Evidence map›Paper›PMID 38766819›Full record

ArticleCurrent computer-aided drug design2025

Flavonoids and Organic Acids Affect Phase II Metabolism based on the Regulation of UGT1A1 Expression and Function.

Lin Zhang, Xuerong Zhang, Caiyan Wang

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Article in Current computer-aided drug design, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

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2citing papers in PubMed
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1 · What the graph read from it

What it found

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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

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3 · Its place in the literature

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2 citing papers in PubMed.

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4 · The record

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5 · Who and what money

Authors and funding

3 authors.

Lin ZhangState Key Laboratory of Traditional Chinese Medicine Syndrome, International Institute for Translational Chinese, Guangzhou University of Chinese Medicine, Guangzhou, 510006, China.ORCID 0000-0001-8021-3003
Xuerong ZhangState Key Laboratory of Traditional Chinese Medicine Syndrome, International Institute for Translational Chinese, Guangzhou University of Chinese Medicine, Guangzhou, 510006, China.
Caiyan WangState Key Laboratory of Traditional Chinese Medicine Syndrome, International Institute for Translational Chinese, Guangzhou University of Chinese Medicine, Guangzhou, 510006, China.

Funding

National Natural Science Foundation of China 81930114, 82322074Research Foundation of Education Bureau of Guangdong Province 2022ZDZX2010Science and Technology Program of Guangzhou 202201011420
6 · The paper itself

Abstract

backgroundExogenous substances modulate metabolism by regulating the expression and function of UDP-glycosyltransferases (UGTs). However, the exact mechanism in the intestine was rarely understood. Herein, we explored the effects of representative flavonoids and organic acids on the regulation of UGT1A1.

methodsMTT assays and western blot analysis were used to explore the effect of polyphenols. X-ray diffraction was used to reveal the catalytic mechanisms of UGTs.

resultsMTT assays showed that these compounds basically had almost no cytotoxicity, even in concentrations up to 200 μM. However, through western blot assays, UGT1A1 expression was increased after being treated with liquiritigenin and caffeic acid. Furthermore, liquiritigenin and caffeic acid enhanced the nuclear translocation of Nrf2. Moreover, a 2.5-Å crystal structure of the complex containing UGTs C-terminal domain and organic acid was solved, and the UDPGA binding pocket could be occupied by organic acid, suggesting the enzyme activity might be impaired by organic acid.

conclusionAbove all, liquiritigenin and caffeic acid maintained the metabolism balance by upregulating the expression of UGT1A1 via Nrf2 activation and inhibiting the enzyme activity in Caco-2 cells.

Indexed as

Caffeic AcidsFlavanonesFlavonoidsGlucuronosyltransferaseCaco-2 CellsHumansNF-E2-Related Factor 2caffeic acidCaffeic AcidsFlavanonesFlavonoidsGlucuronosyltransferaseliquiritigeninNFE2L2 protein, humanNF-E2-Related Factor 2Crystal structureflavonoids.mechanismNrf2polyphenolsUGTs

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.