2. Academic Validation
  3. Efficient Discovery of Syk-Targeting Phenolic Acids from Orthosiphon aristatus and Their Antiplatelet Activities

Efficient Discovery of Syk-Targeting Phenolic Acids from Orthosiphon aristatus and Their Antiplatelet Activities

  • J Agric Food Chem. 2025 Dec 25. doi: 10.1021/acs.jafc.5c12916.
Guoqing Qin 1 2,  Wanmin Sha 3,  Mingge Zhang 1 2,  Biling Li 3,  Pengju Guo 1 4,  Chenxi Wang 1,  Wenqiong Wang 1 2,  Liang Hu 3,  Lijiang Xuan 1 2
Affiliations

Affiliations

  • 1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai 201203, China.
  • 2 University of Chinese Academy of Sciences, No.19A Yuquan Road, Beijing 100049, China.
  • 3 The Research Center for Cardiovascular diseases, The Research Center for Traditional Chinese Medicine, Shanghai Institute of Infectious Diseases and Biosecurity, School of Integrative Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
  • 4 School of Pharmacy, Fudan University, Shanghai 201203, China.
PMID: 41449956 DOI: 10.1021/acs.jafc.5c12916
Abstract

Orthosiphon aristatus is widely used as a popular functional tea in Southeast Asian countries. A TLC/UPLC-TOF-MS/polymeric MDF strategy was designed to guide the isolation of 25 phenolic acids (PAs) from O. aristatus, including 14 new compounds (1-14). Through extensive spectroscopic analysis, the structures of the compounds were elucidated. Additionally, plausible biosynthetic pathways were deduced. The antiplatelet aggregation activities of the PAs were evaluated. Compounds of the salvianolic acid type exhibited broad-spectrum antiplatelet effects, with compound 17 demonstrating the most potent effect in a concentration-dependent manner. Bicyclo[2.2.2]octane-type PAs were highly specific to collagen-induced aggregation, with 22 demonstrating the most potent effect. It has been further confirmed that active bicyclo[2.2.2]octane-type PAs (22 and 23) can directly interact and inhibit Syk and then inhibit the GPVI pathway, which is unique to collagen-induced aggregation. The work laid the foundation for the further development of O. aristatus as a cardiovascular health supplement.

Keywords

Orthosiphon aristatus; antiplatelet activities; phenolic acids; polymeric MDF technology.

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