Chillemi F, Francescato P, Fraccari A, Galatulas I
Dipartimento di Chimica Organica e Industriale, Milano, Italy.
Anticancer Res. 1998 Mar-Apr;18(2A):757-8.
In search of more potent compounds endowed with a cytotoxic activity, a new series of basic peptides was synthesized using solid-phase methods. All peptides were purified by preparative reverse-phase HPLC and characterized by electrospray mass spectrometry. The cytotoxic activity was determined in cultured HeLa cells. The hexadecapeptides 5 and 6 showed a 50% inhibition at the concentration of 30 micrograms/ml. The salmina and the polyamino acids of L-arginine, L-histidine and L-lysine, containing sixteen residues, were virtually inactive. This demonstrates that a specific peptide sequence is necessary to obtain a positive response in HeLa test.
为了寻找具有更强细胞毒性活性的化合物，采用固相方法合成了一系列新的碱性肽。所有肽均通过制备型反相高效液相色谱法纯化，并通过电喷雾质谱进行表征。在培养的HeLa细胞中测定细胞毒性活性。十六肽5和6在浓度为30微克/毫升时显示出50%的抑制率。含有16个残基的鲑精蛋白以及L-精氨酸、L-组氨酸和L-赖氨酸的多氨基酸实际上没有活性。这表明在HeLa试验中获得阳性反应需要特定的肽序列。
