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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2007-10-22
pubmed:abstractText
Chalcones are considered the precursors of flavonoids and have been identified as interesting compounds with antitumor properties. Boronic-chalcone derivatives are more toxic to breast cancer cells compared to normal breast cells. Here, we studied the antitumor activities of trans-4-lodo,4'-boranyl-chalcone (TLBC), which is a boronic-chalcone derivative, in several glioma cell lines. TLBC showed a dose-dependent inhibition with inhibitory concentration 50% value in the muM range (5.5-25.5 microM) in various glioma cell lines. Flow cytometric and western blot assay demonstrated that TLBC induced apoptosis independent of changes to the tumor suppressor p53. This cytotoxic effect was the caspase-dependent manner. Also, TLBC lowered levels of anti-apoptotic Bcl-2 and/or Bcl-X(L) protein in several of the cell lines. To examine the antitumor effect of TLBC in vivo, we used a malignant glioma xenograft model. This result showed that in the mice treated with TLBC at 20 mg/kg, mean tumor volume was reduced by 43.9% (P < 0.01) in comparison with the control group. Immunohistochemical and western blot analysis showed that Bcl-2 protein levels were decreased and Bax protein levels were slightly increased in the tumors injected with 20 mg/kg TLBC compared with the control tumors. Therefore, we conclude that TLBC may be a potential chemotherapeutic agent for human glioma.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
0167-594X
pubmed:author
pubmed:issnType
Print
pubmed:volume
85
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
123-32
pubmed:meshHeading
pubmed-meshheading:17530176-Animals, pubmed-meshheading:17530176-Antineoplastic Agents, pubmed-meshheading:17530176-Apoptosis, pubmed-meshheading:17530176-Boron Compounds, pubmed-meshheading:17530176-Brain Neoplasms, pubmed-meshheading:17530176-Caspases, pubmed-meshheading:17530176-Cell Cycle, pubmed-meshheading:17530176-Cell Line, Tumor, pubmed-meshheading:17530176-Chalcones, pubmed-meshheading:17530176-Dose-Response Relationship, Drug, pubmed-meshheading:17530176-Gene Expression Regulation, Neoplastic, pubmed-meshheading:17530176-Glioma, pubmed-meshheading:17530176-Humans, pubmed-meshheading:17530176-Inhibitory Concentration 50, pubmed-meshheading:17530176-Mice, pubmed-meshheading:17530176-Mice, Nude, pubmed-meshheading:17530176-Proto-Oncogene Proteins c-bcl-2, pubmed-meshheading:17530176-Statistics, Nonparametric, pubmed-meshheading:17530176-Tumor Suppressor Protein p53, pubmed-meshheading:17530176-Xenograft Model Antitumor Assays, pubmed-meshheading:17530176-bcl-2-Associated X Protein
pubmed:year
2007
pubmed:articleTitle
Trans-4-lodo,4'-boranyl-chalcone induces antitumor activity against malignant glioma cell lines in vitro and in vivo.
pubmed:affiliation
Department of Neurosurgery, Kobe University Graduate School of Medicine, 7-5-1, Kusunoki-cho, Chuo-ku, Kobe, 650-0017, Japan. takasasa@med.kobe-u.ac.jp
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't