Pauwels S, Dockray G J, Walker R
Gastroenterology. 1987 May;92(5 Pt 1):1220-5. doi: 10.1016/s0016-5085(87)91081-x.
The metabolism of synthetic human sulfated heptadecapeptide gastrin (G-17) was studied in normal human volunteers. Plasma concentrations were measured by radioimmunoassay using antibodies specific for intact G-17, and for the C- and N- terminus of G-17, during and after infusion of both sulfated and unsulfated G-17. With all three antibodies, plasma concentrations at a steady state were higher during infusion of sulfated compared with unsulfated G-17. In addition, the half-life in plasma measured by the three antibodies was two to five times higher for sulfated G-17 compared with unsulfated G-17. The half-life measured by N-terminal-specific antibodies was greater than that with antibodies specific for C-terminal or intact G-17. The difference was accounted for by the production during infusion of N-terminal fragments of relatively long half-life. The pattern of fragments generated during infusion of sulfated G-17 resembled that during unsulfated G-17 infusion, but there was no evidence of desulfation in the systemic circulation. The results indicate that in humans, sulfation protects G-17 from metabolism.
在正常人类志愿者中研究了合成的人硫酸化十七肽胃泌素（G-17）的代谢。在输注硫酸化和未硫酸化的G-17期间及之后，使用针对完整G-17以及G-17的C端和N端的特异性抗体，通过放射免疫测定法测量血浆浓度。使用所有三种抗体时，输注硫酸化G-17期间的稳态血浆浓度高于未硫酸化的G-17。此外，与未硫酸化的G-17相比，硫酸化G-17通过三种抗体测得的血浆半衰期高出两到五倍。通过N端特异性抗体测得的半衰期大于针对C端或完整G-17的特异性抗体测得的半衰期。这种差异是由于输注期间产生了半衰期相对较长的N端片段。输注硫酸化G-17期间产生的片段模式类似于输注未硫酸化G-17期间的模式，但在体循环中没有脱硫酸的证据。结果表明，在人类中，硫酸化可保护G-17不被代谢。
