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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
2009-4-17
pubmed:abstractText
Isodon diterpenoids have received considerable phytochemical and biological attention for their strong antitumor activity with low toxicity. In this study, ExcisaninA, a diterpenoid compound purified from Isodon MacrocalyxinD, was tested on human Hep3B and MDA-MB-453 cell lines and Hep3B xenograft models. The results showed ExcisaninA could inhibit the proliferation of Hep3B and MDA-MB-453 cells via induction of apoptosis, with the evidence of increasing AnnexinV-positive cells and characteristic morphologic changes of apoptosis in the nucleus. Also, ExcisaninA sensitized Hep3B cells to 5-fluorouracil treatment or MDA-MB-453 cells to ADM treatment in vitro. In Hep3B xenograft models, ExcisaninA at 20 mg/kg/d remarkably decreased the xenograft tumor size and induced tumor cells apoptosis using transferase-mediated FITC-12-dUTP nick-end labeling assay. More importantly, we found that ExcisaninA could inhibit AKT activity and block its signal pathway in vitro and in vivo. And treatment with ExcisaninA significantly reduced the number of viable cells in Hep3B/myr-AKT1 cells more than that in control cells. Together, ExcisaninA might be a potent inhibitor of AKT signaling pathway in tumor cells. These data provide validation for the development of ExcisaninA to treat cancers displaying elevated levels of AKT.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
1535-7163
pubmed:author
pubmed:issnType
Print
pubmed:volume
8
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
873-82
pubmed:dateRevised
2009-11-19
pubmed:meshHeading
pubmed-meshheading:19372560-Animals, pubmed-meshheading:19372560-Antineoplastic Agents, pubmed-meshheading:19372560-Apoptosis, pubmed-meshheading:19372560-Blotting, Western, pubmed-meshheading:19372560-Breast Neoplasms, pubmed-meshheading:19372560-Carcinoma, Hepatocellular, pubmed-meshheading:19372560-Cell Proliferation, pubmed-meshheading:19372560-Diterpenes, pubmed-meshheading:19372560-Drugs, Chinese Herbal, pubmed-meshheading:19372560-Fluorescent Antibody Technique, pubmed-meshheading:19372560-Humans, pubmed-meshheading:19372560-In Situ Nick-End Labeling, pubmed-meshheading:19372560-Isodon, pubmed-meshheading:19372560-Liver Neoplasms, pubmed-meshheading:19372560-Mice, pubmed-meshheading:19372560-Mice, Inbred BALB C, pubmed-meshheading:19372560-Mice, Nude, pubmed-meshheading:19372560-Protein-Serine-Threonine Kinases, pubmed-meshheading:19372560-Proto-Oncogene Proteins c-akt, pubmed-meshheading:19372560-RNA, Messenger, pubmed-meshheading:19372560-RNA, Small Interfering, pubmed-meshheading:19372560-Reverse Transcriptase Polymerase Chain Reaction, pubmed-meshheading:19372560-Signal Transduction, pubmed-meshheading:19372560-Tumor Cells, Cultured, pubmed-meshheading:19372560-Xenograft Model Antitumor Assays
pubmed:year
2009
pubmed:articleTitle
ExcisaninA, a diterpenoid compound purified from Isodon MacrocalyxinD, induces tumor cells apoptosis and suppresses tumor growth through inhibition of PKB/AKT kinase activity and blockade of its signal pathway.
pubmed:affiliation
State Key Laboratory of Oncology in South China, Cancer Center, Sun Yat-sen University, 651 Dongfeng Road East, Guangzhou 510060, China.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't