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目的探讨放线菌素２３－２１（Ａｃｔ２３－２１）的抗肿瘤作用以及对敏感肿瘤细胞核酸和蛋白质合成、ｃＡＭＰ含量的影响。方法Ｐ３８８、Ｌ１２１０白血病小鼠抑瘤实验观察Ａｃｔ２３－２１对荷瘤鼠生存期的影响；中性红活染及台盼蓝排染法测定Ａｃｔ２３－２１对体外癌细胞的抑制作用；液体闪烁计数法测量氚标记前体参入肿瘤细胞核酸或蛋白质的速率；放射免疫法测定细胞内ｃＡＭＰ含量。结果Ａｃｔ２３－２１对小鼠Ｐ３８８、Ｌ１２１０白血病均有抑制效应，以Ｐ３８８受抑更显著，小鼠生存期延长率达１１５％；对多种体外癌细胞如ＨＬ－６０、ＳＧＣ－７９０１、ＦＧＣ８５、Ｈｅｌａ、ＭＧＣ８０３具有显著抑制作用，其中ＨＬ－６０、ＳＧＣ－７９０１细胞最敏感；对Ｐ３８８、ＳＧＣ－７９０１、ＨＬ－６０细胞的［３Ｈ］ＵＲ参入具有快速明显的抑制；对艾氏腹水癌、ＨＬ－６０细胞的ｃＡＭＰ含量具有显著的提高作用。结论Ａｃｔ２３－２１具有抗肿瘤作用，同时抑制肿瘤细胞ＲＮＡ合成、提高肿瘤细胞ｃＡＭＰ含量。
Objective To investigate the anti-tumor effects of actinomycin 23-21 (Act23-21) and its effects on nucleic acid, protein synthesis and cAMP content in sensitive tumor cells. Methods The anti-tumor effect of P388 and L1210 leukemia mice was observed to observe the effect of Act23-21 on the survival time of tumor-bearing mice. Neutral red staining and trypan blue exclusion were used to determine the inhibitory effect of Act23-21 on cancer cells in vitro. Liquid scintillation counting was performed. The rate of incorporation of precursor-incorporated nucleic acids or proteins into tumor cells was measured by radioimmunoassay, and intracellular cAMP content was determined by radioimmunoassay. RESULTS: Act23-21 had inhibitory effects on P388 and L1210 leukemia in mice. The inhibition of P388 was more pronounced, and the survival rate of mice was increased by 115%. Various in vitro cancer cells such as HL-60, SGC-7901, and FGC85 were found. Hela and MGC803 have significant inhibitory effects, among which HL-60 and SGC-7901 cells are the most sensitive; they have rapid and obvious inhibition of [3H]UR incorporation into P388, SGC-7901, and HL-60 cells; Ehrlich ascites carcinoma, HL The -60 cells had a significant increase in cAMP content. Conclusion Act23-21 has anti-tumor effect, while inhibiting RNA synthesis in tumor cells and increasing cAMP content in tumor cells.