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首页> 外文期刊>Anticancer Research: International Journal of Cancer Research and Treatment >In vitro histoculture drug response assay and in vivo blood chemistry of a novel Pt(IV) compound, K104.
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In vitro histoculture drug response assay and in vivo blood chemistry of a novel Pt(IV) compound, K104.

机译：新型Pt（IV）化合物K104的体外组织培养药物反应测定和体内血液化学。

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BACKGROUND: The newly synthesized octahedral Pt(IV) complex series showed potent antitumor activities, both in vitro and in vivo. Carboplatin, possessing a soluble leaving ligand, is known to be less toxic than cisplatin. The synthesized K104 is a Pt(IV) complex with a malonato leaving group and seven-membered ring structure between the central platinum and amine carrier ligands. In this study, the histoculture drug response assay (HDRA) of K104 on human cancer tissues was investigated in vitro and nephrotoxicity was examined in vivo. MATERIALS AND METHODS: Cytotoxicity was tested in various cancer cell lines, and the HDRA of K104 was evaluated by MTT assay in vitro using colorectal and breast cancer tissues from patients. In order to compare the nephrotoxicity of K104 with cisplatin and carboplatin, blood serum levels of BUN, creatinine and uric acid in ICR mice were measured. RESULTS: K104 showed more effective anticancer activities than carboplatin in most cancer cell lines. In HDRA, K104 showed a 50.0-66.7% efficacy rate compared with 33.3% of cisplatin and 58.3% of carboplatin against colorectal cancer patient tissues. In breast cancer tissues, K104 only showed an efficacy rate above 50%. The serum levels of BUN, creatinine and uric acid did not change after a single intraperitoneal administration of K104 (90 mg/kg) in ICR mice. CONCLUSION: K104 showed more effective anticancer activities than carboplatin. Cisplatin was associated with nephrotoxic effects, but K104 did not change the serum levels of BUN, creatinine and uric acid in vivo. These results suggest that K104 is a promising anticancer agent in view of its high efficacy against human solid cancer and lower toxicity in vivo.
机译：背景：新合成的八面体Pt（IV）配合物系列在体外和体内均显示出有效的抗肿瘤活性。已知具有可溶的离去配体的卡铂的毒性小于顺铂。合成的K104是一种Pt（IV）络合物，具有丙二酸酯离去基团和中心铂和胺载体配体之间的七元环结构。在这项研究中，在体外研究了人类癌症组织上K104的组织培养药物反应测定（HDRA），并在体内检查了肾毒性。材料与方法：在多种癌细胞系中测试了细胞毒性，并使用来自患者的结直肠和乳腺癌组织通过MTT法体外评估了K104的HDRA。为了比较K104与顺铂和卡铂的肾毒性，测定了ICR小鼠的血清BUN，肌酐和尿酸水平。结果：在大多数癌细胞系中，K104显示出比卡铂更有效的抗癌活性。在HDRA中，K104对结直肠癌患者组织的有效率为50.0-66.7％，而顺铂为33.3％，卡铂为58.3％。在乳腺癌组织中，K104仅显示超过50％的有效率。在ICR小鼠中腹膜内注射K104（90 mg / kg）后，BUN，肌酐和尿酸的血清水平没有变化。结论：K104具有比卡铂更有效的抗癌活性。顺铂与肾毒性作用有关，但K104不能改变体内的BUN，肌酐和尿酸血清水平。这些结果表明，鉴于其对人实体癌的高功效和体内较低的毒性，K104是一种有前途的抗癌药。

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