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2.
Toxicol Rep ; 9: 1537-1547, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36518414

RESUMEN

Intestinal mucositis (IM) is a frequent adverse effect in anticancer therapy without standard treatment. The oil obtained from sucupira (Pterodon emarginatus) has anti-inflammatory properties, and the soybean lecithin reduces the intestinal toxicity of several xenobiotics. However, their water insolubility impairs the in vivo application. For this reason, we evaluated if the nanoencapsulation of sucupira oil (SO) in lecithin-based nanocapsules (SO-NC) could be a therapeutically effective system for the treatment of IM in murine cisplatin (CDDP)-induced intestinal mucositis model. SO was analyzed by LC-HRMS/MS and HPLC. SO-NC was prepared by nanoprecipitation and characterized using DLS, HPLC, and AFM. Mice body weight and food consumption were assessed daily during experimental mucositis induced by CDDP. The animals were euthanized, and intestinal permeability, inflammatory mediators, and intestinal histology were performed. SO-NC demonstrated adequate characteristics for oral administration as size under 300 nm, IP < 0.3, high EE, and spherical shape. In vitro cytotoxicity performed against RAW 264.7 cell lines resulted in cell viability above 80 % confirming the non-cytotoxic profile of SO (IC50 268 µg/mL) and SO-NC (IC50 118.5 µg/mL) up to 117.2 µg/mL. The untreated mice showed intestinal toxicity after i.p. of CDDP, principally weight loss, increased intestinal permeability, and MPO and TNF-α levels. Surprisingly, the administration of SO to CDDP-mucositis animals did not circumvent the CDDP effects and increased intestinal permeability. However, SO-NC proved efficient in mitigating the experimental intestinal mucositis by improving intestinal epithelium architecture, reducing intestinal permeability, and improving the MPO levels. In conclusion, SO-NC can positively impact intestinal mucositis by promoting mucosal recovery. This is a promising strategy for developing a new treatment for intestinal mucositis.

3.
Inflammopharmacology ; 29(1): 123-135, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-32924074

RESUMEN

BACKGROUND: Bothrops moojeni snake venom (VBm) has toxins that cause pronounced tissue damage and exacerbated inflammatory reaction. Cannabis sativa L. is a plant species that produces an oil (CSO) rich in unsaturated fatty acids. Nano-emulsions have several advantages, such as better stability and higher penetrating power in membranes. Therefore, this study evaluated the effect of a nano-emulsion based on this herbal derivative (NCS) against VBm-induced inflammation in Wistar rats. METHODS: The CSO and NCS were submitted to physicochemical characterization. The inflammatory process was induced by the VBm (0.10 mg/kg) as follows: rat paw edema, peritonitis, analysis of leukocyte infiltrate in gastrocnemius muscle of rats and formation of granulomatous tissue. RESULTS: No significant changes were observed when the NCS was submitted to the centrifugation and thermal stress tests. There was no phase separation, changes in density (0.978 ± 0.01 g/cm3) and viscosity (0.889 ± 0.15). The droplet diameter ranged from 119.7 ± 065 to 129.3 ± 0.15 nm and the polydispersity index ranged from 0.22 ± 0.008 to 0.23 ± 0.011. The results showed that treatments with CSO (200 and 400 mg/kg) and NCS (100 mg/kg) were able to decrease significantly (p < 0.001) the formation of edema and granulomatous tissue. The CSO and NCS groups significantly attenuated (p < 0.001) the recruitment of inflammatory cells in the tests for peritonitis and leukocyte infiltrate. The histopathological analysis of the gastrocnemius muscle showed a reduction in tissue damage caused by VBm. CONCLUSION: The results obtained in this study showed anti-inflammatory activity of the CSO which may be due to a high UFA content. The nanosizing, as evidenced by the incorporation of the CSO in the NCS improved the effect and opens the perspective for the obtainment of a nanomedicine in which a kinetic stable phytotherapic can be used at low doses.


Asunto(s)
Cannabis/química , Venenos de Crotálidos/toxicidad , Inflamación/tratamiento farmacológico , Aceites de Plantas/farmacología , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/farmacología , Bothrops , Edema/tratamiento farmacológico , Edema/patología , Emulsiones , Inflamación/patología , Masculino , Músculo Esquelético/efectos de los fármacos , Músculo Esquelético/patología , Nanoestructuras , Tamaño de la Partícula , Aceites de Plantas/administración & dosificación , Ratas , Ratas Wistar
4.
Drug Deliv Transl Res ; 10(6): 1764-1770, 2020 12.
Artículo en Inglés | MEDLINE | ID: mdl-32876880

RESUMEN

Oil in water nano-emulsions are drug delivery systems constituted by liquid lipophilic nano-droplets dispersed through the external aqueous phase, often reaching the kinetic stability with surfactant as stabilizers. Essential oils can be the oily phase or the source of bioactive compounds. In this study, the essential oil of Aeollanthus suaveolens-a plant used in folk medicine due to its psychopharmacological effects-was used for preparation of fine nano-emulsions by a low-energy titrating method. Monodisperse small nano-droplets (ca. 70 nm; PdI 0.200) were assembled by using blends of non-ionic surfactants, indicating modulation on surfactant system lead to altering the physical property. In a separate set of experiments, we investigated the role of this modulation on biological properties of the optimal nano-emulsion. The zebrafish embryos were more susceptible to the nano-emulsion than the bulk essential oil, showing the improved bioactivity due to nano-sizing. Therefore, adult zebrafish was treated, and paralysis was observed in the groups treated with the nano-emulsion, being this finding in accordance with hypnosis. At the same essential oil dose, another behavior was observed, suggesting that expected dose-dependent effects associated to sedative-hypnotics can be achieved by nano-sizing of psychoactive essential oils. This paper contributes to the state-of-art drug delivery systems by opening perspectives for novel sedative-hypnotics nano-emulsified essentials oils that can reach hypnotic effects at considerably lower dose, when compared with bulk materials, being useful for further completed dose-response studies.Graphical abstract.


Asunto(s)
Lamiaceae/química , Aceites Volátiles/farmacología , Aceites de Plantas/farmacología , Animales , Emulsiones , Nanotecnología , Aceites Volátiles/química , Aceites de Plantas/química , Tensoactivos , Agua , Pez Cebra
5.
J Appl Biomed ; 18(4): 126-135, 2020 12.
Artículo en Inglés | MEDLINE | ID: mdl-34907765

RESUMEN

Dyslipidemias are lipid metabolism alterations that cause increased levels of serum lipoprotein, cholesterol, and triglycerides. These alterations are associated with a higher incidence of cardiovascular diseases and are a risk factor for atherosclerosis development. This study aimed to evaluate the effect of Rosmarinus officinalis essential oil (EORO, 100 mg/kg) and its nanoemulsion (NEORO, 500 µg/kg) on Triton and coconut saturated-fat-induced (CSF) dyslipidemias using Wistar rats. The phytochemical evaluation of EORO performed by gas chromatography-mass spectroscopy (GC-MS) revealed 1,8-cineole (33.70%), camphor (27.68%), limonene (21.99%), and α-pinene (8.13%) as its major compounds. Triton-induced dyslipidemia significantly increased total cholesterol, LDL, and triglycerides levels. On the other hand, the groups treated with EORO and NEORO had significantly reduced total cholesterol, LDL, and triglycerides compared to the group treated only with Triton. Similar results were observed on the positive control treated with simvastatin. Dyslipidemia induced with coconut saturated-fat (CSF) caused abdominal fat gain, hypercholesterolemia, hypertriglyceridemia, increased LDL levels, and atherogenesis in the aorta. In contrast, the groups treated with EORO, NEORO, and simvastatin had significantly reduced hypercholesterolemia and hypertriglyceridemia, reduced abdominal fat gain, and absence of atherogenesis in the vascular endothelium. Overall, in the Triton-induced dyslipidemia model, EORO treatment had superior values than NEORO's (and simvastatin), although the differences were not too high, while in the CSF model, the values were mixed. In this manner, our results show an anti-dyslipidemic and anti-atherogenic activity effect by EORO and NEORO.


Asunto(s)
Aterosclerosis , Dislipidemias , Hipercolesterolemia , Hipertrigliceridemia , Aceites Volátiles , Rosmarinus , Animales , Ratas , LDL-Colesterol , Dislipidemias/inducido químicamente , Dislipidemias/tratamiento farmacológico , Hipercolesterolemia/tratamiento farmacológico , Hipertrigliceridemia/tratamiento farmacológico , Sistema de Administración de Fármacos con Nanopartículas , Aceites Volátiles/química , Aceites Volátiles/farmacología , Ratas Wistar , Rosmarinus/química , Simvastatina , Triglicéridos
6.
J Med Entomol ; 57(3): 788-796, 2020 05 04.
Artículo en Inglés | MEDLINE | ID: mdl-31840745

RESUMEN

Siparuna guianensis (Laurales: Siparunaceae) has a terpene-rich essential oil with great potential for larvicides. The poor water miscibility of their compounds makes nano-emulsions of great interest for novel bioactive systems, including for control of Aedes aegypti (Diptera: Culicidae). This species is adapted to urban environments with important role in the epidemiology of some arboviruses such as dengue, chikungunya fever, zika, and urban yellow fever. The aim of the present study was to evaluate the feasibility of nano-emulsification to affect Ae. aegypti larvae. An optimal system was achieved by using a nonionic single surfactant, highlighted by its satisfactory size distribution profile. Moreover, improved larvicidal activity in comparison to bulk essential oil can be observed for the nano-emulsions. The estimated LC50 and LC90 values after 24 h of treatment of larvae with the essential oil were, respectively, 86.5232 and 134.814 µg/ml, while the estimated LC50 and LC90 value after treatment with the nano-emulsion were 24.7572 and 75.2452 µg/ml, respectively. The utilization of a simple technique to produce a fine nano-emulsion opens perspective for further integrative practices of mosquito control and giving value to this Amazon plant species may encourage its sustainable use and contribute to conservation policies.


Asunto(s)
Aedes , Insecticidas/análisis , Laurales/química , Aceites Volátiles/química , Animales , Formas de Dosificación , Dosificación Letal Mediana , Nanoestructuras , Aceites Volátiles/administración & dosificación
7.
Pharmaceuticals (Basel) ; 12(4)2019 Nov 30.
Artículo en Inglés | MEDLINE | ID: mdl-31801207

RESUMEN

The plant species Libidibia ferrea (Mart. ex Tul.) LP Queiroz var. ferrea basionym of Caesalpinia ferrea (Mart. ex Tul.) is used in various regions of Brazil in folk medicine in the treatment of several health problems, especially in acute and chronic inflammatory processes. Most of the preparations employed are alcoholic. Therefore, this study aimed to evaluate the acute toxicity of the hydroethanolic extract of fruits of Libidibia ferrea (EHEFLf) in zebrafish, emphasizing the possible changes in the organic-cellular level of the gills, liver, kidneys, and intestine and on embryos. The result obtained by LC-M/MS from EHEFLf indicated a high concentration of possible polyhydroxylated substances. EHEFLf, at a dose of 2 g/kg orally, produced non-significant alterations of the analyzed organs. However, for embryos, the treatment with different concentrations demonstrated heart toxicity that was concentration-dependent. There is no evidence of a correlation of the observed effects with the phytochemical composition, and considering the species of animal used, it can be suggested that the oral use of L. ferrea hydroethanolic extract has an acceptable degree of safety for use as an oral medicinal product. and embryo results have shown significant affinity to the heart; however, it is perceived to be related to the concentrations used.

8.
Artículo en Inglés | MEDLINE | ID: mdl-31093296

RESUMEN

The inhabitants of the floodplain of the Mazagão River in the State of Amapá in the Brazilian Amazon have inherited from indigenous African and Cabocla cultures indications for the use and forms of preparation of medicinal plants to cure diseases of the body and spirit. This study aimed to perform an ethnopharmacological survey of medicinal plants used by the riparian community of the floodplains of the Mazagão River, in the State of Amapá. In this study, we chose semistructured interviews with socioeconomic, ethnopharmacological, and ethnobotanical aims. The collection of medicinal plants occurred during guided tours. The Use Value (UV), Informant Consensus Factor (ICF), Correction Factor (CF), and Fidelity level (FL) were calculated. There were 130 species of medicinal plants, distributed in 116 genera and 57 families; Fabaceae (16), Lamiaceae (14), Euphorbiaceae (7), and Arecaceae (6) include 33.33% of the total species sampled. All 95 native species of floodplain forests were previously described, and 35 are exotic species. The species with the highest UV (≥ 0.5) at the mouth of the Mazagão River were Carapa guianensis (0.91), Pentachlethra macroloba (0.83), Dalbergia subcymosa (0.77), Uncaria tomentosa (0.75), Otacanthus azureus (0.62), Virola surinamensis (0.62), Hura crepitans (0.58), Euterpe oleracea (0.56), and Arrabidaea chica (0.51). These species were also the ones that presented the highest ICF among the informants and 100% in FL for a specific therapeutic use. The study is comprised of 16 categories of therapeutic use, of which the majority of the plants used are related to diseases such as microbial infections (20.67%, 73 species), gastrointestinal disorders (13.31%), and inflammation (11.61%). The results showed that knowledge about the use of medicinal plants along the rivers and streams that form the mouth of the Mazagão River is evenly distributed. Most of the interviewees present diversified knowledge about the medicinal resources because they have a close relationship with the floodplain forest. Native species of this forest predominate among the most commonly used medicinal plants as subsidies for future pharmacological studies.

9.
Rev. bras. farmacogn ; 28(5): 618-625, Sept.-Oct. 2018. tab, graf
Artículo en Inglés | LILACS | ID: biblio-977723

RESUMEN

Abstract Aedes aegypti (Diptera: Culicidae) is the main vector of some neglected diseases, including dengue. It is very important to develop formulations that increase effectiveness of vector control with low toxicity. Quercetin is a plant-derived flavonoid that modulates the development of some insects. The low water solubility of quercetin impairs the development of water-dispersible commercial products. To circumvent this problem, the preparation of nanoformulations is considered promising. Thus, this study aimed to evaluate the effect of bulk and quercetin nanosuspension against A. aegypti larvae and also to investigate their ecotoxicity. Quercetin nanosuspension was produced by a solvent displacement method followed by solvent evaporation and was maintained in two different temperatures (4 and 25 ºC). Its size distribution and zeta potential were monitored along 30 days. The influence of quercetin nanosuspension and bulk-quercetin was investigated at various concentrations against A. aegypti and the green algae Chlorella vulgaris. The quercetin nanosuspension presented higher stability at 4 ºC and negative zeta potential values. Quercetin nanosuspension and bulk-quercetin adversely affected the larvae development, especially at the highest concentrations. Larvae mortality was between 44% and 100% (48 h) for quercetin nanosuspension at 100 and 500 ppm, respectively. The bulk-quercetin induced around 50% mortality regardless the concentration used at this same time-period. Absence of emerging mosquitoes from water was observed on the survival larvae of all the treated groups. Quercetin nanosuspension was less toxic than bulk-quercetin against C. vulgaris, especially at higher concentrations. These data indicate that quercetin nanosuspension may represent a potential larvicide for A. aegypti control, once they induced larvae death and inhibited the survival ones to emerge from water. In addition, it did not demonstrated ecotoxicity against a non-target organism, highlighting its better properties, when compared to the bulk-quercetin.

11.
Inflammopharmacology ; 26(4): 1057-1080, 2018 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-29404883

RESUMEN

The essential oil from Rosmarinus officinalis L. (OERO) has bioactive compounds with anti-inflammatory activity. The objective of this study was to evaluate the anti-inflammatory potency of nanoemulsions containing essential oil of Rosmarinus officinalis L. (NOERO, NECHA, NECULT, and NECOM) in vitro and in vivo. This study was accomplished in a quantitative format through tests with diphenyl picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cellular antioxidant activity (CCA), determination of nitric oxide production, cellular viability and anti-inflammatory activity in zebrafish. OERO's were submitted to the analysis-coupled gas chromatography-mass spectrometry (GC-MS), which highlighted 1,8-cineol and camphor as major compounds. NOEROs were obtained by a low-energy method and presenting the medium size smaller than 200 nm. The efficiency of encapsulation by spectrometry and gas chromatographic analysis was 67.61 and 75.38%, respectively. In the CCA assay, all of the samples presented percentage values of inhibition similar to the quercetin pattern, indicating antioxidant activity. In the test for determination of NO·, all of the samples inhibited the production of NO· when compared to LPS, and NOEROS were more effective than OEROS to 5 µg/mL. In the cell viability assay, the cells remained viable after contact with the samples, demonstrating an absence of cytotoxicity. This study showed that all nanoemulsions (NECHA, NECULT, and NECOM) showed no toxicity to macrophages, besides demonstrating antioxidant activity and potentiation of the essential oil effect in the proliferation of viable fibroblasts. Nanoemulsions has also shown the ability to potentiate the anti-inflammatory action of essential oils by exerting immunomodulatory activity by inhibiting the production of the pro-inflammatory mediator nitric oxide. The results obtained with NECHA in zebrafish confirm the hypothesis that prominent terpenic compounds, alpha-pinene, 1,8-cineole, and camphor, became more available at the target sites, inhibiting the inflammatory process in this animal species.


Asunto(s)
Antiinflamatorios/farmacología , Nanopartículas , Aceites Volátiles/farmacología , Rosmarinus/química , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/aislamiento & purificación , Antioxidantes/administración & dosificación , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Modelos Animales de Enfermedad , Emulsiones , Fibroblastos/efectos de los fármacos , Fibroblastos/metabolismo , Cromatografía de Gases y Espectrometría de Masas , Inflamación/tratamiento farmacológico , Inflamación/patología , Masculino , Ratones , Ratones Endogámicos BALB C , Óxido Nítrico/metabolismo , Aceites Volátiles/administración & dosificación , Aceites Volátiles/aislamiento & purificación , Tamaño de la Partícula , Pez Cebra
12.
Inflammopharmacology ; 26(1): 183-195, 2018 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-28707182

RESUMEN

We evaluate the anti-inflammatory and antialgic potency of a nanoemulsion (NEORO) containing the essential oil of Rosmarinus officinalis L. (EORO), which is composed primarily of limonene, camphor and 1,8-cineole. The EORO and NEORO were administered orally 30 min prior to starting the experiments. In a test of rat paw oedema induced by carrageenan, NEORO was effective in doses of 498 µg/kg, and it inhibited 46% of the maximum peak of the oedema; in a dose of 300 mg/kg, EORO inhibited 50% of the maximum peak of the oedema. In an acetic acid-induced writhing test, NEORO yielded a dose-dependent effect, and a dose of 830 µg/kg inhibited 84% of the algesic process; a dose of 100 mg/kg of EORO inhibited 55%. In an assay for H2S production in rat stomachs, a dose of 498 µg/kg of NEORO inhibited H2S production in all of the measurement phases, and a dose of 100 mg/kg EORO inhibited 60% and influenced the effect of the ethanol significantly, reducing the production of H2S. We suggest that NEORO potentiated the effect of EORO, demonstrating effectiveness in doses 600 times lower than those applied with EORO. Among the major compounds of EORO, the camphor molecule exhibited the largest number of interactions with the therapeutic targets related to the inflammatory process, suggesting that it is responsible for EORO's anti-inflammatory and antialgic effects. This work paves the way for future investigations related to the therapeutic role of NEORO in the inflammation process.


Asunto(s)
Antiinflamatorios/farmacología , Emulsiones/farmacología , Inflamación/tratamiento farmacológico , Nanopartículas/administración & dosificación , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Rosmarinus/química , Animales , Carragenina/farmacología , Ciclohexenos/farmacología , Edema/inducido químicamente , Edema/tratamiento farmacológico , Limoneno , Masculino , Simulación del Acoplamiento Molecular/métodos , Ratas , Ratas Wistar , Terpenos/farmacología
13.
Acta Trop ; 178: 163-168, 2018 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-29196196

RESUMEN

Schistosomiasis is promoted for species from Schistosoma genus affecting over 200 million people worldwide. Molluscicides are an efficient method to control this disease, being able to reduce intermediate host snail Biomphalaria glabrata number. In function of resistance cases using niclosamide, natural products are promisors to discover new drugs. Manilkara subsericea is endemic to Brazilian sandbanks of Rio de Janeiro State and wide ranges of biological activities. However, there is no studies evaluating its effects as molluscicidal agent. We tested crude extract from leaves of M. subsericea molluscicidal action, as well it ethyl-acetate fraction and isolated substances against B. glabrata. M. subsericea leaves crude extract and ethyl acetate fraction induced 80±4.13% and 86.66±4.59% mortality of adult snails at concentrations of 250ppm after 96h, and their LD50 values were 118.7±1.62 and 23.41±1.15ppm respectively. Isolated substances from M. subsericea were also considered active. Quercetin, myricetin and ursolic acid, at concentration of 100ppm (96h), were able to induce mortality levels of 100%, 80% and 53.33%, respectively. Our results suggest that M. subsericea can be considered promising as a molluscicide agent.


Asunto(s)
Biomphalaria/efectos de los fármacos , Manilkara/química , Moluscocidas/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta/química , Animales , Brasil , Moluscocidas/química , Extractos Vegetales/química
14.
J Bioenerg Biomembr ; 49(6): 473-483, 2017 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-29147831

RESUMEN

Chagas disease is caused by the Trypanosoma cruzi affecting millions of people, and widespread throughout Latin America. This disease exhibits a problematic chemotherapy. Benznidazole, which is the drug currently used as standard treatment, lamentably evokes several adverse reactions. Among other options, natural products have been tested to discover a novel therapeutic drug for this disease. A lot of plants from the Brazilian flora did not contain studies about their biological effects. Restinga de Jurubatiba from Brazil is a sandbank ecosystem poorly studied in relation to plant biological activity. Thus, three plant species from Restinga de Jurubatiba were tested against in vitro antiprotozoal activity. Among six extracts obtained from leaves and stem parts and 2 essential oils derived from leave parts, only 3 extracts inhibited epimastigote proliferation. Substances present in the extracts with activity were isolated (quercetin, myricetin, and ursolic acid), and evaluated in relation to antiprotozoal activity against epimastigote Y and Dm28 Trypanosoma cruzi strains. All isolated substances were effective to reduce protozoal proliferation. Essentially, quercetin and myricetin did not cause mammalian cell toxicity. In summary, myricetin and quercetin molecule can be used as a scaffold to develop new effective drugs against Chagas's disease.


Asunto(s)
Antiprotozoarios/aislamiento & purificación , Ecosistema , Extractos Vegetales/toxicidad , Trypanosoma cruzi/efectos de los fármacos , Animales , Antiprotozoarios/química , Antiprotozoarios/toxicidad , Brasil , Línea Celular , Enfermedad de Chagas/prevención & control , Flavonoides/toxicidad , Humanos , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Quercetina/toxicidad
15.
Biomed Pharmacother ; 96: 182-190, 2017 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-28987941

RESUMEN

INTRODUCTION: Portulaca pilosa L., belonging to the family Portulacaceae, is a common herbaceous plant in the Americas and in the Amazon, is popularly known as love-grown and is traditionally used as an aid in the treatment of burns, buds, insect bites and wound healing. This study aims to evaluate the non-clinical topical healing activity of the P. pilosa gel (GPP) and the propyleneglycol extract of P. pilosa (EPP) in Wistar rats. METHODS: For the healing activity, wistar rats were divided into the following groups: negative control (GVE - vehicle, 150mg/kg), positive control (Fibrinase®- FIB, 100U/kg), Portulaca pilosa gel 10%, (GPP, 150mg/kg), and propylenglycollic extract of Portulaca pilosa (EPP, 150 mg/kg), which were submitted to a surgical procedure to obtain the wounds, and were treated topically for 7days. After treatment, the treated area was removed and a histopathological analysis was performed. RESULTS: The EPP when analyzed in HPLC was able to identify the presence of gallic acid. EPP significantly modulated the tissue inflammatory response, presenting low number of inflammatory cells in the histopathological study. Treatment with EPP and GPP significantly stimulated angiogenesis and this response was superior to the fibrinase® group. Treatment with EPP and GPP significantly stimulated the proliferation of fibroblasts. The groups treated with EPP and GPP presented an organization pattern of the epidermis and dermis better than the control group, with a mild inflammatory process, with fibroblast proliferation and increased formation of collagen fibers. CONCLUSION: Thus, from the results obtained it can be suggested that the phytochemical marker of the P. pilosa species for healing activity is gallic acid and, together with the macroscopic and microscopic findings triggered by the topical applications of EPP and GPP, it can be concluded that this plant species has topical healing activity, with great potential for use, since this pharmacological action is associated with a possible topical anti-inflammatory activity.


Asunto(s)
Extractos Vegetales/uso terapéutico , Portulaca , Herida Quirúrgica/tratamiento farmacológico , Cicatrización de Heridas/efectos de los fármacos , Animales , Femenino , Geles , Masculino , Componentes Aéreos de las Plantas , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Distribución Aleatoria , Ratas , Ratas Wistar , Herida Quirúrgica/patología , Cicatrización de Heridas/fisiología
16.
Rev. bras. farmacogn ; 26(5): 634-639, Sept.-Oct. 2016. tab, graf
Artículo en Inglés | LILACS | ID: lil-796135

RESUMEN

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.

17.
J Sep Sci ; 39(7): 1273-7, 2016 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-26888377

RESUMEN

Tropane alkaloids are bioactive metabolites with great importance in the pharmaceutical industry and the most important class of natural products found in the Erythroxylum genus. However, these compounds are usually separated by traditional chromatographic techniques, in which the sample is progressively purified in multiple chromatographic steps, resulting in a time- and solvent-consuming procedure. In this work we present the isolation of a novel alkaloid, 6ß,7ß-dibenzoyloxytropan-3α-ol, together with the two known 3α-benzoyloxynortropan-6ß-ol and 3α,6ß-dibenzoyloxytropane alkaloids, directly from the crude alkaloid fraction from the leaves of Erythroxylum subsessile, by using a single run pH-zone-refining counter-current chromatography method. The ethyl acetate/water (1:1, v/v) biphasic solvent system with triethylamine and HCl as retention and eluter agents, respectively, was used to isolate tropane alkaloids for the first time. The structures of the isolated alkaloids were elucidated by spectroscopic methods.


Asunto(s)
Distribución en Contracorriente/métodos , Erythroxylaceae/química , Hojas de la Planta/química , Tropanos/aislamiento & purificación , Concentración de Iones de Hidrógeno , Estructura Molecular , Tropanos/química
18.
Pharmacogn Mag ; 11(Suppl 4): S533-7, 2015 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-27013790

RESUMEN

BACKGROUND: Manilkara subsericea (Sapotaceae) is a species widely spread in the sandbanks of Restinga de Jurubatiba National Park (Rio de Janeiro, Brazil). It is commonly known as "maçaranduba", "maçarandubinha" and "guracica", being used in this locality as food, and timber. However, M. subsericea remains almost unexplored regarding its chemical constituents, including secondary metabolites from the leaves. OBJECTIVE: Identify the chemical constituents from the leaves of M. subsericea. MATERIALS AND METHODS: Leaves were macerated with ethanol (96% v/v), and dried crude ethanolic extract was sequentially washed with the organic solvents in order to obtain an ethyl acetate fraction. Substances from this fraction were identified by different techniques, such as negative-ion electrospray ionization Fourier and (1)H and (13)C nuclear magnetic resonance (NMR). Fresh leaves from M. subsericea were also submitted to hydrodistillation in order to obtain volatile substances, which were identified by gas chromatograph coupled to mass spectrometer. RESULTS: NMR(1)H and (13)C spectra allowed for the identification of the compounds myricetin, quercetin, and kaempferol from the ethyl acetate fraction. The negative-ion electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry mass spectrum also revealed the presence in this fraction of a polyhydroxytriterpene acid (pomolic acid), and some flavonoids, such as quercitrin, and myricitrin. In all 34 volatile compounds were identified by gas chromatography-mass spectrometry, including monoterpenes, sesquiterpenes, and long chain hydrocarbons. CONCLUSION: This study describes the first reports concerning the phytochemical information about leaves from M. subsericea. SUMMARY: Manilkara subsericea fruits proved to be a rich source of triterpenes. However, no phytochemical studies were carried out with leaves. Thus, we described identification of volatile substances from its essential oils, in addition to non-reported triterpene and flavonoids from this species.

19.
J Nanobiotechnology ; 12: 22, 2014 May 18.
Artículo en Inglés | MEDLINE | ID: mdl-24886215

RESUMEN

BACKGROUND: Plants have been recognized as a good source of insecticidal agents, since they are able to produce their own defensives to insect attack. Moreover, there is a growing concern worldwide to develop pesticides with low impact to environment and non-target organisms. Hexane-soluble fraction from ethanolic crude extract from fruits of Manilkara subsericea and its triterpenes were considered active against a cotton pest (Dysdercus peruvianus). Several natural products with insecticidal activity have poor water solubility, including triterpenes, and nanotechnology has emerged as a good alternative to solve this main problem. On this context, the aim of the present study was to develop an insecticidal nanoemulsion containing apolar fraction from fruits of Manilkara subsericea. RESULTS: It was obtained a formulation constituted by 5% of oil (octyldodecyl myristate), 5% of surfactants (sorbitan monooleate/polysorbate 80), 5% of apolar fraction from M. subsericea and 85% of water. Analysis of mean droplet diameter (155.2 ± 3.8 nm) confirmed this formulation as a nanoemulsion. It was able to induce mortality in D. peruvianus. It was observed no effect against acetylcholinesterase or mortality in mice induced by the formulation, suggesting the safety of this nanoemulsion for non-target organisms. CONCLUSIONS: The present study suggests that the obtained O/A nanoemulsion may be useful to enhance water solubility of poor water soluble natural products with insecticidal activity, including the hexane-soluble fraction from ethanolic crude extract from fruits of Manilkara subsericea.


Asunto(s)
Emulsiones/química , Heterópteros/efectos de los fármacos , Insecticidas/química , Manilkara/química , Extractos Vegetales/química , Acetilcolinesterasa/metabolismo , Animales , Emulsiones/toxicidad , Femenino , Heterópteros/fisiología , Insecticidas/toxicidad , Masculino , Ratones , Extractos Vegetales/toxicidad , Solubilidad
20.
Biomed Res Int ; 2014: 408068, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24511532

RESUMEN

Snake venom is composed of a mixture of substances that caused in victims a variety of pathophysiological effects. Besides antivenom, literature has described plants able to inhibit injuries and lethal activities induced by snake venoms. This work describes the inhibitory potential of ethanol, hexane, ethyl acetate, or dichloromethane extracts and fractions from stem and leaves of Manilkara subsericea against in vivo (hemorrhagic and edema) and in vitro (clotting, hemolysis, and proteolysis) activities caused by Lachesis muta venom. All the tested activities were totally or at least partially reduced by M. subsericea. However, when L. muta venom was injected into mice 15 min first or after the materials, hemorrhage and edema were not inhibited. Thus, M. subsericea could be used as antivenom in snakebites of L. muta. And, this work also highlights Brazilian flora as a rich source of molecules with antivenom properties.


Asunto(s)
Antivenenos/administración & dosificación , Extractos Vegetales/administración & dosificación , Venenos de Serpiente/toxicidad , Animales , Antivenenos/química , Brasil , Manilkara/química , Ratones , Extractos Vegetales/química , Viperidae
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