Evidence map›Paper›PMID 21649640›Full record

ArticleBritish journal of pharmacology2011

Scoparone potentiates transactivation of the bile salt export pump gene and this effect is enhanced by cytochrome P450 metabolism but abolished by a PKC inhibitor.

Dongfang Yang, Jian Yang, Deshi Shi, Ruitang Deng, Bingfang Yan

Open access · greenAbstract read
In one paragraph

Article in British journal of pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
1.7field-weighted citation impact, top 16% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

19 citing papers in PubMed, 40 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Review
  6. Frontiers in endocrinology · 2021
    Review
  7. Regulation of Cytochrome P450 2a5 byFrontiers in pharmacology · 2021
    Article
  8. Article
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

5 authors at 1 institution in 1 country.

Dongfang YangDepartment of Biomedical Sciences, Center for Pharmacogenomics and Molecular Therapy, University of Rhode Island, Kingston, RI 02881, USA.
Jian Yang
Deshi Shi
Ruitang Deng
Bingfang Yan
University of Rhode Island · US

Funding

Signaling of the Pregnane X ReceptorR01GM061988 · NIGMS · UNIVERSITY OF RHODE ISLAND · PI DENG, RUITANG · 2000 to 2016
$3.0M
Crosstalk between estrogen and bile acid signaling pathwayR01DK087755 · NIDDK · UNIVERSITY OF RHODE ISLAND · PI DENG, RUITANG · 2010 to 2014
$1.4M
Molecular Toxicology of CarboxylesterasesR01ES007965 · NIEHS · UNIVERSITY OF RHODE ISLAND · PI YAN, BINGFANG · 2003 to 2006
$1.2M
Transcription Activation-Based Herb-Drug InteractionsF05AT003019 · NCCIH · UNIVERSITY OF RHODE ISLAND · PI YANG, JIAN · 2005 to 2009
$247k
NCCIH NIH HHS F05 AT003019NCCIH NIH HHS F05AT003019NCRR NIH HHS P20RR01645NIDDK NIH HHS R01 DK087755NIDDK NIH HHS R01DK087755NIEHS NIH HHS R01 ES007965NIEHS NIH HHS R01ES07965NIGMS NIH HHS R01 GM061988NIGMS NIH HHS R01GM61988
6 · The paper itself

Abstract

background and purposeHyperbilirubinaemia and cholestasis are two major forms of liver abnormality. The Chinese herb Yin Chin has been used for thousands of years to treat liver dysfunctions. In mice, this herb and its principal ingredient scoparone were found to accelerate the clearance of bilirubin accompanied by the induction of uridine diphosphate-5'-glucuronosyltransferase-1A1 (UGT1A1), a bilirubin processing enzyme. The aim of this study was to determine whether scoparone induces the expression of human UGT1A1. In addition, the expression of the bile salt export pump (BSEP), a transporter of bile acids, was determined. EXPERIMENTAL APPROACH: Primary human hepatocytes and hepatoma line Huh7 were treated with scoparone, chenodeoxycholic acid (CDCA) or both. The expression of UGT1A1 and BSEP mRNA was determined. The activation of the human BSEP promoter reporter by scoparone was determined in Huh7 cells by transient transfection and in mice by bioluminescent imaging. The metabolism of scoparone was investigated by recombinant CYP enzymes and pooled human liver microsomes. KEY

resultsScoparone did not enhance the expression of either human BSEP or, surprisingly, UGT1A1. However, scoparone significantly potentiated the expression of BSEP induced by CDCA. Consistent with this, scoparone potentiated the stimulant effect of CDCA on the human BSEP promoter. This potentiation was enhanced by co-transfection of cytochrome P4501A2 but abolished by the PKC inhibitor GF109203X. CONCLUSIONS AND IMPLICATIONS: Scoparone and Yin Chin normalize liver function primarily by enhancing the secretion of bile acids, and this effect probably varies depending on the metabolic rate of scoparone.

Indexed as

AnimalsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily B, Member 11Blotting, WesternCell Line, TumorCholagogues and CholereticsCoumarinsCytochrome P-450 CYP1A2Cytochrome P-450 Enzyme SystemDrug SynergismGenes, ReporterGlucuronosyltransferaseHepatocytesHumansMiceMicrosomes, LiverABCB11 protein, humanAbcb11 protein, mouseATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily B, Member 11Cholagogues and CholereticsCoumarinsCYP1A2 protein, humanCytochrome P-450 CYP1A2Cytochrome P-450 Enzyme SystemGlucuronosyltransferaseProtein Kinase InhibitorsscoparoneUGT1A1 Enzyme

Identifiers

PMID21649640
PMCPMC3221107
OpenAlexW1743171185

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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.