Hu Z L, Zhang J P, Zhao J P, Tian M, Li G C, Qian D H
Research Laboratory of Natural and Synthetic Drugs, School of Pharmacy, Second Military University, Shanghai.
Yao Xue Xue Bao. 1993;28(5):332-6.
The effects of six naphthalenesulfonamide derivatives were studied on the LPS-induced release of tumor necrosis factor (TNF) from mouse peritoneal macrophages primed with A23187. The calmodulin (CaM) antagonist, N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7) and its derivatives N-(6-aminobutyl)-5-chloro-1-naphthalenesulfonamide and N-(6-aminoethyl)-5-chloro-1-naphthalenesulfonamide (10-400 ng/ml) were found to inhibit LPS-induced TNF release in a dose-dependent manner, and the protein kinase C (PKC) activator, N-(n-heptyl)-5-chloro-1-naphthalenesulfonamide (SC-10) and its two derivatives, N-(n-quinyl)-5-chloro-1-naphthalenesulfonamide and N-(n-butyl)-5-chloro-1-naphthalenesulfonamide (1-16 micrograms/ml) were shown to increase LPS-induced TNF release at suboptimal doses in a dose-dependent manner. These results suggest that the LPS-induced release of TNF is CaM-dependent and PKC may play an important role in this process.
研究了六种萘磺酰胺衍生物对脂多糖（LPS）诱导的、经A23187预处理的小鼠腹腔巨噬细胞释放肿瘤坏死因子（TNF）的影响。发现钙调蛋白（CaM）拮抗剂N-(6-氨基己基)-5-氯-1-萘磺酰胺（W-7）及其衍生物N-(6-氨基丁基)-5-氯-1-萘磺酰胺和N-(6-氨基乙基)-5-氯-1-萘磺酰胺（10 - 400纳克/毫升）以剂量依赖方式抑制LPS诱导的TNF释放，而蛋白激酶C（PKC）激活剂N-(正庚基)-5-氯-1-萘磺酰胺（SC-10）及其两种衍生物N-(正喹基)-5-氯-1-萘磺酰胺和N-(正丁基)-5-氯-1-萘磺酰胺（1 - 16微克/毫升）在次优剂量下以剂量依赖方式增加LPS诱导的TNF释放。这些结果表明，LPS诱导的TNF释放依赖于CaM，并且PKC可能在此过程中起重要作用。
