Abstract
Three new triterpenoids, celastrusins A-C (1-3), together with 3-O-caffeoyl-α-amyrin (4) were isolated from the root bark of Celastrus orbiculatus. Their structures were identified by spectroscopic analysis, X-ray crystallography using Cu Kα radiation, and the comparison of both observed and reported spectroscopic data. An in vitro bioassay revealed that the caffeoyl triterpenoid esters 1, 3, and 4 possess neuroprotective effects against oxygen-glucose deprivation (OGD) induced SH-SY5Y cell damage. Further animal studies indicated that compound 1 significantly reduced brain infarction after transient middle cerebral artery occlusion (MCAO) in rats using a 10 mg/kg (i.v.) dose.
MeSH terms
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Animals
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Caffeic Acids / chemistry
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Caffeic Acids / isolation & purification*
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Caffeic Acids / pharmacology*
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Celastrus / chemistry*
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Cerebral Arterial Diseases / drug therapy
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Crystallography, X-Ray
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Dose-Response Relationship, Drug
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Drugs, Chinese Herbal / chemistry
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Drugs, Chinese Herbal / isolation & purification*
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Drugs, Chinese Herbal / pharmacology*
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Esters
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Humans
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Ischemia / drug therapy*
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Male
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Molecular Conformation
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Molecular Structure
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Neuroprotective Agents / chemistry*
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Neuroprotective Agents / isolation & purification*
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Neuroprotective Agents / pharmacology*
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Nuclear Magnetic Resonance, Biomolecular
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Oleanolic Acid / analogs & derivatives
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Plant Bark / chemistry
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Plant Roots / chemistry
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Rats
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Triterpenes / chemistry
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Triterpenes / isolation & purification*
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Triterpenes / pharmacology*
Substances
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Caffeic Acids
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Drugs, Chinese Herbal
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Esters
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Neuroprotective Agents
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Triterpenes
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celastrusin A
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celastrusin B
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celastrusin C
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Oleanolic Acid
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beta-amyrin