Abstract
New compounds bastadin 20 (9), 15,34-O-disulfatobastadin 7 (10), and 10-O-sulfatobastadin 3 (11) were isolated from Ianthella basta collected in Exmouth Gulf, Western Australia. Compounds 10 and 11 exhibited moderate differential activity as SR Ca2+ channel agonists (EC50 13.6 and 100 microM, respectively) of the Ry1R FKBP12 complex, while the potency of 9 was almost half that of 10 (EC50 20.6 microM). The problem of dereplication of bastadins was addressed using 1H-NMR "fingerprinting" of MeO signals in the corresponding permethyl bastadin derivatives.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Calcium Channel Agonists / chemistry*
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Calcium Channel Agonists / pharmacology
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Calcium Channels / drug effects
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Calcium Channels / metabolism*
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Cell Line
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Halogenated Diphenyl Ethers
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Magnetic Resonance Spectroscopy
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Muscle Proteins / drug effects
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Muscle Proteins / metabolism*
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Peptides, Cyclic / chemistry*
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Peptides, Cyclic / pharmacology
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Phenyl Ethers / chemistry*
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Phenyl Ethers / pharmacology
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Porifera / chemistry*
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Ryanodine Receptor Calcium Release Channel
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Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
Substances
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10-O-sulfatobastadin 3
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15,34-O-disulfatobastadin 7
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Calcium Channel Agonists
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Calcium Channels
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Halogenated Diphenyl Ethers
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Muscle Proteins
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Peptides, Cyclic
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Phenyl Ethers
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Ryanodine Receptor Calcium Release Channel
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bastadin 20