RY10-4, a novel anti-tumor compound, exhibited its anti-angiogenesis activity by down-regulation of the HIF-1α and inhibition phosphorylation of AKT and mTOR

Liu, Ziwei; Yuan, Qianying; Xue-nong, Zhang; Xiong, Chaomei; Xue, Pingping; Ruan, Jinlan

doi:10.1007/s00280-012-1873-3

Cited by 7 publications

(2 citation statements)

References 34 publications

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“…This is also in line with previous studies that revealed increased levels of ROS in prostate and breast cancer cells after treatment with 1 or 2 [9,26]. Moreover, RY10-4, another synthetic protoflavone analog, was reported to down-regulate HIF-1α expression in breast cancer cell lines [29].…”

Section: Discussionsupporting

confidence: 84%

Lower antioxidative capacity of multidrug-resistant cancer cells confers collateral sensitivity to protoflavone derivatives

Stanković

Dankó

Martins

et al. 2015

Cancer Chemother Pharmacol

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Section: Discussionsupporting

confidence: 84%

Lower antioxidative capacity of multidrug-resistant cancer cells confers collateral sensitivity to protoflavone derivatives

Stanković

Dankó

Martins

et al. 2015

Cancer Chemother Pharmacol

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“…In our laboratory, RY10-4 was designed and synthesized as a protoapigenone analog, as an attempt to develop a novel anti-tumor compound. According to some previously researches and reports [ 12 , 13 ], RY10-4 had potent anti-tumor activities against human breast cancer cells. In another report, RY10-4 could induce autophagic cell death in MCF-7 cells while protoapigenone could not [ 6 ].…”

Section: Discussionmentioning

confidence: 99%

RY10-4 Inhibits the Proliferation of Human Hepatocellular Cancer HepG2 Cells by Inducing Apoptosis In Vitro and In Vivo

et al. 2016

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This study aimed to investigate the anti-tumor activity of RY10-4, a small molecular that was designed and synthesized based on the structure of protoapigenone. A previous screening study showed that RY10-4 possessed anti-proliferative effects against HepG2 human hepatocellular carcinoma cells. However, the full range of RY10-4 anti-cancer effects on liver tumors and the underlying mechanisms have not been identified. Herein, employing flow cytometry, and Western blot analysis, we demonstrate that RY10-4 can induce cell cycle arrest, intracellular reactive oxygen species (ROS) production and apoptosis in HepG2 cells. In HepG2 cell xenograft tumor model, RY10-4 significantly inhibited the growth of tumors and induced apoptosis in tumor cells, with little side effects. Moreover, RY10-4 caused the suppression of STAT3 activation, which may be involved the apoptosis induction. In addition, RY10-4 inhibited the proliferation of Hep3B and HuH-7 human hepatocellular carcinoma cells in a concentration-dependent manner. Taken together, our results suggest that RY10-4 has a great potential to develop as chemotherapeutic agent for liver cancer.

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The HIF-1 transcription complex is essential for translational control of myeloid hematopoietic cell function by maintaining mTOR phosphorylation

Yasinska

Gibbs

Lall

et al. 2013

Cell. Mol. Life Sci.

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Mammalian myeloid cells are crucial effectors of host innate immune defense. Normal and pathological responses of these cells require adaptation to signaling stress through the hypoxia-inducible factor 1 (HIF-1) transcription complex. Adapted cells activate the mammalian target of rapamycin (mTOR), via S2448 phosphorylation, which induces de novo translation of vital signaling proteins. However, the molecular mechanisms underlying this signaling dogma remain unclear. Here, we demonstrate for the first time that inactivation of HIF-1, by silencing its inducible alpha subunit, significantly decreases mTOR S2448 phosphorylation caused by ligand-dependent activation of human myeloid leukemia cells. This shows that HIF-1 is essential for the activation of mTOR and serves at a crucial juncture of myeloid cell function in both in vitro and in vivo systems.

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RY10-4, a novel anti-tumor compound, exhibited its anti-angiogenesis activity by down-regulation of the HIF-1α and inhibition phosphorylation of AKT and mTOR

Abstract: The structure of 4-hydroxy-2,5-cyclohexadien-1-one should be the effective pharmacophore of RY10-4. RY10-4 got fine performance in anti-tumor and anti-angiogenesis assay, and thus, the quinol compound will be the new hot-spot for further anti-tumor agency development.

Cited by 7 publications

References 34 publications

Lower antioxidative capacity of multidrug-resistant cancer cells confers collateral sensitivity to protoflavone derivatives

Lower antioxidative capacity of multidrug-resistant cancer cells confers collateral sensitivity to protoflavone derivatives

RY10-4 Inhibits the Proliferation of Human Hepatocellular Cancer HepG2 Cells by Inducing Apoptosis In Vitro and In Vivo

The HIF-1 transcription complex is essential for translational control of myeloid hematopoietic cell function by maintaining mTOR phosphorylation

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