To analyze naringin, naringenin and its metabolites in rat urine and feces after intragastric administration of alcohol extract of Exocarpium Citri Grandis, healthy SD rats were fed with alcohol extract of Exocarpium Citri Grandis for 3 days. On the last day, 0-24 h feces and 0-4 h, 4-8 h, 8-24 h urine were collected and analyzed by UPLC-Q-TOF/MS. The post-acquisition data were processed using Metabolynx The result is that naringin and its 6 metabolites, naringenin and its 4 metabolites were detected in the urine of rat. Meanwhile, naringin and its 3 metabolites, naringenin and its 2 metabolites were detected in the feces of rat.

Objective To study the regulation effect of estrogen in expression of matrix metalloproteinase-9 (MMP-9) in the central nervous system (CNS) in mice with experimental autoimmune encephalomyelitis ( EAE).Methods The 60 mice were overiectomized and 2 weeks later EAE was induced with MOG35-55 peptide in these mice.They were divided into a treatment group and a control group.The treatment group was treated with estrogen and the control group was given PBS.Clinical symptoms in these two groups were scored and compared.HE staining was used to observe inflammation in the brain and spinal cord.The MMP-9 expression in the CNS was examined by quantitative real-time PCR and immunofluorescence staining.Results The incidence of disease was lower (treatment and control group were 8/30 and 28/30 respectively) and clinical symptoms were milder (treatment and control group were 3.23±0.83 and 1.62 ±1.00 respectively,t=3.811 and P＜0.05) in the treatment group than those in the control group.HE staining showed the decreased infiltration of inflammatory cell in the treatment group (Treatment group:inflammatory score were 0.895 ±0.206,0.752 ±0.302,0.732 ±0.183 in acute,relief and chronic phase respectively;Control group:inflammatory score were 3.472 ±0.635,2.881 ±0.662,1.891 ± 0.482 in acute,relief and chronic phase respectively.t = 8.622,6.543 and 5.027,all P ＜ 0.05).The quantitative real-time PCR and immunofluorescence staining showed that the expression of MMP9 in the CNS was decreased in the treatment group.Conclusion Estrogen may decrease MMP-9 expression in the CNS,reduce inflammation and clinical symptoms in mice with EAE.

OBJECTIVETo analyze naringin, naringenin and its metabolites in rat plasma after intragastric administration of exocarpium Citri grandis alcohol extract.

METHODRat blood samples were collected 1.0 hour after oral administration of 50 g x kg(-1) exocarpium Citri grandis alcohol extract and analyzed by UPLC-Q-TOF with MS(E) function. The post-acquisition data were processed using Metabolynx.

RESULTNaringin (M1), naringenin (M2), naringin-5-O-glucuronide (M3), naringin-4-O-glucuronide (M4), glucuronide conjugate of naringenin (M5), naringin-4-O-sulfate (M6), methylated conjugate of hydroxylated naringenin (M7), glucuronide and sulfate conjugate of naringenin (M8), glucuronide conjugate of hydroxylated naringenin (M9) in rat plasma were detected. M3, M4, M6 were first reported as the metabolites of naringin. M7, M9 were first reported as the metabolites of naringenin.

CONCLUSIONThe results indicated that naringin, naringenin can be metabolited as the forms of glucuronidation, sulfation and naringenin can also be metabolited as the forms of methylation with hydroxylation and glucuronidation with hydroxylation in vivo after administration.

Animals ; Chromatography, High Pressure Liquid ; Citrus ; chemistry ; Drug Administration Routes ; Flavanones ; blood ; metabolism ; Male ; Mass Spectrometry ; Plant Extracts ; administration & dosage ; blood ; metabolism ; Random Allocation ; Rats ; Rats, Sprague-Dawley