Wang Yun, Li Xin-Yu, Wu Sheng-Li, Gongpan Pianchou, Yang Yi, Huang Mei, Li Da-Hong, Geng Chang-An
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; State Key Laboratory of Phytochemistry and Natural Medicines, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, People's Republic of China.
State Key Laboratory of Phytochemistry and Natural Medicines, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, People's Republic of China; University of Chinese Academy of Sciences, Beijing 100049, People's Republic of China.
Fitoterapia. 2025 Jun;183:106566. doi: 10.1016/j.fitote.2025.106566. Epub 2025 Apr 23.
Thirteen diarylheptanoids, including four undescribed ones (1-4), were isolated from the leaves of Amomum tsao-ko. Compounds 1 and 2 are two unusual diarylheptanoid-phenylpropanoid hybrids. Several of the isolates were tested for their biological activity in promoting GLP-1 secretion and inhibiting multiple type 2 diabetes-related enzymes. 2-Hydroxymusaitinerin A (1) demonstrated broad inhibitory activity against GPa, PTP1B and α-glucosidase with inhibition rates of 99.0 %, 59.4 % and 55.9 %, respectively at 200 μM. Platyphyllone (12) is a mixed-type inhibitor of α-glucosidase (IC = 25.8 μM), inhibiting the enzyme through both non-competitive and anti-competitive modes, as shown by enzyme kinetic study. Fluorescence quenching test confirmed that compound 12 directly interacted with α-glucosidase, forming a basal complex via a single binding site. Molecular docking predicted hydrogen-bonding interactions between OH-4'', OH-5 and 3‑carbonyl groups of 12 and α-glucosidase. This study highlights that the leaves of Amomum tsao-ko are a rich source of diarylheptanoids with multi-enzyme inhibitory effects.
