Brunet C, Luyckx M, Cazin M, Lesieur I, Lesieur D, Lespagnol C, Delacourte A, Mallevais M L
Methods Find Exp Clin Pharmacol. 1985 Nov;7(11):579-83.
Nine (amino-methyl)-2 acrylophenone derivatives having in vitro antimicrotubular activities very similar to those of colchicine are tested on Triton WR 1339-induced hyperlipidemia in rats. By producing a disorganization of the microtubular system, these drugs reduce the lipoprotein secretory process from hepatocytes, and more particularly the triglyceride-rich VLDL secretory process, such that the serum triglyceride, cholesterol and phospholipid levels are decreased. On the other hand, HDL-cholesterol and HDL-phospholipids are increased in a significant manner. Other studies show that serum apoprotein B levels are decreased while serum apoprotein A1 levels are increased. These results are interesting since atherogenous risk is now known to be dyslipemia-related, and is not the same according to the fact that lipids are bound to one or another lipoprotein. Among the four most effective compounds (5,7,8 and 9) three of them possess a methoxy group on the aromatic ring, which seems to distinguish that series from the other two.
九种（氨基甲基）-2-丙烯基苯酮衍生物在体外具有与秋水仙碱非常相似的抗微管活性，它们被用于检测对 Triton WR 1339 诱导的大鼠高脂血症的作用。通过引起微管系统的紊乱，这些药物减少了肝细胞的脂蛋白分泌过程，尤其是富含甘油三酯的极低密度脂蛋白（VLDL）的分泌过程，从而使血清甘油三酯、胆固醇和磷脂水平降低。另一方面，高密度脂蛋白胆固醇（HDL-胆固醇）和高密度脂蛋白磷脂显著增加。其他研究表明，血清载脂蛋白 B 水平降低，而血清载脂蛋白 A1 水平升高。这些结果很有意思，因为现在已知动脉粥样硬化风险与血脂异常有关，并且根据脂质与一种或另一种脂蛋白结合的情况而有所不同。在四种最有效的化合物（5、7、8 和 9）中，其中三种在芳香环上具有甲氧基，这似乎使该系列与其他两种有所区别。
