Protective effects and metabolomics analysis of dihydromyricetin on cyclophosphamide-induced hepatotoxicity in mice

Cyclophosphamide (CTX) is a chemotherapeutic agent with cytotoxic and immunosuppressive activity. It is used to treat a wide variety of cancers and autoimmune diseases. However, side effects caused by its toxic metabolites, especially hepatotoxicity, limit its clinical application. The natural dihyd...

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Main Authors: Fei Teng, Haina Wang
Format: Article
Language:English
Published: Elsevier 2025-12-01
Series:Pharmaceutical Science Advances
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Online Access:http://www.sciencedirect.com/science/article/pii/S2773216925000017
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author Fei Teng
Haina Wang
author_facet Fei Teng
Haina Wang
author_sort Fei Teng
collection DOAJ
description Cyclophosphamide (CTX) is a chemotherapeutic agent with cytotoxic and immunosuppressive activity. It is used to treat a wide variety of cancers and autoimmune diseases. However, side effects caused by its toxic metabolites, especially hepatotoxicity, limit its clinical application. The natural dihydroflavonol compound dihydromyricetin (DHM) has anticancer, anti-inflammatory, and antioxidant properties. This study aimed to evaluate the protective effects of DHM against CTX-induced hepatotoxicity in mice. Male ICR mice were pretreated with DHM (100, 200, and 400 ​mg/kg b.w.) orally before intraperitoneal injection with CTX (100 ​mg/kg b.w.) for 7 days. The mice were then sacrificed to analyze biochemical and histological parameters as well as metabolomics profiles. DHM ameliorated CTX-induced elevations in the liver index, alanine aminotransferase, aspartate transaminase, and malondialdehyde levels, and pathological changes and increased levels of glutathione and antioxidant enzymes, such as superoxide dismutase and catalase. Based on a KEGG pathway analysis of altered serum and liver metabolites, OXPHOS may play an important role in the observed protective effects. Further analysis revealed that DHM increased the activity of Na+-K+-ATPase in mice, which affected CTX-induced mitochondrial energy metabolism. To conclude, DHM protected against CTX-induced hepatotoxicity, possibly through reducing oxidative stress and regulating energy metabolism, providing a potential strategy for treatment and prevention.
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spelling doaj-art-95b44040926c4efd9661b2ef15b2b7e22025-08-20T03:00:50ZengElsevierPharmaceutical Science Advances2773-21692025-12-01310006310.1016/j.pscia.2025.100063Protective effects and metabolomics analysis of dihydromyricetin on cyclophosphamide-induced hepatotoxicity in miceFei Teng0Haina Wang1School of Pharmaceutical Sciences, Shandong University, Jinan, 250012, PR ChinaCorresponding author.; School of Pharmaceutical Sciences, Shandong University, Jinan, 250012, PR ChinaCyclophosphamide (CTX) is a chemotherapeutic agent with cytotoxic and immunosuppressive activity. It is used to treat a wide variety of cancers and autoimmune diseases. However, side effects caused by its toxic metabolites, especially hepatotoxicity, limit its clinical application. The natural dihydroflavonol compound dihydromyricetin (DHM) has anticancer, anti-inflammatory, and antioxidant properties. This study aimed to evaluate the protective effects of DHM against CTX-induced hepatotoxicity in mice. Male ICR mice were pretreated with DHM (100, 200, and 400 ​mg/kg b.w.) orally before intraperitoneal injection with CTX (100 ​mg/kg b.w.) for 7 days. The mice were then sacrificed to analyze biochemical and histological parameters as well as metabolomics profiles. DHM ameliorated CTX-induced elevations in the liver index, alanine aminotransferase, aspartate transaminase, and malondialdehyde levels, and pathological changes and increased levels of glutathione and antioxidant enzymes, such as superoxide dismutase and catalase. Based on a KEGG pathway analysis of altered serum and liver metabolites, OXPHOS may play an important role in the observed protective effects. Further analysis revealed that DHM increased the activity of Na+-K+-ATPase in mice, which affected CTX-induced mitochondrial energy metabolism. To conclude, DHM protected against CTX-induced hepatotoxicity, possibly through reducing oxidative stress and regulating energy metabolism, providing a potential strategy for treatment and prevention.http://www.sciencedirect.com/science/article/pii/S2773216925000017DihydromyricetinCyclophosphamideHepatotoxicityMetabolomics
spellingShingle Fei Teng
Haina Wang
Protective effects and metabolomics analysis of dihydromyricetin on cyclophosphamide-induced hepatotoxicity in mice
Pharmaceutical Science Advances
Dihydromyricetin
Cyclophosphamide
Hepatotoxicity
Metabolomics
title Protective effects and metabolomics analysis of dihydromyricetin on cyclophosphamide-induced hepatotoxicity in mice
title_full Protective effects and metabolomics analysis of dihydromyricetin on cyclophosphamide-induced hepatotoxicity in mice
title_fullStr Protective effects and metabolomics analysis of dihydromyricetin on cyclophosphamide-induced hepatotoxicity in mice
title_full_unstemmed Protective effects and metabolomics analysis of dihydromyricetin on cyclophosphamide-induced hepatotoxicity in mice
title_short Protective effects and metabolomics analysis of dihydromyricetin on cyclophosphamide-induced hepatotoxicity in mice
title_sort protective effects and metabolomics analysis of dihydromyricetin on cyclophosphamide induced hepatotoxicity in mice
topic Dihydromyricetin
Cyclophosphamide
Hepatotoxicity
Metabolomics
url http://www.sciencedirect.com/science/article/pii/S2773216925000017
work_keys_str_mv AT feiteng protectiveeffectsandmetabolomicsanalysisofdihydromyricetinoncyclophosphamideinducedhepatotoxicityinmice
AT hainawang protectiveeffectsandmetabolomicsanalysisofdihydromyricetinoncyclophosphamideinducedhepatotoxicityinmice