Phytochemical profile and biological activities of Bromelia antiacantha extracts / Perfil fitoquímico e atividades biológicas de extratos de Bromelia antiacantha

Reports from popular medicine usually act as a basis for the development of new drugs from natural compounds with therapeutic actions for serious diseases and prevalence such as cancer. Bromelia antiacantha Bertol. is a species of the Bromeliaceae family, considered an unconventional food plant, found in the south and midwest regions of Brazil. Despite the high nutritional content and pharmacological potential of its fruits, few scientific studies report its biological actions. Thus, this study evaluates the phytochemical profile of aqueous and ethanol extracts obtained from B. antiacantha fruits, as well as their possible antioxidant, antitumor, and cytotoxic activities. The aqueous extract exhibited phenolic compounds and flavonoids, while ethanol extracts indicated the presence of flavonoids and coumarin in their composition, regardless of the region of collection. The ethanolic extract demonstrated a more promising antioxidant effect than the aqueous extract and also induced a significant inhibition in the viability of human cervical cancer cells of the SiHa strain. In addition, treatment with both extracts did not alter the viability of non-tumor cells of the immortalized human keratinocyte lineage (HaCaT). These results bring new data about extracts obtained from a native plant, edible and traditionally used in popular medicine, opening new perspectives for its possible therapeutic application.

Relatos da medicina popular costumam atuar como referencial para o desenvolvimento de novos fármacos a partir de moléculas naturais com ações terapêuticas para doenças de alta gravidade e prevalência como o câncer. Bromelia antiacantha Bertol. é uma espécie da família Bromeliaceae, considerada uma planta alimentícia não convencional (PANC), encontrada nas regiões sul e centro-oeste do Brasil. Apesar do alto teor nutritivo e potencial farmacológico de seus frutos, poucos estudos científicos relatam suas ações biológicas. Desta forma, este estudo avalia o perfil fitoquímico de extratos aquoso e etanólico obtidos de frutos de B. antiacantha, bem como a sua possível ação antioxidante, antitumoral e citotóxica. O extrato aquoso apresentou compostos fenólicos e flavonoides, enquanto os extratos etanólicos apontam a presença de flavonóides e cumarina em sua composição, independente da região de coleta. O extrato etanólico demonstrou efeito antioxidante mais promissor do que o extrato aquoso e também induziu uma inibição significativa na viabilidade de células humanas de câncer cervical da linhagem SiHa. Além disso, o tratamento com ambos extratos não alterou a viabilidade de células não tumorais da linhagem de queratinócitos humanos imortalizados (HaCaT). Estes dados trazem novas informações sobre extratos obtidos de uma espécie vegetal nativa, comestível e já utilizada tradicionalmente, mas abrindo novas perspectivas quanto a possíveis aplicações terapêuticas.

Analysis of the toxicological and pharmacokinetic profile of Kaempferol-3-O-ß-D-(6"-E-p-coumaryl) glucopyranoside - Tiliroside: in silico, in vitro and ex vivo assay / Análise do perfil toxicológico e farmacocinético de Kaempferol-3-O-ß-D- (6 "-E-p-cumaril) glucopiranosídeo - Tilirosídeo: ensaio in silico, in vitro e ex vivo

Abstract Tiliroside is a glycosidic flavonoid present in many plants species including Helicteres velutina K. Schum (Malvaceae sensu lato), commonly known in Brazil as "pitó". This molecule has been shown to have many biological activities, however no study has been carried out to investigate the toxicity of this substance. The present work aimed to evaluate the possible cellular toxicity in silico, in vitro and ex-vivo of the kaempferol-3-O-β-D-(6"-E-p-coumaroyl) glucopyranoside (tiliroside), through chemical structure analysis, toxicity assessment and predictive bioactive properties, using human samples for in vitro and ex-vivo tests. The in silico analysis suggests that tiliroside exhibited great absorption index when penetrating biological membranes. In addition, it also displayed considerable potential for cellular protection against free radicals, and anticarcinogenic, antioxidant, antineoplastic, anti-inflammatory, anti-hemorrhagic and antithrombotic activities. The assessment of the hemolytic and genotoxic effects of tiliroside showed low hemolysis rates in red blood cells and absence of cellular toxicity in the oral mucosa cells. The data obtained indicate that this molecule could be a promising therapeutic approach as a possible new drug with biotechnological potential.

Resumo O tilirosídeo é um flavonóide glicosídico presente em muitas espécies de plantas, incluindo Helicteres velutina K. Schum (Malvaceae sensu lato), conhecida no Brasil como "pitó". Esta molécula mostrou ter muitas atividades biológicas, porém nenhum estudo foi realizado para investigar a toxicidade dessa substância. O presente trabalho teve como objetivo avaliar a possível toxicidade celular in silico, in vitro e ex-vivo do kaempferol-3-O-β-D- (6 "-Ep-coumaroil) glucopiranosídeo (tilirosídeo), por meio de análises de estrutura química, toxicidade avaliação e propriedades bioativas preditivas, utilizando amostras humanas para testes in vitro e ex-vivo. A análise in silico sugere que o tilirosídeo exibe bom índice de absorção para penetrar nas membranas biológicas. Além disso, apresentou considerável potencial de proteção celular contra os radicais livres e com atividades anticarcinogênica, antioxidante, antineoplásica, antiinflamatória, anti-hemorrágica e antitrombótica. A avaliação dos efeitos hemolíticos e genotóxicos do tilirosídeo mostrou baixas taxas de hemólise nas hemácias e ausência de toxicidade em células da mucosa oral. Os dados obtidos indicam que esta molécula pode possuir uma abordagem terapêutica promissora como uma possível nova droga com potencial biotecnológico.

Otimização de método extrativo para raízes de Arctium lappa L / Extractive method optimization for Arctium lappa l. Roots / Optimización de un método de extracción de raíces de Arctium lappa L

Arctium lappa L. é indicada no Formulário de Fitoterápicos da Farmacopeia Brasileira para o tratamento de distúrbios urinários leves. Estudos já demonstraram o potencial antioxidante, anti-inflamatório e antidiabético deste extrato, onde foram identificados fenóis, lignanas, taninos e flavonoides. O objetivo deste trabalho foi otimizar o método extrativo de raízes de A. lappa. Realizou-se o preparo de extratos por diferentes métodos: Ultrassom, Soxhlet, maceração e turbo extração. A otimização foi realizada por turbo extração seguindo um planejamento fatorial 23, empregando como fatores: teor alcoólico, concentração da matéria prima e tempo de extração. Os extratos foram avaliados quanto ao resíduo seco, teores de fenóis e flavonoides, e atividade antioxidante. Com relação ao resíduo seco, e aos teores de fenóis e flavonoides, os métodos de ultrassom e turbo extração demonstraram melhor poder extrativo. Devido ao menor tempo e custo operacional, a otimização foi realizada por turbo extração, e o extrato otimizado foi obtido utilizando álcool 60%, em proporção matéria prima solvente 1:10 e tempo de extração de 15 minutos. Estas análises poderão nortear futuros testes de transposição de método para escala industrial, diminuindo mão de obra, tempo e custos, visando obter produtos fitoterápicos mais eficientes, com valor acessível à população.

Arctium lappa L. is indicated in the Brazilian Pharmacopeia Herbal Medicines Form for the treatment of mild urinary disorders. Studies have already demonstrated the antioxidant, anti-inflammatory and antidiabetic potential of this extract, where phenols, lignans, tannins and flavonoids were identified. The objective of this work was to optimize the extractive method of A. lappa roots. Extracts were prepared by different methods: Ultrasound, Soxhlet, maceration and vortical extraction. The optimization was performed by vortical extraction following a 23 full factorial design, using as factors: alcohol content, drug concentration and extraction time. The extracts were evaluated for dry residue, phenols and flavonoids contents, and antioxidant activity. Regarding the dry residue, and the phenols and flavonoids contents, the ultrasound and vortical extraction methods showed better extractive power. Due to the lower operating time and cost, the optimization was performed by vortical extraction, and the optimized extract was obtained using 60% alcohol, in a 1:10 drug solvent ratio and extraction time of 15 minutes. These assessments guide the future tests of transposition of the method to an industrial scale, reducing manpower, time and costs, aiming to obtain more efficient phytotherapic products, with affordable value for the population.

Arctium lappa L. está indicado en la Formulacao de Fitoterápicos da Farmacopeia Brasileira para el tratamiento de trastornos urinarios leves. Los estudios han demostrado el potencial antioxidante, antiinflamatorio y antidiabético de este extracto, donde se identificaron fenoles, lignanos, taninos y flavonoides. El objetivo de este trabajo fue optimizar el método extractivo de las raíces de A. lappa. Los extractos se prepararon por diferentes métodos: Ultrasonido, Soxhlet, maceración y turboextracción. La optimización se realizó mediante turboextracción siguiendo una planificación factorial de 23, empleando como factores: tenor alcohólico, concentración de materia prima y tiempo de extracción. Se evaluaron los extractos para determinar el residuo seco, el contenido de fenoles y flavonoides y la actividad antioxidante. En cuanto al contenido de residuo seco, fenoles y flavonoides, los métodos de extracción por ultrasonidos y turbo demostraron un mejor poder de extracción. Debido al menor tiempo y coste operativo, la optimización se realizó mediante turboextracción, y el extracto optimizado se obtuvo utilizando alcohol 60%, en proporción disolvente-materia 1:10 y tiempo de extracción de 15 minutos. Estos análisis podrán orientar futuros ensayos de transposición del método para escala industrial, reduciendo mano de obra, tiempo y costes, con el objetivo de obtener productos fitoterapéuticos más eficientes, con valor accesible para la población.

Estudo do potencial antiviral sobre Sars Cov-2 dos compostos identificados nas folhas do extrato bruto de Eugenia pyriformis / Study of the antiviral potential on Sars Cov-2 of compounds identified in the leaves of the gross extract of Eugenia pyriformis / Estudio del potencial antiviral sobre Sars Cov-2 de los compuestos identificados en las hojas del extracto crudo de Eugenia pyriformis

Eugenia pyriformis Cambess (Myrtaceae), conhecida popularmente como uvaia. Em seus frutos são encontrados compostos fenólicos com ação antioxidante e nas folhas foram detectados altos teores de flavonoides e taninos hidrolisados que se mostraram inibidor da protease de 2019 - nCoV e SARS-CoV. Neste sentido, o objetivo deste estudo foi a obtenção do extrato bruto das folhas, a análise da composição química e a possibilidade da ação antiviral frente ao SARS COV-2. O extrato bruto (EB) foi obtido a partir das folhas secas de E. pyriformis, pela técnica de maceração dinâmica com esgotamento do solvente (etanol 90º GL) e concentrado em evaporador rotativo. Seis gramas do EB foram fracionados em cromatografia em coluna, e eluído com hexano, diclorometano, acetato de etila e metanol, as frações foram concentradas em um evaporador rotativo (Tecnal TE-210). O EB e as frações foram identificadas por cromatografia líquida de alta eficiência à espectrometria de massas de alta resolução (CLAE-ESI/qTOF). A identificação química do extrato bruto e frações das folhas de E. pyriformis evidenciou a presença de compostos fenólicos destacando os ácidos fenólicos, flavonoides e taninos. De forma complementar, foi realizado um levantamento bibliográfico sobre a provável ação antiviral dos compostos fenólicos e taninos presentes nas folhas de uvaia. Os resultados evidenciaram que os flavonoides quercetina e kaempferol possuem ação antiviral quando se ligam a glicoproteína do envelope ou capsídeo viral interferindo na ligação e penetração do vírus na célula. Este resultado coloca as folhas de E. pyriformis na lista de plantas com ação antiviral.

Eugenia pyriformis Cambess (Myrtaceae), popularly known as uvaia. In its fruits, phenolic compounds with antioxidant action are found and in the leaves, high levels of flavonoids and hydrolyzed tannins were detected, which proved to be an inhibitor of the 2019 protease - nCoV and SARS-CoV. In this sense, the objective of this study was to obtain the crude extract of the leaves, the analysis of the chemical composition and the possibility of antiviral action against SARS COV-2. The crude extract (EB) was obtained from the dried leaves of E. pyriformis, by the dynamic maceration technique with solvent exhaustion (ethanol 90º GL) and concentrated in a rotary evaporator. Six grams of EB were fractionated in column chromatography, and eluted with hexane, dichloromethane, ethyl acetate and methanol, the fractions were concentrated on a rotary evaporator (Tecnal TE-210). EB and fractions were identified by high performance liquid chromatography using high resolution mass spectrometry (HPLC-ESI/qTOF). The chemical identification of the crude extract and fractions of E. pyriformis leaves evidenced the presence of phenolic compounds, highlighting phenolic acids, flavonoids and tannins. In addition, a bibliographic survey was carried out on the probable antiviral action of phenolic compounds and tannins present in uvaia leaves. The results showed that the flavonoids quercetin and kaempferol have antiviral action when they bind to the envelope glycoprotein or viral capsid, interfering with the binding and penetration of the virus into the cell. This result places E. pyriformis leaves in the list of plants with antiviral action.

Eugenia pyriformis Cambess (Myrtaceae), conocida popularmente como uvaia. En sus frutos se encuentran compuestos fenólicos con acción antioxidante y en las hojas se detectaron altos contenidos de flavonoides y taninos hidrolizados que demostraron inhibir la proteasa de 2019 - nCoV y SARS-CoV. En este sentido, el objetivo de este estudio fue obtener el extracto crudo de las hojas, el análisis de la composición química y la posibilidad de acción antiviral contra el SARS COV-2. El extracto crudo (EB) se obtuvo a partir de las hojas secas de E. pyriformis, mediante la técnica de maceración dinámica con agotamiento del disolvente (etanol 90º GL) y se concentró en evaporador rotatorio. Seis gramos de EB se fraccionaron en cromatografía en columna, y se eluyeron con hexano, diclorometano, acetato de etilo y metanol, las fracciones se concentraron en un evaporador rotatorio (Tecnal TE-210). El EB y las fracciones se identificaron mediante cromatografía líquida de alta resolución a espectrometría de masas de alta resolución (HPLC-ESI/qTOF). La identificación química del extracto crudo y de las fracciones de las hojas de E. pyriformis mostró la presencia de compuestos fenólicos destacando los ácidos fenólicos, los flavonoides y los taninos. De forma complementaria, se realizó un estudio bibliográfico sobre la probable acción antiviral de los compuestos fenólicos y los taninos presentes en las hojas de la uva. Los resultados mostraron que los flavonoides quercetina y kaempferol tienen acción antiviral cuando se unen a la glicoproteína de la envoltura o cápside viral, interfiriendo en la unión y penetración del virus en la célula. Este resultado sitúa a las hojas de E. pyriformis en la lista de plantas con acción antiviral.

Evaluation of antioxidant activity, phenolic content, anthocyanins, and flavonoids of fresh and dried 'Biloxi' blueberries / Evaluación de la actividad antioxidante, contenido fenólico, antocianinas y flavonoides de arándanos 'Biloxi' frescos y secos

BACKGROUND: The phytochemical content present in blueberries has generated great interest, especially in the nutra-pharmaceutical industry, where it is known as the "super fruit" due to its prevention and treatment of neurodegenerative diseases (cardiovascular diseases, diabetes, and cancer, among others). OBJECTIVES: This study evaluated the functional potential of fresh blueberries and dried blueberries using forced convection by measuring phytochemical content to conclude if this drying technology is convenient for prolonging the product's shelf life. METHODS: For this purpose, antioxidant activity, phenolic content, total anthocyanins, and total flavonoids of 'Biloxi' blueberry cultivars were determined. Fresh and dried blueberries' results were studied. Fruit extracts were analyzed to determine antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH) as a free radical, total phenolic content with Folin-Ciocalteu reagent, total anthocyanins by pH differential method, and total flavonoids by Aluminum Chloride method. RESULTS: Results for fresh blueberries yielded ranges of antioxidant activity (90.8-93.9% Free radical scavenging rate), total phenolic content (275 to 645mgGAE/100gFW), total anthocyanins content (28.55 to 43.75mgCy3G/100gFW) and total flavonoids content (159.92 to 335.75mgQE/100gFW). For the forced convection oven process, ranges of antioxidant activity (85.5-92.6% Free radical scavenging rate), total phenolic content (261 to 308mgGAE/100gFW), total anthocyanins content (4.74 to 5.12mgCy3G/100gFW) and total flavonoids content (30.66±0.38mgQE/100gFW) were obtained. CONCLUSIONS: In general, blueberries studied proved to have similar concentrations of functional properties compared to a wide variety of cultivars grown around the globe. Furthermore, higher concentrations of phytochemical content than those reported previously for strawberries, blackberries, and raspberries were evidenced. Although dried blueberries studied proved to have diminished phytochemical content, this functional component content stands out among the fruits market and give nutritional value to end consumers. Drying processes could potentially increase the commerce of blueberries by significantly reducing their perishable nature

CONTEXTO: El contenido fitoquímico presente en los arándanos ha generado gran interés, especialmente en la industria nutra-farmacéutica donde es conocido como una "super fruta" debido a su ayuda en la prevención y tratamiento de enfermedades neurodegenerativas, enfermedades cardiovasculares, diabetes, cáncer, entre otras. OBJETIVOS: Este estudio evaluó el potencial funcional de arándanos frescos y deshidratados por convección forzada mediante la determinación de su contenido fitoquímico con el objetivo de concluir si esta tecnología de secado es conveniente para aumentar la vida útil del producto. MÉTODOS: Para este propósito, se determinó la actividad antioxidante, el contenido fenólico, las antocianinas totales y los flavonoides totales de cultivos de arándanos 'Biloxi' La información recopilada de la literatura fue analizada. Se estudió el contenido en compuestos funcionales en arándanos frescos y deshidratados. Los extractos de fruta fueron analizados para determinar actividad antioxidante por medio de 2,2-Difenil-1-Picrilhidrazilo (DPPH) como radical libre, fenólicos totales con el reactivo Folin-Ciocalteu, antocianinas totales usando el método diferencial de pH y flavonoides totales con el método de Cloruro de Aluminio. RESULTADOS: Para los arándanos frescos se obtuvieron rangos de actividad antioxidante de 90.8-93.9% Tasa de captación de radicales libres, contenido fenólico total de 275-645mgEAG/100gPF, contenido de antocianinas totales de 28.55-43.75mgCy3G/100gPF y contenido total de flavonoides de 159.92-335.75mgEQ/100gPF. Para los arándanos deshidratados por convección forzada, se obtuvieron rangos de actividad antioxidante de 85.5-92.6% Tasa de captación de radicales libres, contenido fenólico total de 261-308mgEAG/100gPF, contenido de antocianinas totales de 4.74-5.12mgCy3G/100gPF y contenido total de flavonoides de 30.24-30.96mgEQ/100gPF. CONCLUSIONES: En general, los arándanos estudiados probaron tener concentraciones similares de propiedades funcionales comparados con una amplia variedad de cultivos alrededor del mundo. Además, fueron evidenciadas concentraciones más altas de contenido fitoquímico comparadas con las reportadas previamente para fresas, moras y frambuesas. Aunque los arándanos secos estudiados demostraron tener menor contenido fitoquímico, la cantidad de estos componentes funcionales destaca dentro del mercado de las frutas y dan valor nutricional a los consumidores. Los procesos de secado pueden potencialmente incrementar el comercio de arándanos derivado de una disminución significativa en su naturaleza perecedera

Estudio fitoquímico de Argyrochosma Nivea (poir) Windham (cuti cuti) / Phytochemical study of argyrochosma nivea (poir.) windham (poir.) desv. (cuti cuti)

Nuestro país presenta un gran potencial de plantas medicinales en todo su territorio, por ser megadiverso, con muchas regiones agroecologicas y formaciones vegetales, pese a ello es incipiente la atención al desarrollo de las cadenas de valor del potencial de plantas medicinales, constituyendo un desafío el registro adecuado, con calidad y seguridad porque previenen y solucionan dificultades de salud por sus principios activos. Argyrochosma nivea (Poir.) Windham, "cuti cuti" conocido también como Notholaena nivea. Objetivos: Determinar los grupos metabólicos del extracto alcohólico al 20% de Argyrochosma nivea (Poir.) Windham, administrado a pacientes de diabetes del programa de medicina complementaria, EsSALUD Huancayo. Materiales y métodos: Estudios descriptivo, comparativo. La recolección de información relevante de aspectos botánicos, etnobotánicos, etnofarmacológicos y fitoquímicos sobre Argyrochosma nivea se realizó mediante la búsqueda en las bases de datos Scopus, ScienceDirect, PubMed y la biblioteca virtual del CONCYTEC (servicio de esa institución que reúne revistas de SciELO-Perú y la producción científica y tecnológica del Perú); además, se utilizó el buscador Google-Académico con el fin de agotar la búsqueda. Los términos de búsqueda fueron "Argyrochosma nivea", "Notholaena nivea" o "cuti cuti". Resultados: La Tintura de Argyrochosma nivea al 20% preparado con alcohol etílico al 50% en el analisis fitoquimico realizado se encontro compuestos de Flavanoides totales 0.111 mg de Catequina/ml, Flavonoides totales 0.133 mg de Quercitina /ml, Polifenoles totales 5.189 mg de ácido gálico/ml, Capacidad Antioxidante* 424.701 µ mol trolox/ml, Rutina 0.00579 mg de Rutina/ml, Quercitina 0.105mg/ml y Cumarinas 0.170 mg /ml. Ausencia de antocianinas totales, estos valores aportan la capacidad antioxidante de "cuti cuti", y el contenido de flavonoides (quercetina), permite la prevalencia en el tratamiento de la diabetes. Conclusión: El Estudio fitoquimico de Argyrochosma nivea (Poir.) Windham (Cuti cuti) mediante el análisis por espectrofotometría y análisis por HPLC verifico la existencia de 7 compuestos Flavanoides totales 0.111 mg de Catequina/ml, Flavonoides totales 0.133 mg de Quercitina /ml, Polifenoles totales 5.189 mg de ácido gálico/ml, Capacidad Antioxidante* 424.701 µ mol trolox/ml, Rutina 0.00579 mg de Rutina/ml, Quercitina 0.105mg de Qu ercitina/ml y Cumarinas 0.170 mg de Cumarina/ml(AU)

Our country has a great potential for medicinal plants throughout its territory, as it is megadiverse, with many agroecological regions and plant formations, despite this, attention to the development of value chains for the potential of medicinal plants is incipient, constituting a I challenge the proper registration, with quality and safety because they prevent and solve health difficulties due to their active ingredients. Argyrochosma nivea (Poir.) Windham, "cuti cuti" also known as Notholaena nivea. Objectives: To determine the metabolic groups of the 20% alcoholic extract of Argyrochosma nivea (Poir.) Windham, administered to diabetes patients of the complementary medicine program, EsSALUD Huancayo. Methods: Descriptive, comparative studies. The collection of relevant information on botanical, ethnobotanical, ethnopharmacological and phytochemical aspects of Argyrochosma nivea was carried out by searching the Scopus, ScienceDirect, PubMed databases and the virtual library of CONCYTEC (a service of that institution that brings together SciELO-Peru journals). and the scientific and technological production of Peru); In addition, the Google-Academic search engine was used in order to exhaust the search. The search terms were "Argyrochosma nivea", "Notholaena nivea" or "cuti cuti". Results: The Argyrochosma nivea tincture at 20% prepared with 50% ethyl alcohol in the phytochemical analysis carried out found compounds of total Flavanoids 0.111 mg of Catechin / ml, total Flavonoids 0.133 mg of Quercetin / ml, total Polyphenols 5.189 mg of acid gallic/ml, Antioxidant Capacity* 424.701 µmol trolox/ml, Rutin 0.00579 mg Rutin/ml, Quercetin 0.105mg/ml and Coumarins 0.170 mg/ml. Absence of total anthocyanins, these values provide the antioxidant capacity of "cuti cuti", and the content of flavonoids (quercetin), allows prevalence in the treatment of diabetes. Conclusion: The phytochemical study of Argyrochosma nivea (Poir.) Windham (Cuti cuti) through spectrophotometric analysis and HPLC analysis verified the existence of 7 total Flavanoid compounds 0.111 mg of Catechin/ml, total Flavonoids 0.133 mg of Quercetin /ml, Total polyphenols 5.189 mg of gallic acid/ml, Antioxidant Capacity* 424.701 µ mol trolox/ml, Rutin 0.00579 mg of Rutin/ml, Quercetin 0.105mg of Quercetin/ml and Coumarins 0.170 mg of Coumarin/ml(AU)

Cápsulas de polvo de arándano como propuesta nutracéutica para mejorar la bioaccesibilidad de compuestos fenólicos / Blueberry Powder capsules as a nutraceutical proposal to improve bioaccessibility of phenolic compounds. Introduction

El arándano (Vaccinium corymbosum L.) posee un alto contenido de compuestos fenólicos los cuales han sido estudiados principalmente por su actividad antioxidante, antiobesogénica, antiinflamatoria, entre otras. Objetivo. Evaluar el efecto de la digestión gastrointestinal in vitro sobre la bioaccesibilidad de compuestos fenólicos y actividad antioxidante de una formulación nutracéutica de arándano (cápsula), comparado con arándano fresco y polvo. Materiales y métodos. Se obtuvieron extractos metanólicos de muestras de arándano fresco y liofilizado y se determinó su contenido de fenoles, flavonoides y antocianinas totales, así como también actividad antioxidante. Se llevó a cabo un ensayo de simulación de digestión gastrointestinal para evaluar la bioaccesibilidad de los compuestos fenólicos presentes en las muestras. Resultados. Los resultados mostraron que la digestión gástrica de arándano en polvo y en cápsula promovió una mayor bioaccesibilidad de fenoles (42% y 40%), flavonoides (52% y 33%) y antocianinas (45% y 40%) comparado con digestos de arándano fresco. Posterior a la digestión intestinal, la bioaccesibilidad de fenoles (63%) y flavonoides (67%) fue mayor en la cápsula de arándano comparada con su contraparte arándano en polvo. Las condiciones de digestión intestinal afectaron negativamente la bioaccesibilidad de las antocianinas independientemente del tipo de muestra evaluada. Conclusión. Las condiciones de digestión gástrica promueven una mayor estabilidad de los compuestos fenólicos en arándano en polvo y en cápsula lo que pudiera ser relevante para el mantenimiento de un ambiente antioxidante a este nivel. Las condiciones de digestión intestinal afectaron de manera particular a los compuestos fenólicos de arándano fresco y polvo, pero no a la cápsula, lo que puede sugerir que el encapsulamiento protegió de las condiciones alcalinas a los fenoles presentes. Se sugieren estudios posteriores sobre absorción in vitro de los componentes remanentes en intestino y sus posibles efectos sobre biomarcadores de estrés oxidativo en modelos in vivo(AU)

Blueberry (Vaccinium corymbosum L.) has a high content of phenolic compounds which have been studied mainly for their antioxidant, antiobesogenic, anti-inflammatory activity, among others. Objetive. The objective of the present study was to evaluate the effect of in vitro gastrointestinal digestion on the bioaccessibility of phenolic compounds and antioxidant activity of a nutraceutical formulation of blueberry (capsule), compared to fresh and powder blueberry. Materials and methods. Methanolic extracts of fresh and lyophilized blueberry were obtained and determined its total phenols, flavonoids, anthocyanins content, as well as antioxidant activity. A gastrointestinal digestion simulation test also was carried out to assess the bioaccessibility of the phenolic compounds found in samples. Results. The results showed that gastric digestion of powder and capsule blueberry promoted greater bioaccessibility of phenols (42% and 40%), flavonoids (52% and 33%) and anthocyanins (45% and 40%), compared to fresh blueberry digests. After intestinal digestion, the bioaccessibility of phenols (63%) and flavonoids (67%) was higher in the blueberry capsule compared to its powdered blueberry counterpart. The intestinal digestion conditions negatively affected the bioaccessibility of anthocyanins regardless of the type of sample evaluated. Conclusion. Gastric digestion conditions promote greater stability of phenolic compounds in powdered and capsule blueberries, which could be relevant for the maintenance of an antioxidant environment at this level. The intestinal digestion conditions particularly affected the phenolic compounds of fresh and lyophilized blueberry, but not the capsule, which may suggest that encapsulation protected the phenols present from alkaline conditions. Further studies on in vitro absorption of the remaining components in the intestine and their possible effects on oxidative stress biomarkers in in vivo models are suggested(AU)

Consumption of mate Ilex paraguariensis: a folk beverage with antioxidant power against myocardial ischemic injury

The effects of the aqueous extract of Ilex paraguariensis (Ip)and the flavonoid quercetin were tested during the induction of in vivomyocardial ischemia/ reperfusion in Rattus norvegicus. The antioxidant power of the extract and quercetin were chemically determined. The experimental groups were: control, ischemia/reperfusion induction, Iporal treatment, Iporal treatment and ischemia /reperfusion, quercetin oral treatment, and quercetin oral treatment and ischemia/reperfusion. Rats were anesthetized with sodium thiopental and xylazine via intraperitoneal injection and subsequently underwent 15 minutes of ischemia followed by 15 minutes of reperfusion. Ischemia was promoted by tying the left anterior descending coronary artery. Areas of risk and infarction were stained by intravenous Evans blue and triphenyl tetrazolium chloride. Reactive oxygen species (ROS), antioxidant capacity against peroxylradicals, and lipid peroxidation of the myocardium were quantified. A significant reduction in areas of risk and infarction was detected in the ischemic myocardium treated with Ipand quercetin; ROS generation and lipid peroxidation were significantly reduced, and the antioxidant capacity was elevated. Oral administration of Ippromoted antioxidant benefits in the myocardium during ischemia and reperfusion, which reduced infarction. We suggest that Mate (a hot drink made from steeped dried leaves of Ip) consumption is a potential cardioprotective habit of indigenous people from southern South American countries, which must be better understood scientifically and ethnographically.

Cytotoxic effect of hydroalcoholic extract of Cota tinctoria (L) J. Gay on AGS and Hep-G2 cancer cell lines / Efecto citotóxico del extracto hidroalcohólico de Cota tinctoria (L) J. Gay sobre líneas celulares de cáncer AGS y Hep-G2

Cota tinctoria is a medicinal plant which has been used for management of cancer in folk medicine of various regions. The aim of present study is to investigate cytotoxic activity of different concentrations of hydroalcoholic extract of C. tinctoria flowers on gastric (AGS) and liver (Hep-G2) cancer cell lines as well as Human Natural GUM fibroblast (HUGU) cells. Cell mortality rates were examined after 24, 48 and 72 h incubations using the MTT assay. IC50of extract on AGS cells after 24, 48 and 72h was 1.46, 1.29 and 1.14 µg/mL respectively. The extract demonstrated IC50 of 5.15, 3.92 and 2.89 µg/mL on Hep-G2 cells after 24, 48 and 72 h respectively. No cytotoxic effect was detected on HUGU (Human Natural GUM fibroblast) cells. C. tinctoria seems to have a promising potential to be considered as a source for anticancer drug discovery. However, more experimental and clinical studies are required.

Cota tinctoria es una planta medicinal que se ha utilizado para el tratamiento del cáncer en la medicina popular de varias regiones. El objetivo del presente estudio es investigar la actividad citotóxica de diferentes concentraciones de extracto hidroalcohólico de flores de C. tinctoria en líneas celulares de cáncer gástrico (AGS) e hígado (Hep-G2), así como en células de fibroblasto GUM humano natural (HUGU). Se examinaron las tasas de mortalidad celular después de incubaciones de 24, 48 y 72 h utilizando el ensayo MTT. La CI50 del extracto en células AGS después de 24, 48 y 72 h fue de 1,46; 1,29 y 1,14 µg respectivamente. El extracto demostró una CI50 de 5,15, 3,92 y 2,89 µg/mL en células Hep-G2 después de 24, 48 y 72 h, respectivamente. No se detectó ningún efecto citotóxico en las células HUGU (fibroblasto GUM humano natural). C. tinctoria parece tener un potencial prometedor para ser considerada como una fuente de descubrimiento de fármacos contra el cáncer. Sin embargo, se requieren más estudios experimentales y clínicos.

The Relationship Between Neuroprotective Activity and Antigenotoxic and Acetylcholinesterase Inhibitory Effects of Glaucium corniculatum Extracts

Abstract The purpose of this study was to investigate the relationship between the acetylcholinesterase (AChE) inhibitory and antigenotoxic effect with the neuroprotective activity of Glaucium corniculatum methanol and water extracts rich in rutin and quercetin flavonoids. Neuroprotective activity in terms of cell survival and development against oxidative damage was measured by MTT assay and microscopic analysis in H2O2-induced NGF-differentiated PC12 (dPC12) cells. QRT-PCR and western blot hybridization method was employed for the determination of AChE inhibition of the extracts in the same cell model, and the genotoxic and antigenotoxic effects were identified with Comet assay with human lymphocytes. H2O2-induced vitality loss in dPC12 cells was inhibited in pre-treated cells with these plant extracts. Moreover, extracts stimulated neurite formation and prevented the oxidative stress-induced reduction in neurite growth. In general, it was determined that G. corniculatum methanol extract containing higher amounts of rutin and quercetin was more effective than water extract in terms of AChE inhibitory, antigenotoxic and also neuroprotective effect. In this study, it was shown for the first time that both AChE inhibitory and antigenotoxic effects of G. corniculatum may be effective in neuroprotection and it's protective and therapeutic effects against neurodegeneration may be related to the flavonoid content.

Influência da Delfinidina como potencial modulador da capacidade imunorregulatória das Células-Tronco Mesenquimais / Influence of Delphinidin as a potential modulator of the immunoregulatory capacity of Mesenchymal Stem Cells

As Células-Tronco Mesenquimais (CTMs), são células multipotentes, presentes em diversos tecidos, sendo bastante estudada devido sua capacidade imunorregulatória por meio da liberação de fatores solúveis. Fatores estes que atuam sobre as funções de células do sistema imunitário. Simultaneamente, estudos indicam que os compostos flavonoides, em destaque a Delfinidina, presente em alguns frutos e flores, possuem atuação anti-inflamatória e inibitória sobre células do sistema imunitário. Todavia, são escassos os estudos em relação entre a capacidade imunorregulatória da CTM e a influência da Delfinidina, sendo este o objetivo deste estudo. Inicialmente, a Delfinidina 3-O-ß-D-glicosídeo foi escolhido, devido a sua maior estabilidade e a dose de 50 µM foi selecionada após análise por citometria de fluxo que mostrou aumento da fase proliferativa do ciclo celular. Posteriormente ao realizar análise da produção de fatores solúveis pelas CTM, os resultados mostraram aumento da produção de IL-10, TGF-ß e Oxido nítrico pelas CTM tratadas com Delfinidina. Bem como, diminuição da expressão de p-NF-κB/NF-κB pelas CTMs tratadas com Delfinidina, quando avaliadas por Wersten Blot. Adicionalmente, para analisar a Delfinidina sobre os efeitos imunorregulatórios da CTM sob macrófagos (RAW 264.7), célula esta, importante no sistema imune inato. Foram realizadas culturas condicionadas, com posterior análise da produção de fatores solúveis, os resultados mostraram aumento da produção de IL-10, e diminuição da produção de TNF-α, IL-1α e IL-12 pelos macrófagos, nas culturas condicionadas. Assim como, diminuição da expressão do fator p-NF-κB/NF-κB pelos macrófagos nas culturas condicionadas, quando avaliadas por Wersten Blot. Ademais, ao analisar a atividade metabólica dos macrófagos por ensaio de MTT, os resultados mostraram que as culturas condicionadas e a Delfinidina per si foi capaz de diminuir a atividade metabólica, sem alterar os efeitos anti-inflamatórios sobre a célula. Em síntese, a Delfinidina mostrou acentuar a atuação imunorregulatória da CTM sobre a linhagem macrofágica, célula esta, de grande importância para o sistema imune inato

Mesenchymal Stem Cells (MSCs) are multipotent cells present in various tissues, being widely studied due to their immunoregulatory capacity through the release of soluble factors. These factors act on the functions of cells of the immune system. Simultaneously, studies indicate that flavonoid compounds, especially Delphinidin, present in some fruits and flowers, have anti inflammatory and inhibitory effects on immune system cells. However, there are few studies on the relationship between the immunoregulatory capacity of MSC and the influence of Delphinidin, which is the objective of this study. Initially, Delphinidin 3-O-ß-D-glycoside was chosen due to its greater stability and the 50 µM dose was selected after analysis by flow cytometry which showed an increase in the proliferative phase of the cell cycle. Subsequently, when analyzing the production of soluble factors by MSCs, the results showed an increase in the production of IL-10, TGF-ß and nitric oxide by MSCs treated with Delphinidin. As well as decreased expression of p-NF-κB/NF-κB by MSCs treated with Delphinidin, when evaluated by Wersten Blot. Additionally, to analyze Delphinidin on the immunoregulatory effects of MSC on macrophages (RAW 264.7), this cell is important in the innate immune system. Conditioned cultures were performed, with subsequent analysis of the production of soluble factors, the results showed an increase in the production of IL-10, and a decrease in the production of TNF-α, IL-1α and IL-12 by macrophages, in the conditioned cultures. As well as decreased expression of p-NF-κB/NF-κB factor by macrophages in conditioned cultures, when evaluated by Wersten Blot. Furthermore, when analyzing the metabolic activity of macrophages by MTT assay, the results showed that conditioned cultures and Delphinidin itself was able to decrease the metabolic activity, without altering the anti-inflammatory effects on the cell. In summary, Delphinidin has shown to enhance the immunoregulatory action of MSC on the macrophage lineage, a cell that is of great importance for the innate immune system

Phytochemical composition and biological activities of extracts from ten species of the family Melastomataceae Juss / Composição fitoquímica e atividades biológicas de extratos de dez espécies da família Melastomataceae Juss

Abstract Plants possess a renewable source of metabolites with enormous chemical structural diversity, which may have potential therapeutic relevance. Furthermore, this chemical diversity favors the possibility of finding new and different chemical constituents with antimicrobial, antioxidant and anti-tumor activities. This work analyzed preliminary phytochemical profiles and evaluated the antimicrobial, antioxidant and cytotoxic activities of hexane extracts of leaves of ten species of the family Melastomataceae. Phytochemical screening was performed using staining methods while total phenols and flavonoids were quantified by spectrophotometry. Antimicrobial activity was evaluated using the disk diffusion method. Antioxidant activity was determined by the 2,2-diphenyl-1-picrylhydrazil (DPPH) method. Toxicity was recorded using the lethality test with Artemia salina Leach (1819). Cytotoxic activity of the extracts was assessed in vitro with acute monocytic leukemia cells (THP-1). Phytochemical analysis detected the presence of tannins, terpenes, steroids, polyphenols and flavonoids and the absence of alkaloids. Clidemia capitellata (Bonpl.) D. Don had the greatest amount of polyphenols (205.95 mg/g ± 4.14) while Clidemia hirta (L.) D. Don had the highest content of total flavonoids (143.99 mg/g ± 4.18). The hexane extracts did not show antimicrobial activity nor toxicity against Artemia salina. The extract of Tibouchina francavillana Cogn. was the most active in sequestering the DPPH radical. The extracts showed cytotoxicity in THP-1 cells with the appearance of apoptotic bodies and cell death. The extracts of Miconia amoena, Clidemia sericea and Clidemia capitellata are non-toxic against Artemia salina and induce the formation of apoptotic bodies and cell death of the THP-1 lineage.

Resumo Os vegetais apresentam uma fonte renovável de metabólitos com enorme diversidade química estrutural, os quais podem apresentar potencial relevante na terapêutica, aumentando as possibilidades de encontrar novos e diferentes constituintes químicos com atividades antimicrobiana, antioxidante e antitumoral. Este trabalho analisou o perfil fitoquímico preliminar e as atividades antimicrobiana, antioxidante, citotóxica dos extratos em hexano das folhas de dez espécies da família Melastomataceae. A triagem fitoquímica foi executada utilizando métodos de coloração e quantificação de fenóis e flavonoides totais por espectrofotometria. A atividade antimicrobiana foi realizada pelo método de difusão em disco. A atividade antioxidante foi determinada pelo método 2,2-difenil-1-picrilhidrazila (DPPH). A toxicidade foi registrada utilizando o ensaio de letalidade com Artemia salina Leach (1819). A atividade citotóxica dos extratos foi realizada in vitro com células leucêmicas monocítica aguda (THP-1). A análise fitoquímica detectou a presença de taninos, terpenos, esteroides, polifenóis, flavonoides e ausência de alcaloides. A maior quantificação de polifenóis foi da Clidemia capitellata (Bonpl.) D. Don (205,95 mg/g ± 4,14) e o extrato de Clidemia hirta (L.) D. Don apresentou maior teor de flavonoides totais (143,99 mg/g ± 4,18). Os extratos hexânicos não demostraram atividade antimicrobiana e nem toxicidade frente à Artemia salina. O extrato de Tibouchina francavillana Cogn. foi o mais ativo no sequestro do radical DPPH. Os extratos apresentaram citotoxicidade em células THP-1, com visualização de corpos apoptóticos e morte celular. Os extratos de Miconia amoena, Clidemia sericea e Clidemia capitellata são atóxicos contra Artemia salina e induzem a formação de corpos apoptóticos e morte celular da linhagem THP-1.

Casticin inhibits the proliferation, migration and invasion of bladder cancer cells by inhibition of TM7SF4 expression / 中华肿瘤杂志

Objective: To explore the effect and mechanism of Casticin (CAS) on the proliferation, migration and invasion of bladder cancer T24 cells. Methods: T24 cells were cultured in vitro and divided into control group, 5, 10, 20 μmol/L CAS groups, si-NC group, si-TM7SF4 group, CAS+ pcDNA group and CAS+ pcDNA-TM7SF4 group. Cell counting kit-8 (CCK-8) was used to detect cell proliferation; Transwell was used to detect cell migration and invasion; western blot was used to detect the protein expressions of cyclin D1, p21, MMP-2, MMP-9 and TM7SF4, and real-time quantitative reverse transcription polymerase chain reaction (RT-qPCR) was used to detect the expression of TM7SF4 mRNA. Results: The inhibition rates of T24 cells in the 5, 10, 20 μmol/L CAS groups were (17.68±1.41)%, (33.54±3.16)% and (61.44±5.50)%, respectively, higher than (0.00±0.00)% of the control group (P<0.001), but the numbers of migration and invasion were 72.83±5.66, 59.13±4.27, 41.25±3.22 and 55.83±5.15, 42.19±3.06, 31.13±3.22, respectively, lower than 86.11±5.16 and 68.82±5.29 of the control group (P<0.001). The protein expression levels of cyclin D1, MMP-2, MMP-9, TM7SF4 and the expression levels of TM7SF4 mRNA in the 5, 10, and 20 μmol/L CAS groups were lower than the control group (P<0.001). However, the protein expression levels of p21 were 0.37±0.03, 0.51±0.04, and 0.66±0.06, respectively, higher than 0.25±0.03 in the control group (P<0.001). The inhibition rate of T24 cells in the si-TM7SF4 group was (50.35±4.67)%, higher than (6.31±0.58)% in the si-NC group (P<0.001), but the numbers of migration and invasion were 53.51±4.18 and 42.92±3.81, lower than 85.26±4.99 and 67.93±4.64 of the si-NC group (P<0.001). The protein expression levels of TM7SF4, CyclinD1, MMP-2, MMP-9 in the si-TM7SF4 group were lower than the si-NC group (P<0.001). However, the protein expression level of p21 in the si-TM7SF4 group was higher than the si-NC group (P<0.001). The inhibitory rate of T24 cells in the CAS+ pcDNA-TM7SF4 group was (21.45±2.46)%, lower than (64.06±4.49)% of the CAS+ pcDNA group (P<0.001), but the number of migration and invasion in the CAS+ pcDNA-TM7SF4 group were 75.66±6.57 and 59.35±5.40, higher than 40.43±3.85 and 30.25±3.32 in the CAS+ pcDNA group (P<0.001). The protein expression levels of TM7SF4, CyclinD1, MMP-2 and MMP-9 in the CAS+ pcDNA-TM7SF4 group were higher than the CAS+ pcDNA group (P<0.001), but the protein expression level of p21 was lower than the CAS+ pcDNA group (P<0.001). Conclusion: CAS may suppress the proliferation, migration and invasion of bladder cancer T24 cells by inhibiting the expression of TM7SF4.

Research progress on Astragali Radix and prediction of its quality markers (Q-markers) / 中国中药杂志

Astragali Radix, a medicinal herb for invigorating Qi, has anti-aging, anti-tumor, immunoregulatory, blood sugar-and lipid-lowering, anti-fibrosis, anti-radiation and other pharmacological effects. This article reviewed the studies about the chemical components and pharmacological effects of Astragali Radix. According to the theory of quality markers(Q-markers) of Chinese medicinal materials, we predicted the Q-markers of Astragali Radix from traditional efficacy, chemical component validity, measurability, plant phylogeny, and pharmacokinetis. The results showed that total polysaccharides, flavonoids(e.g., calycosin-7-O-β-D-glucoside, formononetin, calycosin, quercetin, and ononin), and saponins(e.g., astragalosides Ⅱ, Ⅲ, and Ⅳ) can be taken as the main Q-markers. This review lays a foundation for regulating the quality research and standard establishment of Astragali Radix, and benefits the control and quality supervision of the production process of Astragali Radix and its related products.

Preparation and characterization of fenugreek leaf flavonoids and their protective effects against oxidative damage to hepatocytes / 中国中药杂志

The present study investigated the main components of fenugreek(Trigonella foenum-graecum L.) leaf flavonoids(FLFs) and their antioxidant activity. FLFs were prepared and enriched by solvent extraction, and the flavonoids were characterized by high-performance liquid chromatography-quadrupole-time-of-flight tandem mass spectrometry(HPLC-Q-TOF-MS/MS). The protective effect of FLFs against H_2O_2-induced stress damage to L02 hepatocytes was also investigated. Firstly, the cell viability was measured by MTT assay. The oxidative stress injury model was induced by H_2O_2 in L02 cells. The release of lactate dehydrogenase(LDH), the content of reduced glutathione(GSH) and malondialdehyde(MDA), and the activities of superoxide dismutase(SOD) and catalase(CAT) were measured by assay kits. Hoechst fluorescence staining was performed to observe the cell apoptosis. The expression levels of c-Jun N-terminal kinase(JNK), extracellular signal-regulated kinase 1/2(ERK1/2), nuclear factor erythroid-2 related factor 2(Nrf2), heme oxygenase 1(HO-1), and their phosphorylated proteins were detected by Western blot. Based on the MS fragment ion information and data in databases, FLFs contained eight flavonoids with quercetin and kaempferol as the main aglycons. The cell viabi-lity assay revealed that as compared with the conditions in the H_2O_2 treatment group, 3.125-25 μg·mL~(-1) FLFs could increase the viability of L02 cells, reduce LDH release and MDA content in a dose-dependent manner, potentiate the activities of SOD, CAT, and GSH, decrease the phosphorylation of JNK and ERK1/2 proteins, and up-regulate the expression of Nrf2 and HO-1. The results of fluorescence staining showed that the nucleus of the H_2O_2 treatment group showed concentrated and dense strong blue fluorescence, while the blue fluorescence intensity of the FLFs group decreased significantly. FLFs showed a protective effect against H_2O_2-induced oxidative damage in L02 cells, and the underlying mechanism is associated with the enhancement of cell capability in clearing oxygen free radicals and the inhibition of apoptosis by the activation of the MAPKs/Nrf2/HO-1 signaling pathway. The antioxidant effect of fenugreek leaf is related to its rich flavonoids.

Icariin improves renal interstitial fibrosis in a rat model of chronic renal failure by regulating mitochondrial dynamics / 中国中药杂志

This study aims to explore the effect of icariin(ICA) on mitochondrial dynamics in a rat model of chronic renal failure(CRF) and to investigate the molecular mechanism of ICA against renal interstitial fibrosis(RIF). CRF was induced in male Sprague-Dawley(SD) rats with 5/6(ablation and infarction, A/I) surgery(right kidney ablation and 2/3 infarction of the left kidney). Four weeks after surgery, the model rats were randomized into the following groups: 5/6(A/I) group, 5/6(A/I)+low-dose ICA group, and 5/6(A/I)+high-dose ICA group. Another 12 rats that received sham operation were randomly classified into 2 groups: sham group and sham+ICAH group. Eight weeks after treatment, the expression of collagen-Ⅰ(Col-Ⅰ), collagen-Ⅲ(Col-Ⅲ), mitochondrial dynamics-related proteins(p-Drp1 S616, p-Drp1 S637, Mfn1, Mfn2), and mitochondrial function-related proteins(TFAM, ATP6) in the remnant kidney tissues was detected by Western blot. The expression of α-smooth muscle actin(α-SMA) was examined by immunohistochemical(IHC) staining. The NRK-52 E cells, a rat proximal renal tubular epithelial cell line, were cultured in vitro and treated with ICA of different concentration. Cell viability was detected by CCK-8 assay. In NRK-52 E cells stimulated with 20 ng·mL~(-1) TGF-β1 for 24 h, the effect of ICA on fibronectin(Fn), connective tissue growth factor(CTGF), p-Drp1 S616, p-Drp1 S637, Mfn1, Mfn2, TFAM, and ATP6 was detected by Western blot, and the ATP content and the mitochondrial morphology were determined. The 20 ng·mL~(-1) TGF-β1-stimulated NRK-52 E cells were treated with or without 5 μmol·L~(-1) ICA+10 μmol·L~(-1) mitochondrial fusion promoter M1(MFP-M1) for 24 h and the expression of fibrosis markers Fn and CTGF was detected by Western blot. Western blot result showed that the levels of Col-Ⅰ, Col-Ⅲ, and p-Drp1 S616 were increased and the levels of p-Drp1 S637, Mfn1, Mfn2, TFAM, and ATP6 were decreased in 5/6(A/I) group compared with those in the sham group. The levels of Col-Ⅰ, Col-Ⅲ, and p-Drp1 S616 were significantly lower and the levels of p-Drp1 S637, Mfn1, Mfn2, TFAM, and ATP6 were significantly higher in ICA groups than that in 5/6(A/I) group. IHC staining demonstrated that for the expression of α-SMA in the renal interstitium was higher in the 5/6(A/I) group than in the sham group and that the expression in the ICA groups was significantly lower than that in the 5/6(A/I) group. Furthermore, the improvement in the fibrosis, mitochondrial dynamics, and mitochondrial function were particularly prominent in rats receiving the high dose of ICA. The in vitro experiment revealed that ICA dose-dependently inhibited the increase of Fn, CTGF, and p-Drp1 S616, increased p-Drp1 S637, Mfn1, Mfn2, TFAM, and ATP6, elevated ATP content, and improved mitochondrial morphology of NRK-52 E cells stimulated by TGF-β1. ICA combined with MFP-M1 further down-regulated the expression of Fn and CTGF in NRK-52 E cells stimulated by TGF-β1 compared with ICA alone. In conclusion, ICA attenuated RIF of CRF by improving mitochondrial dynamics.

UPLC-Q-TOF-MS analysis of chemical constituents of classical prescription Yiguanjian standard decoction / 中国中药杂志

An UPLC-Q-TOF-MS method was employed to characterize and classify the chemical components of the standard decoction of Yiguanjian, a classical famous recipe. Chromatographic separation was performed on an Acquity HSS T3(2.1 mm ×100 mm, 1.8 μm) column with a mobile phase of 0.1% formic acid water-0.1% formic acid acetonitrile using gradient elution. The flow rate was 0.4 mL·min~(-1) and the column temperature was 40 ℃. Mass spectrometry was performed on electrospray ionization source(ESI) with positive and negative ion scanning modes. The potential compounds were identified by comparing the reference compounds, analyzing the mass spectrometry data and matching the published articles on Masslynx 4.1 software and SciFinder database. Finally, a total of 113 compounds, including 11 amino acids, 19 terpenoids, 13 phthalides, 11 steroidal saponins, 10 coumarins, 9 alkaloids, 7 flavonoids, 8 phenylethanoid glycosides, 8 organic acids and 17 other categories were identified. The established method systematically and accurately characterized the chemical components in Yiguanjian, which could provide experimental evidences for the subsequent studies on the pharmacodynamical material basis and quality control of Yiguanjian.

Research progress on chemical constituents and pharmacological activities of Morus alba / 中国中药杂志

Morus alba, a traditional economic crop, is also a significant medicinal plant. The branches(Mori Ramulus), leaves(Mori Folium), roots and barks(Mori Cortex), and fruits(Mori Fructus) of M. alba are rich in chemical components, such as alkaloids, flavonoids, flavanols, anthocyanins, benzofurans, phenolic acids, and polysaccharides, and possess hypoglycemic, hypolipidemic, anti-inflammatory, anti-tumor, anti-microbial, liver protective, immunoregulatory, and other pharmacological activities. This study analyzed the sources, classification, and functions of the main chemical components in M. alba and systematically summarized the latest research results of essential active components in M. alba and their pharmacological effects to provide references for in-depth research and further development as well as utilization of active components in M. alba.

Research advances in chemical constituents and pharmacological activities of Dendrobium plants / 中国中药杂志

Dendrobii Caulis are commonly used tonic Chinese medicinal materials with a long history of application. As demonstrated by pharmacological results, the chemical constituents and the extracts of Dendrobii Caulis have anti-inflammatory, antibacte-rial, antioxidant, and anti-tumor effects, and can also regulate immunity, lower blood pressure, and regulate blood sugar. The active ingredients contained are widely concerned by scholars. This paper comprehensively summarized the chemical constituents and pharmacological activities of Dendrobium plants reported so far. The chemical constituents isolated from Dendrobium plants are mainly alkaloids, sesquiterpenoids, flavonoids, fluorenones, coumarins, bibenzyls, phenanthrenes, lignans, steroids, phenols, and polysaccharides. This paper is expected to provide a reference for further research, development, and utilization of Dendrobium plants.

Baicalin inhibits LPS/IFN-γ-induced inflammation via TREM2/TLR4/NF-κB pathway in BV2 cells / 中国中药杂志

This study investigated the mechanism of baicalin on lipopolysaccharide(LPS)/interferon γ(IFN-γ)-induced inflammatory microglia based on the triggering receptor expressed on myeloid cells 2(TREM2)/Toll-like receptor 4(TLR4)/nuclear factor kappaB(NF-κB) pathway. Specifically, LPS and IFN-γ were used to induce inflammation in mouse microglia BV2 cells. Then the normal group, model group, low-dose(5 μmol·L~(-1)) baicalin group, medium-dose(10 μmol·L~(-1)) baicalin group, high-dose(20 μmol·L~(-1)) baicalin group, and minocycline(10 μmol·L~(-1)) group were designed. Cell viability was detected by CCK-8 assay and cell morphology was observed under bright field. The expression of interleukin-1β(IL-1β), interleukin-4(IL-4), inducible nitric oxide synthase(iNOS), interleukin-6(IL-6), interleukin-10(IL-10), and arginase-1(Arg-1) mRNA was detected by real-time quantitative PCR, the protein expression of tumor necrosis factor-α(TNF-α), IL-1β, TREM2, TLR4, inhibitor kappaB-alpha(IκBα), p-IκBα, NF-κB p65 and p-NF-κB p65 by Western blot, and transfer of NF-κB p65 from cytoplasm to nucleus by cellular immunofluorescence. Compared with the normal group, most of the BV2 cells in the model group tended to demonstrate the pro-inflammatory M1 amoeba morphology, and the model group showed significant increase in the mRNA levels of IL-1β, IL-6, and iNOS, decrease in the mRNA levels of IL-4, IL-10, and Arg-1(P<0.01), rise of the protein expression of TNF-α, IL-1β, TLR4, p-IκBα, and p-NF-κB p65(P<0.01), reduction in TREM2 protein expression, and increase in the expression of NF-κB p65 in nucleus. Compared with the model group, baicalin groups and minocycline group showed the recovery of BV2 cell morphology, significant decrease in the mRNA levels of IL-1β, IL-6 and iNOS, increase in the mRNA levels of IL-4, IL-10, and Arg-1(P<0.01), reduction in the protein expression of TNF-α, IL-1β, TLR4, p-IκBα, and p-NF-κB p65(P<0.05), rise of TREM2 protein expression, and decrease in the expression of NF-κB p65 in nucleus. In summary, these results suggest that baicalin can regulate the imbalance between TREM2 and TLR4 of microglia and inhibit the activation of downstream NF-κB, thus promoting the polarization of microglia from pro-inflammatory phenotype to anti-inflammatory phenotype.