Biography:

Abstract:

Berberis vulgaris has been used extensively in traditional medicine to treat a number of diseases. The aim of this study is to evaluate and compare the bioactivities of the ethanolic extract of Berberis vulgaris roots (BVEtOH), isolated berberine (BB) and two semi-synthesized compounds; berberrubine (M1) and di-berberine sulfate (Di-BB). These bioactivities included; cytotoxic, anti-hepatitis C virus, anticholinesterase and antioxidant effects. Berberine was isolated from BV as free base and iodide salt and was used for the semi-synthesis of M1 and Di-BB. Berberine content of the BVEtOH was analyzed by HPLC. The compounds were identified using possible spectral analyses such as IR, 1H-NMR, 13C- NMR and LC/MS. The ethanolic extract and all compounds showed significant cytotoxic effects with small IC50 against three types of tumor cell lines; HepG-2, MCF-7 and Caco-2. Compounds were also investigated for in vitro effect on the replication of HCV-RNA in peripheral blood mononuclear cells (PBMCs) infected with the virus. Out of the tested samples, only three proved to inhibit the viral replication inside the infected cells as evidence by the absence of a fragment at 174 bp, identified in positive control. The ethanolic extract, berberine and di-berberine sulfate were able to inhibit the replication of RNA at a dose of 100 mg/mL. Both berberine chloride and iodide were inactive as antiviral. For in vitro liver anticholinesterase activity, all compounds showed inhibitory effects on the enzyme with different IC50. Our compounds also showed antioxidant activity towards in vitro induced lipid peroxidation in mice liver homogenate as evidence by decreasing malondialdehyde (MDA) level. Our findings suggest that BVEtOH, its isolated berberine, M1 and Di-BB have cytotoxic, antiviral, anticholinesterase and antioxidant activities.