Evidence map›Paper›PMID 27277973›Full record

ArticleScientific reports2016

Pharmacological exploitation of the phenothiazine antipsychotics to develop novel antitumor agents-A drug repurposing strategy.

Chia-Hsien Wu, Li-Yuan Bai, Ming-Hsui Tsai, Po-Chen Chu, Chang-Fang Chiu, Michael Yuanchien Chen, Shih-Jiuan Chiu, Jo-Hua Chiang, Jing-Ru Weng

Open access · goldAbstract read
In one paragraph

Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
43citing papers in PubMed, 1 pooled it
4.7field-weighted citation impact, top 5% 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

43 citing papers in PubMed, 1 synthesis or guideline pooled it, 88 citations in OpenAlex.

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  15. Anti-glioblastoma activity of monensin and its analogs in an organoid model of cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2022
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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

9 authors at 5 institutions in 1 country.

Chia-Hsien WuInstitute of Biological Chemistry, Academia Sinica, Taipei 115, Taiwan.
Li-Yuan BaiCollege of Medicine, China Medical University, Taichung 404, Taiwan.
Ming-Hsui TsaiGraduate Institute of Clinical Medical Science, China Medical University, Taichung 404, Taiwan.
Po-Chen ChuInstitute of Biological Chemistry, Academia Sinica, Taipei 115, Taiwan.
Chang-Fang ChiuDivision of Hematology and Oncology, Department of Internal Medicine, China Medical University Hospital, Taichung 404, Taiwan.
Michael Yuanchien ChenDepartment of Oral &Maxillofacial Surgery, China Medical University Hospital, Taichung 404, Taiwan.
Shih-Jiuan ChiuSchool of Pharmacy, Taipei Medical University, Taipei 110, Taiwan.
Jo-Hua ChiangDepartment of Biological Science and Technology, China Medical University, Taichung 404, Taiwan.
Jing-Ru WengDepartment of Biological Science and Technology, China Medical University, Taichung 404, Taiwan.
China Medical University · TWChina Medical University Hospital · TWInstitute of Biological Chemistry, Academia Sinica · TWNational Cheng Kung University · TWTaipei Medical University · TW

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Phenothiazines (PTZs) have been used for the antipsychotic drugs for centuries. However, some of these PTZs have been reported to exhibit antitumor effects by targeting various signaling pathways in vitro and in vivo. Thus, this study was aimed at exploiting trifluoperazine, one of PTZs, to develop potent antitumor agents. This effort culminated in A4 [10-(3-(piperazin-1-yl)propyl)-2-(trifluoromethyl)-10H-phenothiazine] which exhibited multi-fold higher apoptosis-inducing activity than the parent compound in oral cancer cells. Compared to trifluoperazine, A4 demonstrated similar regulation on the phosphorylation or expression of multiple molecular targets including Akt, p38, and ERK. In addition, A4 induced autophagy, as evidenced by increased expression of the autophagy biomarkers LC3B-II and Atg5, and autophagosomes formation. The antitumor activity of A4 also related to production of reactive oxygen species and adenosine monophosphate-activated protein kinase. Importantly, the antitumor utility of A4 was extended in vivo as it, administrated at 10 and 20 mg/kg intraperitoneally, suppressed the growth of Ca922 xenograft tumors. In conclusion, the ability of A4 to target diverse aspects of cancer cell growth suggests its value in oral cancer therapy.

Indexed as

Drug RepositioningAnimalsAntineoplastic AgentsAntipsychotic AgentsApoptosisBiomarkers, TumorCell Line, TumorCell ProliferationCell SurvivalDNA DamageGene Expression Regulation, NeoplasticHumansInhibitory Concentration 50MaleMiceMice, NudeAntineoplastic AgentsAntipsychotic AgentsBiomarkers, TumorPhenothiazinesReactive Oxygen Species

Identifiers

PMID27277973
PMCPMC4899727
OpenAlexW2418617791

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.