Cui Weina, Wang Chao, Zhao Ming, Peng Shiqi
College of Pharmaceutical Sciences, Peking University, Beijing, PR China.
Prep Biochem Biotechnol. 2002 Aug;32(3):253-68. doi: 10.1081/PB-120013472.
The objective of this study was to establish the solution method of GHRPS, the synthetic oligopeptides Tyr-Gly-Gly-Phe-Met-NH2, Tyr-Gly-Gly-Phe-Met-OH, Tyr-Gly-Gly-Phe-Leu-NH2, Tyr-Gly-Gly-Phe-Leu-OH, Tyr-Gly-Gly-Phe-Gly-NH2, and Tyr-Gly-Gly-Phe-Gly-OH, to verify their effect on osteoporosis. Male ICR mice (20+/-2 g) were used. The intramuscular injection dose of 6.3 mg/kg prednisone induced a significant decrease of body and femur weight of the animals. The subcutaneous injection dose of 18 microg/kg synthetic peptide was not effective to prevent the decrease of body and femur weight of the animals. The subcutaneous injection dose of 6.3 mg/kg prednisone elicited a decrease in content of femur calcium and in the level of serum calcium of the animals. The subcutaneous injection dose of 18 microg/kg Tyr-Gly-Gly-Phe-Leu-NH2, or Tyr-Gly-Gly-Phe-Leu-OH, or Tyr-Gly-Gly-Phe-Gly-NH2 significantly increased the content of femur calcium and decreased the level of serum calcium of the animals. It was also observed that the subcutaneous injection dose of 18 microg/kg Tyr-Gly-Gly-Phe-Gly-OH, Tyr-Gly-Gly-Phe-Leu-OH, Tyr-Gly-Gly-Phe-Met-OH, Tyr-Gly-Gly-Phe-Met-NH2 significantly increased the content of femur phosphorous and decreased the activity of ALP of the animals.
本研究的目的是建立生长激素释放肽类似物（GHRPS）的解决方法，即合成寡肽酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-甲硫氨酸-NH2、酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-甲硫氨酸-OH、酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-亮氨酸-NH2、酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-亮氨酸-OH、酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-甘氨酸-NH2和酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-甘氨酸-OH，以验证它们对骨质疏松症的影响。使用雄性ICR小鼠（20±2 g）。肌肉注射剂量为6.3 mg/kg的泼尼松导致动物体重和股骨重量显著下降。皮下注射剂量为18 μg/kg的合成肽对预防动物体重和股骨重量的下降无效。皮下注射剂量为6.3 mg/kg的泼尼松导致动物股骨钙含量和血清钙水平下降。皮下注射剂量为18 μg/kg的酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-亮氨酸-NH2、或酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-亮氨酸-OH、或酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-甘氨酸-NH2显著增加了动物股骨钙含量并降低了血清钙水平。还观察到，皮下注射剂量为18 μg/kg的酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-甘氨酸-OH、酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-亮氨酸-OH、酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-甲硫氨酸-OH、酪氨酸-甘氨酸-甘氨酸-苯丙氨酸-甲硫氨酸-NH2显著增加了动物股骨磷含量并降低了碱性磷酸酶活性。
