Abstract
Stepwise modification of ovatodiolide revealed a prodrug, NMP-diepoxyovatodiolide, which can provide sustained release of an active compound, substantial metabolic stability and a unique accumulation profile in the liver. Besides, NMP-diepoxyovatodiolide demonstrated therapeutic benefits in an acute autoimmune hepatitis mouse model and a broad safety window. Therefore, NMP-diepoxyovatodiolide is a very promising candidate for further development of liver-related drugs.
MeSH terms
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Animals
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Disease Models, Animal
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Diterpenes / administration & dosage
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Diterpenes / chemistry
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Diterpenes / pharmacokinetics*
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Hepatitis, Autoimmune / drug therapy*
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Hepatitis, Autoimmune / metabolism
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Mice
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Mice, Inbred C57BL
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Microsomes, Liver / chemistry
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Microsomes, Liver / metabolism
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Molecular Structure
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Prodrugs / administration & dosage
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Prodrugs / chemistry
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Prodrugs / pharmacokinetics*
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Rats
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Rats, Sprague-Dawley
Substances
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Diterpenes
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Prodrugs
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ovatodiolide