RESUMO
Brasiliensic acid (Bras) is a chromanone isolated from Calophyllum brasiliense Cambèss. bark extracts with confirmed potential activity on gastric ulcer and Helicobacter pylori infection. This study aimed to investigate the in vitro and in vivo toxicity of Bras and molecular docking studies on its interactions with the H. pylori virulence factors and selected gastric cancer-related proteins. Cytotoxicity was evaluated by alamarBlue© assay, genotoxicity by micronucleus and comet assays, and on cell cycle by flow cytometry, using Chinese hamster epithelial ovary cells. Bras was not cytotoxic to CHO-K1 cells, and caused no chromosomal aberrations, nor altered DNA integrity. Furthermore, Bras inhibited damages to DNA by H2O2 at 1.16 µM. No cell cycle arrest was observed, but apoptosis accounted for 31.2% of the cell death observed in the CHO-K1 at 24 h incubation of the IC50. Oral acute toxicity by Hippocratic screening test in mice showed no relevant behavioral change/mortality seen up to 1,000 mg/kg. The molecular docking approach indicated potential interactions between Bras and the various targets for peptic ulcer and gastric cancer, notably CagA virulence factor of H. pylori and VEGFR-2. In conclusion, Bras is apparently safe and an optimization for Bras can be considered for gastric ulcer and cancer.Communicated by Ramaswamy H. Sarma.
RESUMO
SUMMARY Introduction: The species Calophyllum brasiliense Cambés (Calophyllaceae) is widespread throughout Central and South America. The stem bark infusion is used for lowering blood glucose. Aim: To optimize the spray dry extract ofthis plant using a D-optimal experimental design. Materials and methods: As factors were used the air-drying speed (3.5-4.5 m3/h), the feed flow rate of the suspension (5-11 mL/ min), and the inlet air temperature (90-130 °C). The dried extract was characterized by measuring the phenolics and flavonoids content, moisture, the water activity, apparent densities, flowability, and compressibility. The antioxidant activity, the inhibitory activity of lipase and alpha-glycosidase, and the antiglycant activity of the spray dried extract (SDE) were evaluated. Subsequently, the hypoglycemic activity was evaluated in rats by monitoring the blood glucose level, triglycerides, and cholesterol. Results: Inlet air temperature and feed flow rate were the factors that most affected the yield and phenolic content. SDE showed a potent antioxidant effect (IC50 1.83 μg/mL), a potent a-glycosidase (IC50 74.45 μg/mL) and pancreatic lipase (IC50 27.33 μg/mL) inhibition. A potent antiglycation effect (IC50 9.45^g/mL) was also observed. Conclusion: the SDE showed a potent hypoglycemic effect at 100 mg/kg. These results suggest that SDE could activate four important pathways that can contribute to diabetes control.
Resumen Introducción: la especie Calophyllum brasiliense (Calophyllaceae) está muy extendida en Centro y Suramérica. La infusión del tronco reduce los niveles de glucosa en sangre. bjetivo: optimizar el extracto seco por aspersión (SDE) de esta planta utilizando un diseño experimental D-óptimal. Materiales y métodos: como factores se utilizaron la velocidad del gas secante (aire, 3,5-4,5 m3/h), la temperatura de entrada del aire fue 90-130 °C y la velocidad de alimentación, 5-11 mL/min. Se determinó el contenido de fenoles y flavonoides en el extracto seco, la humedad residual, la actividad del agua, las densidades aparentes, fluidez y compresibilidad. Se evaluó la actividad antioxidante e inhibidora de lipasa y alfa-glicosidasa y la actividad antiglicante. También se evaluó la actividad hipoglicemiante midiendo glucosa en sangre, triglicéridos y colesterol. Resultados: la temperatura del aire de entrada y la velocidad de alimentación afectaron, significativamente, el rendimiento y contenido de fenoles. El SDE mostró un potente efecto antioxidante (IC50 1,83 μg/mL), una potente inhibición de a-glicosidasa (IC50 74,45 μg/mL) y de lipasa pancreática (IC50 27,33 μg/ mL). Se observó un fuerte efecto antiglicante (IC50 9,45 μg/mL). Conclusiones: el SDE mostró un potente efecto hipoglicemiante a 100 mg/kg. Estos resultados sugieren que el SDE podría actuar activando cuatro vías importantes para el control de la diabetes.
RESUMO Introdução: a espécie Calophyllum brasiliense (Calophyllaceae) é amplamente distribuída na América do Sul e Central. A infusão da casca do caule reduz os níveis de glicose no sangue. Objetivo: otimizar o extrato seco por pulverização (SDE) desta planta usando um planejamento experimental D-ótimo. Materiais e métodos: a velocidade do gás de secagem ar (3,5-4,5 m3/h), a temperatura de entrada do ar (90-130 °C) e a taxa de alimentação (5-11 mL/min) foram usados como fatores. Foi determinado o teor de fenóis e flavonóides no extrato seco, a umidade residual, a atividade de água, as densidades aparentes, a fluidez e a compressibilidade. Avaliou-se a atividade antioxidante e a atividade inibitória de lipase e alfa-glicosidase, e a atividade antiglicante do extrato seco. A atividade hipoglicêmica foi avaliada em ratos diabeticos, medindo a glicose no sangue, triglicerídeos e colesterol. Resultados: a temperatura de entrada do ar e a taxa de alimentação afetaram significativamente o desempenho e o conteúdo de fenois. O SDE mostrou um potente efeito antioxidante (IC50 1,83 μg/mL), uma significativa inibição de a-glicosidase (IC50 74,45 ig/mL) e da lipase pancreática (IC50 27,33 μg/mL). Um forte efeito antiglicante também foi observado (IC50 9,45 μg/mL). O SDE mostrou um forte efeito hipogli-cemiente à concentração de 100 mg/kg. Conclusões: Esses resultados sugerem que o SDE poderia atuar ativando quatro vias importantes para o controle do diabetes.
RESUMO
In the present work, the MeOH extract from stem barks of Calophyllum brasiliense Cambess. (Clusiaceae) displayed activity against amastigote forms of Trypanosoma cruzi and Leishmania infantum and was subjected to a bioactivity-guided fractionation to give two related coumarins - calanolides E1 (1) and E2 (2). Compounds 1 and 2 were actives to T. cruzi with EC50 values of 12.1 and 8.2 µM, respectively. When tested against L. infantum, the EC50 values were 37.1 and 29.1 µM, respectively. Compound 2, corresponding to anti isomer, showed the best selectivity index (SI) with values >24.4 to T. cruzi and >6.9 to L. infantum in comparison to the syn isomer 1. Furthermore, using an in silico multi-parametric prediction, both compounds did not contain any PAINS sub-structures. Therefore, these data suggest that coumarins 1 and 2 may contribute as scaffolds for the design of novel drug candidates for leishmaniasis and Chagas disease.
Assuntos
Calophyllum , Clusiaceae , Leishmania infantum , Piranocumarinas , Trypanosoma cruzi , Cumarínicos/farmacologiaRESUMO
Chagas Disease is a neglected tropical disease caused by the protozoan parasite Trypanosoma cruzi which affects 6-8 million people, mostly in Latin America. The medical treatment is based on two nitroimidazole compounds, which have limited effectiveness in the chronic phase of the disease and produce several adverse effects; consequently, there is an urgent need to develop new, safe, and effective drugs. Previous reports had shown that natural coumarins, especially mammea A/BA isolated from the tropical tree Calophyllum brasiliense, is a promissory molecule for developing new drugs, due to its potent activity, higher than benznidazole, selectivity, and its low toxicity in mice. However, its mode of action is still unknown. In the present work, we evaluated the mechanism of action of the coumarin mammea A/BA (93.6%), isolated from the tropical tree C. brasiliense on Querétaro strain (Tc1) of T. cruzi. This compound was tested in vitro on epimastigotes and trypomastigotes of T. cruzi for intracellular esterase activity, plasma membrane integrity, phosphatidylserine exposure, ROS production, mitochondrial membrane potential, caspase-like activity, DNA integrity, cell cycle and autophagy. Mammea A/BA showed a 50% lethal concentration (LC50) of 85.8 and 36.9 µM for epimastigotes and trypomastigotes respectively. It affected intracellular esterase activity, produced important plasma membrane damage and induced phosphatidylserine exposure. An increase in reactive oxygen species (ROS) and decrease in mitochondrial membrane potential were detected. Caspase-like activity was present in both parasite forms producing DNA integrity damage. This compound also induced a cell cycle arrest in the G1 phase and the presence of autophagy vacuoles. The above data suggest that mammea A/BA induce cell death of T. cruzi by autophagy and apoptosis-like phenomena and support our suggestion that mammea A/BA could be a promising molecule for the development of new drugs to treat Chagas Disease.
Assuntos
Calophyllum/química , Cumarínicos/química , Cumarínicos/farmacologia , Tripanossomicidas/química , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Doença de Chagas/tratamento farmacológico , Doença de Chagas/parasitologia , Humanos , Mammea/química , Estresse Oxidativo/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Trypanosoma cruzi/citologia , Trypanosoma cruzi/metabolismoRESUMO
BACKGROUND: The current drugs for Chagas Disease caused by the protozoan Trypanosoma cruzi have limited therapeutic potential and are associated with serious side effects. Natural products can aid to develop new chemotherapeutic agents. Several natural coumarins, especially Mammea A/BA, have shown significant activity against T. cruzi and low toxicity on human lymphocytes, but its effectivity on a wide range of strains need to be tested, as well as to deepen in their mode of action and safety. HYPOTHESIS/PURPOSE: To discern the effects and explore the action mechanisms of mammea A/BA and a mixture of mammea coumarins isolated from Calophyllum brasiliense on Mexican strains of T. cruzi belonging to different genotypes and compare its effectivity with the drug benznidazole. STUDY DESIGN: We evaluated the trypanocidal activity in vitro of mammea A/BA (93.6%), and a mixture of coumarins, mammea A/BAâ¯+â¯A/BBâ¯+â¯A/BD (86:10:1%) on Mexican T. cruzi strains belonging to different genotypes Ninoa, Querétaro (TcI) and Ver6 (TcVI). MATERIAL AND METHODS: Mammea A/BA and the mixture of coumarins, were isolated from Calophyllum brasiliense, identified by proton NMR and purity determined by HPLC. The in vitro trypanocidal activity was evaluated on mobility, growth recovery, morphology and infectivity of T. cruzi. The cytotoxicity on mammalian cells was compared with benznidazole. The ultrastructure of the treated epimastigotes was analyzed by transmission electron microscopy (TEM). RESULTS: Mammea A/BA and the mixture of coumarins showed high trypanocidal activity, affecting the mobility, growth recovery, morphology, ultrastructure of epimastigotes, and drastically reduce trypomastigotes infectivity on Vero cells. These substances were four times more potent than benznidazole and showed low cytotoxicity and high selectivity index. The TEM showed severe alterations on the plasmatic membrane, nuclear envelope, as well as, mitochondrial swelling, that leads to the death of parasites. CONCLUSION: Mammea A/BA (93.6%) and a mixture of mammea A/BAâ¯+â¯A/BB and A/BD (86: 10: 1%) isolated from the tropical tree C. brasiliense showed higher trypanocidal activity than the current drug benznidazole on three Mexican strains of T. cruzi. These compounds induced severe physiological and morphological alterations. These results suggest their possible use in preclinical studies.
Assuntos
Calophyllum/química , Cumarínicos/farmacologia , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Trypanosoma cruzi/ultraestrutura , Animais , Doença de Chagas/tratamento farmacológico , Doença de Chagas/parasitologia , Chlorocebus aethiops , Cumarínicos/química , Cumarínicos/isolamento & purificação , Avaliação Pré-Clínica de Medicamentos , México , Células VeroRESUMO
Soulattrolide is a natural coumarin synthesized by the leaves of species of Calophyllum (Calophyllaceae) rain forest trees, including the American C. brasiliense, and the Asian C. teysmanii. Soulattrolide is a potent inhibitor of the reverse transcriptase from HIV-1 (RT-HIV-1), and active against Mycobacterium tuberculosis. However, the effects of this coumarins on other systems, remains to be evaluated. C. brasiliense is used in traditional medicine for the treatment of pain and inflammation. Therefore, we decided to explore the antinociceptive, anti-inflammatory activity of soulattrolide in mice, as well as, some of its possible effects on the CNS. Soulattrolide showed antinociceptive effects in the writhing test (ED50 = 33.8 mg/kg), as well as, in the formalin test with an ED50 = 7.9, and 22.1 mg/kg for Phases 1 and 2, respectively. The highest dose of soulattrolide (50 mg/kg) induced 40% of antinociception in the hot plate test. Regarding to anti-inflammatory activity, in the 12-O-Tetradecanoylphorbol-13-acetate (TPA) test, soulattrolide showed an IC50 = 1.81 µmol/ear, whereas in the myeloperoxidase assay, it showed an inhibition of 87% (1 µmol/ear). Soulattrolide showed sedative effects on the pentobarbital-induced sleeping time test, and the rotarod test, but lacked antidepressant activity on the tail suspension test. In conclusion, we report for the first time, the antinociceptive effects of soulattrolide in mice, like those of naproxen; soulattrolide also showed mild anti-inflammatory activity, as well as mild sedative and anxiolytic properties, therefore, it has also activity on the CNS.
Assuntos
Analgésicos/farmacologia , Ansiolíticos/farmacologia , Anti-Inflamatórios/farmacologia , Fármacos do Sistema Nervoso Central/farmacologia , Cumarínicos/farmacologia , Medição da Dor/efeitos dos fármacos , Analgésicos/química , Animais , Ansiolíticos/química , Anti-Inflamatórios/química , Fármacos do Sistema Nervoso Central/química , Cumarínicos/química , Relação Dose-Resposta a Droga , Hipnóticos e Sedativos/química , Hipnóticos e Sedativos/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Medição da Dor/métodosRESUMO
The phytoremediation potential of Brazilian trees species Calophyllum brasiliense, Eremanthus crotonoides, Hymenaea courbaril, Inga striata, and Protium heptaphyllum was investigated for contaminated soils containing ametryn and hexazinone. Visual injury, chlorophyll content, plant height, leaf temperature, leaf number, and water-efficient use were evaluated. Residual herbicides at soil substrates were analyzed by LC/MS. Among the species C. brasiliense and H. courbaril were tolerant to both herbicides. P. Heptaphyllum presented tolerance at ametryn treatment. E. crotonoides, I. striata, and P. heptaphyllum died in hexazinone treatment. A high content of residual ametryn was found for E. crotonoides. In ametryn treatment, residual herbicide has decreased for C. brasiliense and E. crotonoides species. C. brasiliense highlighted among others becoming a good agent for phytoremediation of soils contaminated with traces of ametryn and hexazinone.
Assuntos
Herbicidas/análise , Poluentes do Solo/análise , Solo/química , Árvores/crescimento & desenvolvimento , Triazinas/análise , Biodegradação Ambiental , BrasilRESUMO
Mast cells (MCs) are important effectors in allergic reactions since they produce a number of pre-formed and de novo synthesized pro-inflammatory compounds in response to the high affinity IgE receptor (FcεRI) crosslinking. IgE/Antigen-dependent degranulation and cytokine synthesis in MCs have been recognized as relevant pharmacological targets for the control of deleterious inflammatory reactions. Despite the relevance of allergic diseases worldwide, efficient pharmacological control of mast cell degranulation has been elusive. In this work, the xanthone jacareubin was isolated from the heartwood of the tropical tree Callophyllum brasilense, and its tridimensional structure was determined for the first time by X-ray diffraction. Also, its effects on the main activation parameters of bone marrow-derived mast cells (BMMCs) were evaluated. Jacareubin inhibited IgE/Ag-induced degranulation in a dose-response manner with an IC50â¯=â¯46â¯nM. It also blocked extracellular calcium influx triggered by IgE/Ag complexes and by the SERCA ATPase inhibitor thapsigargin (Thap). Inhibition of calcium entry correlated with a blockage on the reactive oxygen species (ROS) accumulation. Antioxidant capacity of jacareubin was higher than the showed by α-tocopherol and caffeic acid, but similar to trolox. Jacareubin shown inhibitory actions on xanthine oxidase, but not on NADPH oxidase (NOX) activities. In vivo, jacareubin inhibited passive anaphylactic reactions and TPA-induced edema in mice. Our data demonstrate that jacareubin is a potent natural compound able to inhibit anaphylactic degranualtion in mast cells by blunting FcεRI-induced calcium flux needed for secretion of granule content, and suggest that xanthones could be efficient anti-oxidant, antiallergic, and antiinflammatory molecules.
Assuntos
Anafilaxia/metabolismo , Cálcio/metabolismo , Mastócitos/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Receptores de IgE/antagonistas & inibidores , Xantonas/farmacologia , Animais , Degranulação Celular/efeitos dos fármacos , Degranulação Celular/fisiologia , Células Cultivadas , Relação Dose-Resposta a Droga , Líquido Extracelular/efeitos dos fármacos , Líquido Extracelular/metabolismo , Masculino , Mastócitos/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos C57BL , Difração de Raios X , Xantonas/isolamento & purificaçãoRESUMO
Jacareubin is a xanthone isolated from the heartwood of Calophyllum brasiliense with antibacterial and gastroprotective properties and the intention for clinical use as an anti-cancer treatment (due to the similar chemical structure to other anti-neoplastic drugs) requires an investigation of whether this compound can generate adverse effects on non-transformed cells. Jacareubin (0.5-1000µM in DMSO) was more cytotoxic on phytohemagglutinin (PHA)-stimulated normal human peripheral blood mononuclear cells (PBMCs; IC50 at 72h by MTT: 85.9µM) than on G0 phase-PBMCs (IC50 315.6µM) using trypan blue exclusion and formazan metabolism assays. Jacareubin had lower toxicity on PBMCs than Taxol (1µM). Jacareubin presented cytostatic activity because it inhibited PHA-stimulated PBMCs proliferation (from 2.5µM; CFSE dilution and replication index). Jacareubin induced PBMCs arrest in G0/G1 phase of the cell cycle (from 5µM) as evaluated by DNA content. Moreover, Jacareubin generated genotoxicity by breaking DNA strands selectively in PHA-stimulated PBMCs (from 5µM) rather than on resting PBMCs using the single-cell gel electrophoresis assay and increasing the frequency of micronucleated (MN) PBMCs in vitro (from 5µM) and frequency of hypodiploid cells (from 10µM). When 100mg/kg Jacareubin was injected i.p. into mice (a fifth of the LD50; 0.548g/kg. Approximately to 300µM in vitro), we observe no increase in the MN level in bone marrow cells. Jacareubin can be consider for further anti-tumoural activity due to its preferential genotoxic, cytotoxic and cytostatic actions on proliferating cells rather than on resting cells and the lack of in vivo genotoxicity.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Calophyllum/química , Dano ao DNA , Eritrócitos/efeitos dos fármacos , Leucócitos Mononucleares/efeitos dos fármacos , Extratos Vegetais/farmacologia , Xantonas/farmacologia , Adulto , Aneuploidia , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/toxicidade , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Morte Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Eritrócitos/patologia , Humanos , Concentração Inibidora 50 , Leucócitos Mononucleares/patologia , Masculino , Camundongos Endogâmicos BALB C , Micronúcleos com Defeito Cromossômico/induzido quimicamente , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Medição de Risco , Fatores de Tempo , Xantonas/isolamento & purificação , Xantonas/toxicidade , Adulto JovemRESUMO
Calophyllum brasiliense is used as anti-inflammatory and analgesic in Brazilian traditional medicine. Thus, the main purpose of this study is to evaluate the antinociceptive effect of the chloroform fraction of C. brasiliense (CFCB) roots and to investigate its main mechanism of action. The antinociceptive effect of CFCB was evaluated in mice using acetic acid-induced writhing, formalin-induced paw licking, and hot-plate tests and capsaicin- and glutamate-induced nociception. Brasiliensic acid and 1,2-dimethoxyxanthone were isolated and evaluated in writhing test. The amount of 1,2-dimethoxyxanthone was determined in the fraction by UPLC-DAD. CFCB inhibited abdominal constrictions induced by acetic acid up to 97%, with an ID50 of 9.4 mg/kg (i.p.) and 131.8 mg/kg (p.o.). In the formalin test, CFCB impaired paw licking with an ID50 of 26.3 mg/kg for the first phase and 27.5 mg/kg for the second phase (i.p.). The painful response evoked by capsaicin and glutamate was significantly reduced (ID50 26.7 and 47.9 mg/kg, i.p.). The latency time was increased up to 76% at 60 mg/kg (i.p.) in the hot-plate test. 1,2-Dimethoxyxanthone was almost three times more potent (ID50 27.6 µmol/kg, i.p.) than brasiliensic acid (72.0 µmol/kg) in acetic acid-induced writhing test. The amount of the xanthone was estimated as 92.5 mg/g in the extract. CFCB inhibited the nociceptive response associated to several agents. TRPV1 channels play an important role in the mechanism of action of the fraction. In addition, 1,2-dimethoxyxanthone largely contributes to the antinociceptive effect of CFCB.
Assuntos
Analgésicos/farmacologia , Calophyllum , Medicina Tradicional , Extratos Vegetais/farmacologia , Animais , Brasil , Calophyllum/química , Masculino , Camundongos , Canais de Cátion TRPV/fisiologiaRESUMO
Abstract In order to obtain an arbuscular mycorrhizal fungi (AMF) native inoculum from Sierra de Moa and determine the most appropriate conditions for its big scale production, four light and temperature combinations were tested in three plant species (Calophyllum antillanum, Talipariti elatum and Paspalum notatum). Growth and development parameters, as well as the mycorrhizal functioning of the seedlings were evaluated. The natural light treatment under high temperatures (L-H) was the most suitable for the growth and development of the three plant species, showing the highest total biomass values, mainly of root, and a positive root-shoot ratio balance. This treatment also promoted higher values of root mycorrhizal colonization, external mycelium and AMF spore density. A total of 38 AMF species were identified among the plants and environmental conditions tested. Archaeospora sp.1, Glomus sp.5, Glomus brohultii and G. glomerulatum were observed in all the treatments. The L-H condition can be recommended for native inoculum production, as it promotes a better expression of the AM symbiosis and an elevated production of mycorrhizal propagules.
Assuntos
Raízes de Plantas/microbiologia , Micorrizas , Meio Ambiente , Microbiologia do Solo , Esporos Fúngicos , Simbiose , Contagem de Colônia Microbiana , Micorrizas/crescimento & desenvolvimento , Plântula/crescimento & desenvolvimento , Plântula/microbiologiaRESUMO
In order to obtain an arbuscular mycorrhizal fungi (AMF) native inoculum from Sierra de Moa and determine the most appropriate conditions for its big scale production, four light and temperature combinations were tested in three plant species (Calophyllum antillanum, Talipariti elatum and Paspalum notatum). Growth and development parameters, as well as the mycorrhizal functioning of the seedlings were evaluated. The natural light treatment under high temperatures (L-H) was the most suitable for the growth and development of the three plant species, showing the highest total biomass values, mainly of root, and a positive root-shoot ratio balance. This treatment also promoted higher values of root mycorrhizal colonization, external mycelium and AMF spore density. A total of 38 AMF species were identified among the plants and environmental conditions tested. Archaeospora sp.1, Glomus sp.5, Glomus brohultii and G. glomerulatum were observed in all the treatments. The L-H condition can be recommended for native inoculum production, as it promotes a better expression of the AM symbiosis and an elevated production of mycorrhizal propagules.(AU)
Assuntos
Micorrizas , Glomeromycota , Conservação dos Recursos Naturais/métodos , Conservação de Terras , CubaRESUMO
In order to obtain an arbuscular mycorrhizal fungi (AMF) native inoculum from Sierra de Moa and determine the most appropriate conditions for its big scale production, four light and temperature combinations were tested in three plant species (Calophyllum antillanum, Talipariti elatum and Paspalum notatum). Growth and development parameters, as well as the mycorrhizal functioning of the seedlings were evaluated. The natural light treatment under high temperatures (L-H) was the most suitable for the growth and development of the three plant species, showing the highest total biomass values, mainly of root, and a positive root-shoot ratio balance. This treatment also promoted higher values of root mycorrhizal colonization, external mycelium and AMF spore density. A total of 38 AMF species were identified among the plants and environmental conditions tested. Archaeospora sp.1, Glomus sp.5, Glomus brohultii and G. glomerulatum were observed in all the treatments. The L-H condition can be recommended for native inoculum production, as it promotes a better expression of the AM symbiosis and an elevated production of mycorrhizal propagules.
Assuntos
Meio Ambiente , Micorrizas , Raízes de Plantas/microbiologia , Contagem de Colônia Microbiana , Micorrizas/crescimento & desenvolvimento , Plântula/crescimento & desenvolvimento , Plântula/microbiologia , Microbiologia do Solo , Esporos Fúngicos , SimbioseRESUMO
ABSTRACT Diabetes mellitus is a chronic and severe metabolic dysfunction, it's slow and progressive evolution interferes directly in the metabolism of carbohydrates, fats and proteins, causing hyperglycemia, glycosuria, polydipsia, hyperlipidaemia, among others. The aim of this study was to evaluate the antidiabetic effect of hydroethanolic extract and granulated of Calophyllum brasiliense Cambess., Clusiaceae, species in diabetic rats as well as it's biochemical parameters. The results demonstrated that both the pharmaceutical forms, hydroethanolic extract and granulated, were able to reduce significantly (p < 0.001) hyperglycemia and glycosuria, in addition to improve polydipsia, polyuria, and weight loss. Treatments using hydroethanolic extract and granulated were also able to reduce significantly levels of triacylglycerides, cholesterol and low-density lipoprotein, as well as the transaminases, urea and creatinine levels. Therefore, it is concluded that these pharmaceutical forms have anti-diabetic effect and act improving the biochemical parameters, this effect is probably due to the high content of polyphenolic compounds found in the formulations.
RESUMO
Calophyllum brasiliense (Calophyllaceae) is a tropical rain forest tree distributed in Central and South America. It is an important source of tetracyclic dipyrano coumarins (Soulatrolide) and Mammea type coumarins. Soulatrolide is a potent inhibitor of HIV-1 reverse transcriptase and displays activity against Mycobacterium tuberculosis. Meanwhile, Mammea A/BA and A/BB, pure or as a mixture, are highly active against several human leukemia cell lines, Trypanosoma cruzi and Leishmania amazonensis. Nevertheless, there are few studies evaluating their safety profile. In the present work we performed toxicogenomic and toxicological analysis for both type of compounds. Soulatrolide, and the Mammea A/BA + A/BB mixture (2.1) were slightly toxic accordingly to Lorke assay classification (DL50 > 3000 mg/kg). After a short-term administration (100 mg/kg/daily, orally, 1 week) liver toxicogenomic analysis revealed 46 up and 72 downregulated genes for Mammea coumarins, and 665 up and 1077 downregulated genes for Soulatrolide. Gene enrichment analysis identified transcripts involved in drug metabolism for both compounds. In addition, network analysis through protein-protein interactions, tissue evaluation by TUNEL assay, and histological examination revealed no tissue damage on liver, kidney and spleen after treatments. Our results indicate that both type of coumarins displayed a safety profile, supporting their use in further preclinical studies to determine its therapeutic potential.
Assuntos
Calophyllum/química , Cumarínicos/toxicidade , Toxicogenética , Animais , Masculino , Camundongos , Medição de RiscoRESUMO
The Calophyllum genus is well-known for its antimicrobial and cytotoxic activities, and therefore, we analyzed these biological activities for resins of Calophyllum antillanum and Calophyllum inophyllum growing in Cuba. C. antillanum resins showed a potent activity against Plasmodium falciparum (IC50 = 0.3 ± 0.1 µg/mL), while its cytotoxicity against MRC-5 cells was much lower (IC50 = 21.6 ± 1.1 µg/mL). In contrary, the resin of C. inophyllum showed an unspecific activity. The presence of apetalic acid, isoapetalic acid, calolongic acid, pinetoric acid I, pinetoric acid II, isocalolongic acid, pinetoric acid III, and isopinetoric acid III in C. antillanum resins was also confirmed. These results demonstrated for the first time the potential activity of C. antillanum resins against P. falciparum.
Assuntos
Anti-Infecciosos/farmacologia , Calophyllum/química , Plasmodium falciparum/efeitos dos fármacos , Resinas Vegetais/química , Anti-Infecciosos/isolamento & purificação , Calophyllum/classificação , Candida albicans/efeitos dos fármacos , Linhagem Celular , Cromonas/isolamento & purificação , Cromonas/farmacologia , Escherichia coli/efeitos dos fármacos , Humanos , Isoflavonas/isolamento & purificação , Isoflavonas/farmacologia , Leishmania infantum/efeitos dos fármacos , Estrutura Molecular , Staphylococcus aureus/efeitos dos fármacos , Trichophyton/efeitos dos fármacos , Trypanosoma/efeitos dos fármacosRESUMO
This study evaluated the wound healing effects of topical application of an emulsion containing the HPLC-standardised extract from Calophyllum brasiliense Cambess (Clusiaceae) leaves in rats. The macroscopic analysis demonstrated that the wounds treated with the C. brasiliense emulsion healed earlier than the wounds treated with emulsion base and Dersani®. The percentage of wound healing in the group treated with the C. brasiliense emulsion was significantly higher than in the other groups at 7 and 14 days. On day 14, the animals treated with the C. brasiliense emulsion exhibited a 90.67% reduction of the wound areas. The histological evaluation revealed that on day 21, the group treated with the C. brasiliense emulsion exhibited a significant increase in fibroblasts compared with the other groups. Thus, the C. brasiliense emulsion had healing properties in the topical treatment of wounds and accelerated the healing process.
Assuntos
Calophyllum/química , Extratos Vegetais/farmacologia , Pele/efeitos dos fármacos , Cicatrização/efeitos dos fármacos , Administração Cutânea , Animais , Cromatografia Líquida de Alta Pressão , Emulsões , Fibroblastos/efeitos dos fármacos , Masculino , Extratos Vegetais/administração & dosagem , Folhas de Planta/química , Ratos , Ratos WistarRESUMO
Tropical trees of Calophyllum genus (Calophyllaceae) have chemical and biological importance as potential source of secondary active metabolites which can lead to the development of new drugs. Research on this species has been rising since 1992 due to the discovering of anti-HIV properties of Calanolide A found in Calophyllum inophyllum leaves. This compound is the most important natural product for potential development of new anti-HIV drugs and phytomedicines. The scientometric analysis (1953-2014) here performed revealed that the most studied species of Calophyllum genus are: C. inophyllum and C. brasiliense, distributed in the Asian, and American continents, respectively. Current research on these species is carried out mainly in India and Brazil, respectively, where these species grow. Research on C. brasiliense is focused mainly on ecological, antiparasitic, cytotoxic properties, and isolation of new compounds. Chemical studies and biodiesel development are the main topics in the case of C. inophyllum. Text mining analysis revealed that coumarins, and xanthones are the main secondary active metabolites responsible for most of the reported pharmacological properties, and are potential compounds for the treatment of leukemia and against intracellular parasites causing American Trypanosomiasis and Leshmaniasis. On the other hand, C. inophyllum represents an important source for the development of 2nd generation biodiesel. Medicinal and industrial applications of these species may impulse sustainable forest plantations. To our knowledge this is the first scientometric and text mining analysis of chemical and biomedical research on Calophyllum genus, C. brasiliense and C. inophyllum.
RESUMO
This work aimed to study the effect of the Calophyllum brasiliense seed coat on the seed germination process. To this end, three experiments were conducted in laboratory, greenhouse and screenhouse. From a total of six treatments, five are related to the seed coat (mechanical scarification; mechanical scarification followed by 2 hours in water, chemical scarification, hot water immersion and complete seed coat removal) and one control. Laboratory and greenhouse experiments were conducted in a completely randomized design (CRD). Screenhouse experiment was conducted in a completely randomized block design (RBD). We evaluated the total percentage, the speed index and the average time of germination or emergence. Data were subjected to analysis of variance and means compared by LSD test, at 5%. Under the conditions of this work, it was possible to infer that, in laboratory, mechanical scarification followed by 2 hours in water increases the proportion and germination speed index (GSI), in the greenhouse, the complete seed coat removal increases the percentage and emergence speed index (ESI), and in the screenhouse, mechanical scarification followed by 2 hours in water and chemical scarification presented the best results. The average germination time was not significantly different in the three experiments evaluated.
Objetivou-se com este trabalho estudar o efeito do envoltório da semente de Calophyllum brasiliense no processo de germinação. Foram montados três experimentos, sendo estes conduzidos em laboratório, casa de vegetação e telado. Avaliaram-se seis tratamentos, sendo cinco relacionados ao envoltório (escarificação mecânica; escarificação mecânica seguido por 2h em água; escarificação química; imersão em água quente; e retirada total do envoltório) e a testemunha. Os experimentos em laboratório e casa de vegetação foram conduzidos em delineamento inteiramente casualizado. No telado, o experimento foi conduzido em delineamento em blocos casualizados. Avaliaram-se a percentagem total; o índice de velocidade e o tempo médio de germinação ou emergência. Os dados foram submetidos à análise de variância e as médias comparadas pelo teste t (LSD) a 5% de probabilidade. Foi possível inferir que no laboratório, a escarificação mecânica, seguido por 2h em água, aumenta a percentagem e o índice de velocidade de germinação (IVG); na casa de vegetação, a retirada total do envoltório aumenta a percentagem e o índice de velocidade de emergência (IVE); e no telado, a escarificação mecânica, seguida por 2h em água, e a escarificação química apresentam os melhores resultados. O tempo de germinação não apresentou diferença significativa nos três experimentos avaliados.
Assuntos
Calophyllum , Clusiaceae , Germinação , Dormência de Plantas , SementesRESUMO
Calophyllum brasiliense Cambess. is a tree species that is presented as an alternative to replace endangered species of hardwood. The morphology and anatomy of the seedling of this species is the object of the present study. Seedlings at different stages of development were obtained in greenhouse and analyzed fresh and fixed in FAA (Formalin- Acetic-Alcohol) 50. The anatomical analysis was done by the freehand and microtome sections, according to standard techniques in plant anatomy. The seedling and/or tirodendro is cryptocotylar and hypogeal, has cataphylls, and presents eophylls and metaphylls simple with venation pinnate craspedodromous simple. The root is polyarch, the hypocotyl is very short, the cotyledons have an oily and starchy reserve, the epicotyl has stem structure, and eophylls and metaphylls are dorsiventral. The seedling may be classified in the Horsfieldia type/subtype.
Calophyllum brasiliense Cambess. é uma planta arbórea que se apresenta como possível alternativa para substituir espécies em extinção com madeira nobre. A morfologia e anatomia da plântula desta espécie é objeto do presente trabalho. As plântulas, em diferentes fases de desenvolvimento, foram obtidas em casa de vegetação e analisadas a fresco e fixadas em FAA 50. A análise anatômica foi feita mediante seções a mão livre e microtômicas, de acordo com técnicas usuais em anatomia vegetal. A plântula e/ou tirodendro é criptocotiledonar e hipogeia, possui catafilos, e apresenta eófilos e metafilos simples de venação pinada craspedódroma simples. A raiz é poliarca, o hipocótilo é muito reduzido, os cotilédones possuem reserva amilácea e oleaginosa, o epicótilo tem natureza caulinar e os eofilos e metafilos são dorsiventrais. A plântula enquadra-se no tipo e subtipo Horsfieldia.