported for the first time as a natural product. The structure of compound 1 was determined as 2α,3β,19α,23,24-pentahydroxyurs-12-ene by extensive use of 1D and 2D NMR spectroscopic methods. Compound 1 exhibited moderate antifungal activity against Cladosporium cladosporioides.

In vitro propagation of Maytenus ilicifolia (Celastraceae) as potential source for antitumoral and antioxidant quinomethide triterpenes production. A rapid quantitative method for their analysis by reverse-phase high-performance liquid chromatography

Buffa Filho, Waldemar; Bolzani, Vanderlan da Silva; Furlan, Maysa; Vaz Pereira, Sarazete Izidia; Pereira, Ana Maria Soares; Françab, Suzelei Castro
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 137-146
ENG
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Cell culture of Maytenus ilicifolia were established in order to produce and to quantify the antitumoral and antioxidant quinonemethide triterpenes. In vitro calli were induced from leaf explants of native plants and cultured in semi-solid medium under controlled conditions of humidity, temperature and photoperiod. The quinonemethide triterpenes showed maximum accumulation in the logarithmic phase growth of the cell culture. A rapid, sensitive and reliable reverse-phase HPLC method was used for quantitative determination of the antitumoral and antioxidant quinonemethide triterpenes, 22β-hydroxymaytenin and maytenin in callus of Maytenus ilicifolia. Well resolved peaks with good detection response and linearity in the range 1.0 - 100 μg/mL were obtained. This quantitative work was performed by an external standard method.

Anti-trypanosomal activity of pentacyclic triterpenes isolated from Austroplenckia populnea (Celastraceae)

DUARTE,Lucienir Pains; VIEIRA FILHO,Sidney Augusto; SILVA,Grácia Divina de Fátima; SOUSA,José Rego de; PINTO,Artur da Silveira
Fonte: Instituto de Medicina Tropical Publicador: Instituto de Medicina Tropical
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/04/2002 EN
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Four pentacyclic triterpenes isolated from Austroplenckia populnea and four compounds of known anti T. cruzi or anti-malarial activity were tested. Of those triterpenes tested 20alpha-hydroxy-tingenone showed high activity, epikatonic acid was less active, while populnilic and populninic acids were inactive against the trypanosome of the subgenus Schizotrypanum tested. Benzonidazole, nifurtimox, ketoconazole and primaquine presented a remarkable dose-dependent inhibitory effect reaching practically to a total growth inhibition of the parasite at the end of incubation time. The trypanosome tested appear to be a suitable model for preliminary screen for anti T. (S.) cruzi compounds.

Triterpenes and antitubercular activity of Byrsonima crassa

Higuchi,Celio Takashi; Pavan,Fernando Rogério; Leite,Clarice Queico Fujimura; Sannomiya,Miriam; Vilegas,Wagner; Leite,Sergio Roberto de Andrade; Sacramento,Luis Vitor S.; Sato,Daisy Nakamura
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/01/2008 EN
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We evaluated the potential antitubercular activity of triterpenes obtained from leaves and bark of Byrsonima crassa. From chloroform extracts of the leaves, by bioassay-guided fractionation, we obtained mixtures of known triterpenes: α-amyrin, β-amyrin and their acetates, lupeol, oleanolic acid, ursolic acid and α-amyrinone. Tested against Mycobacterium tuberculosis, the triterpenes exhibited minimum inhibitory concentrations (MICs) of 31.25 - 312.25 µg/mL. β-amyrin and friedelin, isolated from the chloroform extract of bark, showed MICs of 312.25 and 125 µg/mL respectively. This is the first report of the identification and determination of the activity of B. crassa triterpenes against M. tuberculosis.

Evaluation of antimicrobial activity and toxic potential of extracts and triterpenes isolated from Maytenus imbricata

Rodrigues,Vanessa G.; Duarte,Lucienir P.; Silva,Grácia D. F.; Silva,Fernando C.; Góes,Jefferson V.; Takahashi,Jacqueline A.; Pimenta,Lúcia P. S.; Vieira Filho,Sidney A.
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/01/2012 EN
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The phytochemical study of hexane/ethyl ether (1:1) extract of the roots of M. imbricata, Celastraceae, resulted in the isolation and characterization of six known triterpenes: 11α-hydroxylup-20(29)-en-3-one, previously isolated from this species besides, 3β,11α-di-hydroxylup-20(29)-ene, 3,7-dioxofriedelane, 3-oxo-29-hydroxyfriedelane, tingenone and 6-oxo-tingenol. The chemical structures of these triterpenes were established by spectrometric data (IR, ¹H and 13C NMR) and through comparison with literature data. The hexane/ethyl ether (1:1), ethyl acetate and methanol extracts, and 11α-hydroxylup-20(29)-en-3-one, tingenone and 6-oxo-tingenol, showed antimicrobial properties on in vitro assays. All extracts and triterpenes, except 3β,11α-di-hydroxylup-20(29)-ene, presented toxicity demonstrated by the larvicidal effect test using Artemia salina.

Triterpenes from Minquartia guianensis (Olacaceae) and in vitro antimalarial activity

Cursino,Lorena Mayara de Carvalho; Nunez,Cecilia Veronica; Paula,Renata Cristina de; Nascimento,Maria Fernanda Alves do; Santos,Pierre Alexandre dos
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/01/2012 EN
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Minquartia guianensis, popularly known as acariquara, was phytochemically investigated. The following triterpenes were isolated from the dichloromethane extract of leaves: lupen-3-one (1), taraxer-3-one (2) and oleanolic acid (3). The dichloromethane extract of branches yielded the triterpene 3β-methoxy-lup-20(29)-ene (4). The chemical structures were characterized by NMR data. Plant extracts, substance 3, squalene (5) and taraxerol (6), (5 and 6 previously isolated), were evaluated by in vitro assay against chloroquine resistant Plasmodium falciparum. The dichloromethane extract of leaves and the three triterpenes assayed have shown partial activity. Thus, these results demonstrated that new potential antimalarial natural products can be found even in partially active extracts.

Triterpenes from the flowers of Gochnatia polymorpha subsp. floccosa

Silva,Luana B.; Strapasson,Regiane L. B.; Riva,Dilamara; Salvador,Marcos J.; Stefanello,Maria Élida A.
Fonte: Sociedade Brasileira de Farmacognosia Publicador: Sociedade Brasileira de Farmacognosia
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/06/2011 EN
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Phytochemical study of the flowers of Gochnatia polymorpha subsp. floccosa, Asteraceae, yielded eleven known triterpenes identified as lupeol, lupeyl acetate, lupeyl palmitate, taraxasterol, taraxasteryl acetate, pseudotaraxasterol, pseudotaraxasterol acetate, α-amyrin, α-amyryl palmitate, β-amyrin and β-amyryl palmitate, along with sitosterol, stigmasterol, palmitic and stearic acids. These compounds are been reported for the first time in the species. The compounds were identified by analysis of NMR spectra (¹H, 13C and DEPT), GC-MS and comparison with literature data. Previous work have reported the isolation of triterpenes, diterpenes, sesquiterpenes, flavonoids, coumarins and phenolic compounds from aerial parts and roots from G. polymorpha.

Evaluation of the bactericidal and trypanocidal activities of triterpenes isolated from the leaves, stems, and flowers of Lychnophora pinaster

Abreu,Viviane G. C.; Takahashi,Jacqueline A.; Duarte,Lucienir P.; Piló-Veloso,Dorila; Junior,Policarpo A. S.; Alves,Rosana O.; Romanha,Alvaro J.; Alcântara,Antônio F. C.
Fonte: Sociedade Brasileira de Farmacognosia Publicador: Sociedade Brasileira de Farmacognosia
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/08/2011 EN
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The phytochemical investigation on the aereal parts of Lychnophora pinaster Mart., Asteraceae, was carried to isolation of triterpenes. 3-O-Acetyl-lupeol (1), 3-O-acetyl-pseudotaraxasterol (2), and 3-O-acetyl-α-amyrin (3) were isolated from hexanic extract and 4,4-dimethyl-cholesta-22,24-dien-5-ol (4), α-amyrin (5), and lupeol (6) were isolated from hexanic/dichlorometanic extract of the leaves. Compounds Δ7-bauerenyl acetate (7), friedelin (8), stigmasterol (9), and sitosterol (10) were isolated from the hexanic/dichlorometanic extract of the stems. The steroids 9 and 10 were also isolated from the hexanic/dichlorometanic extract of the flowers. Triterpenes 1, 3, 4, and 7 are described for the first time in the genus Lychnophora. The apolar fractions of the leaf and stem extracts and some isolated triterpenes showed low trypanocidal activity. Moreover, apolar fractions of the leaf and stem extracts and 5 showed antibacterial action against Staphylococcus aureus.

HPLC-UV and LC-MS analysis of quinonemethides triterpenes in hydroalcoholic extracts of "espinheira santa" (Maytenus aquifolium Martius, Celastraceae) leaves

Nossack,Ana C.; Celeghini,Renata M. dos S.; Lanças,Fernando M.; Yariwake,Janete H.
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/08/2004 EN
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Some quinonemethide triterpenes are known for their cytotoxicity, and the presence of these compounds has been reported in several Maytenus (Celastraceae) species, including Maytenus aquifolium Martius, one of the species known in Brazil as "espinheira santa". A quantitative HPLC-UV procedure was therefore developed with the purpose of devising a useful analytical method for evaluating the quality of "espinheira santa"-based phytomedicines. Quinonemethide triterpenes pristimerin and maitenin were quantified in hydroalcoholic and aqueous extracts ("teas") prepared from the leaves and root bark of M. aquifolium. Analyses by liquid chromatography coupled to mass spectrometry (LC-MS), using the atmospheric pressure chemical ionization (APCI) interface, provided unequivocal confirmation of the presence of maitenin and pristimerin in M. aquifolium hydroalcoholic extracts, although these compounds were below detection limits in aqueous extracts.

Three new triterpenes from the resinous bark of Protium kleinii and their antinociceptive activity

Lima,Fabiana V.; Malheiros,Angela; Otuki,Michel F.; Calixto,João B.; Yunes,Rosendo A.; Cechinel Filho,Valdir; Delle Monache,Franco
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/06/2005 EN
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Three novel pentacyclic triterpenes have been isolated from the resin of Protium kleinii and their structures elucidated by NMR spectroscopy as 3-oxo-11beta,16beta-dihydroxy-urs-12-ene (1), 3-oxo-11beta-hydroxy-urs-12-ene (2) and 3-oxo-11beta-hydroxy-olean-12-ene (3). The systemic administration of the above compounds (10-100 mg kg-1, i.p.) was able to inhibited both first and second phase of the formalin-induced nociception in mice. The known triterpenes 3beta,16beta-dihydroxy-olean-12-ene (brein) (4) and a mixture of alpha (5)- and beta-amyrin (6) were also found.

Pentacyclic triterpenes from branches of Maytenus robusta and in vitro cytotoxic property against 4T1 cancer cells

Sousa,Grasiely Faria de; Soares,Daniel Crístian Ferreira; Mussel,Wagner da Nova; Pompeu,Nana Flora Elias; Silva,Grácia Divina de Fátima; Vieira Filho,Sidney Augusto; Duarte,Lucienir Pains
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/08/2014 EN
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Two new friedelane-type compounds 1 and 2 and five known pentacyclic triterpenes were isolated from branches of Maytenus robusta. Their structures were identified as 3,16-dioxo-29-hydroxyfriedelane (1), 3-oxo-16b,29-dihydroxyfriedelane (2), 3-oxofriedelane (3), 3b-friedelinol (4), 3,16-dioxofriedelane (5), 3-oxo-29-hydroxyfriedelane (6), and 3,16-dioxo-12a-hydroxyfriedelane (7). The structures and the stereochemistry of triterpenes 1 and 2 were established through infrared (IR), 1D/2D nuclear magnetic resonance (NMR), high-resolution atmospheric pressure chemical ionization mass spectrometry (HR-APCIMS) spectral data and powder X-ray diffraction. The in vitro cytotoxic property of triterpenes 1 to 6 on 4T1 murine breast cancer cells was evaluated. The triterpenes 1 and 2 showed cytotoxic activity against 4T1 cells at a lower concentration.

Atividade anti-tripanosomicida de triterpenes pentacíclicos isolados de Austroplenckia populnea (Celastraceae); Anti-trypanosomal activity of pentacyclic triterpenes isolated from Austroplenckia populnea (Celastraceae)

DUARTE, Lucienir Pains; VIEIRA FILHO, Sidney Augusto; SILVA, Grácia Divina de Fátima; SOUSA, José Rego de; PINTO, Artur da Silveira
Fonte: Universidade de São Paulo. Instituto de Medicina Tropical de São Paulo Publicador: Universidade de São Paulo. Instituto de Medicina Tropical de São Paulo
Tipo: info:eu-repo/semantics/article; info:eu-repo/semantics/publishedVersion; ; ; ; ; Formato: application/pdf
Publicado em 01/04/2002 ENG
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Foram testados quatro triterpenos pentacíclicos isolados de Austroplenckia populnea e quatro compostos de conhecida atividade anti-T. cruzi ou anti-malárica. Dos triterpenos testados 20alfa-hidroxi-tingenona mostrou atividade elevada, ácido epicatônico foi menos ativo, enquanto ácido populnílico e populnínico foram inativos contra o tripanossoma do subgênero Schizotrypanum testado. Benzonidazole, nifurtimox, cetoconazole e primaquina apresentaram efeito inibitório dose-dependente atingindo praticamente a inibição total do crescimento do parasita no final do tempo de incubação. O tripanossoma testado mostrou ser um modelo adequado para uma seleção preliminar de compostos anti. T. (S.) cruzi.; Four pentacyclic triterpenes isolated from Austroplenckia populnea and four compounds of known anti T. cruzi or anti-malarial activity were tested. Of those triterpenes tested 20alpha-hydroxy-tingenone showed high activity, epikatonic acid was less active, while populnilic and populninic acids were inactive against the trypanosome of the subgenus Schizotrypanum tested. Benzonidazole, nifurtimox, ketoconazole and primaquine presented a remarkable dose-dependent inhibitory effect reaching practically to a total growth inhibition of the parasite at the end of incubation time. The trypanosome tested appear to be a suitable model for preliminary screen for anti T. (S.) cruzi compounds.

Celastráceas: Fontes de Triterpenos Pentacíclicos com Potencial Atividade Biológica; Celastraceae Family: Source of Pentacyclic Triterpenes with Potential Biological Activity

Fernando César Silva; Universidade Federal de Minas Gerais; Lucienir P. Duarte; Universidade Federal de Minas Gerais; Sidney A. Vieira Filho; Universidade Federal de Ouro Preto
Fonte: Revista Virtual de Química Publicador: Revista Virtual de Química
Tipo: ; Formato: binary/octet-stream
Publicado em 01/11/2014 PT
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A família Celastraceae, comumente conhecida como família agridoce, devido ao sabor de seus frutos, possui diversos relatos de uso na medicina popular. Na América do Sul é representada, principalmente, pelo gênero Maytenus, que tem atraído a atenção de muitos pesquisadores por suas propriedades antitumorais. Dos metabólitos isolados, os triterpenos pentacíclicos se destacam, sendo que, os de esqueleto quinonametídeo são os marcadores quimiotaxônomicos dessa família. Os esqueletos triterpênicos têm 30 carbonos compreendendo cinco anéis de seis membros cada ou quatro anéis de seis membros mais um anel de cinco. Eles são de grande interesse devido às diversas atividades biológicas apresentadas, servindo como candidatos ou protótipos de novos fármacos. Devido a todas essas características, em poucos anos, inúmeros estudos têm sido dedicados aos triterpenos. DOI: 10.5935/1984-6835.20140079; The Celastraceae family, commonly known as bittersweet family due to flavor of its fruits, has several use reports in folk medicine. In South America it is mainly represented by the Maytenus genus, which has attracted the attention of many researchers for its anti-tumor properties. From the isolated metabolites, the pentacyclic triterpenes stand out...