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目的:设计合成灯盏乙素生物素标记探针4和10,并考查其抗肿瘤活性。方法:以灯盏乙素苷元与生物素为原料,经过酯化反应、酰胺反应、水解反应、取代反应等,在灯盏乙素苷元的4’位引入生物素标记,得到灯盏乙素生物素标记探针4和10,并对其进行细胞水平的抗肿瘤活性研究。结果:合成的探针化合物及中间体均经过1H-NMR,13C-NMR,ESI-MS进行了结构表征,确证结构与目标产物一致。细胞实验结果表明灯盏乙素生物素标记探针4和10均具有较好的抗肿瘤活性。结论:灯盏乙素生物素标记探针4和10均表现出与灯盏乙素相当的抗肿瘤活性,将为进一步的灯盏乙素抗肿瘤靶标的发现奠定基础。
OBJECTIVE: To design and synthesize steryl bine biotin labeled probes 4 and 10 and to examine its antitumor activity. Methods: Using scutellarin aglycones and biotin as raw materials, biotinylation was introduced at the 4′-position of scutellarin aglycones through esterification reaction, amide reaction, hydrolysis reaction, and substitution reaction to obtain breviscapine biotin. Probes 4 and 10 were labeled and studied for their antitumor activity at the cellular level. RESULTS: The synthesized probe compounds and their intermediates were characterized by 1H-NMR, 13C-NMR and ESI-MS. The structures were confirmed to be consistent with the target products. The results of cell experiments showed that scutellarin biotin labeled probes 4 and 10 all had good antitumor activity. CONCLUSIONS: Both scutellarin-biotinylated probes 4 and 10 exhibit antitumor activity comparable to scutellarin and will lay the foundation for the further discovery of scutellarin antitumor targets.