Licochalcone A displays potent and broad-spectrum inhibition on human UDP-glucuronosyltransferases

来源 :2015年第一届药代动力学朝阳论坛 | 被引量 : 0次 | 上传用户:clhhjq
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
  Licochalcone A (LCA), a major bioactive compound isolated from the roots of Glycyrrhiza glabra, displays multiple bioactivities, such as anti-parasitic, anti-inflammatory and anti-cancer.The aim of the present study is to evaluate the inhibitory effects of LCA on human UDP-glucuronosyltransferases (UGTs).The human recombinant UGT isoforms were used as enzyme source, and a nonspecific substrate 4-methylumbelliferone (4-MU) was ultilized as probe sbustrate.Our results demonstrated that LCA displayed strong inhibitory effects towards UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A9 and 2B7 (0.09μmol/L ≤ IC50 ≤ 6.12 μmol/L), and moderate inhibitory effects towards UGT1A8, 1A10, 2B4, 2B15 and 2B17 (IC50 =20.16, 18.01, 24.22, 12.95 and 31.92 μ mol/L, respectively).
其他文献
  Triptolide, which is separated from Tripterygium wilfordii Hook F, has a wide range of pharmacological activities.Han et al reported that CYP2E1, 1A2, 3A1 a
会议
  Pyrrolizidine alkaloids (PAs) are a kind of hepatotoxic alkaloids, which widely exist in plants.Cytochrome P450 (CYP) 3A mediates metabolic activation of PA
会议
  Licochalcone A (LCA) is a major bioactive compound isolated from traditional Chinese medicine liquorice which possesses multiple pharmacological effects inc
会议
  Compared to traditional cytotoxic agents, gefitinib, an orally available EGFR tyrosine kinase inhibitors, can prolong survival of NSCLC patients and cause f
会议
  Carboxylesterases (CEs) catalyze hydrolytic and transesterification reactions with a vast number of endogenous and exogenous substrates including fatty acid
会议
  Stem-cell fate in the plant of Arabidopsis thaliana is controlled by a complex regulatory network of signaling molecules and transcription factors.The class
  A canthopanax senticosus (AS) Harms is distributed widely in regions such as the Heilongjiang, Jilin Province of the People's Republic of China, the norther
会议
  Catechol-O-methyltransferase (COMT), one of the phase Ⅱ metabolizing enzymes, plays important roles in the metabolsim of endogenous and xenobiotic catechol
会议
  Current antidepressant paroxetine therapies have an unsatisfactorily high failure rate with up to 60% of depressed patients suffering from treatment-resista
会议
  EPG5 was identified as essential for autophagy in a genetic screen in Caenorhabdis elegans.Subsequently, a human disease, called Vici syndrome, characterize
会议