Linagliptin attenuates kidney cancer in rats via AMPK activation and suppression of YAP/TAZ/HIF-1α signaling

Publikation: Beitrag in FachzeitschriftArtikelForschungPeer-Review

Autorschaft

  • Tahani Saeedi
  • Mohannad Almikhlafi
  • Hossein M Elbadawy
  • Muayad S Albadrani
  • Rehab F Abdel-Rahman
  • Gihan F. Asaad
  • Fatma A Ibrahim
  • Aya A. Shokry
  • Tuba Esatbeyoglu
  • Sherif M. Afifi
  • Hany M Fayed
  • Marawan A. Elbaset

Externe Organisationen

  • Taibah University
  • National Research Centre (NRC)
  • Cairo University
  • Università di Bologna
  • Indiana University School of Medicine (IUSM)
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Details

OriginalspracheEnglisch
Aufsatznummer107393
FachzeitschriftEuropean Journal of Pharmaceutical Sciences
Jahrgang217
Frühes Online-Datum1 Dez. 2025
PublikationsstatusVeröffentlicht - 1 Feb. 2026

Abstract

This study investigated the renoprotective action of linagliptin compared to doxorubicin against thioacetamide (TAA) and diethyl nitrosamine (DEN)-induced renocarcinogenesis in a rat model. Male Wistar rats were divided into control, renocarcinogenesis (RCC), doxorubicin group (7.5 mg/kg, i.p., once weekly), and linagliptin (Lina) groups (3 and 6 mg/kg/day, p.o.). The experiment included renal function parameters, oxidative stress markers, and predominant molecular pathways involved in renal pathogenesis. The RCC model significantly impaired renal function, as reflected in elevated serum levels of urea and creatinine. It also resulted in elevated oxidative stress, as reflected in increased malondialdehyde (MDA) content and decreased glutathione and superoxide dismutase (GSH and SOD) activities. The model disrupted several molecular pathways, including the AMP-activated protein kinase (AMPK) pathway, and enhanced oncogenic and inflammatory markers such as Yes-associated protein/ Transcriptional coactivator with PDZ-binding motif/ Hypoxia-inducible factor 1-alpha (YAP/TAZ/ HIF-1α), nuclear factor erythroid 2-related factor 2/ Sirtuin 1(Nrf2/SIRT1), and signal transducer and activator of transcription 3 (STAT3). Treatment with linagliptin, particularly the high dose (6 mg/kg/day), was found to be superior to doxorubicin treatment in terms of correction of renal function and markers of oxidative stress. Linagliptin effectively regulated the AMPK pathway, reduced markers of inflammation, restored the expression of genes with key roles in renal protection, reduced proliferating Cell Nuclear Antigen (PCNA), and elevated Caspase-3. The high dose of linagliptin exhibited superior results in most of the parameters, which approached control levels more than those with the lower dose and doxorubicin. These findings demonstrate that linagliptin, especially at 6 mg/kg/day, exhibits significant renoprotective activities through multifarious mechanisms involving antioxidant action and regulation of key molecular pathways. The present study presents evidence for the potential therapeutic application of linagliptin in renal manifestations of renocarcinogenesis.

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Linagliptin attenuates kidney cancer in rats via AMPK activation and suppression of YAP/TAZ/HIF-1α signaling. / Saeedi, Tahani; Almikhlafi, Mohannad; Elbadawy, Hossein M et al.
in: European Journal of Pharmaceutical Sciences, Jahrgang 217, 107393, 01.02.2026.

Publikation: Beitrag in FachzeitschriftArtikelForschungPeer-Review

Saeedi, T, Almikhlafi, M, Elbadawy, HM, Albadrani, MS, Abdel-Rahman, RF, Asaad, GF, Ibrahim, FA, Shokry, AA, Esatbeyoglu, T, Afifi, SM, Fayed, HM & Elbaset, MA 2026, 'Linagliptin attenuates kidney cancer in rats via AMPK activation and suppression of YAP/TAZ/HIF-1α signaling', European Journal of Pharmaceutical Sciences, Jg. 217, 107393. https://doi.org/10.1016/j.ejps.2025.107393
Saeedi, T., Almikhlafi, M., Elbadawy, H. M., Albadrani, M. S., Abdel-Rahman, R. F., Asaad, G. F., Ibrahim, F. A., Shokry, A. A., Esatbeyoglu, T., Afifi, S. M., Fayed, H. M., & Elbaset, M. A. (2026). Linagliptin attenuates kidney cancer in rats via AMPK activation and suppression of YAP/TAZ/HIF-1α signaling. European Journal of Pharmaceutical Sciences, 217, Artikel 107393. https://doi.org/10.1016/j.ejps.2025.107393
Saeedi T, Almikhlafi M, Elbadawy HM, Albadrani MS, Abdel-Rahman RF, Asaad GF et al. Linagliptin attenuates kidney cancer in rats via AMPK activation and suppression of YAP/TAZ/HIF-1α signaling. European Journal of Pharmaceutical Sciences. 2026 Feb 1;217:107393. Epub 2025 Dez 1. doi: 10.1016/j.ejps.2025.107393
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title = "Linagliptin attenuates kidney cancer in rats via AMPK activation and suppression of YAP/TAZ/HIF-1α signaling",
abstract = "This study investigated the renoprotective action of linagliptin compared to doxorubicin against thioacetamide (TAA) and diethyl nitrosamine (DEN)-induced renocarcinogenesis in a rat model. Male Wistar rats were divided into control, renocarcinogenesis (RCC), doxorubicin group (7.5 mg/kg, i.p., once weekly), and linagliptin (Lina) groups (3 and 6 mg/kg/day, p.o.). The experiment included renal function parameters, oxidative stress markers, and predominant molecular pathways involved in renal pathogenesis. The RCC model significantly impaired renal function, as reflected in elevated serum levels of urea and creatinine. It also resulted in elevated oxidative stress, as reflected in increased malondialdehyde (MDA) content and decreased glutathione and superoxide dismutase (GSH and SOD) activities. The model disrupted several molecular pathways, including the AMP-activated protein kinase (AMPK) pathway, and enhanced oncogenic and inflammatory markers such as Yes-associated protein/ Transcriptional coactivator with PDZ-binding motif/ Hypoxia-inducible factor 1-alpha (YAP/TAZ/ HIF-1α), nuclear factor erythroid 2-related factor 2/ Sirtuin 1(Nrf2/SIRT1), and signal transducer and activator of transcription 3 (STAT3). Treatment with linagliptin, particularly the high dose (6 mg/kg/day), was found to be superior to doxorubicin treatment in terms of correction of renal function and markers of oxidative stress. Linagliptin effectively regulated the AMPK pathway, reduced markers of inflammation, restored the expression of genes with key roles in renal protection, reduced proliferating Cell Nuclear Antigen (PCNA), and elevated Caspase-3. The high dose of linagliptin exhibited superior results in most of the parameters, which approached control levels more than those with the lower dose and doxorubicin. These findings demonstrate that linagliptin, especially at 6 mg/kg/day, exhibits significant renoprotective activities through multifarious mechanisms involving antioxidant action and regulation of key molecular pathways. The present study presents evidence for the potential therapeutic application of linagliptin in renal manifestations of renocarcinogenesis.",
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Download

TY - JOUR

T1 - Linagliptin attenuates kidney cancer in rats via AMPK activation and suppression of YAP/TAZ/HIF-1α signaling

AU - Saeedi, Tahani

AU - Almikhlafi, Mohannad

AU - Elbadawy, Hossein M

AU - Albadrani, Muayad S

AU - Abdel-Rahman, Rehab F

AU - Asaad, Gihan F.

AU - Ibrahim, Fatma A

AU - Shokry, Aya A.

AU - Esatbeyoglu, Tuba

AU - Afifi, Sherif M.

AU - Fayed, Hany M

AU - Elbaset, Marawan A.

N1 - Publisher Copyright: © 2025 The Author(s)

PY - 2026/2/1

Y1 - 2026/2/1

N2 - This study investigated the renoprotective action of linagliptin compared to doxorubicin against thioacetamide (TAA) and diethyl nitrosamine (DEN)-induced renocarcinogenesis in a rat model. Male Wistar rats were divided into control, renocarcinogenesis (RCC), doxorubicin group (7.5 mg/kg, i.p., once weekly), and linagliptin (Lina) groups (3 and 6 mg/kg/day, p.o.). The experiment included renal function parameters, oxidative stress markers, and predominant molecular pathways involved in renal pathogenesis. The RCC model significantly impaired renal function, as reflected in elevated serum levels of urea and creatinine. It also resulted in elevated oxidative stress, as reflected in increased malondialdehyde (MDA) content and decreased glutathione and superoxide dismutase (GSH and SOD) activities. The model disrupted several molecular pathways, including the AMP-activated protein kinase (AMPK) pathway, and enhanced oncogenic and inflammatory markers such as Yes-associated protein/ Transcriptional coactivator with PDZ-binding motif/ Hypoxia-inducible factor 1-alpha (YAP/TAZ/ HIF-1α), nuclear factor erythroid 2-related factor 2/ Sirtuin 1(Nrf2/SIRT1), and signal transducer and activator of transcription 3 (STAT3). Treatment with linagliptin, particularly the high dose (6 mg/kg/day), was found to be superior to doxorubicin treatment in terms of correction of renal function and markers of oxidative stress. Linagliptin effectively regulated the AMPK pathway, reduced markers of inflammation, restored the expression of genes with key roles in renal protection, reduced proliferating Cell Nuclear Antigen (PCNA), and elevated Caspase-3. The high dose of linagliptin exhibited superior results in most of the parameters, which approached control levels more than those with the lower dose and doxorubicin. These findings demonstrate that linagliptin, especially at 6 mg/kg/day, exhibits significant renoprotective activities through multifarious mechanisms involving antioxidant action and regulation of key molecular pathways. The present study presents evidence for the potential therapeutic application of linagliptin in renal manifestations of renocarcinogenesis.

AB - This study investigated the renoprotective action of linagliptin compared to doxorubicin against thioacetamide (TAA) and diethyl nitrosamine (DEN)-induced renocarcinogenesis in a rat model. Male Wistar rats were divided into control, renocarcinogenesis (RCC), doxorubicin group (7.5 mg/kg, i.p., once weekly), and linagliptin (Lina) groups (3 and 6 mg/kg/day, p.o.). The experiment included renal function parameters, oxidative stress markers, and predominant molecular pathways involved in renal pathogenesis. The RCC model significantly impaired renal function, as reflected in elevated serum levels of urea and creatinine. It also resulted in elevated oxidative stress, as reflected in increased malondialdehyde (MDA) content and decreased glutathione and superoxide dismutase (GSH and SOD) activities. The model disrupted several molecular pathways, including the AMP-activated protein kinase (AMPK) pathway, and enhanced oncogenic and inflammatory markers such as Yes-associated protein/ Transcriptional coactivator with PDZ-binding motif/ Hypoxia-inducible factor 1-alpha (YAP/TAZ/ HIF-1α), nuclear factor erythroid 2-related factor 2/ Sirtuin 1(Nrf2/SIRT1), and signal transducer and activator of transcription 3 (STAT3). Treatment with linagliptin, particularly the high dose (6 mg/kg/day), was found to be superior to doxorubicin treatment in terms of correction of renal function and markers of oxidative stress. Linagliptin effectively regulated the AMPK pathway, reduced markers of inflammation, restored the expression of genes with key roles in renal protection, reduced proliferating Cell Nuclear Antigen (PCNA), and elevated Caspase-3. The high dose of linagliptin exhibited superior results in most of the parameters, which approached control levels more than those with the lower dose and doxorubicin. These findings demonstrate that linagliptin, especially at 6 mg/kg/day, exhibits significant renoprotective activities through multifarious mechanisms involving antioxidant action and regulation of key molecular pathways. The present study presents evidence for the potential therapeutic application of linagliptin in renal manifestations of renocarcinogenesis.

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