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首页> 外文期刊>Clinical and experimental pharmacology & physiology >Effects of econazole on Ca2+ levels in and the growth of human prostate cancer PC3 cells.
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Effects of econazole on Ca2+ levels in and the growth of human prostate cancer PC3 cells.

机译：官果对人前列腺癌PC3细胞Ca2 +水平和生长的影响。

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1. Econazole is used clinically as an antifungal drug with many different in vitro effects. However, the effects of econazole on prostate cancer cells are unknown. The effects of econazole on intracellular Ca2+ concentrations ([Ca2+]i) in and the proliferation of human PC3 prostate cancer cells was explored in the present study using fura-2 and tetrazolium as fluorescent dyes. 2. At a concentration of 0.1 micromol/L, econazole started to increase [Ca2+]i in a concentration-dependent manner. The econazole-induced increase in [Ca2+]i was reduced by 48% by removal of extracellular Ca2+, suggesting that the econazole-induced increase in [Ca2+]i was composed of extracellular Ca2+ influx and intracellular Ca2+. 3. This econazole-induced Ca2+ influx was via an L-type Ca2+ channel-like pathway. In Ca2+-free medium, 1 micromol/L thapsigargin, an inhibitor of the endoplasmic reticulum Ca2+-ATPase, caused a monophasic increase in [Ca2+]i, after which the effect of econazole to increase [Ca2+]i was substantially inhibited. Conversely, pretreatment with 5 micromol/L econazole to deplete intracellular Ca2+ stores totally prevented thapsigargin from releasing more Ca2+. 4. The phospholipase C (PLC) inhibitor U73122 (2 micromol/L) abolished the increase in [Ca2+]i induced by 10 micromol/L ATP (a Ca2+ mobilizer that needs inositol 1,4,5-trisphosphate). 5. Overnight incubation with 1-30 micromol/L econazole inhibited proliferation of PC3 cells in a concentration-dependent manner. 6. These findings suggest that, in PC3 cells, econazole increases [Ca2+]i by stimulating Ca2+ influx into cells and Ca2+ release from the endoplasmic reticulum via a PLC-independent mechanism. Econazole is cytotoxic at submicromolar concentrations.
机译：1.辛烷唑临床用作抗真菌药物，具有许多不同的体外效应。然而，生态杂唑对前列腺癌细胞的影响是未知的。在本研究中，使用Fura-2和Torzolium作为荧光染料，在本研究中探讨了生态唑对细胞内Ca2 +浓度（[Ca2 +] I）和增殖人PC3前列腺癌细胞的影响。 2.以0.1微摩洛/升浓度，生态唑以浓度依赖性方式增加[Ca2 +] i。通过去除细胞外CA2 +，官果诱导的[Ca2 +] I的增加48％，表明Econazole诱导的[Ca2 +] I的增加由细胞外Ca2 +流入和细胞内Ca2 +组成。 3.这种杂唑诱导的Ca2 +流入是通过L型Ca2 +沟道状途径。在Ca2 + -Free培养基中，1μmol/ L Thapsigargin，内质网Ca2 + -AtPase的抑制剂导致[Ca2 +] I的单相增加，之后产生了生态唑增加[Ca2 +] I的作用。相反，用5微摩洛/ l杂唑进行预处理，以消耗细胞内Ca2 +商店完全防止Thapsigargin释放更多CA2 +。 4.磷脂酶C（PLC）抑制剂U73122（2微摩洛/升）废除了10μm诱导的[Ca2 +] I的增加（需要肌醇1,4,5-三磷酸的Ca2 +动员剂）。 5.与1-30微摩洛/升杂唑过夜孵育，以浓度依赖性方式抑制PC3细胞的增殖。 6.这些发现表明，在PC3细胞中，Econazole通过刺激Ca 2 +流入细胞和Ca2 +通过PLC的机制从内质网释放来增加[Ca2 +] I。 Econazole是亚微粒摩尔浓度的细胞毒性。

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