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2.
Pharm Biol ; 62(1): 577-591, 2024 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-39016037

RESUMEN

CONTEXT: The botanical species Bauhinia guianensis Aublet (Leguminosae-Cercidoideae) is traditionally used in the Amazon for medicinal purposes. OBJECTIVE: The acute toxicity of the hydroethanolic extracts from B. guianensis leaves and stems (HELBg and HESBg) was evaluated in zebrafish (Danio rerio), with emphasis on the embryonic developmental stage and adult alterations. MATERIALS AND METHODS: Extracts were analyzed on LC-DAD-MS/MS. Zebrafish eggs were inoculated individually with concentrations of HELBg and HESBg (0.25, 0.5, 0.75, 1.0, and 1.5 µg/mL), observed for 96 h. Adult zebrafish were treated with a single oral dose (100, 200, 500, 1000, and 2000 mg/kg) of HELBg and HESBg, observed for 48 h. RESULTS: HELBg and HESBg analysis detected 55 compounds. Both extracts exhibited toxicity, including embryo coagulation at higher doses of HELBg and absence of heartbeats in embryos at all doses of HESBg. Behavioral variations were observed; tissue alterations in adult zebrafish were found at the highest doses, primarily in the liver, intestine, and kidneys because of HELBg and HESBg effects. The LD50 of HESBg was 1717 mg/kg, while HELBg exceeded the limit dose of 2000 mg/kg. CONCLUSIONS: The study on acute toxicity of B. guianensis extracts exhibits significant toxic potential, emphasizing effects on embryonic and adult zebrafish. The results suggest relative safety of the species preparations, encouraging further clinical trials on potential biological activities.


Asunto(s)
Bauhinia , Embrión no Mamífero , Extractos Vegetales , Hojas de la Planta , Pruebas de Toxicidad Aguda , Pez Cebra , Animales , Extractos Vegetales/toxicidad , Extractos Vegetales/aislamiento & purificación , Bauhinia/química , Embrión no Mamífero/efectos de los fármacos , Dosificación Letal Mediana , Relación Dosis-Respuesta a Droga , Tallos de la Planta , Etanol/toxicidad , Espectrometría de Masas en Tándem , Masculino , Solventes/química , Femenino
3.
Molecules ; 28(17)2023 Sep 02.
Artículo en Inglés | MEDLINE | ID: mdl-37687240

RESUMEN

There are several Amazonian plant species with potential pharmacological validation for the treatment of acute kidney injury, a condition in which the kidneys are unable to adequately filter the blood, resulting in the accumulation of toxins and waste in the body. Scientific production on plant compounds capable of preventing or attenuating acute kidney injury-caused by several factors, including ischemia, toxins, and inflammation-has shown promising results in animal models of acute kidney injury and some preliminary studies in humans. Despite the popular use of Amazonian plant species for kidney disorders, further pharmacological studies are needed to identify active compounds and subsequently conduct more complex preclinical trials. This article is a brief review of phytocompounds with potential nephroprotective effects against acute kidney injury (AKI). The classes of Amazonian plant compounds with significant biological activity most evident in the consulted literature were alkaloids, flavonoids, tannins, steroids, and terpenoids. An expressive phytochemical and pharmacological relevance of the studied species was identified, although with insufficiently explored potential, mainly in the face of AKI, a clinical condition with high morbidity and mortality.


Asunto(s)
Lesión Renal Aguda , Animales , Humanos , Lesión Renal Aguda/tratamiento farmacológico , Riñón , Flavonoides , Inflamación , Modelos Animales
4.
Molecules ; 28(18)2023 Sep 19.
Artículo en Inglés | MEDLINE | ID: mdl-37764465

RESUMEN

Dyslipidemia presents high levels of serum cholesterol and is characterized as a risk factor for cardiovascular diseases, especially for the development of atherosclerosis. E. oleracea oil (OFEO), A. esculentus oil (OFAE), B. orellana oil (OFBO), and Chronic SM® granules (CHR) are rich in bioactive compounds with the potential to treat changes in lipid metabolism. This study investigated the effects of treatments with oils from A. esculentus, E. oleracea, B. orellana, and Chronic SM® on Cocos nucifera L. saturated-fat-induced dyslipidemia. The chromatographic profile showed the majority presence of unsaturated fatty acids in the tested oils. The quantification of tocotrienols and geranylgeraniol in OFBO and CHR was obtained. Treatments with OFEO, OFAE, OFBO, and CHR were able to significantly reduce glycemia, as well as hypertriglyceridemia, total cholesterol, and LDL-cholesterol, besides increasing HDL-cholesterol. The treatments inhibited the formation of atheromatous plaques in the vascular endothelium of the treated rats. The obtained results suggest that the OFEO, OFAE, OFBO, and CHR exhibit antidyslipidemic effects and antiatherogenic activity.


Asunto(s)
Abelmoschus , Aterosclerosis , Dislipidemias , Euterpe , Ratas , Animales , Ratas Wistar , Bixaceae , Aterosclerosis/tratamiento farmacológico , Aterosclerosis/etiología , Dislipidemias/tratamiento farmacológico , Dislipidemias/etiología , HDL-Colesterol , Aceites
5.
Microorganisms ; 11(4)2023 Apr 21.
Artículo en Inglés | MEDLINE | ID: mdl-37110512

RESUMEN

Endophytic fungi are those that present part of their life cycle in healthy tissues of different plant hosts in symbiosis without causing harm. At the same time, fungus-plant symbiosis makes it possible for microorganisms to synthesize their own bioactive secondary metabolites while in the stationary stage. To accomplish this, the endophytic fungus Trichoderma asperellum was isolated from Bertholletia excelsa (Brazil nut) almonds. The fungus was cultivated and extracted with ethyl acetate, obtaining AM07Ac. Then, using HPTLC (High-performance thin-layer chromatography) and nuclear magnetic resonance (1H NMR), ß-amyrin, kaempferol, and brucine were identified as major compounds. Further in vivo assays in zebrafish demonstrated the activity of AM07Ac on melanogenesis by producing a concentration-response inhibitory effect, which, through an in silico study, proved to be related to the noted major compounds known to inhibit tyrosinase activity. The inhibition of tyrosinase prevents melanin accumulation in skin. Therefore, these results imply the importance of investigating microorganisms and their pharmacological activities, in particular the endophytic fungus Trichoderma asperellum as a generator of active metabolites for melanogenesis modulation.

6.
Am J Mens Health ; 17(2): 15579883231167819, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37081737

RESUMEN

Acmella oleracea (L.) R. K. Jansen (Asteraceae) is a plant species widely used in traditional Amazonian medicine to treat sexual dysfunction. The use of this plant has gained popularity because of its sensory properties, such as a tingling sensation. In this study on patients with premature ejaculation, we evaluated the clinical action of a nano-formulation containing an ethanolic extract of A. oleracea inflorescences. Major constituents in the extracts were identified based on gas chromatographic analysis. Participants used a spray preparation based on the A. oleracea extract for 12 weeks, during which they were instructed to apply the product 5 min prior to sexual intercourse. To assess therapeutic efficacy, participants were required to record the mean intravaginal latency time for ejaculation (IELT). During the period of spray treatment, the nano-formulation of A. oleracea increased participant IELT values (M = 293 s) compared with the baseline values (193 s). This nano-formulation reported clinical action in patients with premature ejaculation. It is accordingly considered to have potential application as a therapeutic alternative with benefits for both patients and their partners. Given the small number of participants in this study, further multicenter studies involving a larger number of participants are needed to confirm these observations.


Asunto(s)
Asteraceae , Eyaculación Prematura , Masculino , Humanos , Eyaculación Prematura/tratamiento farmacológico , Proyectos Piloto , Composición de Medicamentos , Extractos Vegetales/uso terapéutico , Asteraceae/química
7.
Inflammopharmacology ; 31(2): 877-886, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-36853419

RESUMEN

Bixa orellana L. is a plant popularly known as "ucurum", "annatto", and "achiote". It is native to South America, and its seeds are an abundant source of geranylgeraniol and tocotrienols. Nanoencapsulation is a valuable technique that can decrease the drug needed to achieve an effect, decreasing potential toxicity, side effects and potentiate the anti-inflammatory effect. This study aimed to evaluate the acute toxicity of an intramuscular application of a nanodispersion containing a standardized extract from the seeds of Bixa orellana (NBO) in Wistar rats. The chemical evaluation showed δ-tocotrienol at 0.725 ± 0.062 mg/mL (72.6 ± 0.9%). The stability study showed the nanoparticles had an average size from 53.15 ± 0.64 to 59.9 ± 3.63 nm, with a polydispersity index ranging from 0.574 ± 0.032 to 0.574 ± 0.32, Zeta potential from 18.26 ± 0.59 to 19.66 ± 1.45 mV. After testing the intramuscular application of NBO with doses from 1 to 5 mg/kg in animals, it was observed that the acute treatment did not elicit any toxic effects within this range. The dose of 10 mg/kg, although not affecting hematological and biochemical parameters (CPK, LDH, myoglobin, AST, ALT, TC, TG, glucose levels, creatinine, and urea), could induce some muscle tissue changes, including leukocyte infiltration, morphological chances, and potentially necrosis. In conclusion, the results showed that the treatments devoided toxicity between 1 and 5 mg/kg.


Asunto(s)
Bixaceae , Tocotrienoles , Ratas , Animales , Ratas Wistar , Tocotrienoles/farmacología , Tocotrienoles/uso terapéutico , Antiinflamatorios/toxicidad , Semillas , Extractos Vegetales/toxicidad , Extractos Vegetales/uso terapéutico
8.
Pharmaceuticals (Basel) ; 15(11)2022 Nov 19.
Artículo en Inglés | MEDLINE | ID: mdl-36422566

RESUMEN

The zebrafish is a popular organism to test the toxicity of compounds. Here, we evaluate the acute and reproductive toxicity of Ormona SI® (OSI) and RC® (ORC), two herbal products developed for menopausal women with tocotrienols, geranylgeraniol, isoflavones, and anthocyanins. The acute toxicity was evaluated by behavioral alterations, lethality, and tissue changes (intestine, liver, kidney) after oral treatment with high product doses (500, 1000, and 2000 mg/kg). The reproductive toxicity was evaluated after 21 days of oral treatment with OSI and ORC at 200 mg/kg. Our results show that the LD50 could not be assessed due to the low mortality rate even with the highest dose; the behavioral alterations were not different from those of the group treated only with the vehicle (2% DMSO). The tissue changes were minor in OSI and more severe in ORC at the highest (2000 mg/kg) dose, while no tissue abnormality was observed at 500 mg/kg. In the reproductive assessment, continuous treatment could decrease the maturation of the reproductive cells, which also significantly decreases the egg spawning. This effect was attributed to the estrogenic activity of the isoflavones. In conclusion, the acute toxicity analysis shows that the products did not elicit lethal or sublethal effects observed in the model when used up to 500 mg/kg. Regarding the reproductive toxicity, decreased fertility was observed, which was expected due to the presence of isoflavones (phytoestrogens). Considering that the product is intended for menopausal and postmenopausal women, the presence of isoflavones is beneficial. Further studies should be performed to corroborate these results in mammals.

9.
Toxicol Res (Camb) ; 11(3): 520-528, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35782641

RESUMEN

Kefiran is a polysaccharide present in kefir grains that have been widely explored due to its potential health benefits. The objective of this work was to characterize and quantify the components present in the ethanolic extract of milk kefir grains; to study its pharmacokinetic and toxicological properties in silico and evaluate the acute toxicity of the kefiran in zebrafish. The prediction of pharmacokinetic properties was performed by QikProp software. In silico toxicity assessment was performed using the DEREK (deductive estimate of risk from existing knowledge) software. In the chromatographic, kefiran was identified as the major component. Results showed that the kefiran had low human oral absorption and intestinal absorption its due poor solubility profile; low logP value, indicating its lipophilicity and the low MDCK and Caco-2 cells permability, and unable to cross the blood-brain barrier. Kefiran did not present any structural warning for in silico toxicity. In zebrafish, the dose of 2,000 mg/kg of kefiran produced nonsignificant alterations in the analyzed organs. It can be said then that kefiran has an acceptable degree of safety for use in the development of drugs or functional foods. Further research such as in vivo testing to confirm its pharmacological potential is currently underway.

10.
Molecules ; 27(5)2022 Feb 28.
Artículo en Inglés | MEDLINE | ID: mdl-35268686

RESUMEN

Some significant compounds present in annatto are geranylgeraniol and tocotrienols. These compounds have beneficial effects against hyperlipidemia and chronic diseases, where oxidative stress and inflammation are present, but the exact mechanism of action of such activities is still a subject of research. This study aimed to evaluate possible mechanisms of action that could be underlying the activities of these molecules. For this, in silico approaches such as ligand topology (PASS and SEA servers) and molecular docking with the software GOLD were used. Additionally, we screened some pharmacokinetic and toxicological parameters using the servers PreADMET, SwissADME, and ProTox-II. The results corroborate the antidyslipidemia and anti-inflammatory activities of geranylgeraniol and tocotrienols. Notably, some new mechanisms of action were predicted to be potentially underlying the activities of these compounds, including inhibition of squalene monooxygenase, lanosterol synthase, and phospholipase A2. These results give new insight into new mechanisms of action involved in these molecules from annatto and Chronic®.


Asunto(s)
Dislipidemias , Tocotrienoles , Bixaceae , Carotenoides , Diterpenos , Simulación del Acoplamiento Molecular , Extractos Vegetales/farmacología , Tocotrienoles/farmacología
11.
Acta Parasitol ; 67(1): 322-329, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-34426891

RESUMEN

PURPOSE: The class Myxozoa consists of microscopic spores that typically present uniform morphological simplifications, containing one or two sporoplasms surrounded by valve cells. The present study analysed the morphological and phylogenetic characteristics of what proved to be a new species of Ceratomyxa found in the gallbladder of Mesonauta festivus Heckel, 1840 captured on the Piririm River in the municipality of Macapá, in Amapá state, Brazil. METHODS: The fish were collected in gillnets, and were transported alive to Amapá State University in Macapá for the analysis of the organs. Crescent- or arch-shaped free spores were observed under light microscopy, containing two polar capsules and a suture line, which is typical of the morphology of the genus Ceratomyxa, contained within plasmodia that had snake-like movements. The gallbladder was conserved in 80% alcohol for the analysis of the 18S rDNA gene, and in Davidson solution for standardhistology. RESULTS: Ceratomyxa spores (n = 20) were observed in 11 of the 50 samplesanalysed, and thus had a prevalence of 22%, and had a mean length of 4.2 ± 0.5 µm, mean thickness of 22.75 ± 0.3 µm, and two polar capsules, 1.86 ± 0.3 µm long and 1.63 ± 0.1 µm thick. CONCLUSIONS: The phylogenetic analysis indicated that the new species forms a cluster with other freshwater Amazonian Ceratomyxa species, described previously. The new species represents the first description of a taxon of the genus Ceratomyxain fish from the Brazilian state of Amapá.


Asunto(s)
Cíclidos , Enfermedades de los Peces , Myxozoa , Enfermedades Parasitarias en Animales , Animales , Brasil , Vesícula Biliar , Humanos , Filogenia , Esporas Protozoarias
12.
Molecules ; 26(24)2021 Dec 17.
Artículo en Inglés | MEDLINE | ID: mdl-34946746

RESUMEN

Plant-derived products may represent promising strategies in the treatment of Neglected Tropical Diseases (NTDs). From this perspective, it is observed that the Amazon phytogeographic region contains the tribe Canarieae of the Burseraceae family, composed of trees and shrubs supplied with resin channels. Its uses in folk medicine are related to aromatic properties, which have numerous medicinal applications and are present in reports from traditional peoples, sometimes as the only therapeutic resource. Despite its economic and pharmacological importance in the region, and although the family is distributed in all tropical and subtropical regions of the world, most of the scientific information available is limited to Asian and African species. Therefore, the present work aimed to review the secondary metabolites with possible pharmacological potential of the species Trattinnickia rhoifolia Willd, popularly known as "Breu sucuruba". To this end, an identification key was created for chemical compounds with greater occurrence in the literature of the genus Trattinnickia. The most evident therapeutic activities in the consulted studies were antimicrobial, antioxidant, anti-inflammatory, antiviral, antifungal, anesthetic and antiparasitic. An expressive chemical and pharmacological relevance of the species was identified, although its potential is insufficiently explored, mainly in the face of the NTDs present in the Brazilian Amazon.


Asunto(s)
Anestésicos , Antiinfecciosos , Antioxidantes , Burseraceae/química , Fitoquímicos , Extractos Vegetales , Anestésicos/química , Anestésicos/uso terapéutico , Antiinfecciosos/química , Antiinfecciosos/uso terapéutico , Antioxidantes/química , Antioxidantes/uso terapéutico , Brasil , Humanos , Fitoquímicos/química , Fitoquímicos/uso terapéutico , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico
13.
Pharmaceuticals (Basel) ; 14(9)2021 Aug 26.
Artículo en Inglés | MEDLINE | ID: mdl-34577555

RESUMEN

Hancornia speciosa Gomes is a tree native to Brazil and has therapeutic potential for several diseases. Ethnopharmacological surveys have reported that the plant is used as a hypoglycemic agent and to lose weight. This study aimed to evaluate the effects of the aqueous extract from H. speciosa latex (LxHs) in a zebrafish model of diabetes. The extract was evaluated through high-performance thin-layer chromatography (HTPLC), nuclear magnetic resonance (NMR), and Fourier-transform infrared spectroscopy (FT-IR). We then tested treatments with LxHs (500, 1000, and 1500 mg/kg) by assessing blood glucose levels in alloxan-induced diabetic animals, and metformin was used as a control. The toxicity was evaluated through histopathology of the pancreas and biochemical assessment of serum levels of AST, ALT, creatinine, and urea. The extract was also assessed for acute toxicity through several parameters in embryos and adult animals. Finally, we performed in silico analysis through the SEA server and docking using the software GOLD. The phytochemical study showed the compounds cornoside, dihydrocornoide, and 1-O-methyl-myoinositol (bornesitol). The treatment with all doses of LxHs significantly decreased alloxan-induced hyperglycemia without any significant histological or biochemical abnormalities. No significant frequency of teratogenesis was observed in the embryos exposed to the extract, and no significant behavioral changes or deaths were observed in adult animals. In silico, the results showed a potential interaction between inositol and enzymes involved in carbohydrates' metabolism. Overall, the results show a hypoglycemic activity of the extract in vivo, with no apparent toxicity. The computational studies suggest this could be at least partially due to the presence of bornesitol, since inositols can interact with carbohydrates' enzymes.

14.
Inflammopharmacology ; 29(5): 1519-1537, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-34498144

RESUMEN

Fatty amides (N-alkylamides) are bioactive lipids that are widely distributed in microorganisms, animals, and plants. The low yield in the extraction process of spilantol, a fatty amide, which is mainly related to its diverse biological effects, compromises its application on a large scale. Thus, this study proposes an alternative method to synthesise fatty amides from Bertholletia excelsa (AGBe) oil, with a chemical structure similar to that of spilantol. Carrageenan-induced abdominal oedema in vivo models were used in zebrafish (Danio rerio). In in vivo studies, oral AGBe produced no signs of toxicity. In the histopathological study, AGBe did not cause significant changes in the main metabolising organs (liver, kidneys, and intestines). All doses of AGBe (100 mg/kg, 500 mg/kg, and 750 mg/kg) were effective in reducing oedema by 65%, 69%, and 95%, respectively, producing a dose-response effect compared to the control group, and spilantol-inhibited oedema by 48%. In the in silico study, with the use of molecular docking, it was observed that among the AGBe, the molecules 18:1, ω-7-ethanolamine, and 18:1, ω-9-ethanolamine stood out, with 21 interactions for COX-2 and 20 interactions for PLA2, respectively, surpassing the spilantol standard with 15 interactions for COX-2 and PLA2. The anti-inflammatory action hypothesis was confirmed in the in silico study, demonstrating the involvement of AGBe in the process of inhibiting the enzymes COX-2 and PLA2. Therefore, based on all the results obtained and the fact that until the dose of 1000 mg/kg was administered orally in zebrafish, it was not possible to determine the LD50; it can be said that AGBe is effective and safe for anti-inflammatory activity.


Asunto(s)
Antiinflamatorios/farmacología , Bertholletia/química , Edema/tratamiento farmacológico , Alcamidas Poliinsaturadas/farmacología , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/aislamiento & purificación , Carragenina , Relación Dosis-Respuesta a Droga , Simulación del Acoplamiento Molecular , Alcamidas Poliinsaturadas/química , Alcamidas Poliinsaturadas/aislamiento & purificación , Relación Estructura-Actividad , Pruebas de Toxicidad Aguda , Pez Cebra
15.
Molecules ; 26(16)2021 Aug 04.
Artículo en Inglés | MEDLINE | ID: mdl-34443306

RESUMEN

This study aimed to evaluate and compare the effects of co-treatment with purified annatto oil (PAO) or its granules (GRA, Chronic®) with that of testosterone on the orchiectomy-induced osteoporosis in Wistar rats. After surgery, rats were treated from day 7 until day 45 with testosterone only (TES, 7 mg/kg, IM) or TES + PAO or GRA (200 mg/kg, p.o.). The following parameters were evaluated: food/water intake, weight, HDL, LDL, glucose, triglycerides (TG), total cholesterol (TC), alkaline phosphatase levels, blood phosphorus and calcium contents, femur weight, structure (through scanning electron microscopy), and calcium content (through atomic absorption spectrophotometry). Our results show that orchiectomy could significantly change the blood lipid profile and decrease bone integrity parameters. Testosterone reposition alone could improve some endpoints, including LDL, TC, bone weight, and bone calcium concentration. However, other parameters were not significantly improved. Co-treatment with PAO or GRA improved the blood lipid profile and bone integrity more significantly and improved some endpoints not affected by testosterone reposition alone (such as TG levels and trabeculae sizes). The results suggest that co-treatment with annatto products improved the blood lipid profile and the anti-osteoporosis effects of testosterone. Overall, GRA had better results than PAO.


Asunto(s)
Bixaceae/química , Carotenoides/química , Fémur/efectos de los fármacos , Lípidos/sangre , Orquiectomía , Osteoporosis/sangre , Osteoporosis/etiología , Extractos Vegetales/química , Aceites de Plantas/farmacología , Testosterona/farmacología , Animales , Peso Corporal/efectos de los fármacos , Conducta de Ingestión de Líquido/efectos de los fármacos , Conducta Alimentaria/efectos de los fármacos , Fémur/ultraestructura , Masculino , Sustancias Protectoras/farmacología , Ratas Wistar
16.
Rev Bras Parasitol Vet ; 30(3): e004621, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34190777

RESUMEN

The present study describes a new species of the genus Sphaerospora found in the urinary bladder of the flag cichlid, Mesonauta festivus collected in Corre Água district of the municipality of Macapá, Amapá State (Brazil). The study includes morphological and phylogenetic analyses of the new parasite, to determine the relationship of the new species with related myxosporean species. The new species has polysporous plasmodia, which vary in size and shape. The mature myxospores are subspherical shape in valvar view. In the sutural view, the myxospores are 5.3±0.2 (5.2-5.6) µm in length and 7.0±0.7 (6.3-7.7) µm in width, with two piriform polar capsules equal size, 2.5±0.2 (2.3-2.8) µm in length and 1.8±0.2 (1.6-2.0) µm in width. The phylogenetic analyses of a partial sequence of the 18S rRNA gene confirmed the status of the new species and determined the relationship of the new species and related myxosporean species.The sum of the evidence indicates that, Sphaerospora festivus n. sp. belongs to the family Sphaerosporidae, and is the first record of the genus Sphaerospora from Brazil.


Asunto(s)
Cíclidos , Enfermedades de los Peces , Myxozoa , Parásitos , Enfermedades Parasitarias en Animales , Animales , Brasil , ADN Ribosómico , Myxozoa/genética , Filogenia
17.
Naunyn Schmiedebergs Arch Pharmacol ; 394(6): 1177-1190, 2021 06.
Artículo en Inglés | MEDLINE | ID: mdl-33515278

RESUMEN

This research aimed to assess the effect of perillyl alcohol (PA) on convulsive behavior in vivo using adult zebrafish (Danio rerio, both sexes). The seizures were induced with pentylenetetrazole (PTZ) intraperitoneally at 170 mg/kg, and diazepam (DZP) was used as the control anticonvulsant (2 mg/kg, oral); PA was tested at 10, 50, and 100 mg/kg orally. The groups had ten animals per group (total n = 60), observed for 10 minutes after seizure induction. We manually appraised typical seizure phenotypes for quantification and used an animal tracking software (Toxtrac) to assess the motor parameters. Next, we sought to find a mechanism of action for PA anticonvulsant activity in silico using a structure-based activity prediction server and molecular docking. The results show that PTZ induced seizure-like behavior in all untreated animals with hyperlocomotion episodes, seizure itself, posture loss, and immobility. DZP inhibited the seizures in all animals of the positive control group. PA, in turn, inhibited the occurrence of seizures in a dose-dependent manner, with frequencies of 90%, 70%, and 40% (for 10, 50, and 100 mg/kg, respectively). The PA treatments also decreased several seizure endpoints in a dose-dependent manner. Also, the difference of the group treated with highest dose of PA was statistically significant compared with the negative control group for all the endpoints assessed (p < 0.05, Kruskal-Wallis). The in silico analyses suggested that PA can affect the GABAergic system, which might be involved in its anticonvulsant activity, but other mechanisms cannot be ruled out. Overall, our results suggest an anticonvulsant potential in perillyl alcohol.


Asunto(s)
Anticonvulsivantes/farmacología , Conducta Animal/efectos de los fármacos , Monoterpenos/farmacología , Convulsiones/tratamiento farmacológico , Animales , Anticonvulsivantes/administración & dosificación , Diazepam/farmacología , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Femenino , Masculino , Simulación del Acoplamiento Molecular , Monoterpenos/administración & dosificación , Gravedad del Paciente , Pentilenotetrazol , Convulsiones/fisiopatología , Pez Cebra
18.
J Biomol Struct Dyn ; 39(3): 1017-1028, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-32028848

RESUMEN

The objectives of this study were to extract and purify Bixin from the seeds of Bixa orellana and to evaluate its hypoglycemic activity in vivo, as well as, to conduct an in silico study of selectivity on peroxisome proliferator-activated receptors via molecular docking and molecular dynamics simulations. Oral administration of Bixin (10 mg/kg) significantly reduced their glucose level that was alloxan-induced diabetic rats. Bixin showed in silico selectivity on peroxisome proliferator-activated receptors (PPARs), particularly by the peroxisome proliferator-activated receptor gamma (PPARγ), which supports the hypoglycemic activity of Bixin. From the results obtained, it can be inferred that Bixin presents hypoglycemic characteristics, which was confirmed by the results obtained from the in vivo and in silico tests. Bixin may act by other pathways to control blood glucose and thus it is possible that it presents a different toxicity profile than troglitazone, rosiglitazone and pioglitazone. However, more studies on the activity and toxicity of Bixin are needed to evaluate for further clinical use. Communicated by Ramaswamy H. Sarma.


Asunto(s)
Diabetes Mellitus Experimental , Tiazolidinedionas , Aloxano , Animales , Carotenoides , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/farmacología , Simulación del Acoplamiento Molecular , PPAR gamma , Ratas
19.
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
20.
Rev. bras. parasitol. vet ; 30(3): e004621, 2021. tab, graf
Artículo en Inglés | LILACS, VETINDEX | ID: biblio-1288709

RESUMEN

Abstract The present study describes a new species of the genus Sphaerospora found in the urinary bladder of the flag cichlid, Mesonauta festivus collected in Corre Água district of the municipality of Macapá, Amapá State (Brazil). The study includes morphological and phylogenetic analyses of the new parasite, to determine the relationship of the new species with related myxosporean species. The new species has polysporous plasmodia, which vary in size and shape. The mature myxospores are subspherical shape in valvar view. In the sutural view, the myxospores are 5.3±0.2 (5.2-5.6) μm in length and 7.0±0.7 (6.3-7.7) μm in width, with two piriform polar capsules equal size, 2.5±0.2 (2.3-2.8) μm in length and 1.8±0.2 (1.6-2.0) μm in width. The phylogenetic analyses of a partial sequence of the 18S rRNA gene confirmed the status of the new species and determined the relationship of the new species and related myxosporean species.The sum of the evidence indicates that, Sphaerospora festivus n. sp. belongs to the family Sphaerosporidae, and is the first record of the genus Sphaerospora from Brazil.


Resumo O presente estudo tem como objetivo descrever uma nova espécie de Sphaerospora encontrado na bexiga urinária de Mesonauta festivus, coletado no distrito Corre Água, no município de Macapá, estado do Amapá (Brasil). Foram realizadas análises morfométricas e filogenéticas, nas quais se avaliou a relação entre as espécies de mixosporídeos já descritas. A nova espécie possui plasmódio poliespórico, que varia em tamanho e forma. Os esporos maduros são subesféricos. Na visão sutural, apresentam 5,3 ± 0,2 (5,2-5,6) μm de comprimento e 7,0 ± 0,7 (6,3-7,7) μm de largura, com duas cápsulas polares piriformes de tamanhos iguais, 2,5 ± 0,2 (2,3-2,8) μm de comprimento e 1,8 ± 0,2 (1,6-2,0) μm de largura. As análises filogenéticas das sequências parciais do gene 18S rDNA confirmam ser uma nova espécie e determinou a relação desta com outros myxozoários já relatados. Conclui-se que a espécie em estudo pertence à família Sphaerosporidae, gênero Sphaerospora, e nova espécie, Sphaerospora festivus n. sp. e primeira ocorrência de parasitos desse gênero no Brasil.


Asunto(s)
Animales , Parásitos , Enfermedades Parasitarias en Animales , Cíclidos , Myxozoa/genética , Enfermedades de los Peces , Filogenia , Brasil , ADN Ribosómico
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