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目的为提高灯盏乙素的生物利用度,设计合成了一系列灯盏乙素衍生物,评价其抗脂质过氧化和抗肿瘤的生物活性。方法通过羟乙基化、羟丙基化、酯化反应合成了一系列灯盏乙素衍生物,采用生化法测试部分衍生物对小鼠脑脂质过氧化产物丙二醛(malondialdehyde,MDA)的抑制作用,采用台盼蓝法测试体外抑制白血病细胞HL-60生长活性。结果合成了13个灯盏乙素衍生物,其中7个为未见文献报道的新化合物,其结构经1H-NMR和MS确证;化合物1、13对MDA的抑制作用显著,6-9具有中等强度的抗肿瘤活性。结论灯盏乙素结构中的酚羟基是其抑制脂质过氧化产物MDA的活性基团,葡萄糖醛酸的6-位游离羧基能够增强抗肿瘤活性。
Objective To improve the bioavailability of scutellarin, a series of scutellarin derivatives were designed and synthesized to evaluate the biological activity of anti-lipid peroxidation and anti-tumor. Methods A series of scutellarin derivatives were synthesized by hydroxyethylation, hydroxypropylation and esterification. The effects of some derivatives on malondialdehyde (MDA) Inhibition by trypan blue assay in vitro inhibition of leukemia cells HL-60 growth activity. Results Thirteen scutellarin derivatives were synthesized, of which seven were novel compounds which were not reported in the literature. Their structures were confirmed by 1H-NMR and MS. Compounds 1 and 13 had a significant inhibitory effect on MDA with 6-9 moderate intensity Antitumor activity. Conclusion The phenolic hydroxyl group in the scutellarin structure is the active group that inhibits the lipid peroxidation product MDA. The free carboxyl group at the 6-position of glucuronic acid can enhance the antitumor activity.