RESUMEN
Herein, a nano-micelle drug delivery system was developed to orally improved zingerone's bioavailability and its antitumor effect. Indeed, zingerone-loaded d-α-tocopheryl polyethylene glycol succinate micelles (ZTMs) were effectively prepared, characterised and assessed. The ZTMs had diameter, polydispersity index, and zeta potential of 50.62 ± 0.25 nm, 0.168 ± 0.006, and -28.07 ± 0.33 mV, respectively, coupled with a high entrapment efficiency (m/m, %) were 94.71 ± 2.02. The release rate of ZTMs in three media was significantly greater than that of free zingerone. Intriguingly, results obtained from pharmacokinetic studies showed that the oral bioavailability of the ZTMs was enhanced by 5.10 times in comparison with the free zingerone. Further, the half inhibitory concentration (IC50) of ZTMs and free zingerone was 7.56 µg/ml and 14.30 µg/ml, respectively, on HepG2 cells. Hence, ZTMs may be used as a potential approach to enrich the solubility, bioavailability, and concomitant anti-proliferative effect of zingerone in vitro.
Asunto(s)
Micelas , Sistema de Administración de Fármacos con Nanopartículas , Disponibilidad Biológica , Portadores de Fármacos , Sistemas de Liberación de Medicamentos , Liberación de Fármacos , Guayacol/análogos & derivados , PolietilenglicolesRESUMEN
Moringa seed extract containing 1-O-(4-hydroxy-methylphenyl)-α-l-rhamno-pyranoside (GR) has been reported to ameliorate CCl4 induced hyperlipidemia in the liver. However, it is unclear whether GR has any therapeutic effect on NAFLD. This study aimed to determine the hypolipidemic and concomitant hepatoprotective potential of GR. The structure and purity of GR were assessed and characterized using high performance liquid chromatography-mass spectrometry (UPLC-MS/MS). The NAFLD model was established based on the L02 cells in vitro. After GR intervention, intracellular fat deposition and reactive oxygen content were significantly reduced, GR could up-regulation of AMPK and PPARα and the down-regulation of mTOR and SREBP-1, which play a key role in liver lipid homeostasis. In vivo experiments revealed that GR intervention significantly decreased serum fat content, inhibited liver injury, and increased antioxidant mechanism in mice fed with high fat diet. Hence, GR demonstrated promising hypolipidemic and hepatoprotective activities, serving as a potential candidate for NAFLD therapy.
Asunto(s)
Moringa , Enfermedad del Hígado Graso no Alcohólico , Animales , Alcoholes Bencílicos , Cromatografía Liquida , Dieta Alta en Grasa , Metabolismo de los Lípidos , Hígado/metabolismo , Ratones , Ratones Endogámicos C57BL , Enfermedad del Hígado Graso no Alcohólico/tratamiento farmacológico , Enfermedad del Hígado Graso no Alcohólico/genética , Espectrometría de Masas en TándemRESUMEN
Ectomesenchymal stem cells (EMSCs) are typical adult stem cells obtained from the cranial neural crest. They have the potential to differentiate into various cell types, such as osseous cells, neurons and glial cells. Three-dimensional (3 D) printing is a novel method to construct biological structures by rapid prototyping. Previously, our group reported on the stemness and multi-lineage differentiation potential of EMSCs on gels. However, the exploration of EMSCs in 3 D printing and then evaluation of the growth and neuronal differentiation of EMSCs on extruded 3 D printable hybrid hydrogels has not been reported. Therefore, the current study explored the novel hybrid Sodium alginate-Matrigel (SA-MA) hydrogel extruded 3 D printing to design an in vitro scaffold to promote the differentiation and growth of EMSCs. In addition, the physical properties of the hydrogel were characterized and its drug-releasing property determined. Notably, the results showed that the construct exhibited a sustain-released effect of growth factor BDNF in accordance with the Higuchi equation. Moreover, the cell survival rate on the 3 D printed scaffold was 88.22 ± 1.13% with higher neuronal differentiation efficiency compared with 2 D culture. Thus, SA-MA's ability to enhanced EMSCs neuronal differentiation offers a new biomaterial for neurons regeneration in the treatment of spinal cord injury.