Alberghina M, Brogna A, Mangiameli A, Marletta F, Rizzarelli E, Sammartano S
Farmaco Sci. 1982 Dec;37(12):805-14.
The effect of simple and mixed copper(II) complexes of L-tryptophan (trp) and L-phenylalanine (phe) on the gastric acid secretion was investigated in Shay rats. Graded doses (from 15 to 75 mg/kg) of [Cu(trp)2(H2O)], [Cu(phe)2(H2O)] and [Cu(trp)(phe)(H2O)], administered i.g., caused a progressive inhibition of gastric acid secretion. The antisecretory activity of the mixed complex, [Cu(trp)(phe)(H2O)], was significantly greater (ID50 = 33 +/- 3 mg/kg) than that of the simple complexes [Cu(trp)2(H2O)] (ID50 = 48 +/- 3 mg/kg) and [Cu(phe)2(H2O)] (ID50 = 43 +/- 3 mg/kg). At the experimental conditions of intragastric pH, the different biological activities were directly related to the percentage of neutral species present in solution as determined by means of potentiometric measurements (at 37 degrees, I = 0.15 mol dm-3 in NaClO4). A possible mechanism of action of the investigated compounds is discussed.
在沙伊大鼠中研究了L-色氨酸(trp)和L-苯丙氨酸(phe)的简单及混合铜(II)配合物对胃酸分泌的影响。经口给予不同剂量(15至75毫克/千克)的[Cu(trp)2(H2O)]、[Cu(phe)2(H2O)]和[Cu(trp)(phe)(H2O)],可逐渐抑制胃酸分泌。混合配合物[Cu(trp)(phe)(H2O)]的抗分泌活性(半数抑制剂量ID50 = 33 ± 3毫克/千克)明显高于简单配合物[Cu(trp)2(H2O)](ID50 = 48 ± 3毫克/千克)和[Cu(phe)2(H2O)](ID50 = 43 ± 3毫克/千克)。在胃内pH的实验条件下,通过电位测量法(在37摄氏度、I = 0.15摩尔/立方分米的高氯酸钠溶液中)测定,不同的生物活性与溶液中中性物种的百分比直接相关。文中还讨论了所研究化合物可能的作用机制。