7-O -Methylwogonin from Scutellaria baicalensis Disturbs Mitotic Progression by Inhibiting Plk1 Activity in Hep3B Cells
- Authors
- Woo, Sang-Uk; Jang, Hay-Ran; Chin, Young-Won; Yim, Hyungshin
- Issue Date
- Feb-2019
- Publisher
- GEORG THIEME VERLAG KG
- Keywords
- 7-O-methylwogonin; polo-like kinase 1; Scutellaria baicalensis; Lamiaceae; anticancer; mitosis
- Citation
- PLANTA MEDICA, v.85, no.3, pp.217 - 224
- Indexed
- SCIE
SCOPUS
- Journal Title
- PLANTA MEDICA
- Volume
- 85
- Number
- 3
- Start Page
- 217
- End Page
- 224
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/3541
- DOI
- 10.1055/a-0731-0394
- ISSN
- 0032-0943
- Abstract
- Polo-like kinase 1, a mitotic Ser/Thr kinase, has emerged as a molecular target for the development of anticancer drugs. In this study, we found that polo-like kinase 1 activity was inhibited by 7- O -methylwogonin and related flavones, including baicalein, dihydrobaicalein, and viscidulin II, isolated from Scutellaria baicalensis . Although dihydrobaicalein exhibited the highest polo-like kinase 1 inhibitory activity among the four compounds, it also inhibited other kinases, such as vaccinia-related kinase 2 and polo-like kinase 2. Baicalein and viscidulin II also showed low selectivity to polo-like kinase 1 since they inhibited polo-like kinase 3 and polo-like kinase 2, respectively. However, 7- O -methylwogonin exhibited selective polo-like kinase 1 inhibitory activity, as evidenced from in vitro kinase assays based on fluorescence resonance energy transfer assays and ADP-Glo kinase assays. In addition, examination of mitotic morphology and immunostaining using specific antibodies for the mitotic markers, p-histone H3 and mitotic protein monoclonal 2, in Hep3B cells showed that 7- O -methylwogonin treatment increased mitotic cell populations due to inhibition of mitotic progression as a result of polo-like kinase 1 inhibition. The pattern of 7- O -methylwogonin-induced mitotic arrest was similar to that of BI 2536, a specific polo-like kinase 1 inhibitor. Thus, it was suggested that 7- O -methylwogonin disturbed mitotic progression by inhibiting polo-like kinase 1 activity. These data suggest that 7- O -methylwogonin, a polo-like kinase 1 inhibitor, may be a useful anticancer agent because of its polo-like kinase 1 selectivity and effectiveness.
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