Yu Jia,Ya-qiong Zhang,Tong-dan Liu,Meng-yuan Xia,Chun-lin Long,Li Wang,Yue-hu Wang,Yi Kong.Chemical constituents from heartwoods of Caesalpinia sappan with antiplatelet aggregation activities[J].Chinese Herbal Medicines (CHM),2019,11(4):423-428
Chemical constituents from heartwoods of Caesalpinia sappan with antiplatelet aggregation activities
  
DOI:10.1016/j.chmed.2019.09.001
中文关键词:  
英文关键词:antiplatelet aggregation  Caesalpinia sappan  phenols  protease-activated receptor 4
基金项目:
Author NameAffiliation
Yu Jia a Yunnan Agricultural University, Kunming 650201, China c Key Laboratory of Economic Plants and Biotechnology and Yunnan Key Laboratory for Wild Plant Resources, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China 
Ya-qiong Zhang b School of Life Science & Technology, China Pharmaceutical University, Nanjing 210009, China 
Tong-dan Liu b School of Life Science & Technology, China Pharmaceutical University, Nanjing 210009, China 
Meng-yuan Xia a Yunnan Agricultural University, Kunming 650201, China c Key Laboratory of Economic Plants and Biotechnology and Yunnan Key Laboratory for Wild Plant Resources, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China 
Chun-lin Long d College of Life and Environmental Sciences, Minzu University of China, Beijing 100081, China 
Li Wang a Yunnan Agricultural University, Kunming 650201, China 
Yue-hu Wang c Key Laboratory of Economic Plants and Biotechnology and Yunnan Key Laboratory for Wild Plant Resources, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China 
Yi Kong b School of Life Science & Technology, China Pharmaceutical University, Nanjing 210009, China 
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中文摘要:
      
英文摘要:
      Objective To clarify the active constituents of the heartwoods of Caesalpinia sappan, a traditional Chinese medicine with the functions of promoting blood circulation (Huoxue in Chinese) and removing blood stasis (Quyu in Chinese). Methods The chemical constituents were isolated and purified by combination of silica gel and Sephadex LH-20 column chromatography, along with semipreparative HPLC. Their chemical structures were established by multiple spectroscopic methods and comparison with literature data. The in vitro antiplatelet aggregation activities were evaluated using mouse platelet induced by AYPGKF-NH2, a gold agonist of protease-activated receptor 4 (PAR4). Results Two new phenols, methyl 2-(4,4′,5′-trihydroxy-2′-(methoxymethyl) biphenyl-2-yloxy) acetate (1) and 1′-methylcaesalpin J (2), together with 24 known compounds (3-26), were isolated from the heartwoods of C. sappan. Among them, sappanchalcone (16) and brazilin (20) showed inhibitory activities against mouse platelet aggregation with IC50 values of 114.8 μmol/L and 100.8 μmol/L, respectively. Conclusion Antiplatelet compounds from C. sappan targeting at PAR4 are reported for the first time.
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