Ohmura E, Tsushima T, Emoto N, Obuchi E, Shizume K
Life Sci. 1987 Aug 10;41(6):691-6. doi: 10.1016/0024-3205(87)90448-6.
The effects of compounds with tumor promoting activity (mezerein, teleocidin and palytoxin) on rat growth hormone (rGH) release was compared to that of TPA (12-O-tetradecanoyl phorbol-13-acetate). Mezerein and teleocidin both of which are activators of protein kinase C (TPA type tumor promoter), elicited rGH release about 3.5 to 4 fold above control values. The ED 50 was 16 nM for mezerein, 1.1 nM for teleocidin and 1.5 nM for TPA. In contrast to mezerein or teleocidin, a non-TPA type tumor promoter (palytoxin) which does not activate protein kinase C failed to stimulate rGH release. These observations suggest that the activation of protein kinase C is essential in the release of rGH induced by the tumor promoters.
将具有促肿瘤活性的化合物(芫花酯甲、远藤菌素和岩沙海葵毒素)对大鼠生长激素(rGH)释放的影响与12-O-十四酰佛波醇-13-乙酸酯(TPA)进行了比较。芫花酯甲和远藤菌素均为蛋白激酶C的激活剂(TPA类肿瘤促进剂),它们引起的rGH释放比对照值高约3.5至4倍。芫花酯甲的半数有效剂量(ED50)为16 nM,远藤菌素为1.1 nM,TPA为1.5 nM。与芫花酯甲或远藤菌素不同,一种不激活蛋白激酶C的非TPA类肿瘤促进剂(岩沙海葵毒素)未能刺激rGH释放。这些观察结果表明,蛋白激酶C的激活在肿瘤促进剂诱导的rGH释放中至关重要。