Evidence mapPaperPMID 39110778Full record

ArticleScience translational medicine2024

Piplartine attenuates aminoglycoside-induced TRPV1 activity and protects from hearing loss in mice.

Marisa Zallocchi, Sarath Vijayakumar, Jonathan Fleegel, Lyudmila Batalkina, Katyarina E Brunette, Dhaval Shukal, Zhiyong Chen, Olivier Devuyst, Huizhan Liu, David Z Z He and 6 more

Abstract read
In one paragraph

Article in Science translational medicine, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
field-weighted citation impact
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

7 citing papers in PubMed.

  1. Article
  2. Pharmacologic Inhibition of JAK1/2 Potentiates Aminoglycoside-Induced Ototoxicity.Otology & neurotology : official publication of the American Otological Society, American Neurotology Society [and] European Academy of Otology and Neurotology · 2026
    Article
  3. Article
  4. TRP channels in mammalian hearing loss.Frontiers in molecular neuroscience · 2025
    Review
  5. Article
  6. Review
  7. Review
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

16 authors.

Marisa ZallocchiCreighton University School of Medicine, Omaha, NE 68178, USA.
Sarath VijayakumarCreighton University School of Medicine, Omaha, NE 68178, USA.
Jonathan FleegelCreighton University School of Medicine, Omaha, NE 68178, USA.
Lyudmila BatalkinaCreighton University School of Medicine, Omaha, NE 68178, USA.
Katyarina E BrunetteCreighton University School of Medicine, Omaha, NE 68178, USA.
Dhaval Shukal
Zhiyong ChenInstitute of Physiology, University of Zürich, Zürich CH-8057, Switzerland.
Olivier DevuystInstitute of Physiology, University of Zürich, Zürich CH-8057, Switzerland.
Huizhan LiuCreighton University School of Medicine, Omaha, NE 68178, USA.
David Z Z HeCreighton University School of Medicine, Omaha, NE 68178, USA.
Ali Sajid ImamiDepartment of Neurosciences, University of Toledo, Toledo, OH 43614, USA.
Abdul-Rizaq Ali HamoudDepartment of Neurosciences, University of Toledo, Toledo, OH 43614, USA.
Robert McCullumsmithDepartment of Neurosciences, University of Toledo, Toledo, OH 43614, USA.
Martin Conda-SheridanUniversity of Nebraska Medical Center, Omaha, NE 68198, USA.
Luana Janaína De CamposUniversity of Nebraska Medical Center, Omaha, NE 68198, USA.
Jian ZuoCreighton University School of Medicine, Omaha, NE 68178, USA.

Funding

UNMC/EPPLEY CANCER CENTER SUPPORT GRANTP30CA036727 · UNIVERSITY OF NEBRASKA MEDICAL CENTER · 1985 to 2025
$11.0M
Nebraska Research Network in Functional GenomicsP20GM103427 · UNIVERSITY OF NEBRASKA MEDICAL CENTER · 2025 to 2025
$3.9M
Understanding the progression of hearing loss in an endolymphatic hydrops modelP20GM139762 · CREIGHTON UNIVERSITY · 2025 to 2025
$2.2M
Therapeutics to prevent aminoglycoside-induced hearing lossR44DC019065 · TING THERAPEUTICS, INC. · 2025 to 2025
$524k
NCI NIH HHS P30 CA036727NIDCD NIH HHS R01 DC021070NIDCD NIH HHS R43 DC019065NIDCD NIH HHS R44 DC019065NIGMS NIH HHS P20 GM103427NIGMS NIH HHS P20 GM139762
6 · The paper itself

Abstract

Hearing loss is a major health concern in our society, affecting more than 400 million people worldwide. Among the causes, aminoglycoside therapy can result in permanent hearing loss in 40% to 60% of patients receiving treatment, and despite these high numbers, no drug for preventing or treating this type of hearing loss has yet been approved by the US Food and Drug Administration. We have previously conducted high-throughput screenings of bioactive compounds, using zebrafish as our discovery platform, and identified piplartine as a potential therapeutic molecule. In the present study, we expanded this work and characterized piplartine's physicochemical and therapeutic properties. We showed that piplartine had a wide therapeutic window and neither induced nephrotoxicity in vivo in zebrafish nor interfered with aminoglycoside antibacterial activity. In addition, a fluorescence-based assay demonstrated that piplartine did not inhibit cytochrome C activity in microsomes. Coadministration of piplartine protected from kanamycin-induced hair cell loss in zebrafish and protected hearing function, outer hair cells, and presynaptic ribbons in a mouse model of kanamycin ototoxicity. Last, we investigated piplartine's mechanism of action by phospho-omics, immunoblotting, immunohistochemistry, and molecular dynamics experiments. We found an up-regulation of AKT1 signaling in the cochleas of mice cotreated with piplartine. Piplartine treatment normalized kanamycin-induced up-regulation of TRPV1 expression and modulated the gating properties of this receptor. Because aminoglycoside entrance to the inner ear is, in part, mediated by TRPV1, these results suggested that by regulating TRPV1 expression, piplartine blocked aminoglycoside's entrance, thereby preventing the long-term deleterious effects of aminoglycoside accumulation in the inner ear compartment.

Indexed as

AminoglycosidesHearing LossPiperidonesTRPV Cation ChannelsAnimalsAnimals, Genetically ModifiedFemaleMaleMiceModels, MolecularMolecular StructurePhosphorylationProtein Structure, TertiarySignal TransductionZebrafishZebrafish ProteinsAminoglycosidesPiperidonespiperlongumineTRPV1 protein, mouseTRPV1 protein, zebrafishTRPV Cation ChannelsZebrafish Proteins

Identifiers

PMID39110778
PMCPMC11392653

What Socratic holds

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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 Socratic graph.