Guo Xiao, Cao Xuedan, Fang Xiugui, Guo Ailing, Li Erhu
College of Food Science and Technology, Huazhong Agricultural University, Wuhan, China.
Zhejiang Citrus Research Institute, Zhejiang Academy of Agricultural Sciences, Taizhou, China.
Int J Food Sci Nutr. 2022 Jun;73(4):480-490. doi: 10.1080/09637486.2021.2012562. Epub 2022 Jan 2.
This study examined the effects of phase II metabolism and efflux transportation on the bioavailability of naringin, hesperidin, and their aglycones (naringenin and hesperetin) in rats. Results indicated naringin and hesperidin have a lower oral bioavailability than their aglycones. Of all the phase II enzymes tested, UDP-glucuronosyltransferase (UGT) 1A1, UGT1A2, UGT1A3, UGT1A7 and SULT sulfotransferase (SULT) 1B1 were of minor importance regarding the phase II metabolism of naringenin and hesperetin in the small intestine. Naringin, hesperidin, and their aglycones were all extensively metabolised in the liver. Naringin and hesperidin were more extensively transported by efflux transporters compared to their aglycones. Significant correlations between phase II enzymes and efflux transporters were detected. In conclusion, more extensive metabolism of naringin and hesperidin than their aglycones in the small intestine, and the interplay of phase II enzymes and efflux transporters in the small intestine explain the lower relative oral bioavailability of naringin and hesperidin than their aglycones.
本研究考察了Ⅱ相代谢和外排转运对大鼠体内柚皮苷、橙皮苷及其苷元（柚皮素和橙皮素）生物利用度的影响。结果表明，柚皮苷和橙皮苷的口服生物利用度低于其苷元。在所有测试的Ⅱ相酶中，尿苷二磷酸葡萄糖醛酸基转移酶（UGT）1A1、UGT1A2、UGT1A3、UGT1A7和磺基转移酶（SULT）1B1在小肠中对柚皮素和橙皮素的Ⅱ相代谢作用较小。柚皮苷、橙皮苷及其苷元在肝脏中均被广泛代谢。与它们的苷元相比，柚皮苷和橙皮苷被外排转运体转运的程度更高。检测到Ⅱ相酶与外排转运体之间存在显著相关性。总之，柚皮苷和橙皮苷在小肠中的代谢比其苷元更广泛，以及小肠中Ⅱ相酶和外排转运体的相互作用解释了柚皮苷和橙皮苷相对于其苷元较低的口服生物利用度。
