A chlorinated 2-(2-phenylethyl)chromone in artificial agarwood as a DRD5 agonist and mediates the cAMP/Ca²⁺ signaling pathway to intervene in the growth and proliferation of gastric cancer cells
A chlorinated 2-(2-phenylethyl)chromone from artificial agarwood of Aquilaria sinensis was identified as a dopamine receptor D5 (DRD5) agonist. Comprehensive analyses the protein–protein interaction network, molecular docking, ADMET prediction, and molecular dynamics simulation revealed strong DRD5 binding and modulation of the cAMP/Ca²⁺ pathway in gastric cancer. The compound exhibited potent cytotoxic activity against MGC-803 and SGC-7901 cells in vitro. ADMET profiling revealed favorable pharmacokinetics and a promising safety profile. Compound CHE emerges as a promising lead therapeutic candidate for gastric cancer derived from agarwood. • The novel chlorinated chromone compound CHE is identified for the first time as a dopamine receptor D5 (DRD5) agonist. • Compound CHE inhibits gastric cancer cell proliferation and targets treatment through the cAMP/Ca 2 + pathway. • Compound CHE possesses excellent pharmacokinetic properties.
Authors
- Shu-Nan Zhang
- W Y Hou
- Yang Liu (ORCID: https://orcid.org/0000-0002-0367-8189)
- Jian Feng (ORCID: https://orcid.org/0000-0002-1177-9377)
- Zi-Xiao Jiang
- Mei-Ran Wang
Institutions
- Chinese Academy of Medical Sciences & Peking Union Medical College (CN)
- State Administration of Traditional Chinese Medicine of the People's Republic of China (CN)
- Hainan Provincial Hospital of Traditional Chinese Medicine (CN)
Publication Details
- Journal
- Phytochemistry Letters
- Published
- 2026-01-06
- DOI
- https://doi.org/10.1016/j.phytol.2026.104112
- Primary Topic
- Wood and Agarwood Research
- Type
- article
- Field-Weighted Citation Impact
- 0.00