β-Ionone derived chalcones as potent antiproliferative agents.
A series of β-ionone derived chalcones were evaluated for cytotoxic activity against various human cancer cell lines using SRB dye assay. All the compounds displayed moderate to high cytotoxic effect against almost all the cancer cell lines. The results also revealed the effect of substituents of the aromatic ring on their inhibitory potential. In general, compounds bearing electron withdrawing groups such as nitro, fluoro, chloro and bromo showed more inhibitory potential than those bearing electron donating groups. The nitro substituted compound (7h) showed comparatively more inhibitory potential than other derivatives, therefore, it was further investigated for observing its effect on cell morphology in Chinese hamster ovary (CHO) cells by using phase contrast imaging, cell cycle analysis and annexin-FITC apoptosis assay. The treated cells exhibited the characteristics of apoptosis i.e. cell shrinkage, chromatin condensation and nuclear fragmentation, and induced the inhibition of cell proliferation by arresting the cells at G0 phase.
Bio-Organic and Photochemistry Laboratory, Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar 143 005, Punjab, India.
Vishal
V
Sharma
Ashun
A
Chaudhary
Saroj
S
Arora
Ajit K
AK
Saxena
Mohan Paul S
MP
Ishar
D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D016466:CHO Cells; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D061986:MCF-7 Cells; D015394:Molecular Structure; D045792:Norisoprenoids / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D047188:Chalcones; D045792:Norisoprenoids; C008157:beta-ionone
Antiproliferative activity; Apoptosis; Cell cycle arrest; Chalcones; Morphological analysis; β-Ionone