ABSTRACT
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.
Subject(s)
Humans , Soil Microbiology , Bacillus/physiology , Colorectal Neoplasms/drug therapy , Cell Proliferation/drug effects , Phenotype , Bacillus/isolation & purification , Bacillus/genetics , In Vitro Techniques , RNA, Ribosomal, 16S , Adenocarcinoma/drug therapy , Cell Survival/drug effects , Polymerase Chain Reaction , Cell Line, Tumor/drug effects , Genotype , Antarctic RegionsABSTRACT
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.
Subject(s)
Humans , Plants, Medicinal , Ethnobotany , Surveys and Questionnaires , MexicoABSTRACT
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.
Subject(s)
Breast Neoplasms , Bauhinia , Cell Proliferation , MCF-7 Cells , Fabaceae , Anti-Bacterial Agents , AntioxidantsABSTRACT
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.
ABSTRACT
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.
Subject(s)
Humans , Oils, Volatile , Annonaceae , Burseraceae , Myrtaceae , Calophyllum , Brazil , Plant Leaves , HydrogenABSTRACT
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.
Subject(s)
Plant Extracts/pharmacology , Chloroform , Plectranthus/chemistry , Cell Line, Tumor/drug effects , Cell Proliferation/drug effects , In Vitro Techniques , Plant Extracts/chemistry , Ethnobotany , Cuba , Diterpenes/pharmacology , Diterpenes/chemistryABSTRACT
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.
Subject(s)
Humans , Acetic Acid , Fruit , Vaccinium , Polyphenols , AnthocyaninsABSTRACT
The aim of the present study was to evaluate the antiproliferative activity of crude extracts from leaves of Bauhinia variegata and Leptadenia reticulata using fission yeast Schizosaccharomyces pombe as a model. The crude extracts of both plants were prepared by three experimental conditions (25°C, elevated temperature and ultrasound waves) and four solvent systems [Water, Methanol, Water: Methanol (1:1) and Chloroform: Methanol (1:1)]. MTT assay was performed for estimating the cell viability and the results were expressed as % growth inhibition. Overall based on the MTT assay performed on yeast cells, Water: Methanol, Methanol and Water extracts showed higher antiproliferative activity than the positive control (Paclitaxel) in a dose-dependent manner. For Bauhinia variegata and Leptadenia reticulata, methanol extract (25°C temperature & elevated temperature, respectively) exhibited highest inhibition which was approximately 80%. In conclusion, this study has indicated that Bauhinia variegata and Leptadenia reticulata extracts possess strong antiproliferative activity. Furthermore, it could act as a potential source for identifying new molecules with chemotherapeutic potential against cancer.
ABSTRACT
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.
Subject(s)
Humans , Plant Leaves , Psidium , Cell Proliferation/drug effects , Phytochemicals/pharmacology , Anti-Bacterial Agents/pharmacology , Sesquiterpenes/pharmacology , Oils, Volatile/pharmacology , Plant Extracts/pharmacology , Microbial Sensitivity Tests , Azulenes/pharmacology , Monocyclic Sesquiterpenes , Polycyclic Sesquiterpenes , Gas Chromatography-Mass SpectrometryABSTRACT
Background: The study of plant-associated microorganisms is very important in the discovery and development of bioactive compounds. Pseudomonas is a diverse genus of Gammaproteobacteria comprising more than 60 species capable of establishing themselves in many habitats, which include leaves and stems of many plants. There are reports of metabolites with diverse biological activity obtained from bacteria of this genus, and some of the metabolites have shown cytotoxic activity against cancer cell lines. Because of the high incidence of cancer, research in recent years has focused on obtaining new sources of active compounds that exhibit interesting pharmacodynamic and pharmacokinetic properties that lead to the development of new therapeutic agents. Results: A bacterial strain was isolated from tumors located in the stem of Pinus patula, and it was identified as Pseudomonas cedrina. Extracts from biomass and broth of P. cedrina were obtained with chloroform:methanol (1:1). Only biomass extracts exhibited antiproliferative activity against human tumor cell lines of cervix (HeLa), lung (A-549), and breast (HBL-100). In addition, a biomass extract from P. cedrina was fractioned by silica gel column chromatography and two diketopiperazines were isolated: cyclo-(L-Prolyl-L-Valine) and cyclo-(L-Leucyl-L-Proline). Conclusions: This is the first report on the association of P. cedrina with the stems of P. patula in Mexico and the antiproliferative activity of extracts from this species of bacteria against human solid tumor cell lines.
Subject(s)
Pseudomonas/chemistry , Pinus/microbiology , Cell Line, Tumor/drug effects , Antineoplastic Agents/pharmacology , Plants/microbiology , Symbiosis , Biomass , Gammaproteobacteria/chemistry , Cell Proliferation/drug effectsABSTRACT
Objective: To investigate the in vitro antiproliferative action of essential oil from Salvia officinalis L. (S. officinalis) grown in Sicily (Italy), and its main components on hormone-dependent cancer cell lines. Methods: S. officinalis essential oil was prepared by hydrodistillation. The actions of the S. officinalis essential oil and its three principal components ( -thujone, 1,8-cineole and camphor) were evaluated in LNCaP cells (prostate carcinoma), MCF7 cells (breast carcinoma) and HeLa cells (cervical carcinoma) at various dosages and diverse time points. Cell viability and proliferation were estimated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Results: S. officinalis essential oil at doses of 100 μg/mL and 200 μg/mL induced a significant reduction of cell viability in MCF7, LNCaP and HeLa cell lines after a 48-hour incubation. The same cell lines also showed decreased cell viability when they were treated with a mixture of three major components of the essential oil, at doses of 100 μg/mL and 200 μg/mL, after a 48-hour incubation. Conclusions: These preliminary results could shed light on the formulation of new therapeutic agents with antiproliferative activity. Thus supplementary investigations are fundamental to examine the molecular mechanisms of the anticancer effects of this species of Salvia in cancer cells and to achieve confirmation of its in vivo anticancer activity.
ABSTRACT
Abstract Plants are the main sources of natural antioxidants in the form of phenolic compounds, which help human beings to deal with oxidative stress, caused by free radical damage. For this reason, the present study was carried out to evaluate the antiproliferative, antioxidant and inhibition of oxidative DNA damage activities of n-butanol extract obtained from aerial parts of Limonium bonduelli. The antioxidant potential was determined using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and inhibition of lipid peroxidation assay. Antiproliferative activity was evaluated using xCELLigence RTCA instrument on two tumor cell lines; HT-29 (human colon adenocarcinoma) and HeLa (human cervix carcinoma). DNA damage inhibition was evaluated using photolyzing 46966 plasmid. Also, total phenolic and total flavonoid contents were determined using a spectrophotometric method. Total phenolic (343 ± 0.05 µg/mg) and flavonoid (220.5 ± 0.04 µg/mg) were indicated as gallic acid and quercetin equivalents respectively. The extract exhibited significant IC50 values in lipid peroxidation (IC50= 181.18 ± 0.65 µg/mL) and DPPH radical scavenging assays (IC50= 14.92 ± 0.032 µg/mL). The extract also partially protected 46966 plasmid DNA from free radical-mediated oxidative stress in a DNA damage inhibition assay and showed concentration-dependent antiproliferative effects. n-butanol extract of L. bonduelli is a rich source of natural antioxidants and anticancer agents.
Subject(s)
Plumbaginaceae/chemistry , Antioxidants , In Vitro Techniques/instrumentation , Oxidative StressABSTRACT
Tragia brevipes and Tetradenia riparia have been widely used in traditional medicine. T. brevipes relief stomach pain and in treatment of rheumatism while T. riparia; heal chest pains, stomach-ache, malaria and act as antioxidant. However, scanty data exist on their potential anticancer activity. The total phenolic content was determined and anti-proliferative activity of the Methanol-Dichloromethane extract from the leaves evaluated against cancerous cell lines. The total phenolic content of the plants extract was determined using an UV visual spectrophotometer at 765 nm. The 3- (4-5-dimethyl-2-thiazoly)-2, 5-diphenyltetrazolium bromide (MTT) cell proliferation bioassay was used to test for anti-proliferative activity on Hela (cervical), DU145 (prostrate) and HCC (breast) cancer cell lines and Vero (normal) cell. T. brevipes and T. riparia had a phenolic concentration of 30.44 and 20.25 µg/ml, respectively. Both plants showed anti-proliferative activity on cancer cells with the most inhibited being DU145 with an IC50 of 29.67 ± 4.60 µg/ml for T. brevipes and 11.45 ± 0.87 µg/ml for T. riparia. The standard 5 Fluorouracil had an IC50 of 5.04 ± 4.12 µg/ml on DU145. T. riparia had the highest antiproliferative activity of 65.54 ± 16.85 µg/ml on Hela cells and 62.84 ± 1.10 µg/ml on HCC. T. brevipes had an IC50 of 661.11 ± 15. 12 µg/ml on Hela cells and 703.09 ± 18.35 µg/ml on HCC. Extracts from both plants were highly selective on DU145 cancer cells with a selectivity index (SI) of 21.62 for T. brevipes and 7.88 for T. riparia. Methanol-Dichloromethane extracts from T. brevipes and T. riparia exert anti-proliferative activity, however, the active compound (s) and the mechanisms of anti-proliferative action need to be investigated further.
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Rumex nepalensis Spreng. (Polygonaceae) commonly known as Nepal Dock has wide-spectrum therapeutic potencies and is extensively used for centuries in traditional medicine systems. The leaves of this plant are edible and a rich source of natural antioxidants. They act as a possible food supplement and are largely used in pharmaceutical industry. Extracts and metabolites from this plant exhibits pharmacological activities including anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral, insecticidal, purgative, analgesic, antipyretic, anti-algal, central nervous system depressant, genotoxic, wound healing and skeletal muscle relaxant activity. Due to its remarkable biological activities, it has the potential to act as a rich source of drug against life threatening diseases. However, more studies are needed to scientifically validate the traditional uses of this plant, beside isolating and identifying their active principles and characterizing the mechanisms of action. We present herein a critical account of its botany, ecology, traditional uses, phytoconstituent profile and major pharmacological activities reported in recent years and therefore will provide a source of information on this plant for further studies.
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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.
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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: -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.
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Twelve novel 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid(CDDO) derivatives were designed and synthesized(9a-91) by introducing different heterocyclic rings to 17-COOH of CDDO through various linkers.Their structures were determined by ESI-MS,IR and 1 H NMR.The antiproliferative activity of the synthetic derivatives against human cancer cells HCT-116,A549 and HepG2 was evaluated by MTT assay.Several compounds showed potent inhibitory activities against test cell lines.Among them,compound 9c showed more potent antiproliferative activity than the CDDO-imidazolide (CDDO-Im).Moreover,rat plasma stability assay showed that compound 9c was more stable than CDDO-Im.
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A series of 5H-benzo[b] carbazole derivatives were synthesized to find new TopⅡ inhibitors.The substitution pattern at C-9 was discussed.All 16 compounds were tested for their antiproliferative activities against 4 tumor cell lines (SMMC-7721,S1,HCT116,and HeLa) by sulforhodamine B assay.Four compounds were found to inhibit the proliferation of all tested cell lines.And compound 10e displayed the best antiproliferative activity against all 4 tested cell lines with IC50 values of 5.06,4.50,5.29,and 6.32 μmol/L,respectively.
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El Agraz (Vaccinium meridionale Swartz), es una baya que posee alta capacidad antioxidante debido a su contenido de compuestos polifenólicos como antocianinas, ácidos fenólicos y flavonoides. El objetivo de este estudio fue evaluar la composición proximal inicial y el efecto en las características fisicoquímicas (pH, °Brix, acidez titulable (AT)), actividad antioxidante y antiproliferativa de néctares elaborados a partir de agraz liofilizado, almacenados du- rante 42 días. Se prepararon dos néctares: NA (sacarosa) y NB (aspartame), se evaluó cambio en pH, °Brix y AT cada7días durante el almacenamiento. Se determinó contenido de fenoles y antocianinas totales mediante Folin-Ciocalteau y método diferencial de pH, respectivamente, actividad antioxidante mediante FRAP y ORAC. Se analizó la actividad antiproliferativa con sulforodamina B en células SW480 (adenocarcinoma de colon). Los resultados mostraron que ambos néctares presentaron estabilidad en °Brix, pH yAT y el NB presentó menor aporte calórico. El contenido de fenoles totales aumentó durante el almacenamiento. El contenido de antocianinas y capacidad antioxidante se redujo significativamente (p<0,05). NA presentó mejor actividad antiproliferativa a las 72h, con un porcentaje de inhibición del crecimiento celular a una concentración de 1g/mL de 63,50% (IC50=0,6g/mL). Se puede concluir que NA presentó mayor capacidad antiproliferativa y NB mejor actividad antioxidante, que aunque disminuyó significativamente durante el almacenamiento, continuó siendo alta comparada con estudios reportados en la literatura. Para productos realizados a partir de bayas del género Vaccinium. Se requieren estudios adicionales in vivo que permitan comprobar su eficacia quimiopreventiva y dilucidar mecanismos moleculares de acción para beneficio de la salud humana, demostrando su potencial funcional descrito hasta ahora in vitro(AU)
Effect of storage time on the physicochemical characteristics, antioxidant and antiproliferative nectar of unripe (Vaccinium meridionale Swartz). Agraz (Vaccinium meridionale Swartz) is a berry that has high antioxidant capacity due to its content of polyphenolic compounds as anthocyanins, phenolic acids and flavonoids. The aim of this study was to evaluate the initial proximal composition and the effect on the physicochemical characteristics (pH, ° Brix, titratable and acidity (TA), antioxidant and antiproliferative activity of nectars made from unripe lyophilized and stored for 42 days. Two nectars were prepared: NA (sucrose) and NB (aspartame), was evaluated change in pH, °Brix and AT every 7 days during storage. It was determined and total phenols content by Folin-Ciocalteu anthocyanins and pH differential method, respectively, antioxidant activity by FRAP and ORAC. Antiproliferative activity with sulforhodamine B in SW480 cells (colon adenocarcinoma) were analyzed. The results showed that both were stable nectars ° Brix, pH and changes in AT. The NB has lower calories. The content of total phenols increased during storage. The anthocyanin content and antioxidant capacity was significantly reduced (p <0.05). NA presented better antiproliferative activity at 72 h, with a percentage of inhibition of cell growth at a concentration of 1g / ml of 63.50% (IC50 = 0.6 g/mL). It can be concluded that NA had a higher antiproliferative capacity and NB better antioxidant activity than even decreased significantly during storage, remained high com- pared to studies reported in the literature. Further studies "in vivo" to verify their chemopreventive efficacy and elu- cidate molecular mechanisms of action for the benefit of human health, showing their functional potential described so far "in vitro" are required(AU)
Subject(s)
Humans , Male , Female , Vaccinium , Plant Nectar/analysis , Polyphenols , Antioxidants , Food Storage , Diet, Food, and Nutrition , Nutritive ValueABSTRACT
Dietary components present in foods, spices and herbs are source of natural compounds viz. phenols, flavonoids, tocopherols, ascorbic acid and carotenoids with potential benefits. Ginger is one such herb commonly used throughout the world as a spice for dietary as well as medicinal purpose since ancient period. Here, we investigated the methanolic extract of Zingiber officinale rhizome (ZOME) for anticancer activity against human cervical cancer HeLa cells and breast cancer MDA-MB-231 cells and antioxidant activity using 1,1-diphenyl-2-picryl hydroxyl (DPPH) scavenging assay, 2,2'-azinobis-3-ethylbenzothiozoline-6-sulfonic acid (ABTS) cation decolorization test. Antiproliferative activity was substantiated by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT) and colony formation assay for cell viability and cell proliferation, Hoechst staining was performed to examine apoptosis. Our results demonstrated that ZOME inhibited the proliferation and colony formation in HeLa and MDA-MB-231 cells, in a dose- and time-dependent manner and induced typical changes in nuclear morphology, chromatin condensation and fragmentation, membrane shrinkage and blebbing in both cells indicated apoptotic property of Z. officinale. ZOME exhibited potent antiradical activity against DPPH and ABTS. On the basis of the results of the present study, it may be suggested that Z. officinale has promising anticancer and antioxidant properties. Since, Z officinale has been commonly used throughout the world as a spice for dietary as well as for medicinal purposes since prehistoric times. Therefore, enriched use of Z. officinale as dietary material could be recommended in ethno-medicine for the management of cervical and breast cancers. Moreover, further studies are needed to isolate and characterize the potent compounds for further adjuvant therapy against such malignancies.