Yanapirut P, Berger M R, Reinhardt M, Schmähl D
Deutsches Krebsforschungszentrum, Institut für Toxikologie und Chemotherapie, Heidelberg, Fed. Rep. of Germany.
Arzneimittelforschung. 1991 Jun;41(6):652-5.
The in vitro antineoplastic activity of hexadecylphosphocholine (HPC, CAS 58066-85-6) on methylnitrosourea (MNU)-induced mammary carcinoma in Sprague-Dawley rats and human mammary carcinoma was investigated with the modified Hamburger-Salmon-Colony-Assay (HSCA). The effect of HPC was also compared with ilmofosine (alkyllysophospholipid derivative) and N-(2-chloroethyl-N-nitroso-N'-2-hydroxyethylurea (HECNU). Moreover, the modified HSCA was performed with bone marrow cells and KB cells. In this investigation, no specific antineoplastic effect of the test compounds on MNU-induced mammary carcinoma and human mammary carcinoma was found in HSCA. Thus the antineoplastic activity of the compounds could not be compared on these cell types. In vitro, effects were only observed in bone marrow and KB cells at a very low concentration. The in vitro effect of HPC on mammary carcinoma cells, evaluated through HSCA, did not predict the effect of HPC in vivo. The reason has remained unknown but some hypotheses are discussed. Because of the contrary results of HPC in vitro and in vivo, it should be pointed out that drug development in this class of compounds mainly has to depend on in vivo experiments.
采用改良的汉堡-萨尔蒙集落形成试验（HSCA），研究了十六烷基磷酸胆碱（HPC，化学物质登记号58066-85-6）对甲基亚硝基脲（MNU）诱导的斯普拉格-道利大鼠乳腺癌和人乳腺癌的体外抗肿瘤活性。还将HPC的作用与 ilmofosine（烷基溶血磷脂衍生物）和N-(2-氯乙基)-N-亚硝基-N'-2-羟乙基脲（HECNU）进行了比较。此外，用骨髓细胞和KB细胞进行了改良的HSCA。在本研究中，在HSCA中未发现受试化合物对MNU诱导的乳腺癌和人乳腺癌有特异性抗肿瘤作用。因此，无法在这些细胞类型上比较化合物的抗肿瘤活性。在体外，仅在极低浓度下在骨髓和KB细胞中观察到作用。通过HSCA评估的HPC对乳腺癌细胞的体外作用并不能预测HPC在体内的作用。原因尚不清楚，但讨论了一些假设。由于HPC在体外和体内的结果相反，应该指出，这类化合物的药物开发主要必须依赖于体内实验。
