目的： 观察三肽化合物酪丝亮肽的抗肿瘤作用，探讨其对单核巨噬细胞的激活作用。 方法： 观察YSL对人肝癌BEL-7402裸鼠移植瘤的抑制作用；观察YSL对体外培养BEL-7402细胞体系的抑制作用；观察YSL对PEMφ杀伤肿瘤细胞BEL-7402及B16-F10的影响；观察YSL对PEMφ分泌合成IL-1β，TNF-α和NO等细胞毒效应分子的影响。 结果： YSL能显著抑制BEL-7402移植瘤裸鼠的肿瘤生长，给药剂量为160 μg/(kg·d)时疗效最显著，抑制率为44.03％；YSL体外对BEL-7402细胞生长有一定的抑制作用，与阴性对照组比较有显著性差异（P<0.05）；YSL能增强裸鼠PEMφ对BEL-7402，B16-F10杀伤作用，与生理盐水对照组相比有显著性差异（P<0.05）；YSL能增强Balb/c小鼠PEMφ对BEL-7402,B16-F10杀伤作用，与生理盐水对照组相比有显著性差异（P<0.05）；YSL能促进小鼠PEMφ分泌合成细胞毒效应分子IL-1β，TNF-α和NO，与生理盐水对照组相比有显著性差异（P<0.05）。 结论： YSL能够抑制BEL-7402的增殖，增强单核巨噬细胞的细胞毒功能，促进细胞毒效应分子IL-1β，TNF-α和NO的分泌合成。

Objective: To investigate the anti-tumor effects of the tripeptide tyroserleutide (YSL) and to discuss its mechanisms by activating monocyte-macrophages. Methods: To apply human hepatocarcinoma BEL-7402 tumor transplanted in nude mice to examine the anti-tumor effects of YSL. To apply human hepatocarcinoma cell BEL-7402 to investigated the cytotoxicity of YSL against human hepatocarcinoma BEL-7402 cell line in vitro. To explore the activating effects of YSL on the peritoneal macrophage (PEMφ) functions of cytotoxicity against tumor cell lines (BEL-7402, B16-F10) in vitro and to detected the effects of YSL on the content of cytotoxicity effectors IL-1β, TNF-α and NO produced by PEMφ. Results: YSL could inhibit the growth of transplanted tumor BEL-7402 in nude mice, the inhibition rate of 160 μg/(kg·d) was 44.03%. The tumoricidal activity of YSL against BEL-7402 cell line in vitro was observed when compared with the control group ( P <0.05). YSL could activated PEMφ of nude mice and markedly enhance cytotoxicity against tumor cell lines (BEL-7402, B16-F10) when compared with the control group ( P <0.05). YSL could activated PEMφ of Balb/c mice and marked enhance cytotoxicity against tumor cell lines (BEL-7402, B16-F10) when compared with producing group ( P <0.05). YSL could stimulate the contents of the cytotoxicity effectors of IL-1β, TNF-α and NO produced by PEMφ ( P <0.05). Conclusions: YSL had inhibition functions against human hepatocarcinoma BEL-7402.YSL could increase the cytotoxicity of monocyte-macrophages and stimulate producing of the contents of the cytotoxicity effector of IL-1β, TNF-α and NO.

国家“863”高技术研究发展计划资助项目（2004AA2z3170）; 教育部重点项目（03007）