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首页> 外文期刊>World Journal of Gastroenterology >Antitumor efficacy of lidamycin on hepatoma and active moiety of its molecule
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Antitumor efficacy of lidamycin on hepatoma and active moiety of its molecule

机译：利达霉素对肝癌及其分子活性部分的抗肿瘤作用

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AIM: To study the in vitro and in VIVO antitumor effect of lidamycin (LDM) on hepatoma and the active moiety of its molecule. METHODS: MTT assay was used to determine the growth inhibition of human hepatoma BEL-7402 cells, SMMC-7721 cells and mouse hepatoma H22 cells. The In vivo therapeutic effects of lidamycin and mitomycin C were determined by transplantable hepatoma 22 (H22) in mice and human hepatoma BEL-7402 xenografts in athymic mice. RESULTS: In terms of IC_(50) values, the cytotoxicity of LDM was 10 000-fold more potent than that of mitomycin C (MMC) and adriamycin (ADM) in human hepatoma BEL-7402 cells and SMMC-7721 cells. LDM molecule consists of two moieties, an aproprotein (LDP) and an enediyne chromophore (LDC). In terms of IC_(50) values, the potency of LDC was similar to LDM. However, LDP was 10~5-fold less potent than LDM and LDC to hepatoma cells. For mouse hepatoma H22 cells, the IC_(50) value of LDM was 0.025 nmol/L. Given by single intravenous injection at doses of 0.1, 0.05 and 0.025 mg/kg, LDM markedly suppressed the growth of hepatoma 22 in mice by 84.7%, 71.6% and 61.8%, respectively. The therapeutic indexes (TI) of LDM and MMC were 15 and 2.5, respectively. By 2 iv. injections in two experiments, the growth inhibition rates by LDM at doses of 0.1, 0.05, 0.025, 0.00625 and 0.0125 mg/kg were 88.8-89.5%, 81.1-82.5%, 71.2-74.9%, 52.3-59.575%, and 33.3-48.3%, respectively. In comparison, MMC at doses of 5, 2.5, and 1.25 mg/kg inhibited tumor growth by 69.7-73.6%, 54.0-56.5%, and 31.5-52.2%, respectively. Moreover, in human hepatoma BEL-7402 xenografts, the growth inhibition rates by LDM at doses of 0.05 mg/kg x2 and 0.025 mg/kg x2 were 68.7% and 27.2%, respectively. However, MMC at the dose of 1.25 mg/kg x2 showed an inhibition rate of 34.5%. The inhibition rate of tumor growth by LDM was higher than that by MMC at the tolerated dose. CONCLUSION: Both LDM and its chromophore LDC display extremely potent cytotoxicity to hepatoma cells. LDM shows a remarkable therapeutic efficacy against murine and human hepatomas in vivo.
机译：目的：研究利达霉素（LDM）对肝癌及其分子活性部分的体外和体内抗肿瘤作用。方法：采用MTT法检测人肝癌BEL-7402细胞，SMMC-7721细胞和小鼠肝癌H22细胞的生长抑制作用。利达霉素和丝裂霉素C的体内治疗作用由小鼠中的可移植肝癌22（H22）和无胸腺小鼠中的人肝癌BEL-7402异种移植物确定。结果：就IC_（50）值而言，LDM对人肝癌BEL-7402细胞和SMMC-7721细胞的细胞毒性比丝裂霉素C（MMC）和阿霉素（ADM）的细胞毒性强1万倍。 LDM分子由两个部分组成，一个是前蛋白（LDP），一个是二烯基生色团（LDC）。就IC_（50）值而言，LDC的效力类似于LDM。然而，LDP对肝癌细胞的效力比LDM和LDC低10-5倍。对于小鼠肝癌H22细胞，LDM的IC_（50）值为0.025 nmol / L。通过以0.1、0.05和0.025 mg / kg的剂量进行单次静脉内注射，LDM显着抑制小鼠肝癌22的生长，分别达到84.7％，71.6％和61.8％。 LDM和MMC的治疗指数（TI）分别为15和2.5。到2 iv。在两个实验中，LDM在0.1、0.05、0.025、0.00625和0.0125 mg / kg剂量下的生长抑制率分别为88.8-89.5％，81.1-82.5％，71.2-74.9％，52.3-59.575％和33.3-分别为48.3％。相比之下，MMC的剂量分别为5、2.5和1.25 mg / kg，分别抑制肿瘤生长69.7-73.6％，54.0-56.5％和31.5-52.2％。此外，在人肝癌BEL-7402异种移植物中，LDM在0.05 mg / kg x2和0.025 mg / kg x2剂量下的生长抑制率分别为68.7％和27.2％。但是，MMC的剂量为1.25 mg / kg x2时，抑制率为34.5％。在耐受剂量下，LDM对肿瘤生长的抑制率高于MMC。结论：LDM及其生色团LDC均对肝癌细胞具有极强的细胞毒性。 LDM在体内对鼠类和人肝癌显示出显着的治疗功效。

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