Evidence map›Paper›PMID 35011295›Full record

ArticleMolecules (Basel, Switzerland)2021

Anti-Inflammatory Activity of a CB2 Selective Cannabinoid Receptor Agonist: Signaling and Cytokines Release in Blood Mononuclear Cells.

Antonella Capozzi, Daniela Caissutti, Vincenzo Mattei, Francesca Gado, Stefano Martellucci, Agostina Longo, Serena Recalchi, Valeria Manganelli, Gloria Riitano, Tina Garofalo and 3 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.

0numbers the graph read from it
0cells of the map it votes in
25citing papers in PubMed
2.6field-weighted citation impact, top 11% 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

25 citing papers in PubMed, 29 citations in OpenAlex.

  1. Article
  2. Review
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  4. Supercritical CONutrients · 2026
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  7. Review
  8. Article
  9. Article
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  11. Review
  12. Article
  13. Review
  14. Current and Potential Use of Biologically Active Compounds Derived fromInternational journal of molecular sciences · 2024
    Review
  15. The Elusive Truth of Cannabinoids for Rheumatic Pain.Current rheumatology reports · 2024
    Review
  16. Review
  17. Review
  18. Article
  19. Review
  20. Article
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

13 authors at 3 institutions in 1 country.

Antonella CapozziDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.
Daniela CaissuttiDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.
Vincenzo MatteiDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.ORCID 0000-0003-4677-088X
Francesca GadoDipartimento di Farmacia, Università di Pisa, 56126 Pisa, Italy.ORCID 0000-0003-2971-0834
Stefano MartellucciDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.ORCID 0000-0002-3952-3162
Agostina LongoDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.
Serena RecalchiDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.
Valeria ManganelliDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.
Gloria RiitanoDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.
Tina GarofaloDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.ORCID 0000-0003-0645-2510
Maurizio SoriceDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.
Clementina ManeraDipartimento di Farmacia, Università di Pisa, 56126 Pisa, Italy.
Roberta MisasiDipartimento di Medicina Sperimentale, Università Sapienza Roma, 00161 Rome, Italy.
Sapienza University of Rome · ITTecnologie Avanzate (Italy) · ITUniversity of Pisa · IT

Funding

National Interest Research Projects Prin 2017 2017SA5837PRA - Progetti di Ricerca di Ateneo, university of Pisa PRA_2020-2021_58
6 · The paper itself

Abstract

The endocannabinoid system (ECS) exerts immunosuppressive effects, which are mostly mediated by cannabinoid receptor 2 (CBR2), whose expression on leukocytes is higher than CBR1, mainly localized in the brain. Targeted CBR2 activation could limit inflammation, avoiding CBR1-related psychoactive effects. Herein, we evaluated in vitro the biological activity of a novel, selective and high-affinity CBR2 agonist, called JT11, studying its potential CBR2-mediated anti-inflammatory effect. Trypan Blue and MTT assays were used to test the cytotoxic and anti-proliferative effect of JT11 in Jurkat cells. Its pro-apoptotic activity was investigated analyzing both cell cycle and poly PARP cleavage. Finally, we evaluated its impact on LPS-induced ERK1/2 and NF-kB-p65 activation, TNF-α, IL-1β, IL-6 and IL-8 release in peripheral blood mononuclear cells (PBMCs) from healthy donors. Selective CB2R antagonist SR144528 and CBR2 knockdown were used to further verify the selectivity of JT11. We confirmed selective CBR2 activation by JT11. JT11 regulated cell viability and proliferation through a CBR2-dependent mechanism in Jurkat cells, exhibiting a mild pro-apoptotic activity. Finally, it reduced LPS-induced ERK1/2 and NF-kB-p65 phosphorylation and pro-inflammatory cytokines release in human PBMCs, proving to possess in vitro anti-inflammatory properties. JT11 as CBR2 ligands could enhance ECS immunoregulatory activity and our results support the view that therapeutic strategies targeting CBR2 signaling could be promising for the treatment of chronic inflammatory diseases.

Indexed as

AnimalsAnti-Inflammatory AgentsApoptosisCannabinoid Receptor AgonistsCell Line, TumorCell ProliferationCells, CulturedCell SurvivalCytokinesHumansInflammation MediatorsLeukocytes, MononuclearMitogen-Activated Protein Kinase 1Mitogen-Activated Protein Kinase 3Molecular StructurePhosphorylationAnti-Inflammatory AgentsCannabinoid Receptor AgonistsCytokinesInflammation MediatorsMAPK1 protein, humanMAPK3 protein, humanMitogen-Activated Protein Kinase 1Mitogen-Activated Protein Kinase 3Receptor, Cannabinoid, CB2anti-inflammatory activityCB2RCB2R agonistimmunomodulation

Identifiers

PMID35011295
PMCPMC8746368
OpenAlexW4200052474

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.