Selective induction of apoptosis in T-cell acute lymphoblastic leukemia by pristimerin through dual PI3K/AKT pathway inhibition and ROS generation

<p>T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematological malignancy characterized by the aberrant activation of survival pathways, particularly the PI3K/AKT axis. Pristimerin (Prist), a naturally occurring quinonemethide triterpenoid, has recently gained attention for its...

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التفاصيل البيبلوغرافية
المؤلف الرئيسي: Shilpa Kuttikrishnan (3520079) (author)
مؤلفون آخرون: Zahwa Mariyam (22504034) (author), Fareed Ahmad (134672) (author), Mohammad Suleman (22927387) (author), Ummu Habeeba (22504037) (author), Anu J. Panicker (22927390) (author), Kirti S. Prabhu (4246144) (author), Maysaloun Merhi (4246147) (author), Said Dermime (79420) (author), Ammira S. Al Shabeeb Akil (22155844) (author), Ajaz A. Bhat (12984701) (author), Abdul W. Ansari (14557391) (author), Shahab Uddin (154400) (author)
منشور في: 2025
الموضوعات:
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_version_ 1864513531528871936
author Shilpa Kuttikrishnan (3520079)
author2 Zahwa Mariyam (22504034)
Fareed Ahmad (134672)
Mohammad Suleman (22927387)
Ummu Habeeba (22504037)
Anu J. Panicker (22927390)
Kirti S. Prabhu (4246144)
Maysaloun Merhi (4246147)
Said Dermime (79420)
Ammira S. Al Shabeeb Akil (22155844)
Ajaz A. Bhat (12984701)
Abdul W. Ansari (14557391)
Shahab Uddin (154400)
author2_role author
author
author
author
author
author
author
author
author
author
author
author
author_facet Shilpa Kuttikrishnan (3520079)
Zahwa Mariyam (22504034)
Fareed Ahmad (134672)
Mohammad Suleman (22927387)
Ummu Habeeba (22504037)
Anu J. Panicker (22927390)
Kirti S. Prabhu (4246144)
Maysaloun Merhi (4246147)
Said Dermime (79420)
Ammira S. Al Shabeeb Akil (22155844)
Ajaz A. Bhat (12984701)
Abdul W. Ansari (14557391)
Shahab Uddin (154400)
author_role author
dc.creator.none.fl_str_mv Shilpa Kuttikrishnan (3520079)
Zahwa Mariyam (22504034)
Fareed Ahmad (134672)
Mohammad Suleman (22927387)
Ummu Habeeba (22504037)
Anu J. Panicker (22927390)
Kirti S. Prabhu (4246144)
Maysaloun Merhi (4246147)
Said Dermime (79420)
Ammira S. Al Shabeeb Akil (22155844)
Ajaz A. Bhat (12984701)
Abdul W. Ansari (14557391)
Shahab Uddin (154400)
dc.date.none.fl_str_mv 2025-11-08T09:00:00Z
dc.identifier.none.fl_str_mv 10.1016/j.ejphar.2025.178329
dc.relation.none.fl_str_mv https://figshare.com/articles/journal_contribution/Selective_induction_of_apoptosis_in_T-cell_acute_lymphoblastic_leukemia_by_pristimerin_through_dual_PI3K_AKT_pathway_inhibition_and_ROS_generation/30970681
dc.rights.none.fl_str_mv CC BY 4.0
info:eu-repo/semantics/openAccess
dc.subject.none.fl_str_mv Biomedical and clinical sciences
Immunology
Oncology and carcinogenesis
Pharmacology and pharmaceutical sciences
PristimerinT-cell acute lymphoblastic leukemia
PI3K/AKT signaling pathway
Apoptosis
Cell cycle arrest
Molecular docking
dc.title.none.fl_str_mv Selective induction of apoptosis in T-cell acute lymphoblastic leukemia by pristimerin through dual PI3K/AKT pathway inhibition and ROS generation
dc.type.none.fl_str_mv Text
Journal contribution
info:eu-repo/semantics/publishedVersion
text
contribution to journal
description <p>T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematological malignancy characterized by the aberrant activation of survival pathways, particularly the PI3K/AKT axis. Pristimerin (Prist), a naturally occurring quinonemethide triterpenoid, has recently gained attention for its anti-cancer potential. In this study, we demonstrate that Prist effectively inhibits the proliferation of T-ALL cell lines (Jurkat and Molt 4) by inducing G0/G1 cell cycle arrest and triggering intrinsic and extrinsic caspase-dependent apoptosis. Prist significantly increases reactive oxygen species (ROS) levels and depletes glutathione (GSH), leading to mitochondrial dysfunction and cytochrome c release. Notably, ROS scavenging with N-acetylcysteine (NAC) abrogated Prist-induced apoptosis, highlighting ROS as a critical mediator of its cytotoxicity. Network pharmacology and molecular docking revealed AKT as a key target of Prist, with strong binding affinity confirmed through docking analysis. Prist downregulated phosphorylated AKT and inhibitor of apoptosis proteins (XIAP, cIAP1/2), supporting its pro-apoptotic mechanism. Importantly, Prist inhibited the proliferation and AKT phosphorylation in activated primary human T cells but spared resting T cells, indicating selective cytotoxicity. These findings establish Prist as a promising therapeutic candidate for T-ALL through the selective targeting of PI3K/AKT-driven survival signaling.</p><h2>Other Information</h2> <p> Published in: European Journal of Pharmacology<br> License: <a href="http://creativecommons.org/licenses/by/4.0/" target="_blank">http://creativecommons.org/licenses/by/4.0/</a><br>See article on publisher's website: <a href="https://dx.doi.org/10.1016/j.ejphar.2025.178329" target="_blank">https://dx.doi.org/10.1016/j.ejphar.2025.178329</a></p>
eu_rights_str_mv openAccess
id Manara2_01ffa1da65c0169515cd74f2479938be
identifier_str_mv 10.1016/j.ejphar.2025.178329
network_acronym_str Manara2
network_name_str Manara2
oai_identifier_str oai:figshare.com:article/30970681
publishDate 2025
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repository.name.fl_str_mv
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rights_invalid_str_mv CC BY 4.0
spelling Selective induction of apoptosis in T-cell acute lymphoblastic leukemia by pristimerin through dual PI3K/AKT pathway inhibition and ROS generationShilpa Kuttikrishnan (3520079)Zahwa Mariyam (22504034)Fareed Ahmad (134672)Mohammad Suleman (22927387)Ummu Habeeba (22504037)Anu J. Panicker (22927390)Kirti S. Prabhu (4246144)Maysaloun Merhi (4246147)Said Dermime (79420)Ammira S. Al Shabeeb Akil (22155844)Ajaz A. Bhat (12984701)Abdul W. Ansari (14557391)Shahab Uddin (154400)Biomedical and clinical sciencesImmunologyOncology and carcinogenesisPharmacology and pharmaceutical sciencesPristimerinT-cell acute lymphoblastic leukemiaPI3K/AKT signaling pathwayApoptosisCell cycle arrestMolecular docking<p>T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematological malignancy characterized by the aberrant activation of survival pathways, particularly the PI3K/AKT axis. Pristimerin (Prist), a naturally occurring quinonemethide triterpenoid, has recently gained attention for its anti-cancer potential. In this study, we demonstrate that Prist effectively inhibits the proliferation of T-ALL cell lines (Jurkat and Molt 4) by inducing G0/G1 cell cycle arrest and triggering intrinsic and extrinsic caspase-dependent apoptosis. Prist significantly increases reactive oxygen species (ROS) levels and depletes glutathione (GSH), leading to mitochondrial dysfunction and cytochrome c release. Notably, ROS scavenging with N-acetylcysteine (NAC) abrogated Prist-induced apoptosis, highlighting ROS as a critical mediator of its cytotoxicity. Network pharmacology and molecular docking revealed AKT as a key target of Prist, with strong binding affinity confirmed through docking analysis. Prist downregulated phosphorylated AKT and inhibitor of apoptosis proteins (XIAP, cIAP1/2), supporting its pro-apoptotic mechanism. Importantly, Prist inhibited the proliferation and AKT phosphorylation in activated primary human T cells but spared resting T cells, indicating selective cytotoxicity. These findings establish Prist as a promising therapeutic candidate for T-ALL through the selective targeting of PI3K/AKT-driven survival signaling.</p><h2>Other Information</h2> <p> Published in: European Journal of Pharmacology<br> License: <a href="http://creativecommons.org/licenses/by/4.0/" target="_blank">http://creativecommons.org/licenses/by/4.0/</a><br>See article on publisher's website: <a href="https://dx.doi.org/10.1016/j.ejphar.2025.178329" target="_blank">https://dx.doi.org/10.1016/j.ejphar.2025.178329</a></p>2025-11-08T09:00:00ZTextJournal contributioninfo:eu-repo/semantics/publishedVersiontextcontribution to journal10.1016/j.ejphar.2025.178329https://figshare.com/articles/journal_contribution/Selective_induction_of_apoptosis_in_T-cell_acute_lymphoblastic_leukemia_by_pristimerin_through_dual_PI3K_AKT_pathway_inhibition_and_ROS_generation/30970681CC BY 4.0info:eu-repo/semantics/openAccessoai:figshare.com:article/309706812025-11-08T09:00:00Z
spellingShingle Selective induction of apoptosis in T-cell acute lymphoblastic leukemia by pristimerin through dual PI3K/AKT pathway inhibition and ROS generation
Shilpa Kuttikrishnan (3520079)
Biomedical and clinical sciences
Immunology
Oncology and carcinogenesis
Pharmacology and pharmaceutical sciences
PristimerinT-cell acute lymphoblastic leukemia
PI3K/AKT signaling pathway
Apoptosis
Cell cycle arrest
Molecular docking
status_str publishedVersion
title Selective induction of apoptosis in T-cell acute lymphoblastic leukemia by pristimerin through dual PI3K/AKT pathway inhibition and ROS generation
title_full Selective induction of apoptosis in T-cell acute lymphoblastic leukemia by pristimerin through dual PI3K/AKT pathway inhibition and ROS generation
title_fullStr Selective induction of apoptosis in T-cell acute lymphoblastic leukemia by pristimerin through dual PI3K/AKT pathway inhibition and ROS generation
title_full_unstemmed Selective induction of apoptosis in T-cell acute lymphoblastic leukemia by pristimerin through dual PI3K/AKT pathway inhibition and ROS generation
title_short Selective induction of apoptosis in T-cell acute lymphoblastic leukemia by pristimerin through dual PI3K/AKT pathway inhibition and ROS generation
title_sort Selective induction of apoptosis in T-cell acute lymphoblastic leukemia by pristimerin through dual PI3K/AKT pathway inhibition and ROS generation
topic Biomedical and clinical sciences
Immunology
Oncology and carcinogenesis
Pharmacology and pharmaceutical sciences
PristimerinT-cell acute lymphoblastic leukemia
PI3K/AKT signaling pathway
Apoptosis
Cell cycle arrest
Molecular docking