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This review presents advances in the implementation of high - throughput se quencing and its application to the knowledge of medicinal plants. We conducted a bibliographic search of papers published in PubMed, Science Direct, Google Scholar, Scopus, and Web of Science databases and analyzed the obtained data using VOSviewer (versi on 1.6.19). Given that medicinal plants are a source of specialized metabolites with immense therapeutic values and important pharmacological properties, plant researchers around the world have turned their attention toward them and have begun to examine t hem widely. Recent advances in sequencing technologies have reduced cost and time demands and accelerated medicinal plant research. Such research leverages full genome sequencing, as well as RNA (ribonucleic acid) sequencing and the analysis of the transcr iptome, to identify molecular markers of species and functional genes that control key biological traits, as well as to understand the biosynthetic pathways of bioactive metabolites and regulatory mechanisms of environmental responses. As such, the omics ( e.g., transcriptomics, metabolomics, proteomics, and genomics, among others) have been widely applied within the study of medicinal plants, although their usage in Colombia is still few and, in some areas, scarce. (185)

El extracto de cloroformo (CE) y las fracciones obtenidas de las raíces de Aldama arenaria se evaluaron para determinar su actividad antiproliferativa in vitro contra 10 líneas ce lulares tumorales humanas [leucemia (K - 562), mama (MCF - 7), ovario que expresa un fenotipo resistente a múltiples fármacos (NCI/ADR - RES), melanoma (UACC - 62), pulmón (NCI - H460), próstata (PC - 3), colon (HT29), ovario (OVCAR - 3), glioma (U251) y riñón (786 - 0)]. CE presentó actividad antiproliferativa débil a moderada (log GI 50 medio 1.07), mientras que las fracciones 3 y 4, enriquecidas con diterpenos de tipo pimarane [ent - pimara - 8 (14), ácido 15 - dien - 19 - oico y ent - 8(14),15 - pimaradien - 3 ß - ol], presentaron activid ad moderada a potente para la mayoría de las líneas celulares, con un log GI 50 medio de 0.62 y 0.59, respectivamente. Los resultados mostraron una acción antiproliferativa in vitro prometedora de las muestras obtenidas de A. arenaria , con los mejores resul tados para NCI/ADR - RES, HT29 y OVCAR - 3, y valores de TGI que van desde 5.95 a 28.71 µg.mL - 1, demostrando que los compuestos de esta clase pueden ser prototipos potenciales para el descubrimiento de nuevos agentes terapéuticos

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Cancer cells modify lipid metabolism to proliferate, Passiflora edulis ( P. edulis ) fruit juice (ZuFru) has antitumor activity, but whether a mechanism is through modulation of cell lipids is unknown. T o establish if ZuFru modifies cholesterol and triglycerides in SW480 and SW620. ZuFru composition was studied by phytochemical march; antiproliferative activity by sulforhodamine B, cholesterol , and triglycerides by Folch method. Z ufru contains anthocyanins, flavonoids, alkaloids , and tannins. Cell lines showed differences in their growth rate ( p =0.049). At 39.6 µg/m L of ZuFru, cell viability was decreased: SW480 (45.6%) and SW620 (45.1%). In SW480, cholesterol (44.6%) and triglycerides (46.5%) decreased; In SW620, cholesterol decreased 14.8% and triglycerides increased 7%, with significant differences for both lines. A ntiproliferative activity of ZuFru could be associated with the inhibition of intracellular biosynthesis of cholesterol and triglycerides in SW480. Action mechanisms need to be further investigated.

Las células cancerosas modifican el metabolismo lipídico para proliferar; el zumo de fruta (ZuFru) de Passiflora edulis ( P. edulis ) tiene activida d antitumoral, sin embargo, se desconoce si se involucran los lípidos celulares. E stablecer si ZuFru modifica colesterol y triglicéridos en células SW480 y SW620. C omposición del ZuFru, actividad antiproliferativa, colesterol y triglicéridos. Se encontraro n antocianinas, flavonoides, alcaloides y taninos. Las líneas celulares mostraron diferencias en su tasa de crecimiento ( p =0 . 049); ZuFru 39,6 µg/ml se disminuyó la viabilidad celular; SW480 (45,6%) y SW620 (45,1%); en SW480 colesterol (44,6%) y triglicérid os (46,5%) en SW620, colesterol (14,8%) y los triglicéridos aumentaron 7%, con diferencias significativas para ambas líneas. La actividad antiproliferativa del ZuFru podría estar asociada a la inhibición de la biosíntesis intracelular de colesterol y de tr iglicéridos en SW480, pero no en SW620. Estos mecanismos de acción deben ser fuertemente investigados.

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SUMMARY: Cancer is the second leading cause of death in the world and colorectal cancer is the only cancer that has shown a sustained increase in mortality in the last decade. In the search for new chemotherapeutic agents against cancer, extremophilic microorganisms have shown to be a potential source to obtain molecules of natural origin and with selective cytotoxic action towards cancer cells. In this work we analyzed the ability of a collection of Antarctic soil bacteria, isolated on Collins Glacier from the rhizosphere of Deschampsia antarctica Desv plant, to secrete molecules capable of inhibiting cell proliferation of a colorectal cancer tumor line. Our results demonstrated that culture supernatants from the Antarctic bacteria K2I17 and MI12 decreased the viability of LoVo cells, a colorectal adenocarcinoma cell line. Phenotypic and genotypic characterization of the Antarctic bacteria showed that they were taxonomically related and nucleotide identity analysis based on the 16S rRNA gene sequence identified the bacterium K2I17 as a species belonging to the genus Bacillus.

El cáncer es la segunda causa de muerte en el mundo y el cáncer colorrectal es el único que presenta un aumento sostenido de la mortalidad en la última década. En la búsqueda de nuevos agentes quimioterapeúticos contra el cáncer, se ha propuesto a los microorganismos extremófilos como una fuente potencial para obtener moléculas de origen natural y con acción citotóxica selectiva hacia las células cancerígenas. En este trabajo analizamos la capacidad de una colección de bacterias de suelo antártico, aisladas en el glaciar Collins desde rizosfera de la planta de Deschampsia antarctica Desv, de secretar moléculas capaces de inhibir la proliferación celular de una línea tumoral de cáncer colorrectal. Nuestros resultados demostraron que los sobrenadantes de cultivo de las bacterias antárticas K2I17 y MI12 disminuyeron la viabilidad de la línea celular de adenocarcinoma colorrectal LoVo, en un ensayo de reducción metabólica de MTT. La caracterización fenotípica y genotípica de las bacterias antárticas, demostró que estaban relacionadas taxonómicamente y el análisis de la identidad nucleotídica en base a la secuencia del gen ARNr 16S identificó a la bacteria K2I17 como una especie perteneciente al género Bacillus.

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Methanol extract of Muntingia calabura L. leaf (MEMCL) has been shown to exert the antiproliferative activity against the HT-29 (human colon adenocarcinoma) cell line. To further investigate on the medicinal potential of this plant, MEMCL was sequentially partitioned to obtain the petroleum ether, ethyl acetate and aqueous partitions, whichwas then tested against the HT-29 cell line and also subjected to the in vitro anti-inflammatory study. The most effective partition was also subjected to the phytoconstituents analysis using the UHPLC-ESI-MS. Findings showed that the ethyl acetate partition (EAP) exerts the most effective antiproliferative activity (IC50 = 58.0 ± 12.9 µg/mL) without affecting the 3T3 normal fibroblast cells, exhibits the highest anti-inflammatory effect when assessed using the lipoxygenase (> 95%) and xanthine oxidase (> 70%) assays, and contained various types of polyphenolics. In conclusion, M. calabura exerts apoptotic-mediated antiproliferative activity, partly via the anti-inflammatory action and synergistic action between the polyphenolics.

Se ha demostrado que el extracto metanólico de hoja de Muntingia calabura L. (MEMCL) ejerce actividad antiproliferativa contra la línea celular HT-29 (adenocarcinoma de colon humano). Para investigar más a fondo el potencial medicinal de esta planta, MEMCL se dividió secuencialmente para obtener el éter de petróleo, el acetato de etilo y las particiones acuosas, que luego se probó contra la línea celular HT-29 y también se sometió al estudio antiinflamatorio in vitro. La partición más eficaz también se sometió al análisis de fitoconstituyentes utilizando UHPLC-ESI-MS. Los resultados mostraron que la partición de acetato de etilo (EAP) ejerce la actividad antiproliferativa más efectiva (IC50= 58.0 ± 12.9 µg/mL) sin afectar las células de fibroblastos normales 3T3, exhibe el mayor efecto antiinflamatorio cuando se evalúa usando la lipoxigenasa (> 95%) y ensayos de xantina oxidasa (> 70%), y contenían varios tipos de polifenoles. En conclusión, M. calabura ejerce una actividad antiproliferativa mediada por apoptosis, en parte a través de la acción antiinflamatoria y la acción sinérgica entre los polifenoles.

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The objective of this work was to collect information on the curative use of plants in the municipality of Teziutlán, Puebla through semi-structured interviews. Thus, 78 plants used for medicinal purposes were identified, of which 40 are native to Mexico and 38 introduced; The value of use (UV) of each one and the Informant's Consensus Factor (FCI) of 10 categories of diseases were calculated. The five most frequently used plants are Ruta chalepensis L., Rosmarinus officinalis, Arnica montana, Loeselia mexicana (Lam.) Brandegee and Sambucus cerulea var., Neomexicana, which underwent a chemical and pharmacological review. On the other hand, the most frequent preparations are infusion and decoction, using mainly leaves (49.34%) and flowers (19.51%). It is concluded that the inhabitants of Teziutlán have a fairly homogeneous ethnomedical knowledge, setting the standard for research on its pharmacological properties.

El objetivo del presente trabajo fue recopilar información sobre el uso curativo de las plantas del municipio de Teziutlán, Puebla por medio de entrevistas semiestructuradas. Así, se identificaron 78 plantas utilizadas con fines medicinales, de las cuales 40 son propias de México y 38 introducidas; se calculó el valor de uso (UV) de cada una y el Factor de Consenso del Informante (FCI) de 10 categorías de padecimientos. Las cinco plantas utilizadas con mayor frecuencia son Ruta chalepensis L., Rosmarinus officinalis, Arnica montana, Loeselia mexicana (Lam.) Brandegee y Sambucus cerulea var., neomexicana, a las que se les hizo una revisión química y farmacológica. Por otro lado, las preparaciones más frecuentes son infusión y decocción, utilizando principalmente hojas (49.34 %) y flores (19.51 %). Se concluye que los habitantes de Teziutlán cuentan con un conocimiento etnomédico bastante homogéneo, dando la pauta para investigaciones sobre sus propiedades farmacológicas.

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Bauhinia variegata plant is a very popular and traditionally potent ethnomedicine. Therefore, it is need of hour to study ameliorative characteristics of B. variegata for novel secondary metabolites. The current study was designed to explore antiproliferative potential of B. variegata due to scant reports on this aspect. Extracts of various parts (flowers, leaves, bark, stem, and roots) were prepared by successive maceration using organic solvents in increasing order of polarity (n-hexane, ethyl acetate, methanol, and water). The determination of polyphenolic contents was done by using colorimetric methods while antioxidant potential was measured using reducing power assay. Brine shrimp lethality assay was performed for determining preliminary cytotoxicity and antiproliferative activity against breast cancer MCF-7 cell line using MTT protocols. Moreover, antimicrobial activities were detected by using disc diffusion assay. The alpha-amylase assay was performed to monitor the antidiabetic potential of the plant. In case of phytochemical analysis methanolic extract of leaves and bark showed highest phenolic and flavonoids contents. n-Hexane and ethyl acetate extracts of stem and roots exhibited more than 90% mortality with LD50 ranges between 1-25 µg/mL when studied by brine shrimp lethality assay. n-Hexane and ethyl acetate extracts of roots and stem also showed antiproliferative activity against human breast cancer MCF-7 cell line with IC50 values ranges between 12.10-14.20 µg/mL. Most of the extracts displayed moderately high antibacterial and antifungal activities. The n-hexane extract of roots showed antidiabetic activity with 60.80 ± 0.20% inhibition of alpha-amylase. In sum, these preliminary results will be useful for further compound isolation from selected plant parts for the discovery of antibacterial, antidiabetic, and anticancer lead candidates.

A planta Bauhinia variegata é uma etnomedicina muito popular e tradicionalmente potente. Portanto, as características de melhoria de B. variegata foram estudadas. Foi avaliada a determinação dos teores antioxidantes e polifenólicos. O ensaio de letalidade do camarão de salmoura foi realizado para determinar a citotoxicidade preliminar e a atividade antiproliferativa contra linhas de células de câncer de mama MCF-7 usando protocolos de MTT. Além disso, foram detectadas atividades antimicrobianas. O ensaio da alfa-amilase foi realizado para monitorar o potencial antidiabético da planta. Dentre vinte amostras diferentes, o extrato metanólico (EM) da casca apresentou os maiores teores fenólicos totais. A EM das folhas apresentou excelente conteúdo de flavonoides, atividade antioxidante significativa foi exibida pelo extrato hexânico do caule. O extrato do caule de hexano exibe 77,40% como citotóxico em DL50 10,50 µg/mL quando avaliado através do ensaio de letalidade de artêmia. Extratos de hexano e acetato de etila de raiz e caule mostraram atividade antiproliferativa contra a linhagem celular MCF7 de câncer de mama humano (IC50 12,10-14,20 µg/mL). Para potencial antimicrobiano importante, vários extratos exibiram excelentes atividades antibacteriana e antifúngica, enquanto o extrato de n-hexano da raiz mostrou atividade antidiabética (60,80 ± 0,20% na concentração de 200 µg/mL). Em suma, estes resultados preliminares serão úteis para isolamento adicional de compostos a partir de partes de plantas selecionadas para a descoberta de candidatos a antibacterianos, antidiabéticos e anticâncer.

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Abstract Bauhinia variegata plant is a very popular and traditionally potent ethnomedicine. Therefore, it is need of hour to study ameliorative characteristics of B. variegata for novel secondary metabolites. The current study was designed to explore antiproliferative potential of B. variegata due to scant reports on this aspect. Extracts of various parts (flowers, leaves, bark, stem, and roots) were prepared by successive maceration using organic solvents in increasing order of polarity (n-hexane, ethyl acetate, methanol, and water). The determination of polyphenolic contents was done by using colorimetric methods while antioxidant potential was measured using reducing power assay. Brine shrimp lethality assay was performed for determining preliminary cytotoxicity and antiproliferative activity against breast cancer MCF-7 cell line using MTT protocols. Moreover, antimicrobial activities were detected by using disc diffusion assay. The alpha-amylase assay was performed to monitor the antidiabetic potential of the plant. In case of phytochemical analysis methanolic extract of leaves and bark showed highest phenolic and flavonoids contents. n-Hexane and ethyl acetate extracts of stem and roots exhibited more than 90% mortality with LD50 ranges between 1-25 µg/mL when studied by brine shrimp lethality assay. n-Hexane and ethyl acetate extracts of roots and stem also showed antiproliferative activity against human breast cancer MCF-7 cell line with IC50 values ranges between 12.10-14.20 µg/mL. Most of the extracts displayed moderately high antibacterial and antifungal activities. The n-hexane extract of roots showed antidiabetic activity with 60.80 ± 0.20% inhibition of alpha-amylase. In sum, these preliminary results will be useful for further compound isolation from selected plant parts for the discovery of antibacterial, antidiabetic, and anticancer lead candidates.

Resumo A planta Bauhinia variegata é uma etnomedicina muito popular e tradicionalmente potente. Portanto, as características de melhoria de B. variegata foram estudadas. Foi avaliada a determinação dos teores antioxidantes e polifenólicos. O ensaio de letalidade do camarão de salmoura foi realizado para determinar a citotoxicidade preliminar e a atividade antiproliferativa contra linhas de células de câncer de mama MCF-7 usando protocolos de MTT. Além disso, foram detectadas atividades antimicrobianas. O ensaio da alfa-amilase foi realizado para monitorar o potencial antidiabético da planta. Dentre vinte amostras diferentes, o extrato metanólico (EM) da casca apresentou os maiores teores fenólicos totais. A EM das folhas apresentou excelente conteúdo de flavonoides, atividade antioxidante significativa foi exibida pelo extrato hexânico do caule. O extrato do caule de hexano exibe 77,40% como citotóxico em DL50 10,50 µg/mL quando avaliado através do ensaio de letalidade de artêmia. Extratos de hexano e acetato de etila de raiz e caule mostraram atividade antiproliferativa contra a linhagem celular MCF7 de câncer de mama humano (IC50 12,10-14,20 µg/mL). Para potencial antimicrobiano importante, vários extratos exibiram excelentes atividades antibacteriana e antifúngica, enquanto o extrato de n-hexano da raiz mostrou atividade antidiabética (60,80 ± 0,20% na concentração de 200 µg/mL). Em suma, estes resultados preliminares serão úteis para isolamento adicional de compostos a partir de partes de plantas selecionadas para a descoberta de candidatos a antibacterianos, antidiabéticos e anticâncer.

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The search for compounds with anticancer effects is of paramount importance today due to the high incidence of the disease. The Euphorbiaceae family is known for having compounds with therapeutic properties, one of its genera being Croton. It has several species, which contain compounds already known for their biological activities, presenting anti-inflammatory, antimicrobial and anticancer properties. Thus, the cytotoxicity/antiproliferative activity of semi-purified fractions and compounds isolated from Croton echioides in liver tumor cells of Rattus norvegicus (HTC) was evaluated by the MTT test. The semi-purified fractions showed cytotoxicity at concentrations above 200 µg/mL, at 24, 48 and 72 hours, reaching cell viability of 24.78% [400 µg/mL] at 24 hours, 12.79% [500 µg/mL] at 48 hours and 10.57% [300 µg/mL] at 72 hours. For the isolated compounds, lupeol had a cytotoxic effect in all concentrations (1, 5, 10, 15, 20, 40, 60, 80 and 100 µg/mL) and tested times (24, 48 and 72 hours), reaching minimum viability of 4.37% [100 µg/mL], within 72 hours. The clerodan diterpenes CEH-1 and CEH-4 also showed antiproliferative activity, with minimum viability of 36.19% [100 µg/mL] over 72 hours and 21.33% [100 µg/mL] over 48 hours, respectively. However, the clerodan diterpenes CEH-2 and CEH-3 did not shows a cytotoxic effect for HTC cells. Thus, there is a cytotoxic/antiproliferative potential of C. echioides against tumor cells, with targeted to mitochondrial enzymes, associated with cell proliferation, indicating that this species deserves prominence in the search for new molecules for the treatment of cancer.

A busca por compostos com efeitos anticâncer é de suma importância nos dias atuais devido à alta incidência desta doença. A família Euphorbiaceae é conhecida por possuir compostos com propriedades terapêuticas, sendo um de seus gêneros o Croton. Este possui diversas espécies, que contêm compostos já conhecidos por suas atividades biológicas, apresentando propriedades anti-inflamatórias, antimicrobianas e anticancerígenas. Assim, a citotoxicidade/atividade antiproliferativa de frações semipurificadas e compostos isolados de Croton echioides em células tumorais hepáticas de Rattus norvegicus (HTC) foi avaliada pelo teste MTT. As frações semipurificadas apresentaram citotoxicidade em concentrações acima de 200 µg/mL, em 24, 48 e 72 horas, atingindo viabilidade celular de 24,78% [400 µg/mL] em 24 horas, 12,79% [500 µg/mL] em 48 horas e 10,57% [300 µg/mL] às 72 horas. Para os compostos isolados, o lupeol teve efeito citotóxico em todas as concentrações (1, 5, 10, 15, 20, 40, 60, 80 e 100 µg/mL) e tempos testados (24, 48 e 72 horas), atingindo a viabilidade mínima de 4,37% [100 µg/mL], em 72 horas. Os diterpenos clerodan CEH-1 e CEH-4 também apresentaram atividade antiproliferativa, com viabilidade mínima de 36,19% [100 µg/mL] em 72 horas e 21,33% [100 µg/mL] em 48 horas, respectivamente. No entanto, os diterpenos clerodanos CEH-2 e CEH-3 não apresentaram efeito citotóxico para células HTC. Assim, existe um potencial citotóxico/antiproliferativo de C. echioides contra células tumorais, com enzimas direcionadas a enzimas mitocondriais, associadas à proliferação celular, indicando que esta espécie merece destaque na busca de novas moléculas para o tratamento do câncer.

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ABSTRACT: Glycosaminoglycans (GAGs) are long-chain polysaccharides that are divided into sulphates and non-sulphates, these being chondroitin sulphate, heparan sulphate, dermatan sulphate, heparin sulphate and the only non-sulphate in the group is hyaluronic acid. GAGs are obtained from animal tissue and by an expensive low-yield extraction process; however, they are highly commercially valued polysaccharides and exploited in the biomedical market. Their disaccharidic composition, chain length and sulfation pattern present great variability depending on the species and extraction factors. GAGs possess immunomodulatory, antioxidant, antiviral, anti-inflammatory, neuroprotective, antiproliferative and anticoagulant properties, functioning as therapeutic agents modulating an array of biological processes. This report presents the general aspects of each GAG, source and extraction process, in addition to the characteristics that give them the most varied therapeutic properties and pharmacological applications.

RESUMO: Os glicosaminoglicanos (GAGs) são polissacarídeos de cadeias longas que se dividem em sulfatados e não sulfatados, sendo estes, sulfato de condroitina, sulfato de heparana, sulfato de dermatana, sulfato de heparina e o único não sulfatado do grupo que é o ácido hialurônico. Os GAGs são encontrados em todo tecido animal, são extraídos por um processo de alto custo e baixo rendimento, no entanto, o material obtido é valorizado comercialmente e amplamente explorado no mercado biomédico. Sua composição dissacarídica, comprimento da cadeia e padrão de sulfatação apresentam grande variabilidade dependendo das espécies e fatores de extração. Os GAGs possuem propriedades imunomoduladoras, antioxidantes, antivirais, anti-inflamatórias, neuroprotetoras, antiproliferativas e anticoagulantes, além de farmacológicas, funcionando como agentes terapêuticos moduladores de uma série de processos biológicos. Este relatório apresenta os aspectos gerais de cada GAG, fonte e processo de extração, além das características que lhes conferem as mais variadas propriedades terapêuticas e aplicações farmacológicas.

RESUMO

Glycosaminoglycans (GAGs) are long-chain polysaccharides that are divided into sulphates and non-sulphates, these being chondroitin sulphate, heparan sulphate, dermatan sulphate, heparin sulphate and the only non-sulphate in the group is hyaluronic acid. GAGs are obtained from animal tissue and by an expensive low-yield extraction process; however, they are highly commercially valued polysaccharides and exploited in the biomedical market. Their disaccharidic composition, chain length and sulfation pattern present great variability depending on the species and extraction factors. GAGs possess immunomodulatory, antioxidant, antiviral, anti-inflammatory, neuroprotective, antiproliferative and anticoagulant properties, functioning as therapeutic agents modulating an array of biological processes. This report presents the general aspects of each GAG, source and extraction process, in addition to the characteristics that give them the most varied therapeutic properties and pharmacological applications.(AU)

Os glicosaminoglicanos (GAGs) são polissacarídeos de cadeias longas que se dividem em sulfatados e não sulfatados, sendo estes, sulfato de condroitina, sulfato de heparana, sulfato de dermatana, sulfato de heparina e o único não sulfatado do grupo que é o ácido hialurônico. Os GAGs são encontrados em todo tecido animal, são extraídos por um processo de alto custo e baixo rendimento, no entanto, o material obtido é valorizado comercialmente e amplamente explorado no mercado biomédico. Sua composição dissacarídica, comprimento da cadeia e padrão de sulfatação apresentam grande variabilidade dependendo das espécies e fatores de extração. Os GAGs possuem propriedades imunomoduladoras, antioxidantes, antivirais, anti-inflamatórias, neuroprotetoras, antiproliferativas e anticoagulantes, além de farmacológicas, funcionando como agentes terapêuticos moduladores de uma série de processos biológicos. Este relatório apresenta os aspectos gerais de cada GAG, fonte e processo de extração, além das características que lhes conferem as mais variadas propriedades terapêuticas e aplicações farmacológicas.(AU)

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Abstract This paper reports the in vitro antiproliferative effects, antiprotozoal, anti-herpes and antimicrobial activities of 32 organic extracts of 14 marine sponges and 14 corals collected in northeast Brazilian coast. The ethanolic extracts of the sponges Amphimedon compressa and Tedania ignis, and the acetone extract of Dysidea sp. showed relevant results concerning the antiproliferative effects against A549, HCT-8, and PC-3 cell lines by sulforhodamine B assay, but also low specificity. Concerning the antiprotozoal screening, the ethanolic extract of Amphimedon compressa and the acetone and ethanolic extracts of Dysidea sp. were the most active against Leishmania amazonensis and Trypanosoma cruzi expressing β-galactosidase in THP-1 cells. In the preliminary anti-HSV-1 (KOS strain) screening, the ethanolic extracts of the sponges Amphimedon compressa, Haliclona sp. and Chondrosia collectrix inhibited viral replication by more than 50%. The most promising anti-herpes results were observed for the ethanolic extract of Haliclona sp. showing high selective indices against HSV-1, KOS and 29R strains (SI> 50 and >79, respectively), and HSV-2, 333 strain (IS>108). The results of the antibacterial screening indicated that only the ethanolic extract of Amphimedon compressa exhibited a weak activity against Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli by the disk diffusion method. In view of these results, the extracts of Amphimedon compressa, Tedania ignis and Dysidea sp. were selected for further studies aiming the isolation and identification of the bioactive compounds with antiproliferative and/or antiprotozoal activities. The relevant anti-herpes activity of the ethanolic extract of Haliclona sp. also deserves special attention, and will be further investigated.

Resumo Este artigo reporta as atividades in vitro antiproliferativa, atiprotozoárica, anti-herpética e antimicrobiana de 32 extratos orgânicos provenientes de 14 esponjas marinhas e 14 corais coletados no litoral nordestino brasileiro. Os extratos etanólicos das esponjas Amphimedon compressa e Tedania ignis, e o extrato acetônico de Dysidea sp. demonstraram resultados promissores em relação aos efeitos antiproliferativos frente as linhagens celulares A549, HCT-8, PC-3 pelo método da sulforrodamina B, mas sem especificidade. Em relação à atividade antiprotozárica, os extratos etanólico de Amphimedon compressa e acetônico e etanólico de Dysidea sp. apresentaram atividade contra Leishmania amazonensis e Trypanosoma cruzi através do método de expressão de β-galactosidase em células THP-1. Na investigação preliminar de atividade antiviral frente ao vírus Herpes simplex tipo 1 (cepa KOS), os extratos etanólicos das esponjas Amphimedon compressa, Haliclona sp. e Chondrosia collectrix inibiram mais de 50% da replicação viral. O extrato etanólico da esponja Haliclona sp. demonstrou resultados promissores para atividade anti-herpética com altos índices de seletividade para as cepas KOS (IS >50) e 29R (IS>79) frente ao VHS-1 e cepa 333 (IS>108) frente ao VHS-2. O extrato etanólico da esponja Amphimedon compressa exibiu uma pequena atividade contra Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli pelo método de difusão em disco. De acordo com os resultados apresentados, os extratos das esponjas Amphimedon compressa, Tedania ignis e Dysidea sp. serão selecionados para futuros estudos de isolamento e identificação dos compostos bioativos para as atividades antiproliferativa e antiprozoárica. O extrato etanólico de Haliclona sp. será investigado por possuir atividade relevante anti-herpética.

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Abstract Essential oils, which may be extracted from several parts of plants, have different biological activities. The Brazilian Cerrado has a large variety of plants that yield essential oils, even though many have not been studied yet. Taking into account the biodiversity of this biome, this study aimed at evaluating the antiproliferative activity of essential oils extracted from three species of plants of the Cerrado in Goiás state: Campomanesia adamantium (Cambess.) O. Berg, Protium ovatum (Engl. in Mart.) and Cardiopetalum calophyllum (Schltdl.). Essential oils were extracted from both C. adamantium and C. calophyllum leaves and from P. ovatum leaves and green fruits by hydrodistillation carried out by a Clevenger-type apparatus. The chemical composition of the essential oils was determined by Gas Chromatography coupled to Mass Spectrometry (GC-MS). The following major chemical constituents were identified in the essential oils under investigation: β-myrcene (62.00%), spathulenol (28.78%), germacrene-B (18.27%), β-caryophyllene oxide (16.40%), β-caryophyllene (14.00%), α-pinene (11.30%), viridiflorol (9.99%), limonene (7.30%) and (Z,E)-pharnesol (6.51%). The antiproliferative activity was evaluated in different human tumor cell lines: breast adenocarcinoma (MCF-7), cervical adenocarcinoma (HeLa) and glioblastoma (M059J). A normal human cell line was included (GM07492A, lung fibroblasts). Results showed that essential oils from C. adamantium leaves got the lowest values of IC50 in all strains of tumor cells under evaluation. They were significantly lower than the ones of the normal cell line, an evidence of selectivity. It is worth mentioning that this is the first report of the antiproliferative activity of essential oils from C. adamantium , P. ovatum and C. calophyllum against human tumor cells.

Resumo Os óleos essenciais podem ser extraídos de várias partes das plantas e apresentam diversas atividades biológicas. O Cerrado brasileiro possui uma grande variedade de plantas produtoras de óleos essenciais muitas delas ainda não estudadas. Levando-se em consideração a biodiversidade desse bioma, o objetivo deste trabalho foi avaliar a atividade antiproliferativa dos óleos essenciais extraídos de três espécies de plantas ocorrentes no Cerrado do estado de Goiás: Campomanesia adamantium (Cambess.) O. Berg, Protium ovatum (Engl. in Mart.) e Cardiopetalum calophyllum (Schltdl.). Os óleos essenciais foram obtidos das folhas de C. adamantium e C. calophyllum e das folhas e frutos verdes de P. ovatum por hidrodestilação, usando o aparelho do tipo Clevenger. A composição química dos óleos essenciais foi determinada pelo método de Cromatografia Gasosa acoplada à Espectrometria de Massas (CG-EM). Os constituintes químicos majoritários identificados nos óleos essenciais estudados foram: β-mirceno (62,00%), espatulenol (28,78%), germacreno-B (18,27%), óxido de β-cariofileno (16,40%), β-cariofileno (14,00%), α-pineno (11,30%), viridiflorol (9,99%), limoneno (7,30%) e (Z,E)-farnesol (6,51%). A atividade antiproliferativa foi avaliada em diferentes linhagens de células tumorais humanas: adenocarcinoma de mama (MCF-7), adenocarcinoma cervical (HeLa) e gliobastoma (M059J), além de, uma linhagem celular humana normal (GM07492A, fibroblastos pulmonares). O óleo essencial das folhas de C. adamantium exibiu menores valores de CI50 em todas as linhagens celulares tumorais avaliadas, sendo menores que aquele obtido na linhagem celular normal, indicando seletividade. Este é o primeiro relato da atividade antiproliferativa dos óleos essenciais de C. adamantium , P. ovatum e C. calophyllum contra células tumorais humanas.

Assuntos

RESUMO

Chloroform extract (CE) and fractions obtained from Aldama arenaria roots were evaluated for their in vitro antiproliferative activity against 10 human tumor cell lines [leukemia (K-562), breast (MCF-7), ovary expressing a multidrug-resistant phenotype (NCI/ADR-RES), melanoma (UACC-62), lung (NCI-H460), prostate (PC-3), colon (HT29), ovary (OVCAR-3), glioma (U251), and kidney (786-0)]. CE presented weak to moderate antiproliferative activity (mean log GI50 1.07), whereas fractions 3 and 4, enriched with pimaranetype diterpenes [ent-pimara-8(14),15-dien-19-oic acid and ent-8(14),15-pimaradien-3ß-ol], presented moderate to potent activity for most cell lines, with mean log GI50 of 0.62 and 0.59, respectively. The results showed promising in vitro antiproliferative action of the samples obtained from A. arenaria, with the best results for NCI/ADR-RES, HT29, and OVCAR-3, and TGI values ranging from 5.95 to 28.71 µg.ml -1, demonstrating that compounds of this class may be potential prototypes for the discovery of new therapeutic agents.

El extracto de cloroformo (CE) y las fracciones obtenidas de las raíces de Aldama arenaria fueron evaluadas por su actividad antiproliferativa in vitro contra 10 líneas celulares tumorales humanas [leucemia (K-562), mama (MCF-7), ovario que expresa un fenotipo resistente a múltiples fármacos (NCI/ADR-RES), melanoma (UACC-62), pulmón (NCI-H460), próstata (PC-3), colon (HT29), ovario (OVCAR-3), glioma (U251) y riñón (786-0)]. CE presentó actividad antiproliferativa débil a moderada (log GI50 promedio de 1.07), mientras que las fracciones 3 y 4, enriquecidas con diterpenos de tipo pimarane [ent-pimara-8 (14), ácido 15-dien-19-oico y ent-8 (14), 15-pimaradien-3ß-ol], presentaron actividad moderada a potente para la mayoría de las líneas celulares, con un log GI50 promedio de 0.62 y 0.59, respectivamente. Los resultados mostraron una prometedora acción antiproliferativa in vitro de las muestras obtenidas de A. arenaria, con los mejores resultados para NCI/ADR-RES, HT29 y OVCAR-3, y valores de TGI que van desde 5.95 a 28.71 µg.ml -1, lo que demuestra que los compuestos de esta clase pueden ser prototipos potenciales para el descubrimiento de nuevos agentes terapéuticos.

Assuntos

RESUMO

This paper reports the in vitro antiproliferative effects, antiprotozoal, anti-herpes and antimicrobial activities of 32 organic extracts of 14 marine sponges and 14 corals collected in northeast Brazilian coast. The ethanolic extracts of the sponges Amphimedon compressa and Tedania ignis, and the acetone extract of Dysidea sp. showed relevant results concerning the antiproliferative effects against A549, HCT-8, and PC-3 cell lines by sulforhodamine B assay, but also low specificity. Concerning the antiprotozoal screening, the ethanolic extract of Amphimedon compressa and the acetone and ethanolic extracts of Dysidea sp. were the most active against Leishmania amazonensis and Trypanosoma cruzi expressing -galactosidase in THP-1 cells. In the preliminary anti-HSV-1 (KOS strain) screening, the ethanolic extracts of the sponges Amphimedon compressa, Haliclona sp. and Chondrosia collectrix inhibited viral replication by more than 50%. The most promising anti-herpes results were observed for the ethanolic extract of Haliclona sp. showing high selective indices against HSV-1, KOS and 29R strains (SI> 50 and >79, respectively), and HSV-2, 333 strain (IS>108). The results of the antibacterial screening indicated that only the ethanolic extract of Amphimedon compressa exhibited a weak activity against Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli by the disk diffusion method. In view of these results, the extracts of Amphimedon compressa, Tedania ignis and Dysidea sp. were selected for further studies aiming the isolation and identification of the bioactive compounds with antiproliferative and/or antiprotozoal activities. The relevant anti-herpes activity of the ethanolic extract of Haliclona sp. also deserves special attention, and will be further investigated.(AU)

Este artigo reporta as atividades in vitro antiproliferativa, atiprotozoárica, anti-herpética e antimicrobiana de 32 extratos orgânicos provenientes de 14 esponjas marinhas e 14 corais coletados no litoral nordestino brasileiro. Os extratos etanólicos das esponjas Amphimedon compressa e Tedania ignis, e o extrato acetônico de Dysidea sp. demonstraram resultados promissores em relação aos efeitos antiproliferativos frente as linhagens celulares A549, HCT-8, PC-3 pelo método da sulforrodamina B, mas sem especificidade. Em relação à atividade antiprotozárica, os extratos etanólico de Amphimedon compressa e acetônico e etanólico de Dysidea sp. apresentaram atividade contra Leishmania amazonensis e Trypanosoma cruzi através do método de expressão de -galactosidase em células THP-1. Na investigação preliminar de atividade antiviral frente ao vírus Herpes simplex tipo 1 (cepa KOS), os extratos etanólicos das esponjas Amphimedon compressa, Haliclona sp. e Chondrosia collectrix inibiram mais de 50% da replicação viral. O extrato etanólico da esponja Haliclona sp. demonstrou resultados promissores para atividade anti-herpética com altos índices de seletividade para as cepas KOS (IS >50) e 29R (IS>79) frente ao VHS-1 e cepa 333 (IS>108) frente ao VHS-2. O extrato etanólico da esponja Amphimedon compressa exibiu uma pequena atividade contra Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli pelo método de difusão em disco. De acordo com os resultados apresentados, os extratos das esponjas Amphimedon compressa, Tedania ignis e Dysidea sp. serão selecionados para futuros estudos de isolamento e identificação dos compostos bioativos para as atividades antiproliferativa e antiprozoárica. O extrato etanólico de Haliclona sp. será investigado por possuir atividade relevante anti-herpética.(AU)

Assuntos

RESUMO

Background:Vaccinium meridionale produces fruits with a high content of anthocyanins and polyphenols with great antioxidant capacity. Objective: produce vinegar from V. meridionale alcoholic beverages and to determine the content of bioactive antioxidant compounds, antioxidant capacity, and cytotoxic activity on colorectal cancer cells. Methods: Wine and vinegar samples were obtained by fermentation of V. meridionale berries juice, using three extractive processes: mechanical maceration (MAC), preheating to 80°C (CAL) and a combination of both (MIX). During acetic fermentation, titratable acidity and acetic acid content were evaluated. Fermentation progress was recorded and compared by measuring the antioxidant potential by DPPH, FRAP, and ORAC. Polyphenols, anthocyanins and hydroxycinnamic acids were quantified. Finally, the antiproliferative activity of vinegar was evaluated in SW480 colon cancer cells. Results: In acetic fermentation, yield and productivity were independent of extraction, indicating that they do not affect the biotransformation of alcohol into vinegar. The alcoholic beverages showed the highest antioxidant activity; after acetic fermentation, a decrease in antioxidant potential was observed in all three extractive processes evaluated. The different vinegar obtained by CAL and MIX, showed the highest values of antioxidant activity, polyphenols, and anthocyanins. The inhibition of the antiproliferative activity of vinegar was dose-dependent and showed an IC50 of 536 µg/mL. Conclusions: The vinegar prepared from V. meridionale berries presented an outstanding antioxidant and antiproliferative activity. The reason is the contents of bioactive compounds and their antioxidant power, which may contribute to chemoprevention in secondary cancer prevention.

Antecedentes: Vaccinium meridionale produce frutos con alto contenido en antocianinas y polifenoles con elevada capacidad antioxidante. Objetivo: Producir vinagre a partir de bebidas alcohólicas de V. meridionale y determinar el contenido de compuestos bioactivos antioxidantes, capacidad antioxidante y actividad citotóxica sobre células de cáncer colorrectal. Métodos: Muestras de Vino y vinagre fueron obtenidas mediante fermentación del jugo de V. meridionale, usando tres procesos extractivos: maceración mecánica (MAC), precalentamiento a 80 °C (CAL) y una combinación de ambos (MIX). En la fermentación acética fueron evaluadas la acidez titulable y el contenido de ácido acético. Se registró y comparó la evolución de la fermentación midiendo el potencial antioxidante por DPPH, FRAP y ORAC. Se cuantificaron los polifenoles, antocianinas y ácidos hidroxicinámicos. Finalmente, la actividad antiproliferativa del vinagre fue evaluada en células de cáncer de colon SW480. Resultados: En la fermentación acética, el rendimiento y la productividad fueron independientes de la extracción indicando que no afectan la biotransformación del alcohol en vinagre. Las bebidas alcohólicas mostraron la mayor actividad antioxidante, después de la fermentación acética se observó una disminución del potencial antioxidante en los tres procesos extractivos evaluados. Los vinagres obtenidos por CAL y MIX, presentaron los mayores valores de actividad antioxidante, polifenoles y antocianinas. La inhibición de la actividad antiproliferativa del vinagre fue dosis dependiente y mostró un IC50 de 536 µg/mL. Conclusiones: El vinagre preparado a partir de bayas de V. meridionale presentó una excelente actividad antioxidante y antiproliferativa debido al contenido de compuestos bioactivos y poder antioxidante que puede contribuir a la quimioprevención en la prevención secundaria del cáncer.

Assuntos

RESUMO

Essential oils, which may be extracted from several parts of plants, have different biological activities. The Brazilian Cerrado has a large variety of plants that yield essential oils, even though many have not been studied yet. Taking into account the biodiversity of this biome, this study aimed at evaluating the antiproliferative activity of essential oils extracted from three species of plants of the Cerrado in Goiás state: Campomanesia adamantium (Cambess.) O. Berg, Protium ovatum (Engl. in Mart.) and Cardiopetalum calophyllum (Schltdl.). Essential oils were extracted from both C. adamantium and C. calophyllum leaves and from P. ovatum leaves and green fruits by hydrodistillation carried out by a Clevenger-type apparatus. The chemical composition of the essential oils was determined by Gas Chromatography coupled to Mass Spectrometry (GC-MS). The following major chemical constituents were identified in the essential oils under investigation: -myrcene (62.00%), spathulenol (28.78%), germacrene-B (18.27%), -caryophyllene oxide (16.40%), -caryophyllene (14.00%), -pinene (11.30%), viridiflorol (9.99%), limonene (7.30%) and (Z,E)-pharnesol (6.51%). The antiproliferative activity was evaluated in different human tumor cell lines: breast adenocarcinoma (MCF-7), cervical adenocarcinoma (HeLa) and glioblastoma (M059J). A normal human cell line was included (GM07492A, lung fibroblasts). Results showed that essential oils from C. adamantium leaves got the lowest values of IC50 in all strains of tumor cells under evaluation. They were significantly lower than the ones of the normal cell line, an evidence of selectivity. It is worth mentioning that this is the first report of the antiproliferative activity of essential oils from C. adamantium , P. ovatum and C. calophyllum against human tumor cells.(AU)

Os óleos essenciais podem ser extraídos de várias partes das plantas e apresentam diversas atividades biológicas. O Cerrado brasileiro possui uma grande variedade de plantas produtoras de óleos essenciais muitas delas ainda não estudadas. Levando-se em consideração a biodiversidade desse bioma, o objetivo deste trabalho foi avaliar a atividade antiproliferativa dos óleos essenciais extraídos de três espécies de plantas ocorrentes no Cerrado do estado de Goiás: Campomanesia adamantium (Cambess.) O. Berg, Protium ovatum (Engl. in Mart.) e Cardiopetalum calophyllum (Schltdl.). Os óleos essenciais foram obtidos das folhas de C. adamantium e C. calophyllum e das folhas e frutos verdes de P. ovatum por hidrodestilação, usando o aparelho do tipo Clevenger. A composição química dos óleos essenciais foi determinada pelo método de Cromatografia Gasosa acoplada à Espectrometria de Massas (CG-EM). Os constituintes químicos majoritários identificados nos óleos essenciais estudados foram: -mirceno (62,00%), espatulenol (28,78%), germacreno-B (18,27%), óxido de -cariofileno (16,40%), -cariofileno (14,00%), -pineno (11,30%), viridiflorol (9,99%), limoneno (7,30%) e (Z,E)-farnesol (6,51%). A atividade antiproliferativa foi avaliada em diferentes linhagens de células tumorais humanas: adenocarcinoma de mama (MCF-7), adenocarcinoma cervical (HeLa) e gliobastoma (M059J), além de, uma linhagem celular humana normal (GM07492A, fibroblastos pulmonares). O óleo essencial das folhas de C. adamantium exibiu menores valores de CI50 em todas as linhagens celulares tumorais avaliadas, sendo menores que aquele obtido na linhagem celular normal, indicando seletividade. Este é o primeiro relato da atividade antiproliferativa dos óleos essenciais de C. adamantium , P. ovatum e C. calophyllum contra células tumorais humanas.(AU)

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RESUMO

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.

Assuntos

RESUMO

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.(AU)

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.(AU)

RESUMO

Abstract This paper reports the in vitro antiproliferative effects, antiprotozoal, anti-herpes and antimicrobial activities of 32 organic extracts of 14 marine sponges and 14 corals collected in northeast Brazilian coast. The ethanolic extracts of the sponges Amphimedon compressa and Tedania ignis, and the acetone extract of Dysidea sp. showed relevant results concerning the antiproliferative effects against A549, HCT-8, and PC-3 cell lines by sulforhodamine B assay, but also low specificity. Concerning the antiprotozoal screening, the ethanolic extract of Amphimedon compressa and the acetone and ethanolic extracts of Dysidea sp. were the most active against Leishmania amazonensis and Trypanosoma cruzi expressing -galactosidase in THP-1 cells. In the preliminary anti-HSV-1 (KOS strain) screening, the ethanolic extracts of the sponges Amphimedon compressa, Haliclona sp. and Chondrosia collectrix inhibited viral replication by more than 50%. The most promising anti-herpes results were observed for the ethanolic extract of Haliclona sp. showing high selective indices against HSV-1, KOS and 29R strains (SI> 50 and >79, respectively), and HSV-2, 333 strain (IS>108). The results of the antibacterial screening indicated that only the ethanolic extract of Amphimedon compressa exhibited a weak activity against Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli by the disk diffusion method. In view of these results, the extracts of Amphimedon compressa, Tedania ignis and Dysidea sp. were selected for further studies aiming the isolation and identification of the bioactive compounds with antiproliferative and/or antiprotozoal activities. The relevant anti-herpes activity of the ethanolic extract of Haliclona sp. also deserves special attention, and will be further investigated.

Resumo Este artigo reporta as atividades in vitro antiproliferativa, atiprotozoárica, anti-herpética e antimicrobiana de 32 extratos orgânicos provenientes de 14 esponjas marinhas e 14 corais coletados no litoral nordestino brasileiro. Os extratos etanólicos das esponjas Amphimedon compressa e Tedania ignis, e o extrato acetônico de Dysidea sp. demonstraram resultados promissores em relação aos efeitos antiproliferativos frente as linhagens celulares A549, HCT-8, PC-3 pelo método da sulforrodamina B, mas sem especificidade. Em relação à atividade antiprotozárica, os extratos etanólico de Amphimedon compressa e acetônico e etanólico de Dysidea sp. apresentaram atividade contra Leishmania amazonensis e Trypanosoma cruzi através do método de expressão de -galactosidase em células THP-1. Na investigação preliminar de atividade antiviral frente ao vírus Herpes simplex tipo 1 (cepa KOS), os extratos etanólicos das esponjas Amphimedon compressa, Haliclona sp. e Chondrosia collectrix inibiram mais de 50% da replicação viral. O extrato etanólico da esponja Haliclona sp. demonstrou resultados promissores para atividade anti-herpética com altos índices de seletividade para as cepas KOS (IS >50) e 29R (IS>79) frente ao VHS-1 e cepa 333 (IS>108) frente ao VHS-2. O extrato etanólico da esponja Amphimedon compressa exibiu uma pequena atividade contra Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli pelo método de difusão em disco. De acordo com os resultados apresentados, os extratos das esponjas Amphimedon compressa, Tedania ignis e Dysidea sp. serão selecionados para futuros estudos de isolamento e identificação dos compostos bioativos para as atividades antiproliferativa e antiprozoárica. O extrato etanólico de Haliclona sp. será investigado por possuir atividade relevante anti-herpética.

RESUMO

Abstract Essential oils, which may be extracted from several parts of plants, have different biological activities. The Brazilian Cerrado has a large variety of plants that yield essential oils, even though many have not been studied yet. Taking into account the biodiversity of this biome, this study aimed at evaluating the antiproliferative activity of essential oils extracted from three species of plants of the Cerrado in Goiás state: Campomanesia adamantium (Cambess.) O. Berg, Protium ovatum (Engl. in Mart.) and Cardiopetalum calophyllum (Schltdl.). Essential oils were extracted from both C. adamantium and C. calophyllum leaves and from P. ovatum leaves and green fruits by hydrodistillation carried out by a Clevenger-type apparatus. The chemical composition of the essential oils was determined by Gas Chromatography coupled to Mass Spectrometry (GC-MS). The following major chemical constituents were identified in the essential oils under investigation: -myrcene (62.00%), spathulenol (28.78%), germacrene-B (18.27%), -caryophyllene oxide (16.40%), -caryophyllene (14.00%), -pinene (11.30%), viridiflorol (9.99%), limonene (7.30%) and (Z,E)-pharnesol (6.51%). The antiproliferative activity was evaluated in different human tumor cell lines: breast adenocarcinoma (MCF-7), cervical adenocarcinoma (HeLa) and glioblastoma (M059J). A normal human cell line was included (GM07492A, lung fibroblasts). Results showed that essential oils from C. adamantium leaves got the lowest values of IC50 in all strains of tumor cells under evaluation. They were significantly lower than the ones of the normal cell line, an evidence of selectivity. It is worth mentioning that this is the first report of the antiproliferative activity of essential oils from C. adamantium , P. ovatum and C. calophyllum against human tumor cells.

Resumo Os óleos essenciais podem ser extraídos de várias partes das plantas e apresentam diversas atividades biológicas. O Cerrado brasileiro possui uma grande variedade de plantas produtoras de óleos essenciais muitas delas ainda não estudadas. Levando-se em consideração a biodiversidade desse bioma, o objetivo deste trabalho foi avaliar a atividade antiproliferativa dos óleos essenciais extraídos de três espécies de plantas ocorrentes no Cerrado do estado de Goiás: Campomanesia adamantium (Cambess.) O. Berg, Protium ovatum (Engl. in Mart.) e Cardiopetalum calophyllum (Schltdl.). Os óleos essenciais foram obtidos das folhas de C. adamantium e C. calophyllum e das folhas e frutos verdes de P. ovatum por hidrodestilação, usando o aparelho do tipo Clevenger. A composição química dos óleos essenciais foi determinada pelo método de Cromatografia Gasosa acoplada à Espectrometria de Massas (CG-EM). Os constituintes químicos majoritários identificados nos óleos essenciais estudados foram: -mirceno (62,00%), espatulenol (28,78%), germacreno-B (18,27%), óxido de -cariofileno (16,40%), -cariofileno (14,00%), -pineno (11,30%), viridiflorol (9,99%), limoneno (7,30%) e (Z,E)-farnesol (6,51%). A atividade antiproliferativa foi avaliada em diferentes linhagens de células tumorais humanas: adenocarcinoma de mama (MCF-7), adenocarcinoma cervical (HeLa) e gliobastoma (M059J), além de, uma linhagem celular humana normal (GM07492A, fibroblastos pulmonares). O óleo essencial das folhas de C. adamantium exibiu menores valores de CI50 em todas as linhagens celulares tumorais avaliadas, sendo menores que aquele obtido na linhagem celular normal, indicando seletividade. Este é o primeiro relato da atividade antiproliferativa dos óleos essenciais de C. adamantium , P. ovatum e C. calophyllum contra células tumorais humanas.