2. Academic Validation
  3. Antiplatelet activity of loureirin A by attenuating Akt phosphorylation: In vitro studies

Antiplatelet activity of loureirin A by attenuating Akt phosphorylation: In vitro studies

  • Eur J Pharmacol. 2015 Jan 5;746:63-9. doi: 10.1016/j.ejphar.2014.10.059.
Hong-Zhen Hao 1,  Ao-Di He 2,  Dao-Chun Wang 3,  Zhao Yin 2,  Ya-Jun Zhou 2,  Gang Liu 2,  Ming-Lu Liang 2,  Xing-Wen Da 2,  Guang-Qiang Yao 2,  Wen Xie 2,  Ji-Zhou Xiang 2,  Zhang-Yin Ming 4
Affiliations

Affiliations

  • 1 Department of Pharmacology, School of Basic Medicine, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China; Department of Pharmacy, The First Affiliated Hospital of Shantou University Medical College, Shantou, Guangdong 515041, China.
  • 2 Department of Pharmacology, School of Basic Medicine, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China.
  • 3 Department of Traditional Chinese Medicine, Renmin Hospital of Wuhan University, Wuhan 430060, China.
  • 4 Department of Pharmacology, School of Basic Medicine, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China. Electronic address: [email protected].
PMID: 25445049 DOI: 10.1016/j.ejphar.2014.10.059
Abstract

Loureirin A is a flavonoid extracted from Dragon׳s Blood that has been used to promote blood circulation and remove stasis in Chinese traditional medicine. However, the mechanisms of these effects are not fully understood. We explored the anti-platelet activity and underlying mechanism of loureirin A in vitro. Our results indicated that loureirin A negatively affected agonist-induced platelet aggregation such as collagen, collagen-related peptide (CRP), ADP and Thrombin. Loureirin A inhibited collagen-induced platelet ATP secretion and thrombin-stimulated P-Selectin expression in a dose-dependent manner. Platelet spreading on immobilized fibrinogen was significantly impaired in the presence of loureirin A. Immunoblotting analysis indicated that 100μM of loureirin A almost completely eliminated collagen-induced Akt phosphorylation at Ser473. Interestingly, a submaximal dose (50μM) of loureirin A had an additive inhibitory effect with the phosphoinositide 3-kinase (PI3K) inhibitor Ly294002 on collage-induced Akt phosphorylation in platelets. Taken together, loureirin A had an inhibitory effect on platelet activation, perhaps through an impairment of PI3K/Akt signaling.

Keywords

Aggregation; Loureirin A; PI3K/Akt; Platelet; Spreading.

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