Konno Y, Takahashi S, Naruse R, Mikami T, Matsumoto T, Suzuki S, Suzuki M
Department of Microbiology, Tohoku College of Pharmacy, Miyagi, Japan.
Biol Pharm Bull. 1994 May;17(5):748-52. doi: 10.1248/bpb.17.748.
A conjugate of bleomycin (BLM) and the mannan of bakers' yeast (Saccharomyces cerevisiae wild type strain) (WNM) was synthesized. The assay of its antimetastatic effect on Lewis lung carcinoma (3LL) implanted in C57BL/6 mice showed that this conjugate exhibited a higher antimetastatic effect and longer life-span elongation than those of free bleomycin and mannan with corresponding doses. This conjugate was also found to kill the 3LL cells in vitro. 14C-Labeled mannan-bleomycin conjugate was much more bound than 14C-labeled dextran-bleomycin conjugate to the 3LL. It was concluded that the anti-cancer mechanism of this conjugate, WNM-BLM possessed a specific binding effect to the tumor cells and exhibited a cytocidal effect on the 3LL target cells.
合成了博来霉素(BLM)与面包酵母(酿酒酵母野生型菌株)甘露聚糖(WNM)的共轭物。对植入C57BL/6小鼠体内的Lewis肺癌(3LL)进行的抗转移作用测定表明,与相应剂量的游离博来霉素和甘露聚糖相比,该共轭物表现出更高的抗转移作用和更长的寿命延长效果。还发现该共轭物在体外可杀死3LL细胞。14C标记的甘露聚糖 - 博来霉素共轭物比14C标记的葡聚糖 - 博来霉素共轭物与3LL的结合更多。得出结论,该共轭物WNM - BLM的抗癌机制对肿瘤细胞具有特异性结合作用,并对3LL靶细胞表现出杀细胞作用。