Evidence map›Paper›PMID 22300367›Full record

ArticleBritish journal of pharmacology2012

Pharmacokinetic interaction study of sulphasalazine in healthy subjects and the impact of curcumin as an in vivo inhibitor of BCRP.

Hiroyuki Kusuhara, Hidetoshi Furuie, Akihiro Inano, Akihiro Sunagawa, Saiko Yamada, Chunyong Wu, Shinya Fukizawa, Nozomi Morimoto, Ichiro Ieiri, Mariko Morishita and 5 more

Open access · bronzeAbstract readControlled Clinical Trial
In one paragraph

Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.

0numbers the graph read from it
0cells of the map it votes in
44citing papers in PubMed
5.4field-weighted citation impact, top 3% 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

44 citing papers in PubMed, 137 citations in OpenAlex.

  1. Trial
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  4. Curcumin Between Pleiotropic Potential and Translational Constraints.International journal of molecular sciences · 2026
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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

15 authors at 6 institutions in 1 country.

Hiroyuki KusuharaLaboratory of Molecular Pharmacokinetics, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japan.
Hidetoshi Furuie
Akihiro Inano
Akihiro Sunagawa
Saiko Yamada
Chunyong Wu
Shinya Fukizawa
Nozomi Morimoto
Ichiro Ieiri
Mariko Morishita
Kiminobu Sumita
Hiroshi Mayahara
Takuya Fujita
Kazuya Maeda
Yuichi Sugiyama
The University of Tokyo · JPHoshi University · JPOsaka Hospital · JPJapan Association for Development of Community Medicine · JPKyushu University · JPRitsumeikan University · JP

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

BACKGROUND AND PURPOSE An ATP-binding cassette (ABC) transporter, breast cancer resistance protein (BCRP)/ABCG2, limits oral bioavailability of sulphasalazine. Here we examined the effect of curcumin, the principal curcuminoid of turmeric, on oral bioavailability of microdoses and therapeutic doses of sulphasalazine in humans. EXPERIMENTAL APPROACH Effects of curcumin were measured on the ATP-dependent sulphasalazine uptake by hBCRP-expressing membrane vesicles and on oral bioavailability of sulphasalazine in wild-type and Bcrp(-/-) mice. Eight healthy Japanese subjects received an oral dose of sulphasalazine suspension (100 µg) or tablets (2 g) alone or after curcumin tablets (2 g). Uptake of sulphasalazine was studied in HEK293 cells transfected with the influx transporter (OATP)2B1. KEY RESULTS Curcumin was a potent hBCRP inhibitor in vitro (K(i) 0.70 ± 0.41 µM). Curcumin increased the area under the curve (AUC)(0-8) of plasma sulphasalazine eightfold in wild-type mice at 300 and 400 mg·kg(-1), but not in Bcrp(-/-) mice. Curcumin increased AUC(0-24) of plasma sulphasalazine 2.0-fold at microdoses and 3.2-fold at therapeutic doses in humans. Non-linearity of the dose-exposure relationship was observed between microdoses and therapeutic doses of sulphasalazine. Sulphasalazine was a substrate for OATP2B1 (K(m) 1.7 ± 0.3 µM). Its linear index (dose/K(m)) at the therapeutic dose was high and may saturate OATP2B1. CONCLUSIONS AND IMPLICATIONS Curcumin can be used to investigate effects of BCRP on oral bioavailability of drugs in humans. Besides the limited dissolution, OATP2B1 saturation is a possible mechanism underlying non-linearity in the dose-exposure relationship of sulphasalazine.

Indexed as

AnimalsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily G, Member 2Biological AvailabilityCurcuminDNA, ComplementaryFemaleHEK293 CellsHumansMaleMiceMice, KnockoutOrganic Anion TransportersSulfasalazineTransfectionAbcg2 protein, mouseATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily G, Member 2CurcuminDNA, ComplementaryOrganic Anion TransportersSLCO2B1 protein, humanSulfasalazine

Identifiers

PMID22300367
PMCPMC3402804
OpenAlexW1601512098

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.