Tondelli L, Garbesi A, Morelli S, Calastretti A, Copreni E, Gong L, Nicolin A
ICoCEA, CNR, Bologna Italy.
Anticancer Drugs. 1996 Feb;7(2):189-94.
An oligodeoxynucleotide (ODN), capable of reducing the growth of human B lymphocytes carrying the t(14;18) chromosome translocation, was prepared in different 'chemical versions': unmodified phosphodiester, phosphorothioate and phosphodiester capped with L-2'-deoxycytidine. Their binding affinity to the complementary synthetic target was studied by the melting point assay. The ODNs, administered to DOHH2 cells, were compared for stability in the culture medium, cellular uptake, time course of the intact sequence concentration within the cell and ability to inhibit cell growth. The 5', 3'-L-capped derivative and the phosphorothioate had comparable potency, superior to that of the unmodified ODN, in agreement with the concentration of undegraded ODNs within the cell.
制备了一种能够抑制携带t(14;18)染色体易位的人B淋巴细胞生长的寡脱氧核苷酸(ODN)，其有不同的“化学形式”：未修饰的磷酸二酯、硫代磷酸酯以及用L-2'-脱氧胞苷封端的磷酸二酯。通过熔点测定法研究了它们与互补合成靶标的结合亲和力。将这些ODN应用于DOHH2细胞，比较它们在培养基中的稳定性、细胞摄取、细胞内完整序列浓度的时间进程以及抑制细胞生长的能力。5'、3'-L封端衍生物和硫代磷酸酯具有相当的效力，优于未修饰的ODN，这与细胞内未降解ODN的浓度一致。
