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Molecules 2016, 21(1), 102; doi:10.3390/molecules21010102

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

1,†
,
1
,
2,†,* , 1
and
1,†,*
1
School of Public Health, Xinjiang Medical University, No. 393 Xinyi Road, Urumqi 830011, Xinjiang Uyghur Autonomous Region, China
2
Key Laboratory for Uighur Medicine, Institute of Materia Medica of Xinjiang, No. 140 Xinhua South Road, Tianshan District, Urumqi 830000, Xinjiang Uyghur Autonomous Region, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 25 November 2015 / Revised: 11 January 2016 / Accepted: 13 January 2016 / Published: 18 January 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [3726 KB, uploaded 18 January 2016]   |  

Abstract

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. View Full-Text
Keywords: Cistanche tubulosa; phenylethanol glycosides from Cistanche (CPHGs); echinacoside; acteoside; hepatic stellate cells (HSC); TGF-β1/smad Cistanche tubulosa; phenylethanol glycosides from Cistanche (CPHGs); echinacoside; acteoside; hepatic stellate cells (HSC); TGF-β1/smad
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

You, S.-P.; Ma, L.; Zhao, J.; Zhang, S.-L.; Liu, T. 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 2016, 21, 102.

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