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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2016-01-01
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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 |
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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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