A New P-Glycoprotein Inhibitor from the Caper Spurge (Euphorbia l athyris)

The macrocyclic lathyrane polyester Euphorbia factor L10 (1a) has been obtained from the seeds of the caper spurge (E. lathyris). The interaction of L10 (1a) and its acetyl derivative (1b) with P-glycoprotein, a multidrug transporter overexpressed in cancer cells and responsible for resistance to ch...

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Bibliographic Details
Published in:	Journal of natural products (Washington, D.C.) Vol. 66; no. 1; pp. 140 - 142
Main Authors:	Appendino, Giovanni, Della Porta, Carla, Conseil, Gwenaëlle, Sterner, Olov, Mercalli, Enrico, Dumontet, Charles, Di Pietro, Attilio
Format:	Journal Article
Language:	English
Published:	Washington, DC American Chemical Society 01-01-2003 Glendale, AZ American Society of Pharmacognosy
Subjects:	ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors Biochemistry, Molecular Biology Biological and medical sciences Chemical Sciences Diterpenes - chemistry Diterpenes - isolation & purification Diterpenes - pharmacology Drug Resistance, Multiple Drug Resistance, Neoplasm Drug Screening Assays, Antitumor Euphorbia - chemistry General pharmacology Germany Humans K562 Cells - drug effects Kemi Leukemia Life Sciences Medical sciences Molecular Structure Natural Sciences Naturvetenskap Organic Chemistry Organisk kemi Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments Plants, Medicinal - chemistry Seeds - chemistry Tumor Cells, Cultured - drug effects Europe Germany Euphorbia lathyris Seeds Leukemia Ketol P Glycoprotein Alcohol Medicinal plant Dicotyledones Multiple resistance Angiospermae Euphorbiaceae Inhibition Acylate Tumor cell Carrier protein Human Transmembrane protein Terpenoid Pharmacognosy Tetracyclic compound In vitro Biological activity Cell line Plant origin Diterpene Isolation Spermatophyta Enone Structural analysis
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Summary:	The macrocyclic lathyrane polyester Euphorbia factor L10 (1a) has been obtained from the seeds of the caper spurge (E. lathyris). The interaction of L10 (1a) and its acetyl derivative (1b) with P-glycoprotein, a multidrug transporter overexpressed in cancer cells and responsible for resistance to chemotherapy, was investigated. The results established lathyrane diterpenoids as a novel chemotype for P-glycoprotein inhibitors.
Bibliography:	ark:/67375/TPS-QRDGB3MV-D istex:DAF2025FB85BB492BF15AA319DC57403010D2966 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0163-3864 1520-6025
DOI:	10.1021/np0203537