Paszkiewicz-Gadek A, Chlabicz J, Gałasiński W
Department of General and Organic Chemistry, Medical Academy, Białystok, Poland.
Pol J Pharmacol Pharm. 1988 Mar-Apr;40(2):183-90.
Five potential oncostatics of plant origin (reserpine, amphotericin B, rutoside, digoxin, dry aloe extract), and cyclic AMP were investigated for their effect on protein synthesis. The solutions of digoxin and dry aloe extract inhibited protein biosynthesis in vitro. The direct inhibiting effect of digoxin on the ribosomes suggests that this drug forms an inactive complex with this organelle. Therefore it can be concluded that ribosome is the target site of digoxin action. Aloin and aloeemodin are responsible for the inhibitory effect of the solution of dry aloe extract. They inhibit markedly [14C]-leucine incorporation into proteins. Aloin and aloeemodin do not influence directly the ribosomes, but they inhibit elongation factors and peptidyltransferase activities in the complete elongation system. Some preliminary experiments have shown that direct interaction between these substances and elongation factor EF-2 should be taken in account. This observation is the subject of further experiments, in which the characteristics of the inhibitory effect of the components isolated from dry aloe extract will be performed.
研究了五种植物源潜在抑癌剂(利血平、两性霉素B、芦丁、地高辛、干芦荟提取物)以及环磷酸腺苷对蛋白质合成的影响。地高辛溶液和干芦荟提取物溶液在体外抑制蛋白质生物合成。地高辛对核糖体的直接抑制作用表明该药物与这种细胞器形成无活性复合物。因此可以得出结论,核糖体是地高辛作用的靶位点。芦荟苷和芦荟大黄素是干芦荟提取物溶液产生抑制作用的原因。它们显著抑制[14C] - 亮氨酸掺入蛋白质。芦荟苷和芦荟大黄素不直接影响核糖体,但它们在完整的延伸系统中抑制延伸因子和肽基转移酶活性。一些初步实验表明,应考虑这些物质与延伸因子EF - 2之间的直接相互作用。这一观察结果是进一步实验的主题,在进一步实验中将研究从干芦荟提取物中分离出的成分的抑制作用特性。