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1.
J Oleo Sci ; 73(4): 583-591, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38556291

RESUMO

In this study, it is demonstrated that natural microalgae oils, which contain fatty acid components including docosahexaenoic acid (DHA), could be directly applied to fabricate vesicular structures in aqueous phase through a forced formation process. The microalgae oil vesicles had initial average diameters of 170- 230 nm with negative charges apparently caused by dissociation of the fatty acid components. The vesicles possessed excellent stability with lifetimes for at least 450 days. The formation of the vesicular structures with hydrophilic cores/regions was confirmed by the transmission electron microscopy (TEM) image and successful encapsulation of a hydrophilic material. For encapsulation of a hydrophobic material, lutein, the vesicle size was increased probably due to the insertion of lutein into the hydrophobic vesicular bilayer structures. The analysis of Fourier transform infrared (FTIR) spectroscopy suggested that the vesicular bilayer fluidity was decreased by encapsulating lutein. However, the lutein-encapsulating microalgae oil vesicles still possessed high stability and the vesicular structures could maintain intact even at an environmental temperature up to 60℃. Applicability of the microalgae oil vesicles as drug delivery carriers was also demonstrated by successful encapsulation of curcumin. However, when the loaded curcumin was increased to a certain amount, physical stability of the microalgae oil vesicles was significantly reduced. This is probably because the vesicular structures with only limited spaces for accommodating hydrophobic materials were strongly affected by encapsulating a large amount of curcumin. It is interesting to note that by adding egg L-α-phosphatidylcholine, the curcumin encapsulation-induced instability of the microalgae oil vesicles could be alleviated. The results indicated that vesicular structures could be fabricated from microalgae oils and the microalgae oil vesicles were capable of encapsulating hydrophilic or hydrophobic materials for drug delivery applications. The findings lay a background for further dosage form development of nutritional supplements encapsulated by natural microalgae oils.


Assuntos
Curcumina , Microalgas , Microalgas/química , Luteína , Óleos , Portadores de Fármacos/química , Ácidos Docosa-Hexaenoicos
2.
Diagnostics (Basel) ; 11(9)2021 Sep 20.
Artigo em Inglês | MEDLINE | ID: mdl-34574069

RESUMO

Transcutaneous bilirubinometer devices are widely applied to assess neonatal hyperbilirubinemia. However, the optimal skin site and timing of transcutaneous bilirubin (TCB) measurements for the strongest correlation with total serum bilirubin (TSB) levels after phototherapy are still unclear. We conducted a retrospective observational study evaluating the correlation of TCB and TSB levels in neonates postphototherapy. The TCB measurements on the forehead and mid-sternum at 0 and 30 min postphototherapy were assessed by using a JM-103 bilirubinometer. Paired TCB and TSB measurements were assessed by Pearson correlation and Bland-Altman plots. We analyzed 40 neonates with 96 TSB and 384 TCB measurements. The TSB level correlated moderately with the forehead TCB level at 30 min postphototherapy (r = 0.65) and less strongly with the midsternum TCB level at 0 min postphototherapy (r = 0.52). The forehead at 30 min after cessation of phototherapy was the best time point and location of TCB measurement for the assessment of neonatal jaundice status. The reliability of TCB measurements varied across skin sites and durations after phototherapy. The effectiveness of TCB measurement to assess neonatal hyperbilirubinemia is much better on covered skin areas (foreheads) 30 min postphototherapy. The appropriate application of transcutaneous bilirubinometers could aid in clinical practice and avoid unnecessary management.

3.
Plant Dis ; 105(12): 4121-4131, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34213966

RESUMO

Welsh onion (Allium fistulosum L.) is one of the main and oldest vegetable crops grown in Taiwan. A severe epidemic of leaf blight in Welsh onion caused by a Stemphylium-like pathogen was found in Sanxing, Taiwan, from 2018 to 2020. However, correct species identification, biology, and control of Stemphylium leaf blight (SLB) of Welsh onion are not well-established. Therefore, the main objective of this study was to investigate the causal agent of SLB in Sanxing and evaluate the in vitro sensitivity of Stemphylium-like pathogen to commonly used fungicides. A phylogenetic analysis based on combining the internal transcribed spacer (ITS) region and glyceraldedyhe-3-phosphate dehydrogenase (gapdh) and calmodulin (cmdA) gene sequences together with morphological features identified that S. vesicarium is associated with SLB in Sanxing. When inoculated onto Welsh onion leaves, the isolates caused symptoms identical to those observed in the field; therefore, S. vesicarium was reisolated and Koch's postulates were confirmed. We observed a higher incidence of SLB symptoms on the oldest leaves compared with younger leaves. The maximum and minimum temperatures for in vitro mycelial growth and conidial germination (%) of S. vesicarium were 20 to 30°C and 5°C, respectively. Sixteen fungicides were tested for their effectiveness to reduce the mycelial growth and conidial germination of S. vesicarium in vitro. Boscalid plus pyraclostrobin, fluopyram, fluxapyroxad, and fluxapyroxad plus pyraclostrobin were highly effective at reducing mycelial growth and conidial germination in S. vesicarium. However, strobilurin fungicides (azoxystrobin and kresoxim-methyl) commonly used in Welsh onion production in Sanxing were ineffective. This study discusses the emergence of SLB caused by S. vesicarium in the foliar disease complex affecting Welsh onion and the management of the disease using fungicides with different modes of action in Taiwan. The research will support the sustainable management of SLB in Sanxing, Taiwan; however, further field assessments of the fungicides are warranted.


Assuntos
Allium , Ascomicetos , Ascomicetos/genética , Cebolas , Filogenia , Taiwan
4.
J Med Food ; 22(5): 469-478, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-31084539

RESUMO

Aging and lifestyle factors, including high-sugar and high-fat diets, promote a systemic metabolic imbalance that promotes neurodegeneration. Hericium erinaceus has long been used in traditional Chinese medicine. Recently, its functional activities, such as antimetabolic dysfunction, antineuroinflammatory activities, and stimulation of nerve growth factor (NGF) synthesis, have been revealed. This study demonstrated that Hericium erinaceus mycelium (HEM) and an isolated diterpenoid derivative, erinacine A (EA), may reverse spatial learning disabilities in aging mice (15 months old) fed with a high-fat and high-sucrose diet (HFSD). Aging mice were randomly assigned to one of four treatment groups: (1) a chow diet (control), (2) an HFSD, and an HFSD supplemented with either (3) HEM or (4) EA for 18 weeks. The Morris water maze (MWM) and Y-maze were used for behavioral assessments. Both HEM- and EA-treated mice had shorter mean daily escape latencies than HFSD-treated mice in the MWM. In addition, HEM-treated mice had a slightly increased exploratory time and frequency in the novel arm in the Y-maze. Quantitative PCR revealed that both HEM- and EA-treated mice exhibited reduced messenger RNA (mRNA) expression of tumor necrosis factor-α, interleukin-1ß, and HEM-treated mice exhibited increased mRNA expression of NGF and NeuN in the hippocampus. Moreover, HEM and EA also decreased body weight, abdominal fat, plasma glucose, serum and liver total cholesterol, and liver triacylglycerol. Thus, HEM may be a potential health-promoting supplement for minimizing the progression of aging and obesity-induced neurodegeneration by reducing metabolic abnormalities and neuroinflammatory cytokines and increasing neurogenesis factors.


Assuntos
Envelhecimento/efeitos dos fármacos , Basidiomycota/química , Dieta Hiperlipídica/efeitos adversos , Diterpenos/administração & dosagem , Doenças Metabólicas/tratamento farmacológico , Sacarose/efeitos adversos , Envelhecimento/metabolismo , Envelhecimento/psicologia , Animais , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Hipocampo/fisiopatologia , Humanos , Masculino , Aprendizagem em Labirinto , Doenças Metabólicas/etiologia , Doenças Metabólicas/metabolismo , Doenças Metabólicas/psicologia , Camundongos , Camundongos Endogâmicos C57BL , Micélio/química , Fator de Crescimento Neural/genética , Fator de Crescimento Neural/metabolismo , Aprendizagem Espacial/efeitos dos fármacos
5.
Am J Chin Med ; 46(3): 537-549, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29595072

RESUMO

Platycodin D (PD) is the main active saponin isolated from Platycodon grandiflorum (PG) and is reported to exhibit anticancer, anti-angiogenic, anti-inflammation and anti-obesity biological effects. The current study aims to evaluate the therapeutic efficacy of PD in cardiac fibrosis and for hypertrophy in spontaneous hypertension rats (SHRs) and to verify inhibition of the signaling pathway. Significant increases in the cardiac functional indices of left ventricular internal diameter end diastole (LVIDd) and left ventricular internal diameter end systole (LVIDs); the eccentric hypertrophy marker p-MEK5; concentric hypertrophy markers, such as CaMKII[Formula: see text] and calcineurin; and expression levels of NFATc3, p-GATA4 and BNP were observed in spontaneously hypertensive groups. PD treatment reversed these increases in SHRs. In addition, an increase in the fibrosis markers FGF2, uPA, MMP2, MMP9, TGF[Formula: see text]-1 and CTGF during cardiac hypertrophy was detected by western blotting analyses. These results demonstrated that PD treatment considerably attenuates cardiac fibrosis. Histopathological examination revealed that PD treatment remarkably reduced collagen accumulation in contrast to spontaneously hypertensive groups. This study clearly suggests that PD provides myocardial protection by alleviating two damaging responses to hypertension, fibrosis and hypertrophy, in the heart.


Assuntos
Cardiomegalia/tratamento farmacológico , Miocárdio/patologia , Fitoterapia , Saponinas/uso terapêutico , Triterpenos/uso terapêutico , Animais , Cardiomegalia/etiologia , Cardiomegalia/metabolismo , Cardiomegalia/patologia , Colágeno/metabolismo , Modelos Animais de Doenças , Fibrose , Miocárdio/metabolismo , Platycodon/química , Ratos Endogâmicos SHR , Ratos Endogâmicos WKY , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação
6.
Clin Cancer Res ; 24(5): 1176-1189, 2018 03 01.
Artigo em Inglês | MEDLINE | ID: mdl-29222162

RESUMO

Purpose: MPT0L145 has been developed as a FGFR inhibitor exhibiting significant anti-bladder cancer activity in vitro and in vivo via promoting autophagy-dependent cell death. Here, we aim to elucidate the underlying mechanisms.Experimental Design: Autophagy flux, morphology, and intracellular organelles were evaluated by Western blotting, transmission electron microscope, and fluorescence microscope. Molecular docking and surface plasmon resonance assay were performed to identify drug-protein interaction. Lentiviral delivery of cDNA or shRNA and CRISPR/Cas9-mediated genome editing was used to modulate gene expression. Mitochondrial oxygen consumption rate was measured by a Seahorse XFe24 extracellular flux analyzer, and ROS level was measured by flow cytometry.Results: MPT0L145 persistently increased incomplete autophagy and phase-lucent vacuoles at the perinuclear region, which were identified as enlarged and alkalinized late-endosomes. Screening of a panel of lipid kinases revealed that MPT0L145 strongly inhibits PIK3C3 with a Kd value of 0.53 nmol/L. Ectopic expression of PIK3C3 reversed MPT0L145-increased cell death and incomplete autophagy. Four residues (Y670, F684, I760, D761) at the ATP-binding site of PIK3C3 are important for the binding of MPT0L145. In addition, MPT0L145 promotes mitochondrial dysfunction, ROS production, and DNA damage, which may in part, contribute to cell death. ATG5-knockout rescued MPT0L145-induced cell death, suggesting simultaneous induction of autophagy is crucial to its anticancer activity. Finally, our data demonstrated that MPT0L145 is able to overcome cisplatin resistance in bladder cancer cells.Conclusions: MPT0L145 is a first-in-class PIK3C3/FGFR inhibitor, providing an innovative strategy to design new compounds that increase autophagy, but simultaneously perturb its process to promote bladder cancer cell death. Clin Cancer Res; 24(5); 1176-89. ©2017 AACR.


Assuntos
Autofagia/efeitos dos fármacos , Classe III de Fosfatidilinositol 3-Quinases/antagonistas & inibidores , Compostos de Fenilureia/farmacologia , Receptores de Fatores de Crescimento de Fibroblastos/antagonistas & inibidores , Triazinas/farmacologia , Neoplasias da Bexiga Urinária/tratamento farmacológico , Autofagia/genética , Proteína 5 Relacionada à Autofagia/genética , Proteína 5 Relacionada à Autofagia/metabolismo , Linhagem Celular Tumoral , Cisplatino/farmacologia , Cisplatino/uso terapêutico , Classe III de Fosfatidilinositol 3-Quinases/metabolismo , Avaliação Pré-Clínica de Medicamentos , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Técnicas de Inativação de Genes , Humanos , Simulação de Acoplamento Molecular , Compostos de Fenilureia/uso terapêutico , Ligação Proteica , Pirimidinas/farmacologia , Receptores de Fatores de Crescimento de Fibroblastos/metabolismo , Triazinas/uso terapêutico , Neoplasias da Bexiga Urinária/patologia
7.
J Ethnopharmacol ; 205: 41-50, 2017 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-28473244

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Platycodon grandiflorum (PG) is a Chinese medical plant used for decades as a traditional prescription to eliminate phlegm, relieve cough, reduce inflammation and lower blood pressure. PG also has a significant effect on the cardiovascular systems. MATERIALS AND METHODS: The aqueous extract of Platycodon grandiflorum (JACQ.) A. DC. root was screened for inhibiting Ang II-induced IGF-IIR activation and apoptosis pathway in H9c2 cardiomyocytes. The effects were also studied in spontaneously hypertensive rats (five groups, n=5) using low and high doses of PG for 50 days. The Ang II-induced IGF-IIR activation was analyzed by luciferase reporter, RT-PCR, western blot and surface IGF-IIR expression assay. Furthermore, the major active constituent of PG was carried out by high performance liquid chromatography-mass spectrometry (HPLC-MS). RESULTS: Our results indicate that a crude extract of PG significantly suppresses the Ang II-induced IGF-IIR signaling pathway to prevent cardiomyocyte apoptosis. PG extract inhibits Ang II-mediated JNK activation and SIRT1 degradation to reduce IGF-IIR activity. Moreover, PG maintains SIRT1 stability to enhance HSF1-mediated IGF-IIR suppression, which prevents cardiomyocyte apoptosis. In animal models, the administration of PG markedly reduced this apoptotic pathway in the heart of SHRs. CONCLUSION: Taken together, PG may be considered as an effective treatment for cardiac diseases in hypertensive patients.


Assuntos
Angiotensina II/farmacologia , Apoptose/efeitos dos fármacos , Extratos Vegetais/farmacologia , Platycodon/química , Receptor IGF Tipo 2/metabolismo , Animais , Linhagem Celular , Regulação da Expressão Gênica/efeitos dos fármacos , Mioblastos/efeitos dos fármacos , Extratos Vegetais/química , Ratos , Ratos Endogâmicos WKY , Receptor IGF Tipo 2/genética , Saponinas/química , Saponinas/farmacologia , Triterpenos/química , Triterpenos/farmacologia
8.
J Am Chem Soc ; 132(38): 13371-80, 2010 Sep 29.
Artigo em Inglês | MEDLINE | ID: mdl-20822102

RESUMO

A new type of glycan array covalently or noncovalently attached to aluminum oxide-coated glass (ACG) slides has been developed for studies of enzymatic reactions and protein binding. To prepare the noncovalent array, glycans with a polyfluorinated hydrocarbon (-C(8)F(17)) tail are spotted robotically onto the ACG slide surface containing a layer of polyfluorinated hydrocarbon terminated with phosphonate. After incubation and washing, the noncovalent array can be characterized by MS-TOF via ionization/desorption at a low laser energy without addition of matrix. A representative cellotetraose array was developed to study the activity and specificity of different cellulases and to differentiate the exo- and endoglucanase activities. To prepare the covalent array, glycans with a phosphonic acid tail were synthesized and spotted robotically onto the ACG slide surface. After incubation, the slides can be used directly for quantitative protein binding analysis. Compared to the preparation of glycan arrays on glass slides and other surfaces, this method of arraying using phosphonic acid reacting with ACG is more direct, convenient, and effective and represents a new platform for the high-throughput analysis of protein-glycan interactions.


Assuntos
Óxido de Alumínio/química , Vidro , Organofosfonatos/química , Polissacarídeos/química , Celulase/química , Espectrometria de Massas
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