Influence of B ring structure on cell cycle inhibitory activities of flavonols in a human oesophageal adenocarcinoma cell line (OE33)
The effects of three structurally related flavonols (kaempferol, quercetin, myricetin) on anti-proliferation and cell cycle arrest in human oesophageal adenocarcinoma OE33 cells were determined and compared by MTT assay and flow cytometry analysis. The results showed that three flavonols not only inhibited proliferation but also induced G2/M arrest in OE33 cells. Moreover, G2/M arrest-inducing activity of quercetin (with two hydroxyl groups in the B ring) was better than that of kaempferol (with one hydroxyl group in the B ring) and myricetin (with three hydroxyl groups in the B ring). It was further corroborated by comparing G2/M arrest-inducing activity of two flavones (apigenin and luteolin) whose B rings were same to kaempferol and quercetin, respectively. Additionally, the results of real-time RT-PCR and Western-blot analysis showed that the expressions of GADD45β and 14-3-3σ were upregulated but the expression of cyclin B1was downregulated by flavonols at the mRNA and the protein levels. It is suggested that the influence of B ring structure on cell cycle inhibitory activities of flavonols might result from the regulatory expression of these genes at the mRNA and protein levels.
Flavonols Apoptosis Anticancer activity Structure-activity relationship
Qiang Zhang Xinhuai Zhao
Key Lab of Diary Science of Ministry of Education,Northeast Agricultural University,150030 Harbin,Ch Key Lab of Diary Science of Ministry of Education,Northeast Agricultural University,150030 Harbin,Ch
国际会议
北京
英文
1-4
2009-06-11（万方平台首次上网日期，不代表论文的发表时间）