Demethoxycurcumin induces Bcl-2 mediated G2/M arrest and apoptosis in human glioma U87 cells.
Docking analysis of curcumin (C1), demethoxycurcumin (C2) and bisdemethoxycurcumin (C3) with Bcl-2 illustrated that among the three curcuminoids, C2 binds more efficiently into its putative active site. C1, C2 and C3 were purified from turmeric rhizomes to demonstrate the molecular mechanism of their anticancer activity on human glioma U87 cells. Human glioma U87 cells treated with curcuminoids resulted in activation of Bcl-2 mediated G2 checkpoint, which was associated with the induction of G2/M arrest and apoptosis. The binding of C1, C2 and C3 with Bcl-2 protein was confirmed with circular dichroism (CD) spectroscopy. Present work revealed that C2 induced Bcl-2 mediated G2/M arrest and apoptosis most effectively.
Dr. B.R. Ambedkar Center for Biomedical Research, Medicinal Chemistry Division University of Delhi, North Campus, Mall Road, Delhi 110007, India. pmluthra@acbr.du.ac.in
Pratibha Mehta
PM
Luthra
Rakesh
R
Kumar
Amresh
A
Prakash
D017209:Apoptosis; D001665:Binding Sites; D001932:Brain Neoplasms / Q000378:metabolism*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003474:Curcumin / Q000031:analogs & derivatives* / Q000494:pharmacology; D036381:Diarylheptanoids; D015536:Down-Regulation; D016195:G2 Phase / Q000187:drug effects; D005910:Glioma / Q000378:metabolism*; D006801:Humans; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000819:agonists* / Q000378:metabolism
D036381:Diarylheptanoids; D019253:Proto-Oncogene Proteins c-bcl-2; D003474:Curcumin; C050229:demethoxycurcumin