Mu Y, Kamada H, Kodaira H, Sato K, Tsutsumi Y, Maeda M, Kawasaki K, Nomizu M, Yamada Y, Mayumi T
Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamadaoka, Osaka, Suita, 565-0871, Japan.
Biochem Biophys Res Commun. 1999 Nov 2;264(3):763-7. doi: 10.1006/bbrc.1999.1567.
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.
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。
