2013
DOI: 10.1021/jm400881m
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Abstract: ClC-3 chloride (Cl(-)) channel has been shown to be involved in cell proliferation, cell cycle, and cell migration processes. Herein, we found that a series of bufadienolides isolated from toad venom were a novel class of ClC-3 Cl(-) channel activators with antitumor activities. Bufalin, which has the most potent antitumor activity, and 15β-acetyloxybufalin, which has no antitumor activity, were chosen as representative compounds to investigate the role of the ClC-3 Cl(-) channel. It was found that bufalin rap… Show more

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Cited by 50 publications
(41 citation statements)
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“…These results provide the first and compelling evidence that ClC-3 is critically linked to preadipocyte apoptosis induced by saturated FFA in vitro and in T2DM. ClC-3 has been suggested to be essential for apoptosis in a variety of cell types, such as vascular smooth muscle cells [19,34], endothelial progenitor cells [21], tumor and carcinoma cells [38,39] and bronchial and intestinal epithelial cells [20,40,41], and thus may play roles in the disease processes of hypertensive vascular remodeling [19], inflammatory responses [20] and tumor cell death [38]. Our presented data demonstrated that ClC-3 protein expression and cellular apoptosis in preadipocytes could be significantly increased in response to saturated FFAs (palmitate), but not unsaturated FFAs.…”
Section: Discussionmentioning
confidence: 99%
“…These results provide the first and compelling evidence that ClC-3 is critically linked to preadipocyte apoptosis induced by saturated FFA in vitro and in T2DM. ClC-3 has been suggested to be essential for apoptosis in a variety of cell types, such as vascular smooth muscle cells [19,34], endothelial progenitor cells [21], tumor and carcinoma cells [38,39] and bronchial and intestinal epithelial cells [20,40,41], and thus may play roles in the disease processes of hypertensive vascular remodeling [19], inflammatory responses [20] and tumor cell death [38]. Our presented data demonstrated that ClC-3 protein expression and cellular apoptosis in preadipocytes could be significantly increased in response to saturated FFAs (palmitate), but not unsaturated FFAs.…”
Section: Discussionmentioning
confidence: 99%
“…ClC-3, a member of the voltage-gated chloride channel family, shows the properties of cell cycle-dependent expression and subcellular distribution, and plays an important role in the regulation of cell proliferation, migration and apoptosis, especially in cancerous cells (Hong et al, 2015;Liu et al, 2013;Mao et al, 2012Mao et al, , 2013Xu et al, 2014;Zhang et al, 2013a). The inducible ClC-3 gene deletion eliminating native VRAC in adult mice overwhelmingly suggested that ClC-3 is a key component of native VRAC in mammalian heart, not in the brain (Xiong et al, 2010).…”
Section: Introductionmentioning
confidence: 99%
“…ClC-3 chloride channels and AQPs are involved in the growth/proliferation, migration and/or invasion of cancer cells, and cell volume regulation plays a pivotal role in all of these processes (Frede et al, 2013;Huber et al, 2012;Liu et al, 2013;Mao et al, 2012Mao et al, , 2013Verkman, 2012;Zhang et al, 2013a,b;Zhu et al, 2012). The ClC-3 volume-sensitive Cl − channel has been confirmed to be expressed in cancerous nasopharyngeal epithelial cells by us previously, but the expression of AQPs in these cells has not been clarified.…”
Section: Inhibition Of Regulatory Volume Decrease By Aqp-3-sirna and mentioning
confidence: 98%