Antibacterial and Antifungal Activities of Compounds Isolated from Gymnosporia Royleana (Celastraceae) / Actividades antibacterianas y antifúngicas de compuestos aislados de Gymnosporia Royleana (Celastraceae)

ABSTRACT Objective: In the present study, five new source compounds isolated from aerial parts of Gymnosporia royleana (G royleana) were screened for antibacterial and antifungal activities. Methods: Extraction from plant material was carried out using cold maceration technique. Isolation of pure compounds was accomplished through repeated column chromatography of different fractions obtained from crude extract and using silica gel as stationary phase. Their structures were established via advanced spectroscopic techniques along with the spectral data previously reported for these compounds. Dilution method was used for the evaluation of antimicrobial potential of the compounds against various microbial strains. Results: Among the tested compounds, Gymnosporin B displayed moderate antimicrobial activity against Escherichia Coli (E coli), Staphylococcus aureus (S aureus), Candida albicans (C albicans) and Aspergillus flavus (A flavus) [minimum inhibitory concentration (MIC) range; 32-64 μg/mL]. Similarly, Gymnosporin C also showed moderate activity against E coli and S aureus (MIC; 32 μg/mL each) as well as weak activity against C albicans and A flavus (MIC; 64 μg/mL each). However, Royaflavone showed moderate antibacterial activity against S aureus only (MIC; 32 μg/mL). Antimicrobial activity of the rest of the compounds was weak and negligible. Conclusion: The present study has provided fascinating results of antimicrobial activities of the isolated compounds. However, the broad antimicrobial spectrum of Gymnosporin B and Gymnosporin C demands for further exploration of these triterpenes, both on the basis of mechanism and quantitative structure-activity relationship.

RESUMEN Objetivo: En el presente estudio, cinco nuevos compuestos de origen aislados de partes aéreas de Gymnosporia royleana (G royleana) fueron tamizados en sus actividades antibacterianas y antifúngicas. Métodos: La extracción de material vegetal se realizó mediante la técnica de maceración en frío. El aislamiento de compuestos puros se logró a través de la cromatografía en columna repetida de diversas fracciones obtenidas del extracto crudo y usando gel de silicona como fase estacionaria. Sus estructuras fueron establecidas mediante técnicas espectroscópicas avanzadas junto con los datos espectrales previamente reportados para estos compuestos. El método de dilución fue usado para evaluar el potencial antimicrobiano de los compuestos contra diversas cepas microbianas. Resultados: Entre los compuestos sometidos a prueba, Gymnosporina B mostró una actividad antimicrobiana moderada contra Escherichia Coli (E coli), Staphylococcus aureus (S aureus), Candida Albicans (C albicans) y Aspergillus flavus (A flavus) [rango de concentración inhibitoria mínima (CIM); 32 - 64 μg/mL]. De manera similar, Gymnosporina C también mostró actividad moderada contra E coli y S aureus (CIM; 32 μg/mL cada uno) así como débil actividad frente a C albicans y A flavus (CIM; 64 μg/mL cada uno). Sin embargo, Royaflavone mostró actividad antibacteriana moderada sólo frente a S aureus (CIM; 32 μg/mL). La actividad antimicrobiana del resto de los compuestos fue débil e insignificante. Conclusión: El presente estudio ha proporcionado resultados interesantes acerca de las actividades antimicrobianas de los compuestos aislados. Sin embargo, el amplio espectro antimicrobiano de la Gymnosporina B y la Gymnosporina C exige una mayor exploración de estos triterpenos, tanto sobre la base del mecanismo como a partir de la relación cuantitativa estructura-actividad.

Antidiarrheal activity of extracts from Maytenus gonoclada and inhibition of Dengue virus by lupeol

ABSTRACT Diarrhea is an infectious disease caused by bacterial, virus, or protozoan, and dengue is caused by virus, included among the neglected diseases in several underdeveloped and developing countries, with an urgent demand for new drugs. Considering the antidiarrheal potential of species of Maytenus genus, a phytochemical investigation followed by antibacterial activity test with extracts of branches and heartwood and bark of roots from Maytenus gonoclada were conducted. Moreover, due the frequency of isolation of lupeol from Maytenus genus the antiviral activity against Dengue virus and cytotoxicity of lupeol and its complex with β-cyclodextrins were also tested. The results indicated the bioactivity of ethyl acetate extract from branches and ethanol extract from heartwood of roots of M. gonoclada against diarrheagenic bacteria. The lupeol showed potent activity against Dengue virus and low cytotoxicity in LLC-MK2 cells, but its complex with β-cyclodextrin was inactive. Considering the importance of novel and selective antiviral drug candidates the results seem to be promising.

Maytenus distichophylla and Salacia crassifolia: source of products with potential acetylcholinesterase inhibition

ABSTRACT The phytochemical study of the extract leaves from Maytenus distichophylla Mart. and Salacia crassifolia (Mart. ex Schult.) G. Don, Celastraceae, resulted in the isolation of 3-oxofriedelane, 3β-hydroxyfriedelane, 3β,24-dihydroxyfriedelane, 3-oxo-28,29-dihydroxyfriedelane, two mixtures of pentacyclic triterpenes (α-amyrin with β-amyrin and 3β-stearyloxy-urs-12-ene with 3β-stearyloxy-olean-12-ene), 3β-palmityloxy-urs-12-ene, the steroid β-sitosterol and its glycosylated derivative β-glucosyl-β-sitosterol, tritriacontanoic acid and the natural polymer gutta percha. The chemical structures of these constituents were established by IR, 1H and 13C NMR spectral data. Crude extracts, the mixtures of triterpenes and the isolated constituents were subjected to in vitro acetylcholinesterase inhibitory evaluation. Acetylcholinesterase inhibitory effect was observed for crude chloroform extract leaves from M. distichophylla (100%) and S. crassifolia (97.93 ± 5.63%) and for the triterpenes 3β,24-dihydroxyfriedelane (99.05 ± 1.12%), 3-oxo-28,29-dihydroxyfriedelane (90.59 ± 3.76%) and 3β-palmityloxy-urs-12-ene (97.93 ± 1.47%). The percent inhibitions induced by these natural products were very similar to those produced by physostigmine (93.94 ± 2.10%) a standard acetylcholinesterase inhibitor. Therefore, these results open perspectives for the use of these species as source of compounds with similar physostigmine pharmacological effect.

Triterpenes and Beta-agarofurane sesquiterpenes from tissue culture ofMaytenus boaria / Triterpenos y Beta-agarofuranos sesquiterpenos desde cultivo de tejidos de Maytenus boaria

Leaf explants of Maytenus boaria were induced towards callus tissue culture with different mixture of cytokinins and auxins. MeOH extract of callus was partitioned with AcOEt and water, and through repeated chromatography procedures were isolated and identified, four triterpenes and three beta-agarofuran sesquiterpenes.

Explantes de hojas de Maytenus boaria fueron inducidos a formar callos mediante diferentes mezclas de citoquininas y auxinas. Un extracto metanólico de los callos fue fraccionado con AcOEt y agua, y mediante repetidas cromatografías fueron aislados e identificados siete compuestos, cuatro triterpenos y 3 sesquiterpenos del tipo agarofurano.

A new cytotoxic triterpenoid from microtropis triflora merr. et freem / 中国药学杂志

To study the chemical constituents of Microtropis triflora Merr. et Freem. METHODS: The compounds were isolated and purified by various chromatographic technigues such as silica gel, Sephadex LH -20, and pre-HPLC. Their structures were identified on the basis of chemical properties and spectral analysis. RESULTS: Ten triterpenes were isolated and elucidated as 3, 25-epoxy-lα, 3α, 11α 12, 23, 25-hexahydroxy-urs-12-en(l), β-amyrin(2), β-amyrin palmitate(3), 3β-hydroxy-l1-oxo-olean-12-enyl-3-palmitate(4), lupeol(5), friedelin (6), 3-oxo-28-friedelanoic acid(7), oleanolic acid(8), salaspermic acid (9), and orthosphenic acid(10). CONCLUSION: Compound 1 is a new compound and has cytotoxic activity against Bcap37 and SMMC7721 cells with IC50 values of 27.86 and 11.38 μg· mL-1, respectively.

Analgesic and Acute Anti-inflammatory Activities of Aqueous Root Extract of Salacia lehmbachii.

Aim: Salacia lehmbachii is used in South Eastern Nigeria folk medicine to treat abdominal pain, inflammatory disorders and malaria symptom without scientific documentation. The aim of this study was therefore, to assess possible analgesic and anti-inflammatory activities of aqueous root extract of Salacia lehmbachii (ARESL) in albino rats. Place and Duration of Study: The study was done in World Bank Step B Anti-Malaria Laboratory, Department of Pharmacology, Faculty of Basic Medical Sciences, University of Calabar, Calabar-Nigeria, between November 2013 and January 2014. Methodology: Analgesic and anti-inflammatory properties of ARESL were assessed in Wistar rats at doses of 200 and 400 mg/kg. To assess analgesic activity, acetic acidinduced writhing and formalin tests were used. To assess anti-inflammatory property, carrageenan and dextran-induced hind paw edema were used. Differences between group means were compared statistically by one-way analysis of variance (ANOVA) followed by Tukey test as post hoc. Results: In acetic acid-induced writhing test, the extract, at a dose of 400 mg/kg, showed a maximum inhibition (P=.05) of 71.66% of writhing while the standard drug Aspirin inhibited 81.05% of writhing compared to untreated control group. In formalin test, ARESL showed a maximum inhibition (P =.05) of 71.77% at a dose of 400 mg/kg while standard drug Pethidine showed 76.11%. For carrageenan-induced paw edema test, ARESL at a dose of 400 mg/kg showed maximum 85.90% inhibition (P =.05) of inflammatory activity while dextran-induced showed 87.9%. Conclusion: ARESL possesses analgesic and anti-inflammatory activities which corroborate the aqueous extract being used in folk medicine.

Ocorrência de cochonilhas em espinheira-santa (Maytenus ilicifolia Mart. ex Reissek) / Occurrence of mealybugs in "espinheira-santa" (Maytenus ilicifolia Mart. ex Reissek)

Maytenus ilicifolia é uma espécie medicinal nativa do Brasil que vem sendo cultivada para atender a crescente demanda do mercado. Os fatores que interferem na produção, tal como a incidência de pragas e doenças, devem ser estudados para garantir o incremento na produtividade. O objetivo deste trabalho foi registrar a ocorrência e a identificação de cochonilhas associadas a 15 acessos de espinheira-santa (Maytenus ilicifolia) do Banco Ativo de Germoplasma da Embrapa Clima Temperado e do Instituto Federal Sul-rio-grandense. Foi registrada a quantidade de plantas infestadas em cada acesso e identificado, em laboratório, as espécies de cochonilhas infestantes. O número de plantas infestadas variou entre os acessos. Foram identificadas as cochonilhas Ceroplastes sp. e Saissetia oleae, família Coccidae. Dos 10 acessos infestados, 23 (11,3%) plantas apresentaram infestação com Ceroplastes sp. e, apenas uma (0,5%), com Saissetia oleae. O acesso 133 mostrou a maior incidência de Ceroplastes sp. (33,3%), seguido do acesso 130 (25,0%). O acesso 123 foi o que apresentou menor quantidade de plantas infestadas (4,8%). Saissetia oleae ocorreu em apenas uma planta, pertencente ao acesso 136 (5,6%).

Maytenus ilicifolia is a medicinal species native to Brazil which has been cultivated to meet the growing market demand. Factors that interfere with the production, such as the incidence of pests and diseases, should be studied to ensure increased productivity. The aim of this study was to record the occurrence and the identification of mealybugs associated with 15 "espinheira-santa" (Maytenus ilicifolia) accessions from the Active Germplasm Bank of "Embrapa Clima Temperado" and "Instituto Federal Sul-rio-grandense". The quantity of infested plants in each accession was recorded and the species of infested mealybugs were identified in the laboratory. The number of infested plants varied among accessions. The identified mealybugs were Ceroplastes sp. and Saissetia oleae, family Coccidae. Of 10 infested accessions, 23 plants (11.3%) showed infestation with Ceroplastes sp., and only one (0.5%) with Saissetia oleae. Accession 133 showed the highest incidence of Ceroplastes sp. (33.3%), followed by accession 130 (25.0%). Accession 123 had the least amount of infested plants (4.8%). Saissetia oleae occurred in only one plant, belonging to accession 136 (5.6%).

Antinociceptive effects of an extract, fraction and an isolated compound of the stem bark of Maytenus rigida

The antinociceptive activity of the Maytenus rigida Mart. (Celastraceae) ethanol extract and its ethyl acetate fraction as well as of (-)-4'-methylepigallocatechin (1), a previously isolated compound, was demonstrated in vivo. ED50 for 1 in the writhing test was 14.14 mg/kg. The acetic acid-induced writhing was inhibited by 98.4, 84.4, and 58.3%, respectively, when mice were treated with the ethanol extract, ethyl acetate fraction, and 1. In the hot plate test, mice pretreated with 1 showed significantly increased reaction times (60-89%). Oral administration of 1 significantly inhibited first and second phases of the formalin-induced pain (50 and 26.5%, respectively), whereas indomethacin inhibited only the second phase of the test (41.2%). Ethanol extract and its fraction showed effects on inflammatory pain, while neurogenic and inflammatory pain suppression by 1 is a strong indication of the presence of both central and peripheral effects and suggests its analgesic and anti-inflammatory potential.

Maytenus salicifolia Reissek, Celastraceae: triterpenes isolated from stems and antioxidant property of extracts from aerial parts

Six pentacyclic triterpenes were isolated from hexane extract of stems of Maytenus salicifolia Reissek, Celastraceae: 30-hydroxyfriedelan-3-one (1), 3,16-dioxofriedelane (2), friedeline (3), lupeol (4), betuline (5) and lup-20(29)-en-3,30-diol (6). The structure each one was established on the basis of detailed ¹H and 13C NMR spectral investigation and by comparison with the respective literature values. For compound 1, the complete 2D NMR (HMBC, HMQC and NOESY) spectral data were herein reported for the first time. Compounds 1, 2, 5 and 6 were isolated for the first time from this plant. Antioxidant activity is described for some extracts from species of the Celastraceae family, then, the extracts from aerial parts of M. salicifolia were evaluated in relation to antioxidant potential using the DPPH method. Compared to quecertin, the AcEt extract (EAF) from leaves, AcEt (EAPF) and MeOH (EMPF) from pulp fruit and AcEt (EAT) and MeOH (EMT) from stems showed significant antioxidant property.

Avaliação da atividade antimicrobiana de Maytenus rigida Mart. (Celastraceae) / Evaluation of the antimicrobial activity of Maytenus rigida Mart. (Celastraceae)

A realização de estudos farmacológicos é fundamental para comprovar a eficácia do uso de plantas medicinais pela população para o tratamento de doenças e descobrir novos fitoterápicos. Esse estudo teve como objetivo avaliar o potencial antimicrobiano do extrato etanólico e fase acetato de etila do bom nome (Maytenus rigida Mart.) sobre Staphylococcus aureus ATCC 25923, 3 amostras de Staphylococcus aureus multirresistentes isoladas de pacientes com infecções nosocomiais, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 e Salmonella sp. (228-R-Tet, 118-R-Sut e 01-S) isoladas de ambiente aquático, utilizando o método de difusão em agar. Os testes revelaram que o extrato e fase de M. rigida apresentaram atividade antimicrobiana in vitro frente a todas as cepas de S. aureus testadas, apresentando concentração inibitória mínima (MIC) de 400 mg mL-1. Entretanto, estes produtos não apresentaram atividade frente às linhagens de bactérias Gram-negativas testadas, Escherichia coli, Pseudomonas aeruginosa e Salmonella sp.

Ppharmacological studies are essential to prove the effectiveness of using medicinal plants to treat diseases and discover new phytotherapics. This study aimed to evaluate the antimicrobial potential of ethanol and ethyl acetate extracts of "bom-nome" (Maytenus rigida Mart.) against Staphylococcus aureus ATCC 25923, three samples of multiresistant Staphylococcus aureus isolated from patients with nosocomial infections, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 and Salmonella sp. (228-R-Tet, 118-R-Sut and 01-S) isolated from water environment, using the agar diffusion test. Both extracts showed in vitro antimicrobial activity against all S. aureus strains, presenting 400 mg mL-1 minimum inhibitory concentration (MIC). However, these products did not show activity against strains of the Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa and Salmonella sp.

Evaluation of the genotoxic potential of Austroplenckia populnea (Reiss) Lundell chloroform fraction from barkwood extract in rodent cells in vivo / Avaliação do potencial genotóxico da fração clorofórmica de cascas do caule de Austroplenckia populnea em células de roedores in vivo

The genotoxic effect of the Austroplenckia populnea chloroform fraction from barkwood extract was tested in vivo on peripheral blood cells of Swiss mice with the comet assay (SCGE), and the clastogenic effect was investigated on peripheral blood cells of Swiss mice and bone marrow cells of Wistar rats, with the micronucleus and chromosome aberrations tests. The animals were treated by gavage with 3 concentrations of the extract: 300, 600 and 900 mg.kg-1. Peripheral blood cells of Swiss mice were collected 4 and 24 hours after the treatment to the SCGE assay and 48 and 72 hours to the micronucleus test. Bone marrow cells of Wistar rats were collected 24 hours after the treatment to the micronucleus and chromosome aberration tests. The results showed that the A. populnea chloroform fraction induced an increase in the average number of DNA damage in peripheral blood cells at the three concentrations tested, but this increase was not statistically significant. In the micronucleus and chromosome aberrations test, no significant increase was observed in the mean number of micronucleated polychromatic erythrocytes (MNPCE) of Swiss mice or MNPCE or chromosome aberrations for the rat bone marrow cells, for any of the tested doses. Our findings enable us to conclude that by the comet assay, A. populnea chloroform fraction from barkwood extract showed no genotoxic effects, and by the micronucleus and chromosome aberration tests, the extract fraction showed no clastogenic/aneugenic effects on the rodent cells tested.

O possível efeito genotóxico da fração clorofórmica de cascas de caule de Austroplenckia populnea foi testado in vivo em células do sangue periférico de camundongos Suíços pelo ensaio cometa, e o seu possível efeito clastogênico foi investigado em células de sangue periférico de camundongos Suíços e células da medula óssea de ratos Wistar, respectivamente pelos testes do micronúcleo e de aberrações cromossômicas. Os animais foram tratados por via oral com três concentrações do extrato: 300, 600 e 900 mg.kg-1 de peso corpóreo. Células do sangue periférico dos camundongos foram coletadas 4 e 24 horas após o tratamento para a realização do ensaio cometa, e 48 e 72 horas para o teste do micronúcleo. Células da medula óssea dos ratos Wistar foram coletadas 24 horas após o tratamento para os testes do micronúcleo e de aberrações cromossômicas. Os resultados mostraram que a fração clorofórmica do extrato de A. populnea induziu um pequeno aumento no número médio de danos ao DNA nas células sanguíneas nas três concentrações testadas, mas tal aumento não foi estatisticamente significativo. Nos testes do micronúcleo e de aberrações cromossômicas não houve um aumento significativo no número médio de eritrócitos policromáticos micronucleados (EPM) dos camundongos, bem como nos EPM e aberrações cromossômicas nas células da medula óssea dos ratos, em nenhuma das doses testadas. Nossos resultados nos permitem concluir que, pelo ensaio cometa, a fração clorofórmica de cascas do caule de A. populnea não apresentou efeito genotóxico, e, pelos testes do micronúcleo e de aberrações cromossômicas, o extrato não mostrou efeitos clastogênicos e/ou aneugênicos nas células analisadas dos roedores.

Four Brazilian Maytenus salicifolia Reissek (Celastraceae) groups studied by TLC and UV/Vis spectrophotometry / Estudo de quatro populações de Maytenus salicifolia Reissek (Celastraceae) por CCD e espectrometria na região do UV/Vis

The great variety of angiosperms shows the need to development of botanical classification systems supported by phytochemistry, biochemistry and others. Recently, techniques of analysis used for the isolation and characterization of secondary metabolites have been employed as auxiliary quick and efficient methods for the identification and classification of plant species. M. salicifolia is popularly known in Brazil, as "small coffee" and decoct obtained from its fresh leaves is topically used to alleviate itches and other skins allergic symptoms. This work presents the use of TLC and UV/Vis spectrophotomety processes to be applied like an auxiliary method in botanical taxonomy. The results demonstrate that this process can be used in differentiation of the same genera species, and in the selection of chemical variations between individuals of the same species.

A grande variedade de angiospermas apontou a necessidade do desenvolvimento de sistemas de classificação botânica apoiada pela fitoquímica, bioquímica e outras. Recentemente, técnicas de análise utilizadas para o isolamento e caracterização de metabólitos secundários vêm sendo empregadas como métodos auxiliares rápidos e eficientes para identificação e classificação de espécies vegetais. M. salicifolia é popularmente conhecida no Brasil, como "cafezinho". O chá obtido a partir de folhas frescas é usado topicamente para aliviar pruridos e sintomas alergiformes. Este trabalho apresenta a utilização do CCD em sílica gel e espectrofotometria no UV / Vis como métodos auxiliares na identificação botânica de M. salicifolia. Os resultados demonstraram que este processo pode ser usado na diferenciação de plantas do mesmo gênero, assim como detectar variações químicas entre indivíduos de uma mesma espécie.

Evaluation of antibacterial activity of "Mangabarana" Austroplenckia populnea Reissek (Celastraceae) / Avaliação da atividade antibacteriana de "Mangabarana" Austroplenckia populnea Reissek (Celastraceae)

Austroplenckia populnea (Mangabarana) is popularly used by people from Minas Gerais, Brazil for dysenteries diseases treatment. Antitumor and antiulcer activities were also attributed to this plant. Extracts obtained using solvents of different polarities and pentacyclic triterpenes (PCTTs) isolated from these extracts through phytochemical methods were submitted to antibacterial assays. The results showed the existence of this activity and open perspectives for news studies with other organic compounds isolated from this plant.

Austroplenckia populnea (Mangabarana) é popularmente utilizada em Minas Gerais, Brasil, para o tratamento de disenterias. A ela também são atribuídas propriedades antitumoral e antiúlcera. Extratos de partes desta planta obtidos com solventes de diferentes polaridades e triterpenos pentacíclicos (TTPCs) isolados destes, por métodos fitoquímicos foram submetidos a testes de atividade antibacteriana. Os resultados mostraram a existência desta atividade e abriram perspectivas para a continuidade dos estudos com outros compostos orgânicos isolados desta planta.

Atividade antioxidante das folhas de espinheira-santa - Maytenus ilicifolia Mart. ex Reiss., secas em diferentes temperaturas / Antioxidant activity of "espinheira-santa" - Maytenus ilicifolia Mart. ex Reiss., leaves dried in different temperatures

Maytenus ilicifolia Mart. ex Reiss, a espinheira-santa verdadeira, é largamente utilizada para tratamento de gastrites e úlceras estomacais. O seu valor terapêutico é atribuído principalmente aos polifenóis (flavonóides e taninos) e triterpenos. Os polifenóis são bastante estudados e estão relacionados à atividade antioxidante exercida pela planta. Existem vários métodos para avaliar a atividade antioxidante, a qual pode ser medida a capacidade antioxidante total utilizando o método de formação do complexo fosfomolibdênio e a atividade antioxidante em relação à redução de um radical, utilizando-se o DPPH (2,2-difenil-1-picrilhidrazila). A atividade antioxidante das folhas de espinheira-santa seca em diferentes temperaturas foi avaliada, visando verificar a possível influência das temperaturas de secagens e seu poder antioxidante. Foram utilizadas cinco temperaturas (40, 50, 60, 70 e 80 ºC) e uma temperatura de secagem de rotina, de um produtor/beneficiador de plantas medicinais. As menores temperaturas apresentaram as maiores atividades antioxidantes.

Maytenus ilicifolia Mart. ex Reiss, the true "espinheira-santa" is widely used for treating gastritis and stomach ulcers. Its therapeutic values are due mainly polyphenols (flavonoids and tannins) and triterpens. Polyphenols are largely studied and they are related to the antioxidant activity of the plants. There are several methods for evaluating the antioxidant activity, which can measured the total antioxidant capacity through the formation of a phosphomolybdenum complex and the antioxidant activity related to the reduction of one radical, using the DPPH (2,2-diphenyl-1-picrylhydrazyl). The antioxidant activity of "espinheira-santa" dried leaves in different temperatures was measured in order to evaluated the possible influence of drying temperatures under its antioxidant power. Five temperatures used were (40, 50, 60, 70 and 80 ºC) and a drying routine of medicinal plants as well. Lower temperatures showed the highest antioxidant activities.

Revisão da Maytenus ilicifolia Mart. ex Reissek, Celastraceae. Contribuição ao estudo das propriedades farmacológicas / Review of Maytenus ilicifolia Mart. ex Reissek, Celastraceae. Contribution to the studies of pharmacological properties

A Maytenus ilicifolia Mart. ex Reissek, Celastraceae, vem sendo utilizada à muitos anos na terapêutica clínica, contudo suas propriedades farmacológicas continuam sob estudo. O objetivo desse trabalho é fornecer subsídios teóricos para o aprimoramento dos estudos, em especial os estudos clínicos, e assim estabelecer definitivamente as propriedades reais da Maytenus ilicifolia.

The Maytenus ilicifolia Mart. ex Reissek, Celastraceae has been used for many years as a medicine in the therapeutic in Brazil. However, the pharmacological action still under evaluation by many research centres. The aim of this study is stablish, based in clinical trials, the real properties of Maytenus ilicifolia.

Antioxidant activity of Maytenus imbricata Mart., Celastraceae / Atividade antioxidante de Maytenus imbricata Mart., Celastraceae

The free radical scavenging activity (FRS) using 2,2-diphenyl-1-picrylhydrazyl (DPPH), the reducer power and the total phenolic concentration of extracts and compounds isolated from leaves, branches and roots of Maytenus imbricata Mart. (Celastraceae) were evaluated. Some extracts, a mixture of phenolic compounds (MPC) and epicatechin showed higher RP and FRS (DPPH) activities in comparison with the standard butylhydroxyanisole (BHA) and galic acid (GA) used in assays. The ethyl acetate extract from leaves showed higher total phenolic content and also higher RP and FRS (DPPH) than the other extracts. These facts indicate that there are some relations between phenolic concentration in the extract and the antioxidant activity and the reducer power. The solvent used in the extraction process influences the chemical composition of the extracts and consequently its antioxidant and reducer power activities.

A atividade antioxidante, poder redutor (RP) e a atividade coletora de radicais livres (FRS) usando 2,2-difenil-1-picrilhidrazil (DPPH), e a concentração de substâncias fenólicas totais dos extratos e substâncias isoladas das folhas, caules e raízes de Maytenus imbricata Mart. (Celastraceae) foram avaliados. Alguns extratos, a mistura de compostos fenólicos e epicatequina mostraram alto poder redutor e atividade antioxidante (DPPH) em comparação com o padrão butilhidroxianisol (BHA) e ácido gálhico (GA) utilizados no ensaio. O extrato acetato de etila das folhas mosraram alto teor de substâncias fenólicas e alto poder redutor e atividade antioxidante em relação aos outros extratos. Este fato indica haver alguma relação entre a concentração de substâncias fenólicas e o poder redutor. O solvente usado no processo de extração influencia a composição química dos extratos e, consequentemente, as atividades redutoras e antioxidantes.

Evaluation of the toxicity and antiulcerogenic activity of the ethanol extract of Maytenus obtusifolia Mart. leaves / Avaliação da toxicidade e atividade antiulcerogênica do extrato etanólico das folhas de Maytenus obtusifolia Mart

Maytenus obtusifolia é utilizada na medicina popular para o tratamento de úlceras graves, inflamações gerais e câncer. Apesar da importância etnofarmacológica desta espécie, nenhum estudo foi realizado para avaliar a sua toxicidade e atividade antiulcerogênica. Neste estudo, nós avaliamos a toxicidade e propriedade antiulcera do extrato etanólico das folhas de Maytenus obtusifolia (MO-EtOH). O MO-EtOH (10-1000 µg/mL) mostrou baixa toxicidade para as larvas de A. salina com CL50 maior que 1000 µg/mL. O MO-EtOH (2000 mg/kg, p.o.) nγo alterou o peso corporal e peso dos órgãos dos camundongos, mas foi observado um aumento no consumo de água dos machos e uma diminuição do consumo alimentar das fêmeas. Durante o estudo não foram observadas mortes e nem alterações macroscópicas nos órgãos dos camundongos. MO-EtOH (62,5, 125, 250 e 500 mg/kg) e lansoprazol (30 mg/kg) reduziram significativamente o índice ulcerativo para 65,58 ± 8,74, 43,00 ± 9,53, 15,50 ± 7,56, 54,75 ± 8,88 e 36,13 ± 9,55, respectivamente, em comparação com salina 82,13 ± 12,48. Em conclusão, o MO-EtOH apresentou baixa toxicidade e atividade antiulcerogênica, o que confirma o uso popular de M. obtusifolia.

Maytenus obtusifolia is used in folk medicine for the treatment of serious ulcers, general inflammations and cancer. Despite of the ethnopharmacological importance of this species, no study was conducted to evaluate its toxicity and antiulcerogenic activity. In this study, we evaluated the toxicity and antiulcerogenic property of the ethanol extract of the leaves of Maytenus obtusifolia (MO-EtOH). The MO-EtOH (10-1000 µg/mL) showed low toxicity for larvae of A. salina with LC50 higher than 1000 µg/mL. The MO-EtOH (2000 mg/kg, p.o.) did not change the body and organs weight of the mice, but it was observed an increase in the water consumption of males and a decrease in the food consumption of females. During the study no deaths and no macroscopic changes in the organs were observed in the mice. MO-EtOH (62.5, 125, 250 and 500 mg/kg) and lansoprazole (30 mg/kg) significantly reduced the ulcerative index for 65.58 ± 8.74, 43.00 ± 9.53, 15.50 ± 7.56, 54.75 ± 8.88 and 36.13 ± 9.55, respectively, in comparison with saline 82.13 ± 12.48. In conclusion, the MO-EtOH showed low toxicity and antiulcerogenic activity, confirming the popular use of M. obtusifolia.

Variabilidade em matrizes de acessos de espinheira-santa / Variability in matrices of espinheira-santa accessions

Maytenus ilicifolia e M. aquifolium são espécies nativas do Brasil, popularmente conhecidas como espinheira-santa, sendo indicadas para gastrite e para úlcera estomacal. A Embrapa Clima Temperado e a Universidade Federal de Pelotas (UFPel) mantêm um banco de germoplasma destas espécies. Com o objetivo de identificar a variabilidade fenotípica para alguns caracteres morfológicos em matrizes de espinheira-santa, estimar a dissimilaridade e agrupar os acessos através de análises multivariadas, 105 acessos foram caracterizados morfologicamente. Foram avaliados os caracteres comprimento e largura de fruto, número de sementes por fruto, comprimento e largura de folha, relação comprimento/largura de folha e número de espinhos por folha. Foi estimada a distância euclidiana e os acessos foram agrupados pelo método de otimização de Tocher. Foi observada uma ampla variabilidade para todos os caracteres analisados. O número de espinhos por folha foi o caráter que mais contribuiu para a divergência. Os caracteres morfológicos permitiram separar os acessos em sete grupos. A maior dissimilaridade foi entre os acessos 57 (M. ilicifolia) e 91 (M. aquifolium). Não foi evidenciada uma separação de acordo com a localização geográfica dos acessos. Na análise de agrupamento foram identificados dois grupos que apresentavam tanto acessos de M. ilicifolia quanto de M. aquifolium, o que indica proximidade filogenética entre estas espécies.

Maytenus ilicifolia and M. aquifolium are native Brazilian species popularly known as espinheira-santa, being indicated for gastritis and stomach ulcer. Embrapa Clima Temperado and Universidade Federal de Pelotas (UFPel) keep a gene bank of these species. With the objective of identifing phenotypic variability for some morphological characters in matrices of espinheira-santa, estimating dissimilarity and clustering accessions through multivariate analysis, 105 accessions had been morphologically characterized. The characteristics evaluated were fruit length, fruit width, number of seeds per fruit, leaf length, leaf width, leaf length/leaf width ratio and number of thorns per leaf. The euclidean distance was estimated and accessions were clustered by Tocher optimization method. A wide variability for all the characteristics analyzed was observed. The number of thorns per leaf was the characteristics that more contributed to the divergence. The morphological characteristics enabled to separate the accesses in seven clusters. The higher dissimilarity was between accessions 57 (M. ilicifolia) and 91 (M. aquifolium). There was no evidence of a separation in accordance to the geographic localization of the accessions. In the clustering analysis were identified two clusters that had accessions of both species, M. ilicifolia and M. aquifolium, indicating phylogenetic relatedness between these species.

Pharmacological studies of ethanolic extracts of Maytenus rigida Mart (Celastraceae) in animal models

The crude ethanol extract (EEOH) of the bark of Maytenus rigida Mart (Celastraceae) a plant used in Brazil herbal traditional medicine, was tested for anti-inflammatory, antiulcer and antidiarrhoeal activities in animal models. No acute toxicological sign was observed in animals treated with the highest dose (5000 mg/kg, p.o. or 2000 mg/kg i.p.) of EEOH. The extract doses of 250, 500 or 750 mg/kg revealed a significant inhibitory effect (P < 0,01) in carrageenin-induced rat paw oedema and exhibited ulcer-protective properties against ethanol-induced ulceration in rats. An anti-diarrhoeal activity (P < 0.01) was also observed in castor-oil-induced diarrhoeal in mice. The intestinal transit was significantly (P < 0.01) reduced, however the pretreatment did not reduce the weight of intestinal contents. These results support the popular applications of Maytenus rigida for the treatment of inflammation, ulcer and diarrhoea in Brazil herbal traditional medicine.

O extrato etanólico bruto (EEOH) da casca de Maytenus rigida Mart (Celastraceae) uma planta da medicina popular do Brasil, foi testado para a atividade antiinflamatória, antiúlcera e antidiarréica em modelos animais. Não foi observado sinal de toxicidade aguda nos animais tratados com doses elevadas do EEOH (5000 mg/kg, v.o. ou 2000 mg/kg i.p.). O extrato nas doses de 250, 500 e 750 mg/kg mostrou um significante efeito inibitório (P < 0,01) no edema de pata induzido por carragenina e exibiu propriedade protetora contra a ulceração induzida por etanol em ratos. Também uma atividade antidiarréica (P < 0,01) foi observada na diarréia induzida por óleo de rícino em camundongos. O trânsito intestinal foi reduzido significativamente (P < 0.01), porém o pré-tratamento não reduziu o peso do conteúdo intestinal em ratos. Os resultados dão suporte à utilização de Maytenus rigida na medicina popular do Brasil para o tratamento da inflamação, da úlcera e da diarréia.

Celastraceae endémicas del Perú

La familia Celastraceae es reconocida en el Perú por presentar ocho géneros y 29 especies (Brako & Zarucchi, 1993; Ulloa Ulloa et al., 2004), la mayoría lianas. En este trabajo reconocemos cuatro endemismos en dos géneros. Estos taxones endémicos ocupan principalmente las regiones Matorral Desértico y Mesoandina, entre los 600 y 3300 m de altitud. Se aplicaron las categorías y criterios de la UICN a dos especies. Una especie se encuentra representada en el Sistema Nacional de Áreas Naturales Protegidas por el Estado.

The Celastraceae are represented in Peru by eight genera and 29 species (Brako & Zarucchi, 1993; Ulloa Ulloa et al., 2004), mainly lianas. Here we recognize four endemic taxa in two genera. Endemic Celastraceae grow in Desert Shrubland and Mesoandean regions, between 600 and 3300 m elevation. We applied IUCN categories and criteria to two species. One endemic Celastraceae is represented within Peru's protected areas system.