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1.
Chem Biodivers ; : e202400680, 2024 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-38748618

RESUMEN

The study aimed to assess the chemical composition of Miconia ibaguensis leaves extracts and fractions obtained from the ethanolic extract (EE), along with evaluating their antifungal, antibacterial, antidiabetic, and antioxidant activities. The ethyl acetate fraction (EAF) exhibited potent antifungal activity against Candida spp (1.95 - 3.90 µg mL-1) and potent antioxidant activity in the DPPH (1.74 ± 0.07 µg mL-1), FRAP (654.01 ± 42.09 µmol ETrolox/gsample), and ORAC (3698.88 ± 37.28 µmol ETrolox/gsample) methods. The EE displayed inhibition against the α-amylase enzyme (8.42 ± 0.05 µg mL-1). Flavonoids, hydrolysable tannins, triterpenoids, and phenolic acids, identified in the EE and fractions via (-)-HPLC-ESI-MS/MS analysis, were found to contribute to the species' biological activity potentially. These findings suggest promising avenues for further research and potential applications in pharmacology and natural products, offering new possibilities in the fight against global health issues.

2.
Molecules ; 28(13)2023 Jul 06.
Artículo en Inglés | MEDLINE | ID: mdl-37446907

RESUMEN

The present study aims to explore the anti-inflammatory potential activity of the hexane extract from branches (HEB) of Endlicheria paniculata (Lauraceae) and its main compound, methyldehydrodieugenol B, in the inflammatory response induced by a murine implant sponge model. HPLC-ESI/MS analysis of HEB led to the identification of six chemically related neolignans, with methyldehydrodieugenol B as the main compound. An in silico analysis of the pharmacokinetic parameters of the identified compounds suggested moderate solubility but good absorption and biodistribution in vivo. Thus, the treatment of mice with HEB using in vivo assays indicated that HEB promoted pro-inflammatory, antiangiogenic, and antifibrogenic effects, whereas treatment with methyldehydrodieugenol B caused anti-inflammatory, antifibrogenic, and antiangiogenic effects. The obtained results shown the therapeutic potential of HEB and methyldehydrodieugenol B in the treatment of pathologies associated with inflammation and angiogenesis, including chronic wounds.


Asunto(s)
Hexanos , Lauraceae , Ratones , Animales , Distribución Tisular , Extractos Vegetales/farmacología , Inflamación/tratamiento farmacológico , Antiinflamatorios/farmacología , Lauraceae/química , Factores de Transcripción con Motivo Hélice-Asa-Hélice Básico
3.
Chem Biodivers ; 18(10): e2100503, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-34418297

RESUMEN

Infections caused by parasitic worms impose a considerable worldwide health burden. One of the most impactful is schistosomiasis, a disease caused by blood-dwelling of the genus Schistosoma that affects more than 230 million people worldwide. Since praziquantel has also been extensively used to treat schistosomiasis and other parasitic flatworm infections, there is an urgent need to identify novel anthelmintic compounds, mainly from natural sources. In this study, the hexane extract from roots of Piper malacophyllum (Piperaceae) showed to be mainly composed for gibbilimbol B by HPLC/ESI-HRMS. Based on this result, this compound was isolated by chromatographic steps and its structure was confirmed by NMR. In vitro bioassays showed that gibbilimbol B was more active than praziquantel against larval stage of S. mansoni, with effective concentrations of 50 % (EC50 ) and 90 % (EC90 ) values of 2.6 and 3.4 µM, respectively. Importantly, gibbilimbol B showed no cytotoxicity to mammalian cells at a concentration 190 times greater than the antiparasitic effect, giving support for the anthelmintic potential of gibbilimbol B as lead compound for novel antischistosomal agents.


Asunto(s)
Fenoles/farmacología , Piperaceae/química , Extractos Vegetales/farmacología , Schistosoma mansoni/efectos de los fármacos , Animales , Estructura Molecular , Fenoles/química , Fenoles/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Raíces de Plantas/química
4.
J Sci Food Agric ; 101(3): 1202-1208, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-32789937

RESUMEN

BACKGROUND: Eugenia calycina is an endemic species in the Brazilian savannah (the Cerrado) and it is threatened with extinction. Several species of Eugenia are used as insecticides or insect repellents. No data are available on the larvicidal activity of E. calycina. The chemical composition of the essential oil (EO) from leaves of Eugenia calycina was analyzed by gas chromatography coupled to mass spectrometry (GC-MS) and the larvicidal activity against Aedes aegypti larvae in the third stage of development was studied. RESULTS: Oxygenated and non-oxygenated sesquiterpenes were identified, and the main compounds were bicyclogermacrene, spathulenol, and ß-caryophyllene. The EO was fractionated in a chromatographic column and three compounds were isolated and identified: spathulenol, aromadendrane-4ß,10α-diol, and 1ß-11-dihydroxy-5-eudesmene. It is the first time that the last two compounds have been identified in E. calycina. The exposure times in the larvicidal test were 24 h and 48 h and the LC50 values obtained were 199.3 and 166.4 µg mL-1 . The cytotoxicity of the EO in mammalian cells (HeLa and Vero) was evaluated for 24 and 48 h of incubation. The cytotoxic concentrations of the EO for HeLa and Vero cells (266.8 ± 46.5 and 312.1 ± 42.5 µg mL-1 , respectively) in 48 h of exposure were higher than the LC50 , showing low cytotoxicity at the concentration exhibiting larvicidal activity, resulting in a positive selectivity index. CONCLUSION: These results indicate that the EO of E. calycina showed high activity against the A. aegypti larvae but lower cytotoxicity to mammalian cells. The leaves of E. calycina are therefore a very promising source of natural larvicidal products. © 2020 Society of Chemical Industry.


Asunto(s)
Aedes/efectos de los fármacos , Eugenia/química , Insecticidas/farmacología , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Aedes/crecimiento & desarrollo , Animales , Brasil , Chlorocebus aethiops , Cromatografía de Gases y Espectrometría de Masas , Insecticidas/química , Larva/efectos de los fármacos , Larva/crecimiento & desarrollo , Aceites Volátiles/química , Extractos Vegetales/química , Hojas de la Planta/química , Células Vero
5.
Bioorg Chem ; 105: 104335, 2020 12.
Artículo en Inglés | MEDLINE | ID: mdl-33074116

RESUMEN

Banisteriopsis argyrophylla belongs to the Malpighiaceae family, which is a species from Cerrado, also known as "cipó-prata" or "cipó-folha-de-prata." Several species of this family present biological potential. This work reports the chemical identification of the ethanol extract (EE) and its fractions from B. argyrophylla leaves and shows the analysis of the antioxidant activity and inhibitory effects on activities of α-amylase, α-glucosidase and lipase, and non-enzymatic glycation. The ethyl acetate fraction (EAF) and n-butanol fraction (BF) showed antioxidant activity, with IC50 values of 4.1 ± 0.1 and 4.8 ± 0.1 µg mL-1, respectively, by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method, and IC50 values of 6046.3 ± 174.2 and 6264.2 ± 32.2 µmol Trolox eq g-1 by the oxygen radical absorbance capacity (ORAC) method. Furthermore, the DPPH method with these fractions presented electroactive species with antioxidant potential, as shown by the differential pulse voltammetry (DPV) method. The inhibitory effects of the EAF and BF were demonstrated by the following results: IC50 of 5.1 ± 0.3 and 2.5 ± 0.2 µg mL-1 for α-amylase, IC50 of 1093.5 ± 26.0 and 1250.8 ± 21.9 µg mL-1 for α-glucosidase, IC50 of 8.3 ± 4.1 and 4.4 ± 1.0 µg mL-1 for lipase, and IC50 of 1.3 ± 0.1 and 0.9 ± 0.1 µg mL-1 for glycation. Some bioactive compounds were identified by (-)-ESI-MS/MS, such as catechin, procyanidins, glycosylated flavonoids, kaempferol, and megastigmane glucosides. The antidiabetic activity of B.argyrophylla has been reported for the first time.


Asunto(s)
Antioxidantes/química , Banisteriopsis/química , Inhibidores Enzimáticos/química , Extractos Vegetales/química , Hojas de la Planta/química , alfa-Amilasas/antagonistas & inhibidores , alfa-Glucosidasas/metabolismo , Antioxidantes/farmacología , Catequina/química , Catequina/farmacología , Ciclohexanonas/química , Ciclohexanonas/farmacología , Evaluación Preclínica de Medicamentos , Inhibidores Enzimáticos/farmacología , Flavonoides/química , Flavonoides/farmacología , Glucósidos/química , Glucósidos/farmacología , Glicosilación , Humanos , Hipoglucemiantes/química , Quempferoles/química , Quempferoles/farmacología , Lipasa/metabolismo , Norisoprenoides/química , Norisoprenoides/farmacología , Extractos Vegetales/farmacología , Proantocianidinas/química , Proantocianidinas/farmacología
6.
An Acad Bras Cienc ; 92(suppl 2): e20201216, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33084762

RESUMEN

Staphylococcus aureus (S. aureus) is a highly versatile Gram-positive bacterium that is carried asymptomatically by up to 30% of healthy people, while being a major cause of healthcare-associated infections, making it a worldwide problem in clinical medicine. The adaptive evolution of S. aureus strains is demonstrated by its remarkable capacity to promptly develop high resistance to multiple antibiotics, thus limiting treatment choice. Nowadays, there is a continuous demand for an alternative to the use of antibiotics for S. aureus infections and a strategy to control the spread or to kill phylogenetically related strains. In this scenario, bacteriocins fit as with a promising and interesting alternative. These molecules are produced by a range of bacteria, defined as ribosomally synthesized peptides with bacteriostatic or bactericidal activity against a wide range of pathogens. This work reviews ascertained the main antibiotic-resistance mechanisms of S. aureus strains and the current, informative content concerning the applicability of the use of bacteriocins overlapping the use of conventional antibiotics in the context of S. aureus infections. Besides, we highlight the possible application of these biomolecules on an industrial scale in future work.


Asunto(s)
Bacteriocinas , Infecciones Estafilocócicas , Antibacterianos/farmacología , Antibacterianos/uso terapéutico , Bacterias Grampositivas , Humanos , Pruebas de Sensibilidad Microbiana , Infecciones Estafilocócicas/tratamiento farmacológico , Staphylococcus aureus
7.
ScientificWorldJournal ; 2019: 9423658, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30853865

RESUMEN

The species Inga laurina is native to the Brazilian Cerrado. There are no studies about the chemical composition and biological activities of extracts of this endangered species. The ethanolic extract and its successive fractions are rich in phenolic compounds and presented good antifungal activities. HPLC/MS-MS/MS and H1/C13 analysis led to the identification of seventeen compounds, most of which are gallic acid derivatives, myricetin and quercetin glycosides. The ethyl acetate fraction (EAF) contained high levels of total phenolics, expressed in milligrams of gallic acid equivalents per gram of extract (475.3 ± 1.9 mg GAE gextract -1) and flavonoids expressed in milligrams of quercetin equivalents per gram of extract (359.3 ± 10.6 mg QE gextract -1). This fraction was active against fungi of the Candida genus. The EAF showed MIC value 11.7 µg mL-1 against C. glabrata and a selectivity index of 1.6 against Vero cells. The flavonol glycoside myricetin-3-O-rhamnoside was isolated for the first time from the Inga laurina. These results make I. laurina a promising plant as a source of pharmaceutical and biological active antifungal compounds.


Asunto(s)
Antifúngicos/farmacología , Citotoxinas/farmacología , Fabaceae/química , Extractos Vegetales/farmacología , Antifúngicos/química , Antifúngicos/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Citotoxinas/química , Citotoxinas/aislamiento & purificación , Flavonoides/química , Flavonoides/aislamiento & purificación , Fenoles/química , Fenoles/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta/química , Proantocianidinas/química , Proantocianidinas/aislamiento & purificación , Espectrometría de Masas en Tándem
8.
An Acad Bras Cienc ; 90(2 suppl 1): 2179-2188, 2018 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-29451601

RESUMEN

The genus Corynebacterium includes species of great importance in medical, veterinary and biotechnological fields. The genus-specific families (PLfams) from PATRIC have been used to observe conserved proteins associated to all species. Our results showed a large number of conserved proteins that are associated with the cellular division process. Was not observe in our results other proteins like FtsA and ZapA that interact with FtsZ. Our findings point that SepF overlaps the function of this proteins explored by molecular docking, protein-protein interaction and sequence analysis. Transcriptomic analysis showed that these two (Sepf and FtsZ) proteins can be expressed in different conditions together. The work presents novelties on molecules participating in the cell division event, from the interaction of FtsZ and SepF, as new therapeutic targets.


Asunto(s)
Proteínas Bacterianas/fisiología , División Celular/fisiología , Corynebacterium/citología , Citocinesis/fisiología , Proteínas del Citoesqueleto/fisiología , Proteínas Bacterianas/genética , Corynebacterium/fisiología , Proteínas del Citoesqueleto/genética , Perfilación de la Expresión Génica , Simulación del Acoplamiento Molecular , Mapeo de Interacción de Proteínas
9.
BMC Microbiol ; 16: 100, 2016 Jun 02.
Artículo en Inglés | MEDLINE | ID: mdl-27251711

RESUMEN

BACKGROUND: Corynebacterium pseudotuberculosis can be classified into two biovars or biovars based on their nitrate-reducing ability. Strains isolated from sheep and goats show negative nitrate reduction and are termed biovar Ovis, while strains from horse and cattle exhibit positive nitrate reduction and are called biovar Equi. However, molecular evidence has not been established so far to understand this difference, specifically if these C. pseudotuberculosis strains are under an evolutionary process. RESULTS: The ERIC 1 + 2 Minimum-spanning tree from 367 strains of C. pseudotuberculosis showed that the great majority of biovar Ovis strains clustered together, but separately from biovar Equi strains that also clustered amongst themselves. Using evolutionarily conserved genes (rpoB, gapA, fusA, and rsmE) and their corresponding amino acid sequences, we analyzed the phylogenetic relationship among eighteen strains of C. pseudotuberculosis belonging to both biovars Ovis and Equi. Additionally, conserved point mutation based on structural variation analysis was also carried out to elucidate the genotype-phenotype correlations and speciation. We observed that the biovars are different at the molecular phylogenetic level and a probable anagenesis is occurring slowly within the species C. pseudotuberculosis. CONCLUSIONS: Taken together the results suggest that biovar Equi is forming the biovar Ovis. However, additional analyses using other genes and other bacterial strains are required to further support our anagenesis hypothesis in C. pseudotuberculosis.


Asunto(s)
Proteínas Bacterianas/genética , Corynebacterium pseudotuberculosis/clasificación , Corynebacterium pseudotuberculosis/genética , Análisis de Secuencia de ADN/métodos , Animales , Bovinos , Secuencia Conservada , ADN Bacteriano/genética , Evolución Molecular , Cabras , Caballos , Nitratos/metabolismo , Filogenia , Mutación Puntual , Ovinos
10.
Bioorg Chem ; 69: 167-182, 2016 12.
Artículo en Inglés | MEDLINE | ID: mdl-27842248

RESUMEN

Annona crassiflora Mart., whose fruit is popularly known as araticum, is a member of the Annonaceae family found in the Brazilian Cerrado. Although this plant has several medicinal uses, its bioactive molecules are not fully understood. A bioguided assay was performed to identify the main bioactive compounds of A. crassiflora fruit peel from the ethanol extract fractions with antioxidant capacity and α-amylase, α-glucosidase and glycation inhibitory activities. Ethyl acetate and n-butanol fractions showed, respectively, higher antioxidant capacity (DPPH IC50 1.5±0.1 and 0.8±0.1µgmL-1, ORAC 3355±164 and 2714±79µmoltroloxeq/g, and FRAP 888±16 and 921±9µmoltroloxeq/g) and inhibitory activities against α-amylase (IC50 4.5±0.8 and 1.7±0.3µgmL-1), α-glucosidase (IC50 554.5±158.6 and 787.8±140.6µgmL-1) and glycation (IC50 14.3±3.3 and 16.0±4.2µgmL-1), and lower cytotoxicity, compared to the other fractions and crude ethanol extract. The HPLC-ESI-MS/MS analysis identified various biomolecules known as potent antioxidants, such as chlorogenic acid, (epi)catechin, procyanidins, caffeoyl-hexosides, quercetin-glucosides and kaempferol. The fruit peel of A. crassiflora, a specie from Cerrado, the Brazilian Savanna, provided a source of antioxidant compounds with properties to block carbohydrate digestive enzymes and formation of glycation products. Thus, there is potential to use the by-products of araticum in order to identify and isolate phytochemicals for application in nutraceutical supplements, food additives and pharmaceuticals products.


Asunto(s)
Annona/química , Antioxidantes/farmacología , Inhibidores Enzimáticos/farmacología , Fibroblastos/efectos de los fármacos , Frutas/química , alfa-Amilasas/antagonistas & inhibidores , alfa-Glucosidasas/metabolismo , Animales , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Fibroblastos/metabolismo , Ratones , Células 3T3 NIH , Relación Estructura-Actividad , alfa-Amilasas/metabolismo
11.
Vet Ophthalmol ; 18 Suppl 1: 125-31, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-25273613

RESUMEN

PURPOSE: The purpose of this study was to establish reference values for diagnostic ophthalmic tests in sambar deer (Rusa unicolor) as well as to describe the most relevant features of the bony orbital anatomy and ocular histology. METHOD: Twenty healthy animals, free living in a forest reserve, that were captured for clinical evaluation as part of a health survey were evaluated. Schirmer tear test-1 (STT1), conjunctival microbiota, intraocular pressure (IOP), conjunctival cytology, anatomy of the bony orbit, and ocular histology were studied. RESULTS: Mean ± SD STT1 and IOP values were 18.8 ± 4.7 mm and 11.4 ± 2.8 mmHg, respectively. IOP was significantly higher in adult (4-8 years) animals (P = 0.04). Bacterial growth was present in 100% of the samples, with a prevalence for Staphylococcus sp. and Bacillus sp. The conjunctival cytology revealed predominance of columnar epithelial cells with mild pigmentation. The sambar deer orbit is completely encompassed by bone. The ocular histology was very similar to most mammalians. CONCLUSIONS: The findings in this study will be useful in the diagnosis of ocular diseases in Rusa unicolor.


Asunto(s)
Ciervos/anatomía & histología , Técnicas de Diagnóstico Oftalmológico/veterinaria , Órbita/anatomía & histología , Animales , Conjuntiva/citología , Femenino , Presión Intraocular , Masculino
12.
Vet Ophthalmol ; 18 Suppl 1: 30-9, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-24171896

RESUMEN

PURPOSE: The aim of this study was to establish normal ophthalmic parameters for selected diagnostic tests, and to describe the orbital anatomy and adnexal histology of the broad-snouted caiman. METHOD: A total of 35 Caiman latirostris that were free of obvious ocular diseases were used to measure the parameters in this investigation. Ages ranged from 5 to 15 years. Ophthalmic diagnostic tests were conducted, including evaluation of tear production with Schirmer Tear test-1 (STT1), culture of the conjunctival bacterial flora, applanation tonometry, conjunctival cytology, nictiating membrane incursion frequency test (NMIFT), endodontic absorbent paper point tear test (EAPPTT), palpebral fissure length measurement (PFL) and B-mode ultrasonography. Adnexal histology and skull samples were studied. RESULTS: Mean (±SD) STT1 was 3.4 ± 3.6 mm/min (95% confidence interval of 2.01-4.78 mm/min), intraocular pressure (IOP) was 12.9 ± 6.2 mmHg, NMIFT was 6.0 ± 3.5, EAPPTT was 17.1 ± 2.5 mm/min, PFL was 28.9 ± 3.0 mm, anterior chamber depth was 3.1 ± 0.3 mm, lens axial length was 8.4 ± 0.6 mm, vitreous chamber depth was 7.9 ± 0.7 mm and axial globe length was 19.9 ± 1.3 mm. For all animals evaluated, Bacillus sp., Diphteroids and Staphylococcus sp. were predominant.


Asunto(s)
Caimanes y Cocodrilos/anatomía & histología , Técnicas de Diagnóstico Oftalmológico/veterinaria , Ojo/anatomía & histología , Glándula de Harder/anatomía & histología , Membrana Nictitante/anatomía & histología , Animales , Femenino , Masculino
13.
Vet Ophthalmol ; 18 Suppl 1: 46-52, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-24783966

RESUMEN

PURPOSE: The aim of this study was to establish normal ophthalmic parameters for select diagnostic tests in red-footed tortoises (Chelonoides carbonaria). A total of 52 animals, approximately 20-30 years old, were studied. METHOD: Ophthalmic diagnostic tests included culturing of the normal conjunctival bacterial flora in summer and winter, evaluation of tear production using Schirmer tear test (STT) and endodontic absorbent paper point tear test in two different environmental temperatures (EAPPTT-1 at 32 °C and EAPPTT-2 at 18 °C), cytology of conjunctival cells, B-mode ultrasonography, measurement of palpebral fissure length (PFL), and applanation tonometry (in two different positions). RESULTS: In both seasons, Gram-positive bacteria were predominant. Median (± IQR/2) STT was 12.0 ± 3.5 mm/min, EAPPTT-1 was 15.9 ± 0.7 mm/15 s, and EAPPTT-2 was 15.4 ± 0.4 mm/min (OD) and 17.8 ± 1.0 mm/min (OS). Anterior chamber depth was 1.0 ± 0.1 mm, lens axial length was 2.3 ± 0.1 mm, vitreous chamber depth was 4.3 ± 0.2 mm, and axial globe length was 7.7 ± 0.3 mm. PFL was 11.7 ± 1.7 mm. Intraocular pressure was 11.5 ± 2.8 mmHg for males and 14.0 ± 3.5 mmHg for females (dorsoventral position) and 18.0 ± 3.2 mmHg for males and 24.1 ± 3.0 mmHg for females (ventrodorsal position with inclination of 45°). The ophthalmic parameters reported here can aid in the diagnosis of eye diseases in red-footed tortoises (Chelonoides carbonaria).


Asunto(s)
Técnicas de Diagnóstico Oftalmológico/veterinaria , Ojo/anatomía & histología , Tortugas/anatomía & histología , Animales , Femenino , Masculino
14.
Molecules ; 19(5): 5761-76, 2014 May 05.
Artículo en Inglés | MEDLINE | ID: mdl-24802987

RESUMEN

Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro antiparasitic activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-activity relationships were performed using Decision Trees.


Asunto(s)
Relación Estructura-Actividad , Triterpenos/administración & dosificación , Triterpenos/síntesis química , Anacardiaceae/química , Anacardiaceae/efectos de los fármacos , Animales , Antiparasitarios/administración & dosificación , Antiprotozoarios/administración & dosificación , Enfermedad de Chagas/tratamiento farmacológico , Enfermedad de Chagas/genética , Enfermedad de Chagas/patología , Humanos , Leishmania/efectos de los fármacos , Extractos Vegetales/química , Hojas de la Planta/química , Triterpenos/química , Trypanosoma cruzi/efectos de los fármacos
15.
Molecules ; 19(4): 4560-77, 2014 Apr 11.
Artículo en Inglés | MEDLINE | ID: mdl-24731985

RESUMEN

The seasonal chemical composition of essential oils from Inga laurina was determined by GC/MS. In the stem bark's essential oil extracted during the dry season, the presence of terpenoids (30.05%) stood out, and phytol (9.76%) was the major compound identified. For the stem bark oil obtained during the rainy season, in addition to terpenoids (26.63%), a large amount of fatty acids (46.84%) were identified, in particular palmitic acid (25.40%). Regarding the leaves' essential oil obtained in the dry season, esters (42.35%) were the main components. The main ester present was (Z)-hex-3-enyl benzoate (10.15%) and the major compound of this oil was (Z)-hex-3-en-1-ol (14.23%). Terpenoids (33.84%), long-chain alkanes (27.04%) and fatty acids (21.72%) were the main components of the essential oil from leaves in the rainy season. Phytol (33.21%), nonacosane (21.95%) and palmitic acid (15.20%) were the major compounds identified. The antimicrobial activity against aerobic and anaerobic oral bacteria was evaluated by the microdilution broth method and cytotoxic activity was carried out with Vero cells. The essential oils from the rainy season showed a better inhibition of the bacterial growth with Minimal Inhibitory Concentrations (MIC) values of 25 or 50 µg·mL⁻¹ for aerobic bacteria, and high selectivity against bacteria was observed. The large amount of fatty acids in rainy season oils may be related to the better inhibitory effects observed.


Asunto(s)
Antiinfecciosos/química , Citotoxinas/química , Fabaceae/química , Aceites Volátiles/química , Aceites de Plantas/química , Animales , Antiinfecciosos/farmacología , Bacterias Aerobias/efectos de los fármacos , Bacterias Aerobias/crecimiento & desarrollo , Bacterias Anaerobias/efectos de los fármacos , Bacterias Anaerobias/crecimiento & desarrollo , Supervivencia Celular/efectos de los fármacos , Chlorocebus aethiops , Citotoxinas/farmacología , Ésteres , Ácidos Grasos/clasificación , Ácidos Grasos/aislamiento & purificación , Aceites Volátiles/farmacología , Especificidad de Órganos , Corteza de la Planta/química , Hojas de la Planta/química , Aceites de Plantas/farmacología , Estaciones del Año , Terpenos/clasificación , Terpenos/aislamiento & purificación , Células Vero
16.
Sleep Med ; 119: 535-548, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38810479

RESUMEN

OBJECTIVE: Sleep stages can provide valuable insights into an individual's sleep quality. By leveraging movement and heart rate data collected by modern smartwatches, it is possible to enable the sleep staging feature and enhance users' understanding about their sleep and health conditions. METHOD: In this paper, we present and validate a recurrent neural network based model with 23 input features extracted from accelerometer and photoplethysmography sensors data for both healthy and sleep apnea populations. We designed a lightweight and fast solution to enable the prediction of sleep stages for each 30-s epoch. This solution was developed using a large dataset of 1522 night recordings collected from a highly heterogeneous population and different versions of Samsung smartwatch. RESULTS: In the classification of four sleep stages (wake, light, deep, and rapid eye movements sleep), the proposed solution achieved 71.6 % of balanced accuracy and a Cohen's kappa of 0.56 in a test set with 586 recordings. CONCLUSION: The results presented in this paper validate our proposal as a competitive wearable solution for sleep staging. Additionally, the use of a large and diverse data set contributes to the robustness of our solution, and corroborates the validation of algorithm's performance. Some additional analysis performed for healthy and sleep apnea population demonstrated that algorithm's performance has low correlation with demographic variables.


Asunto(s)
Algoritmos , Síndromes de la Apnea del Sueño , Fases del Sueño , Humanos , Síndromes de la Apnea del Sueño/diagnóstico , Masculino , Femenino , Fases del Sueño/fisiología , Persona de Mediana Edad , Adulto , Dispositivos Electrónicos Vestibles , Redes Neurales de la Computación , Fotopletismografía/instrumentación , Fotopletismografía/métodos , Polisomnografía/instrumentación , Frecuencia Cardíaca/fisiología , Acelerometría/instrumentación , Acelerometría/métodos , Anciano
17.
J Ethnopharmacol ; 319(Pt 3): 117315, 2024 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-37852339

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Maytenus ilicifolia Mart. ex Reissek, a medicinal plant used for treating gastritis, ulcers, and gastric disorders, possesses therapeutic properties attributed to diverse leaf compounds-terpenoids, alkaloids, flavonoids, phenols, and tannins, reflecting the ethnopharmacological knowledge of traditional users. AIMS OF THE STUDY: We aimed to assess the antioxidant and antiglycant capacities of Maytenus ilicifolia's ethanolic extract and organic fractions, identify bioactive compounds through HPLC-MS/MS analysis, and conduct phytochemical assessments. We also assessed their potential to inhibit digestive and cholinesterase enzymes, mitigate oxidation of human LDL and rat hepatic tissue, and examine their antimicrobial and cytotoxic properties. MATERIALS AND METHODS: Organic fractions (hexane - HF-Mi, dichloromethane - DMF-Mi, ethyl acetate - EAF-Mi, n-butanol - BF-Mi, and hydromethanolic - HMF-Mi) were obtained via liquid-liquid partitioning. Antioxidant (DPPH, FRAP, ORAC) and antiglycant (BSA/FRU, BSA/MGO, ARG/MGO/LDL/MGO models) capacities were tested. Phytochemical analysis employed HPLC-MS/MS. We also studied the inhibitory effects on α-amylase, acetylcholinesterase, butyrylcholinesterase, human LDL and rat hepatic tissue oxidation, antimicrobial activity, and cytotoxicity against RAW 264.7 macrophages. RESULTS: HPLC-ESI-MS/MS identified antioxidant compounds such as catechin, quercetin, and kaempferol derivatives. Ethanolic extract (EE-Mi) and organic fractions demonstrated robust antioxidant and antiglycant activity. EAF-Mi and BF-Mi inhibited α-amylase (2.42 µg/mL and 7.95 µg/mL) compared to acarbose (0.144 µg/mL). Most organic fractions exhibited ∼50% inhibition of acetylcholinesterase and butyrylcholinesterase, rivaling galantamine and rivastigmine. EAF-Mi, BF-Mi, and EE-Mi excelled in inhibiting lipid peroxidation. All fractions, except HMF-Mi, effectively countered LDL oxidation, evidenced by the area under the curve. These fractions protected LDL against lipid peroxidation. CONCLUSION: This study unveils Maytenus ilicifolia's ethanolic extract and organic fractions properties. Through rigorous analysis, we identify bioactive compounds and highlight their antioxidant, antiglycant, enzyme inhibition, and protective properties against oxidative damage. These findings underline its significance in modern pharmacology and its potential applications in healthcare.


Asunto(s)
Antiinfecciosos , Celastraceae , Maytenus , Humanos , Animales , Ratas , Peroxidación de Lípido , Acetilcolinesterasa , Butirilcolinesterasa , Antioxidantes/farmacología , Reacción de Maillard , Óxido de Magnesio , Espectrometría de Masas en Tándem , Fitoquímicos , alfa-Amilasas , Extractos Vegetales/farmacología
18.
J Pharm Biomed Anal ; 245: 116143, 2024 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-38678859

RESUMEN

Centella asiatica (L.) Urb. is a small herbaceous plant belonging to the Apiaceae family that is rich in triterpenes, such as asiaticoside and madecassoside. Centella asiatica finds broad application in promoting wound healing, addressing skin disorders, and boosting both memory and cognitive function. Given its extensive therapeutic potential, this study aimed not only to investigate the Centella asiatica ethanolic extract but also to analyze the biological properties of its organic fractions, such as antioxidant antiglycation capacity, which are little explored. We also identified the main bioactive compounds through spectrometry analysis. The ethanolic extract (EE) was obtained through a static maceration for seven days, while organic fractions (HF: hexane fraction; DF: dichloromethane fraction; EAF: ethyl acetate fraction; BF: n-butanol fraction and HMF: hydromethanolic fraction) were obtained via liquid-liquid fractionation. The concentration of phenolic compounds, flavonoids, and tannins in each sample was quantified. Additionally, the antiglycation (BSA/FRU, BSA/MGO, and ARG/MGO models) and antioxidant (FRAP, ORAC, and DPPH) properties, as well as the ability to inhibit LDL oxidation and hepatic tissue peroxidation were evaluated. The inhibition of enzyme activity was also analyzed (α-amylase, α-glycosidase, acetylcholinesterase, and butyrylcholinesterase). We also evaluated the antimicrobial and cytotoxicity against RAW 264.7 macrophages. The main compounds present in the most bioactive fractions were elucidated through ESI FT-ICR MS and HPLC-ESI-MS/MS analysis. In the assessment of antioxidant capacity (FRAP, ORAC, and DPPH), the EAF and BF fractions exhibited notable results, and as they are the phenolic compounds richest fractions, they also inhibited LDL oxidation, protected the hepatic tissue from peroxidation and inhibited α-amylase activity. Regarding glycation models, the EE, EAF, BF, and HMF fractions demonstrated substantial activity in the BSA/FRU model. However, BF was the only fraction that presented non-cytotoxic activity in RAW 264.7 macrophages at all tested concentrations. In conclusion, this study provides valuable insights into the antioxidant, antiglycation, and enzymatic inhibition capacities of the ethanolic extract and organic fractions of Centella asiatica. The findings suggest that further in vivo studies, particularly focusing on the butanol fraction (BF), may be promising routes for future research and potential therapeutic applications.


Asunto(s)
Antioxidantes , Centella , Lipoproteínas LDL , Oxidación-Reducción , Extractos Vegetales , Albúmina Sérica Bovina , Triterpenos , alfa-Amilasas , Animales , Extractos Vegetales/farmacología , Extractos Vegetales/química , alfa-Amilasas/antagonistas & inhibidores , alfa-Amilasas/metabolismo , Centella/química , Antioxidantes/farmacología , Antioxidantes/química , Ratones , Oxidación-Reducción/efectos de los fármacos , Glicosilación/efectos de los fármacos , Albúmina Sérica Bovina/metabolismo , Lipoproteínas LDL/metabolismo , Triterpenos/farmacología , Triterpenos/química , Células RAW 264.7
19.
J Med Primatol ; 42(2): 101-4, 2013 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-23311626

RESUMEN

BACKGROUND: The accumulation of pus in the orbit originating from an infected dental root is classified as odontogenic intraorbital abscess. METHODS: Clinical, laboratory, and image evaluation of a non-human primate was performed. RESULTS: The patient was cured after surgical therapy. CONCLUSIONS: This represents the first report of an odontogenic periodontal abscess in Cebus apella.


Asunto(s)
Cebus , Exoftalmia/veterinaria , Enfermedades de los Monos/diagnóstico , Enfermedades de los Monos/patología , Enfermedades de los Monos/cirugía , Órbita/patología , Absceso Periodontal/veterinaria , Animales , Exoftalmia/etiología , Exoftalmia/cirugía , Masculino , Absceso Periodontal/complicaciones , Absceso Periodontal/cirugía
20.
Molecules ; 18(4): 4588-98, 2013 Apr 18.
Artículo en Inglés | MEDLINE | ID: mdl-23599016

RESUMEN

The chemical composition of the essential oils from leaves, bark and wood of Cassia bakeriana Craib. was determined by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). Alcohols, aldehydes and fatty acids were the major components in leaf and bark oil, while wood essential oil was rich in fatty acids. Terpenes such as linalool, (E)-nerolidol and phytol were present in low concentrations. The antimicrobial activity against aerobic and anaerobic oral bacteria was evaluated using the microdilution method, as was the cell viability test carried out with Vero cells. The oils from leaves and bark showed high antimicrobial activity, with minimum inhibitory concentrations between 62.5 and 125 µg·mL⁻¹ for most of the tested bacteria, including Streptococcus mutans, the main etiological agent of dental caries. Leaves oil displayed the lowest cytotoxic effect (EC50 of 153 µg·mL⁻¹), while wood oil exhibited the highest toxicity to Vero cells. C. bakeriana oils are thus a source of biologically active compounds against aerobic and anaerobic oral microorganisms. This study is the first report on the chemical composition, antimicrobial activity and cytotoxicity of C. bakeriana.


Asunto(s)
Antiinfecciosos/química , Antiinfecciosos/farmacología , Bacterias Aerobias/efectos de los fármacos , Bacterias Anaerobias/efectos de los fármacos , Cassia/química , Aceites Volátiles/química , Aceites Volátiles/farmacología , Animales , Antiinfecciosos/toxicidad , Proliferación Celular/efectos de los fármacos , Chlorocebus aethiops , Caries Dental/microbiología , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/toxicidad , Streptococcus mutans/efectos de los fármacos , Células Vero
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