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L-脯氨酸-间-双(2-氯乙基)胺基-L-苯丙氨酰基-L-正缬氨酸乙酯盐酸盐(MF13)是一个新颖的含三肽的氮芥类化合物。本课题组以往的体内外研究数据表明,MF13单药给药时,对多种不同来源的人肝癌细胞系均有较强的抗增殖活性。本文主要研究MF13与其他抗肿瘤药物联合使用时对肝癌的抑制作用。联合化疗体外实验结果显示,MF13与丝裂霉素C(MMC)在适宜浓度下联合应用时,对Bel-7402细胞的抗增殖活性有协同作用;MF13与长春新碱(VCR)联用无协同作用。联合化疗裸鼠体内实验结果表明,2 mg·kg~(-1) MF13与50 mg·kg~(-1)环磷酰胺(CTX)或2 mg·kg~(-1) MMC联用,协同作用显著;然而,2 mg·kg~(-1) MF13与0.3 mg·kg~(-1) VCR联合使用时无协同作用。联合化疗的体内外实验结果一致。本研究结果表明,无论单药给药还是联合化疗,MF13都是一个有潜在应用前景的抗肝癌化合物。
L-Proline-m-bis (2-chloroethyl) amino-L-phenylalanyl-L-norvaline ethyl ester hydrochloride (MF13) is a novel tripeptide-containing nitrogen mustard Compounds. Our previous data from in vitro and in vivo studies showed that MF13 alone had a strong antiproliferative activity on human hepatocellular carcinoma cell lines of many different origins. This article focuses on the MF13 and other anti-tumor drugs when used in combination with the inhibition of liver cancer. The results of combination chemotherapy showed that the combination of MF13 and mitomycin C (MMC) had a synergistic effect on the antiproliferative activity of Bel-7402 cells when treated with appropriate concentration of MF13. Combination of MF13 with VCR effect. The results of in vivo experiments in combination chemotherapy of nude mice showed that MF13 at 2 mg · kg -1 was synergized with 50 mg · kg -1 cyclophosphamide (CTX) or 2 mg · kg -1 MMC, However, there was no synergistic effect when 2 mg · kg -1 MF13 was administered in combination with 0.3 mg · kg -1 VCR. The results of in vitro and in vivo experiments were the same. The results of this study show that MF13 is a potential anti-hepatoma compound with potential application both in monotherapy and in combination with chemotherapy.