Collery P, Lechenault F, Cazabat A, Juvin E, Khassanova L, Evangelou A, Keppler B
Département des Maladies Respiratoires, Hôpital Maison Blanche, Reims, France.
Anticancer Res. 2000 Mar-Apr;20(2A):955-8.
The effects of two gallium (Ga) compounds, Ga chloride (GaCl3) and tris(8-quinolinolato)Ga (III) on the viability of A549 human malignant lung adenocarcinoma cells were investigated. The results demonstrated that both drugs reduced the viability of A549 cells but to different extents. The inhibitory effects of tris(8-quinolinolato)Ga (III) were 10 times more profound than those produced by GaCl3. The IC50 was obtained with 2.5 microM of tris(8-quinolinolato)Ga (III) and 25 microM GaCl3 after an exposure time of 48 hours. Further, whereas the inhibitory effects of GaCl3 were both dose and time-dependent those of tris(8-quinolinolato)Ga (III) appeared to be only dose-dependent, indicating differences in their mechanism of action. Comparison with data drawn from the literature suggests that GaCl3 seems to be in the same range of activity as Ga nitrate or Ga-pyridoxal isocotinoyl hydrazone. Tris(8-quinolinolato)Ga (III) could be as effective as transferrin-Ga, but with the advantage of oral administration and a greater bioavailability of the tris(8-quinolinolato)Ga (III) compound.
研究了两种镓（Ga）化合物，氯化镓（GaCl3）和三（8-喹啉醇）镓（III）对A549人恶性肺腺癌细胞活力的影响。结果表明，两种药物均降低了A549细胞的活力，但程度不同。三（8-喹啉醇）镓（III）的抑制作用比GaCl3产生的抑制作用强10倍。在暴露48小时后，三（8-喹啉醇）镓（III）的IC50为2.5 microM，GaCl3的IC50为25 microM。此外，GaCl3的抑制作用是剂量和时间依赖性的，而三（8-喹啉醇）镓（III）的抑制作用似乎仅为剂量依赖性，表明它们的作用机制存在差异。与文献数据比较表明，GaCl3的活性范围似乎与硝酸镓或吡啶醛异烟酰腙镓相同。三（8-喹啉醇）镓（III）可能与转铁蛋白镓一样有效，但具有口服给药的优势，且三（8-喹啉醇）镓（III）化合物的生物利用度更高。
