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目的:合成1,8-二羟基-3-乙酰基-6-甲基-9,10蒽醌,探讨该合成产物对人卵巢癌细胞(SKOV3)的生长抑制作用。方法:以大黄素为基础结构,化学全合成1,8-二羟基-3-乙酰基-6-甲基-9,10蒽醌;构建SKOV3与人脐静脉血管内皮细胞(HUVEC)的交换培养液条件共培养体系,以卡铂为对照药,MTT法检测合成产物对单独培养SKOV3和HUVEC的半数抑制浓度(IC50)及条件共培养体系中两种细胞的IC50。结果:化合物结构经IR,1H-NMR和13C-NMR确证。合成产物和卡铂对单独培养SKOV3的IC50分别为111.72,177.63μmol·L-1,对单独培养HUVEC的IC50分别为198.11,131.53μmol·L-1;合成产物和卡铂对条件共培养体系中SKOV3的IC50分别为104.48,180.7μmol·L-1,对HUVEC的IC50分别为239.22,178.62μmol·L-1。结论:1,8-二羟基-3-乙酰基-6-甲基-9,10蒽醌显示出比卡铂更为优越的抑制卵巢癌细胞生长活性;合成产物对单独培养和条件培养基共培养细胞的IC50值不同,反映了单细胞体系与条件培养基共培养体系在药物筛选结果上的差异。
OBJECTIVE: To synthesize 1,8-dihydroxy-3-acetyl-6-methyl-9,10-anthraquinone and investigate the inhibitory effect of this synthetic product on human ovarian cancer cell line SKOV3. METHODS: Emodin was used as the basic structure to synthesize 1,8-dihydroxy-3-acetyl-6-methyl-9,10-anthraquinone chemically. The exchange culture between SKOV3 and human umbilical vein endothelial cells (HUVECs) Liquid condition co-culture system and carboplatin as control. The half-inhibitory concentration (IC50) of the synthesized product on SKOV3 and HUVEC alone and the IC50 of two kinds of cells under the condition of co-culture system were measured by MTT assay. Results: The structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR. IC50 of the synthesized product and carboplatin alone cultured SKOV3 were 111.72,177.63μmol·L-1, IC50 of cultured HUVEC were 198.11, 131.53μmol·L-1 respectively; the synthesis product and carboplatin in conditional co-culture system The IC50 of SKOV3 was 104.48,180.7μmol·L-1, and the IC50 of HUVEC were 239.22,178.62μmol·L-1, respectively. CONCLUSION: 1,8-dihydroxy-3-acetyl-6-methyl-9,10-anthraquinone showed more superior inhibitory effect on the growth of ovarian cancer cells than carboplatin. IC50 values of cultured cells are different, reflecting the single cell system and conditioned medium co-culture system in drug screening results on the differences.