Aamal G El-Waseif, Mahmoud Elshal, Dalia H El-Kashef, Nashwa M Abu-Elsaad
{"title":"针对TLR4/NF-κB/HIF-1α和TGF-β/Smad信号通路,维生素D受体激活剂paricalcitol减轻胺碘酮诱导的大鼠肺毒性","authors":"Aamal G El-Waseif, Mahmoud Elshal, Dalia H El-Kashef, Nashwa M Abu-Elsaad","doi":"10.1007/s00210-025-04568-z","DOIUrl":null,"url":null,"abstract":"<p><p>Amiodarone, an antiarrhythmic drug, has been reported to precipitate lung injury by various mechanisms. Vitamin D receptor (VDR) is extensively expressed in the lung, and the disrupted vitamin D/VDR axis may underlie various lung disorders. Therefore, the current study intended to explore the beneficial impact of paricalcitol, a VDR activator, on amiodarone-provoked lung injury and elucidate its possible involved molecular mechanisms. Male Wistar rats were intraperitoneally injected with paricalcitol (0.2 µg/kg) and orally administered amiodarone (40 mg/kg) once daily for four weeks. Our findings revealed that paricalcitol diminished BALF leucocyte count and total protein, serum LDH activity, and pulmonary histopathological changes and counteracted pulmonary oxidative stress. Moreover, paricalcitol decreased pulmonary toll-like receptor 4 (TLR4), nuclear factor kappa B (NF-κB) p65, tumor necrosis factor alpha (TNF-α), transforming growth factor-beta 1 (TGF-β1), and phosphorylated small mothers against decapentaplegic 3 (pSmad 3) levels in line with less lung fibrosis percentage. Interestingly, these results were accompanied by suppressed hypoxia-inducible factor-1α (HIF-1α) lung expression. Taken together, paricalcitol protected against amiodarone-induced lung damage in rats through antioxidant, anti-inflammatory, and antifibrotic activities.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1000,"publicationDate":"2025-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Attenuating amiodarone-induced lung toxicity by the vitamin D receptor activator paricalcitol in rats: targeting TLR4/NF-κB/HIF-1α and TGF-β/Smad signaling pathways.\",\"authors\":\"Aamal G El-Waseif, Mahmoud Elshal, Dalia H El-Kashef, Nashwa M Abu-Elsaad\",\"doi\":\"10.1007/s00210-025-04568-z\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Amiodarone, an antiarrhythmic drug, has been reported to precipitate lung injury by various mechanisms. Vitamin D receptor (VDR) is extensively expressed in the lung, and the disrupted vitamin D/VDR axis may underlie various lung disorders. Therefore, the current study intended to explore the beneficial impact of paricalcitol, a VDR activator, on amiodarone-provoked lung injury and elucidate its possible involved molecular mechanisms. Male Wistar rats were intraperitoneally injected with paricalcitol (0.2 µg/kg) and orally administered amiodarone (40 mg/kg) once daily for four weeks. Our findings revealed that paricalcitol diminished BALF leucocyte count and total protein, serum LDH activity, and pulmonary histopathological changes and counteracted pulmonary oxidative stress. Moreover, paricalcitol decreased pulmonary toll-like receptor 4 (TLR4), nuclear factor kappa B (NF-κB) p65, tumor necrosis factor alpha (TNF-α), transforming growth factor-beta 1 (TGF-β1), and phosphorylated small mothers against decapentaplegic 3 (pSmad 3) levels in line with less lung fibrosis percentage. Interestingly, these results were accompanied by suppressed hypoxia-inducible factor-1α (HIF-1α) lung expression. Taken together, paricalcitol protected against amiodarone-induced lung damage in rats through antioxidant, anti-inflammatory, and antifibrotic activities.</p>\",\"PeriodicalId\":18876,\"journal\":{\"name\":\"Naunyn-Schmiedeberg's archives of pharmacology\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":3.1000,\"publicationDate\":\"2025-10-14\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Naunyn-Schmiedeberg's archives of pharmacology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1007/s00210-025-04568-z\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Naunyn-Schmiedeberg's archives of pharmacology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1007/s00210-025-04568-z","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Attenuating amiodarone-induced lung toxicity by the vitamin D receptor activator paricalcitol in rats: targeting TLR4/NF-κB/HIF-1α and TGF-β/Smad signaling pathways.
Amiodarone, an antiarrhythmic drug, has been reported to precipitate lung injury by various mechanisms. Vitamin D receptor (VDR) is extensively expressed in the lung, and the disrupted vitamin D/VDR axis may underlie various lung disorders. Therefore, the current study intended to explore the beneficial impact of paricalcitol, a VDR activator, on amiodarone-provoked lung injury and elucidate its possible involved molecular mechanisms. Male Wistar rats were intraperitoneally injected with paricalcitol (0.2 µg/kg) and orally administered amiodarone (40 mg/kg) once daily for four weeks. Our findings revealed that paricalcitol diminished BALF leucocyte count and total protein, serum LDH activity, and pulmonary histopathological changes and counteracted pulmonary oxidative stress. Moreover, paricalcitol decreased pulmonary toll-like receptor 4 (TLR4), nuclear factor kappa B (NF-κB) p65, tumor necrosis factor alpha (TNF-α), transforming growth factor-beta 1 (TGF-β1), and phosphorylated small mothers against decapentaplegic 3 (pSmad 3) levels in line with less lung fibrosis percentage. Interestingly, these results were accompanied by suppressed hypoxia-inducible factor-1α (HIF-1α) lung expression. Taken together, paricalcitol protected against amiodarone-induced lung damage in rats through antioxidant, anti-inflammatory, and antifibrotic activities.
期刊介绍:
Naunyn-Schmiedeberg''s Archives of Pharmacology was founded in 1873 by B. Naunyn, O. Schmiedeberg and E. Klebs as Archiv für experimentelle Pathologie und Pharmakologie, is the offical journal of the German Society of Experimental and Clinical Pharmacology and Toxicology (Deutsche Gesellschaft für experimentelle und klinische Pharmakologie und Toxikologie, DGPT) and the Sphingolipid Club. The journal publishes invited reviews, original articles, short communications and meeting reports and appears monthly. Naunyn-Schmiedeberg''s Archives of Pharmacology welcomes manuscripts for consideration of publication that report new and significant information on drug action and toxicity of chemical compounds. Thus, its scope covers all fields of experimental and clinical pharmacology as well as toxicology and includes studies in the fields of neuropharmacology and cardiovascular pharmacology as well as those describing drug actions at the cellular, biochemical and molecular levels. Moreover, submission of clinical trials with healthy volunteers or patients is encouraged. Short communications provide a means for rapid publication of significant findings of current interest that represent a conceptual advance in the field.