RESUMEN
Isoliquiritigenin (ISL) possesses a variety of pharmacological activities amid poor solubility in water which has restricted its clinical application. In this study, isoliquiritigenin-loaded F127/P123 polymeric micelles (ISL-FPM) were successfully prepared and evaluated in vitro and in vivo. The particle size, polydispersity index, and zeta potential of the selected formulation were 20.12 ± 0.72 nm, 0.183 ± 0.046, and -38.31 ± 0.33 mV, respectively, coupled with high encapsulation efficiency of 93.76 ± 0.31%. Drug-loading test showed the solubility of ISL after formulating into micelles was 232 times higher than its intrinsic solubility. Moreover, critical micelle concentration (CMC) was tested with fluorescence probe method and turned out to be quite low, which implied high stability of ISL-FPM. Release profile in HCl (pH 1.2), double distilled water, and PBS (pH 7.4) of ISL-FPM reached over 80%, while free ISL was around 40%. Pharmacokinetic research revealed that formulated ISL-FPM significantly increased bioavailability by nearly 2.23-fold compared to free ISL. According to the results of in vitro antioxidant activity, scavenging DPPH activity of ISL was significantly strengthened when it was loaded into polymeric micelles. Altogether, ISL-FPM can act as a promising approach to improve solubility as well as enhance bioavailability and antioxidant activity of ISL.
Asunto(s)
Chalconas/química , Chalconas/farmacocinética , Polietilenos/química , Polímeros/química , Polipropilenos/química , Animales , Antioxidantes/química , Antioxidantes/farmacología , Disponibilidad Biológica , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Masculino , Micelas , Tamaño de la Partícula , Ratas , Ratas Sprague-Dawley , Solubilidad/efectos de los fármacosRESUMEN
Sclerotinia ginseng is a necrotrophic soil pathogen that mainly infects the root and basal stem of ginseng, causing serious commercial losses. Sclerotia, which are important in the fungal life cycle, are hard, asexual, resting structures that can survive in soil for several years. Generally, sclerotium development is accompanied by the exudation of droplets. Here, the yellowish droplets of S. ginseng were first examined by sodium dodecyl sulfate-polyacrylamide gel electrophoresis, and the proteome was identified by a combination of different analytical platforms. A total of 59 proteins were identified and classified into six categories: carbohydrate metabolism (39%), oxidation-reduction process (12%), transport and catabolism (5%), amino acid metabolism (3%), other functions (18%), and unknown protein (23%), which exhibited considerable differences in protein composition compared with droplets of S. sclerotium. In the carbohydrate metabolism group, several proteins were associated with sclerotium development, particularly fungal cell wall formation. The pathogenicity and virulence of the identified proteins are also discussed in this report. The findings of this study may improve our understanding of the function of exudate droplets as well as the life cycle and pathogenesis of S. ginseng.
RESUMEN
In this study, five phenolic compounds of ginseng rhizosphere soil were identified by HPLC, including gallic acid, salicylic acid, 3-phenylpropionic acid, benzoic acid and cinnamic acid. The results show that five phenolic compounds inhibited mycelium growth and spore germination at high concentration, but promoted mycelium growth and spore germination at low concentration. Gallic acid, salicylic acid, benzoic acid of 0.5 mmol·L-1 and 3-phenylpropionic acid, cinnamic acid of 0.05 mmol·L-1 could significantly promote the spore germination, mycelium growth and disease severity of Cylindrocarpon destructans.
