The flavonoid eupatorin inactivates the mitotic checkpoint leading to polyploidy and apoptosis

Salmela, Anna-Leena; Pouwels, Jeroen; Kukkonen-Macchi, Anu; Waris, Sinikka; Toivonen, Pauliina; Jaakkola, Kimmo; Mäki-Jouppila, Jenni H.E.; Kallio, Lila; Kallio, Marko J.

doi:10.1016/j.yexcr.2011.12.014

Cited by 21 publications

(24 citation statements)

References 51 publications

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“…Both aurora A and B were inhibited approximately to the same extent (70% and 79% of residual activity, respectively). Similarly, Salmela and coworkers [18] observed significant inhibition of aurora B activity in vitro with recombinant enzyme (IC 50 approx. 20 μM) as well as downregulation of the activating autophosphorylation on T232 in cell lysates.…”

Section: Eupatorin Is a Nonspecific Kinase Inhibitormentioning

confidence: 83%

“…Aurora B is also a part of SAC and sustains activated when kinetochors are attached to microtubules but are not under tension [25,26]. Inhibition of its function in mitotic cells causes inactivation of SAC and forced exit from mitosis with perturbed cytokinesis [18]. High concentrations of eupatorin inhibit aurora kinases in cells as well as in vitro with purified enzyme as shown in recent study by Salmela and coworkers [18].…”

Section: The Extract As Well As the Eupatorin Standard Induces G2/m Amentioning

confidence: 92%

“…Inhibition of its function in mitotic cells causes inactivation of SAC and forced exit from mitosis with perturbed cytokinesis [18]. High concentrations of eupatorin inhibit aurora kinases in cells as well as in vitro with purified enzyme as shown in recent study by Salmela and coworkers [18]. In asynchronous population of HeLa cells only a part of them is present in mitosis and only these cells override mitotic checkpoint upon treatment with high doses of eupatorin, they do not undergo cytokinesis and exit mitosis in tetraploid, polynucleated state.…”

Section: The Extract As Well As the Eupatorin Standard Induces G2/m Amentioning

confidence: 99%

“…These observations suggest that eupatorin could become an anticancer agent with desired selectivity between cancer and normal cells. In a recently published study [18], eupatorin was found in a high-throughput screen of 2000 bioactive compounds as a new spindle assembly checkpoint (SAC) inhibitor.…”

Section: Introductionmentioning

confidence: 99%

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Antiproliferative and antiangiogenic effects of flavone eupatorin, an active constituent of chloroform extract of Orthosiphon stamineus leaves

et al. 2012

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Section: Eupatorin Is a Nonspecific Kinase Inhibitormentioning

confidence: 83%

Section: The Extract As Well As the Eupatorin Standard Induces G2/m Amentioning

confidence: 92%

Section: The Extract As Well As the Eupatorin Standard Induces G2/m Amentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Antiproliferative and antiangiogenic effects of flavone eupatorin, an active constituent of chloroform extract of Orthosiphon stamineus leaves

et al. 2012

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“…Flavonoids have been demonstrated to exhibit anti-inflammatory, -allergic, -oxidative, -damage and -tumour effects (17,18). In recent years, studies on flavonoids have entered a new phase with these compounds revealed to inhibit proliferation of cancer cells, including breast, colon, lung, cervical and liver cancers and lymphoma cells (19)(20)(21)(22)(23). In addition, alpinetin has also been identified to inhibit proliferation of leukemic cells (24).…”

Section: Discussionmentioning

confidence: 99%

Alpinetin promotes Bax translocation, induces apoptosis through the mitochondrial pathway and arrests human gastric cancer cells at the G2/M phase

Wang

Lü

et al. 2012

Molecular Medicine Reports

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Abstract. Alpinetin is a natural flavonoid widely distributed inZingiberaceae. Previous studies have demonstrated that alpinetin markedly inhibits tumour growth. However, the molecular mechanisms underlying the antitumour effects of alpinetin are unclear. Bcl-2-associated X protein (Bax) translocation is known to activate the mitochondrial-dependent endogenous apoptosis pathway. The aim of the current study was to investigate the roles of Bax and the mitochondrial pathway during alpinetin-induced gastric cancer cell apoptosis and the effects of alpinetin on the cell cycle. Human gastric cancer cells were treated with various doses of alpinetin and an MTT assay was performed to measure cell viability, flow cytometry to measure the apoptotic rate, changes in the cell cycle and mitochondrial membrane potential and western blot analysis to detect the expression levels of relevant proteins. Results demonstrate that alpinetin induces apoptosis in human gastric cancer cells in a dose-and time-dependent manner. During the early stages of apoptosis, alpinetin may alter mitochondrial membrane potential leading to release of cytochrome c from mitochondria, activation of caspase family members and ultimately apoptosis of human gastric cancer cells. Results of the present study indicate that alpinetin-induced human gastric cancer cell apoptosis is associated with the mitochondrial pathway.

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Recent Advancements on Transition‐Metal‐Catalyzed, Chelation‐Induced ortho‐Hydroxylation of Arenes

Iqbal

Joshi

2020

Adv Synth Catal

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The phenols are key intermediates as well as desired products in many target oriented syntheses. The conversion of CÀ H bond to CÀ O bond is one of the most challenging tasks in organic synthesis. In last few decades, the hydroxylation of aromatic compounds has drawn a considerable attention because of their importance in Pharmaceutical industry, material chemistry, polymers and in agrochemicals. Indeed, transition-metal-catalyzed, coordination-assisted regio-and chemoselective orthohydroxylation of arenes has become very efficient and popular strategy to obtain good yields of phenols with tolerance of a wide range of functional groups. This review is the comprehensive summary of recent advancement on Pd-, Ru-, Rh-, Cu-and Ir-catalyzed, chelation-controlled regioselective ortho-CÀ H bond hydroxylation of aromatic compounds in the presence of diverse hydroxylating agents. The review has been classified on the sources of hydroxylating agents used in reaction.

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The flavonoid eupatorin inactivates the mitotic checkpoint leading to polyploidy and apoptosis

Cited by 21 publications

References 51 publications

Antiproliferative and antiangiogenic effects of flavone eupatorin, an active constituent of chloroform extract of Orthosiphon stamineus leaves

Antiproliferative and antiangiogenic effects of flavone eupatorin, an active constituent of chloroform extract of Orthosiphon stamineus leaves

Alpinetin promotes Bax translocation, induces apoptosis through the mitochondrial pathway and arrests human gastric cancer cells at the G2/M phase

Recent Advancements on Transition‐Metal‐Catalyzed, Chelation‐Induced ortho‐Hydroxylation of Arenes

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