Philipov S, Ivanovska N, Nikolova P
Institute of Organic Chemistry, Bulgarian Academy of Sciences, Sofia, Bulgaria.
Pharmazie. 1998 Oct;53(10):694-8.
The inhibitory effect of 15 semi-synthetic analogues of glaucine (1) on the lipopolysaccharide (LPS)-induced and the concanavalin A (Con A)-induced proliferation of mouse splenocytes was compared in vitro. Isoboldine (3), bracteoline (4) and dehydroglaucine (9) showed a significantly higher potency to suppress LPS-induced proliferation than 1, while 7-hydroxy-4-methylglaucine (8), 7-formyldehydroglaucine (11), 7-acetyldehydroglaucine (13), 7-benzoyldehydroglaucine (14), oxoglaucine (15) and glaucine-quinol (16) were less inhibitory. Compounds 3, 4, boldine (5), 15 and 16 surpassed significantly the inhibition expressed by 1 on Con A-induced proliferative response. The effect was equal to the inhibition determined for mitomycin C (Mit C) with both mitogens. In contrast to all others analogues, thaliporphine (2) stimulated splenocyte proliferation in both assays. Antibody response against sheep red blood cells (SRBC) was lowered most strongly by cataline (6), 7-methyldehydroglaucine (10) and 16.
在体外比较了15种青藤碱（1）的半合成类似物对脂多糖（LPS）诱导的和伴刀豆球蛋白A（Con A）诱导的小鼠脾细胞增殖的抑制作用。异波尔定（3）、苞叶碱（4）和去氢青藤碱（9）对LPS诱导的增殖的抑制效力显著高于1，而7-羟基-4-甲基青藤碱（8）、7-甲酰基去氢青藤碱（11）、7-乙酰基去氢青藤碱（13）、7-苯甲酰基去氢青藤碱（14）、氧代青藤碱（15）和青藤碱喹啉（16）的抑制作用较弱。化合物3、4、波尔定（5）、15和16对Con A诱导的增殖反应的抑制作用显著超过1。该作用与用两种促细胞分裂剂测定的丝裂霉素C（Mit C）的抑制作用相当。与所有其他类似物相反，紫堇灵（2）在两种测定中均刺激脾细胞增殖。对绵羊红细胞（SRBC）的抗体反应被加他林（6）、7-甲基去氢青藤碱（10）和16最强烈地降低。
