2. Academic Validation
  3. Screening of direct thrombin inhibitors from Radix Salviae Miltiorrhizae by a peak fractionation approach

Screening of direct thrombin inhibitors from Radix Salviae Miltiorrhizae by a peak fractionation approach

  • J Pharm Biomed Anal. 2015 May 10;109:85-90. doi: 10.1016/j.jpba.2015.02.020.
Jun Lu 1,  Hui-Peng Song 1,  Ping Li 2,  Ping Zhou 1,  Xin Dong 1,  Jun Chen 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Natural Medicines, China Pharmaceutical University, No. 24 Tongjia Lane, Nanjing, 210009, China.
  • 2 State Key Laboratory of Natural Medicines, China Pharmaceutical University, No. 24 Tongjia Lane, Nanjing, 210009, China. Electronic address: [email protected].
  • 3 State Key Laboratory of Natural Medicines, China Pharmaceutical University, No. 24 Tongjia Lane, Nanjing, 210009, China. Electronic address: [email protected].
PMID: 25819728 DOI: 10.1016/j.jpba.2015.02.020
Abstract

Thrombin plays a significant role in thromboembolic disease. In this work, a peak fractionation approach combined with an activity assay method was used to screen direct Thrombin inhibitors from Radix Salviae Miltiorrhizae (RSM), a famous herbal remedy for the treatment of cardiovascular diseases in China. A total of 91 fractions were collected from the RSM extract, and 19 fractions out of them showed Thrombin inhibitory effects with dose-effect relationship. Among them, three compounds were unambiguously identified as 15, 16-dihydrotanshinone I, cryptotanshinone and tanshinone IIA with IC50 values of 29.39, 81.11 and 66.60μM, respectively. The three compounds were reported with direct Thrombin inhibition activities for the first time and their ligand-thrombin interactions were explored by a molecular docking research. These results may contribute to explain the medical benefit of RSM for the prevention and treatment of cardiovascular diseases.

Keywords

High-throughput screening; Peak fractionation; QTOF mass spectrometry; Radix Salviae Miltiorrhizae; Thrombin inhibitor.

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