Abstract
Selaginpulvilins A-D (1-4), four new phenols with an unprecedented 9,9-diphenyl-1-(phenylethynyl)-9H-fluorene skeleton, together with four known selaginellins (5-8) were isolated from Selaginella pulvinata. Their structures were elucidated by spectroscopic analysis and chemical correlation. The structure of 1 was confirmed by single-crystal X-ray diffraction. Compounds 1-8 exhibited remarkable inhibitory activities (IC50 values in the range of 0.11-5.13 μM) against phosphodiesterase-4 (PDE4), a drug target for the treatment of asthma and chronic obstructive pulmonary disease.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Biological Products / chemistry
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Biological Products / isolation & purification
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Biological Products / pharmacology*
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Crystallography, X-Ray
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Cyclic Nucleotide Phosphodiesterases, Type 4 / metabolism*
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Dose-Response Relationship, Drug
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Fluorenes / chemistry*
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Fluorenes / pharmacology*
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Humans
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Models, Molecular
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Molecular Structure
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Phosphodiesterase 4 Inhibitors / chemistry
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Phosphodiesterase 4 Inhibitors / isolation & purification
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Phosphodiesterase 4 Inhibitors / pharmacology*
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Selaginellaceae / chemistry*
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Structure-Activity Relationship
Substances
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9,9-diphenyl-1-(phenylethynyl)-9H-fluorene
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Biological Products
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Fluorenes
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Phosphodiesterase 4 Inhibitors
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Cyclic Nucleotide Phosphodiesterases, Type 4