Evidence map›Paper›PMID 27006687›Full record

ArticleChinese medicine2016

Kinetics of cytochrome P450 enzymes for metabolism of sodium tanshinone IIA sulfonate in vitro.

Dong-Sheng Ouyang, Wei-Hua Huang, Dan Chen, Wei Zhang, Zhi-Rong Tan, Jing-Bo Peng, Yi-Cheng Wang, Ying Guo, Dong-Li Hu, Jian Xiao and 1 more

Open access · goldAbstract read
In one paragraph

Article in Chinese medicine, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
3.2field-weighted citation impact, top 9% 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

4 citing papers in PubMed, 14 citations in OpenAlex.

  1. Review
  2. Pharmaceutical biology · 2020
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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

11 authors at 2 institutions in 1 country.

Dong-Sheng OuyangDepartment of Clinical Pharmacology, Xiangya Hospital, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China ; Institute of Clinical Pharmacology, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China.
Wei-Hua HuangDepartment of Clinical Pharmacology, Xiangya Hospital, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China.
Dan ChenDepartment of Clinical Pharmacology, Xiangya Hospital, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China.
Wei ZhangDepartment of Clinical Pharmacology, Xiangya Hospital, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China.
Zhi-Rong TanDepartment of Clinical Pharmacology, Xiangya Hospital, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China.
Jing-Bo PengDepartment of Clinical Pharmacology, Xiangya Hospital, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China.
Yi-Cheng WangInstitute of Clinical Pharmacology, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China.
Ying GuoInstitute of Clinical Pharmacology, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China.
Dong-Li HuInstitute of Clinical Pharmacology, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China.
Jian XiaoDepartment of Pharmacy, Xiangya Hospital, Central South University, 87 Xiangya Road, Changsha, 410008 Hunan China.
Yao ChenDepartment of Clinical Pharmacology, Xiangya Hospital, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China ; Institute of Clinical Pharmacology, Central South University, 110 Xiangya Road, Changsha, 410078 Hunan China.
Central South University · CNXiangya Hospital Central South University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundSodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA for treating cardiovascular disorders. The roles of cytochrome P450 enzymes (CYPs) in the metabolism of STS have remained unclear. This study aims to screen the main CYPs for metabolism of STS and study their interactions in vitro.

methodsSeven major CYPs were screened for metabolism of STS by human liver microsomes (HLMs) or recombinant CYP isoforms. Phenacetin (CYP1A2), coumarin (CYP2A6), tolbutamide (CYP2C9), metoprolol (CYP2D6), chlorzoxazone (CYP2E1), S-mephenytoin (CYP2C19), and midazolam (CYP3A4) were used as probe substrates to determine the potential of STS in affecting CYP-mediated phase I metabolism in humans. Enzyme kinetic studies were performed to investigate the modes of inhibition of the enzyme-substrate interactions by GraphPad Prism Enzyme Kinetic 5 Demo software.

resultsSodium tanshinone IIA sulfonate inhibited the activity of CYP3A4 in a dose-dependent manner by the HLMs and CYP3A4 isoform. The K m and V max values of STS were 54.8 ± 14.6 µM and 0.9 ± 0.1 nmol/mg protein/min, respectively, for the HLMs and 7.5 ± 1.4 µM and 6.8 ± 0.3 nmol/nmol P450/min, respectively, for CYP3A4. CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, and CYP2C19 showed minimal or no effects on the metabolism of STS.

conclusionThis in vitro study showed that STS mainly inhibited the activities of CYP3A4.

Identifiers

PMID27006687
PMCPMC4802617
OpenAlexW2312010870

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Registered trials

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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.