Fishbein J D, Dobrowsky R T, Bielawska A, Garrett S, Hannun Y A
Department of Pediatrics, Duke University Medical Center, Durham, North Carolina 27710.
J Biol Chem. 1993 May 5;268(13):9255-61.
Ceramide is emerging as a potential physiologic regulator of growth and differentiation in mammalian cells. This regulation may be mediated through the action of a serine/threonine ceramide-activated protein phosphatase (CAPP). In this study, the existence of a ceramide-mediated pathway of cell regulation in Saccharomyces cerevisiae was investigated. Incubating exponentially growing S. cerevisiae cells with 1-20 microM cell-permeable ceramide (C2-ceramide) produced a dose-dependent inhibition of proliferation. A number of other lipids and detergents, such as arachidonate, oleate, Triton X-100, dioctanoylglycerol, and phenylaminoalcohol ceramide analogs, were largely ineffective, demonstrating the specificity of the response. Stereospecificity was demonstrated, in that the D enantiomer of erythro-C2-ceramide was more potent than the L enantiomer. More dramatically, a highly specific structural requirement for C2-ceramide was demonstrated, in that 1-12 microM C2-dihydroceramide was completely ineffective at inhibiting growth. Since C2-dihydroceramide lacks the 4-5 trans double bond present in C2-ceramide, this suggests that the antiproliferative properties of C2-ceramide depend upon the presence of the double bond. This raises an interesting possibility; the dehydrogenase responsible for introduction of the double bond during endogenous ceramide synthesis may regulate cell growth by controlling the cellular concentrations of dihydroceramide and ceramide. The oxygenase responsible for introduction of the final hydroxyl group in phytoceramide could provide a similar regulatory function in yeast. The potential role of CAPP in ceramide action in yeast was investigated next. Crude extracts of S. cerevisiae also contained a ceramide-dependent serine/threonine phosphatase activity, which was sensitive to inhibition by okadaic acid. This enzyme exhibited stereospecificity and structural requirements identical to that of the ceramide-induced growth inhibition. We conclude that both the growth-inhibitory response to ceramide and CAPP activity are conserved in S. cerevisiae. The identical stereochemical and structural requirements in both the biological and phosphatase assays suggest that the anti-proliferative effects of ceramide in yeast may be mediated in part through the action of CAPP.
神经酰胺正逐渐成为哺乳动物细胞生长和分化的一种潜在生理调节因子。这种调节可能是通过一种丝氨酸/苏氨酸神经酰胺激活蛋白磷酸酶(CAPP)的作用来介导的。在本研究中,对酿酒酵母中神经酰胺介导的细胞调节途径的存在进行了研究。用1 - 20微摩尔可透过细胞的神经酰胺(C2 - 神经酰胺)孵育指数生长的酿酒酵母细胞,产生了剂量依赖性的增殖抑制。许多其他脂质和去污剂,如花生四烯酸、油酸、曲拉通X - 100、二辛酰甘油和苯氨基醇神经酰胺类似物,大多无效,这证明了反应的特异性。证明了立体特异性,即赤藓糖型C2 - 神经酰胺的D对映体比L对映体更有效。更显著的是,证明了对C2 - 神经酰胺有高度特异性的结构要求,即1 - 12微摩尔的C2 - 二氢神经酰胺在抑制生长方面完全无效。由于C2 - 二氢神经酰胺缺乏C2 - 神经酰胺中存在的4 - 5反式双键,这表明C2 - 神经酰胺的抗增殖特性取决于双键的存在。这提出了一个有趣的可能性;负责在内源性神经酰胺合成过程中引入双键的脱氢酶可能通过控制二氢神经酰胺和神经酰胺的细胞浓度来调节细胞生长。负责在植物神经酰胺中引入最终羟基的加氧酶在酵母中可能提供类似的调节功能。接下来研究了CAPP在酵母中神经酰胺作用的潜在作用。酿酒酵母的粗提物也含有一种依赖神经酰胺的丝氨酸/苏氨酸磷酸酶活性,该活性对冈田酸抑制敏感。这种酶表现出与神经酰胺诱导的生长抑制相同的立体特异性和结构要求。我们得出结论,酿酒酵母中对神经酰胺的生长抑制反应和CAPP活性都是保守的。生物学和磷酸酶测定中相同的立体化学和结构要求表明,神经酰胺在酵母中的抗增殖作用可能部分是通过CAPP的作用来介导的。