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PP-07

Therapeutic potential and molecular docking analysis of bioactive extracts

and components from Polygonum aviculare: Antioxidant, anti-α-glucosidase,

and anti-inflammation via M1/M2 macrophage modulation

2
#,1
Yuen-Sing Lee, Sin-Min Li, Jih-Jung Chen* ,1,2

1 Biomedical Industry Ph.D. Program, College of Life Sciences, National Yang Ming Chiao
Tung University, Taipei 112304, Taiwan
2 Department of Pharmacy, College of Pharmaceutical Sciences, National Yang Ming Chiao
Tung University, Taipei 112304, Taiwan
* E-mail: jjungchen@nycu.edu.tw

Abstract
The aerial parts of Polygonum aviculare have been used in traditional Chinese medicine to
treat inflammation and metabolic dysfunction. In our study, the bioactivities of various solvent
extracts were evaluated. The methanol extract showed the highest total flavonoid content (TFC)
and the strongest DPPH scavenging ability, while the 100°C water extract showed the highest
total phenolic content (TPC) and the strongest antioxidant effect in ABTS, superoxide, and
FRAP assays. The acetone extract showed the strongest NO inhibitory activity. Compound 3
showed superior antioxidant capacity in the FRAP assay (TE = 25511.50 ± 88.61 mM/g), which
was significantly higher than the positive control BHT (TE = 4561.78 ± 12.93 mM/g).
Compounds 1 (IC50 = 12.60 ± 2.03 μM), 3 (IC50 = 5.04 ± 1.25 μM), and 9 (IC50 = 15.06 ± 1.50
μM) exhibited strong anti-NO activities, surpassing the positive control apigenin (IC50 = 15.08
± 1.86 μM). Compound 9 exhibited the most potent α-glucosidase inhibitory activity (IC50 =
4.50 ± 0.90 µM), demonstrated strong anti-NO activity, and downregulated iNOS, COX-2, and
p-p38, while also restoring KLF4 and Arg-1 expression, indicating M2 macrophage polarization.
Molecular docking supported these findings, with compound 3 showing the highest binding
affinities to α-glucosidase (–8.6 kcal/mol) and iNOS (–9.0 kcal/mol), followed by compound 9
(α-glucosidase: –8.5 kcal/mol and iNOS: –8.6 kcal/mol). These results highlight P. aviculare
and its bioactive components as potential multifunctional natural agents for the treatment of
oxidative stress, hyperglycemia, and inflammatory diseases.

Keywords: Polygonum aviculare; Flavonoids; Traditional Chinese Medicine