| Structure-activity relationship of seco-tanapartholides isolated from Achillea falcata for inhibition of HaCaT cell growth. | |
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MedLine Citation:
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PMID: 19464086 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Four sesquiterpene lactones were isolated from Achillea falcata, through bioassay-guided fractionation, based on their differential ability to affect HaCaT cell growth. Identified seco-tanapartholides: 3-beta-methoxy-iso-seco-tanapartholide (1), tanaphillin (2), iso-seco-tanapartholide (3), and 8-hydroxy-3-methoxy-iso-seco-tanaparatholide (4) were found to differentially decrease keratinocyte cell viability. In addition, the stereoselectivity, lipophilicity, and number and position of hydroxyl groups present in these compounds were correlated with their biological activities for HaCaT cell growth inhibition. Statistical analyses confirmed an enhanced potency of the beta-OH iso-seco-tanapartholide over the alpha:beta-OH diastereoisomeric mixture. The highest potency, however, was mainly the function of the enhanced lipophilicity of the molecule. |
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Authors:
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Akram Ghantous; Niveen Nasser; Ihab Saab; Nadine Darwiche; Najat A Saliba |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2009-05-04 |
Journal Detail:
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Title: European journal of medicinal chemistry Volume: 44 ISSN: 1768-3254 ISO Abbreviation: Eur J Med Chem Publication Date: 2009 Sep |
Date Detail:
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Created Date: 2009-07-20 Completed Date: 2009-10-14 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0420510 Medline TA: Eur J Med Chem Country: France |
Other Details:
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Languages: eng Pagination: 3794-7 Citation Subset: IM |
Affiliation:
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American University of Beirut, Department of Biology, Beirut, Lebanon. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Achillea
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chemistry* Cell Line, Tumor Cell Proliferation / drug effects Cell Survival / drug effects Growth Inhibitors / chemistry*, isolation & purification, pharmacology* Humans Keratinocytes / cytology Lactones / chemistry, isolation & purification, pharmacology Plant Components, Aerial / chemistry* Sesquiterpenes, Guaiane / chemistry*, isolation & purification, pharmacology* Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Growth Inhibitors; 0/Lactones; 0/Sesquiterpenes, Guaiane |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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