Assessment of the inhibition potential of Licochalcone A against human UDP-glucuronosyltransferases

Hong, Xin; Qi, Xiaoyi; Wu, Jingjing; Wang, Xinxin; Li, Yan; Hong, James Y.; He, Wei; Xu, Wei; Ge, Guang-Bo; Yang, Ling

doi:10.1016/j.fct.2016.02.007

Cited by 48 publications

(32 citation statements)

References 66 publications

(74 reference statements)

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“…55 It should be noted that some previous investigations have revealed that licorice constituents can affect the pharmacokinetic behaviour of some therapeutic drugs via inhibiting the hepatic drug metabolizing enzymes (cytochrome P450 enzymes and UDP-glucuronosyltransferases). [56][57][58] In this study, our results demonstrate that thrombin activity can be inhibited by the chalcones in licorice. Therefore, it is conceivable that both pharmacokinetic and pharmacodynamics interactions may occur when anticoagulant or antiplatelet drugs are used in combination with licorice-containing products.…”

Section: Discussionsupporting

confidence: 58%

Inhibition of human thrombin by the constituents of licorice: inhibition kinetics and mechanistic insights through in vitro and in silico studies

et al. 2020

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Section: Discussionsupporting

confidence: 58%

Inhibition of human thrombin by the constituents of licorice: inhibition kinetics and mechanistic insights through in vitro and in silico studies

et al. 2020

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“…, indinavir, nilotinib and sorafenib) or herbal extracts (such as milk thistle, green tea and psoralea corylifolia), as well as several natural compounds in herbs or foods (such as amentoflavone, licochalcone A and emodin) are potent UGT1A1 inhibitors, which could significantly inhibit their activities and lead to undesirable effects 17. , 18. , 19.…”

Section: Introductionmentioning

confidence: 99%

Recent progress and challenges in screening and characterization of UGT1A1 inhibitors

Xia

Finel

et al. 2019

Acta Pharmaceutica Sinica B

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Uridine-diphosphate glucuronosyltransferase 1A1 (UGT1A1) is an important conjugative enzyme in mammals that is responsible for the conjugation and detoxification of both endogenous and xenobiotic compounds. Strong inhibition of UGT1A1 may trigger adverse drug/herb–drug interactions, or result in metabolic disorders of endobiotic metabolism. Therefore, both the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have recommended assaying the inhibitory potential of drugs under development on the human UGT1A1 prior to approval. This review focuses on the significance, progress and challenges in discovery and characterization of UGT1A1 inhibitors. Recent advances in the development of UGT1A1 probes and their application for screening UGT1A1 inhibitors are summarized and discussed in this review for the first time. Furthermore, a long list of UGT1A1 inhibitors, including information on their inhibition potency, inhibition mode, and affinity, has been prepared and analyzed. Challenges and future directions in this field are highlighted in the final section. The information and knowledge that are presented in this review provide guidance for rational use of drugs/herbs in order to avoid the occurrence of adverse effects via UGT1A1 inhibition, as well as presenting methods for rapid screening and characterization of UGT1A1 inhibitors and for facilitating investigations on UGT1A1—ligand interactions.

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“…Potent inhibition of UGT1A1 may result in partial or complete loss of UGT1A1 activity, and then increase the exposure of bilirubin and other endogenous (e.g., steroid hormones and bile acids) and xenobiotics (e.g., drugs, chemical carcinogens, and environmental pollutants), which may lead to a series of undesirable effects including jaundice, liver dysfunction and carcinogenesis. Several studies show that tolcapone, entacapone, licochalcone A, fructus psoraleae, amentoflavone displayed strong inhibitory effects on human UGT1A1 [1,[18][19][20]. These findings provide a deep understanding of potential drug interactions between above mentioned drugs and UGT1A1 substrates via UGT1A1 inhibition, and will be helpful for guiding reasonable applications of above mentioned drugs and its related medical preparations in the future.…”

Section: Discussionmentioning

confidence: 78%

Molecular probes for identification of UDP-glucuronosyltransferase 1 gene polymorphisms for Gilbert's syndrome diagnosis

Wu¹,

Zhou²,

Song³

et al. 2018

biomedicalresearch

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The T-3279G mutation in Phenobarbital Responsive Enhancer Modulein (PBREM), TA-insertion in the TATA box, creating the A(TA)7TAA motif instead of the A(TA)6TAA, and G211A mutation in coding exon 1, particularly in Asians, of human UGT1A1 (UDP-glucoronosyltransferase) gene are the three common polymorphisms of Gilbert's syndrome. This article employed dot blot hybridization to detect the T-3279G, A(TA)6/7TAA and G211A mutation of UGT1A1 gene in 15 patients. In the dot blot hybridization assay, PCR products were denatured and spotted on positively charged nylon membranes instead of acrylamide-modified slides. Then three pairs of probes were labeled by digoxigenin and hybridized with the spotted array. After hybridization, the signal was visualized using TMB color development solution and all possible polymorphisms of the T-3279G, A(TA)6/7TAA and G211A in 15 Chinese patients with hyperbilirubinemia were successfully identified. The results of 15 samples by dotblot hybridization were consistent with the sequencing results. The data showed that dot blot hybridization assay is a quick and low cost method to detect UGT1A1 gene polymorphisms and helpful to diagnosis of Gilbert's syndrome.

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Assessment of the inhibition potential of Licochalcone A against human UDP-glucuronosyltransferases

Cited by 48 publications

References 66 publications

Inhibition of human thrombin by the constituents of licorice: inhibition kinetics and mechanistic insights through in vitro and in silico studies

Inhibition of human thrombin by the constituents of licorice: inhibition kinetics and mechanistic insights through in vitro and in silico studies

Recent progress and challenges in screening and characterization of UGT1A1 inhibitors

Molecular probes for identification of UDP-glucuronosyltransferase 1 gene polymorphisms for Gilbert's syndrome diagnosis

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