Acacetin alleviates energy metabolism disorder through promoting white fat browning mediated by AC-cAMP pathway

Acacetin (ACA), a flavone isolated from Chinese traditional medical herbs, has numerous pharmacological activities. However, little is known about the roles in white fat browning and energy metabolism. In the present study, we investigated whether and how ACA would improve energy metabolism in vivo and in vitro. ACA (20 mg/kg) was intraperitoneally injected to the mice with obesity induced by HFD for 14 consecutive days (in vivo); differentiated 3T3-L1 adipocytes were treated with ACA (20 µmol/L and 40 µmol/L) for 24 h (in vitro). The metabolic profile, lipid accumulation, fat-browning and mitochondrial contents, and so on were respectively detected. The results in vivo showed that ACA significantly reduced the body weight and visceral adipose tissue weight, alleviated the energy metabolism disorder, and enhanced the browning-related protein expressions in adipose tissue of rats. Besides, the data in vitro revealed that ACA significantly reduced the lipid accumulation, induced the expressions of the browning-related proteins and cAMP-dependent protein kinase A (PKA), and increased the mitochondrium contents, especially enhanced the energy metabolism of adipocytes; however, treatment with beta-adrenergic receptor blocker (propranolol, Pro) or adenyl cyclase (AC) inhibitor (SQ22536, SQ) abrogated the ACA-mediated effects. The data demonstrate that ACA alleviates the energy metabolism disorder through the pro-browning effects mediated by the AC-cAMP pathway. The findings would provide the experimental foundation for ACA to prevent and treat obesity and related metabolism disorders. (AU)

Chryseriol attenuates the progression of OVA-induced asthma in mice through NF-kB/HIF-1α and MAPK/STAT1 pathways

Background: Asthma is a hackneyed chronic inflammatory disease of the airway. Chryseriol (CSR) is a kind of flavonoid, and has the effect of bronchiectasis, indicating its potential application for treating respiratory diseases. However, the functions of CSR in asthma have not been reported till now. Materials and methods: The histopathologic changes of the lung tissues were assessed by hematoxylin and eosin staining. The cell apoptosis was identified through terminal deoxynucleotidyl transferase-mediated dUTP nick end labelling assay. Total numbers of eosinophils, neutrophils, and macrophages were assessed under microscope. The levels of interleukin (IL)-1β, IL-4, IL-5, and IL-13 were detected by enzyme-linked-immunosorbent serologic assay. The airway hyper-responsiveness (AHR) was evaluated by the whole body plethysmography. The levels of methane dicarboxylic aldehyde, superoxide dismutase, glutathione S-transferase, and glutathione in lung homogenates were confirmed by using corresponding commercial kits. The protein expressions were examined by Western blot analysis. Results: The ovalbumin (OVA) was utilized to establish asthma mouse model. At first, it was revealed that CSR treatment reduced lung injury in OVA-stimulated mice. Moreover, cell apoptosis was enhanced after OVA stimulation but was attenuated by CSR treatment. In addition, CSR treatment decreased the infiltration of inflammatory cells and the production of inflammatory factors in OVA-treated mice. Further investigations demonstrated that CSR treatment relieved AHR in OVA-stimulated mice. The oxidative stress was strengthened in OVA-treated mice, but these effects were relieved by CSR treatment. Lastly, it was discovered that CSR treatment retarded nuclear factor kappa B (NF-κB)/hypoxia-inducible factor 1 alpha (HIF-1α) and p38 mitogen-activated protein kinase (MAPK)/signal transducer and activator of transcription 1 (STAT1) pathways in OVA-triggered asthma mice (AU)

Efecto de seis flavonoides sobre el crecimiento de la línea de melanoma humano SK-MEL-1

Propósito: Estudiamos la respuesta antiproliferativa de la línea celular de melanoma humano SK-MEL-1 al tratamiento con seis flavonoides y la relación con su estructura química. Material y métodos: Realizamos ensayos de viabilidad celular a 24 y 72 horas, mediante el test colorimétrico con 3-[4,5-Dimetiltiazol-2-il]-2,5-difeniltetrazolio (MTT).Resultados: A las 24 horas de exposición solo dos, tangeretina y luteolina, presentaban ligera inhibición a la máxima concentración utilizada, no observando respuesta con el resto de las sustancias. A las 72 horas, la tangeretina mostraba una clara inhibición del crecimiento y la 7,3`-dimetilhesperetina presentaba inhibición a la máxima concentración, mientras que con los restantes fue negativa. Conclusiones: Los resultados sugieren que la ausencia de doble enlace C2-C3 en flavonoides hidroxilados conlleva la pérdida de su actividad (hesperetina), y que la presencia de al menos tres grupos metoxilados adyacentes confiere un efecto antiproliferativo más potente (tangeretina) (AU)

Estudio del efecto solvatocrómico en derivados fenólicos naturales / Study of the solvatochromic effect on natural phenolic compounds

Se describen las características espectrofluorimétricas de dos derivados de quercetina aislados de las hojas de Flaveria bidentis, un derivado de 6-prenilpinocembrina, aislado de las raíces de Dalea elegans y un compuesto de estructura antraquinónica aislado de las hojas de Heterophyllaea pustulata. Todos ellos presentan espectros de absorción con máximos en la región UV-visible acordes con los grupos cromóforos presentes en su estructura. Los cuatro compuestos estudiados presentan fluorescencia nativa. La posición de los máximos de emisión de fluorescencia se modifica en función del disolvente. Los desplazamientos producidos están relacionados con el diferente grado de solvatación de las moléculas en estado excitado según la polaridad del disolvente. La adición de ácidos minerales provoca desplazamientos en los máximos de fluorescencia concordantes con los ya descritos para compuestos de estructura similar. Estas modificaciones espectrales tienen un gran interés analítico desde el punto de vista de la identificación y caracterización de productos naturales de estructura fenólica (AU)