Luteolin from Flos Chrysanthemi and its derivatives: New small molecule Bcl-2 protein inhibitors |
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| Affiliation: | 1. Clermont Université, Université d''Auvergne, Unité de Nutrition Humaine, BP 10448, F-63000 CLERMONT-FERRAND, Cedex, France;2. INRA, UMR 1019, UNH, CRNH Auvergne, F-63000 CLERMONT-FERRAND, Cedex, France;3. CHU Clermont-Ferrand, Service de Nutrition Clinique, F-63003 CLERMONT-FERRAND, Cedex, France;4. Nutrition Unit, Geneva University Hospital, Geneva, Switzerland;5. CHU Clermont-Ferrand, Service de Cardiologie, F-63003 CLERMONT-FERRAND, Cedex, France;6. CHU Clermont-Ferrand, Service de Chirurgie Vasculaire, F-63003 CLERMONT-FERRAND, Cedex, France |
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| 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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| Keywords: | Luteolin Bcl-2 protein Apoptosis Anti-tumor |
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