RESUMEN
@#In order to investigate the therapeutic effects of scutellarein on acute pharyngitis, 60 rats were randomly divided into five groups: blank group, model group, low-dose scutellarein group, high-dose scutellarein group and positive drug group. HE staining, blood-cell-analyzer, IL-6, IL-1β and TNF-α ELISA kit were used to study the effects of scutellarein on acute pharyngitis in pharyngeal tissue morphology, the counts of white blood cells and neutrophil and the serum concentrations of TNF-α, IL-1β and IL-6. Meanwhile, forty mice were randomly divided into four groups: blank group, low-dose scutellarein group, high-dose scutellarein group and positive drug group. Then, hot plate and writhing test of mice were carried out to study the analgesic effects of scutellarein. Results showed that, compared to the model group, scutellarein improved the physical status of acute pharyngitis rats, reduced the number of white blood cells significantly(P< 0. 05)and decreased the number of neutrophils and the levels of TNF-α, IL-1β and IL-6 in rats serum significantly(P< 0. 01). Meanwhile, scutellarein dramatically improved the pain threshold in hot plate test and decreased the number of writhing mice(P< 0. 01). It can be concluded that scutellarein can be used to treat acute pharyngitis with its anti-inflammatory and analgesic effect.
RESUMEN
@#The aim of this study was to synthesize and evaluate the necrosis avidity of MRI contrast agent based on rhein and linked by ether. The novel ligand 10-{［6-(1, 8-dihydroxyanthraquinone-3-carboxamido)ethoxyethyl］amino}carbonylmethyl-1, 4, 7, 10-tetraazacyclododecan-1, 4, 7-triacetic acid(DO3A-Ether-Rhein, E1)was synthesized by two steps of acylation and deprotection reaction. The paramagnetic gadolinium 10-{［6-(1, 8-dihydroxyanthraquinone-3-carboxamido)ethoxyethyl］amino}carbonylmethyl-1, 4, 7, 10-tetraazacyclododecan-1, 4, 7-triacetic acid(Gd-DO3A-Ether-Rhein, GdE1)was obtained by coordination of Gd3+ with the above ligand. We examined the necrotic avidity of GdE1 in human hepatocellular carcinoma HepG2 cell necrosis induced by hyperthermia in vitro and in rat model with muscular necrosis induced by microwave ablation in vivo by MRI. The MRI was implemented before administration of GdE1 and during 0-9 h after administration of GdE1(0. 1 mmol/kg), and Gd-DOTA(gadolinium 1, 4, 7, 10-tetraacetic acid-1, 4, 7, 10-tetraazacyclo dodecane)was used as control. The signal intensity of necrotic cells(4 369±70)was significantly higher than that of normal cells(2 555±84)(P< 0. 05). Similarly, the contrast ratio between necrotic and normal muscle at 3 h after administration of GdE1(2. 00±0. 12)was remarkblely higher than that at 0 h after administration of GdE1(1. 27±0. 03)(P< 0. 05). Therefore, GdE1 presents good necrosis affinity and has the potential to be used in the diagnosis of necrosis-related diseases.