Regulating mitochondrial oxidative phosphorylation and MAPK signaling: wedelolactone as a novel therapeutic for radiation-induced thrombocytopenia

IntroductionRadiation-induced thrombocytopenia (RIT) is a serious complication of cancer radiotherapy, for which therapeutic options are limited. This study investigates wedelolactone (WED), a metabolite of a botanical drug, as a potential treatment for RIT.MethodsIn vitro experiments were conducted...

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Main Authors: Zhichao Li, Qinyao Li, Shuang Wu, Xinyue Mei, Xiao Qi, Sheng Liu, Gan Qiao, Hongping Shen, Jiesi Luo, Jing Zeng, Feihong Huang, Rong Li, Long Wang
Format: Article
Language:English
Published: Frontiers Media S.A. 2025-04-01
Series:Frontiers in Pharmacology
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Online Access:https://www.frontiersin.org/articles/10.3389/fphar.2025.1508215/full
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author Zhichao Li
Qinyao Li
Shuang Wu
Xinyue Mei
Xiao Qi
Sheng Liu
Gan Qiao
Hongping Shen
Jiesi Luo
Jing Zeng
Feihong Huang
Rong Li
Rong Li
Long Wang
author_facet Zhichao Li
Qinyao Li
Shuang Wu
Xinyue Mei
Xiao Qi
Sheng Liu
Gan Qiao
Hongping Shen
Jiesi Luo
Jing Zeng
Feihong Huang
Rong Li
Rong Li
Long Wang
author_sort Zhichao Li
collection DOAJ
description IntroductionRadiation-induced thrombocytopenia (RIT) is a serious complication of cancer radiotherapy, for which therapeutic options are limited. This study investigates wedelolactone (WED), a metabolite of a botanical drug, as a potential treatment for RIT.MethodsIn vitro experiments were conducted using Meg‐01 and K562 cell lines to evaluate the effects of WED on megakaryocyte differentiation and maturation. Flow cytometry and phalloidin staining were employed to assess the expression of megakaryocyte‐specific markers CD41 and CD61, as well as nuclear polyploidization. A mouse model of RIT was established to assess the efficacy of WED in restoring platelet counts and regulating hematopoiesis. RNA sequencing and western blot analyses were performed to explore the underlying molecular mechanisms.ResultsIn vitro experiments revealed that WED enhanced megakaryocyte differentiation in a dose‐dependent manner, increasing the expression of lineage‐specific markers CD41 and CD61, and promoting polyploidization and cytoskeletal reorganization. In vivo, WED significantly restored platelet counts in the mouse model of RIT and promoted the production of hematopoietic stem cells (HSCs), megakaryocytes, and reticulated platelets. RNA sequencing and western blot revealed that WED-induced megakaryocyte differentiation involves the regulation of mitochondrial oxidative phosphorylation mediated by the AMPK signaling pathway and activation of the MAPK signaling pathway. Inhibition of mitochondrial oxidative phosphorylation or MAPK signaling suppressed WED‐induced megakaryocyte differentiation, highlighting the central role of these pathways.DiscussionThese findings indicate that WED could be a promising therapeutic candidate for RIT, acting through the modulation of oxidative phosphorylation and MAPK signaling pathways to enhance thrombopoiesis.
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spelling doaj-art-393eb6ae32ff47efbd2872e45bc2764e2025-08-20T02:28:58ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122025-04-011610.3389/fphar.2025.15082151508215Regulating mitochondrial oxidative phosphorylation and MAPK signaling: wedelolactone as a novel therapeutic for radiation-induced thrombocytopeniaZhichao Li0Qinyao Li1Shuang Wu2Xinyue Mei3Xiao Qi4Sheng Liu5Gan Qiao6Hongping Shen7Jiesi Luo8Jing Zeng9Feihong Huang10Rong Li11Rong Li12Long Wang13Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, ChinaDepartment of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, ChinaSchool of Basic Medical Sciences, Southwest Medical University, Luzhou, Sichuan, ChinaDepartment of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, ChinaDepartment of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, ChinaDepartment of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, ChinaDepartment of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, ChinaClinical Trial Center, The Affiliated Traditional Chinese Medicine Hospital of Southwest Medical University, Luzhou, Sichuan, ChinaSchool of Basic Medical Sciences, Southwest Medical University, Luzhou, Sichuan, ChinaDepartment of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, ChinaDepartment of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, ChinaDrug Discovery Research Center, Southwest Medical University, Luzhou, Sichuan, ChinaLaboratory for Cardiovascular Pharmacology of Department of Pharmacology, The School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, ChinaDepartment of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, ChinaIntroductionRadiation-induced thrombocytopenia (RIT) is a serious complication of cancer radiotherapy, for which therapeutic options are limited. This study investigates wedelolactone (WED), a metabolite of a botanical drug, as a potential treatment for RIT.MethodsIn vitro experiments were conducted using Meg‐01 and K562 cell lines to evaluate the effects of WED on megakaryocyte differentiation and maturation. Flow cytometry and phalloidin staining were employed to assess the expression of megakaryocyte‐specific markers CD41 and CD61, as well as nuclear polyploidization. A mouse model of RIT was established to assess the efficacy of WED in restoring platelet counts and regulating hematopoiesis. RNA sequencing and western blot analyses were performed to explore the underlying molecular mechanisms.ResultsIn vitro experiments revealed that WED enhanced megakaryocyte differentiation in a dose‐dependent manner, increasing the expression of lineage‐specific markers CD41 and CD61, and promoting polyploidization and cytoskeletal reorganization. In vivo, WED significantly restored platelet counts in the mouse model of RIT and promoted the production of hematopoietic stem cells (HSCs), megakaryocytes, and reticulated platelets. RNA sequencing and western blot revealed that WED-induced megakaryocyte differentiation involves the regulation of mitochondrial oxidative phosphorylation mediated by the AMPK signaling pathway and activation of the MAPK signaling pathway. Inhibition of mitochondrial oxidative phosphorylation or MAPK signaling suppressed WED‐induced megakaryocyte differentiation, highlighting the central role of these pathways.DiscussionThese findings indicate that WED could be a promising therapeutic candidate for RIT, acting through the modulation of oxidative phosphorylation and MAPK signaling pathways to enhance thrombopoiesis.https://www.frontiersin.org/articles/10.3389/fphar.2025.1508215/fullwedelolactonethrombocytopeniaoxidative phosphorylationmegakaryocyte differentiationthrombopoiesis
spellingShingle Zhichao Li
Qinyao Li
Shuang Wu
Xinyue Mei
Xiao Qi
Sheng Liu
Gan Qiao
Hongping Shen
Jiesi Luo
Jing Zeng
Feihong Huang
Rong Li
Rong Li
Long Wang
Regulating mitochondrial oxidative phosphorylation and MAPK signaling: wedelolactone as a novel therapeutic for radiation-induced thrombocytopenia
Frontiers in Pharmacology
wedelolactone
thrombocytopenia
oxidative phosphorylation
megakaryocyte differentiation
thrombopoiesis
title Regulating mitochondrial oxidative phosphorylation and MAPK signaling: wedelolactone as a novel therapeutic for radiation-induced thrombocytopenia
title_full Regulating mitochondrial oxidative phosphorylation and MAPK signaling: wedelolactone as a novel therapeutic for radiation-induced thrombocytopenia
title_fullStr Regulating mitochondrial oxidative phosphorylation and MAPK signaling: wedelolactone as a novel therapeutic for radiation-induced thrombocytopenia
title_full_unstemmed Regulating mitochondrial oxidative phosphorylation and MAPK signaling: wedelolactone as a novel therapeutic for radiation-induced thrombocytopenia
title_short Regulating mitochondrial oxidative phosphorylation and MAPK signaling: wedelolactone as a novel therapeutic for radiation-induced thrombocytopenia
title_sort regulating mitochondrial oxidative phosphorylation and mapk signaling wedelolactone as a novel therapeutic for radiation induced thrombocytopenia
topic wedelolactone
thrombocytopenia
oxidative phosphorylation
megakaryocyte differentiation
thrombopoiesis
url https://www.frontiersin.org/articles/10.3389/fphar.2025.1508215/full
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