Cell survival or apoptosis: rooperol's role as anticancer agent.
Nontoxic hypoxoside, isolated from Hypoxis, is converted to cytotoxic rooperol in the presence of beta-glucosidase. In this study, we investigated rooperol's mechanism of action. IC50 values of hypoxoside and rooperol were determined against the HeLa, HT-29, and MCF-7 cancer cell lines, and peripheral blood mononuclear cells. DNA cell cycle arrest occurred in late G1 and/or early S phases, associated with increased p21(Waf1/Cip1) levels. Apoptosis was shown by caspase-3 and/or caspase-7 activation, phosphatidylserine translocation, DNA fragmentation, cell blebbing, and apoptotic body formation. Increased phospho-Akt, phospho-Bcl-2, and p21(Waf1/Cip1) proteins, and cell size correspond to cell survival strategies (associated with endoreduplication).
Boukes
Gerhardt J
GJ
Department of Biochemistry and Microbiology, Nelson Mandela Metropolitan University, Port Elizabeth, South Africa.
Daniels
Brodie B
BB
Albrecht
Carl F
CF
van de Venter
Maryna
M
D000480:Alkynes / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D053148:Caspase 3 / Q000378:metabolism; D053179:Caspase 7 / Q000378:metabolism; D002396:Catechols / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects*; D053938:DNA Fragmentation / Q000187:drug effects; D005960:Glucosides / Q000494:pharmacology; D006801:Humans; D008858:Microscopy, Phase-Contrast; D010718:Phosphatidylserines / Q000378:metabolism
D000480:Alkynes; D000970:Antineoplastic Agents; D002396:Catechols; D005960:Glucosides; D010718:Phosphatidylserines; C087941:hypoxoside; C079659:rooperol; D053148:Caspase 3; D053179:Caspase 7