Erjavec F, Ferjan I
Department of Pharmacology, Medical Faculty, University of Ljubljana, Yugoslavia.
Agents Actions. 1990 Apr;30(1-2):125-7. doi: 10.1007/BF01969016.
Cardiotonic glycosides modify histamine secretion from rat mast cells in the following way. (1) Preincubation (30 min) of mast cells with liposoluble glycosides (10(-4) mol/l) increases the spontaneous histamine secretion by about 5%. (2) Preincubation of mast cells with 10(-4) mol/l liposoluble glycosides (digitoxin, digoxin, digitoxigenine) decreases histamine release induced by compound 48/80 in the presence of calcium, whereas the water soluble glycoside, strophanthin G, has no effect on the secretion. (3) Preincubation of mast cells in a calcium-free medium with the glycosides (10(-4) mol/l) has a dual-effect on histamine secretion induced by compound 48/80: water soluble glycosides (strophanthin G and K) potentiate histamine release, whereas the liposoluble glycosides (digitoxin, digitoxigenine) decrease the secretory response. The difference in the activity of different glycosides could be explained by their dual effects, namely an inhibition of Na+K(+)-ATPase which leads to an increase in histamine release, and intracellular action(s) of liposoluble glycosides leading to a decrease of histamine secretion.
强心苷以如下方式改变大鼠肥大细胞的组胺分泌。(1)肥大细胞与脂溶性苷(10⁻⁴mol/L)预孵育(30分钟)可使组胺自发分泌增加约5%。(2)肥大细胞与10⁻⁴mol/L脂溶性苷(地高辛、洋地黄毒苷、洋地黄毒苷元)预孵育可降低在有钙存在时由化合物48/80诱导的组胺释放,而水溶性苷毒毛花苷G对分泌无影响。(3)肥大细胞在无钙培养基中与苷(10⁻⁴mol/L)预孵育对化合物48/80诱导的组胺分泌有双重作用:水溶性苷(毒毛花苷G和K)增强组胺释放,而脂溶性苷(地高辛、洋地黄毒苷元)降低分泌反应。不同苷活性的差异可由其双重作用来解释,即抑制Na⁺K⁺-ATP酶导致组胺释放增加,以及脂溶性苷的细胞内作用导致组胺分泌减少。