Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UNIPROT:P10415 (
Bcl-2
)
33,771
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Background and Objectives
: Microtubules are an attractive target for cancer chemotherapy. Previously, we reported that
Ivalin
exhibited excellent anti-migration and anti-invasion activities in human breast cancer cells. Here, we examined the microtubule inhibition effect of
Ivalin
in human hepatocellular carcinoma SMMC-7721 cells.
Materials and Methods
: We used the 3-(4,5-dimethylthiazol)-2,5-diphenyltetrazolium bromide (MTT) assay to evaluate the cell proliferation effect of
Ivalin
and flow cytometry analysis to detect the apoptotic and cell cycle arrest effects of
Ivalin
. Immunofluorescence staining was used to measure the effect of
Ivalin
on the cytoskeleton network, and Western blotting was used to detect the expression levels of Bax,
Bcl-2
, Cdc2, phosphor-Cdc2, Cdc25A, Cyclin B1, and tubulin.
Results
:
Ivalin
induced cell cycle G2/M arrest and subsequent triggered apoptosis in human hepatocellular carcinoma SMMC-7721 cells. Furthermore, microtubules were shown to be involved in
Ivalin
-meditated apoptosis. In this connection,
Ivalin
treatment suppressed cellular microtubule network formation by regulating microtubule depolymerization. Moreover, Western blotting revealed Cdc25A and Cyclin B1 were upregulated in
Ivalin
-meditated cell cycle arrest. Subsequently, the induction of Bax (a proapoptotic protein) and reduction of
Bcl-2
(an anti-apoptotic protein) expression were observed in
Ivalin
-treated SMMC-7721 cells.
Conclusion
:
Ivalin
induced microtubule depolymerization, then blocked cells in mitotic phase, and eventually resulted in apoptosis in SMMC-7721 cells. Collectively, these data indicate that
Ivalin
, acting as a novel inhibitor of microtubules, could be considered as a promising lead in anticancer drug development.
...
PMID:The Novel Nature Microtubule Inhibitor Ivalin Induces G2/M Arrest and Apoptosis in Human Hepatocellular Carcinoma SMMC-7721 Cells In Vitro. 3140 7