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

Autor: Tao Liu, Shi-Lei Zhang, Shu-Ping You, Long Ma, Jun Zhao
Rok vydání: 2016
Předmět:
0301 basic medicine
Cistanche
Pharmaceutical Science
Smad Proteins
SMAD
Pharmacology
Analytical Chemistry
TGF-β1/smad
chemistry.chemical_compound
0302 clinical medicine
Glucosides
Fibrosis
Cistanche tubulosa
phenylethanol glycosides from Cistanche (CPHGs)
echinacoside
acteoside
hepatic stellate cells (HSC)
Drug Discovery
Protein Isoforms
Glycosides
Biochemistry
Chemistry (miscellaneous)
030220 oncology & carcinogenesis
Echinacoside
Molecular Medicine
Signal Transduction
Protective Agents
Article
Cell Line
lcsh:QD241-441
Transforming Growth Factor beta1
03 medical and health sciences
lcsh:Organic chemistry
Phenols
Hepatic Stellate Cells
medicine
Animals
MTT assay
RNA
Messenger
Physical and Theoretical Chemistry
L-Lactate Dehydrogenase
Plant Extracts
business.industry
Organic Chemistry
medicine.disease
Hepatic stellate cell activation
Rats
030104 developmental biology
Gene Expression Regulation
chemistry
Hepatic stellate cell
Hepatic fibrosis
business
Zdroj: Molecules
Molecules; Volume 21; Issue 1; Pages: 102
Molecules, Vol 21, Iss 1, p 102 (2016)
ISSN: 1420-3049
DOI: 10.3390/molecules21010102
Popis: 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.
Databáze: OpenAIRE
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