Abstract

A series of new berbamine derivatives were synthesized, and their cytotoxic activity was evaluated against Human T-cell lymphoma cell line H9 and multiple myeloma cell line RPMI8226 in vitro. Compared with berbamine, the cytotoxicity of the modified derivatives was enhanced, especially simultaneously substituted at OH and 5-position. Compounds 2a and 4b exhibited high antitumor activity. The IC₅₀ value of compound 2a was 0.30 μM for RPMI8226 cells, and the IC₅₀ value of compound 4b was 0.36 μM for H9 cells, whereas berbamine IC₅₀ values were 4.0 μM for H9 cells and 6.19 μM for RPMI8226 cells, respectively.

摘要

合成了一系列新的小檗胺衍生物，并在体外评估了它们对人 T 细胞淋巴瘤细胞系 H9 和多发性骨髓瘤细胞系 RPMI8226 的细胞毒活性。与小檗胺相比，修饰衍生物的细胞毒性增强，尤其是同时取代了 OH 和 5 位。化合物2a和4b表现出高抗肿瘤活性。化合物2a的IC ₅₀值对RPMI8226细胞为0.30 μM ，化合物4b对H9细胞的IC ₅₀值为0.36 μM，而小檗胺IC ₅₀值对H9细胞为4.0 μM，对RPMI8226细胞为6.19 μM。