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Anredera cordifolia (Ten.) Steenis is a vine species native to Brazil that is considered an unconventional food plant and a medicinal species whose phenolic compounds exert antioxidant activity. Since the production of metabolites is determined by environmental factors and leaf maturity, it is important to track these changes in order to determine the best time to harvest. This study aimed to verify whether leaf phenology and seasonality cause variations in the amount of phenolic compounds and in the antioxidant activity of this species. The leaves were collected in different seasons between September 2018 and April 2019, and separated according to maturity: young, mature, and senescent. Daily atmospheric temperature and rainfall data were used to characterize the collection period. The total phenolic content (TPC), determined by Folin-Ciocalteu method, was significantly higher in the young leaves collected in winter, a season of lower temperatures. These leaves showed 54.4 mg of gallic acid equivalents per 100 g of dry matter (mg GAE 100 g-1DM). Other results averaged 25.6 mg GAE 100 g-1DM. The highest antioxidant activity, assessed via the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method, regardless of leaf phenology, was observed in leaves harvested in autumn (73.7%) and winter (71.1%), seasons with lower rainfall. Leaves harvested in summer and spring had lower antioxidant action rates (54.3 e 37.5%, respectively). There was no significant correlation between the total phenolic content and antioxidant activity. Thus, the phenolic composition of A. cordifolia, and consequently its activity on free radicals, varies seasonally in response to temperature and rainfall, and may or may not interact with the age of the leaves.
Anredera cordifolia (Ten.) Steenis é uma trepadeira nativa do Brasil considerada uma planta alimentícia não convencional e uma espécie medicinal, cujos compostos fenólicos exercem ação antioxidante. Como a produção de metabólitos é determinada por fatores ambientais e pela maturidade das folhas, é importante acompanhar essas mudanças a fim de determinar a época de colheita. Neste estudo objetivou-se verificar se a fenologia foliar e a sazonalidade ocasionam variação na quantidade de compostos fenólicos e na ação antioxidante dessa espécie. As folhas foram coletadas em diferentes estações, entre setembro de 2018 e abril de 2019, e separadas conforme a maturidade: jovens, maduras e senescentes. Os dados diários de temperatura atmosférica e pluviosidade foram usados para caracterizar o período de coleta. O conteúdo de fenólicos totais (TPC), determinado pelo método Folin-Ciocalteu, foi significativamente maior nas folhas jovens coletadas no inverno, período caracterizado por temperaturas mais baixas. Estas folhas apresentaram 54,4 mg equivalentes de ácido gálico por 100 g de matéria seca (mg GAE 100 g-1DM) . A média dos outros resultados foi de 25,6 mg GAE 100 g-1DM. A maior ação antioxidante, avaliada pelo método do radical livre 2,2-difenil-1-picrilhidrazil (DPPH), foi observada em folhas colhidas no outono (73,7%) e inverno (71,1%), independentemente da fenologia foliar. Nestes períodos a pluviosidade foi menor. Folhas colhidas no verão e na primavera apresentaram menores percentuais de ação antioxidante (54,3 e 37,5%, respectivamente). Não houve correlação significativa entre o conteúdo de fenólicos totais e a atividade antioxidante. Conclui-se que a composição fenólica de A. cordifolia e, consequentemente, sua ação sobre radicais livres, varia sazonalmente em resposta à temperatura e pluviosidade, podendo ou não interagir com a idade das folhas.
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Plantas Medicinais/crescimento & desenvolvimento , Estações do Ano , Compostos Fenólicos , AntioxidantesRESUMO
Salvia lachnostachys Benth is native to Brazil and has anti-inflammatory, anti-arthritic, cytotoxic, antitumor, and antihyperalgesic activities. The population, including pregnant women, consume this plant to treat pain, inflammation, flu, spasms, insomnia, and depression, mainly. There are no safety reports on the use of this plant during pregnancy. The present study aimed to evaluate the effects of S. lachnostachys ethanolic extract (EESl) on reproductive performance, embryofetal development, and DNA integrity of pregnant female mice. Pregnant females were randomly divided into three experimental groups (n = 10): The Control group was treated with a vehicle, and treatment groups were administered with EESl at 100 and 1000 mg/kg, respectively. Treatment occurred by gavage throughout the gestational period until day 18. Afterward, reproductive performance, embryofetal development, and DNA integrity parameters were evaluated. The results indicated that EESl did not alter any reproductive performance parameters. However, it changed embryofetal outcome through reduced placental weight (EESl 100 mg/kg), decreased fetal weight (EESl 100 and 1000 mg/kg), and increased frequency of small for gestational age fetuses (EESl 1000 mg/kg). In addition, EES1 increased the frequency of external, visceral, and skeletal malformations. Because of the above, it is considered that EESl is not maternotoxic, does not alter reproductive performance, but does alter embryofetal development. Its use in the gestational period is not indicated due to its teratogenic potential.
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Salvia , Teratógenos , Humanos , Gravidez , Feminino , Camundongos , Animais , Placenta , Etanol , Extratos Vegetais/toxicidade , DNARESUMO
Baccharis vulneraria Baker is used popularly for the treatment of skin infections. So, this study aimed investigate the antimicrobial activity and chemical characterization of the essential oil (EO) against microorganisms that cause cutaneous infections. The EO was analyzed by GC-MS. The antimicrobial test was performed using the serial microdilution method, and the antimicrobial activity was determined by the minimum inhibitory concentration against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, Trichophyton interdigitale, Trichophyton rubrum, Fusarium solani and Fusarium oxysporum within the 32-0.0625 mg/mL concentration range. Were identified 31 EO compounds. Its major compounds are bicyclogermacrene, trans-cadin-1,4-diene, ß-caryophyllene, and germacrene A. EO showed antifungal action against T. rubrum and T. interdigitale (2 and 4 mg/mL MIC, respectively). The growth of C. albicans, at 4 mg/mL, decreased by 50% compared to control. The oil had no significant potential for other microorganisms at the selected concentrations.
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Introduction: Tinospora smilacina is a native plant used in traditional medicine by First Nations peoples in Australia to treat inflammation. In our previous study, an optimised Calophyllum inophyllum seed oil (CSO) nanoemulsion (NE) showed improved biomedical activities such as antimicrobial, antioxidant activity, cell viability and in vitro wound healing efficacy compared to CSO. Methods: In this study, a stable NE formulation combining T. smilacina water extract (TSWE) and CSO in a nanoemulsion (CTNE) was prepared to integrate the bioactive compounds in both native plants and improve wound healing efficacy. D-optimal mixture design was used to optimise the physicochemical characteristics of the CTNE, including droplet size and polydispersity index (PDI). Cell viability and in vitro wound healing studies were done in the presence of CTNE, TSWE and CSO against a clone of baby hamster kidney fibroblasts (BHK-21 cell clone BSR-T7/5). Results: The optimised CTNE had a 24 ± 5 nm particle size and 0.21± 0.02 PDI value and was stable after four weeks each at 4 °C and room temperature. According to the results, incorporating TSWE into CTNE improved its antioxidant activity, cell viability, and ability to promote wound healing. The study also revealed that TSWE has >6% higher antioxidant activity than CSO. While CTNE did not significantly impact mammalian cell viability, it exhibited wound-healing properties in the BSR cell line during in vitro testing. These findings suggest that adding TSWE may enhance CTNE's potential as a wound-healing treatment. Conclusion: This is the first study demonstrating NE formulation in which two different plant extracts were used in the aqueous and oil phases with improved biomedical activities.
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Margaritaria nobilis L.f. (Phyllanthaceae), a native Brazilian tree occurring mainly in the Amazon, is used in folk medicine for the treatment of abscesses (bark) and cancer-like symptoms (leaves). The present study evaluates the safety of its acute oral administration and its effects on nociception and plasma leakage. The chemical constitution of the leaf's ethanolic extract is determined by ultra-performance liquid chromatography-high-resolution mass spectrometry (LC-MS. Its acute oral toxicity is evaluated in female rats at a dose of 2000 mg/kg, evaluating the occurrence of deaths and Hippocratic, behavioral, hematological, biochemical, and histopathological changes, as well as food and water consumption and weight gain. Antinociceptive activity is evaluated in male mice with acetic-acid-induced peritonitis (APT) and formalin (FT) tests. An open field (OF) test is performed to verify possible interferences in the animals' consciousness or locomotion. LC-MS analysis shows the presence of 44 compounds classified as phenolic acid derivatives, flavonoids and O-glycosylated derivatives, and hydrolyzable tannins. No deaths or significant behavioral, histological, or biochemical changes are observed in the toxicity assessment. In nociception tests, M. nobilis extract significantly reduces abdominal contortions in APT, demonstrating selectivity for inflammatory components (FT second phase), not interfering in neuropathic components (FT first phase) or consciousness and locomotion levels in OF. Additionally, M. nobilis extract inhibits plasma acetic-acid-induced leakage. These data demonstrate the low toxicity of M. nobilis ethanolic extract, as well as its effectiveness in modulating inflammatory nociception and plasma leakage, possibly related to the flavonoids and tannins present in its composition.
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The mitochondria have an important role in modulating cell cycle progression, cell survival, and apoptosis. In the adult heart, the cardiac mitochondria have a unique spatial arrangement and occupy nearly one-third the volume of a cardiomyocyte, being highly efficient for converting the products of glucose or fatty acid metabolism into adenosine triphosphate (ATP). In cardiomyocytes, the decline of mitochondrial function reduces ATP generation and increases the production of reactive oxygen species, which generates impaired heart function. This is because mitochondria play a key role in maintaining cytosolic calcium concentration and modulation of muscle contraction, as ATP is required to dissociate actin from myosin. Beyond that, mitochondria have a significant role in cardiomyocyte apoptosis because it is evident that patients who have cardiovascular diseases (CVDs) have increased mitochondrial DNA damage to the heart and aorta. Many studies have shown that natural products have mitochondria-modulating effects in cardiac diseases, determining them as potential candidates for new medicines. This review outlines the leading plant secondary metabolites and natural compounds derived from microorganisms as modulators of mitochondrial dysfunctions associated with CVDs.
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Produtos Biológicos , Doenças Cardiovasculares , Humanos , Doenças Cardiovasculares/metabolismo , Produtos Biológicos/farmacologia , Produtos Biológicos/uso terapêutico , Mitocôndrias/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Trifosfato de Adenosina , Miócitos Cardíacos/metabolismoRESUMO
Numerous natural compounds have been identified that are able to induce apoptosis in cancer cells. These compounds have various chemical properties and are found in medicinal plants, vegetables, and fruits that are commonly consumed by humans. Phenols represent important compounds, which have been demonstrated to induce apoptosis in cancer cells, and some of the involved mechanisms have also been determined. The most important and abundant phenolic compounds are tannins, caffeic acid, capsaicin, gallic acid, resveratrol, and curcumin. Induction of apoptosis with the least or no toxicity to natural tissues is one of the useful effects of many plant-based bioactive compounds. Phenols, with anticancer potency at different degrees, serve to induce apoptosis through different pathways, including both extrinsic (Fas) and intrinsic (calcium release, ROS increase, DNA degradation, and mitochondrial membrane impairment). In this review, we report these compounds and their apoptosis-inducing mechanisms. Apoptosis or programmed cell death is a precise and systematic mechanism that is aimed at removing damaged or abnormal cells and is very useful to control, treat, and prevent cancer. Apoptotic cells are characterized by specific morphological features and molecular expression. In addition to physiological stimuli, there are many external factors that can be useful for inducing apoptosis. Also, these compounds can affect the regulatory proteins of the apoptotic pathways, such as the apoptotic proteins (Bid and BAX) and antiapoptotic proteins (Bcl-2). Taking these compounds and their molecular mechanisms into account can help use them in combination with chemical drugs and develop new drugs.
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Apoptose , Leucemia , Humanos , Linhagem Celular , Proteínas Reguladoras de Apoptose/metabolismo , Proteínas Reguladoras de Apoptose/farmacologia , Ácido Gálico/farmacologiaRESUMO
Cancer is a major health problem with significant morbidity and mortality. In addition, plants are a source of metabolites with diverse biological properties, including antitumor potential. In this study, we investigated the in vitro murine lymphoma L5178Y-R cell growth inhibition, human peripheral blood mononuclear cells (PBMC) toxicity and proliferation, and antioxidant, hemolytic, and anti-hemolytic activities of methanol extracts from 15 plants of traditional use in Mexico. Justicia spicigera caused the highest tumor cell growth inhibition with a half maximal inhibitory concentration (IC50) of 29.10 µg/mL and a selectivity index >34.36 compared with those of PBMC, whereas Mimosa tenuiflora showed the highest lymphoproliferative activity from 200 µg/mL compared with that induced by concanavalin A. In addition, M. tenuiflora showed an antioxidant effect (IC50 = 2.86 µg/mL) higher than that of ascorbic acid. Regarding the hemolytic and anti-hemolytic activity, all extracts presented significant anti-hemolytic activity. The extract of J. spicigera is emerging as a possible source of effective antineoplastic compounds.
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Meadowsweet (Filipendula ulmaria (L.) Maxim.) has been widely used in the treatment of various diseases. The pharmacological properties of meadowsweet are derived from the presence of phenolic compounds of a diverse structure in sufficiently large quantities. The purpose of this study was to examine the vertical distribution of individual groups of phenolic compounds (total phenolics, flavonoids, hydroxycinnamic acids, catechins, proanthocyanidins, and tannins) and individual phenolic compounds in meadowsweet and to determine the antioxidant and antibacterial activity of extracts from various meadowsweet organs. It was found that the leaves, flowers, fruits, and roots of meadowsweet are characterized by a high total phenolics content (up to 65 mg g-1). A high content of flavonoids was determined in the upper leaves and flowers (117-167 mg g-1), with high contents of hydroxycinnamic acids in the upper leaves, flowers, and fruits (6.4-7.8 mg g-1); high contents of catechins and proanthocyanidins in the roots (45.1 and 3.4 mg g-1, respectively); and high tannin content in the fruits (38.3 mg g-1). Analysis of extracts by high-performance liquid chromatography (HPLC) showed that the qualitative and quantitative composition of individual phenolic compounds in various parts of the meadowsweet varied greatly. Among the flavonoids identified in meadowsweet, quercetin derivatives dominate, namely quercetin 3-O-rutinoside, quercetin 3-ß-d-glucoside, and quercetin 4'-O-glucoside. Quercetin 4'-O-glucoside (spiraeoside) was found only in the flowers and fruits. Catechin was identified in the leaves and roots of meadowsweet. The distribution of phenolic acids across the plant was also uneven. In the upper leaves, a higher content of chlorogenic acid was determined, and in the lower leaves, a higher content of ellagic acid determined. In flowers and fruits, a higher contents of gallic, caftaric, ellagic, and salicylic acids were noted. Ellagic and salicylic acids were also dominant among phenolic acids in the roots. Based on the results of the analysis of antioxidant activity in terms of the ability to utilize the radicals of 2,2-diphenyl-1-picrylhydrazine (DPPH) and 2,2'-azino-bis(3-ethylbenzthiazolino-6-sulfonic acid) (ABTS) and in terms of iron-reducing ability (FRAP), the upper leaves, flowers, and fruits of meadowsweet can be considered plant raw materials suitable to obtain extracts with high antioxidant activity. Extracts of plant fruits and flowers also showed high antibacterial activity against the bacteria Bacillus subtilis and Pseudomonas aeruginosa.
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Filipendula , Proantocianidinas , Antioxidantes/farmacologia , Antioxidantes/análise , Extratos Vegetais/química , Quercetina/análise , Filipendula/química , Ácidos Cumáricos , Taninos/análise , Flavonoides/química , Fenóis/química , Salicilatos , Antibacterianos/farmacologia , Antibacterianos/uso terapêuticoRESUMO
The immune system protects the body from infectious agents such as bacteria, viruses, or fungi. Once encountered with pathogens or antigens, the innate and adaptive arms of the immune system trigger a strong immune response to eliminate them from the system and protect the body. Thus, well-balanced immunity is pivotal for maintaining human health, as an insufficient level of immune defense leads to infections and tumors. In contrast, the excessive functioning of the immune system causes the development of autoimmune diseases and allergies. Strong immunity requires adequate nutrition, dietary interventions, and sufficient intake of certain vitamins (vitamin C, vitamin D, and folic acid) and minerals (magnesium, zinc, and selenium). Therefore, nutritional and micronutrient deficiencies lead to compromised immunity. Several natural ingredients have shown potent immunomodulatory properties. The immune-enhancing properties of many plants and fungi are due to containing bioactive phytoconstituents such as polyphenols, terpenoids, ß-glucans, vitamins, etc. Probiotics and prebiotics can be used as innovative tools to reduce intestinal inflammation and downregulate hypersensitivity reactions. Plant sources of melatonin, a multifunctional molecule with proven anti-inflammatory and immunomodulatory properties, have been discovered relatively recently. The bioactive compounds augment the immune response by directly increasing the cytotoxic activity of natural killer cells, macrophages, and neutrophils. Many phytoconstituents prevent cell damage due to their powerful antimicrobial, antioxidant, and anti-inflammatory properties. The present review attempts to understand the molecular mechanisms underlying the immune-enhancing properties of some bioactive compounds from plants, fungi, animals, microorganisms, and other natural sources.
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Echinops macrochaetus is a medicinal plant that can be used to cure various diseases. In the present study, plant-mediated zinc oxide nanoparticles (ZnO-NPs) were synthesized using an aqueous leaf extract of the medicinal plant Heliotropium bacciferum and characterized using various techniques. E. macrochaetus was collected from the wild and identified using the internal transcribed spacer sequence of nrDNA (ITS-nrDNA), which showed the closeness to its related genus in a phylogenetic tree. The effect of synthesized biogenic ZnO-NPs was studied on E. macrochaetus in a growth chamber for growth, bioactive compound enhancement and antioxidant system response. The irrigation of plants at a low concentration of ZnO-NPs (T1 = 10 mg/L) induced more growth in terms of biomass, chlorophyll content (273.11 µg/g FW) and carotenoid content (135.61 µg/g FW) than the control and other treatments (T2-20 mg/L and T3-40 mg/L). However, the application of a high concentration of ZnO-NPs (20 and 40 mg/L) increased the level of antioxidant enzymes (SOD, APX and GR), total crude and soluble protein, proline and TBARS contents. The accumulations of the compounds quercetin-3-ß-D-glucoside, luteolin 7-rutinoside and p-coumaric acid were greater in the leaf compared to the shoot and root. A minor variation was observed in genome size in treated plants as compared to the control group. Overall, this study revealed the stimulatory effect of phytomediated ZnO-NPs, which act as bio-stimulants/nano-fertilizers as revealed by more biomass and the higher production of phytochemical compounds in different parts of the E. macrochaetus.
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The demand for medicinal plants is on a rise due to their affordability, accessibility and relatively non-toxic nature. Combretum molle (Combretaceae) is used in African traditional medicine to treat a number of diseases. This study aimed to screen the phytochemical composition of the hexane, chloroform and methanol extracts of C. molle leaves and stems using qualitative phytochemical screening. Additionally, the study aimed to identify the functional phytochemical groups, determine the elemental composition and provide a fluorescence characterization of the powdered leaves and stems by performing Fourier transform infrared spectroscopy (FTIR), energy-dispersive X-ray (EDX) microanalyses and fluorescence microscopy. Phytochemical screening revealed the presence of alkaloids, flavonoids, phenolic compounds, polyphenols, terpenoids, tannins, coumarins, saponins, phytosterols, gums, mucilage, carbohydrates, amino acids and proteins within all leaf and stem extracts. Lipids and fixed oils were additionally present within the methanol extracts. FTIR demonstrated significant peaks in absorption frequency in the leaf at wavelengths of 3283.18, 2917.81, 1617.72, 1318.83, 1233.97, 1032.32 and 521.38 cm-1, and in the stem at 3318.91, 1619.25, 1317.13, 1032.68, 780.86 and 516.39 cm-1. These corresponded to the functional groups of chemical compounds including alcohols, phenols, primary amines, alkyl halides, alkanes and alkyl aryl ethers, corroborating the presence of the detected phytochemicals within the plant. EDX microanalyses showed the elemental composition of the powdered leaves (68.44% C, 26.72% O, 1.87% Ca, 0.96% Cl, 0.93% Mg, 0.71% K, 0.13% Na, 0.12 % Mn and 0.10% Rb) and stems (54.92% C, 42.86% O, 1.7% Ca, 0.43% Mg and 0.09% Mn). Fluorescence microscopy provided a characteristic evaluation of the plant in its powdered form and revealed distinct colour changes in the material when treated with various reagents and viewed under ultraviolet light. In conclusion, the phytochemical constituents of the leaves and stems of C. molle confirm the suitability of this species for use in traditional medicine. The findings from this study suggest the need to validate the use of C. molle in the development of modern medicines.
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Medicinal and herbal plants are abundant sources of phytochemicals, which are biologically active compounds with potential health benefits. The characterisation of phytochemicals has been the subject of many studies, but there is a lack of comprehensive assays to accurately assess the main phytochemical categories and their antioxidant properties. To address this, the present study has developed a multiparametric protocol comprising eight biochemical assays, which quantify the major categories of phytochemicals, including polyphenols, tannins and flavonoids, as well as their antioxidant and scavenging potential. The presented protocol offers several advantages over other methods, including higher sensitivity and significantly lower cost, making it a simpler and more affordable approach compared to commercial kits. The protocol was tested on two datasets with seventeen distinct herbal and medicinal plants, and the results demonstrated its effectiveness in accurately characterising the phytochemical composition of plant samples. The modular design of the protocol allows its adaptation to any spectrophotometric instrumentation, while all assays are simple to follow and require a minimum number of analytical steps.
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Liver problems are a worldwide concern, and conventional medicinal therapies are ineffective. Hence, safeguarding the healthy liver is vital for good health and well-being. Infections due to virus, immune problems, cancer, alcohol abuse, and an overdose of drugs are some of the causes of liver diseases. Antioxidants derived from medicinal plants and conventional dietary sources can protect the liver from damages caused by oxidative stress system and various chemicals. Plants and plant-derived phytochemicals are appealing hepatoprotective agents since they have less side effects and still there is a lot of interest shown in using herbal tonics for treating liver disorders. This review therefore primarily focuses on newly discovered medicinal plants and compounds produced from plants that fall under the classifications of flavonoids, alkaloids, terpenoids, polyphenolics, sterols, anthocyanins, and saponin glycosides, all of which have the potential to be hepatoprotective. Hosta plantaginea, Ligusticum chuanxiong, Daniella oliveri, Garcinia mangostana, Solanum melongena, Vaccinium myrtillus, Picrorhiza kurroa, and Citrus medica are some potential plants having hepatoprotective effects. We conclude that these phytochemicals and the plant extracts listed above are used in the future to treat a variety of liver diseases, additional research is still needed to develop safer and more potent phytochemical drugs.
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Hepatopatias , Plantas Medicinais , Plantas Medicinais/química , Fitoterapia , Antocianinas/uso terapêutico , Hepatopatias/tratamento farmacológico , Hepatopatias/prevenção & controle , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêuticoRESUMO
The role of intestinal barrier homeostasis in an individual's general well-being has been widely addressed by the scientific community. Colorectal cancer is among the illnesses that most affect this biological barrier. While chemotherapy is the first choice to treat this type of cancer, multidrug resistance (MDR) is the major setback against the commonly used drugs, with the ATP-binding cassette transporters (ABC transporters) being the major players. The role of P-glycoprotein (P-gp), multidrug resistance protein 1 (MRP1), or breast cancer resistance protein (ABCG2) in the efflux of chemotherapeutic drugs is well described in cancer cells, highlighting these proteins as interesting druggable targets to reverse MDR, decrease drug dosage, and consequently undesired toxicity. Natural products, especially phytochemicals, have a wide diversity of chemical structures, and some particular classes, such as phenolic acids, flavonoids, or pentacyclic triterpenoids, have been reported as inhibitors of P-gp, MRP1, and ABCG2, being able to sensitize cancer cells to chemotherapy drugs. Nevertheless, ABC transporters play a vital role in the cell's defense against xenobiotics, and some phytochemicals have also been shown to induce the transporters' activity. A balance must be obtained between xenobiotic efflux in non-tumor cells and bioaccumulation of chemotherapy drugs in cancer cells, in which ABC transporters are essential and natural products play a pivotal role that must be further analyzed. This review summarizes the knowledge concerning the nomenclature and function of ABC-transporters, emphasizing their role in the intestinal barrier cells. In addition, it also focuses on the role of natural products commonly found in food products, e.g., phytochemicals, as modulators of ABC-transporter activity and expression, which are promising nutraceutical molecules to formulate new drug combinations to overcome multidrug resistance.
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Identification of bioactive natural products from plants starts with the screening of extracts for a desired bioactivity such as antimicrobial, antifungal, anti-cancer, anti-inflammatory, or neuroprotective. When the bioactivity shows sufficient potency, the plant material is subjected to bio-activity-guided fractionation, which involves, e.g., sequential extraction followed by chromatographic separation, including HPLC. The bioactive compounds are then structurally identified by high-resolution mass spectrometry and nuclear magnetic resonance (NMR). One of the questions that come up during the purification process is how much of the bioactivity originally present in the crude extract is preserved during the purification process. If this is the case, it is interesting to investigate if the loss of total bioactivity is caused by the loss of material during purification or by the degradation or evaporation of potent compounds. A further possibility would be the loss of synergy between compounds present in the mixture, which disappears when the compounds are separated. In this publication, a novel formula is introduced that allows researchers to calculate total bioactivity in biological samples using experimental data from our research into the discovery of anti-inflammatory compounds from Backhousia myrtifolia (Grey Myrtle). The results presented show that a raw ethanolic extract retains slightly more bioactivity than the sum of all sequential extracts per gram of starting material and that-despite a large loss of material during HPLC purification-the total bioactivity in all purified fractions is retained, which is indicative of rather an additive than a synergistic principle.
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Anti-Infecciosos , Produtos Biológicos , Extratos Vegetais/química , Produtos Biológicos/química , Plantas , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologiaRESUMO
ETHNOPHARMACOLOGY RELEVANCE: Alstonia boonei De Wild. (stem bark), Anacardium occidentale L. (stem bark), Azadirachta indica A.Juss (leaves), Enantia chlorantha Oliv. (stem bark), Khaya senegalensis A.Juss (stem bark) Mangifera indica L. (stem bark), and Nauclea latifolia Sm. (stem bark) are used for treating malaria in southwest Nigeria. Surveys revealed that these plants are also employed for treating symptoms of malaria and cerebral malaria in the region. AIM OF THE STUDY: In this study, the effects of freeze-dried extracts of these plants were investigated on synthetic hemozoin (HZ)-induced neuroinflammation, neuronal damage, and increased permeability of brain microvascular endothelial cells. MATERIALS AND METHODS: Effects of freeze-dried plant extracts were investigated on neuroinflammation by measuring levels of pro-inflammatory mediators in culture supernatants, while in-cell western assays were used to measure protein levels of iNOS and NLRP3. Effects on HZ-induced neurotoxicity and ROS generation was measured using MTT and DCFDA assays, respectively. HZ-induced permeability of hCMEC/D3 endothelial cells was determined using the in vitro vascular permeability assay kit. RESULTS: The extracts produced significant (p < 0.05) reduction in TNFα, IL-6, IL-1ß, MCP-1, RANTES and iNOS/NO production in HZ-stimulated BV-2 microglia. Pre-treatment with 50 µg/mL of A. boonei, A. indica, A. occidentale, E. chlorantha and M. indica also resulted in the inhibition of NF-κB activation. Pre-treatment with A. indica produced, A. occidentale, M. indica and A. boonei reduced HZ-induced increased NLRP3 protein expression. HZ-induced increased caspase-1 activity was also reduced by A. boonei, A. occidentale, A. indica, E. chlorantha, and M. indica. Freeze-dried extracts of A. boonei, A. occidentale, A. indica and M. indica produced neuroprotective effect in HT-22 neuronal cells incubated with HZ by preventing HZ-induced neurotoxicity, ROS generation, DNA fragmentation and caspase 3/7 activity. Inhibition of HZ-induced increase in permeability of human hCMEC/D3 brain endothelial cells was also observed with A. boonei, A. occidentale, A. indica and M. indica, while reducing the release of TNFα and MMP-9. CONCLUSIONS: These results suggest that A. boonei, A. occidentale, A. indica and M. indica are neuroprotective through inhibition of neuroinflammation, neuronal damage and increased permeability of blood brain barrier. The outcome of the study provides pharmacological evidence for the potential benefits of plants as herbal treatments for cerebral malaria symptoms.
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Alstonia , Anacardium , Azadirachta , Malária Cerebral , Mangifera , Humanos , Fator de Necrose Tumoral alfa , Malária Cerebral/tratamento farmacológico , Doenças Neuroinflamatórias , Neuroproteção , Células Endoteliais , Espécies Reativas de Oxigênio , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêuticoRESUMO
The current COVID-19 pandemic, characterized by a highly contagious severe acute respiratory syndrome, led us to look for medicinal plants as an alternative to obtain new drugs, especially those with immunomodulatory abilities, capable of acting against the pulmonary infection caused by coronavirus 2 (SARS-CoV-2). Despite medical advances with COVID-19 drugs and vaccines, plant-based compounds could provide an array of suitable candidates to test against this virus, or at the very least, to alleviate some symptoms. Therefore, this review explores some plants widely used in Peru that show immunomodulatory properties or, even more, contain phytoconstituents potentially useful to prevent or alleviate the COVID-19 infection. More interestingly, the present review highlights relevant information from those plants to support the development of new drugs to boost the immune system. We used three criteria to choose nine vegetal species, and a descriptive search was then conducted from 1978 to 2021 on different databases, using keywords focused on the immune system that included information such as pharmacological properties, phytochemical, botanical, ethnobotanical uses, and some clinical trials. From these literature data, our results displayed considerable immunomodulation activity along with anti-inflammatory, antiviral, antioxidant, and antitumoral activities. Noticeably, these pharmacological activities are related with a wide variety of bioactive phytoconstituents (mixtures or isolated compounds) which may be beneficial in modulating the overt inflammatory response in severe COVID-19. Further scientific research on the pharmacological activities and clinical utilization of these potential plants are warranted. Supplementary Information: The online version contains supplementary material available at 10.1007/s43450-023-00367-w.
RESUMO
Withania adpressa Coss. ex is a plant used in traditional medications. Antioxidant, antibacterial, and antifungal properties of the essential oil from leaves of Withania adpressa Coss ex. (EOW) were investigated. EOW was extracted using a Clevenger apparatus, and its volatile compounds were characterized by GC-MS. Antioxidant potency was determined using DPPH, FRAP, and TAC assays. Antibacterial effects were determined vs. Escherichia coli, Klebsiella pneumonia, Staphylococcus aureus, and Streptococcus pneumonia; while its antifungal efficacy was determined vs. Candida albicans, Aspergillus flavus, Aspergillus niger, and Fusarium oxysporum using the disc diffusion and minimum inhibitory concentration bioassays. A chromatographic analysis showed that EOW contained eight phytochemical compounds constituting 99.14% of the total mass of oil. Caryophyllene (24.74%), Longifolene (21.37%), δ-Cadinene (19.08%), and Carene (14.86%) were predominant compounds in EOW. The concentrations required to inhibit 50% of free radical (IC50) values of antioxidant activities of EOW were 0.031 ± 0.006 mg/mL (DPPH), 0.011 ± 0.003 mg/mL (FRAP), and 846.25 ± 1.07 mg AAE/g (TAC). Inhibition zone diameters of EOW vs. bacteria were 18.11 ± 0.5 mm (E. coli), 17.10 ± 0.42 mm (S. aureus), 12.13 ± 0.31 mm (K. pneumoniae), and 11.09 ± 0.47 mm (S. pneumoniae), while MIC values were 51 ± 3, 47 ± 5, 46 ± 3 and 31 ± 1 µg/mL, respectively. Inhibition zone diameters of EOW vs. fungi were 31.32 ± 1.32, 29.00 ± 1.5, 27.63 ± 2.10, and 24.51 ± s1.07 mm for A. flavus, C. albicans, F. oxysporum, and A. niger, respectively. MIC values were 8.41 ± 0.40, 28.04 ± 0.26, 9.05 ± 0.76, and 22.26 ± 0.55 µg/mL, respectively. Importantly, the highest dose of EOW (1 mg/mL) showed negligible (~5%) cytotoxicity against MCF-12, a normal human epithelial cell line derived from the mammary gland, thus underscoring its wide safety and selectivity against tested microbes. To sum it up, EOW has exhibited promising antioxidant and antimicrobial properties, which suggests potential to abrogate antibiotic resistance.
Assuntos
Anti-Infecciosos , Óleos Voláteis , Withania , Humanos , Antifúngicos/farmacologia , Antifúngicos/química , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Antioxidantes/farmacologia , Antioxidantes/química , Staphylococcus aureus , Escherichia coli , Extratos Vegetais/química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química , Antibacterianos/farmacologia , Antibacterianos/química , Candida albicans , Testes de Sensibilidade MicrobianaRESUMO
Medicinal plants have been used since prehistoric times and continue to treat several diseases as a fundamental part of the healing process. Inflammation is a condition characterized by redness, pain, and swelling. This process is a hard response by living tissue to any injury. Furthermore, inflammation is produced by various diseases such as rheumatic and immune-mediated conditions, cancer, cardiovascular diseases, obesity, and diabetes. Hence, anti-inflammatory-based treatments could emerge as a novel and exciting approach to treating these diseases. Medicinal plants and their secondary metabolites are known for their anti-inflammatory properties, and this review introduces various native Chilean plants whose anti-inflammatory effects have been evaluated in experimental studies. Fragaria chiloensis, Ugni molinae, Buddleja globosa, Aristotelia chilensis, Berberis microphylla, and Quillaja saponaria are some native species analyzed in this review. Since inflammation treatment is not a one-dimensional solution, this review seeks a multidimensional therapeutic approach to inflammation with plant extracts based on scientific and ancestral knowledge.