依普黄酮（TC-80）在大鼠体内的代谢。

Metabolism of ipriflavone (TC-80) in rats.

作者信息

Yoshida K, Tsukamoto T, Torii H, Doi T, Naeshiro I, Uemura I, Tanayama S

出版信息

Radioisotopes. 1985 Nov;34(11):612-7. doi: 10.3769/radioisotopes.34.11_612.

DOI:10.3769/radioisotopes.34.11_612

Abstract

Metabolic studies of ipriflavone (TC-80) in rats by gas-liquid chromatography-mass spectrometry led to the characterization of the following metabolites: the parent compound, 7-hydroxy-3-phenyl-4H-1-benzopyran-4-one, 7-hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one, 3-(4-hydroxyphenyl)-7-isopropoxy-4H-1-benzopyran-4-one, 2-(3-phenyl-4-oxo-4H-1-benzopyran-7-yl)oxypropionic acid, 2-[3-(4-hydroxyphenyl)-4-oxo-4H-1-benzopyran-7-yl]oxypropionic acid and 2-[3-(3-hydroxyphenyl)-4-oxo-4H-1-benzopyran-7-yl]oxypropionic acid. From the metabolites identified, TC-80 was shown to be metabolized primarily by oxidation. In vitro study using tissue slices of rats indicated that the above metabolic changes occurred exclusively in the liver. It was also demonstrated that the compound did not undergo metabolic conversion by gut flora of rats.

摘要

采用气液色谱-质谱联用技术对大鼠体内的依普黄酮（TC-80）进行代谢研究，确定了以下代谢产物：母体化合物、7-羟基-3-苯基-4H-1-苯并吡喃-4-酮、7-羟基-3-(4-羟基苯基)-4H-1-苯并吡喃-4-酮、3-(4-羟基苯基)-7-异丙氧基-4H-1-苯并吡喃-4-酮、2-(3-苯基-4-氧代-4H-1-苯并吡喃-7-基)氧基丙酸、2-[3-(4-羟基苯基)-4-氧代-4H-1-苯并吡喃-7-基]氧基丙酸和2-[3-(3-羟基苯基)-4-氧代-4H-1-苯并吡喃-7-基]氧基丙酸。从已鉴定的代谢产物来看，TC-80主要通过氧化进行代谢。利用大鼠组织切片进行的体外研究表明，上述代谢变化仅发生在肝脏中。此外还证明，该化合物不会被大鼠肠道菌群进行代谢转化。