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1.
Drug Deliv Transl Res ; 10(6): 1748-1763, 2020 12.
Artigo em Inglês | MEDLINE | ID: mdl-32924099

RESUMO

The Melaleuca alternifolia essential oil (MEO) has been widely used due to its healing and antimicrobial action. Its incorporation into drug delivery systems is a reality, and numerous studies have already been developed for this purpose. In this regard, the aim of this work was to develop, characterize, and evaluate the in vivo pharmacological activity of bicontinuous microemulsions (BME) containing MEO. Through diagram construction, a formulation consisting of Kolliphor® HS 15 (31.05%), Span® 80 (3.45%), isopropyl myristate (34.5%), and distilled water (31%) was selected and MEO was incorporated in the proportion of 3.45% (v/v). Morphological analysis characterization confirms that the system studied herein is a BME. The evaluated formulation showed physicochemical characteristics that allow its topical use. Rheologically, samples were characterized as pseudo-plastic non-Newtonian thixotropic fluids. The chromatographic method developed is in accordance with the current recommendations. The extraction method used assured a 100% recovery of the pharmacological marker (terpinen-4-ol). In vivo studies suggest that BME loaded with MEO may contribute to the healing process of skin wounds. In addition, it demonstrated antibacterial activity for Gram-positive and Gram-negative bacteria. Therefore, the BME system loaded with MEO is promising as a healing and antimicrobial agent for skin wounds.Graphical abstract.


Assuntos
Antibacterianos , Melaleuca , Óleo de Melaleuca , Cicatrização/efeitos dos fármacos , Antibacterianos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Melaleuca/química , Óleo de Melaleuca/farmacologia
2.
Front Neurosci ; 13: 9, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30728763

RESUMO

Avocado (Persea americana Mill.) is an oleaginous fruit source of fatty acids with high levels of neuroprotective phytocomplexes. The objective of this study was to evaluate the development of reflex and somatic maturation, fatty acid profiles in the brain, and memory in different stages of life in the offspring of dams supplemented with avocado pulp and oil during gestation and lactation. The dams were randomly divided into three groups (n = 15 pups/group), and recieved by gavage supplementation: control group (CG)-distilled water; Avocado Oil (AO)-3,000 mg avocado oil/kg animal weight, and Avocado Pulp (AP)-3,000 mg avocado pulp/kg animal weight. We performed the following tests: Analysis of Somatic Development and Ontogeny of Postnatal Reflex (T0 to T21), the Open Field Habituation Test and the Object Recognition Test (ORT) in the adolescent (T45) and adult (T90) phases. The cerebral fatty acids content was evaluated at times T0, T21, T45, and T90. The results were analyzed using the statistical program GraphPad Prism and significant statistics were considered when p < 0.05. Acceleration of reflex maturation and reflex ontogeny was observed in the offspring of AO and AP fed dams, with the results being more pronounced in the pulp fed group (p < 0.05). All groups presented a decrease in the ambulation parameter in the second exposure to the Open Field Habituation Test, at T45 and T90 (p < 0.05). In the ORT, the AO and AP offspring presented memory improvements in the short and long term in the adult and adolescent phases (p < 0.05). The results of the brain fatty acid profiles presented higher polyunsaturated fatty acids (PUFA) content in the AO and AP groups at T21, T45, and T90. The docosahexaenoic fatty acid (DHA) content was higher at T21 (AO and AP), at T45 (AO and AP), and at T90 (AP) (p < 0.05). The arachidonic acid (ARA) content was higher at T45 (AO and AP), and at T90 (AO) (p < 0.05). Maternal supplementation with avocado oil and pulp anticipates reflex maturation and somatic postnatal development, and improves memory during the adolescent and adult phases.

3.
Comb Chem High Throughput Screen ; 20(3): 247-254, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28000563

RESUMO

Identifying novel bio markers in gastro intestinal disease is a promising method where a comprehensive analysis of the metabolome is performed. Metabolomics has evolved enormously in the past decade, paving a path in gastro intestinal disease research, especially diseases which lead to high morbidity and mortality. Metabolomics involves identifying metabolites such as anti-oxidants, and amino acids etc., which are screened in the urine, feces and tissue samples. Certain cases employ advanced tools like GC-MS, 1HNMR and GC-MS/SPME which reveal valuable information concerning disease severity and differentiation. In light of escalating health care costs and risky invasive procedures, metabolomics can be chosen as a safe yet precise method for screening diseases like ulcerative colitis, Crohns' disease, celiac disease, and gastro intestinal cancers. The present review focuses on major advancements in gastro intestinal metabolomics, giving attention to which parameters are assessed, and to recent changes in metabolite analysis.


Assuntos
Gastroenteropatias/diagnóstico , Biomarcadores , Gastroenteropatias/metabolismo , Ensaios de Triagem em Larga Escala/métodos , Humanos , Metaboloma , Metabolômica/métodos
4.
J Pharm Biomed Anal ; 100: 262-270, 2014 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-25171487

RESUMO

Xylopia langsdorffiana A. St.-Hil. & Tul. (Annonaceae) is popularly known as "pimenteira-da-terra". Various constituents have been isolated from this species, including diterpenes, such as 8(17), 12E, 14-labdatrien-18-oic acid, ent-atisan-7α, 16α-diol (xylodiol), ent-7α-hydroxytrachyloban-18-oic acid (trachylobane-318) and ent-7α-acetoxytrachyloban-18-oic acid, a crystalline solid with a molecular weight of 360 and molecular formula of C22H32O4 (trachylobane-360). When administered intraperitoneally to mice, trachylobane-360 (T-360) significantly inhibits growth of the solid tumor sarcoma 180 transplanted in mice, without causing alterations in biochemical, hematological and histopathological parameters that are frequently associated with the clinical use of antineoplastic. Furthermore, this diterpene blocks voltage-dependent calcium channels (Cav), showing spasmolytic activity. The present study shows that variables such as extraction solvent (methanol, acetonitrile and chloroform), centrifugation force (1000, 7000 and 14,000×g), and centrifugation time (5, 15 and 25min), are important in the liquid-liquid extraction of T-360 from male Swiss mice blood in HPLC-MSn studies. The study confirms matrix influence on recovery and detection of T-360. The recovery for T-360 was 37.02% using chloroform as better extractor solvent, while centrifuged at 14,000×g for 15min demonstrated the importance of the parameters chosen for the extraction/recovery process of analyte. The effect of mice blood matrix for T-360 was -51.23%. This method was optimized by repeating the extraction procedure and acidification of samples. These conditions were essential in increasing recovery (49.47%) by decreasing the matrix effect (-37.60%). The efficiency of the process, after optimization with two extractions and acidification, increased by 14.19% when compared to the initial method, from 18.05% to 32.24%. According to Marchi et al. (2010), the matrix effect does not necessarily need to be reduced or eliminated, but it does need to be identified and quantified. Therefore, these findings are essential for the subsequent evaluation of the pharmacokinetic parameters of this promising natural product.


Assuntos
Antineoplásicos Fitogênicos/sangue , Bloqueadores dos Canais de Cálcio/sangue , Cromatografia Líquida de Alta Pressão/métodos , Diterpenos/sangue , Espectrometria de Massas por Ionização por Electrospray/métodos , Animais , Calibragem , Centrifugação , Clorofórmio/química , Cromatografia Líquida de Alta Pressão/normas , Concentração de Íons de Hidrogênio , Extração Líquido-Líquido , Masculino , Camundongos , Fitoterapia , Plantas Medicinais , Padrões de Referência , Solventes/química , Espectrometria de Massas por Ionização por Electrospray/normas , Fatores de Tempo , Xylopia
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