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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Berbamine: a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity.

Gleevec, which is an inhibitor of the bcr/abl tyrosine kinase, has been a remarkable success for the treatment of chronic myelogenous leukemia (CML). However, a significant proportion of patients chronically treated with Gleevec develop resistance. Here we describe the activity of a natural small molecular compound, berbamine from plant Berberis amurensis that can selectively induce cell death of both Gleevec-sensitive and -resistant Ph+ CML cells. The IC50 values of berbamine were 8.80 microg/ml in Gleevec-sensitive Ph+ CML cells, 11.34 microg/ml in Gleevec-resistant Ph+ CML cells, and 54.40 microg/ml in Ph- KG-1 cells, respectively. Similarly, berbamine was also found to display a selective anti-proliferative activity of primary leukemia cells from CML patients, and its IC50 values were 4.20-10.50 microg/ml in primary CML cells, and 185.20 microg/ml in normal bone marrow cells, respectively. More importantly, our studies demonstrate that berbamine down-regulates p210bcr/abl oncoprotein level, and induces apoptosis of bcr/abl+ cells through caspase-3-dependent pathway. These data suggest that berbamine might be a novel bcr/abl inhibitor with potent anti-leukemia activity.[1]

References

  1. Berbamine: a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity. Xu, R., Dong, Q., Yu, Y., Zhao, X., Gan, X., Wu, D., Lu, Q., Xu, X., Yu, X.F. Leuk. Res. (2006) [Pubmed]
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