Polyphenol-based targeted therapy for oral submucous fibrosis

Area of Science:

• Biomedical Science
• Pharmacology
• Oral Medicine

Background:

• Oral submucous fibrosis (OSF) is a chronic, precancerous condition linked to areca nut use.
• Current treatments like corticosteroid injections offer limited success in managing OSF.
• Developing novel, safer therapeutic agents is crucial for effective OSF management.

Purpose of the Study:

• To identify and evaluate potential polyphenol compounds for oral submucous fibrosis (OSF) therapy.
• To assess the efficacy of epigallocatechin-3-gallate (EGCG) in preclinical models of OSF.
• To investigate EGCG's potential as a safer and more effective treatment for OSF.

Main Methods:

• In silico screening identified promising polyphenols, including EGCG, with high affinity for TGF-β1 and LOX targets.
• In vitro studies evaluated EGCG and quercetin (QUR) on buccal mucosal fibroblasts.
• In vivo studies utilized an areca nut extract-induced rat OSF model to test EGCG hydrogel efficacy.

Main Results:

• EGCG demonstrated superior efficacy and safety over QUR in reducing TGF-β1 and collagen mRNA expression in vitro.
• In vivo, EGCG hydrogel significantly improved OSF conditions, reduced TGF-β1 and collagen levels, and increased mouth opening compared to betamethasone.
• EGCG exhibited antioxidant and anti-inflammatory effects, modulating key fibrotic pathways.

Conclusions:

• Epigallocatechin-3-gallate (EGCG) is a potent phytomolecule with significant therapeutic potential for oral submucous fibrosis (OSF).
• EGCG hydrogel offers a safer, more effective treatment option with improved patient compliance and no reported side effects.
• Further clinical investigation of EGCG topical formulations for OSF is warranted.