Thyroxine (T4)/3,5,3′-Triiodo-L-Thyronine (T3) Ratio Affects the Metabolism of Anti-Colorectal Cancer Drug Irinotecan

被引：0
|
作者：
Kang, Xian-Wu [1 ]
Kong, Bin [1 ]
Chen, Qiang [1 ]
Wang, Zhuo [1 ]
Zhao, Shi-Peng [1 ]
机构：
[1] Hebei Med Univ, Hosp 3, Dept Anorectal Surg, 139 Ziqiang Rd, Shijiazhuang, Hebei, Peoples R China
来源：
LATIN AMERICAN JOURNAL OF PHARMACY | 2016年 / 35卷 / 09期
关键词：
colon cancer; glucuronidation; irinotecan; thyroxine (T4); 3,5,3 '-triiodo-L-thyronine (T3); UDP-GLUCURONOSYLTRANSFERASE UGT; MODEL; TOXICITY; THERAPY; ACIDS;
D O I：
暂无
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Colon cancer remains to threaten the health of humans, and irinotecan is the first-line drug to treat colon cancer. The in vivo metabolism of irinotecan-contains carboxylesterases (CES)-catalyzed hydrolysis reaction to form SN-38 and UDP-glucuronosyltransferase (UGT) 1A1-catalyzed glucuronidation of SN-38. The present study aims to investigate the inhibition of two important endogenous substances thyroxine (T4) and 3,5,3'-triiodo-L-thyronine (T3) on the glucuronidation of SN-38. A 235% of activity was inhibited by 100 mu M of T3, and 962% activity was inhibited by 100 uM of T4. To understand the inhibition mechanism, the inhibition of T4 on the activity of UGT1A1 was determined, and 100 mu M of T4 completely inhibited the activity of UGT1A1. In conclusion, thyroxine (T4)/3,5,3'-triiodo-L-thyronine (T3) ratio affects the metabolism of anti-colorectal cancer drug irinotecan.
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页码：2113 / 2116
页数：4
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