Abstract
Scutellarin (1) has been widely used to treat acute cerebral infarction in clinic, but poor aqueous solubility decreases its bioavailability. Interestingly, scutellarin (1) could be metabolized into scutellarein (2) in vivo. In this study, a sulfonic group was introduced at position C-8 of scutellarein (2) to enhance the aqueous solubility of the obtained derivative (3). DPPH (1,1-diphenyl-2-picrylhydrazyl)-radical scavenging ability and antithrombic activity were also conducted to determine its bioactivity. The result showed that scutellarein derivate (3) could be a better agent for ischemic cerebrovascular disease treatment.
Keywords:
antioxidant; antithrombic; scutellarein; scutellarin; solubility; sulfonated derivative.
MeSH terms
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Animals
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Antioxidants / chemical synthesis
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Antioxidants / chemistry
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Antioxidants / pharmacology
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Apigenin / chemical synthesis
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Apigenin / chemistry
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Apigenin / pharmacology
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Biphenyl Compounds / metabolism
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Brain Ischemia / drug therapy
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Cerebrovascular Disorders / drug therapy
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Chromans / chemical synthesis*
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Chromans / chemistry
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Chromans / pharmacology
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Chromans / therapeutic use
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Erigeron / chemistry
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Fibrinolytic Agents / chemical synthesis*
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Fibrinolytic Agents / pharmacology
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Fibrinolytic Agents / therapeutic use
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Free Radical Scavengers / chemical synthesis
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Free Radical Scavengers / chemistry
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Free Radical Scavengers / pharmacology
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Glucuronates / chemistry
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Glucuronates / pharmacology
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Humans
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Male
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Picrates / metabolism
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Rabbits
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Solubility
Substances
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5,6,7-trihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromene-8-sulfonic acid
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Antioxidants
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Biphenyl Compounds
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Chromans
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Fibrinolytic Agents
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Free Radical Scavengers
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Glucuronates
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Picrates
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scutellarin
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Apigenin
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1,1-diphenyl-2-picrylhydrazyl
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scutellarein