ABSTRACT
A COVID-19 surgiu de forma repentina, acometendo milhões de pessoas e causando muitas mortes no mundo todo. Diante disso, torna-se necessário a busca de substâncias bioativas com propriedades antivirais. No Brasil, a espécie Tetradenia riparia foi inserida como planta ornamental exótica, com aroma intenso e agradável, sendo cultivada em parques, jardins, residenciais e hortos. O objetivo deste estudo foi identificar compostos presentes no extrato bruto das folhas de Tetradenia riparia com interesse antiviral. O extrato bruto das folhas secas foi obtido por maceração dinâmica por esgotamento do solvente e após, concentrado em evaporador rotativo. A composição química do extrato bruto foi analisada por cromatografia líquida de ultra eficiência acoplada à espectrometria de massas de alta resolução (UHPLC-ESI/qTOF). Foram identificados 31 compostos que foram investigados por meio de levantamento bibliográfico quanto ao seu potencial anti- SARS-CoV-2. Os compostos rosmanol, procianidina, cianidina, betulina, ácido betulínico e o ácido sagerínico, apresentaram potencial atividade antiviral sobre o SARS-CoV-2. Esta investigação é promissora, indicando possivelmente que no extrato bruto das folhas de T. ripária existem compostos que podem combater o SARS-CoV-2. Neste sentido, estudos de ancoramento molecular (docking) e análises in silico sobre a proteína Mpro do vírus devem ser realizadas corroborando desta forma a ação dos compostos identificados.
COVID-19 appeared suddenly, affecting millions of people and causing many deaths worldwide. Therefore, it is necessary to search for bioactive substances with antiviral properties. In Brazil, Tetradenia riparia was inserted as an exotic ornamental plant, with an intense and pleasant aroma, cultivated in parks, residential and vegetable gardens. This study aimed to identify compounds present in the crude extract of Tetradenia riparia leaves with antiviral interest. The crude extract of the dried leaves was obtained by dynamic maceration with solvent exhaustion and then concentrated in a rotary evaporator. The chemical composition of the crude extract was analyzed by ultra- performance liquid chromatography coupled with high-resolution mass spectrometry (UHPLC- ESI/qTOF). We identified 31 compounds investigated through a literature review for their anti- SARS-CoV-2 potential. The compounds rosmanol, procyanidin, cyanidin, betulin, betulinic acid, and sagerinic acid showed potential antiviral activity against SARS-CoV-2. Therefore, this investigation is promising, possibly indicating that in the crude extract of T. riparia leaves, there are compounds that can fight SARS-CoV-2. In this sense, molecular docking studies and in silico analyzes on the virus Mpro protein must be carried out, thus corroborating the action of the identified compounds.
SARS-CoV-19 ha aparecido repentinamente, afectando a millones de personas y causando muchas muertes en todo el mundo. Por ello, se hace necesaria la búsqueda de sustancias bioactivas con propiedades antivirales. En Brasil, la especie Tetradenia riparia ha sido introducida como planta ornamental exótica, con un aroma intenso y agradable, siendo cultivada en parques, jardines, residencias y centros de jardinería. El objetivo de este estudio fue identificar los compuestos presentes en el extracto crudo de las hojas de Tetradenia riparia con interés antiviral. El extracto crudo de las hojas secas se obtuvo por maceración dinámica por agotamiento del disolvente y después, se concentró en el evaporador rotatorio. La composición química del extracto crudo se analizó mediante cromatografía líquida de ultra rendimiento acoplada a espectrometría de masas de alto rendimiento (UHPLC-ESI/qTOF). Se identificaron 31 compuestos y se investigó su potencial anti-SARS-CoV-2 mediante un estudio bibliográfico. Los compuestos rosmanol, procianidina, cianidina, betulina, ácido betulínico y ácido sagerínico, mostraron una potencial actividad antiviral sobre el SARS-CoV-2. Esta investigación es prometedora, pues posiblemente indica que en el extracto crudo de las hojas de T. riparia hay compuestos que pueden combatir el SARS-CoV-2. En este sentido, deben realizarse estudios de docking y análisis in silico sobre la proteína Mpro del virus para corroborar la acción de los compuestos identificados.
Subject(s)
Antiviral Agents/analysis , Plant Leaves , Lamiaceae/toxicity , Complex Mixtures/analysis , SARS-CoV-2/drug effects , Chromatography, Liquid/instrumentation , Complex Mixtures , Phytochemicals/analysis , Betulinic Acid/analysisABSTRACT
Cancer is an abnormal and uncontrolled growth of cells that spreads through cell division. There are different types of medicines available to treat cancers, but no drug is found to be fully effective and safe for humans. The major problem involved in the cancer treatments is the toxicity of the established drug and their side effects. Medicinal plants are used as folk medicines in Asian and African populations for thousands of years. 60% of the drugs for treating cancer are derived from plants. More than 3000 plants have anticancer activity. The present review aims at the study of a broad spectrum survey of plants having anticancer components for different type of cancers. This article consists of 364 medicinal plants and their different parts as potential Source of Anticancer Agents.
El cáncer es un crecimiento anormal y descontrolado de células que se disemina a través de la división celular. Hay diferentes tipos de medicamentos disponibles para tratar el cáncer, pero no se ha encontrado ningún medicamento que sea completamente efectivo y seguro para los seres humanos. El principal problema involucrado en los tratamientos del cáncer es la toxicidad del fármaco establecido y sus efectos secundarios. Las plantas medicinales se utilizan como medicinas populares en poblaciones asiáticas y africanas durante miles de años. El 60% de los medicamentos para el tratamiento del cáncer se derivan de plantas. Más de 3000 plantas tienen actividad anticancerígena. La presente revisión tiene como objetivo el estudio de un estudio de amplio espectro de plantas que tienen componentes anticancerígenos para diferentes tipos de cánceres. Este artículo consta de 364 plantas medicinales y sus diferentes partes como fuente potencial de agentes anticancerígenos.
Subject(s)
Plants, Medicinal/chemistry , Anticarcinogenic Agents/pharmacology , Phytochemicals/analysis , Cell Line, Tumor/drug effects , Phytochemicals/pharmacologyABSTRACT
Abstract The continuous prolonged exposures of sun light especially the ultra violet (UV) radiation present in it, cause not only the risk of skin cancer but also it may cause premature skin aging, photodermatoses and actinic keratoses. Flavonoids (including Flavane, Flavanone, Flavone, Flavonol, Isoflavone, Neoflavone etc.) having potent antioxidant activity, used as topical applications for protection against UV induced skin damages as well as for skin care. Most commonly used flavonoid is quercetin (Flavonol), which is present in fruits, vegetables, and herbs. We aim to review the research focused on development of different novel formulations to treat UV radiations induced skin diseases. In this review, several formulations of flavonoid quercetin were discussed and their outcomes were compiled and compared in context to solubility, stability and efficiency of application. On the basis this comparative analysis we have concluded that three formulations, namely glycerosomes, nanostructured lipid carriers and deformable liposomes hold good applications for future aspects for topical delivery of quercetin. These formulations showed enhanced stability, increased quercetin accumulation in different skin layers, facilitated drug permeation in skin and long-lasting drug release.
Subject(s)
Quercetin/analysis , Skin/injuries , Skin Diseases/drug therapy , Skin Neoplasms/pathology , Ultraviolet Rays/adverse effects , Phytochemicals/analysis , Flavonoids/adverse effects , Pharmaceutical Preparations/analysis , Keratosis, Actinic/pathology , Protective Factors , Antioxidants/classificationABSTRACT
The objective of this study is to examine the antidepressant and antioxidant effects of thymoquinone (TQ) on reserpine-induced depression, and to investigate the antidepressant and antioxidant activity of combined treatment of TQ+citalopram. In total, 36 male Wistar rats were randomly divided into 6 groups: 1)control1, 2)control2, 3)reserpine, 4)reserpine+TQ 5)reserpine+citalopram and 6)reserpine+TQ+citalopram. Depression was induced by administering intraperitoneal reserpine of 0.2mg/kg/14days. For antidepressant effects, 10 mg/kg TQ and/or 10 mg/kg citalopram was administered intragastrically 30 minutes prior to the administration of reserpine. Rat behavior was examined using the Behavioral Test following the completion of treatment protocol. Total nitric oxide (NOx) levels, malondialdehyde (MDA) levels, total oxidants status (TOS), total antioxidant status (TAS) in brain cortex, plasma as well as brain cortex glutathione (GSH) and levels of plasma total sulfhydryl groups (RSH) were examined. Treatment with TQ ameliorated the reserpine-induced changes in the Behavioral Test (p<0.05). TQ treatment significantly increased dopamine (DA) and noradrenaline (NA) expressions when compared to the R group (p<0.01). Serotonin (5-HT) expression also increased significantly (p<0.05). Brain cortex and plasma TOS, MDA and NOx levels decreased, whereas TAS, GSH and RSH levels increased (p< 0.05). TQ has the ability to prevent depression induced by reserpine. The combination of TQ+citalopram can be used in the treatment of depression with a stronger antioxidant effect
Subject(s)
Animals , Male , Rats , Nigella sativa/classification , Rats, Wistar , Phytochemicals/analysis , Antidepressive Agents/adverse effects , Antioxidants/adverse effects , Oxidative Stress , DepressionABSTRACT
A comparative study was perfomed with conventional and ultrasound assisted extraction on tomato processing waste. Ultrasound extraction exhibited slightly higher phenolic and flavonoids content, as well as higher ABTS + radical scavenging capacity (4.63 mg GAE.g-1, 0.96 mg RUE.g-1 and 27.90 µmol TE.g -1 respectively). On both extracts, a high percentage of flavonoids was lost during simulated digestion, resulting on a bioacessibility of approximately 13 %. Extracts presented good stability during storage conditions, which indicates a possible technological application.
Foi realizado um estudo comparativo com a extração convencional e assistida por ultrassom em resíduos do processamento de tomate. A extração ultrassônica exibiu teor de fenólicos e flavonóides ligeiramente maiores, bem como maior capacidade antioxidante ABTS + (4,63 mg AG.g-1, 0,96 mg RUE.g-1 e 27,90 µmol TE.g -1, respectivamente). Em ambos os extratos, uma alta porcentagem de flavonóides foi perdida durante a digestão simulada, resultando em uma bioacessibilidade de aproximadamente 13%. Os extratos apresentaram boa estabilidade durante as condições de armazenamento, o que indica uma possível aplicação tecnológica.
Subject(s)
Solanum lycopersicum/chemistry , Phenolic Compounds/analysis , Phytochemicals/analysis , Antioxidants/analysis , UltrasonicsABSTRACT
Reactive oxygen species are implicated in multiple pathological conditions including erectile dysfunction. This study evaluated the in vitro and in vivo antioxidant potential of the methanolic extracts of Inula glomerata and Salacia kraussii. The plant materials were pulverized and extracted with methanol. The phytochemical analysis, ability of the crude extracts to scavenge free radicals (ABTS, DPPH, NO.) in vitroas well as the total phenolic and flavonoid contents was investigated. In vivo, antioxidant potentials of the crude extracts (50/250 mg/kg body weight) were determined in an erectile dysfunction rat model. The phytochemical analysis revealed that both plants contain flavonoids, tannins, terpenoids, and alkaloids. The crude extracts at varying degree of efficiency, scavenged ABTS and DPPH radicals. The crude extracts at low concentrations (50 mg/kg b.w) significantly (p<0.05) diminished the level of malondialdehyde, augmented catalase activities and elevated glutathione levels. However, SOD activities were significantly boosted in a dose-dependent manner by the crude extracts. Therefore, I. glomerataand S. kraussiipossess antioxidant properties, hence, can serve as a therapeutic modality in the treatment of oxidative stress-induced erectile dysfunction.
Las especies reactivas de oxígeno están implicadas en múltiples condiciones patológicas, incluyendo la disfunción eréctil. Este estudio evaluó el potencial antioxidante in vitro e in vivo de extractos metanólicos de Inula glomeratay Salacia kraussii. Los materiales vegetales fueron pulverizados y extraídos con metanol. A estos extractos crudos se les llevó a cabo el análisis fitoquímico junto con el contenido total de fenólicos y flavonoides, así como se les investigó la capacidad in vitro para atrapar radicales (ABTS, DPPH, NO.). Los potenciales antioxidantes in vivo de los extractos crudos (50/250 mg/kg de peso corporal) se determinaron en un modelo en ratas con disfunción eréctil. El análisis fitoquímico reveló que ambas plantas contuvieron flavonoides, taninos, terpenoides y alcaloides. Los extractos crudos con un grado variable de eficiencia, atraparon a los radicales ABTS y DPPH. Los extractos crudos a bajas concentraciones (50 mg/kg p.c) significativamente (p<0.05) disminuyeron el nivel de malondialdehído, aumentaron las actividades de catalasa y elevaron los niveles de glutatión. Sin embargo, las actividades de SOD por los extractos crudos fueron significativamente dosis-dependientes. Así, los extractos de I. glomeratay S. kraussii mostraron propiedades antioxidantes, y por lo tanto, podrían servir como una alternativa terapéutica en el tratamiento de disfunción eréctil inducida por estrés oxidativo.
Subject(s)
Animals , Rats , Plant Extracts/pharmacology , Plant Extracts/chemistry , Inula/chemistry , Salacia/chemistry , Antioxidants/pharmacology , Antioxidants/chemistry , Sulfonic Acids/metabolism , Flavonoids/analysis , Reactive Oxygen Species , Rats, Sprague-Dawley , Oxidative Stress/drug effects , Asteraceae/chemistry , Celastraceae/chemistry , Benzothiazoles/metabolism , Phenolic Compounds/analysis , Phytochemicals/analysis , Nitric Oxide/metabolismABSTRACT
Diabetes mellitus is a metabolic disorder affecting a great part of population around the world. It is the fifth leading death causing disease in the world and its cases are increasing day by day. Traditional medicine is thought to have promising future in the treatment of diabetes mellitus. In contrast to synthetic drugs phytochemicals are considered to be free from side effects. As one of the main class of natural products, alkaloids and their derivatives have been widely used as sources of pharmacological agents against a variety of medical problems. Many studies confirmed the role of alkaloids in the management of diabetes and numerous alkaloids isolated from different medicinal plants were found active against diabetes. Like other natural products, alkaloids regulate glucose metabolism either by inhibiting or inducing multiple candidate proteins including AMP-activated protein kinase, glucose transporters, glycogen synthase kinase-3, sterol regulatory element-binding proteins 1, glucokinase, glucose-6-phosphatase, acetyl-CoA carboxylase among the others. A comprehensive review of alkaloids reported in the literature with anti-diabetic activities and their target enzymes is conducted, with the aim to help in exploring the use of alkaloids as anti-diabetic agents. Future work should focus on rigorous clinical studies of the alkaloids, their development and relevant drug targets.
Subject(s)
Plants, Medicinal/anatomy & histology , Alkaloids/analysis , Phytochemicals/analysis , Metabolism , Sterols/adverse effects , Biological Products , Pharmaceutical Preparations , Glucose-6-Phosphatase/adverse effects , Diabetes Mellitus/pathology , AMP-Activated Protein Kinases , Synthetic DrugsABSTRACT
Piper kadsura (Choisy) Ohwi which belongs to the family Piperaceae, is a well-known medicinal plant possessing high medicinal and various therapeutic properties. It is widely used in traditional Chinese medicine for the treatment of asthma and rheumatic arthritis. Numerous studies on this species have also corroborated the significant anti-inflammatory potential of its extracts and secondary metabolites. The main chemical constituents which have been isolated and identified from P. kadsura are lignans and neolignans, which possess anti-inflammatory activities. The present article aims to provide a review of the studies done on the phytochemistry and antiinflammatory activities of P. kadsura. The scientific journals for this brief literature review were from electronic sources, such as Science Direct, PubMed, Google Scholar, Scopus, and Web of Science. This review is expected to draw the attention of the medical professionals and the general public towards P. kadsura and to open the door for detailed research in the future.
Piper kadsura (Choisy) Ohwi, perteneciente a la familia Piperaceae, es una planta medicinal conocida que posee importantes propiedades medicinales y diversas propiedades terapéuticas. Es ampliamente utilizada en la medicina tradicional china para el tratamiento del asma y la artritis reumática. Numerosos estudios sobre esta especie también han corroborado el destacado potencial antiinflamatorio de sus extractos y metabolitos secundarios. Los principales componentes químicos que se han aislado e identificado de P. kadsura son los lignanos y los neolignanos, que poseen actividades antiinflamatorias. El presente artículo tiene como objetivo proporcionar una revisión de los estudios realizados sobre las actividades fitoquímicas y antiinflamatorias de P. kadsura. Las revistas científicas para esta breve revisión de literatura fueron de fuentes electrónicas, como Science Direct, PubMed, Google Scholar, Scopus y Web of Science. Se espera que esta revisión atraiga la atención de los profesionales médicos y el público en general respecto de P. kadsura y abra la puerta a una investigación detallada en el futuro.
Subject(s)
Piper/chemistry , Anti-Inflammatory Agents/chemistry , Plants, Medicinal , Oils, Volatile/chemistry , Lignans/analysis , Piperaceae/chemistry , Kadsura , Alkaloids/analysis , Phytochemicals/analysis , Medicine, Chinese Traditional , Anti-Inflammatory Agents/pharmacologyABSTRACT
Clinopodium mexicanum (Benth.) Govaerts (Lamiaceae) is a native plant of Mexico. This plant is used in traditional Mexican medicine for the treatment of cultural specific syndromes such as "susto", "nervios" or "espanto", conditions related to anxiety and depression. In addition, it has a high biocultural value for its medicinal and culinary use and for its exchange value in various indigenous areas of México. This review aims to compile updated information about the ethnobotanical, phytochemistry and commercialization aspects of Clinopodium mexicanum, and it focuses on the potential use of this species as a raw material in the phytopharmaceutical industry for the treatment of anxiety and pain. Moreover, it would be a viable productive alternative for many rural communities, which could not only produce the raw material but who could also add value to the sale of the plant.
Clinopodium mexicanum (Benth.) Govaerts, es una planta nativa de México. Es usada en la medicina tradicional mexicana para tratar síndromes de filiación cultural como "susto", "nervios" o "espanto", los cuales están asociados a la ansiedad y depresión. Además, la planta presenta un alto valor biocultural por sus usos: medicinal, culinario y por el valor de cambio que tiene en áreas indígenas de México. La revisión presentada tiene como objetivo compilar información actualizada sobre aspectos etnobotánicos, fitoquímicos y comercialización de Clinopodium mexicanum. Igualmente señalar el potencial uso de esta especie como materia prima para la elaboración de productos para la ansiedad y el dolor por parte de la industria fitofarmacéutica. Además de ser una alternativa productiva para muchas comunidades rurales, las cuales pueden venderla como materia prima o como producto derivado.
Subject(s)
Plants, Medicinal , Ethnobotany , Lamiaceae/chemistry , Medicine, Traditional , Commerce , Phytochemicals/analysis , Indigenous Peoples , MexicoABSTRACT
It is important to determine the chemical composition of fruits in order to establish their potential health benefits for human nutrition and thus stimulate their cultivation and consumption. Therefore, the objective of this study was to determine the physical and chemical parameters, vitamin C content, phenolic compounds, flavonoids and carotenoids, fatty acid profile and antioxidant activity of fruits from different regions of Brazil. We observed that the different regions and fruits studied presented very distinct characteristics. For example, the cupuaçu pit is rich in unsaturated fatty acids, while the genipap and java plum presented high flavonoid content and the butia had a high concentration of carotenoids. Guava was the fruit with the highest antioxidant activity through the ABTS radical, while the yellow mombim presented the best response when the activity was determined by FRAP.
Es importante determinar la composición química de las frutas para establecer sus potenciales beneficios para la salud humana y, por lo tanto, estimular su cultivo y consumo. El objetivo de este estudio fue determinar parámetros físicos y químicos, el contenido de vitamina C, los compuestos fenólicos, los flavonoides y los carotenoides, el perfil de ácidos grasos y la actividad antioxidante de las frutas de diferentes regiones de Brasil. De los resultados obtenidos en este estudio se pudo observar que las diferentes regiones y frutas estudiadas presentaban características muy distintas, ya que la semilla de cupuaçu es rica en ácidos grasos insaturados, mientras que el genipapo y la ciruela java presentaron un alto contenido de flavonoides y el butia presentó alta concentración de carotenoides. La guayaba fue la fruta con la mayor actividad antioxidante determinada por el radical ABTS, mientras que el mombim amarillo presentó la mejor respuesta cuando la actividad fue determinada por FRAP
Subject(s)
Phytochemicals/analysis , Fruit/chemistry , Antioxidants/chemistry , Ascorbic Acid/analysis , Brazil , Carotenoids/analysis , Phenolic Compounds/analysis , Fatty Acids/analysisABSTRACT
The genus Lindera consists of approximately 100 species that are widely distributed in tropical and subtropical areas throughout the world. Most Lindera plants, particularly Lindera aggregata is a well-known traditional Chinese medicine that has important medicinal value and health benefits. Contemporary chemical and pharmacological studies have shown that L. aggregata are a source of structurally diverse molecules having pharmacological potential. In an effort to promote research on L. aggregata and develop therapeutic and pharmacological products, this review describes the structural diversity of its components and pharmacological and biological significance of L. aggregata. This review is based on a literature analysis of scientific journals from electronic sources, such as Science Direct, PubMed, Google Scholar, Scopus and Web of Science. Thus, with the growing interest in traditional medicine and botanical drugs worldwide, L. aggregata will increasingly capture chemists' and pharmacologists' attention because they produce diverse and structurally novel compounds having pharmacological significance.
El género Lindera consta de aproximadamente 100 especies que están ampliamente distribuidas en áreas tropicales y subtropicales en todo el mundo. La mayoría de las plantas de Lindera, particularmente Lindera aggregata, es parte conocida de la medicina tradicional china con un importante valor medicinal y beneficios para la salud. Estudios químicos y farmacológicos contemporáneos han demostrado que L. aggregata es una fuente de moléculas estructuralmente diversas que con potencial farmacológico. En un esfuerzo por promover la investigación sobre L. aggregata y desarrollar productos terapéuticos y farmacológicos, esta revisión describe la diversidad estructural de sus componentes y la importancia farmacológica y biológica de L. aggregata. Esta revisión se basa en un análisis de literatura de revistas científicas de fuentes electrónicas, como Science Direct, PubMed, Google Scholar, Scopus y Web of Science. Por lo tanto, con el creciente interés en la medicina tradicional y las drogas botánicas en todo el mundo, L. aggregata captará cada vez más la atención de los químicos y farmacólogos debido a que producen compuestos diversos y estructuralmente novedosos que tienen importancia farmacológica.
Subject(s)
Biological Products , Lindera/chemistry , Phytochemicals/analysis , Sesquiterpenes/analysis , Oils, Volatile/chemistry , Lauraceae/chemistry , Alkaloids/analysis , Phenolic Compounds/analysis , Phytotherapy , Medicine, TraditionalABSTRACT
Abstract Thevetia peruviana is an ornamental shrub grown-up in many tropical region of the world. This plant produces secondary metabolites with biological properties of interest for the pharmaceutical industry. The objective was to determine the secondary metabolites profile of callus and cell suspension cultures of T. peruviana and compare them with those from explant (fruit pulp). Extracts in 50% aqueous ethanol and ethyl acetate were prepared. The phytochemical analysis was performed using standard chemical tests and thin layer chromatography. In addition, total phenolic and flavonoids compounds (TPC and TFC), total cardiac glycosides (TCG) and total antioxidant activity (TAA) was determined during the cell suspension growth. Phenolic chemical profile was also analyzed by high performance liquid chromatography (HPLC). Common metabolites (alkaloids, amino acids, antioxidants, cardiac glycosides, leucoanthocyanidins, flavonoids, phenols, sugars and triterpenes) were detected in all samples. The maximum production of extracellular TCG, TPC, TFC and TAA in cells suspensions were at 6-12 days; in contrast, intracellular content was relatively constant during the exponential grown phase (0 to 12-days). HPLC analysis detected one compound with retention time at 11.6 min; this compound was tentatively identified as dihydroquercetin, a flavonoid with anti-cancer properties. These results provide evidence on the utility of the in vitro cell cultures of T. peruviana for valuable pharmaceutical compounds production.
Subject(s)
Cells, Cultured , Thevetia/cytology , Phytochemicals/biosynthesis , Triterpenes , Flavonoids , Chromatography, High Pressure Liquid , Anticarcinogenic Agents , Thevetia/chemistry , Culture Techniques , Phytochemicals/analysis , AntioxidantsABSTRACT
Dengue fever has emerged as a big threat to human health since the last decade owing to high morbidity with considerable mortalities. The proposed study aims at the in silico investigation of the inhibitory action against DENV4-NS1 of phytochemicals from two local medicinal plants of Pakistan. Non-Structural Protein 1 of Dengue Virus 4 (DENV4-NS1) is known to be involved in the replication and maturation of viron in the host cells. A total of 129 phytochemicals (50 from Tanacetum parthenium and 79 from Silybum marianum) were selected for this study. The tertiary structure of DENV4-NS1 was predicted based on homology modelling using Modeller 9.18 and the structural stability was evaluated using molecular dynamics simulations. Absorption, distribution, metabolism, excretion and toxicity (ADMET) along with the drug-likeness was also predicted for these phytochemicals using SwissADME and PreADMET servers. The results of ADMET and drug-likeness predictions exhibited that 54 phytochemicals i.e. 25 from Tanacetum parthenium and 29 from Silybum marianum showed effective druglikeness. These phytochemicals were docked against DENV4-NS1 using AutoDock Vina and 18 most suitable phytochemicals with binding affinities ≤ -6.0 kcal/mol were selected as potential inhibitors for DENV4-NS1. Proposed study also exploits the novel inhibitory action of Jaceidin, Centaureidin, Artecanin, Secotanaparthenolide, Artematin, Schizolaenone B, Isopomiferin, 6, 8-Diprenyleriodictyol, and Anthraxin against dengue virus. It is concluded that the screened 18 phytochemicals have strong inhibition potential against Dengue Virus 4.
Subject(s)
Computer Simulation , Proteins/classification , Dengue , Dengue Virus , Phytochemicals/analysis , Plants, Medicinal/metabolism , Pharmacokinetics , Tanacetum parthenium/adverse effects , Molecular Dynamics SimulationABSTRACT
Sólo un 30% de los hogares en México, presentan seguridad alimentaria, es decir, un gran porcentaje de los hogares y por ende de la población no satisfacen las necesidades básicas diarias de macro y micronutrimentos. Los quelites, que se definen como plantas silvestres comestibles (hojas, tallos y flores) son una fuente accesible, continua, económica y adecuada de nutrimentos. Sin embargo, su consumo ha disminuido por modificaciones en las preferencias alimentarias, derivadas de los cambios en estilos de vida. El objetivo del presente trabajo fue valorizar a los quelites como fuente de alimento. Los quelites, aportan proteínas, aminoácidos, minerales (Ca, Mg, Zn), vitaminas (E, C) y fibra. Además, son una excelente fuente de compuestos bioactivos, como ácidos fenólicos (ácido cafeico, ferúlico) y flavonoides (quercetina, kaempferol, espinacetina), carotenoides, ácido α-linolénico y betalainas, que presentan elevada actividad antioxidante. Su consumo habitual se ha relacionado con beneficios a la salud, tales como efectos antitumorales, antihiperlipidémicos y antidiabéticos. Los quelites, además de estar disponibles en forma silvestre, forman parte de las tradiciones culinarias de México, incorporados de forma cruda y cocida en los platillos regionales. Por lo tanto, la revalorización y reincorporación de los quelites en la dieta, puede coadyuvar a cubrir las necesidades nutrimentales, en poblaciones con poco acceso o inseguridad alimentaria, además de contribuir a proporcionar efectos adicionales a través de sus compuestos bioactivos.
Only 30% of households in Mexico present food security, which means a large percentage of households and the population does not meet their needs in terms of macro and micronutrients. Thus, quelites, which are defined as wild edible plants, are an accessible, continuous, economical and adequate source of nutrients. However, quelite consumption in Mexico has been decreasing in response to changes in food preferences and lifestyles, including increased exposure to hypercaloric foods. Therefore, the aim of this work was to discuss the value of quelites as a food source rich in nutrients, proteins, amino acids, minerals (Ca, Mg, Zn), vitamins (E, C) and fiber. We also discuss how quelites are good source of bioactive compounds, such as phenolic acids (caffeic acid, ferulic acid) and flavonoids (quercetin, kaempferol, spinacetin), carotenoids, α-linolenic acid and betalaines. There use have been mainly related to the anti-tumor, antihyperlipidemic and antidiabetic benefits. We further discuss topics related to the culinary traditions of Mexico and the incorporation of quelites in the raw and cooked form in regional markets. The revaluation and the reincorporation of quelites in the diet can help meet nutritional needs, in addition to possibly providing additional health benefits.
Subject(s)
Humans , Plants, Edible , Chenopodium/chemistry , Portulaca/chemistry , Phytochemicals/analysis , Plants, Medicinal , Food Supply , MexicoABSTRACT
Neurolaena lobata (L.) R.Br. ex Cass. (Asteraceae)Is a popular folk remedy for in Central America. The plant is of commercial value in Guatemala but so far there is not any monograph to guide regional laboratories on ensuring identity and chemical tests for this species. As identity test we here run macro and micro morphoanatomical studies of the characters of the vegetative organs. We also developed standard chemical tests for quality by both TLC and HPLC for infusions and tinctures of varying alcoholic strength. Their radical scavenging activities in DPPH and NO were also measured. Macro and micro morphoanatomical characters of the vegetative organs present a set of characteristics to facilitate the identification of dry powdered samples of this species. We developed optimal conditions for the TLC and HPLC phytochemical fingerprints of the 4 most common pharmacopoeial liquid herbal preparations from this herbal drug, namely infusion, 70%, 45% and 20% hydroalcoholic tinctures. Our work provides the Latin-American industry with a set of analyses to establish the identity and chemistry of N. lobata samples for quality control purposes.
Neurolaena lobata (L.) R.Br. ex cass. (Asteraceae) es un remedio popular popular en AmeÌrica Central. La planta tiene un valor comercial en Guatemala, pero hasta el momento no existe una monografiÌa que guiÌe a los laboratorios regionales para garantizar la identidad y las pruebas quiÌmicas para esta especie. Como prueba de identidad proponemos estudios macro y micro morfoanatoÌmicos de los caracteres de los oÌrganos vegetativos. TambieÌn desarrollamos pruebas quiÌmicas de calidad mediante CCF y CLAR para infusiones y tinturas de grado alcohoÌlico variable. TambieÌn se midieron sus actividades de captacioÌn de radicales en DPPH y NO. Los caracteres macro y micro morfoanatoÌmicos de los oÌrganos vegetativos presentan un conjunto de caracteriÌsticas para facilitar la identificacioÌn de muestras de polvo seco de esta especie. Desarrollamos condiciones oÌptimas para las huellas dactilares fitoquiÌmicas de CCF y CLAR de las 4 preparaciones herbales liÌquidas farmacopeÌicas maÌs comunes de esta droga herbal, a saber, infusioÌn, 70%, 45% y 20% tinturas hidroalcohoÌlicas. Nuestro trabajo proporciona a la industria latinoamericana un conjunto de anaÌlisis base para establecer la identidad y la quiÌmica de las muestras de N. lobata con fines de control de calidad.
Subject(s)
Asteraceae/anatomy & histology , Asteraceae/chemistry , Phytochemicals/analysis , Quality Control , Spectrophotometry, Ultraviolet , Free Radical Scavengers , Chromatography, High Pressure Liquid , Chromatography, Thin Layer , Asteraceae/ultrastructure , Guatemala , MicroscopyABSTRACT
Abstract The expression of chemical compounds by individual plants of the same species in different locations may be affected by abiotic factors resulting in differences in the production of allelopathic compounds. The objective of this study was to compare the phytochemical profiles of plant species from two different forest formations in the state of Paraná, Brazil. The forest formations were Seasonal Semideciduous Forest (SSF) and Lowland Ombrophilous Dense Forest (LODF), and the five study species were Jacaranda micrantha, Cecropia pachystachya, Mimosa bimucronata, Schinus terebinthifolius and Cedrela fissilis. Secondary metabolites were extracted by exhaustive extraction with methanol, and the crude extract was fractionated using column chromatography. The fractions were used to calculate the retention factor of the main compounds using thin layer chromatography and phytochemical tests. The classes of compounds identified were practically the same among the analyzed species, however, at different levels of concentration. The type of tannins found in S. terebinthifolius differed between the two forest formations.
Resumo A expressão de compostos químicos de uma mesma espécie pode ser afetada e diferenciada pelos fatores abióticos, resultando em respostas alelopáticas diferenciadas. O objetivo deste trabalho foi comparar o perfil químico de espécies provenientes de duas Formações Florestais do Estado do Paraná. As formações foram a Floresta Estacional Semidecidual e Floresta Ombrófila Densa, sendo as espécies escolhidas: Jacaranda micrantha, Cecropia pachystachya, Mimosa bimucronata, Schinus terebinthifolius e Cedrela fissilis. Foi realizada extração exaustiva dos metabólitos secundários com metanol e o extrato bruto fracionado em coluna cromatográfica. As frações foram utilizadas para calcular o fator de retenção dos constituintes principais empregando cromatografia em camada delgada e para realizar testes fitoquímicos. As classes de compostos identificados foram praticamente as mesmas entre as espécies analisadas, porém, em diferentes níveis de concentração. O tipo de tanino encontrado em S. terebinthifolius foi diferente entre as duas formações florestais.
Subject(s)
Plants/classification , Plants/chemistry , Plant Extracts/analysis , Plant Extracts/chemistry , Forests , Phytochemicals/analysis , BrazilABSTRACT
A Cúrcuma (Curcuma longa) é uma planta originária do sudoeste asiático, que faz parte da família Zingiberaceae. É uma erva amarga, adstringente, com cheiro característico e forte cor amarela e que cujas raízes (rizomas) secas e maceradas têm sido utilizadas atualmente como corante e condimento para carnes e vegetais. O principal composto bioativo da cúrcuma é a curcumina, que se encontra em percentuais de dois a cinco por cento em suas raízes, sendo também é responsável pela sua coloração. Sabendo-se das suas propriedades bioativas e de várias que ainda estão sendo testadas, esse trabalho objetivou apresentar as principais propriedades e usos da cúrcuma. Historicamente a cúrcuma é empregada em diversos medicamentos utilizados pela medicina Ayurveda (sistema medicinal característico da Índia Antiga). Quimicamente é um pó insolúvel na água e no éter etílico, mas solúvel no etanol e acetona, é um diferoilmetano com a fórmula C21H20O6 e peso molecular 368,4. Muitos trabalhos estão sendo produzidos ultimamente buscando entender o funcionamento metabólico da curcumina e suas possíveis atividades biológicas. Entre as propriedades já estudadas destacam-se as capacidades anticoagulante, antifúngica, anti-inflamatória, antimalárica, antioxidante, antiviral, cicatrizante, esquistossomicida, hipolipemiante, leishmanicida, nematocida, tripanocida neuroprotetora, anti-amiloidogênica e imunomoduladora. A curcumina possui a vantagem de ser uma molécula de fácil acesso, uma vez que pode ser adquirida como condimento doméstico em todo o mundo e possui variadas aplicações, porém devido a sua baixa biodisponibilidade, baixa solubilidade em água e alta afinidade pelas proteínas plasmáticas faz-se necessário que novos estudos sejam realizados para que ela possa ser empregada efetivamente como um bioativo vegetal.(AU)
Turmeric (Curcuma longa) is a plant originated from Southeast Asia; it belongs to the Zingiberaceae family. It is a bitter, astringent herb, with a characteristic smell and strong yellow color. Its dried and macerated roots (rhizomes) have been used as coloring and condiment for meat and vegetables. Turmeric main bioactive compound is curcumin, which is found at concentrations of approximately two to five percent on its roots, being also responsible for its coloration. With the knowledge of its bioactive properties and of several other properties that are still being tested, this paper aimed at presenting the main properties and uses of turmeric. Turmeric has historically been used in various medicines by Ayurveda medicine (a medicinal system characteristic of ancient India). Chemically, it is a powder insoluble in either water or ethyl ether, despite being soluble in ethanol and acetone. It is a difoylmethane of formula C21H20O6 and molecular weight 368.4. Many works are being produced seeking to understand the metabolic functioning of curcumin and its possible biological activities. Among the properties already studied, it has proven anticoagulant, antifungal, anti-inflammatory, antimalarial, antioxidant, antiviral, scarring, schistosomicide, hypolipidemic, leishmanicidal, nematocidal, trypanocidal neuroprotective, anti-amyloidogenic and immunomodulatory capacities. Curcumin has the advantage of being an easily accessible molecule as it can be purchased as a domestic condiment worldwide and is widely applied in several cuisines. However, due to its low bioavailability, low water solubility and high affinity for plasma proteins, further studies should be carried out so that it can be effectively employed as a plant bioactive.(AU)
La cúrcuma (Curcuma longa) es una planta originaria del sudeste asiático, pertenece a la familia Zingiberaceae. Es una hierba amarga y astringente, con un olor característico y un fuerte color amarillo y cuyas raíces (rizomas) secas y maceradas se utilizan actualmente como colorante y condimento para carnes y vegetales. El principal compuesto bioactivo de la cúrcuma es la curcumina, que se encuentra cerca del dos al cinco por ciento de sus raíces y también es responsable por su coloración. Debido a sus propiedades bioactivas y de varias que aún se están probando, ese estudio tuvo como objetivo presentar las principales propiedades y usos de la cúrcuma. Históricamente, la cúrcuma es empleada en varias medicinas utilizadas por la medicina Ayurveda (sistema medicinal característico de la antigua India). Químicamente es un polvo insoluble en agua y éter etílico, pero soluble en etanol y acetona, es un diferoilmetano de fórmula C21H20O6 y peso molecular 368.4. Últimamente se están produciendo muchos trabajos que buscan comprender el funcionamiento metabólico de la curcumina y sus posibles actividades biológicas. Entre las propiedades ya estudiadas se encuentran las capacidades anticoagulante, antifúngica, antiinflamatoria, antipalúdica, antioxidante, antiviral, cicatrizante, esquistosomicida, hipolipidémica, leishmanicida, nematocida, tripanocida, neuroprotectora, antiamiloidogénica e inmunomoduladora. La curcumina tiene la ventaja de ser una molécula de fácil acceso, ya que se puede comprar como condimento doméstico en todo el mundo y tiene una variedad de aplicaciones, pero debido a su baja biodisponibilidad, baja solubilidad en agua y alta afinidad por las proteínas plasmáticas se hace necesario que nuevos estudios sean llevados a cabo para que ella pueda ser empleada efectivamente como planta bioactiva.(AU)
Subject(s)
Curcumin/analysis , Curcuma/classification , Curcuma/chemistry , Phytochemicals/analysisABSTRACT
Abstract The present study aims to evaluate the influence of extraction methods on the quality of bioactive compounds and antioxidant capacity in Pterodon emarginatusVogel (sucupira) oils. The oils were extracted from the sucupira seeds by Soxhlet and by the extraction system of Bligh & Dyer. The oils were analyzed as to fatty acid profile, tocopherols, phytosterols, carotenoids, total phenolics, and total antioxidant capacity. The extraction by Soxhlet showed better yield of total lipids and was more efficient to extract tocopherols, phytosterols, and carotenoids, besides presenting better antioxidant activity by DPPH•. However, this method showed insufficient capacity to extract the polar lipid components of the sample, as evidenced by the low results of total phenolic compounds. On the other hand, the Bligh & Dyer method preserved the fatty acid profile and was also effective to extract higher phenolic compounds content and presented superior antioxidant activity when assessed by FRAP, ABTS•+, and oxidative stability index.
Subject(s)
Phytochemicals/analysis , Antioxidants , Chromatography/instrumentation , OxidationABSTRACT
RESUMEN Objetivo Evaluar el efecto analgésico del extracto etanólico de las hojas de Pereskia lychnidiflora, la prospección de metabolitos secundarios y el análisis toxicológico. Materiales y métodos La actividad analgésica fue evaluada mediante la prueba del ácido acético y la formalina en ratones NIH a una concentración de 30, 50 y 100 mg/kg de peso corporal, utilizando como control Ibuprofeno a 200 mg/kg y agua destilada como blanco. La prospección de metabolitos secundarios se realizó por el método de cromatografía de capa fina y la toxicidad del extracto fue evaluada in vivo según la dosis máxima de 2000 mg/kg de peso corporal. Resultados La prospección fitoquímica determinó la presencia de alcaloides, taninos, triterpenos y esteroles como mayores constituyentes químicos. Se determinó que el extracto etanólico de Pereskia lychnidiflora posee una actividad analgésica similar al Ibuprofeno. No se observaron signos de toxicidad en los ratones de experimentación y se clasifica el extracto como no tóxico con una DL50 mayor de 2000 mg/kg. Conclusión El extracto etanólico de Pereskia lychnidiflora tiene un efecto analgésico antiinflamatorio que podría estar condicionado por la presencia de alcaloides, taninos y esteroles (terpenoides) presentes en esta especie vegetal y puede ser clasificado como no tóxico.
ABSTRACT Objective To evaluate the analgesic effect of the ethanolic extract of the leaves of Pereskia lychnidiflora, the prospection of secondary metabolites and the toxicologic analysis. Materials and Methods Analgesic activity was evaluated by testing acetic acid and formalin in NIH mice at a concentration of 30, 50 and 100 mg/kg body weight, using Ibuprofen control at 200 mg/kg and distilled water as the target. Secondary metabolites were prospected using the thin layer chromatography method and the toxicity of the extract was evaluated in vivo according to the maximum dose of 2,000 mg/kg body weight. Results Phytochemical prospecting determined the presence of alkaloids, tannins, triterpenes, and sterols as major chemical constituents. The ethanolic extract of Pereskia lychnidiflora was found to have an analgesic activity similar to ibuprofen. No signs of toxicity were observed in the experimental mice and the extract is classified as non-toxic with a DL50 greater than 2,000 mg/kg. Conclusions The ethanolic extract of Pereskia lychnidiflora has an anti- inflammatory analgesic effect that could be conditioned by the presence of alkaloids, tannins, and sterols (terpenoids) present in this species and can be classified as non-toxic.
Subject(s)
Animals , Male , Mice , Plant Extracts/toxicity , Plant Extracts/therapeutic use , Plant Leaves/chemistry , Cactaceae , Analgesia , Analgesics/toxicity , Analgesics/therapeutic use , Phytotherapy , Plant Extracts/pharmacology , Plant Extracts/chemistry , Ethanol , Phytochemicals/analysis , Analgesics/pharmacology , Analgesics/chemistryABSTRACT
Abstract This work describes the preliminary evaluation of cytotoxic, antimicrobial, molluscicidal, antioxidant and anticholinesterase activities from leaf (LECF) and stem bark alcoholic extracts (BECF) of the species Croton floribundus Spreng. (Euphorbiaceae), popularly known as capixingui or tapixingui. BECF presented significant toxicity (LC50 = 89.6 μg/ml) in the Artemia salina Leach, 1819 (Crustacea: Branchiopoda) bioassay, whereas LECF did not show activity (LC50 > 1000 μg/ml). From DPPH method, the values of IC50 for the LECF and BECF were 61.2 μg/ml and 62.2 μg/ml, respectively, showing that C. floribundus has an expressive antioxidant activity. Antimicrobial susceptibility was evaluated by microdilution technique and only BECF was active against Staphylococcus aureus (MIC = 39.6 μg/ml). The extracts did not present molluscicidal activity against snail Biomphalaria glabrata Say, 1818 (Gastropoda: Planorbidae). Both extracts revealed the presence of several components with an inhibiting capacity of acetylcholinesterase enzyme on the bioautographic assay. C. floribundus showed to be a promising species considering that it exhibited good biological activity in the most assays performed.
Resumo Este trabalho descreve a avaliação preliminar das atividades citotóxica, antimicrobiana, moluscicida, antioxidante e anticolinesterásica de extratos alcoólicos das folhas (LECF) e das cascas do caule (BECF) da espécie Croton floribundus Spreng. (Euphorbiaceae), popularmente conhecida como capixingui ou tapixingui. No bioensaio com Artemia salina Leach, 1819 (Crustacea: Branchiopoda), BECF apresentou toxicidade significante (LC50 = 89,6 µg/ml), enquanto que LECF não apresentou atividade (LC50 > 1000 µg/ml). A partir do método de DPPH, os valores de IC50 para o LECF e BECF foram 61,2 µg/ml e 62,2 µg/ml, respectivamente, evidenciando que C. floribundus tem uma atividade antioxidante expressiva. A susceptibilidade antimicrobiana foi avaliada pela técnica de microdiluição e apenas BECF foi ativo contra Staphylococcus aureus (MIC = 39,6 mg/ml). Os extratos não apresentaram atividade moluscicida contra o caramujo Biomphalaria glabrata Say, 1818 (Gastropoda: Planorbidae). Ambos os extratos revelaram a presença de componentes com capacidade inibidora da enzima acetilcolinesterase no ensaio bioautográfico. C. floribundus mostrou ser uma espécie promissora considerando que exibiu boa atividade biológica na maioria dos ensaios testados.