47肽的微波辅助固相合成工艺研究

目的合成一长链肽47肽。方法采用Fmoc/t-Bu正交保护多肽固相合成策略,使用9-芴甲氧羰基(Fmoc)保护氨基酸的α-氨基,用Liberty微波多肽合成仪,每个耦合循环用20%哌啶脱除Fmoc保护基团,连续添加氨基酸,并用茚三酮法检测反应终点,有效检测反应的进度,最后用82.5%的三氟乙酸将多肽从树脂上切割下来,得到47肽粗品。经过反相高效液相制备系统纯化得到多肽纯品,用反相高效液相分析仪和傅里叶高分辨质谱仪验证该产物。结果高分辨质谱仪验证了该产物,纯品质量分数达98%。结论微波可促进多肽特别是长链肽的合成。

Synthesis of 47 peptide by microwave-assisted solid-phase technology

Objective To investigate the methods of enhancing the permeability in Cinnamon Cortex extract transdermal drug delivery system with ethosomes as a vector. Methods Cassia oil was extracted by steam distillation and injected into ethosomes with different concentration. The amount of cinnamic acid passing through the skin of SD male rats released from ethosomes was determined by HPLC under the model of Franz diffusion cells in vitro. Results Compared to CC, ethosome with 20% ethanol, the permeabilities of CC ethosomes with 30%, 40%, and 50% ethanol were increased by 1.31-, 1.69-, and 2.06-fold, respectively. Compared to CC ethosome with 30% ethanol, the permeabilities were increased by 2.31-, 1.10-, and 3.40-fold, with the penetration enhancer of Azone alone, propylene glycol alone or both, respectively. The permeability of CC ethosome gel was higher than that of CC ethosome and cassia oil gels. Conclusion The transdermal permeability of CC extract is enhanced by rising the concentration of ethanol, adding penetration enhancer, and preparing hydrogel.