Sasaki H, Niimi S, Akiyama M, Tanaka T, Hazato A, Kurozumi S, Fukushima S, Fukushima M
Department of Obstetrics and Gynecology, The Jikei University School of Medicine, Tokyo, Japan.
Cancer Res. 1999 Aug 15;59(16):3919-22.
One of the delta7-prostaglandin A1 derivatives with unique antitumor activities, 13,14-dihydro-15-deoxy-delta7-prostaglandin-A1-methyl ester, was integrated into lipid microspheres (Lipo-TEI9826) and examined for its antitumor effect in vitro and in vivo. The in vitro relative resistance of human ovarian cancer, A2780CP, to cisplatin (CDDP) and Lipo-TEI9826 was 27.3 and 2.0, respectively, compared with A2780, the parent cell line of A2780CP. In in vivo experiments, when A2780CP and the parent cell line A2780 were inoculated into nude mice, A2780CP grew two times more rapidly than did A2780. The growth of A2780CP tumor was not suppressed by CDDP, whereas that of the A2780 tumor was significantly suppressed. Nevertheless, the growth of both the A2780 and the A2780CP inoculated tumors was significantly inhibited by treatment with Lipo-TEI9826 at any time after the initial treatment, compared with the lipid microspheres only. These results show that Lipo-TEI9826 may be an effective antitumor agent and capable of overcoming CDDP resistance.
具有独特抗肿瘤活性的δ7-前列腺素A1衍生物之一，13,14-二氢-15-脱氧-δ7-前列腺素A1甲酯，被整合到脂质微球（Lipo-TEI9826）中，并对其体外和体内抗肿瘤作用进行了研究。与A2780CP的亲本细胞系A2780相比，人卵巢癌A2780CP对顺铂（CDDP）和Lipo-TEI9826的体外相对耐药性分别为27.3和2.0。在体内实验中，当将A2780CP和亲本细胞系A2780接种到裸鼠体内时，A2780CP的生长速度比A2780快两倍。A2780CP肿瘤的生长不受CDDP抑制，而A2780肿瘤的生长则受到显著抑制。然而，与仅使用脂质微球相比，在初始治疗后的任何时间，用Lipo-TEI9826治疗均能显著抑制接种A2780和A2780CP的肿瘤的生长。这些结果表明，Lipo-TEI9826可能是一种有效的抗肿瘤药物，并且能够克服CDDP耐药性。
