INHIBITION OF 12-O-TETRADECANOYLPHORBOL-13-ACETATE-STIMULATED (PI)-P-32 INCORPORATION INTO PHOSPHOLIPIDS AND PROTEIN-PHOSPHORYLATION BY 2,7,11-CEMBRATRIENE-4,6-DIOL, AN ANTI-TUMOR-PROMOTING AGENT
INHIBITION OF 12-O-TETRADECANOYLPHORBOL-13-ACETATE-STIMULATED (PI)-P-32 INCORPORATION INTO PHOSPHOLIPIDS AND PROTEIN-PHOSPHORYLATION BY 2,7,11-CEMBRATRIENE-4,6-DIOL, AN ANTI-TUMOR-PROMOTING AGENT
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DOI：
10.1159/000226545
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发表时间：
1988-03-01
期刊：
影响因子：
3.5
通讯作者：
OHNISHI, A
中科院分区：
文献类型：
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作者：
SAITO, Y;NISHINO, H;OHNISHI, A
α-β-D-半乳糖苷的抗肿瘤促进活性的可能机制2，7，11-柏木三烯-4，6-二醇（α- CBT）进行了研究。α- CBT可抑制TPA刺激的HeLa细胞磷脂中~（32）Pi的掺入。与其他许多抗肿瘤促进剂与钙调素相互作用的性质相反，这些抗肿瘤促进剂被证明抑制TPA刺激的钙调素。32 Pi掺入磷脂中，α- CBT没有显示出与钙调蛋白的任何相互作用;即，通过与Ca+-钙调蛋白结合而增强的N-苯基-1-萘胺的荧光不受α-钙调蛋白处理的影响。认知行为疗法发现TPA刺激的47-kilodation蛋白的磷酸化被人血小板中的蛋白激酶C所磷酸化，该磷酸化被α-认知行为疗法然而，3 H-TPA与小鼠表皮颗粒部分的特异性结合不受α-TPA处理的抑制。认知行为疗法这些结果表明α- CBT通过另一种作用模式而不是对其受体位点的作用来抑制蛋白激酶C的活性，并且该作用和钙调蛋白非依赖性的对α-CBT的磷脂代谢的抑制作用被证明是有效的。CBT可能在体内发挥一定的抗肿瘤促进作用。
A possible mechanism of antitumor-promoting activity of .alpha.-2,7,11-cembratriene-4,6-diol (.alpha.-CBT) was studied. .alpha.-CBT inhibited the 32Pi incorporation into phospholipids of HeLa cells stimulated by 12-O-tetradecanolyphorbol-13-acetate (TPA). In contrast to the property to interact with calmodulin of many other antitumor-promoting agents, which were proved to inhibit TPA-stimulated. 32Pi incorporation into phospholipids, .alpha.-CBT did not show any interaction with calmodulin; i.e., the fluorescence of N-phenyl-1-naphthylamine enhanced by binding with Ca+-calmodulin was not influenced by treatment with .alpha.-CBT. TPA-stimulated phosphorylation of 47-kilodation protein, which is phosphorylated by protein kinase C in human platelets, was found to be inhibited by .alpha.-CBT. However, the specific binding of 3H-TPA to mouse epidermal pariculate fraction was not inhibited by treatment with .alpha.-CBT. These results suggest that .alpha.-CBT inhibits the activity of protein kinase C by another mode of action rather than the effect on its receptor site, and that this action and calmodulin-independent inhibitiory effect on phospholipid metabolism of .alpha.-CBT may play a certain role in its antitumor-promoting activity in vivo.