论文部分内容阅读
目的:对生物活性肽胰安肽的体外稳定性进行研究并初步评价其安全性。方法:取胰安肽分别在胃蛋白酶、胰蛋白酶溶液和血浆中进行孵育,采用电泳法和高效液相色谱法考察其酶稳定性和血浆稳定性;对小鼠灌胃给予胰安肽(15 mg.kg-1)38 d,测定脏器(脾、肝、肾和心脏)指数,对胰安肽进行安全性评价;以MTT法研究胰安肽对人肝细胞癌细胞HepG2细胞的体外增殖抑制作用。结果:胰安肽具有抗胃蛋白酶和胰蛋白酶降解作用,在血浆中具有一定的稳定性。连续给药后脏器指数与未给药的空白对照组比较无显著性差异,表明其对各脏器未见损害作用;胰安肽对HepG2细胞未见体外抑制作用。结论:胰安肽体外具有抗胃蛋白酶和胰蛋白酶降解的作用,长期给药安全性较好,具有开发为口服药物的潜力。
OBJECTIVE: To study the in vitro stability of the bioactive peptide pancreatin peptide and evaluate its safety. METHODS: Pancreatic peptide was incubated in pepsin, trypsin solution and plasma, respectively. The stability of the enzyme and stability of plasma were examined by electrophoresis and HPLC. mg.kg-1) for 38 days, and the safety of pancreatic peptide was evaluated. The proliferation of HepG2 cells in vitro was assayed by MTT assay Inhibition. Results: Pancreatic peptide has anti-pepsin and trypsin degradation, and has certain stability in plasma. After continuous administration, there was no significant difference between the organ index and the control group without drug administration, indicating that it had no damage to various organs. The pancreaticin peptide had no inhibitory effect on HepG2 cells in vitro. CONCLUSION: Pancreatic peptide has anti-pepsin and trypsin-degrading effects in vitro and is safe for long-term administration and has the potential of being developed as an oral drug.