层粘连蛋白相关肽YIGSR与聚乙烯吡咯烷酮的生物偶联由于更长的血浆半衰期而增强了其抗转移作用。

Bioconjugation of laminin-related peptide YIGSR with polyvinyl pyrrolidone increases its antimetastatic effect due to a longer plasma half-life.

作者信息

Mu Y, Kamada H, Kodaira H, Sato K, Tsutsumi Y, Maeda M, Kawasaki K, Nomizu M, Yamada Y, Mayumi T

机构信息

Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamadaoka, Osaka, Suita, 565-0871, Japan.

出版信息

Biochem Biophys Res Commun. 1999 Nov 2;264(3):763-7. doi: 10.1006/bbrc.1999.1567.

DOI:10.1006/bbrc.1999.1567

PMID:10544005

Abstract

Polyvinyl pyrrolidone (PVP) which can be radically synthesized and have a long blood residency was used to modify the laminin-related peptide YIGSR, and its inhibitory effect on experimental lung metastasis of B16-BL6 melanoma cells was examined. The antimetastatic effect of PVP-conjugated YIGSR (PVP-YIGSR) was more than 100-fold greater than that of native YIGSR. When injected intravenously, PVP-YIGSR showed more than a 15-fold longer plasma half-life relative to native YIGSR. In addition, the stability of YIGSR in plasma was increased by conjugation with PVP. These findings suggest that PVP is a useful polymeric modifier for increasing the antimetastatic activity of YIGSR.

摘要

可通过自由基合成且具有较长血液驻留时间的聚乙烯吡咯烷酮（PVP）用于修饰层粘连蛋白相关肽YIGSR，并检测其对B16-BL6黑色素瘤细胞实验性肺转移的抑制作用。PVP偶联的YIGSR（PVP-YIGSR）的抗转移作用比天然YIGSR大100多倍。静脉注射时，PVP-YIGSR的血浆半衰期相对于天然YIGSR延长了15倍以上。此外，YIGSR与PVP偶联后在血浆中的稳定性增加。这些发现表明，PVP是一种用于增强YIGSR抗转移活性的有用聚合物修饰剂。