Enzymatic inhibitory activity of Ficus deltoidea leaf extract on matrix metalloproteinase-2, 8 and 9

Area of Science:

• Biochemistry
• Pharmacology
• Natural Products Chemistry

Background:

• Matrix metalloproteinases (MMPs) dysregulation is implicated in various pathological conditions, often characterized by elevated MMP activity.
• Ficus deltoidea (FD) is a plant recognized for its medicinal properties.
• Understanding the inhibitory effects of FD on MMPs could reveal new therapeutic strategies.

Purpose of the Study:

• To investigate the enzymatic inhibition properties of Ficus deltoidea leaf extract and its key compounds, vitexin and isovitexin, against MMP-2, MMP-8, and MMP-9.
• To explore the binding interactions of vitexin and isovitexin with MMP active sites using computational methods.
• To assess the cytotoxicity and anti-migratory effects of FD leaf extract on endothelial cells.

Main Methods:

• Enzymatic inhibition assays were performed on MMP-2, MMP-8, and MMP-9 using FD leaf extract, vitexin, and isovitexin.
• Computational molecular docking was employed to analyze the binding of vitexin and isovitexin to the active sites of the target MMPs.
• Cytotoxicity and cell migration assays were conducted using the EA.hy 926 endothelial cell line.

Main Results:

• FD leaf extract and its major bioactive compounds, vitexin and isovitexin, demonstrated significant inhibitory activity against MMP-2, MMP-8, and MMP-9.
• Molecular docking studies confirmed that vitexin and isovitexin bind to the active sites of the tested MMPs.
• FD leaf extract exhibited inhibitory effects on endothelial cell migration and showed no significant cytotoxicity.

Conclusions:

• Ficus deltoidea leaf extract possesses notable inhibitory effects on matrix metalloproteinases.
• Vitexin and isovitexin are key compounds in FD responsible for MMP inhibition, binding to their active sites.
• These findings support the therapeutic potential of Ficus deltoidea for pathological conditions associated with MMP dysregulation.