Chemical composition and biological activities of essential oil from flowers of Psidium guajava (Myrtaceae) / Composição química e atividades biológicas do óleo essencial das flores de Psidium guajava (Myrtaceae)

Abstract Xylella fastidiosa is a plant-pathogenic bacterium that lives inside host xylem vessels, where it forms biofilm which is believed to be responsible for disrupting the passage of water and nutrients. Pectobacterium carotovorum is a Gram-negative plant-specific bacterium that causes not only soft rot in various plant hosts, but also blackleg in potato by plant cell wall degradation. Chagas disease, which is caused by Trypanosoma cruzi, has been commonly treated with nifurtimox and benzonidazole, two drugs that cause several side effects. As a result, the use of natural products for treating bacterial and neglected diseases has increased in recent years and plants have become a promising alternative to developing new medicines. Therefore, this study aimed to determine, for the first time, the chemical composition of essential oil from Psidium guajava flowers (PG-EO) and to evaluate its in vitro anti-Xylella fastidiosa, anti-Pectobacterium carotovorum, anti-Trypanosoma cruzi and cytotoxic activities. PG-EO was obtained by hydrodistillation in a Clevenger apparatus while its chemical composition was determined by gas chromatography-flame ionization detection (GC-FID) and gas chromatography-mass spectrometry (GC-MS). Major compounds identified in PG-EO were α-cadinol (37.8%), β-caryophyllene (12.2%), nerolidol (9.1%), α-selinene (8.8%), β-selinene (7.4%) and caryophyllene oxide (7.2%). Results showed that the PG-EO had strong trypanocidal activity against the trypomastigote forms of Trypanosoma cruzi (IC50 = 14.6 μg/mL), promising antibacterial activity against X. fastidiosa (MIC = 12.5 μg/mL) and P. carotovorum (MIC = 62.5 μg/mL), and moderate cytotoxicity against LLCMK2 adherent epithelial cells in the concentration range (CC50 = 250.5 μg/mL). In short, the PG-EO can be considered a new source of bioactive compounds for the development of pesticides and trypanocide drugs.

Resumo Xylella fastidiosa é uma bactéria patogênica que vive dentro dos vasos do xilema hospedeiro, onde forma um biofilme responsável por interromper a passagem de água e nutrientes. Pectobacterium carotovorum é uma bactéria Gram-negativa que causa não só podridão macia em várias plantas hospedeiras, mas também canela-preta na batata por degradação da parede celular da planta. A doença de Chagas, causada pelo Trypanosoma cruzi, é comumente tratada com nifurtimox e benzonidazol, duas drogas que causam vários efeitos colaterais. Como resultado, o uso de produtos naturais para o tratamento de doenças bacterianas e negligenciadas aumentou nos últimos anos e as plantas continuam sendo uma alternativa promissora para o desenvolvimento de novos medicamentos. Portanto, este estudo teve como objetivo determinar, pela primeira vez, a composição química do óleo essencial de flores de Psidium guajava (PG-EO) e avaliar suas propriedades anti-Xylella fastidiosa, anti-Pectobacterium carotovorum, anti-Trypanosoma cruzi e citotóxica in vitro. PG-EO foi obtido por hidrodestilação em um aparelho Clevenger, enquanto sua composição química foi determinada por cromatografia em fase gasosa com detecção por ionização por chama (CG-DIC) e por cromatografia em fase gasosa acoplada à espectrometria de massa (CG-EM). Os principais compostos identificados no PG-EO foram α-cadinol (37,8%), β-cariofileno (12,2%), nerolidol (9,1%), α-selineno (8,8%), β-selineno (7,4%) e óxido de cariofileno (7,2%). Os resultados mostraram que o PG-EO apresentou forte atividade tripanocida contra as formas tripomastigotas de T. cruzi (CI50 = 14,6 μg/mL), promissora atividade antibacteriana contra X. fastidiosa (MIC = 12,5 μg/mL) e P. carotovorum (MIC = 62,5 μg/mL) e citotoxicidade moderada contra células epiteliais aderentes (LLCMK2) na faixa de concentração (CC50 = 250,5 μg/mL). Em suma, o PG-EO pode ser considerado uma nova fonte de compostos bioativos para o desenvolvimento de pesticidas e drogas tripanocidas.

Chemical composition and biological activities of essential oil from flowers of Psidium guajava (Myrtaceae).

Xylella fastidiosa is a plant-pathogenic bacterium that lives inside host xylem vessels, where it forms biofilm which is believed to be responsible for disrupting the passage of water and nutrients. Pectobacterium carotovorum is a Gram-negative plant-specific bacterium that causes not only soft rot in various plant hosts, but also blackleg in potato by plant cell wall degradation. Chagas disease, which is caused by Trypanosoma cruzi, has been commonly treated with nifurtimox and benzonidazole, two drugs that cause several side effects. As a result, the use of natural products for treating bacterial and neglected diseases has increased in recent years and plants have become a promising alternative to developing new medicines. Therefore, this study aimed to determine, for the first time, the chemical composition of essential oil from Psidium guajava flowers (PG-EO) and to evaluate its in vitro anti-Xylella fastidiosa, anti-Pectobacterium carotovorum, anti-Trypanosoma cruzi and cytotoxic activities. PG-EO was obtained by hydrodistillation in a Clevenger apparatus while its chemical composition was determined by gas chromatography-flame ionization detection (GC-FID) and gas chromatography-mass spectrometry (GC-MS). Major compounds identified in PG-EO were α-cadinol (37.8%), ß-caryophyllene (12.2%), nerolidol (9.1%), α-selinene (8.8%), ß-selinene (7.4%) and caryophyllene oxide (7.2%). Results showed that the PG-EO had strong trypanocidal activity against the trypomastigote forms of Trypanosoma cruzi (IC50 = 14.6 µg/mL), promising antibacterial activity against X. fastidiosa (MIC = 12.5 µg/mL) and P. carotovorum (MIC = 62.5 µg/mL), and moderate cytotoxicity against LLCMK2 adherent epithelial cells in the concentration range (CC50 = 250.5 µg/mL). In short, the PG-EO can be considered a new source of bioactive compounds for the development of pesticides and trypanocide drugs.

Antibacterial and antiproliferative activities of the fresh leaf essential oil of Psidium guajava L. (Myrtaceae) / Atividades antibacteriana e antiproliferativa do óleo essencial das folhas frescas de Psidium guajava L. (Myrtaceae)

Abstract This study evaluated the antibacterial and antiproliferative activities of the essential oil of Psidium guajava leaves (PG-EO), traditionally used in folk medicine. The essential oil was obtained from fresh leaves by hydrodistillation, using a modified Clevenger apparatus. The major PG-EO chemical constituents were identified by GC-MS and GC-FID as being β-caryophyllene (16.1%), α-humulene (11.9%), aromadendrene oxide (14.7%), δ-selinene (13.6%), and selin-11-en-4α-ol (12.5%). The antibacterial activity of the essential oil of P. guajava leaves was determined in terms of its minimum inhibitory concentrations (MIC) using the broth microdilution method in 96-well microplates. PG-EO had moderate activity against Streptococcus mutans (MIC = 200 µg/mL), S. mitis (MIC = 200 µg/mL), S. sanguinis (MIC = 400 µg/mL), S. sobrinus (MIC = 100 µg/mL), and S. salivarius (MIC = 200 µg/mL). The antiproliferative activity was evaluated against different tumor cell lines: breast adenocarcinoma (MCF-7), human cervical adenocarcinoma (HeLa), and human gliobastoma (M059J). A normal human cell line (GM07492A, lung fibroblasts) was included. The antiproliferative activity was evaluated using the XTT assay and the results were expressed as IC50. The essential oil showed significantly lower IC50 values against MCF-7 and M059J lines than that obtained for the normal line, showing selectivity. Our results suggest that the essential oil of Psidium guajava L. has promising biological activities and can be considered a new source of bioactive compounds.

Resumo Este estudo avaliou as atividades antibacteriana e antiproliferativa do óleo essencial das folhas frescas de Psidium guajava (PG-OE), tradicionalmente utilizadas na medicina popular. O óleo essencial foi obtido por hidrodestilação das folhas frescas, utilizando aparelho do tipo Clevenger. Os principais constituintes químicos de PG-OE identificados por CG-EM e CG-DIC foram: β-cariofileno (16,1%), α-humuleno (11,9%), óxido de aromadendreno (14,7%), δ-selineno (13,6%) e selin-11-en-4α-ol (12,5%). A atividade antibacteriana do óleo essencial das folhas de P. guajava foi determinada em termo de sua concentração inibitória mínima (CIM) utilizando o método de microdiluição de caldo em microplacas de 96 poços. PG-OE apresentou moderada atividade contra Streptococcus mutans (CIM = 200 μg/mL), S. mitis (CIM = 200 μg/mL), S. sanguinis (CIM = 400 μg/mL), S. sobrinus (CIM = 100 μg/mL) e S. salivarius (CIM = 200 μg/mL). A atividade antiproliferativa foi avaliada frente a diferentes linhagens de células tumorais como: adenocarcinoma de mama (MCF-7), adenocarcinoma cervical humano (HeLa) e gliobastoma humano (M059J). Foi incluída uma linhagem celular humana normal (GM07492A, fibroblastos pulmonares). A atividade antiproliferativa foi avaliada utilizando o ensaio XTT e os resultados foram expressos como CI50. As linhagens MCF-7 e M059J mostraram valores significativamente mais baixos de CI50 do que os obtidos para a linhagem normal, mostrando seletividade. Nossos resultados sugerem que o óleo essencial das folhas frescas de Psidium guajava L. possui atividades biológicas promissoras e pode ser considerado como uma nova fonte de compostos bioativos.

Antibacterial and antiproliferative activities of the fresh leaf essential oil of Psidium guajava L. (Myrtaceae).

This study evaluated the antibacterial and antiproliferative activities of the essential oil of Psidium guajava leaves (PG-EO), traditionally used in folk medicine. The essential oil was obtained from fresh leaves by hydrodistillation, using a modified Clevenger apparatus. The major PG-EO chemical constituents were identified by GC-MS and GC-FID as being ß-caryophyllene (16.1%), α-humulene (11.9%), aromadendrene oxide (14.7%), δ-selinene (13.6%), and selin-11-en-4α-ol (12.5%). The antibacterial activity of the essential oil of P. guajava leaves was determined in terms of its minimum inhibitory concentrations (MIC) using the broth microdilution method in 96-well microplates. PG-EO had moderate activity against Streptococcus mutans (MIC = 200 µg/mL), S. mitis (MIC = 200 µg/mL), S. sanguinis (MIC = 400 µg/mL), S. sobrinus (MIC = 100 µg/mL), and S. salivarius (MIC = 200 µg/mL). The antiproliferative activity was evaluated against different tumor cell lines: breast adenocarcinoma (MCF-7), human cervical adenocarcinoma (HeLa), and human gliobastoma (M059J). A normal human cell line (GM07492A, lung fibroblasts) was included. The antiproliferative activity was evaluated using the XTT assay and the results were expressed as IC50. The essential oil showed significantly lower IC50 values against MCF-7 and M059J lines than that obtained for the normal line, showing selectivity. Our results suggest that the essential oil of Psidium guajava L. has promising biological activities and can be considered a new source of bioactive compounds.

Antibacterial and antiproliferative activities of the fresh leaf essential oil of Psidium guajava L. (Myrtaceae)

Abstract This study evaluated the antibacterial and antiproliferative activities of the essential oil of Psidium guajava leaves (PG-EO), traditionally used in folk medicine. The essential oil was obtained from fresh leaves by hydrodistillation, using a modified Clevenger apparatus. The major PG-EO chemical constituents were identified by GC-MS and GC-FID as being -caryophyllene (16.1%), -humulene (11.9%), aromadendrene oxide (14.7%), -selinene (13.6%), and selin-11-en-4-ol (12.5%). The antibacterial activity of the essential oil of P. guajava leaves was determined in terms of its minimum inhibitory concentrations (MIC) using the broth microdilution method in 96-well microplates. PG-EO had moderate activity against Streptococcus mutans (MIC = 200 µg/mL), S. mitis (MIC = 200 µg/mL), S. sanguinis (MIC = 400 µg/mL), S. sobrinus (MIC = 100 µg/mL), and S. salivarius (MIC = 200 µg/mL). The antiproliferative activity was evaluated against different tumor cell lines: breast adenocarcinoma (MCF-7), human cervical adenocarcinoma (HeLa), and human gliobastoma (M059J). A normal human cell line (GM07492A, lung fibroblasts) was included. The antiproliferative activity was evaluated using the XTT assay and the results were expressed as IC50. The essential oil showed significantly lower IC50 values against MCF-7 and M059J lines than that obtained for the normal line, showing selectivity. Our results suggest that the essential oil of Psidium guajava L. has promising biological activities and can be considered a new source of bioactive compounds.

Resumo Este estudo avaliou as atividades antibacteriana e antiproliferativa do óleo essencial das folhas frescas de Psidium guajava (PG-OE), tradicionalmente utilizadas na medicina popular. O óleo essencial foi obtido por hidrodestilação das folhas frescas, utilizando aparelho do tipo Clevenger. Os principais constituintes químicos de PG-OE identificados por CG-EM e CG-DIC foram: -cariofileno (16,1%), -humuleno (11,9%), óxido de aromadendreno (14,7%), -selineno (13,6%) e selin-11-en-4-ol (12,5%). A atividade antibacteriana do óleo essencial das folhas de P. guajava foi determinada em termo de sua concentração inibitória mínima (CIM) utilizando o método de microdiluição de caldo em microplacas de 96 poços. PG-OE apresentou moderada atividade contra Streptococcus mutans (CIM = 200 g/mL), S. mitis (CIM = 200 g/mL), S. sanguinis (CIM = 400 g/mL), S. sobrinus (CIM = 100 g/mL) e S. salivarius (CIM = 200 g/mL). A atividade antiproliferativa foi avaliada frente a diferentes linhagens de células tumorais como: adenocarcinoma de mama (MCF-7), adenocarcinoma cervical humano (HeLa) e gliobastoma humano (M059J). Foi incluída uma linhagem celular humana normal (GM07492A, fibroblastos pulmonares). A atividade antiproliferativa foi avaliada utilizando o ensaio XTT e os resultados foram expressos como CI50. As linhagens MCF-7 e M059J mostraram valores significativamente mais baixos de CI50 do que os obtidos para a linhagem normal, mostrando seletividade. Nossos resultados sugerem que o óleo essencial das folhas frescas de Psidium guajava L. possui atividades biológicas promissoras e pode ser considerado como uma nova fonte de compostos bioativos.

Chemical composition and biological activities of essential oil from flowers of Psidium guajava (Myrtaceae)

Abstract Xylella fastidiosa is a plant-pathogenic bacterium that lives inside host xylem vessels, where it forms biofilm which is believed to be responsible for disrupting the passage of water and nutrients. Pectobacterium carotovorum is a Gram-negative plant-specific bacterium that causes not only soft rot in various plant hosts, but also blackleg in potato by plant cell wall degradation. Chagas disease, which is caused by Trypanosoma cruzi, has been commonly treated with nifurtimox and benzonidazole, two drugs that cause several side effects. As a result, the use of natural products for treating bacterial and neglected diseases has increased in recent years and plants have become a promising alternative to developing new medicines. Therefore, this study aimed to determine, for the first time, the chemical composition of essential oil from Psidium guajava flowers (PG-EO) and to evaluate its in vitro anti-Xylella fastidiosa, anti-Pectobacterium carotovorum, anti-Trypanosoma cruzi and cytotoxic activities. PG-EO was obtained by hydrodistillation in a Clevenger apparatus while its chemical composition was determined by gas chromatography-flame ionization detection (GC-FID) and gas chromatography-mass spectrometry (GC-MS). Major compounds identified in PG-EO were -cadinol (37.8%), -caryophyllene (12.2%), nerolidol (9.1%), -selinene (8.8%), -selinene (7.4%) and caryophyllene oxide (7.2%). Results showed that the PG-EO had strong trypanocidal activity against the trypomastigote forms of Trypanosoma cruzi (IC50 = 14.6 g/mL), promising antibacterial activity against X. fastidiosa (MIC = 12.5 g/mL) and P. carotovorum (MIC = 62.5 g/mL), and moderate cytotoxicity against LLCMK2 adherent epithelial cells in the concentration range (CC50 = 250.5 g/mL). In short, the PG-EO can be considered a new source of bioactive compounds for the development of pesticides and trypanocide drugs.

Resumo Xylella fastidiosa é uma bactéria patogênica que vive dentro dos vasos do xilema hospedeiro, onde forma um biofilme responsável por interromper a passagem de água e nutrientes. Pectobacterium carotovorum é uma bactéria Gram-negativa que causa não só podridão macia em várias plantas hospedeiras, mas também canela-preta na batata por degradação da parede celular da planta. A doença de Chagas, causada pelo Trypanosoma cruzi, é comumente tratada com nifurtimox e benzonidazol, duas drogas que causam vários efeitos colaterais. Como resultado, o uso de produtos naturais para o tratamento de doenças bacterianas e negligenciadas aumentou nos últimos anos e as plantas continuam sendo uma alternativa promissora para o desenvolvimento de novos medicamentos. Portanto, este estudo teve como objetivo determinar, pela primeira vez, a composição química do óleo essencial de flores de Psidium guajava (PG-EO) e avaliar suas propriedades anti-Xylella fastidiosa, anti-Pectobacterium carotovorum, anti-Trypanosoma cruzi e citotóxica in vitro. PG-EO foi obtido por hidrodestilação em um aparelho Clevenger, enquanto sua composição química foi determinada por cromatografia em fase gasosa com detecção por ionização por chama (CG-DIC) e por cromatografia em fase gasosa acoplada à espectrometria de massa (CG-EM). Os principais compostos identificados no PG-EO foram -cadinol (37,8%), -cariofileno (12,2%), nerolidol (9,1%), -selineno (8,8%), -selineno (7,4%) e óxido de cariofileno (7,2%). Os resultados mostraram que o PG-EO apresentou forte atividade tripanocida contra as formas tripomastigotas de T. cruzi (CI50 = 14,6 g/mL), promissora atividade antibacteriana contra X. fastidiosa (MIC = 12,5 g/mL) e P. carotovorum (MIC = 62,5 g/mL) e citotoxicidade moderada contra células epiteliais aderentes (LLCMK2) na faixa de concentração (CC50 = 250,5 g/mL). Em suma, o PG-EO pode ser considerado uma nova fonte de compostos bioativos para o desenvolvimento de pesticidas e drogas tripanocidas.

Antibacterial activity of commercially available plant-derived essential oils against oral pathogenic bacteria.

This work investigated the antibacterial activity of 15 commercially available plant-derived essential oils (EOs) against a panel of oral pathogens. The broth microdilution method afforded the minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) of the assayed EOs. The EO obtained from Cinnamomum zeylanicum (Lauraceae) (CZ-EO) displayed moderate activity against Fusobacterium nucleatum (MIC and MBC = 125 µg/mL), Actinomyces naeslundii (MIC and MBC = 125 µg/mL), Prevotella nigrescens (MIC and MBC = 125 µg/mL) and Streptococcus mutans (MIC = 200 µg/mL; MBC = 400 µg/mL). (Z)-isosafrole (85.3%) was the main chemical component of this oil. We did not detect cinnamaldehyde, previously described as the major constituent of CZ-EO, in specimens collected in other countries.

Avaliação das atividades antibacteriana, tripanocida e citotóxica do extrato hidroalcóolico das raízes de Tradescantia sillamontana Matuda (Veludo Branco) (Commelinaceae) / Evaluation of antibacterial, trypanocidal and cytotoxical activities of the hydroalcoholic extract from the roots of Tradescantia sillamontana Matuda (Veludo Branco) (Commelinaceae)

RESUMO O objetivo deste estudo foi avaliar o efeito antibacteriano e tripanocida in vitro do extrato hidroalcóolico das raízes de Tradescantia sillamontana Matuda (Commelinaceae), conhecida popularmente como veludo branco. Foi avaliada a atividade antibacteriana in vitro frente às bactérias Streptococcus mitis (CIM = 100 µg/mL; CMB = 150 µg/mL), Streptococcus mutans (CIM = 200 µg/mL; CMB = 220 µg/mL), Streptococcus sanguinis (CIM = 400 µg/mL; CMB = 425 µg/mL), Streptococcus sobrinus (CIM = 400 µg/mL; CMB = 420 µg/mL) e Bacteroides fragilis (CIM = 400 µg/mL; CMB = 430 µg/mL) pelo método de diluição em caldo. Os protozoários da família tripanossomatídeo causam doenças tropicais que costumam ser negligenciadas que costumam ser como a tripanossomíase, para a qual estão disponíveis poucos medicamentos. Neste contexto, o extrato hidroalcóolico das raízes de T. sillamontana também foi avaliado frente às formas tripomastigotas da cepa Y de Trypanosoma cruzi, com promissora atividade frente a este protozoário (IC50 = 2,4 µg/mL). Quando avaliada a atividade citotóxica frente a fibroblastos da linhagem LLCMK2, o extrato apresentou moderada citotoxicidade (CC50 = 480,37 µg/mL). Os resultados ora apresentados para o extrato hidroalcóolico das raízes de Tradescantia sillamontana Matuda demonstraram promissoras atividades antibacteriana e tripanocida, sendo uma fonte alternativa de produtos naturais com atividades contra T. cruzi e algumas bactérias do gênero Streptococcus e Bacteroides.

ABSTRACT The aim of this study was to investigate the in vitro, antibacterial and trypanocidal effect of the hydroalcoholic extract from the roots of Tradescantia sillamontana Matuda (Commelinaceae), commonly known as Veludo branco. The in vitro antibacterial activity against the standard bacteria Streptococcus mitis (MIC = 100µg/mL; MBC = 150 µg/mL), Streptococcus mutans (MIC = 200µg/mL; MBC = 220 µg/mL), Streptococcus sanguinis (MIC = 400µg/mL; MBC = 425 µg/mL), Streptococcus sobrinus (MIC = 400µg/mL; MBC = 420 µg/mL) andBacteroides fragilis (MIC = 400µg/mL; MBC = 430 µg/mL), using microdilution broth methods. Protozoans from the trypanosomatid family cause neglected tropical diseases such as trypanosomiasis, for which few drugs are available. In this context, the hydroalcoholic extract of the Tradescantia sillamontana roots was also investigated with regards to the in vitro effects against the trypomastigote forms of theY strain of Trypanosoma cruzi, showing strong activity against this parasite (IC50 = 2.4 µg/mL). When performing cytotoxic activity against fibroblasts LLCMK2 line, the extract showed moderate cytotoxicity (CC50 = 480.37 mg/mL). The results presented for the hydroalcoholic extract of the roots of Tradescantia sillamontana Matuda demonstrated effective antibacterial and trypanocidal activities and were shown to be an alternative source of natural products with activity against T. cruzi and some bacteria of the genus Streptococcus and Bacteroides.

Rendimento, composição química e atividades antimicrobiana e antioxidante do óleo essencial de folhas de Campomanesia adamantium submetidas a diferentes métodos de secagem / Content, chemical composition and antimicrobial and antioxidant activities of the essential oil from leaves of Campomanesia adamantium submitted to different drying methods

RESUMO Campomanesia adamantium é muito utilizada na medicina popular no tratamento de hipertensão, reumatismo e diabetes. Objetivou-se com o presente trabalho avaliar o rendimento, a composição química, e as atividades antimicrobiana e antioxidante do óleo essencial de folhas de C. adamantium submetidas a diferentes métodos e tempos de secagem. O delineamento utilizado foi inteiramente casualizado, com oito tratamentos e três repetições. O óleo essencial foi extraído por hidrodestilação das folhas e analisado por CG-EM. O tipo de secagem das folhas de C. adamantium influenciou no teor e na composição química do óleo essencial. Os constituintes espatulenol, óxido cariofileno e germacreno-B apresentaram maior concentração na maioria das procedências avaliadas. O óleo essencial das folhas de C. adamantium apresentou moderada atividade antibacteriana em relação a todos os micro-organismos testados. A atividade antioxidante se deu empregando-se o método de redução do radical estável DPPH, sendo observada fraca atividade antioxidante por meio do ensaio utilizado.

ABSTRACT C. adamantiumis widely used in popular medicine for thetreatment of hypertension, rheumatism and diabetes. This study looked to evaluate the essential oil yield, the chemical composition and the antimicrobial and antioxidant activities of the essential oil from leaves of C. adamantium. A completely randomized design was used with eight treatments and three replications. The essential oil obtained by hydrodestillation of the leaves was analyzed by GC-MS. The results show that the drying type and the processing of the leaf influence the content and chemical composition of the essential oil. The compounds spathulenol, caryophyllene oxide and germacrene-B have higher concentrationsin mostorigins. The essentialoil from theleaves of C.adamantiumshowed moderate bacterial activityagainst all tested microorganisms. The antioxidant activity was determined by the methods of reduction of the DPPH stable radical. The antioxidant activity was weak in the test used.

Antibacterial and anti-inflammatory activities of an extract, fractions, and compounds isolated from Gochnatia pulchra aerial parts.

This paper reports on the in vitro antibacterial and in vivo anti-inflammatory properties of a hydroethanolic extract of the aerial parts of Gochnatia pulchra (HEGP). It also describes the antibacterial activity of HEGP fractions and of the isolated compounds genkwanin, scutellarin, apigenin, and 3,5-O-dicaffeoylquinic acid, as evaluated by a broth microdilution method. While HEGP and its fractions did not provide promising results, the isolated compounds exhibited pronounced antibacterial activity. The most sensitive microorganism was Streptococcus pyogenes, with minimum inhibitory concentration (MIC) values of 100, 50 and 25 µg/mL for genkwanin and the flavonoids apigenin and scutellarin, respectively. Genkwanin produced an MIC value of 25 µg/mL against Enterococcus faecalis. A paw edema model in rats and a pleurisy inflammation model in mice aided investigation of the anti-inflammatory effects of HEGP. This study also evaluated the ability of HEGP to modulate carrageenan-induced interleukin-1 beta (IL-1ß), tumor necrosis factor alpha (TNF-α), and monocyte chemoattractant protein-1 (MCP-1) production. Orally administered HEGP (250 and 500 mg/kg) inhibited carrageenan-induced paw edema. Regarding carrageenan-induced pleurisy, HEGP at 50, 100, and 250 mg/kg diminished leukocyte migration by 71.43%, 69.24%, and 73.34% (P<0.05), respectively. HEGP suppressed IL-1ß and MCP-1 production by 55% and 50% at 50 mg/kg (P<0.05) and 60% and 25% at 100 mg/kg (P<0.05), respectively. HEGP abated TNF-α production by macrophages by 6.6%, 33.3%, and 53.3% at 100, 250, and 500 mg/kg (P<0.05), respectively. HEGP probably exerts anti-inflammatory effects by inhibiting production of the pro-inflammatory cytokines TNF-α, IL-1ß, and MCP-1.

Avaliação da atividade antimicobacteriana da lignana diidrocubebina extraída da Piper cubeba e de seus derivados semissintéticos / Evaluation of antimycobacterial activity of dihydrocubebin lignan extracted from Piper cubeba and its semisynthetic derivatives

RESUMO: A atividade antimicobacteriana de diidrocubebina (1), uma lignana dibenzilbutanodioica obtida a partir de extrato etanólico de sementes da Piper cubeba, e seus derivados foram avaliados in vitro contra três diferentes cepas de Mycobacterium utilizando o método de microdiluição. Dentre as lignanas avaliadas 3 e 4 foram as mais ativas, exibindo valores de CIM de 62,5 µg/mL contra M. avium e M. tuberculosis, respectivamente. Os derivados 2-6 obtidos por síntese parcial possuem diferentes substituintes nos carbonos 9 e 9 ', que alteram polaridade, solubilidade e limitam as rotações livres entre C8-C8' em relação de material (1) de partida. As diferenças estruturais entre estes compostos podem fornecer informações importantes sobre a relação estrutura-atividade antimicobacteriana do esqueleto dibenzilbutanodioico, obtido a partir de fonte natural, como um possível alvo para o desenvolvimento de drogas mais potentes contra a tuberculose

ABSTRACT: Evaluation of antimycobacterial activity of dihydrocubebin lignan extracted from Piper cubeba and its semisynthetic derivatives. The antimycobacterial activity of the dihydrocubebin (1), a dibenzylbutanedioiclignan obtained from ethanolic extract of Piper cubeba seeds, and its derivatives were examined in vitro against three different strains of Mycobacterium using amicrodilution method. Among the lignans evaluated, the 3 and 4 samples were the most active ones, displaying MIC values of 62.5 µg/mL against M. avium and M. tuberculosis, respectively. The derivatives 2-6, obtained for partial synthesis, had different substituents in the carbons 9 and 9', fact thatalters the polarity, solubility and restricts the free rotations between the bonds C8-C8' in relation to the starting material (1). The structural differences among these compounds provide important information about the antimycobacterial structure-activity relationship of the dibenzylbutanodioic skeleton, obtained from natural source, such as a possible target for the development of more powerful drugs against tuberculosis

Chemical Analysis and Study of Phenolics, Antioxidant Activity, and Antibacterial Effect of the Wood and Bark of Maclura tinctoria (L.) D. Don ex Steud.

Maclura tinctoria (L.) D. Don ex Steud. has one of the highest qualities among the coefficients for Brazilian woods (up to 9.6) and resistance rates equivalent to Indian teak (Tectona grandis). In this study, the macromolecular constituents and total phenols compounds as well as the antioxidant and antibacterial activities of this wood were evaluated. Total phenols and proanthocyanidin levels were higher in wood when compared with bark levels. The antioxidant activity of wood extracts (IC(50) = 18.7 µg/mL) was more effective than that of bark extracts (IC(50) = 20.9 µg/mL). Wood and bark extracts revealed a high potential for inhibition of aerobic and anaerobic bacteria. The bark extracts were the most active (MIC from 20 to 60 µg/mL). Both antioxidant activity and high potential for bacteria inhibition turn these extracts promising for drug formulations, especially as antibacterial agent.

Antiophidian properties of plant extracts against Lachesis muta venom

Snakebites comprise a serious health problem in several countries due to their global incidence, which exceeds 2.5 million per year, and the elevated number of victim fatalities. To counteract envenomations, antivenoms have been used regularly for more than a century. Apart from side effects including anaphylactic reactions, antivenoms are not able to efficiently neutralize local tissue damage, which contributes to increasing the severity and morbidity observed in patients. This fact, in turn, may be responsible for economic hardship, particularly in rural populations of developing countries. In the present work, we evaluated the antiophidian properties of 12 Brazilian plant extracts against the hemolytic, coagulant, hemorrhagic and proteolytic effects of Lachesis muta venom. Taken together, our data revealed that most of these aqueous products were capable of inhibiting those activities at different levels, except for Sapindus saponaria extract. In contrast, Stryphnodendron barbatiman extract completely neutralized all the analyzed biological activities. Thus, we may conclude that Brazilian flora may also be useful against L. muta accidents.

Preparation and antimicrobial activity of gelatin microparticles containing propolis against oral pathogens.

Gelatin microparticles containing propolis ethanolic extractive solution were prepared by spray-drying technique. Particles with regular morphology, mean diameter ranging of 2.27 microm to 2.48 microm, and good entrapment efficiency for propolis were obtained. The in vitro antimicrobial activity of microparticles was evaluated against microorganisms of oral importance (Enterococcus faecalis, Streptococcus salivarius, Streptococcus sanguinis, Streptococcus mitis, Streptococcus mutans, Streptococcus sobrinus, Candida albicans, and Lactobacillus casei). The utilized techniques were diffusion in agar and determination of minimum inhibitory concentration. The choice of the method to evaluate the antimicrobial activity of microparticles showed be very important. The microparticles displayed activity against all tested strains of similar way to the propolis, showing greater activity against the strains of E. salivarius, S. sanguinis, S. mitis, and C. albicans.