Tissue and species differences in the glucuronidation of glabridin with UDP-glucuronosyltransferases
文献类型：期刊论文
| 作者 | Guo, Bin1,3,4; Fang, Zhongze2,3,4; Yang, Lu3,4; Xiao, Ling5; Xia, Yangliu6; Gonzalez, Frank J.7; Zhu, Liangliang5; Cao, Yunfeng3,4,8; Ge, Guangbo6; Yang, Ling6 |
| 刊名 | chemico-biological interactions
 |
| 出版日期 | 2015-04-25 |
| 卷号 | 231页码:90-97 |
| 关键词 | Glabridin Glucuronidation UDP-glucuronosyltransferases Species differences |
| 英文摘要 | glabridin (ga) has gained wide application in the cosmetics and food industry. this study was performed to investigate its metabolic inactivation and elimination by glucuronidation by use of liver and intestine microsomes from humans (hlm and him) and rats (rlm and rim), and liver microsomes from cynomolgus monkeys and beagle dogs (cylm and dlm). both hydroxyl groups at the c2 and c4 positions of the b ring are conjugated to generate two mono-glucuronides (m1 and m2). him, rim and rlm showed the most robust activity in catalyzing m2 formation with intrinsic clearance values (cl-int) above 2000 mu l/min/mg, with little measurable m1 formation activity. dlm displayed considerable activity both in m1 and m2 formation, with cl-int values of 71 and 214 mu l/min/mg, respectively, while hlm and cylm exhibited low activities in catalyzing m1 and m2 formation, with cl-int values all below 20 mu l/min/mg. it is revealed that ugt1a1, 1a3, 1a9, 2b7, 2b15 and extrahepatic ugt1a8 and 1a10 are involved in ga glucuronidation. nearly all ugts preferred m2 formation except for ugt1a1. notably, ugt1a8 displayed the highest activity with a cl-int value more than 5-fold higher than the other isoforms. chemical inhibition studies, using selective inhibitors of ugt1a1, 1a9, 2b7 and 1a8, further revealed that ugt1a8 contributed significantly to intestinal ga glucuronidation in humans. in summary, this in vitro study demonstrated large species differences in ga glucuronidation by liver and intestinal microsomes, and that intestinal ugts are important for the pathway in humans. (c) 2015 elsevier ireland ltd. all rights reserved. |
| WOS标题词 | science & technology ; life sciences & biomedicine |
| 类目[WOS] | biochemistry & molecular biology ; pharmacology & pharmacy ; toxicology |
| 研究领域[WOS] | biochemistry & molecular biology ; pharmacology & pharmacy ; toxicology |
| 关键词[WOS] | tandem mass-spectrometry ; messenger-rna expression ; isoflavan glabridin ; cynomolgus monkey ; 1a isoforms ; inhibition ; enzymes ; liver ; selectivity ; absorption |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000353741100011 |
| 公开日期 | 2016-05-09 |
| 源URL | [http://cas-ir.dicp.ac.cn/handle/321008/146227]  |
| 专题 | 大连化学物理研究所_中国科学院大连化学物理研究所 |
| 作者单位 | 1.Liaoning Med Univ, Affiliated Hosp 1, Jinzhou, Peoples R China 2.Tianjin Med Univ, Sch Publ Hlth, Dept Toxicol, Tianjin, Peoples R China 3.Chinese Acad Sci, Dalian Inst Chem Phys, Joint Ctr Translat Med, Dalian, Peoples R China 4.Liaoning Med Univ, Affiliated Hosp 1, Dalian, Peoples R China 5.Anqing Normal Univ, Sch Life Sci, Ctr Drug & Food Safety Evaluat, Anqing 246011, Peoples R China 6.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian, Peoples R China 7.NCI, Lab Metab, Ctr Canc Res, NIH, Bethesda, MD 20892 USA 8.Shanghai Inst Planned Parenthood Res, Shanghai Engineer & Technol Res Ctr Reprod Hlth D, Key Lab Contracept & Devices Res NPFPC, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Guo, Bin,Fang, Zhongze,Yang, Lu,et al. Tissue and species differences in the glucuronidation of glabridin with UDP-glucuronosyltransferases[J]. chemico-biological interactions,2015,231:90-97. |
| APA | Guo, Bin.,Fang, Zhongze.,Yang, Lu.,Xiao, Ling.,Xia, Yangliu.,...&Sun, Hongzhi.(2015).Tissue and species differences in the glucuronidation of glabridin with UDP-glucuronosyltransferases.chemico-biological interactions,231,90-97. |
| MLA | Guo, Bin,et al."Tissue and species differences in the glucuronidation of glabridin with UDP-glucuronosyltransferases".chemico-biological interactions 231(2015):90-97. |
入库方式： OAI收割
来源：大连化学物理研究所
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