| The paper aimed at the chemical constituents of Citri Grandis Exocarpium and study the metabolism of the main active ingredient.In the first chapter, a detailed review was given to the latest development of Citri Grandis Exocarpium about its basic source, chemical constituents, quality assessment research, pharmacological effects, clinical application and product development research, and the latest development about naringin, naringenin, limonin, obacunone pharmacological activity and metabolism.In the second chapter, the chemical constituents of Citri Grandis Exocarpium and their relative content in different organs were studied. The compounds were isolated by silica gel and polyamide column chromatography, and their structures were identified on the basis of spectral analysis and physicochemical data. As a result, fortheen compounds were obtained from the 70% ethanol extract, and their structures were elucidated as demethylfuropinnarin (1), bergapten (2), obacunone (3), limonin (4), isolimonexic acid (5), limonexic acid (6), naringin (7), daucosterol (8), ursolic acid (9),β-sitosterol (10), benzoic acid (11), palmitic acid (12), tetracosanoic acid (13), n-octacosanoic acid (14). Compound 1 was first isolated from the Rutaceae, compounds 3 , 4 , 5 , 6 , 8 , 9 ,10 ,11,12 ,13 and 14 were obtained from this plant for the first time.Comprehensive evaluation of Citrus grandis 'Tomentosa' was studied on. Flowers, fruits, leaves of Citrus grandis 'Tomentosa' were analyzed by UPLC -QTOF-MS methods and PCA . Conclusion: The content of naringin, naringenin, obacunone and limonin in flowers and fruits were relatively higher than in leaves, The content of these compounds in flowers was of the highest. The content of isolimonexic acid and limonexic acid in flowers was as much as fruits. The content of these two compounds in leaves was the highest. The content of demethylfuropinnarin in fruit was relatively higher than in flowers and leaves.Using UV, HPLC, respectively ,to analyse the content of total flavonoids, polysaccharides, naringin in flowers, fruits, leaves of Citrus grandis 'Tomentosa'. Conclusion: The content of total flavonoids in flowers was the highest which calculated by drying was 27.35%, the second was fruits, the content of naringin was 15.2%, leaves was the least, only had 4.08 %; The content of naringin in flowers was the highest which calculated by drying was 20.62%, the second was fruits, the content of naringin was 13.1%, leaves was the least, only had 1.97%; The content of neutral polysaccharide and acidic polysaccharidesare in fruits were the highest which calculated by drying were 5.52 % and 4.04 % , the second were flowers, the content of neutral polysaccharide and acidic polysaccharidesare were 3.20 % and 1.93%, leaves were the least, only had 1.38% and 1.50%.In the thrid chapter, the metabolism of the main active ingredient were studied. The healthy SD rats were fed with alcohol extract of Citri Grandis Exocarpium by 50 g·kg-1for 3 days. On the last day, rat blood samples were collected 1.0 hour after oral admimstration, and collecting 0-24 h feces and 0-4 h,4-8 h,8-24 h urine. The samples were analyzed by UPLC-Q-TOF with MSE function. The post-acquisition data were processed using MetabolynxTM. Through this method, The metabolites of the major components of naringin, naringenin, limonin and obacunone in plasma, urine and feces samples were studied. Conclusion: 7 new metabolites of naringin were discovered, they are naringin-5-O-glucuronide, naringin-4'-O-glucuronide, naringin-4-O-sulfate, sulfate conjugate of hydroxylated naringin, hydroxylate conjugate of naringin, glucuronide conjugate of hydroxylated naringin, acetylate conjugate of naringin. 3 new metabolites of naringenin were discovered, they are methylated conjugate of hydroxylated naringenin, glucuronide conjugate of hydroxylated naringenin, reduced naringenin. These results provides new evidence for the research of the metabolism of naringin, naringenin.
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