title: Antiplatelet activity of loureirin A by attenuating Akt phosphorylation: In vitro studies.
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.
authors.affiliation: 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.
authors.forename: Hong-Zhen
authors.initials: HZ
authors.lastname: Hao
authors.affiliation: 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.
authors.forename: Ao-Di
authors.initials: AD
authors.lastname: He
authors.affiliation: Department of Traditional Chinese Medicine, Renmin Hospital of Wuhan University, Wuhan 430060, China.
authors.forename: Dao-Chun
authors.initials: DC
authors.lastname: Wang
authors.affiliation: 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.
authors.forename: Zhao
authors.initials: Z
authors.lastname: Yin
authors.affiliation: 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.
authors.forename: Ya-Jun
authors.initials: YJ
authors.lastname: Zhou
authors.affiliation: 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.
authors.forename: Gang
authors.initials: G
authors.lastname: Liu
authors.affiliation: 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.
authors.forename: Ming-Lu
authors.initials: ML
authors.lastname: Liang
authors.affiliation: 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.
authors.forename: Xing-Wen
authors.initials: XW
authors.lastname: Da
authors.affiliation: 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.
authors.forename: Guang-Qiang
authors.initials: GQ
authors.lastname: Yao
authors.affiliation: 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.
authors.forename: Wen
authors.initials: W
authors.lastname: Xie
authors.affiliation: 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.
authors.forename: Ji-Zhou
authors.initials: JZ
authors.lastname: Xiang
authors.affiliation: 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: zyming@mail.hust.edu.cn.
authors.forename: Zhang-Yin
authors.initials: ZY
authors.lastname: Ming
mesh_terms: D000255:Adenosine Triphosphate / Q000378:metabolism; D000818:Animals; D001792:Blood Platelets / Q000187:drug effects / Q000502:physiology; D047188:Chalcones / Q000494:pharmacology*; D005340:Fibrinogen / Q000737:chemistry / Q000378:metabolism; D005786:Gene Expression Regulation / Q000187:drug effects; D006801:Humans; D055767:Immobilized Proteins / Q000737:chemistry / Q000378:metabolism; D008297:Male; D051379:Mice; D019007:P-Selectin / Q000378:metabolism; D010766:Phosphorylation / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D051057:Proto-Oncogene Proteins c-akt / Q000378:metabolism*; D013917:Thrombin / Q000494:pharmacology
chemical_list: D047188:Chalcones; D055767:Immobilized Proteins; D019007:P-Selectin; D010936:Plant Extracts; D010975:Platelet Aggregation Inhibitors; C560420:loureirin A; D000255:Adenosine Triphosphate; D005340:Fibrinogen; D051057:Proto-Oncogene Proteins c-akt; D013917:Thrombin; C525191:dragon's blood
keywords: Aggregation; Loureirin A; PI3K/Akt; Platelet; Spreading