El Daibani Amal A, Xi Yuecheng, Luo Lijun, Mei Xue, Zhou Chunyang, Yasuda Shin, Liu Ming-Cheh
Department of Pharmacology College of Pharmacy and Pharmaceutical Sciences, University of Toledo Health Science Campus, Toledo, OH, USA.
School of Pharmacy, North Sichuan Medical College, Nanchong, Sichuan, China.
Nat Prod Res. 2020 Mar;34(6):797-803. doi: 10.1080/14786419.2018.1503264. Epub 2018 Nov 6.
Previous studies have revealed sulfation as a major pathway for the metabolism of hesperetin, naringenin and apigenin. The current study was designed to identify the human cytosolic sulfotransferase (SULT) enzyme(s) capable of sulfating these flavonoid compounds. Of the thirteen human SULTs, six (1A1, 1A2, 1A3, 1B2, 1C4, 1E1) displayed significant sulfating activity toward hesperetin, five (1A1, 1A2, 1A3, 1B2, 1C4) displayed sulfating activity towards naringenin, and four (1A1, 1A2, 1A3, 1C4) showed sulfating activity towards apigenin. Of the four human organ specimens tested, liver and intestine cytosols displayed much higher hesperetin-, naringenin- and apigenin-sulfating activity than lung and kidney cytosols. Moreover, sulfation of hesperetin, naringenin and apigenin was shown to take place in HepG2 human hepatoma cells and Caco-2 human colon adenocarcinoma cells under cultured conditions. Taken together, these results provided a biochemical basis underlying the metabolism of hesperetin, naringenin and apigenin through sulfation in humans.[Formula: see text].
先前的研究表明，硫酸化是橙皮素、柚皮素和芹菜素代谢的主要途径。本研究旨在鉴定能够使这些类黄酮化合物硫酸化的人胞质硫酸转移酶（SULT）。在13种人SULT中，6种（1A1、1A2、1A3、1B2、1C4、1E1）对橙皮素表现出显著的硫酸化活性，5种（1A1、1A2、1A3、1B2、1C4）对柚皮素表现出硫酸化活性，4种（1A1、1A2、1A3、1C4）对芹菜素表现出硫酸化活性。在所测试的4种人体器官标本中，肝脏和肠道胞质溶胶对橙皮素、柚皮素和芹菜素的硫酸化活性远高于肺和肾脏胞质溶胶。此外，在培养条件下，橙皮素、柚皮素和芹菜素的硫酸化在HepG2人肝癌细胞和Caco-2人结肠腺癌细胞中发生。综上所述，这些结果为人类通过硫酸化代谢橙皮素、柚皮素和芹菜素提供了生化基础。[公式：见正文]
