Essential oil variability in Eugenia dysenterica fruits.

Essential oils (EOs) of Eugenia dysenterica fruits from seven populations were assessed using GC/MS and chemometric analysis. Variations in EOs between populations and three operational chemical units (OCUs), combined with foliar Mn2+ as an environmental variable, indicate that 86.8% of variation in oils was explained by these predictors. Variance partitioning shows that the largest pure contribution was attributed to foliar Mn2+ (13.1%), followed by OCU (11.4%). Populational origin contributed with lowest variance (6.6%).

A Molecular Networking Strategy: High-Throughput Screening and Chemical Analysis of Brazilian Cerrado Plant Extracts against Cancer Cells.

Plants have historically been a rich source of successful anticancer drugs and chemotherapeutic agents, with research indicating that this trend will continue. In this contribution, we performed high-throughput cytotoxicity screening of 702 extracts from 95 plant species, representing 40 families of the Brazilian Cerrado biome. Activity was investigated against the following cancer cell lines: colon (Colo205 and Km12), renal (A498 and U031), liver (HEP3B and SKHEP), and osteosarcoma (MG63 and MG63.3). Dose-response tests were conducted with 44 of the most active extracts, with 22 demonstrating IC50 values ranging from <1.3 to 20 µg/mL. A molecular networking strategy was formulated using the Global Natural Product Social Molecular Networking (GNPS) platform to visualize, analyze, and annotate the compounds present in 17 extracts active against NCI-60 cell lines. Significant cytotoxic activity was found for Salacia crassifolia, Salacia elliptica, Simarouba versicolor, Diospyros hispida, Schinus terebinthifolia, Casearia sylvestris var. lingua, Magonia pubescens, and Rapanea guianensis. Molecular networking resulted in the annotation of 27 compounds. This strategy provided an initial overview of a complex and diverse natural product data set, yielded a large amount of chemical information, identified patterns and known compounds, and assisted in defining priorities for further studies.

Phytotoxic and antioxidant effects of dichloromethane fraction of Smilax Brasiliensis Sprengel.

Dichloromethane (DCM) fraction and sub-fractions obtained from Smilax brasiliensis leaves were examined in order to determine their phytotoxic and antioxidant effects. The dichloromethane fraction was submitted to a preparative layer chromatography leading to seven sub-fractions (DCM1-DCM7). Gas chromatography-mass spectrometry (GC-MS) was performed on the dichloromethane sub-fractions. The DCM sub-fractions presented phytotoxic potential; at a concentration of 125 µg per plate, DCM6 and DCM4 showed the strongest results on Lactuca sativa and Allium cepa, respectively. The DCM fraction and DCM4 sub-fraction were more effective than 2,6-di-tert-butyl-4-methylphenol (BHT) at scavenging the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. Analysis by GC-MS showed the presence of methyl palmitate (33.05%) in DCM4 and methyl palmitate (17.29%) and methyl oleate (50.96%) in DCM6, suggesting that the activities exhibited by the sub-fractions may be attributed, at least partially, to these major compounds. These results indicate that the DCM sub-fractions of S. brasiliensis could be used as natural herbicides and antioxidants.

Toxicity and phytochemistry of eight species used in the traditional medicine of sul-mato-grossense, Brazil / Toxicidade e fitoquímica de oito espécies usadas na medicina tradicional sul-mato-grossense, Brasil

Abstract The Brazilian Cerrado has several botanical species for medicinal purposes used by traditional communities and many of these plants are not included in the list of Medicinal Plants Research Program of Central Medicines. The purpose of this study was the phytochemical screening and toxicology bioassay front of Brine shrimp L. of ethanolic extracts of eight species of plants used in folk medicine of Campo Grande, Mato Grosso do Sul, Brazil. The ethanolic extracts were submitted to phytochemical screening, determination of phenolic compounds and flavonoids. Toxicological assays were carried front of Brine shrimp according to standard methodology. The analysis TLC and HPLC-DAD confirmed the predominance of phenolic compounds and derivatives, specifically for the quercetin. The most toxic was the C. affinis DC. with death at all concentrations, the A. humile A. St. Hil. showed no mortality and the other species showed intermediate toxicity. The extracts of the investigated species are rich in phenolic compounds and derivatives, specifically quercetin, and feature toxicity between moderate to high, a fact that requires attention, since much of the traditional communities rely on herbal drugs in its raw form with preventive and curative purpose, meeting the basic health care.

Resumo O Cerrado brasileiro possui diversas espécies botânicas com fins medicinais utilizadas por comunidades tradicionais e muitas dessas plantas não estão incluídas na lista do Programa de Pesquisa de Plantas Medicinais da Central de Medicamentos. O objetivo deste estudo foi a triagem fitoquímica e o bioensaio toxicológico frente ao Brine shrimp L. de extratos etanólicos de oito espécies de plantas utilizadas na medicina popular de Campo Grande, Mato Grosso do Sul. Os extratos etanólicos foram submetidos à triagem fitoquímica, determinação de compostos fenólicos e flavonoides. Os ensaios toxicológicos foram realizados frente ao Brine shrimp de acordo com a metodologia padrão. A análise de cromatografia de camada delgada e HPLC-DAD confirmou a predominância de compostos fenólicos e derivados, especificamente para a quercetina. O mais tóxico foi o C. affinis DC. com a morte em todas as concentrações, o A. humile A. St. Hil. não apresentou mortalidade e as demais espécies apresentaram toxicidade intermediária. Os extratos das espécies investigadas são ricos em compostos fenólicos e derivados, especificamente a quercetina e apresentam toxicidade entre moderada a alta, fato que requer atenção, pois grande parte das comunidades tradicionais conta com fitoterápicos em sua forma bruta com preventivo e finalidade curativa, atendendo aos cuidados básicos de saúde.

Antiproliferative Activity and Antioxidant Potential of Extracts of Garcinia gardneriana.

The aim of this study was to evaluate the antiproliferative activity, the antioxidant potential, and the chemical profile obtained from the whole fruit and from leaves of Garcinia gardneriana, a fruit tree from Brazilian Cerrado. To determine in vitro antiproliferative activity, the following neoplastic cell lines were considered, along with an immortalized nontumor cell line. The antioxidant potential was determined, and the evaluation of antiradical air activity was performed. The levels of vitamin C and carotenoids were determined. The chemical profile was analyzed by high-performance liquid chromatography coupled to a diode array detector and a mass spectrometer using electrospray ionization interface. The chloroform fraction of the leaf showed antioxidant activity. The vitamin C content had lower values in fruits and higher in leaves. The content of carotenoids for fruits and leaves was expressive. The ethanolic extract and the hexane and chloroform fractions of fruits were active in all neoplastic lines tested. The leaves showed cytotoxic activity in the hexane fraction in the breast carcinoma line. The analysis of data obtained verified the presence of dimers, monomers, and tetramers of hexoses, polycarboxylic acids, xanthones, flavonoids, biflavonoids, and benzophenones.

Growth, Physiology and Nutrient Use Efficiency in Eugenia dysenterica DC under Varying Rates of Nitrogen and Phosphorus.

The production of high-quality seedlings and their use in commercial planting reduce pressure on natural areas. Eugenia dysenterica DC is a native fruit tree from the Brazilian Cerrado, whose nutritional requirements are still unclear. This study aimed to evaluate the effects of nitrogen (N) and phosphorus (P) supplementation on the physiology, growth and nutrient uptake, and use efficiencies of E. dysenterica seedlings grown in glasshouse conditions. The following rates were used in separate experiments: 0, 50, 100, 200, and 400 mg dm-3 N and 0, 100, 200, 400, and 600 mg dm-3 P. The experiment was conducted in a randomized block with four replications. The lowest N rate (50 mg dm-3) increased the stomatal conductance (gS) and, consequently, resulted in the highest transpiration (E), electron transport (ETR), and photosynthetic (A) rates. Also, rates of 50 mg dm-3 and 100 mg dm-3 N increased the Root Uptake Efficiency (RUE) and plant Nutrient Use Efficiency (NUE) for macronutrients and the RUE for micronutrients, stimulating plant growth. Phosphorous fertilization resulted in the maximum values for photosynthesis, electron transport rate, total dry mass, and NUE at the 200 mg dm-3 rate. The results of this study suggest that fertilization with 50 mg dm-3 N and 200 mg dm-3 P is suitable for the development of E. dysenterica seedlings.

Using the plants of Brazilian Cerrado for wound healing: From traditional use to scientific approach.

ETHNOPHARMACOLOGICAL RELEVANCE: The Brazilian Cerrado is a biome with a remarkable diversity of plant species, many of which are used mainly by local communities as a source of treatment to several pathologic processes, especially for the treatment of wounds. However, no systematic review exists focusing on the plants used in this respect and on the appropriate pharmacological investigations that substantiate the actions that are reported. This study revisits the traditional use of medicinal plants from the Brazilian Cerrado in the treatment of wounds and the pharmacological characteristics of the reported plant species. METHOD: ology: For the present article, previous studies on plants of the Brazilian Cerrado used for wound healing carried out between 1996 and 2018 were researched on various academic databases (PubMed, Elsevier, Springer, Lilacs, Google Escolar, and Scielo). RESULTS: A total of 33 studies were carried out on 29 plant species distributed into 18 families, mainly Fabaceae or Leguminosae (9), Bignoniaceae (2), Asteraceae (2), Euphorbiaceae (2). Considering the great diversity of Cerrado plants, only a small number of wound healing studies were carried out between 1996 and 2018. It was observed that there is a large gap between experimentation assay and traditional use. There are only few connections between the form of use by the population and the experiments conducted in the laboratory. We found that only about 12% of these studies considered to use the methodologies, or at least in parts, to obtain extracts such as those used in folk medicine. Approximately 37% of the experiments were performed using the bark as well as the same ratio for leaves, 6% using the fruits, and 9% using the seeds, roots or flowers. In several studies, there are reports of chemical constituents such as flavonoids and tannins, followed by steroid terpenes, saponins, and fatty acids, and alkaloids. However, approximately 35% of the studies did not supply information about compounds present in the preparation or the effect which could be attributed to these agents in respect to wound healing. Regarding treatment, most of the studies employed a topical treatment, though intraperitoneal and oral treatment were also described using either topical, oil-based formulations, but also gel- or saline-based formulations. CONCLUSIONS: Although, there has been an increase in knowledge about the biological actions of plants from Cerrado biome, the scientific basis for the traditional use of these local medicinal plants in wound healing does not provide sufficient information on the efficacy of the treatment, the molecular mechanisms, or, in particular, the effective doses used and the drug interactions. Thus, focused research investigating these hypotheses from traditional knowledge is necessary to prove the evidence of the potential pharmacological action.

A comprehensive characterization of Solanum lycocarpum St. Hill and Solanum oocarpum Sendtn: Chemical composition and antioxidant properties.

In this study we evaluated the proximate composition of two Solanaceae fruits from Brazilian Cerrado, their mineral content, volatile organic compounds (VOCs), phenolic compounds profile, and antioxidant capacity employing Oxygen Radical Absorbance Capacity (ORAC) assay, for each part of the fruits (pulp, peel and seeds). Our results showed that the pulp has a high moisture content (74.62-85.40 g/100 g) and soluble fiber (1.29-2.06 g/100 g) content, and low fat, protein, and ash content. The peel exhibited high levels of carbohydrates and total fibers (6.55-11.39 and 12.35-13.12 g/100 g, respectively), while the seed presented high content of fat, protein, and insoluble fiber (10.14-12.62, 9.14-13.24 and 19.84-23.15 g/100 g). Potassium is the main mineral found in both fruits. It is the first time that the carbohydrate profile, volatile components, and phenolic compounds of the fruta-do-lobo and juá-açu are reported. 1-Kestose (GF2) and nystose (GF3) were found in both fruits. The main VOCs of juá-açu were esters, while in fruta-do-lobo, aldehydes were the major components. UPLC-Q-ToF fraction analysis of juá-açu and fruta-do-lobo revealed 24 phenolic compounds, most being hydroxycinnamic acids derivatives in juá-açu, and chlorogenic acids in fruta-do-lobo. The antioxidant capacity (ORAC) of the fruits ranged from 1.35 to 11.51 µmol TE/100 mL of extract. These results indicate that Solanum genus can be interesting for the Brazilian fruit market, and that it has potential to be exploited for agroindustry for diversification of fruit products.

Therapeutic Potential of Brazilian Cerrado Campomanesia Species on Metabolic Dysfunctions.

Obesity, in conjunction with other metabolic disorders such as insulin resistance and dyslipidemia, is a feature of metabolic syndrome which is characterized by a pro-inflammatory state and increased oxidative stress. Therefore, antioxidant foods are proposed to prevent and treat these disorders. Medicinal plants are one of the main strategies in this regard. Guavira, a Brazilian Cerrado plant, contains different bioactive compounds with a high antioxidant capacity and without clinical or reproductive toxicity effects. Though there are different varieties of guavira, the principal Brazilian Cerrado guaviras demonstrated hypoglycemic, anti-inflammatory, and hypocholesterolemic actions. There is also a potential antiplatelet agent in C. xanthocarpa, while C. adamantium displayed hypocholesterolemic actions in animal models and human clinical trials. On the other hand, even with a lack of studies related to C. pubescens, it demonstrated anti-inflammatory effects and an antioxidant capacity in in vitro studies. Despite the fact that most of the studies were not performed to evaluate pathological conditions specific to obese animal models or obese subjects, guavira demonstrated effects in metabolic disorders that are commonly related to the obesity context, such as cardiovascular disturbances and hyperglycemia status. This suggests that guavira is a potential therapeutic approach to obesity-induced metabolic syndrome.

Cytotoxic Triterpenes from Salacia crassifolia and Metabolite Profiling of Celastraceae Species.

The new pentacyclic triterpene 11ß-hydroxypristimerin (1), along with the known metabolites pristimerin (2), 6-oxopristimerol (3) and vitideasin (4), were isolated from a Salacia crassifolia root wood extract, following a bioassay-guided fractionation approach. Both the extract and the purified triterpenes displayed pronounced cytotoxic activity against human cancer cell lines. The NCI-60 cell line screen revealed that compound 2 was the most active, with a mean GI50 of 0.17 µM, while compound 1 had a mean GI50 of 8.7 µM. A COMPARE analysis of the screening results showed that pristimerin is likely to be the main compound responsible for the cytotoxic activity of the extract (mean GI50 of 0.3 µg·mL−1). A targeted search for pristimerin and related derivatives using LC-MS/MS revealed the presence of pristimerin (2) and 6-oxopristimerol (3) in all Celastraceae species examined and in all plant parts tested, while vitideasin (4) was only detected in the genus Salacia.

Fruits from the Brazilian Cerrado region: Physico-chemical characterization, bioactive compounds, antioxidant activities, and sensory evaluation.

Given the economic importance of fruit processing, this study aimed to analyze the chemical composition, antioxidant activity, and sensorial acceptance of six fruit pulps from the Brazilian Cerrado. For bioactive compounds of the selected fruits, buriti contains the highest carotenoid content (2.85 mg licopene/100 g e 4.65 mg ß-carotene/100g), however showed the lowest ascorbic acid concentration (7.42 mg/100g); while mangaba contains the highest ascorbic acid concentration (175.06 mg/100g), but obtained the lowest total phenolic compounds (46.85 mg GAEs/100g) and antioxidant capacity. The marolo reported the highest total phenolic compounds (728.17 mg GAEs/100g), total fiber (21.62%), and a high antioxidant potential. Regarding the mineral composition, marolo stood out as potassium (378.69 mg/100g) and magnesium (31.78 mg/100g) contents, and yellow mombin as phosphorus (26.24 mg/100g) content. Finally, juice prepared using cagaita and marolo had greater sensorial acceptance. The composition of fruit pulps indicated the potential there for the development of new food products.

Brazilian Cerrado Qualea grandiflora Mart. Leaves Exhibit Antiplasmodial and Trypanocidal Activities In vitro.

BACKGROUND: The rapid spread of drug-resistant strains of protozoan parasites required the urgent need for new effective drugs. Natural products offer a variety of chemical structures, which make them a valuable source of lead compounds for the development of such new drugs. Cerrado is the second largest biome in Brazil and has the richest flora of all the world savannahs. We selected Qualea grandiflora, a plant species known for its proprieties in folk medicine and its antibacterial activity. OBJECTIVE: However, its antiprotozoal activity was not yet explored. MATERIALS AND METHODS: We investigated the activities of fractions from the ethyl acetate extract of Q. grandiflora leaves against human life forms of Plasmodium falciparum, Trypanosoma cruzi, and Trypanosoma brucei gambiense, and for its cytotoxicity upon the rat L6-myoblast cell line. Ten fractions were produced by ethyl acetate:hexane chromatography. RESULTS AND CONCLUSION: The fractions showed no cytotoxicity against L-6 cells (IC50 > 100 µg/mL) and no hemolysis propriety. Three fractions had a moderate activity against P. falciparum, anyone was active against T. cruzi but four fractions demonstrated a high activity against bloodstream forms of T. brucei gambiense (8.0< IC50 <15 µg/mL). Identification and characterization of the active compounds are currently under investigation. SUMMARY: Qualea grandiflora is an endemic tree of the Brazilian Cerrado, which presents medicinal propertiesTen fractions of the ethyl acetate extract of Q. grandiflora leaves were assessed against Plasmodium falciparum, Trypanosoma Cruzi, and Trypanosoma brucei gambienseNo fraction showed relevant cytotoxicity and hemolysis activityAll the fractions presented antiplasmodial and trypanocidal activitiesThree fractions with moderate antiplasmodial activity (49< IC50 <56 µg/mL)Four fractions with high activity against bloodstream forms of T. brucei gambiense (8.0< IC50 <15 µg/mL). Abbreviations used: CQ: Chloroquine, DMSO: Dimethyl sulfoxide, HEPES: 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid, HMI: Modified Iscove's medium, IC50: Concentration inhibiting 50% of parasite growth, IC90: Concentration inhibiting 90% of parasite growth, MTT: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, RPMI: Roswell Park Memorial Institute, SD: Standard deviation, SI: Ratio of cytotoxicity to biological activity - TC50/IC50, TC50: Concentration causing 50% of cell growth inhibition, TC90: Concentration causing 90% of cell growth inhibition, TLC: Thin-layer chromatography.

Acaricidal activity of ethanolic extracts of Stryphnodendron adstringens and Lafoensia pacari and oil resins from Copaifera sp. and Pterodon emarginatus against Sarcoptes scabiei var. suis / Atividade acaricida dos extratos etanólicos de Stryphnodendron adstringens Mart. e Lafoensia pacari A. St Hil., bem como das óleo-resinas de Copaifera sp. e Pterodon emarginatus Vogel, 1837 contra Sarcoptes scabiei var. suis

In vitro bioassay using Sarcoptes scabiei as a test microorganism is a viable method of study for diverse drugs with acaricidal properties. A great amount of assays proves the diverse and efficient biological activity of extracts and compounds from Brazilian savanna plants. This study had as main object, test and compare the acaricidal activity of four Brazilian Cerrado bioproducts: Stryphnodendron adstringens Mart., Copaifera sp., Lafoensia pacari A. St Hil. and Pterodon emarginatus Vogel, 1837. To perform this test S. scabiei mites were collected from crusts removed on ears of highly infected sows. The mites were selected and separated in Petri dishes with three different concentrations (25, 50 and 75%) of each bioproduct, to evaluate their potential acaricidal activity. The mortality of the mites was counted in each Petri dish every hour, during five hours. The statistical analyses demonstrated differences between the bioproducts tested. The oleoresin of Copaifera sp. and P. emarginatus presented the best results with 100% of mites mortality after treatment. The ethanolic extracts of S. adstringens and L. pacari demonstrated lower acaricidal activity when compared to the oleoresins, with little or no difference among the control groups tested. This bioassay demonstrated to be efficient, reliable, low cost and easy accomplishment. Oil resins from Copaifera sp. and P. emarginatus have in vitro acaricidal activity against adult females of S. scabiei var. suis.(AU)

O uso de Sarcoptes scabiei como microrganismo teste para bioensaio in vitro é um método de estudo viável para diversas drogas acaricidas. Muitos ensaios comprovam a diversidade e eficiência de atividade biocida de extratos e componentes presentes em plantas do cerrado brasileiro. Este trabalho objetivou testar e comparar a atividade acaricida de quatro bioprodutos do cerrado brasileiro: Stryphnodendron adstringens Mart., Lafoensia pacari A. St Hil., Copaifera sp. e Pterodon emarginatus Vogel, 1837. Para este estudo, ácaros S. scabiei foram colhidos em crostas removidas de orelhas de fêmeas suínas altamente infestadas. Os ácaros foram selecionados, separados e colocados em placas de Petri com três diferentes concentrações (25, 50 e 75%) de bioprodutos, para avaliar o potencial de atividade acaricida de cada um. Foi realizada a contagem da mortalidade dos ácaros em cada placa de Petri a cada hora, durante cinco horas. As análises estatísticas demonstraram diferenças entre os bioprodutos testados. As óleo-resinas de Copaifera sp. e P. emarginatus apresentaram os melhores resultados, com 100% de mortalidade dos ácaros após tratamento. Os extratos etanólicos de S. adstringens Mart. e L. pacari demonstraram menor atividade acaricida quando comparados as óleo-resinas, com pequena ou nenhuma diferença entre os resultados dos grupos controle. Este ensaio demonstrou ser uma ferramenta eficiente, confiável, de baixo custo e de fácil realização. As óleo-resinas Copaifera sp. e P. emarginatus possuem atividade acaricida in vitro sobre fêmeas adultas de S. scabiei var. suis.(AU)

Toxicity and phytochemistry of eight species used in the traditional medicine of sul-mato-grossense, Brazil

Abstract The Brazilian Cerrado has several botanical species for medicinal purposes used by traditional communities and many of these plants are not included in the list of Medicinal Plants Research Program of Central Medicines. The purpose of this study was the phytochemical screening and toxicology bioassay front of Brine shrimp L. of ethanolic extracts of eight species of plants used in folk medicine of Campo Grande, Mato Grosso do Sul, Brazil. The ethanolic extracts were submitted to phytochemical screening, determination of phenolic compounds and flavonoids. Toxicological assays were carried front of Brine shrimp according to standard methodology. The analysis TLC and HPLC-DAD confirmed the predominance of phenolic compounds and derivatives, specifically for the quercetin. The most toxic was the C. affinis DC. with death at all concentrations, the A. humile A. St. Hil. showed no mortality and the other species showed intermediate toxicity. The extracts of the investigated species are rich in phenolic compounds and derivatives, specifically quercetin, and feature toxicity between moderate to high, a fact that requires attention, since much of the traditional communities rely on herbal drugs in its raw form with preventive and curative purpose, meeting the basic health care.

Resumo O Cerrado brasileiro possui diversas espécies botânicas com fins medicinais utilizadas por comunidades tradicionais e muitas dessas plantas não estão incluídas na lista do Programa de Pesquisa de Plantas Medicinais da Central de Medicamentos. O objetivo deste estudo foi a triagem fitoquímica e o bioensaio toxicológico frente ao Brine shrimp L. de extratos etanólicos de oito espécies de plantas utilizadas na medicina popular de Campo Grande, Mato Grosso do Sul. Os extratos etanólicos foram submetidos à triagem fitoquímica, determinação de compostos fenólicos e flavonoides. Os ensaios toxicológicos foram realizados frente ao Brine shrimp de acordo com a metodologia padrão. A análise de cromatografia de camada delgada e HPLC-DAD confirmou a predominância de compostos fenólicos e derivados, especificamente para a quercetina. O mais tóxico foi o C. affinis DC. com a morte em todas as concentrações, o A. humile A. St. Hil. não apresentou mortalidade e as demais espécies apresentaram toxicidade intermediária. Os extratos das espécies investigadas são ricos em compostos fenólicos e derivados, especificamente a quercetina e apresentam toxicidade entre moderada a alta, fato que requer atenção, pois grande parte das comunidades tradicionais conta com fitoterápicos em sua forma bruta com preventivo e finalidade curativa, atendendo aos cuidados básicos de saúde.

Cytotoxic Effect of Erythroxylum suberosum Combined with Radiotherapy in Head and Neck Cancer Cell Lines

Abstract The mouth and oropharynx cancer is the 6th most common type of cancer in the world. The treatment may involve surgery, chemotherapy and radiotherapy. More than 50% of drugs against cancer were isolated from natural sources, such as Catharanthus roseus and epipodophyllotoxin, isolated from Podophyllum. The biggest challenge is to maximize the control of the disease, while minimizing morbidity and toxicity to the surrounding normal tissues. The Erythroxylum suberosum is a common plant in the Brazilian Cerrado biome and is popularly known as "cabelo-de-negro". The objective of this study was to evaluate the cytotoxic activity of Erythroxylum suberosum plant extracts of the Brazilian Cerrado biome associated with radiotherapy in human cell lines of oral and hypopharynx carcinomas. Cells were treated with aqueous, ethanolic and hexanic extracts of Erythroxylum suberosum and irradiated at 4 Gy, 6 Gy and 8 Gy. Cytotoxicity was evaluated by MTT assay and the absorbance was measured at 570 nm in a Beckman Counter reader. Cisplatin, standard chemotherapy, was used as positive control. The use of Erythroxylum suberosum extracts showed a possible radiosensitizing effect in vitro for head and neck cancer. The cytotoxicity effect in the cell lines was not selective and it is very similar to the effect of standard chemotherapy. The aqueous extract of Erythroxylum suberosum, combined with radiotherapy was the most cytotoxic extract to oral and hypopharynx carcinomas.

Resumo O câncer de boca e de orofaringe emerge como o 6º tipo de câncer mais comum no mundo. O tratamento pode envolver cirurgia, quimioterapia e radioterapia. Mais de 50% das drogas com atividade de combate ao câncer foram isoladas de fontes naturais, tais como a Catharanthus roseus e a epipodofilotoxina, isolada de Podophyllum. O maior desafio é maximizar o controle da doença, enquanto minimiza a morbidade e toxicidade para os tecidos normais circundantes. O Erythroxylum suberosum é uma planta comum no bioma Cerrado brasileiro e é popularmente conhecida como "cabelo-de-negro". O objetivo deste estudo foi avaliar a citotoxicidade dos extratos da planta Erythroxylum suberosum do bioma Cerrado brasileiro, associados à radioterapia em linhagens celulares humanas de carcinomas de língua e de hipofaringe. As células foram tratadas com os extratos aquoso, etanólico e hexânico do Erythroxylum suberosum e irradiadas com 4 Gy, 6 Gy e 8 Gy. A citotoxidade foi avaliada pelo ensaio de MTT e a absorvância foi medida a 570 nm em uma leitora Beckman. A cisplatina, quimioterápico padrão, foi utilizada como controle positivo. O uso de extratos de Erythroxylum suberosum mostrou potencial efeito radiosensibilizante in vitro no câncer de cabeça e pescoço. O efeito da citotoxicidade nas linhagens foi de forma não seletiva e muito semelhante ao efeito da quimioterapia padrão. O extrato aquoso de Erythroxylum suberosum, combinado com radioterapia, foi o extrato mais citotóxico para os carcinomas de língua e hipofaringe, associados à radioterapia.

In vitro investigation of Brazilian Cerrado plant extract activity against Plasmodium falciparum, Trypanosoma cruzi and T. brucei gambiense.

The threatened Brazilian Cerrado biome is an important biodiversity hotspot but still few explored that constitutes a potential reservoir of molecules to treat infectious diseases. We selected eight Cerrado plant species for screening against the erythrocytic stages of Plasmodium falciparum, human intracellular stages of Trypanosoma cruzi and bloodstream forms of T. brucei gambiense, and for their cytotoxicity upon the rat L6-myoblast cell line. Bioassays were performed with 37 hexane, ethyl acetate and ethanol extracts prepared from different plant organs. Activities against parasites were observed for 24 extracts: 9 with anti-P. falciparum, 4 with anti-T. cruzi and 11 with anti-T. brucei gambiense activities. High anti-protozoal activity (IC50 values < 10 µg/mL) without obvious cytotoxicity to L6 cells was observed for eight extracts from plants: Connarus suberosus, Blepharocalyx salicifolius, Psidium laruotteanum and Myrsine guianensis. Overall, studies of plant extracts will contribute to increase the biodiversity knowledge essential for Cerrado conservation and sustainable development.

Polyphenols from cagaita ( Eugenia dysenterica DC. ) and cambuci ( Campomanesia phaea Berg. ): bioactivities in diet-induced obesity and their metabolic alterations / Polifenóis de cagaita ( Eugenia dysenterica DC. ) e cambuci ( Campomanesia phaea Berg. ): bioatividades na obesidade induzida por dieta e suas alterações metabólicas.

Obesity and overweight have reached epidemic proportions and their prevalence has increased dramatically in the last decades worldwide. This has resulted in a dramatic increase in the incidence of obesity-associated metabolic alterations including type 2 diabetes, cardiovascular complications, and certain types of cancer. Evidences suggest that bioactive compounds present in fruit and vegetables, including polyphenols (or phenolic compounds), may exert beneficial effects against the development of obesity and associated alterations. Brazil is the world's third largest fruit producer and the seventh largest producer of tropical fresh fruits; however, only a few of them are being exploited commercially, perhaps due to the limited amount of information available about their chemical composition, and biochemical, nutritional and functional properties. Cagaita (Eugenia dysenterica DC.) and cambuci (Campomanesia phaea Berg.) are fruit species of the Myrtaceae family growing in the regions of the Brazilian Cerrado and Atlantic Coastal Forest biomes, respectively. Cagaita and cambuci fruits are used in various typical preparations, mainly jams, jellies, ice-cream, and liqueurs; whereas both fruit and leaves are used as popular alternative medicine by local communities to treat various disturbs such as diarrhea, diabetes, and jaundice. Previous studies have demonstrated the antioxidant and antidiabetic potential from cagaita and cambuci polyphenols in in vitro assays. Thus, in the present study, we investigated whether the administration of polyphenol-rich extracts from cagaita and cambuci, at two different doses, protect mice from diet-induced obesity and associated alterations. Two biological models, preventive and therapeutic, were designed for cagaita, and preventive for cambuci. For the preventive protocols, C57BL/6J mice fed either with a chow or a high-fat, high-sucrose (HFHS) diets were daily treated by gavage with water or polyphenols-rich extracts at two doses for 8 weeks. The findings demonstrate that polyphenols from cagaita prevented body weight and fat mass gains, attenuated fasting hyperglycemia and dyslipidemia, and reduced hepatic lipid accumulation. On the other hand, polyphenols from cambuci showed absence of changes in body weight and adiposity; however, an attenuation of adipose tissue inflammation was observed for both doses tested. Additionally, polyphenols from cambuci were effective in ameliorating glucose tolerance, as well as reducing fasting hyperglycemia, and improving dyslipidemia. For the therapeutic protocol, C57BL/6J obese mice induced by the intake of a HFHS diet for six weeks were treated with polyphenols from cagaita at two doses by oral gavage for further 8 weeks. Polyphenols from cagaita improved glucose homeostasis and attenuated dyslipidemia in obese mice, without affecting body weight and adiposity. Mechanistically, these beneficial actions seem to be mediated, at least in part, through a reduction in hepatic inflammation. In conclusion, polyphenols from cagaita and cambuci have a potential protective role in diet-induced obesity and their metabolic alterations

A obesidade é considerada uma das grandes epidemias do século XXI, devido ao aumento de sua prevalência nos últimos anos e às diversas co-morbidades decorrentes destas alterações metabólicas como diabetes mellitus tipo 2, doenças cardiovasculares e alguns tipos de câncer. Evidências sugerem que compostos bioativos presentes em frutas e vegetais, incluindo os polifenóis (ou compostos fenólicos), podem exercer efeitos benéficos contra o desenvolvimento de obesidade e suas alterações associadas. O Brasil é o terceiro produtor mundial de frutas e o sétimo na produção de frutas tropicais, no entanto, um grande número de espécies frutíferas nativas permanece inexplorado em relação a seu potencial nutricional e funcional. Cagaita (Eugenia dysenterica DC.) e cambuci (Campomanesia phaea Berg.) são espécies frutíferas originárias das regiões do Cerrado e da Mata Atlântica, respectivamente, cujos frutos são usados na elaboração de diversos produtos alimentícios, e frutos e folhas de cagaita são usados na medicina popular. Estudos prévios têm demonstrado o potencial antioxidante e antidiabético in vitro dos polifenóis de ambas as frutas. Neste contexto, no presente estudo, foi investigado se a administração de extratos ricos em polifenóis de cagaita e cambuci, em duas doses diferentes, protegem camundongos de obesidade induzida por dieta a suas alterações associadas. Dois modelos biológicos, preventivo e terapêutico, foram desenvolvidos para cagaita, e preventivo para cambuci. Para os protocolos preventivos, foram usados camundongos da linhagem C57BL/6J alimentados com dieta rica em gorduras e sacarose (high-fat high-sucrose diet, HFHS), aos quais foram administrados água (controle) ou extratos ricos em polifenóis por gavagem em duas doses por 8 semanas. Os resultados demonstraram diferentes efeitos para os dois extratos. Os polifenóis de cagaita preveniram ganho de peso corporal e adiposidade, atenuaram hiperglicemia de jejum e dislipidemia, e reduziram acumulação de lipídeos hepáticos. Por outro lado, polifenóis de cambuci não contribuíram na prevenção do ganho de peso corporal e adiposidade, no entanto, foi observada uma atenuação na inflamação do tecido adiposo, em ambas as doses avaliadas. Adicionalmente, polifenóis de cambuci melhoraram a tolerância à glicose, assim como reduziram a hiperglicemia de jejum e atenuaram a dislipidemia. Para o protocolo terapêutico, camundongos da linhagem C57BL/6J foram induzidos à obesidade pela ingestão da dieta alta em gorduras e sacarose por 6 semanas e posteriormente foram tratados com polifenóis de cagaita, em duas doses, por gavagem por 8 semanas. Os polifenóis de cagaita melhoraram a homeostase glicêmica e atenuaram a dislipidemia em camundongos obesos, sem afetar peso corporal e adiposidade. Estes benefícios aparentam ser mediados, ao menos em parte, através da uma redução da inflamação hepática. Em conclusão, polifenóis de cagaita e cambuci têm um papel protetor potencial em obesidade induzida por dieta e suas alterações metabólicas

Medicinal species with gastroprotective activity found in the Brazilian Cerrado.

Peptic and/or duodenal ulcers are characterized by diverse acute and chronic ulcerative lesions that commonly arise in any portion of the gastric mucosa that is exposed to the aggressive action of gastric acid. The pathophysiology of peptic ulcers has been attributed to an imbalance between aggressive and protective factors. In Brazil, medicinal plants are commonly used to treat this ailment. A country with great biodiversity, Brazil is considered a rich source of therapeutic products. There have been popular and pharmacological reports on the medicinal relevance of the Brazilian cerrado plant species, including Ananas ananassoides, Celtis iguanaea, Encholirium spectabile, Hymenaea stigonocarpa, Lafoensia pacari, Qualea grandiflora, Qualea parvifora, Mouriri pusa, Solanum lycocarpum, Solanum paniculatum, Serjania erecta, and Vochysia tucanorum, in the treatment of stomach disorders. The aim of the present review was to report on some of the Brazilian cerrado plants that are used in folk medicine because of their gastroprotective potential and to encourage novel studies in the search and preservation of plants with this therapeutic potential.

Cytotoxicity and apoptogenic effects of Lafoensia pacari.

ETHNOPHARMACOLOGICAL RELEVANCE: The stem barks of Lafoensia pacari have been traditionally used not only by South Amerindians but also by Brazilian and Paraguayan populations for treating a variety of unhealthy conditions to which their biological potential has been scientifically documented in several reports over the last decade. Although its anticancer usage is also popular, no scientific support for such activity has been found. AIM: To provide scientific evidence for the anticancer popularity of Lafoensia pacari. MATERIALS AND METHODS: Extracts prepared according to the popular use along with a methanol extract and its four fractions were produced from Lafoensia pacari stem barks. The chromatogram profile of each one was obtained by HPLC. Several tumor cell lines were exposed to these solutions in in vitro assays and the effects evaluated by morphological, growth, and cell cycle status changes. RESULTS: High toxicity determined by the lactate dehydrogenase levels with a significant drop in the cell proliferation index were found for all cell lines included in this study after exposition to Lafoensia pacari extract and fractions. The morphological features along with the expression of annexin V have strongly suggested apoptosis induction, which has been confirmed by G0/G1 cell cycle arrest. CONCLUSIONS: The data have clearly shown that exposition of human tumor cell lines to Lafoensia pacari stem barks extract leads to apoptosis induction due to cell cycle arrest in G0/G1 phases, supporting its anticancer use.

Discovery of the rapanone and suberonone mixture as a motif for leishmanicidal and antifungal applications.

Leishmaniasis and fungal infections are significant diseases impacting worldwide public health. Treatments have developed greatly over time, however, there is a necessity to discover less toxic drugs, which have greater efficacy and are more economically accessible. This work conducted a screening of Cerrado species extracts: Connarus suberosus Planch. (Connaraceae), Neea theifera Oerst. (Nyctaginaceae) and Myrcia linearifolia Cambess. (Myrtaceae) against Leishmania (Leishmania) amazonensis, dermatophytes and yeasts. Leishmanicidal and antifungal tests were conducted using MTT colorimetric assay and CLSI methodology, respectively. Connarus suberosus extracts presented the most promising results against the aforementioned microorganisms, which has not been described in the literature. The root bark EtOAc extract was selected for chemical fractionation resulting in a mixture of rapanone (1) and a previously unreported compound named as suberonone (2); a mixture of ß-sitosterol (3) and stigmasterol (4); oleic acid (5); geranilgeraniol (6); and two derivatives obtained from 1 and 2 mixture. The rapanone and suberonone mixture demonstrated a MIC of 15.62 µg/mL against Candida albicans ATCC 10231.