Source:http://linkedlifedata.com/resource/pubmed/id/21250700
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2011-2-25
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pubmed:abstractText |
Six lanostane-type triterpene acids (1a-6a), isolated from Poria cocos , and their methyl ester (1b-6b) and hydroxy derivatives (1c-6c) were prepared. Upon evaluation of the cytotoxic activity of these compounds against leukemia (HL60), lung (A549), melanoma (CRL1579), ovary (NIH:OVCAR-3), breast (SK-BR-3), prostate (DU145), stomach (AZ521), and pancreas (PANC-1) cancer cell lines, 11 compounds (5a, 6a, 2b-5b, 1c, and 3c-6c) exhibited activity with single-digit micromolar IC(50) values against one or more cell lines. Poricotriol A (1c), a hydroxy derivative of poricoic acid A (1a), exhibited potent cytotoxicities against six cell lines with IC(50) values of 1.2-5.5 ?M. Poricotriol A induced typical apoptotic cell death in HL60 and A549 cells on evaluation of the apoptosis-inducing activity by flow cytometric analysis. Western blot analysis in HL60 cells showed that poricotriol A activated caspases-3, -8, and -9, while increasing the ratio of Bax/Bcl-2. This suggested that poricotriol A induced apoptosis via both mitochondrial and death receptor pathways in HL60. On the other hand, poricotriol A did not activate caspases-3, -8, and -9, but induced translocation of apoptosis-inducing factor (AIF) from mitochondria and increased the ratio of Bax/Bcl-2 in A549. This suggested that poricotriol A induced apoptosis via the mitochondrial pathway mostly by translocation of AIF, independent from the caspase pathway in A549. Furthermore, poricotriol A was shown to possess high selective toxicity in lung cancer cells since it exhibited only weak cytotoxicity against a normal lung cell line (WI-38).
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Apoptosis Inducing Factor,
http://linkedlifedata.com/resource/pubmed/chemical/Caspases,
http://linkedlifedata.com/resource/pubmed/chemical/Triterpenes,
http://linkedlifedata.com/resource/pubmed/chemical/poricoic acid A
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1520-6025
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
25
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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 |
137-44
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pubmed:meshHeading |
pubmed-meshheading:21250700-Antineoplastic Agents,
pubmed-meshheading:21250700-Apoptosis Inducing Factor,
pubmed-meshheading:21250700-Caspases,
pubmed-meshheading:21250700-Drug Screening Assays, Antitumor,
pubmed-meshheading:21250700-Female,
pubmed-meshheading:21250700-HL-60 Cells,
pubmed-meshheading:21250700-Humans,
pubmed-meshheading:21250700-Inhibitory Concentration 50,
pubmed-meshheading:21250700-Male,
pubmed-meshheading:21250700-Molecular Structure,
pubmed-meshheading:21250700-Poria,
pubmed-meshheading:21250700-Triterpenes
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pubmed:year |
2011
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pubmed:articleTitle |
Cytotoxic and apoptosis-inducing activities of triterpene acids from Poria cocos.
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pubmed:affiliation |
College of Science and Technology, Nihon University, 1-8 Kanda Surugadai, Chiyoda-ku, Tokyo 101-8308, Japan.
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pubmed:publicationType |
Journal Article
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