Eremophila maculata-Isolation of a rare naturally-occurring lignan glycoside and the hepatoprotective activity of the leaf extract.

Authors:
Prof. Hesham El-Beshbishy, PhD
Prof. Hesham El-Beshbishy, PhD
Prof. Medical Biochemistry and Molecular Biology
Professor
Medical Biochemistry and Molecular Biology
Madina, Madina | SA

Phytomedicine 2016 Nov 24;23(12):1484-1493. Epub 2016 Aug 24.

Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, Heidelberg, Germany. Electronic address:

Background: The Australian plant Eremophila maculata F. Muell (Scrophulariaceae) is cultivated worldwide as an ornamental plant.

Purpose: This study was designed to assess the antioxidant and hepatoprotective activities of a methanol extract from E. maculata leaves (EMM) both in vitro and in vivo (rats) experiments. Detailed phytochemical study was done on the extract followed by molecular docking experiments on TNF-α ascertain the efficacy of the isolated compounds.

Methods: The antiproliferative activity was evaluated in the human cancer cell lines A-495, PC3 and HepG2 cells using the SRB method. The antioxidant activitywas evaluated in vitro using the DPPH• assay while the hepatoprotective properties were investigated by determining the amelioration of CCl-induced cytotoxicity and oxidative stress in HepG2 cells. The activity was confirmed in vivo by studying tamoxifen-induced hepatotoxicity in rats. An in-depth phytochemical investigation of a methanol extract was performed using 1D and 2D NMR experiments. In silico molecular modeling studies of the isolated compounds on TNF-α (PDB ID 2AZ5) were carried out using Discovery Studio 2.5 software applying C-Docker protocol.

Results: The IC values of EMM were >500µg/ml for both PC3 and HepG2 cells indicating its safety. Similar to the standard drug silymarin, EMM could restore AST, ALT values; replenish GSH level, SOD activity and TAC in vitro. The hepatoprotective activity was confirmed in vivo in which the extract (20mg/kg body weight) decreased ALT and AST levels by 45.23 and 45.79%, respectively as compared to the tamoxifen treated groups. Oxidative stress was reduced by lowering of thiobarbituric acid reactive substances by 28.57%. Additionally, hepatocyte inflammation was improved by reducing the pro-inflammatory mediator TNF-α by 54.29%. Phytochemical investigation resulted in the isolation of a rare naturally-occurring lignan glycoside, namely pinoresinol-4-O-[6″-O-(E)-feruloyl]-β-D-glucopyranoside for the first time from the Scrophulariaceae in addition to 12 known compounds.Pinoresinol-4-O-[6''-O-(E)-feruloyl]-β-D-glucopyranoside was the strongest inhibitor of TNF-α as evidenced from its higher fitting scores comparable to lead compound.

Conclusions: These findings highlighted for the first time that EMM could be an interesting candidate as a safe, natural liver supplement for relieving of various hepatic disorders and counteracting the effect of many xenobiotics.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.phymed.2016.08.006DOI Listing
November 2016
6 Reads
1 Citation
3.130 Impact Factor

Publication Analysis

Top Keywords

hepg2 cells
12
naturally-occurring lignan
8
activity confirmed
8
lignan glycoside
8
pc3 hepg2
8
confirmed vivo
8
rare naturally-occurring
8
methanol extract
8
hepatoprotective activity
8
oxidative stress
8
phytochemical investigation
8
extract
5
activity
5
drug silymarin
4
values emm
4
protocolresults values
4
silymarin emm
4
c-docker protocolresults
4
emm >500µg/ml
4
standard drug
4

Similar Publications