Allemand I, Christ M, Pannecoucke X, Molina T, Luu B, Briand P
Laboratoire de Génétique et Pathologie Expérimentale, INSERM CJF 90-03, ICGM, Paris, France.
Anticancer Res. 1993 Jul-Aug;13(4):1097-101.
Among their biological properties, several oxysterols display a stronger toxicity towards tumor cells than towards normal cells. Water-soluble phosphodiesters of 7 beta-hydroxycholesterol (JB69 and XA29), that were proved to retain a specific antitumoral activity in vitro, have been recently developed, allowing in vivo studies. They have been assayed on transgenic mice expressing the Large T antigen of SV40 in their liver and developing systematically hepatocarcinoma within 8 months. We show that JB69 and XA29 administered intraperitoneally into transgenic mice, before the onset of adenoma, may prevent or delay the tumor development. Consequently, oxysterol derivatives might constitute new efficient prodrugs against naturally occurring tumors.
在其生物学特性中，几种氧化甾醇对肿瘤细胞的毒性比对正常细胞更强。7β-羟基胆固醇的水溶性磷酸二酯（JB69和XA29）已被证明在体外具有特定的抗肿瘤活性，最近已开发出来，可用于体内研究。它们已在肝脏中表达SV40大T抗原并在8个月内系统性发展为肝癌的转基因小鼠身上进行了测试。我们发现，在腺瘤出现之前腹腔注射到转基因小鼠体内的JB69和XA29可以预防或延缓肿瘤的发展。因此，氧化甾醇衍生物可能构成针对自然发生肿瘤的新型高效前药。
