CAJ | 학술논문

目的合成新型有机锗喹啉酯倍半氧化物,研究它们对体外培养PC-3M细胞的抑制作用,分析作用机理,研究分子结构和抗癌活性之间的关系.方法利用氧化还原、加成、酰化、水解等反应合成了2种新型有机锗喹啉酯化合物.用MTT方法研究化合物分别在10μM,30μM和60μM对PC-3M癌细胞的抑制作用.显微镜下观察药物作用后的PC-3M细胞形态,应用流式细胞光度术检测药物对PC-3M细胞周期的影响.结果 2种化合物对PC-3M的IC50分别为10μM和30μM;10～30μM浓度的药物能使细胞皱缩,碎片增加,药物不仅强烈抑制了细胞的增值,而且对细胞形态也产生了严重影响.细胞生长过程中,G0/G1和G2/M期细胞数量减少而S期细胞数量明显增多.结论合成的新化合物对体外培养PC-3M癌细胞的增殖具有很强的抑制作用,药物与细胞核内DNA发生了相互作用.化合物中甲基的存在不利于抗癌作用的发挥.
목적 합성신형유궤타규람지배반양화물,연구타문대체외배양PC-3M세포적억제작용,분석작용궤리,연구분자결구화항암활성지간적관계.방법 이용양화환원、가성、선화、수해등반응합성료2충신형유궤타규람지화합물.용MTT방법연구화합물분별재10μM,30μM화60μM대PC-3M암세포적억제작용.현미경하관찰약물작용후적PC-3M세포형태,응용류식세포광도술검측약물대PC-3M세포주기적영향.결과 2충화합물대PC-3M적IC50분별위10μM화30μM;10～30μM농도적약물능사세포추축,쇄편증가,약물불부강렬억제료세포적증치,이차대세포형태야산생료엄중영향.세포생장과정중,G0/G1화G2/M기세포수량감소이S기세포수량명현증다.결론 합성적신화합물대체외배양PC-3M암세포적증식구유흔강적억제작용,약물여세포핵내DNA발생료상호작용.화합물중갑기적존재불리우항암작용적발휘.
Objective To synthesize new organogermanium compounds with stronger cytotoxic activities, and study the relationship between the structure and anticancer activity.Methods Two novel organogermanium sesquioxides with quinoline moiety were synthesized by a new method. Cell growth inhibition was measured by the MTT method. PC-3M prostate cancer cell line was treated with newly synthesized compounds. at 10 μm, 30 μm and 60 μm, respectively. The experiments were repeated three times.Results The IC50 of compounds were l0μm and 30μM, respectively. Cell morphology studies indicate that 10-30μM can cause cell irregularity, shrinking, and even fragmentation. Flow cytometeric data showed that the cell number in G0/G1 and G2/M phase was decreased but increased dramatically in S phase in the presence of the compounds.Conclusion The novel compounds exhibited stronger cytotoxic activities. DNA may be the primary target for the newly synthesized Ge132-quinoline compounds.