RESUMEN
Myrcia bella is a medicinal plant used for the treatment of diabetes, hemorrhages, and hypertension in Brazilian folk medicine. Considering that plant extracts are attractive sources of new drugs, the aim of the present study was to verify the influence of incorporating 70% hydroalcoholic of M. bella leaves in nanostructured lipid systems on the mutagenic and antifungal activities of the extract. In this work, we evaluated the antifungal potential of M. bella loaded on the microemulsion against Candida sp for minimum inhibitory concentration, using the microdilution technique. The system was composed of polyoxyethylene 20 cetyl ether and soybean phosphatidylcholine (10%), grape seed oil, cholesterol (10%: proportion 5/1), and purified water (80%). To investigate the mutagenic activity, the Ames test was used with the Salmonella Typhimurium tester strains. M. bella, either incorporated or free, showed an important antifungal effect against all tested strains. Moreover, the incorporation surprisingly inhibited the mutagenicity presented by the extract. The present study attests the antimicrobial properties of M. bella extract, contributing to the search for new natural products with biological activities and suggesting caution in its use for medicinal purposes. In addition, the results emphasize the importance of the use of nanotechnology associated with natural products as a strategy for the control of infections caused mainly by the genus Candida sp.
Asunto(s)
Myrtaceae , Plantas Medicinales , Antifúngicos/farmacología , Mutágenos , Extractos Vegetales/farmacologíaRESUMEN
This study evaluated the effect of experimental solutions containing plant extracts on bacterial species and enamel caries prevention. Microcosm biofilm was produced from human saliva mixed with McBain saliva (0.2% sucrose) on bovine enamel for 5 days (3 days under anaerobiosis and 2 days under aerobiosis) at 37°C. From the 2nd day, the following treatments were applied (1 × 60 s/day): Vochysia tucanorum (10 mg/mL); Myrcia bella (5 mg/mL); Matricaria chamomilla (80 mg/mL); Malva sylvestris, fluoride, and xylitol (Malvatricin Plus®); 0.12% chlorhexidine (CHX, PerioGard®); and PBS (negative control). The medium pH was measured. Quantitative polymerase chain reaction was performed for the detection of Streptococcus mutans and Lactobacillus spp. Enamel demineralization was measured by spectral-domain optical coherence tomography. The data were compared by means of the Kruskal-Wallis/Dunn, two-way ANOVA/Bonferroni, and ANOVA/Tukey tests (p < 0.05). The pH decreased after sucrose exposure; only CHX reestablished pH >5.5 by the last day. CHX also eliminated Lactobacillusspp., but the other treatments did not differ significantly from PBS. Malvatricin Plus® and CHX eliminated S. mutans, but the other treatments did not differ from PBS. Similar results were seen concerning the reduction of lesion depth and reflectivity. The experimental natural-extract solutions were ineffective against cariogenic bacteria and in preventing the development of enamel caries.
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Caries Dental , Malva , Matricaria , Desmineralización Dental , Animales , Biopelículas , Bovinos , Caries Dental/prevención & control , Susceptibilidad a Caries Dentarias , Humanos , Extractos Vegetales/farmacología , Streptococcus mutansRESUMEN
Environmental conditions influence specialized plant metabolism. However, many studies aiming to understand these modulations have been conducted with model plants and/or under controlled conditions, thus not reflecting the complex interaction between plants and environment. To fully grasp these interactions, we investigated the specialized metabolism and genetic diversity of a native plant in its natural environment. We chose Myrcia bella due to its medicinal interest and occurrence in Brazilian savanna regions with diverse climate and soil conditions. An LC-HRMS-based metabolomics approach was applied to analyze 271 samples harvested across seven regions during the dry and rainy season. Genetic diversity was assessed in a subset of 40 samples using amplified fragment length polymorphism. Meteorological factors including rainfall, temperature, radiation, humidity, and soil nutrient and mineral composition were recorded in each region and correlated with chemical variation through multivariate analysis (MVDA). Marker compounds were selected using a statistically informed molecular network and annotated by dereplication against an in silico database of natural products. The integrated results evidenced different chemotypes, with variation in flavonoid and tannin content mainly linked to soil conditions. Different levels of genetic diversity and distance of populations were found to be correlated with the identified chemotypes. These observations and the proposed analytical workflow contribute to the global understanding of the impact of abiotic factors and genotype on the accumulation of given metabolites and, therefore, could be valuable to guide further medicinal exploration of native species.
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Flavonoides/química , Metabolómica/métodos , Myrtaceae/química , Taninos/química , Análisis del Polimorfismo de Longitud de Fragmentos Amplificados , Cromatografía Liquida , ADN de Plantas/genética , Variación Genética , Pradera , Myrtaceae/genética , Extractos Vegetales/químicaRESUMEN
Hymenaea courbaril has been used to treat different diseases, although its properties are yet to be scientifically validated. The objective of this study was to determine the cytotoxicity, genotoxicity, antigenotoxicity and antioxidant potentials of hydroethanolic extract from H. courbaril seeds. Therefore, for the cytotoxicity test an anti-melanoma assay was performed in B16F10 strain cells. The genotoxicity and antigenotoxicity was evaluated in bone marrow cells (Permit number: 002/2010) of mice, the antioxidant activity was determined by the DPPH test and the total flavonoid content was also determined. The hydroethanolic extract showed antigenotoxic effect and antioxidant activity. It was verified that total flavonoid content was 442.25±18.03 mg RE/g dry extract. HPLC-PAD chromatogram revealed presence of flavones as majority compound in evaluated extract. The results allowed us to also infer that the hydroethanolic extract from seeds shows cytotoxic activity against B16F10 melanoma cells line and it has dose-and-time-dependency.
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Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Células de la Médula Ósea/efectos de los fármacos , Hymenaea/química , Melanoma/patología , Extractos Vegetales/farmacología , Animales , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/aislamiento & purificación , Línea Celular Tumoral , Cromatografía Líquida de Alta Presión , Daño del ADN/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Masculino , Ratones , Pruebas de MicronúcleosRESUMEN
CONTEXT: Bauhinia L. species, including Bauhinia holophylla (Bong.) Steud. (Fabaceae), have traditionally been used to treat diabetes. Bauhinia is a complex botanical genus, and the indiscriminate use of the diverse Bauhinia species is reflected in the experimental divergence of their medicinal potential. OBJECTIVE: The hypoglycaemic and hypolipidaemic effects, molecular mechanism of action and phytochemical properties of an authentic extract of B. holophylla leaves were evaluated. MATERIALS AND METHODS: A phytochemical study of a 70% EtOH extract was performed using FIA-ESI-IT-MS/MSn and HPLC-PAD-ESI-IT-MS. The extract (200 or 400 mg/kg b.w.) was administered for 14 days to streptozotocin-induced diabetic Swiss mice. Glucose tolerance and insulin sensitivity, blood parameters, gene and protein expression, and the in vivo and in vitro inhibition of intestinal glucosidases were assessed. RESULTS: HPLC-PAD-ESI-IT-MS analysis identified flavonoid derivatives of quercetin, myricetin, luteolin and kaempferol. Treatment with 400 mg/kg of the extract reduced blood glucose (269.0 ± 32.4 mg/dL vs. 468.0 ± 32.2 mg/dL for diabetic animals), improved glucose tolerance, decreased cholesterol and triglyceride levels, and increased the mRNA expression of proteins involved in glucogenesis in the liver and muscle, such as PI3-K/Akt, GS, GSK3-ß (ser-9), AMPK and Glut4. The activity of intestinal maltase was inhibited in vitro (IC50: 43.0 µg/mL for the extract compared to 516.4 µg/mL for acarbose) and in vivo. DISCUSSION AND CONCLUSIONS: Treatment with B. holophylla was associated with a marked hypoglycaemic effect through the stimulation of glycogenesis and inhibition of gluconeogenesis and intestinal glucose absorption, without increasing basal insulinaemia.
Asunto(s)
Bauhinia/química , Glucemia/biosíntesis , Diabetes Mellitus Experimental/tratamiento farmacológico , Glucógeno Sintasa Quinasa 3 beta/antagonistas & inhibidores , Hipoglucemiantes/uso terapéutico , Extractos Vegetales/uso terapéutico , Animales , Diabetes Mellitus Experimental/sangre , Relación Dosis-Respuesta a Droga , Hipoglucemiantes/aislamiento & purificación , Masculino , Ratones , Extractos Vegetales/aislamiento & purificación , EstreptozocinaRESUMEN
Candida biofilms adhere to the internal surface of removable dentures, which is an etiological factor in the pathogenesis of denture stomatitis (DS). Adhesive materials are used at the base of maxillary complete dentures to improve their retention and chewing qualities. This article reports the antimicrobial activity of the enriched fractions of Equisetum giganteum and Punica granatum incorporated into a denture adhesive against C. albicans biofilm. The biofilms were induced on the surface of heat-cured acrylic resin specimens that were previously treated with a mixture of adhesive/herb extracts. The antimicrobial activity was evaluated by CFU counts, XTT reduction, and SEM and CLSM analysis. Both herb extracts amplified the anti-biofilm action of the adhesive on the acrylic resin by up to 12 h. Therefore, when these extracts were combined with COREGA®, they played a collaborative and innovative role in biofilm control and can be considered alternatives for temporary use in the treatment and/or prevention of DS.
Asunto(s)
Adhesivos/farmacología , Antiinfecciosos/farmacología , Biopelículas/efectos de los fármacos , Candida albicans/efectos de los fármacos , Bases para Dentadura/microbiología , Equisetum/química , Lythraceae/química , Resinas Acrílicas/química , Adhesivos/química , Antiinfecciosos/química , Biopelículas/crecimiento & desarrollo , Cementos Dentales/química , Cementos Dentales/farmacología , Humanos , Estomatitis Subprotética/prevención & controlRESUMEN
The objective of this study was to evaluate the pharmacological mechanisms involved in anti-inflammatory and antidiarrheal actions of hydroalcoholic extract obtained from the leaves of Cissus sicyoides (HECS). The anti-inflammatory effect was evaluated by oral administration of HECS against acute model of edema induced by xylene, and the mechanisms of action were analysed by involvement of arachidonic acid (AA) and prostaglandin E2 (PGE2). The antidiarrheal effect of HECS was observed and we analyzed the motility and accumulation of intestinal fluid. We also analyzed the antidiarrheal mechanisms of action of HECS by evaluating the role of the opioid receptor, α2 adrenergic receptor, muscarinic receptor, nitric oxide (NO) and PGE2. The oral administration of HECS inhibited the edema induced by xylene and AA and was also able to significantly decrease the levels of PGE2. The extract also exhibited significant anti-diarrheal activity by reducing motility and intestinal fluid accumulation. This extract significantly reduced intestinal transit stimulated by muscarinic agonist and intestinal secretion induced by PGE2. Our data demonstrate that the mechanism of action involved in the anti-inflammatory effect of HECS is related to PGE2. The antidiarrheal effect of this extract may be mediated by inhibition of contraction by acting on the intestinal smooth muscle and/or intestinal transit.
Asunto(s)
Antiinflamatorios/administración & dosificación , Antidiarreicos/administración & dosificación , Cissus/química , Edema/tratamiento farmacológico , Intestinos/patología , Extractos Vegetales/administración & dosificación , Animales , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antidiarreicos/química , Antidiarreicos/farmacología , Dinoprostona/metabolismo , Modelos Animales de Enfermedad , Edema/inducido químicamente , Edema/metabolismo , Intestinos/efectos de los fármacos , Masculino , Ratones , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Xilenos/efectos adversosRESUMEN
CONTEXT: "Aroeira" [Myracrodruon urundeuva Allemão (Anacardiaceae)] is a tree whose leaves have been studied for therapeutic purposes in medicine and dentistry. OBJECTIVE: The study chemically identifies the leaf extract of aroeira and determines its effect on human gingival fibroblasts. MATERIALS AND METHODS: An 80% methanol leave extract was obtained by maceration and chemically identified through flow-injection analysis-electrospray ionization-ion trap-tandem mass spectrometry (FIA-ESI-IT-MSn). Cytotoxicity of the aroeira's methanol extract was evaluated in lineage of fibroblasts. Adherent cells were treated with different concentrations of aroeira's methanol extract in the medium: 0.1, 1, 10, 100 and 1000 µg/mL. Control cells were cultivated in the medium only. Analyses were done at 24, 48, 72 and 96 h of culture by neutral red assay; and at 24, 48 and 96 h by crystal violet assay. RESULTS: FIA-ESI-IT-MS analysis determined the presence of compounds, for the first time in the species: quercetin-O-glucuronide and quercetin-O-deoxyhexose-O-glucose in the extract. On one hand, neutral red and crystal violet assay showed a reduction (to 50% up until 100%) of cellular viability of groups of 100 and 1000 µg/mL compared with control at 96 h (p < 0.05). On the other hand, lower concentrations (0.1; 1 and 10 µg/mL) of the extract were similar to that of the control at 96 h (p < 0.05), in general. CONCLUSIONS: In view of the results, we can conclude that the extract of aroeira presents tannins and flavonoids. Furthermore, the extract is capable of modulating the viability of human gingival fibroblasts according to its concentration.
Asunto(s)
Anacardiaceae/química , Extractos Vegetales/farmacología , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Fibroblastos/efectos de los fármacos , Fibroblastos/fisiología , Humanos , Hojas de la Planta , Espectrometría de Masa por Ionización de Electrospray , Espectrometría de Masas en TándemRESUMEN
Bauhinia ungulata is a plant used in Brazilian traditional medicine for the treatment of diabetes. Phytochemical studies revealed flavonoids and the saccharide pinitol related to hypoglycemic activity of the Bauhinia species. To determine the effects of water deficit on ecophysiological parameter and metabolite fingerprints of B. ungulata, specimens were treated with the following water regimens under greenhouse conditions: daily watering (control), watering every 7 days (group 7D), and watering every 15 days (group 15D). Metabolite profiling of the plants subjected to water deficit was determined by LC-HRMS/MS. An NMR-based metabolomics approach applied to analyze the extracts revealed increased levels of known osmoprotective and bioactive compounds, such as D-pinitol, in the water deficit groups. Physiological parameters were determined by gas exchange in planta analysis. The results demonstrated a significant decrease in gas exchange under severe drought stress, while biomass production was not significantly different between the control and group 7D under moderate stress. Altogether, the results revealed that primary and specialized/secondary metabolism is affected by long periods of severe water scarcity downregulating the biosynthesis of bioactive metabolites such as pinitol, and the flavonoids quercetin and kaempferol. These results may be useful for guiding agricultural production and standardizing medicinal herb materials of this medicinal plant.
RESUMEN
Water and nitrogen availability are two major environmental factors that can impair plant growth, and when combined, their effects on plant performance can be either intensified or reduced. The objective of this study was to analyze the influence of nitrogen availability on the responses of Amaranthus cruentus's metabolism to water stress. The plants were cultivated in plastic pots filled with vermiculite, kept under greenhouse conditions, and were watered three times a week with 70% of a full strength nitrogen-free Long Ashton solution, containing 1.97 or 9.88 kg N ha-1 as ammonium nitrate. Photosynthetic parameters were evaluated in planta, and leaves were harvested for chemical analysis of photosynthetic pigments, proline, and phenolic contents. Higher nitrogen supply increased the shoot dry matter, photosynthetic pigments, photosynthesis, stomatal conductance, transpiration, total leaf nitrogen, proline, nitrate, and ammonium but reduced the concentration of flavonoids and total phenols. Six days of water stress did not affect dry matter, photosynthetic pigments, leaf nitrogen, ammonium, or specialized metabolites but increased the proline under high nitrogen and negatively affected stomatal conductance, transpiration, photosynthesis, relative water content, instantaneous water use efficiency, and leaf nitrate. The negative effect was more pronounced under high nitrogen supply. The results show that the addition of a high amount of nitrogen made the physiological processes of plants more sensitive to water stress, indicating that the plant response to water restriction depends on the interaction between the different environmental stressors to which the plants are subjected.
Asunto(s)
Amaranthus , Compuestos de Amonio , Amaranthus/metabolismo , Deshidratación , Sequías , Nitratos , Nitrógeno , Prolina/metabolismo , Estrés FisiológicoRESUMEN
Aim: This study investigated the effect of denture liners surface modification with Equisetum giganteum (EG) and Punica granatum (PG) on Candida albicans biofilm inhibition supposing its usage as a sustained-release therapeutical delivery system for Candida-associated denture stomatitis. Materials & methods:C. albicans biofilm (SC5314 or ATCC 90028) was formed on soft liners superficially modified by a primer mixed to drugs at minimum inhibitory concentrations (0.100 g for EG and PG or 0.016 g for nystatin per ml of primer). After 24 h, 7 or 14 days, antibiofilm activity was evaluated by colony-forming unit counts. Results: Not all groups were equi-efficient to nystatin after 24 h and 7 days. After 14 days, EG and PG efficacies were not different from nystatin (almost 100% inhibition). Conclusion: The proposed protocol presents a promising option to allopathic drugs for Candida-associated denture stomatitis treatment.
Asunto(s)
Alineadores Dentales , Equisetum , Granada (Fruta) , Estomatitis Subprotética , Antifúngicos/farmacología , Biopelículas , Candida albicans , Humanos , Nistatina/farmacología , Estomatitis Subprotética/tratamiento farmacológicoRESUMEN
This study investigated the effects of herbal toothpaste on bacterial counts and enamel demineralization. Thirty-six bovine enamel samples were exposed to a microcosm biofilm using human saliva and McBain saliva (0.2% sucrose) for 5 days at 37 °C and first incubated anaerobically, then aerobically-capnophilically. The following experimental toothpaste slurries (2 × 2 min/day) were applied: (1) Vochysia tucanorum (10 mg/g); (2) Myrcia bella (5 mg/g); (3) Matricaria chamomilla (80 mg/g); (4) Myrrha and propolis toothpaste (commercial); (5) fluoride (F) and triclosan (1450 ppm F), 0.3% triclosan and sorbitol (Colgate®, positive control); (6) placebo (negative control). The pH of the medium was measured, bacteria were analyzed using quantitative polymerase chain reaction, and enamel demineralization was quantified using transverse microradiography. The total bacterial count was reduced by toothpaste containing Myrcia bella, Matricaria chamomilla, fluoride, and triclosan (commercial) compared to the placebo. As far as assessable, Myrcia bella, Matricaria chamomilla, and Myrrha and propolis (commercial) inhibited the outgrowth of S. mutans, while Lactobacillus spp. were reduced/eliminated by all toothpastes except Vochysia tucanorum. Mineral loss and lesion depth were significantly reduced by all toothpastes (total: 1423.6 ± 115.2 vol% × µm; 57.3 ± 9.8 µm) compared to the placebo (2420.0 ± 626.0 vol% × µm; 108.9 ± 21.17 µm). Herbal toothpastes were able to reduce enamel demineralization.
RESUMEN
Myrcia bella Cambess (Myrtaceae) is an important and common plant, native to the Brazilian Cerrado, with cytotoxicity, antimicrobial, and antidiabetic properties. Therefore, the effects of crude hydroalcoholic extract (CE) and fractions of ellagitannins (ELT) and flavonoids (FV) from Myrcia bella leaves were evaluated in a UMR-106 murine osteosarcoma cells and MC3T3 (normal cell). Cell viability and migration, production of reactive oxygen species (ROS) and matrix metalloproteinase (MMP) -2 and -9 activities were evaluated. In general, CE (80 µg/mL), ELT (160 µg/mL) and FV (64 µg/mL) reduced cell viability (p < 0.05). FV (64 µg/mL) was more effective in inhibition of cell migration, ROS production, and MMP-2 activity when compared to CE and ELT. Myrcia bella a rich source of phenolic compounds and its fraction of flavonoids have cytotoxic effects on osteosarcoma cells, preserving the viability of normal osteoblasts. Due to its antioxidant capacity, flavonoid may be a new therapeutic strategy for cancer.
Asunto(s)
Myrtaceae , Osteosarcoma , Ratones , Animales , Flavonoides/farmacología , Taninos/farmacología , Especies Reactivas de Oxígeno , Extractos Vegetales/farmacología , Antioxidantes/farmacología , Fenoles/farmacología , Hojas de la Planta , Taninos Hidrolizables/farmacología , Osteosarcoma/tratamiento farmacológicoRESUMEN
Miconia is one of the largest genus of the Melastomataceae, with approximately 1,000 species. Studies aiming to describe the diverse biological activities of the Miconia species have shown promising results, such as analgesic, antimicrobial and trypanocidal properties. M. albicans leaves were dried, powdered and extracted to afford chloroformic and methanolic extracts. Total phenolic contents in the methanolic extract were determined according to modified Folin-Ciocalteu method. The antioxidant activity was measured using AAPH and DPPH radical assays. Chemical analysis was performed with the n-butanol fraction of the methanolic extract and the chloroformic extract, using different chromatographic techniques (CC, HPLC). The structural elucidation of compounds was performed using 500 MHz NMR and HPLC methods. The methanolic extract showed a high level of total phenolic contents; the results with antioxidant assays showed that the methanolic extract, the n-butanolic fraction and the isolated flavonoids from M. albicans had a significant scavenging capacity against AAPH and DPPH. Quercetin, quercetin-3-O-glucoside, rutin, 3-(E)-p-coumaroyl-α-amyrin was isolated from the n-butanolic fraction and α-amyrin, epi-betulinic acid, ursolic acid, epi-ursolic acid from the chloroformic extract. The results presented in this study demonstrate that M. albicans is a promising species in the search for biologically active compounds.
Asunto(s)
Antioxidantes/análisis , Melastomataceae/anatomía & histología , Melastomataceae/química , Fenoles/análisis , Hojas de la Planta/química , Animales , Antioxidantes/farmacología , Compuestos de Bifenilo/química , Eritrocitos/efectos de los fármacos , Flavonoides/análisis , Flavonoides/farmacología , Radicales Libres/química , Hemólisis/efectos de los fármacos , Humanos , Metanol/química , Estructura Molecular , Fenoles/farmacología , Picratos/química , Extractos Vegetales/química , Extractos Vegetales/farmacologíaRESUMEN
BACKGROUND: Cancer is a multifactorial disease caused by uncontrolled proliferation of cells. About 50-80% of cancer patients develop cachexia, a complex metabolic syndrome associated with an increase of mortality and morbidity. However, there are no effective therapies in medical clinic for cancer cachexia. Vochysia tucanorum Mart. is a common three of the Brazilian "Cerrado". The butanolic fraction of V. tucanorum (Fr-BuVt), very rich in triterpenes with various biological activities, might be interesting in being tested in cancer cachexia syndrome. Hence, the present study was undertaken to investigate the antitumoral activity of Fr-BuVt and its potential against cachexia development. METHODS: Ehrlich tumor was used as model of cancer cachexia. Ascitic Ehrlich tumor cells were collected, processed and inoculated subcutaneously in saline solution (1 × 107/100 µl; ≥95% viability) for the obtention of solid Ehrlich carcinoma. After inoculation, solid Ehrlich carcinoma-bearing mice were treated by 14 consecutive days by gavage with Fr-BuVt (200 mg/kg). Body weight and tumor volume were measure during the treatment period. Tumors were removed, weighed and properly processed to measure the content and phosphorylation levels of key-proteins involved to apoptotic and proliferation process by Western Blot. Muscles and adipose tissues were removed for weighed. Serum was collected to cytokines levels and energetic blood markers measurements. RESULTS: The treatment with the Fr-BuVt (200 mg/kg, 14 days) decreased the solid Ehrlich tumor volume and weight besides increased the expression of the pro-apoptotic proteins caspase-3 and BAX, but also decreased the expression of the proteins involved in proliferation NFκB, mTOR and ERK. In addition, our data shows that the administration of Fr-BuVt was able to prevent the installation of cancer cachexia in Ehrlich carcinoma-bearing mice, since prevented the loss of body weight, as well as the loss of muscle and adipose tissue. Moreover, an improvement in some blood parameters such as decrease in cytokines TNF-α and IL-6 levels is observed. CONCLUSIONS: The study revealed that Fr-BuVt has antitumoral activity and prevent installation of cancer cachexia in Ehrlich model. Therefore, Fr-BuVt may represent an alternative treatment for cancer cachexia.
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Antineoplásicos Fitogénicos/farmacología , Caquexia/prevención & control , Carcinoma de Ehrlich/tratamiento farmacológico , Myrtales/química , Extractos Vegetales/farmacología , Animales , Antineoplásicos Fitogénicos/aislamiento & purificación , Apoptosis/efectos de los fármacos , Peso Corporal/efectos de los fármacos , Brasil , Butanoles , Caquexia/etiología , Carcinoma de Ehrlich/complicaciones , Proliferación Celular/efectos de los fármacos , Citocinas/sangre , Masculino , Ratones , Ensayos Antitumor por Modelo de XenoinjertoRESUMEN
Bauhinia holophylla leaves, also known as "pata-de-vaca", are traditionally used in Brazil to treat diabetes. Although the hypoglycemic activity of this medicinal plant has already been described, the active compounds responsible for the hypoglycemic activity have not yet been identified. To rapidly obtain two fractions in large amounts compatible with further in vivo assay, the hydroalcoholic extract of B. holophylla leaves was fractionated by Vacuum Liquid Chromatography and then purified by medium pressure liquid chromatography combined with an in vivo Glucose Tolerance Test in diabetic mice. This approach resulted in the identification of eleven compounds (1-11), including an original non-cyanogenic cyanoglucoside derivative. The structures of the isolated compounds were elucidated by nuclear magnetic resonance and high-resolution mass spectrometry. One of the major compounds of the leaves, lithospermoside (3), exhibited strong hypoglycemic activity in diabetic mice at the doses of 10 and 20 mg/kg b.w. and prevents body weight loss. The proton nuclear magnetic resonance (1H NMR) quantification revealed that the hydroalcoholic leaves extract contained 1.7% of lithospermoside (3) and 3.1% of flavonoids. The NMR analysis also revealed the presence of a high amount of pinitol (4) (9.5%), a known compound possessing in vivo hypoglycemic activity. The hypoglycemic properties of the hydroalcoholic leaves extract and the traditional water infusion extracts of the leaves of B. holophylla seem thus to be the result of the activity of three unrelated classes of compounds. Such results support to some extent the traditional use of Bauhinia holophylla to treat diabetes.
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Bauhinia/química , Hipoglucemiantes/aislamiento & purificación , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta/química , Acetonitrilos/aislamiento & purificación , Acetonitrilos/farmacología , Animales , Cromatografía Líquida de Alta Presión , Diabetes Mellitus Experimental/tratamiento farmacológico , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Prueba de Tolerancia a la Glucosa , Glicósidos/aislamiento & purificación , Glicósidos/farmacología , Hipoglucemiantes/farmacología , Inositol/análogos & derivados , Inositol/aislamiento & purificación , Inositol/farmacología , Espectroscopía de Resonancia Magnética , Masculino , Ratones , Extractos Vegetales/farmacologíaRESUMEN
OBJECTIVE: This study evaluated the antibiofilm and anti-caries effects of an experimental mouth rinse containing aqueous extract of Matricaria chamomilla L. METHODS: Microcosm biofilm was produced on bovine enamel, from pooled human saliva mixed with McBain saliva, under 0.2 % sucrose exposure, for 5 days. The biofilm was daily treated using (1â¯mL/1â¯min): Vochysia tucanorum Mart. (2.5â¯mg/mL); Myrcia bella Cambess. (1.25â¯mg/mL); Matricaria chamomilla L. (20â¯mg/mL); Malva sylvestris (Malvatricin® Plus-Daudt); 0.12 % Chlorhexidine (PerioGard®-Palmolive, Positive control) and PBS (Negative control). The % dead bacteria, biofilm thickness, EPS biovolume, lactic acid concentration, the CFU counting (total microorganisms, Lactobacillus sp., total streptococci and Streptococcus mutans/S. sobrinus) were determined. Enamel demineralization was measured by TMR. RESULTS: All mouth rinses induced bacterial death compared to PBS (pâ¯<â¯0.0001). The biofilm thickness varied from 12⯱â¯2⯵m (chlorhexidine) to 18⯱â¯2⯵m (V. tucanorum) (ANOVA/Tukey, pâ¯<â¯0.0001). The EPS biovolume varied from 7(4)% (chlorhexidine) to 30(20)% (PBS) (Kruskal-Wallis/Dunn, pâ¯<â¯0.0001). The lactic acid production was reduced by M. sylvestris (1.1⯱â¯0.2â¯g/L) and chlorhexidine (0.6⯱â¯0.2â¯g/L) compared to PBS (2.6⯱â¯1.3â¯g/L) (ANOVA, pâ¯<â¯0.0001). Malva sylvestris and chlorhexidine showed significant low CFU for total microorganisms, Lactobacillus sp. and total streptococci. Only chlorhexidine significantly reduced S. mutans/S. sobrinus. CFUs for total streptococci and Lactobacillus sp, were also significantly reduced by M. chamomilla L. Malva sylvestris (63.4 % of mineral loss reduction), chlorhexidine (47.4 %) and M. chamomilla L. (39.4 %) significantly reduced enamel demineralization compared to PBS (ANOVA/Tukey, pâ¯<â¯0.0001). CONCLUSION: M. chamomilla L. has lower antibiofilm action, but comparable anti-caries effect to those found for chlorhexidine, under this model. CLINICAL RELEVANCE: This study shows that the antibiofilm and anti-caries potential may vary between the commercial and experimental mouth rinses containing natural agents, with promising results for those containing Matricaria chamomilla L. and Malva Sylvestris.
Asunto(s)
Caries Dental , Matricaria , Desmineralización Dental , Animales , Biopelículas , Cariostáticos , Bovinos , Clorhexidina/farmacología , Esmalte Dental , Humanos , Antisépticos Bucales/farmacología , Streptococcus mutansRESUMEN
OBJECTIVES: The aim of this study was to assess the effect of Myracrodruon urundeuva All. and Qualea grandiflora Mart. leaves hydroalcoholic extracts on viability and metabolism of a microcosm biofilm and on enamel demineralization prevention. METHODOLOGY: Microcosm biofilm was produced on bovine enamel using inoculum from pooled human saliva mixed with McBain saliva, under 0.2% sucrose exposure, for 14 days. The biofilm was daily-treated with the extracts for 1 min. At the end, it was analyzed with respect to viability by fluorescence, CFU counting and extracellular polysaccharides (phenol-sulphuric acid colorimetric assay) and lactic acid (enzymatic assay) production. The demineralization was measured by TMR. The data were compared using ANOVA or Kruskal-Wallis (p<0.05). RESULTS: M. urundeuva All. at 100, 10 and 0.1 µg/mL and Q. grandiflora Mart. at 100 and 0.1 µg/mL reduced biofilm viability similarly to positive control (chlorhexidine) and significantly more than the negative-vehicle control (35% ethanol). M. urundeuva at 1000, 100 and 0.1 µg/mL were able to reduce both lactobacilli and mutans streptococci CFU counting, while Q. grandiflora (1000 and 1.0 µg/mL) significantly reduced mutans streptococci CFU counting. On the other hand, the natural extracts were unable to significantly reduce extracellular polysaccharides and lactic acid productions neither the development of enamel carious lesions. CONCLUSIONS: The extracts showed antimicrobial properties on microcosm biofilm, however, they had no effect on biofilm metabolism and caries protection.
Asunto(s)
Anacardiaceae/química , Antiinfecciosos/farmacología , Biopelículas/efectos de los fármacos , Myrtales/química , Extractos Vegetales/farmacología , Desmineralización Dental/prevención & control , Animales , Cariostáticos/farmacología , Bovinos , Recuento de Colonia Microbiana , Esmalte Dental/efectos de los fármacos , Esmalte Dental/microbiología , Ácido Láctico/metabolismo , Lactobacillus/efectos de los fármacos , Masculino , Pruebas de Sensibilidad Microbiana , Viabilidad Microbiana/efectos de los fármacos , Microrradiografía/métodos , Hojas de la Planta/química , Polisacáridos Bacterianos/metabolismo , Reproducibilidad de los Resultados , Saliva/química , Streptococcus mutans/efectos de los fármacosRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Phytotherapy based on plant-derived compounds is an alternative medicinal strategy for the relief of symptoms and the curing of diseases. The leaves of Myracrodruon urundeuva a medicinal plant also known as "aroeira", has been used in traditional medicine as healing, antiulcer and anti-inflammatory to treat skeletal diseases in Brazil, but its role in bone cell toxicity, as well as in bone formation, remains to be established. AIM OF THE STUDY: We sought to determine the in vitro osteogenic effects of a hydroalcoholic M. urundeuva leaves extract in primary human osteoblasts. MATERIALS AND METHODS: Cell viability, reactive oxygen species (ROS) production, alkaline phosphatase (ALP) activity and matrix mineralization were evaluated by MTT assay, DCFH-DA probe, colorimetric-based enzymatic assay and Alizarin Red-staining, respectively. Besides, the matrix metalloproteinase (MMP)-2 and progressive ankylosis protein homolog (ANKH) gene expression were determined by real-time RT-qPCR and MMP-2 activity by zymography. RESULTS: Exposure of osteoblasts to M. urundeuva extract significantly decreased viability and increased reactive oxygen species (ROS) production, regardless of the extract concentration. The M. urundeuva extract at 10⯵g/mL also downregulated matrix metalloproteinase (MMP)-2, while upregulating progressive ankylosis protein homolog (ANKH) gene expression. By contrast, the MMP-2 activity was unchanged. The M. urundeuva extract at 10⯵g/mL also reduced alkaline phosphatase (ALP) activity and mineralization. CONCLUSIONS: Overall, our findings suggest that the inhibition of osteogenic differentiation and matrix mineralization promoted by M. urundeuva may be due more to an increase in oxidative stress than to the modulation of MMP-2 and ANKH expression.
Asunto(s)
Anacardiaceae , Osteoblastos/efectos de los fármacos , Extractos Vegetales/farmacología , Adulto , Fosfatasa Alcalina/metabolismo , Diferenciación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Humanos , Metaloproteinasa 2 de la Matriz/genética , Metaloproteinasa 2 de la Matriz/metabolismo , Osteoblastos/metabolismo , Hojas de la Planta , Especies Reactivas de Oxígeno/metabolismoRESUMEN
AIM OF THE STUDY: Cissus sicyoides L. is a medicinal plant popularly known in Brazil against various diseases and the research interest in this plant is justifiable because of its potential medicinal value in stomachache and gastric ulcer. MATERIALS AND METHODS: The methanolic extract obtained from the leaves of Cissus sicyoides (Cc) was evaluated for the ability to protect the gastric mucosa against injuries caused by necrotizing agents (0.3 M HCl/60% EtOH, absolute ethanol, piroxicam and pylorus ligature) in rodents. We also evaluated microcirculation, antioxidant action and participation of NO (nitric oxide) and sulfhydryls (SH) groups in the Cc gastroprotective action. RESULTS: Administration of Cc significantly reduced gastric lesions induced by different ulcerogenic agents in rodents. This extract administered by oral route significantly increased gastric volume without exerting antisecretory effect. The Cc effect involved an increase of the defense mechanism of the gastrointestinal mucosa such as NO and SH groups that prevent and attenuate the ulcer process. The Cc also has antioxidant property against oxidative stress but does not modify microcirculation response in gastric mucosa. CONCLUSIONS: These results confirmed the traditional use of Cissus sicyoides for the treatment of gastric ulcer.