AI Article Synopsis
- The over-expression of Bcl-2 proteins is linked to tumor development and contributes to resistance against cancer drugs.
- Luteolin, a key component of Flos Chrysanthemi, has been found to bind to and inhibit Bcl-2 proteins.
- Research indicates that luteolin and its modified versions can effectively inhibit Bcl-2, suggesting their potential as new anti-tumor agents, particularly in leukemia treatment.
Article Abstract
Over-expression of the Bcl-2 anti-apoptotic proteins is closely related to tumorigenesis and associated with drug resistance. Here we report that luteolin, a main substance found in Flos Chrysanthemi, directly binds to and shows inhibitory activity against the Bcl-2 protein. We studied the binding mode of luteolin and its derivatives with target proteins, their structure-activity relationship, and their effect on the human leukemia cell line HL-60. The results suggest that luteolin and its derivatives with a benzyl group introduced to the B ring, are new small molecule Bcl-2 protein inhibitors, and their anti-tumor activity is likely related to their effect on the Bcl-2 protein.
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| http://dx.doi.org/10.1016/j.bmcl.2014.08.034 | DOI Listing |
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