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目的:合成(5-氟脲嘧啶-1-乙酸)-4’-姜黄素酯并考察其抗肿瘤活性。方法:5-氟脲嘧啶(5-FU)与氯乙酸在碱性条件下反应得到5-氟脲嘧啶-1-基乙酸(3),再与姜黄素成酯得到(5-氟脲嘧啶-1-乙酸)-4’-姜黄素酯(4);MTT法测定化合物4抗HL60、K562、SGC7901、SW480细胞增殖的活性;H22荷瘤小鼠连续腹腔注射给药8 d后颈椎脱臼处死,剥离肿瘤称重,计算抑瘤率。结果:(5-氟脲嘧啶-1-乙酸)-4’-姜黄素酯抑制HL60、K562、SGC7901、SW480细胞增殖的IC50分别为5.774,11.05,17.83,13.67μg.mL-1;经腹腔注射给予不同剂量的化合物4(80,160,320 mg.kg-1),其对H22荷瘤小鼠肿瘤生长的抑制率分别为26.85%,30.65%和61.37%,与阴性对照组比较,320 mg.kg-1剂量组具有显著性差异(P<0.01)。结论:(5-氟脲嘧啶-1-乙酸)-4’-姜黄素酯体外能明显抑制HL60、K562、SGC7901、SW480等肿瘤细胞增殖,对H22荷瘤小鼠肿瘤生长具有抑制作用,并呈一定量效关系。
AIM: To synthesize (5-fluorouracil-1-acetic acid) -4’-curcumin and study its anti-tumor activity. METHODS: 5-Fluorouracil (5-FU) was reacted with chloroacetic acid under basic condition to get 5-fluorouracil-1-yl acetic acid (3) (4). The activity of compound 4 against HL60, K562, SGC7901 and SW480 cells was measured by MTT assay. After H22 tumor-bearing mice were treated with continuous intraperitoneal injection for 8 days, the cervical dislocation was sacrificed, Peel the tumor weighed, calculate the inhibition rate. Results: IC50 of (5-fluorouracil-1-acetic acid) -4’-curcumin ester on the proliferation of HL60, K562, SGC7901 and SW480 cells were 5.774, 11.05, 17.83 and 13.67 μg.mL- Different doses of Compound 4 (80,160,320 mg.kg-1) were 26.85%, 30.65% and 61.37% respectively for H22 tumor-bearing mice. Compared with the negative control group, the inhibitory rates of 320 mg.kg-1 The dose group had significant difference (P <0.01). CONCLUSION: (5-Fluorouracil-1-acetic acid) -4’-curcumin can significantly inhibit the proliferation of HL60, K562, SGC7901 and SW480 tumor cells in vitro and inhibit the growth of H22 tumor-bearing mice A certain amount of effective relationship.