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The antidiabetic effects of Ge-Gen-Qin-Lian-Tang decoction (GQD) have been proven clinically.In the pharmacological study conducted on STZ-induced diabetic rats, its constitutive aggregates/sediments exhibited stronger hypoglycemic and antioxidant activities than the soluble compositions.This study aims to demonstrate the pharmacological properties of aggregates derived from GQD by measuring permeability of the active monomer phytochemicals (i.g.baicalin) upon Caco-2 cell monolayer and determination of the cellular viability,intracellularly redox status (MDA, SOD) and insulin secretion of pancreatic β-cell INS-1, at the presence of STZ-induced oxidative stress.The aggregates were separated into three fractions namely 400g sediment, 400g supernatant and 15000g sediment by centrifuging at 400 g and 15000 g.Aggregates in the sediment increased the baicalin absorption, showed little toxicity upon pancreatic cells, elevated intracellular SOD level and significantly suppressed the oxidative damages on cellular viability and functions.The 400g sediment had larger particle size and conducted more potent in vitroeffects than the 15000g sediment, implying even the sediments may have contributed to the antidiabetic effectsof the herbal decoction.The action of supermolecular complex and micro/nano-aggregates may provide a new perspective for comprehension of antidiabetic effects of herbal decoction, and a novel model for interpretation of synergistic action among the multiple compositions.