Bastert G, Schmidt-Matthiesen H, Voelcker G, Peter G, Hohorst H J
Z Krebsforsch Klin Onkol Cancer Res Clin Oncol. 1975 Sep 22;84(1):37-47. doi: 10.1007/BF00305687.
A new in vitro assay for screening the sensitivity of human tumour cells against Cyclophosphamide has been developed. While biologically activated Cyclophosphamide was unsuitable because of unpurities in the material, synthetic 4-Hydroxycyclophosphamide was shown to inhibit the incorporation of tritiated uridine and thymidine into the nucleic acids of human tumour cells in vitro. 29 tumours including 14 mammarial carcinomas, 8 ovarial carcinomas and 7 other malignant tumours were tested. While 12 tumours showed a significant and 5 only a slight inhibition of the 3H-uridine incorporation in vitro. 12 tumours showed no effect. Histologically none-differentiated tumours were more sensitive against 4-Hydroxycyclophosphamide as compared with the more differentiated ones. First observations point to 4-Hydroperoxycyclophosphamide instead of 4-Hydroxycyclophosphamide as a more suitable form of activated Cyclophosphamid for the in vitro assay of Cyclophosphamide sensitiveness because of the higher stability and better availability of this compound.
已开发出一种用于筛选人肿瘤细胞对环磷酰胺敏感性的新型体外测定法。由于材料中存在杂质，生物活化的环磷酰胺不适用，而合成的4-羟基环磷酰胺在体外可抑制氚化尿苷和胸腺嘧啶核苷掺入人肿瘤细胞的核酸中。对29个肿瘤进行了测试，其中包括14个乳腺癌、8个卵巢癌和7个其他恶性肿瘤。12个肿瘤在体外对3H-尿苷掺入表现出显著抑制，5个仅表现出轻微抑制，12个肿瘤无作用。组织学上，未分化肿瘤比高分化肿瘤对4-羟基环磷酰胺更敏感。初步观察表明，由于4-氢过氧环磷酰胺具有更高的稳定性和更好的可用性，它比4-羟基环磷酰胺更适合作为环磷酰胺体外敏感性测定中活化环磷酰胺的形式。
