ORIGINAL RESEARCH article
Front. Nutr.
Sec. Food Chemistry
Comparative Inhibitory Effects of Phillyrin and Phillygenin on Elastase: Mechanisms and Therapeutic Potential
Provisionally accepted
- 1The Second Hospital of Tianjin Medical University, Tianjin, China
- 2Changchun Normal University, Changchun, China
- 3The First Hospital of Jilin University, Changchun, China
- 4Department of Neurosurgical Oncology, First Hospital of Jilin University, Changchun, Jilin Province, China
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Elastase, a serine protease, has been implicated in chronic obstructive pulmonary disease and systemic inflammatory response syndrome. In this study, we evaluated the effects of phillyrin and phillygenin, two major Forsythia lignans, on elastase inhibition. Both compounds exhibited competitive inhibition, as confirmed by enzymatic kinetics, spectroscopy, and molecular docking. Phillygenin exhibited stronger activity (IC50 0.5 mmol/L, Ki 4.0 × 10⁻⁴ mol/L) than phillyrin (IC50 1.5 mmol/L, Ki 9.7 × 10⁻⁴ mol/L), likely due to reduced steric hindrance. Spectroscopic analysis revealed ligand-induced conformational changes in elastase, characterized by increased α-helix and random coil content and decreased β-sheet structures. Docking revealed interactions involving π-cation, π-sigma, hydrogen bonds, hydrophobic forces, electrostatics, and van der Waals effects. These results provide mechanistic insights into the inhibitory effects of phillyrin and phillygenin and highlight their potential as therapeutic agents for elastase-related diseases.
Keywords: elastase, inhibition, Lignan compounds, molecular docking, Phillygenin, phillyrin
Received: 13 Oct 2025; Accepted: 13 Jan 2026.
Copyright: © 2026 Zhang, Fu, Lin, Yao, Li, Wang, MO and Guan. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence: Yi Guan
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