根皮素的磷酸化衍生物可抑制培养的神经元和神经胶质肿瘤细胞中环状AMP的积累。

Phosphorylated derivatives of phloretin inhibit cyclic AMP accumulation in neuronal and glial tumor cells in culture.

作者信息

Ortmann R, Nutto D, Jackisch R

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1978 Dec;305(3):233-40. doi: 10.1007/BF00498816.

Abstract

The potencies of polyphloretin phosphate, di-4-phloretin phosphate, 4-phloretin phosphate and phloretin to inhibit the stimulation of cAMP accumulation by prostaglandins, isoproterenol and adenosine were studied in 2 clonal cell lines of CNS origin. The sequence of potency to inhibit PGE1 effects was the same in neuroblastoma (N4TG3) and human astrocytoma cells (1321N1): di-4-phloretin phosphate greater than polyphloretin phosphate greater than phloretin greater than 4-phloretin phosphate. The inhibition of PGE1 stimulated cAMP accumulation by the most prostaglandin-specific inhibitor di-4-phloretin phosphate was rapidly established after its addition, fully reversible after a 30 min preincubation period and independent of the presence of calcium. Kinetic studies of the inhibition of PGE1 effects by di-4-phloretin-phosphate suggest a different type of inhibition in 1321N1 and N4TG3 cells.

摘要

在两种中枢神经系统来源的克隆细胞系中，研究了聚磷酸根皮苷、二 - 4 - 磷酸根皮苷、4 - 磷酸根皮苷和根皮苷抑制前列腺素、异丙肾上腺素和腺苷刺激环磷酸腺苷（cAMP）积累的能力。在神经母细胞瘤（N4TG3）和人星形细胞瘤细胞（1321N1）中，抑制前列腺素E1（PGE1）作用的能力顺序相同：二 - 4 - 磷酸根皮苷＞聚磷酸根皮苷＞根皮苷＞4 - 磷酸根皮苷。最具前列腺素特异性的抑制剂二 - 4 - 磷酸根皮苷添加后能迅速抑制PGE1刺激的cAMP积累，在预孵育30分钟后完全可逆，且与钙的存在无关。二 - 4 - 磷酸根皮苷抑制PGE1作用的动力学研究表明，在1321N1和N4TG3细胞中存在不同类型的抑制作用。