Quetin-Leclercq J, Dupont L, Wright C W, Phillipson J D, Warhurst D C, Angenot L
Service de Pharmacognosie, Institut de Pharmacie, Universitè de Liège, Belgium.
J Pharm Belg. 1991 Mar-Apr;46(2):85-92.
The analyses of the different possible conformations of usambarensine, tubulosine and emetine, which possess interesting cytotoxic and amoebicide properties showed us that they cannot take the planar conformation proposed to explain the activity of this type of molecules on protein synthesis. Nevertheless, a common (non planar) conformation exists where the angles between the two plans containing the aromatic rings are nearly the same for the three compounds. This fact could confirm the hypothesis of a common receptor which would be slightly different in amoebae because of its higher sensitivity to usambarensine.
对具有有趣的细胞毒性和杀阿米巴特性的乌桑巴任碱、微管碱和吐根碱的不同可能构象进行分析后,我们发现它们无法采取为解释这类分子对蛋白质合成的活性而提出的平面构象。然而,存在一种共同的(非平面)构象,对于这三种化合物而言,包含芳香环的两个平面之间的夹角几乎相同。这一事实可以证实存在共同受体的假说,由于变形虫对乌桑巴任碱的敏感性更高,该受体在变形虫中可能会略有不同。