Abstract
A series of 2a-i were prepared from a lead compound, saucerneol B (1) for evaluating their acyl-CoA: cholesterol acyltransferase inhibitory activities. Compounds 2a-g exhibited the high specificity of hACAT-1 than hACAT-2, whereas 2h and 2i showed very weak inhibitory activities in both hACAT-1 and hACAT-2. Saucerneol B (1) exhibited strong cholesterol-lowering effect in high cholesterol-fed mice.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acyl Coenzyme A / metabolism*
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Animals
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Anticholesteremic Agents / chemical synthesis*
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Anticholesteremic Agents / pharmacology
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Furans / chemical synthesis*
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Furans / pharmacology
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Humans
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Keratinocytes / drug effects*
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Keratinocytes / metabolism
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Lignans / chemical synthesis*
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Lignans / pharmacology
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Mice
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Sterol O-Acyltransferase / antagonists & inhibitors*
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Sterol O-Acyltransferase / metabolism
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Structure-Activity Relationship
Substances
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Acyl Coenzyme A
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Anticholesteremic Agents
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Furans
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Lignans
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saucerneol B
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Sterol O-Acyltransferase