Apiin from sugarcane leaves modulates postprandial hyperglycemia by targeting dipeptidyl peptidase IV, α-amylase, and...

Postprandial hyperglycemia is a metabolic abnormality that can emerge early in the progression toward type 2 diabetes and is closely associated with insulin resistance. Sugarcane leaves, an underutilized by-product of sugar production, are rich in flavonoids and therefore represent a promising source of bioactive compounds for glycemic control.

In the present study, 37 phytochemicals previously identified from sugarcane leaves were screened by toxicity prediction and molecular docking against three key targets involved in postprandial glucose regulation, namely dipeptidyl peptidase IV (DPP-IV), α-amylase, and α-glucosidase. Apiin was identified as the most promising candidate and was further evaluated by in vitro enzyme inhibition assays and in vivo validation in high-fat-diet-induced insulin-resistant (IR) mice. Apiin exhibited encouraging inhibitory activity against DPP-IV, α-amylase, and α-glucosidase, with IC₅₀ values of 0.21 ± 0.02, 0.10 ± 0.01 and 0.14 ± 0.02 mg mL^-1, respectively. Molecular docking further indicated that hydrogen bonding played a major role in apiin binding to DPP-IV and α-amylase, whereas hydrophobic and sulfur-X interactions contributed to its recognition by α-glucosidase. Oral administration of apiin significantly reduced postprandial blood glucose excursion and decreased the area under the glucose curve in IR mice.

These findings demonstrate that apiin is a major bioactive constituent of sugarcane leaves with the potential to modulate postprandial glucose homeostasis and support the valorization of sugarcane leaves as a functional food resource. © 2026 Society of Chemical Industry.