Abstract
Bioassay guided fractionation of the ethanolic extract of Polyalthia longifolia var. pendula, led to the discovery of the clerodane diterpene, 16α-hydroxycleroda-3, 13 (14) Z-dien-15, 16-olide (1), as a new structural class of HMG-CoA reductase inhibitor. Importantly, the in vivo effects of 1 corroborated well with its molecular docking analysis and also with its hamster plasma pharmacokinetics.
Copyright © 2011 Elsevier Masson SAS. All rights reserved.
MeSH terms
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Animals
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Cricetinae
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Diterpenes, Clerodane / blood
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Diterpenes, Clerodane / chemistry
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Diterpenes, Clerodane / isolation & purification
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Diterpenes, Clerodane / pharmacology*
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Humans
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Hydroxymethylglutaryl CoA Reductases / chemistry
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Hydroxymethylglutaryl CoA Reductases / metabolism
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Hydroxymethylglutaryl-CoA Reductase Inhibitors / blood
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Hydroxymethylglutaryl-CoA Reductase Inhibitors / chemistry
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Hydroxymethylglutaryl-CoA Reductase Inhibitors / isolation & purification
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Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacology*
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Hypolipidemic Agents / blood
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Hypolipidemic Agents / chemistry
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Hypolipidemic Agents / isolation & purification
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Hypolipidemic Agents / pharmacology*
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Lipid Metabolism / drug effects
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Lipids / blood
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Male
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Models, Molecular
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Plant Extracts / blood
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Plant Extracts / chemistry
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Plant Extracts / isolation & purification
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Plant Extracts / pharmacology*
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Polyalthia / chemistry*
Substances
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Diterpenes, Clerodane
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Hydroxymethylglutaryl-CoA Reductase Inhibitors
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Hypolipidemic Agents
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Lipids
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Plant Extracts
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Hydroxymethylglutaryl CoA Reductases