In the present study,we aimed to ascertain the metabolic detoxification routes of genipin via CYP3A4,SULT2 A1,and UGT1 A1 in Hepa RG cells.It was found that the hepatic CYP3A4,SULT2 A1,and UGT1 A1 synergistically medi...In the present study,we aimed to ascertain the metabolic detoxification routes of genipin via CYP3A4,SULT2 A1,and UGT1 A1 in Hepa RG cells.It was found that the hepatic CYP3A4,SULT2 A1,and UGT1 A1 synergistically mediated the metabolic detoxification of genipin,and the CYP3A4 was the limited enzyme.In detail,the pivotal detoxification pathway was CYP3A4-SULT2 A1/UGT1 A1,indicating that SULT2 A1 and UGT1 A1 further catalyzed the phase II detoxification metabolism followed by the genipin metabolization by CYP3A4 to the phase I metabolites with alleviated toxicity.Our findings provided valuable cues for future studies on the detoxification of genipin,even the compatibility detoxification of Zhi-zi.Moreover,these data facilitated the development and rational administration of genipin and Zhi-zi.展开更多
基金National Natural Science Foundation of China(Grant No.82174067,81960646 and 82004080)。
文摘In the present study,we aimed to ascertain the metabolic detoxification routes of genipin via CYP3A4,SULT2 A1,and UGT1 A1 in Hepa RG cells.It was found that the hepatic CYP3A4,SULT2 A1,and UGT1 A1 synergistically mediated the metabolic detoxification of genipin,and the CYP3A4 was the limited enzyme.In detail,the pivotal detoxification pathway was CYP3A4-SULT2 A1/UGT1 A1,indicating that SULT2 A1 and UGT1 A1 further catalyzed the phase II detoxification metabolism followed by the genipin metabolization by CYP3A4 to the phase I metabolites with alleviated toxicity.Our findings provided valuable cues for future studies on the detoxification of genipin,even the compatibility detoxification of Zhi-zi.Moreover,these data facilitated the development and rational administration of genipin and Zhi-zi.
