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Quercetin induces apoptosis via the mitochondrial pathway in KB and KBv200 cells
Jian-ye Zhang1, Tao Yi, Jing Liu
1School of Chinese Medicine, Hong Kong Baptist University , Kowloon Tong, Kowloon, Hong Kong.
Abstract:
In this study, anticancer activities of six compounds of flavonoids were investigated in human epidermoid carcinoma KB and KBv200 cells. Among these compounds, quercetin and acacetin showed strong inhibition of cell growth in KB and KBv200 cells. IC50 values of quercetin against KB and KBv200 cells were 17.84 ± 4.14 and 18.94 ± 4.75 μM, respectively. The IC50 values of acacetin against KB and KBv200 cells were 41.33 ± 6.05 and 49.04 ± 3.64 μM. The IC50 values of apigenin, kaempferol, kaempferol 3-O-rhamnoside, and quercetin 3-O-rhamnoside were more than 100 μM. Furthermore, quercetin was found to induce apoptosis in KB and KBv200 cells via the mitochondrial pathway, including a decrease of the reactive oxygen species level, loss of mitochondrial membrane potential, release of cytochrome c, activation of caspase-9 and caspase-3, and cleavage of poly (ADP-ribose) polymerase. The apoptosis induced by quercetin was not related to the regulation of Bcl-2 or Bax in KB and KBv200 cells.
Insights
Quercetin and acacetin exhibit potent anticancer effects against human epidermoid carcinoma cells. Quercetin effectively induces apoptosis through the mitochondrial pathway in these cancer cells.
Area of Science:
- Pharmacology
- Cell Biology
- Natural Product Chemistry
Background:
- Flavonoids are plant-derived compounds with diverse biological activities.
- Cancer research continuously seeks novel therapeutic agents from natural sources.
- Understanding flavonoid mechanisms is crucial for drug development.
Purpose of the Study:
- To evaluate the anticancer potential of six flavonoids against human epidermoid carcinoma KB and KBv200 cells.
- To elucidate the mechanism of action for effective compounds.
- To identify promising flavonoid-based anticancer agents.
Main Methods:
- Cell viability assays were performed to determine IC50 values.
- Flow cytometry was used to analyze apoptosis induction.
- Mitochondrial pathway markers (ROS, mitochondrial membrane potential, cytochrome c, caspases, PARP) were assessed.
Main Results:
- Quercetin and acacetin demonstrated significant inhibition of KB and KBv200 cell growth.
- Quercetin displayed IC50 values of 17.84 μM (KB) and 18.94 μM (KBv200).
- Quercetin induced apoptosis via the mitochondrial pathway, involving caspase activation and PARP cleavage, independent of Bcl-2/Bax.
Conclusions:
- Quercetin and acacetin are potent anticancer agents against human epidermoid carcinoma cells.
- Quercetin triggers apoptosis through the mitochondrial pathway, offering a potential therapeutic strategy.
- Further investigation into quercetin's anticancer properties is warranted.
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