Aqueous extract of Rabdosia rubescens leaves: forming nanoparticles, targeting P-selectin, and inhibiting thrombosis

Autor: Feng Qiqi, Tang Jingcheng, Wenyun Xu, Ma Haiping, Jianhui Wu, Ming Zhao, Shiqi Peng, Haimei Zhu, Jiawang Liu, Xueyun Jiang, Yuji Wang
Jazyk: angličtina
Rok vydání: 2015
Předmět:
Blood Platelets
Male
Spectrometry
Mass
Electrospray Ionization
Magnetic Resonance Spectroscopy
antithrombotic ingredient
Platelet Aggregation
Biophysics
Pharmaceutical Science
Bioengineering
Depsides
Biomaterials
chemistry.chemical_compound
In vivo
International Journal of Nanomedicine
Drug Discovery
Antithrombotic
Hydroxybenzoates
Animals
Platelet
Platelet Activating Factor
Rats
Wistar
Blood Coagulation
Chromatography
High Pressure Liquid
Original Research
Chromatography
Arachidonic Acid
Platelet-activating factor
Plant Extracts
Rosmarinic acid
Organic Chemistry
Thrombin
Thrombosis
General Medicine
Flow Cytometry
Rats
Adenosine Diphosphate
Plant Leaves
Adenosine diphosphate
P-Selectin
chemistry
Biochemistry
Cinnamates
Isodon
Platelet aggregation inhibitor
R. rubescens
Nanoparticles
Arachidonic acid
sP-selectin
Platelet Aggregation Inhibitors
Zdroj: International Journal of Nanomedicine
ISSN: 1178-2013
1176-9114
Popis: Yuji Wang,1 Jingcheng Tang,1 Haimei Zhu,1 Xueyun Jiang,1 Jiawang Liu,1 Wenyun Xu,1 Haiping Ma,1 Qiqi Feng,1 Jianhui Wu,1 Ming Zhao,1,2 Shiqi Peng1 1Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, People’s Republic of China; 2Faculty of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung, Taiwan Abstract: The hot water extract of Rabdosia rubescens was traditionally used as an antithrombotic medicine. To explore its antithrombotic utility and mechanism, we carried out a series of invitro and invivo assays in this study. Invitro platelet aggregation assay showed that the half maximal inhibitory concentration values of aqueous extract of R. rubescens leaves (AERL) inhibiting platelet aggregation induced by thrombin, arachidonic acid, adenosine diphosphate, and platelet-activating factor ranged from 0.12 mg/mL to 1.43 mg/mL. The minimal effective oral dose of AERL inhibiting the rats from forming thrombus was 25 mg/kg. Both invitro and invivo actions were correlated with AERL concentration-dependently inhibiting sP-selectin release. In water, AERL formed nanoparticles, and their size depended on the concentration. Docking the five nucleotides, 21phenolic acids, and four diterpenoids identified by high-performance liquid chromatography–photodiode array detector/(-)electrospray ionization-tandem mass spectrometry analysis into the active site of P-selectin, rosmarinic acid was predicted to be the antithrombotic ingredient of AERL. In flow cytometry analysis, 1 µM of rosmarinic acid effectively inhibited sP-selectin release in arachidonic acid-activated platelets. In a rat model, 5 mg/kg of oral rosmarinic acid effectively inhibited thrombosis. Keywords: R. rubescens, sP-selectin, antithrombotic ingredient 
Databáze: OpenAIRE
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