Rietbroek R C, van de Vaart P J, Haveman J, Blommaert F A, Geerdink A, Bakker P J, Veenhof C H
Department of Medical Oncology, Academic Medical Centre, Amsterdam, The Netherlands.
J Cancer Res Clin Oncol. 1997;123(1):6-12. doi: 10.1007/BF01212608.
The cytotoxicity of cisplatin and cisplatin-DNA adduct formation in vitro and in vivo is clearly enhanced by hyperthermia. We investigated whether cytotoxicity and platinum-DNA adduct formation of two promising new third-generation platinum derivatives, lobaplatin [1,2-diamminomethylcyclobutane platinum(II) lactate] and oxaliplatin [oxalato-1,2-diaminocyclohexane platinum(II)], are also enhanced by hyperthermia. Cisplatin was used for comparison. SW 1573 cells were incubated with cisplatin, lobaplatin or oxaliplatin at different concentrations for 1 h at 37 degrees, 41 degrees and 43 degrees C. The reproductive capacity of cells was determined by cloning experiments. Immunocytochemical detection of platinum-DNA adducts was performed with the rabbit antiserum NKI-A59. At 37 degrees C, cisplatin was the most cytotoxic, followed by oxaliplatin and lobaplatin. Hyperthermia clearly enhanced the cytotoxicity of cisplatin, lobaplatin and oxaliplatin. There was no further increase in cytotoxicity at 43 degrees C compared to 41 degrees C for cisplatin and oxaliplatin. A further increase in cytotoxicity at 43 degrees C was observed for lobaplatin. At 43 degrees C thermal enhancement was higher for lobaplatin than for oxaliplatin, with the reverse pattern at 41 degrees C. For both drugs, thermal enhancement of cytotoxicity was lower than observed for cisplatin. Immunocytochemical detection of platinum-DNA adducts was feasible for all the drugs. Adduct formation was enhanced at 43 degrees C for cisplatin, lobaplatin and oxaliplatin with a relative increase of 410%, 170% and 180%. These results seem to confirm that an increase in platinum-DNA adduct formation is involved in the in vitro thermal enhancement of cytotoxicity. The observed thermal enhancement of cytotoxicity of lobaplatin and oxaliplatin in vitro warrants further in vivo investigations.
热疗可显著增强顺铂在体外和体内的细胞毒性以及顺铂 - DNA加合物的形成。我们研究了热疗是否也能增强两种有前景的新型第三代铂衍生物洛铂[1,2 - 二氨甲基环丁烷铂(II)乳酸盐]和奥沙利铂[草酸根 - 1,2 - 二氨基环己烷铂(II)]的细胞毒性及铂 - DNA加合物的形成。以顺铂作为对照。将SW 1573细胞分别与不同浓度的顺铂、洛铂或奥沙利铂在37℃、41℃和43℃下孵育1小时。通过克隆实验测定细胞的增殖能力。用兔抗血清NKI - A59进行铂 - DNA加合物的免疫细胞化学检测。在37℃时,顺铂的细胞毒性最强,其次是奥沙利铂和洛铂。热疗明显增强了顺铂、洛铂和奥沙利铂的细胞毒性。对于顺铂和奥沙利铂,43℃时的细胞毒性与41℃相比没有进一步增加。洛铂在43℃时细胞毒性进一步增加。在43℃时,洛铂的热增强作用高于奥沙利铂,而在41℃时则相反。对于这两种药物,细胞毒性的热增强作用均低于顺铂。所有药物的铂 - DNA加合物免疫细胞化学检测均可行。顺铂、洛铂和奥沙利铂在43℃时加合物形成增加,相对增加分别为410%、170%和180%。这些结果似乎证实铂 - DNA加合物形成的增加与细胞毒性的体外热增强有关。洛铂和奥沙利铂在体外观察到的细胞毒性热增强作用值得进一步进行体内研究。