Ivermectin Attenuates Methotrexate-Induced Liver Fibrosis by Reducing TGF-β and Syndecan-1 Expression

<i>Background and Objectives:</i> Methotrexate (MTX) is widely used in clinical settings but is often associated with hepatotoxic side effects, including oxidative stress, inflammation, and fibrosis. Novel therapeutic strategies are needed to mitigate MTX-induced liver injury. This study...

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Main Authors: Cengiz Dibekoğlu, Kubilay Kemertaş, Hatice Aygun, Oytun Erbaş
Format: Article
Language:English
Published: MDPI AG 2025-06-01
Series:Medicina
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Online Access:https://www.mdpi.com/1648-9144/61/6/1036
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author Cengiz Dibekoğlu
Kubilay Kemertaş
Hatice Aygun
Oytun Erbaş
author_facet Cengiz Dibekoğlu
Kubilay Kemertaş
Hatice Aygun
Oytun Erbaş
author_sort Cengiz Dibekoğlu
collection DOAJ
description <i>Background and Objectives:</i> Methotrexate (MTX) is widely used in clinical settings but is often associated with hepatotoxic side effects, including oxidative stress, inflammation, and fibrosis. Novel therapeutic strategies are needed to mitigate MTX-induced liver injury. This study aimed to evaluate the hepatoprotective effects of ivermectin in a rat model of MTX-induced hepatotoxicity. <i>Materials and Methods:</i> Thirty male Wistar albino rats were randomly divided into three groups (n = 10 per group): control (saline only), MTX (single intraperitoneal dose of 20 mg/kg MTX), and MTX + ivermectin (20 mg/kg MTX + 0.5 mg/kg/day ivermectin for 10 days). At the end of the experiment, blood and liver tissues were collected for histopathological and biochemical evaluation, including ALT, malondialdehyde (MDA), TGF-β, and syndecan-1 levels. <i>Results:</i> MTX administration significantly increased plasma and hepatic MDA, TGF-β, syndecan-1, and ALT levels, alongside histological evidence of necrosis, fibrosis, and inflammatory infiltration (<i>p</i> < 0.001 vs. control). Ivermectin treatment significantly attenuated these alterations, with reductions in MDA (both plasma and liver), TGF-β, syndecan-1, and ALT levels (<i>p</i> < 0.05–0.001 vs. MTX). Histological scoring also revealed improved liver architecture and decreased necrosis, fibrosis, and leukocyte infiltration. <i>Conclusions:</i> Ivermectin demonstrates a strong hepatoprotective effect against MTX-induced liver injury, likely through antioxidant, anti-inflammatory, antifibrotic, and endothelial-protective mechanisms. These findings support the repurposing potential of ivermectin in mitigating drug-induced hepatic damage.
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spelling doaj-art-8eb76a0bb95e429995f2536f31d1cefc2025-08-20T03:16:34ZengMDPI AGMedicina1010-660X1648-91442025-06-01616103610.3390/medicina61061036Ivermectin Attenuates Methotrexate-Induced Liver Fibrosis by Reducing TGF-β and Syndecan-1 ExpressionCengiz Dibekoğlu0Kubilay Kemertaş1Hatice Aygun2Oytun Erbaş3Department of General Surgery, Demiroğlu Bilim University, 34394 Istanbul, TurkeyDepartment of General Surgery, Florence Nightingale Hospital, 34394 Istanbul, TurkeyDepartment of Physiology, Faculty of Medicine, Tokat Gaziosmanpaşa University, 60250 Tokat, TurkeyFaculty of Medicine, BAMER, Biruni University, 34015 Istanbul, Turkey<i>Background and Objectives:</i> Methotrexate (MTX) is widely used in clinical settings but is often associated with hepatotoxic side effects, including oxidative stress, inflammation, and fibrosis. Novel therapeutic strategies are needed to mitigate MTX-induced liver injury. This study aimed to evaluate the hepatoprotective effects of ivermectin in a rat model of MTX-induced hepatotoxicity. <i>Materials and Methods:</i> Thirty male Wistar albino rats were randomly divided into three groups (n = 10 per group): control (saline only), MTX (single intraperitoneal dose of 20 mg/kg MTX), and MTX + ivermectin (20 mg/kg MTX + 0.5 mg/kg/day ivermectin for 10 days). At the end of the experiment, blood and liver tissues were collected for histopathological and biochemical evaluation, including ALT, malondialdehyde (MDA), TGF-β, and syndecan-1 levels. <i>Results:</i> MTX administration significantly increased plasma and hepatic MDA, TGF-β, syndecan-1, and ALT levels, alongside histological evidence of necrosis, fibrosis, and inflammatory infiltration (<i>p</i> < 0.001 vs. control). Ivermectin treatment significantly attenuated these alterations, with reductions in MDA (both plasma and liver), TGF-β, syndecan-1, and ALT levels (<i>p</i> < 0.05–0.001 vs. MTX). Histological scoring also revealed improved liver architecture and decreased necrosis, fibrosis, and leukocyte infiltration. <i>Conclusions:</i> Ivermectin demonstrates a strong hepatoprotective effect against MTX-induced liver injury, likely through antioxidant, anti-inflammatory, antifibrotic, and endothelial-protective mechanisms. These findings support the repurposing potential of ivermectin in mitigating drug-induced hepatic damage.https://www.mdpi.com/1648-9144/61/6/1036ivermectinmethotrexatehepatotoxicityliver fibrosisoxidative stressTGF-β
spellingShingle Cengiz Dibekoğlu
Kubilay Kemertaş
Hatice Aygun
Oytun Erbaş
Ivermectin Attenuates Methotrexate-Induced Liver Fibrosis by Reducing TGF-β and Syndecan-1 Expression
Medicina
ivermectin
methotrexate
hepatotoxicity
liver fibrosis
oxidative stress
TGF-β
title Ivermectin Attenuates Methotrexate-Induced Liver Fibrosis by Reducing TGF-β and Syndecan-1 Expression
title_full Ivermectin Attenuates Methotrexate-Induced Liver Fibrosis by Reducing TGF-β and Syndecan-1 Expression
title_fullStr Ivermectin Attenuates Methotrexate-Induced Liver Fibrosis by Reducing TGF-β and Syndecan-1 Expression
title_full_unstemmed Ivermectin Attenuates Methotrexate-Induced Liver Fibrosis by Reducing TGF-β and Syndecan-1 Expression
title_short Ivermectin Attenuates Methotrexate-Induced Liver Fibrosis by Reducing TGF-β and Syndecan-1 Expression
title_sort ivermectin attenuates methotrexate induced liver fibrosis by reducing tgf β and syndecan 1 expression
topic ivermectin
methotrexate
hepatotoxicity
liver fibrosis
oxidative stress
TGF-β
url https://www.mdpi.com/1648-9144/61/6/1036
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