Abstract
Thirteen jatrophane diterpenoids (1-10, 13-15), three previously isolated (11, 12, 16) and a known tigliane (17) were isolated from the latex of Euphorbia dendroides. The structures and relative configurations of compounds were elucidated by spectroscopic techniques. The P-glycoprotein (P-gp) inhibiting activities of the representative set of jatrophanes (1-6 and 11-16) have been assessed. Jatrophanes 2 and 5 demonstrated the most powerful inhibition of P-gp, higher than R(+)-verapamil and tariquidar in colorectal multi-drug resistant (MDR) cells (DLD1-TxR).
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors*
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology*
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Aporphines / chemistry
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Aporphines / pharmacology
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Cell Line, Tumor
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Cell Survival / drug effects
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Diterpenes / chemistry
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Diterpenes / pharmacology
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Drug Resistance, Neoplasm
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Euphorbia / chemistry*
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Humans
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Magnetic Resonance Spectroscopy
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Molecular Structure
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Quinolines / chemistry
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Quinolines / pharmacology
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Antineoplastic Agents
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Aporphines
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Diterpenes
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Quinolines
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aporphine
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tariquidar