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The objective of the present study was to characterize the action of perilla leaf extract (PLE) and its subfractions and describe its enhancing the activity of γ-glutamylcysteine synthetase (GCS) in a human hepatoma cell culture model.The leaves ofperilla (Perilla frutescens Britton var.japonica Hara) are often used in Asian gourmet food.In solvent extraction from aqueous extract of perilla leaves (PLE-0),we got 5 organic solvent-soluble layers that PLE-Ⅰ (n-hexane-soluble layer),PLE-Ⅱ (chloroform-soluble layer),PLE-Ⅲ(ethyl acetate-soluble layer),PLE-Ⅳ (n-butanol-soluble layer) and PLE-Ⅴ (water-soluble residue layer).PLE-Ⅲ shows the most efficacious on γ-GCS activity on HepG2 cells that were isolated from the ethyl acetate layer of PLE by consecutive solvent partitioning.