半人工合成手性多西紫杉醇对肺腺癌细胞株A549的细胞毒性及放射增敏作用

目的：探讨半人工合成手性多西紫杉醇对人肺癌细胞株A549的细胞毒性及放射增敏作用。方法：半人工合成手性多西紫杉醇，测定其对A549细胞的生长抑制作用，观察其对A549细胞的形态学影响及其放射增敏作用和对动物荷瘤模型的作用。结果：不同浓度半人工合成紫杉醇对A549细胞均有抑制作用，可引起A549细胞G2／M期阻滞，抑制荷瘤小鼠模型肿瘤的生长，其中空白对照组、单纯药物组、单纯放射组和联合处理组的肿瘤体积分别为（7780±1050）mm^3、（4610±950）mm^3、（5540±1035）mm^3和（560±112．5）mm^3。各组间有明显差异。结论：半人工合成紫杉醇对A549细胞株具有明显的抑制作用，且与射线照射有协同作用。

Study of toxicity and radiosensitizing effect of semi-artificial synthetic chiral docetaxel on human lung adenocarcinoma cell line A549.

Objective：To study the toxicity and radiosensitizing effect of semi-artificial synthic chiral docetaxel on human lung adenocareinoma cell line A549. Methods：The chiral docetaxel was synthesized chemically. Inhibition effect of docetaxel on the growth of A549 was determined by MTT assay. The differences of morphology changes were observed by inverted fluoresenee microscope. The A549 cells and mouse-beared tumor were treated with chemically synthesized docetaxel and the inhibitory effects on A549 cells were observed. Results：There were significent differences of inhibition rate among different docetaxel eoncerntrations and time. Treatment of doeetaxel and radiation caused A549 cells G2/M bloek. The xenograft subcutaneous lung cancer cell line A549 of nude mice was successfully reduced by docetaxel. And the volumes of transplantive tumor in control group, docetaxel group, radiation group and docetaxel combined radiation group were （ 7 780 ± 1 050 ） mm^3, （4 610 ± 950 ）mm^3, （ 5 540 ± 1 035 ） mm^3 and （ 560 ± 112. 5 ） mm^3, respectively. Conclusion：Senti-artificial synthetic chiral docetaxel had significantly radiosensitizing effect and toxicity on A549 cells.