Phenylethanol Glycosides from Cistanche tubulosa Suppress Hepatic Stellate Cell Activation and Block the Conduction of Signaling Pathways in TGF-β1/smad as Potential Anti-Hepatic Fibrosis Agents

Cistanche tubulosa is a traditional Chinese herbal medicine widely used for regulating immunity and phenylethanol glycosides (CPhGs) are among the primary components responsible for this activity. Previous studies have indicated the preventive and therapeutic effects of CPhGs on bovine serum albumin...

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Main Authors: Shu-Ping You, Long Ma, Jun Zhao, Shi-Lei Zhang, Tao Liu
Format: Article
Language:English
Published: MDPI AG 2016-01-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/21/1/102
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author Shu-Ping You
Long Ma
Jun Zhao
Shi-Lei Zhang
Tao Liu
author_facet Shu-Ping You
Long Ma
Jun Zhao
Shi-Lei Zhang
Tao Liu
author_sort Shu-Ping You
collection DOAJ
description Cistanche tubulosa is a traditional Chinese herbal medicine widely used for regulating immunity and phenylethanol glycosides (CPhGs) are among the primary components responsible for this activity. Previous studies have indicated the preventive and therapeutic effects of CPhGs on bovine serum albumin (BSA)-induced hepatic fibrosis in rats. The aim of the study was to evaluate the anti-hepatic fibrosis effect of CPhGs and the monomers echinacoside and acteoside by inhibiting hepatic stellate cell (HSC) activation, blocking the conduction of signaling pathways in transforming growth factor-β1 (TGF-β1)/smad, and determine their in vitro hepatoprotective activity. HSC proliferation was obviously inhibited after treatment with CPhGs (100, 50 μg/mL)/echinacoside (500, 250, 125 μg/mL)/acteoside (6, 3 μg/mL), with IC50 values of 119.125, 520.345 and 6.999 μg/mL, respectively, in the MTT assay. Different concentrations of CPhGs/echinacoside/acteoside did not affect the cellular toxicity on HSC according to lactate dehydrogenase (LDH) measurements. Different concentrations of CPhGs/echinacoside/acteoside increased the mRNA level and protein expression of smad7, and decreased the mRNA levels of smad2, smad3 and the protein expression of smad2, phospho-smad2 (p-smad2), smad3, phospho-smad3 (p-smad3) in HSC. In summary, these results demonstrate that CPhGs/echinacoside/acteoside can block the conduction of the signaling pathways in TGF-β1/smad, and inhibit the activation of HSC, suggesting that C. tubulosa may thus be a potential herbal medicine for the treatment of liver fibrosis.
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spelling doaj.art-b7c19cff065e495c91a403ba307f219a2022-12-22T01:22:51ZengMDPI AGMolecules1420-30492016-01-0121110210.3390/molecules21010102molecules21010102Phenylethanol Glycosides from Cistanche tubulosa Suppress Hepatic Stellate Cell Activation and Block the Conduction of Signaling Pathways in TGF-β1/smad as Potential Anti-Hepatic Fibrosis AgentsShu-Ping You0Long Ma1Jun Zhao2Shi-Lei Zhang3Tao Liu4School of Public Health, Xinjiang Medical University, No. 393 Xinyi Road, Urumqi 830011, Xinjiang Uyghur Autonomous Region, ChinaSchool of Public Health, Xinjiang Medical University, No. 393 Xinyi Road, Urumqi 830011, Xinjiang Uyghur Autonomous Region, ChinaKey Laboratory for Uighur Medicine, Institute of Materia Medica of Xinjiang, No. 140 Xinhua South Road, Tianshan District, Urumqi 830000, Xinjiang Uyghur Autonomous Region, ChinaSchool of Public Health, Xinjiang Medical University, No. 393 Xinyi Road, Urumqi 830011, Xinjiang Uyghur Autonomous Region, ChinaSchool of Public Health, Xinjiang Medical University, No. 393 Xinyi Road, Urumqi 830011, Xinjiang Uyghur Autonomous Region, ChinaCistanche tubulosa is a traditional Chinese herbal medicine widely used for regulating immunity and phenylethanol glycosides (CPhGs) are among the primary components responsible for this activity. Previous studies have indicated the preventive and therapeutic effects of CPhGs on bovine serum albumin (BSA)-induced hepatic fibrosis in rats. The aim of the study was to evaluate the anti-hepatic fibrosis effect of CPhGs and the monomers echinacoside and acteoside by inhibiting hepatic stellate cell (HSC) activation, blocking the conduction of signaling pathways in transforming growth factor-β1 (TGF-β1)/smad, and determine their in vitro hepatoprotective activity. HSC proliferation was obviously inhibited after treatment with CPhGs (100, 50 μg/mL)/echinacoside (500, 250, 125 μg/mL)/acteoside (6, 3 μg/mL), with IC50 values of 119.125, 520.345 and 6.999 μg/mL, respectively, in the MTT assay. Different concentrations of CPhGs/echinacoside/acteoside did not affect the cellular toxicity on HSC according to lactate dehydrogenase (LDH) measurements. Different concentrations of CPhGs/echinacoside/acteoside increased the mRNA level and protein expression of smad7, and decreased the mRNA levels of smad2, smad3 and the protein expression of smad2, phospho-smad2 (p-smad2), smad3, phospho-smad3 (p-smad3) in HSC. In summary, these results demonstrate that CPhGs/echinacoside/acteoside can block the conduction of the signaling pathways in TGF-β1/smad, and inhibit the activation of HSC, suggesting that C. tubulosa may thus be a potential herbal medicine for the treatment of liver fibrosis.http://www.mdpi.com/1420-3049/21/1/102Cistanche tubulosaphenylethanol glycosides from Cistanche (CPHGs)echinacosideacteosidehepatic stellate cells (HSC)TGF-β1/smad
spellingShingle Shu-Ping You
Long Ma
Jun Zhao
Shi-Lei Zhang
Tao Liu
Phenylethanol Glycosides from Cistanche tubulosa Suppress Hepatic Stellate Cell Activation and Block the Conduction of Signaling Pathways in TGF-β1/smad as Potential Anti-Hepatic Fibrosis Agents
Molecules
Cistanche tubulosa
phenylethanol glycosides from Cistanche (CPHGs)
echinacoside
acteoside
hepatic stellate cells (HSC)
TGF-β1/smad
title Phenylethanol Glycosides from Cistanche tubulosa Suppress Hepatic Stellate Cell Activation and Block the Conduction of Signaling Pathways in TGF-β1/smad as Potential Anti-Hepatic Fibrosis Agents
title_full Phenylethanol Glycosides from Cistanche tubulosa Suppress Hepatic Stellate Cell Activation and Block the Conduction of Signaling Pathways in TGF-β1/smad as Potential Anti-Hepatic Fibrosis Agents
title_fullStr Phenylethanol Glycosides from Cistanche tubulosa Suppress Hepatic Stellate Cell Activation and Block the Conduction of Signaling Pathways in TGF-β1/smad as Potential Anti-Hepatic Fibrosis Agents
title_full_unstemmed Phenylethanol Glycosides from Cistanche tubulosa Suppress Hepatic Stellate Cell Activation and Block the Conduction of Signaling Pathways in TGF-β1/smad as Potential Anti-Hepatic Fibrosis Agents
title_short Phenylethanol Glycosides from Cistanche tubulosa Suppress Hepatic Stellate Cell Activation and Block the Conduction of Signaling Pathways in TGF-β1/smad as Potential Anti-Hepatic Fibrosis Agents
title_sort phenylethanol glycosides from cistanche tubulosa suppress hepatic stellate cell activation and block the conduction of signaling pathways in tgf β1 smad as potential anti hepatic fibrosis agents
topic Cistanche tubulosa
phenylethanol glycosides from Cistanche (CPHGs)
echinacoside
acteoside
hepatic stellate cells (HSC)
TGF-β1/smad
url http://www.mdpi.com/1420-3049/21/1/102
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