rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2011-4-4
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pubmed:abstractText |
The cytochrome P45O activities of the naturally occurring Amaryllidaceae alkaloid narciclasine (3), isolated from Narcissus pseudonarcissus, and synthetic derivative trans-dihydronarciclasine (5) are reported. While narciclasine was found to possess potent inhibitory activity to human CYP3A4, its dihydro analogue was inactive. This study revealed that the C1-C10b double bond is required for inhibition of this crucial metabolizing enzyme. Compound 5 also demonstrated no inhibition of the related human cytochromes CYP19 and CYP1A1. This study elevates the status of trans-dihydronarciclasine (5) as a highly privileged, readily available molecule, with potent and selective anticancer activity.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Alkaloids,
http://linkedlifedata.com/resource/pubmed/chemical/Amaryllidaceae Alkaloids,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents, Phytogenic,
http://linkedlifedata.com/resource/pubmed/chemical/CYP3A4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 CYP1A1,
http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 CYP3A,
http://linkedlifedata.com/resource/pubmed/chemical/Phenanthridines,
http://linkedlifedata.com/resource/pubmed/chemical/dihydronarciclasine,
http://linkedlifedata.com/resource/pubmed/chemical/narciclasine
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1520-6025
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
28
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pubmed:volume |
74
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
106-8
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pubmed:meshHeading |
pubmed-meshheading:21105682-Alkaloids,
pubmed-meshheading:21105682-Amaryllidaceae Alkaloids,
pubmed-meshheading:21105682-Antineoplastic Agents, Phytogenic,
pubmed-meshheading:21105682-Crystallography, X-Ray,
pubmed-meshheading:21105682-Cytochrome P-450 CYP1A1,
pubmed-meshheading:21105682-Cytochrome P-450 CYP3A,
pubmed-meshheading:21105682-Drug Screening Assays, Antitumor,
pubmed-meshheading:21105682-Humans,
pubmed-meshheading:21105682-Molecular Structure,
pubmed-meshheading:21105682-Narcissus,
pubmed-meshheading:21105682-Phenanthridines,
pubmed-meshheading:21105682-Stereoisomerism
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pubmed:year |
2011
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pubmed:articleTitle |
Human cytochrome P450 liability studies of trans-dihydronarciclasine: a readily available, potent, and selective cancer cell growth inhibitor.
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pubmed:affiliation |
Department of Chemistry and Chemical Biology, McMaster University, 1280 Main Street West, Hamilton, Ontario, Canada, L8S 4M1. jmcnult@mcmaster.ca
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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