Monteith D K, Henry S P, Howard R B, Flournoy S, Levin A A, Bennett C F, Crooke S T
Isis Pharmaceuticals, Carlsbad, CA 92008, USA.
Anticancer Drug Des. 1997 Jul;12(5):421-32.
Treatment of rodents with phosphorothioate oligodeoxynucleotides induces a form of immune stimulation characterized by splenomegaly, lymphoid hyperplasia, hypergammaglobulinemia and mixed mononuclear cellular infiltrates in numerous tissues. Immune stimulation was evaluated in mice with in vivo and in vitro studies using a review of historical data and specific in vivo and in vitro studies. All phosphorothioate oligodeoxynucleotides evaluated induced splenomegaly and B-lymphocyte proliferation. Splenomegaly and B-lymphocyte proliferation increased with dose or concentration of oligodeoxynucleotide. Splenomegaly appeared to occur, at least in part, as a result of stimulation of B-lymphocyte proliferation. There were differences with respect to degree or potency of immune stimulation by different oligodeoxynucleotides. The rank order potencies for B-lymphocyte proliferation in vitro and splenomegaly correlated well for the oligodeoxynucleotides tested. Particular oligodeoxynucleotide sequence motifs or palindromes have been demonstrated to affect in vitro cell proliferation. Inclusion of a 5'-AACGTT-3' palindrome in a phosphorothioate oligodeoxynucleotide sequence significantly enhanced the potency. While inclusion of this palindrome or a CpG motif alone may contribute to the immune stimulation, these palindromes and motifs were clearly not the sole factor required for immune stimulation. Several phosphorothioate oligodeoxynucleotides that did not contain a CpG motif still induced immune stimulation in mice. The immune stimulation induced by phosphorothioate oligodeoxynucleotides was an effect of this class of compounds to which rodents are acutely sensitive.
用硫代磷酸酯寡脱氧核苷酸处理啮齿动物会引发一种免疫刺激形式,其特征为脾肿大、淋巴样增生、高球蛋白血症以及众多组织中的混合单核细胞浸润。通过回顾历史数据以及进行特定的体内和体外研究,在小鼠中评估了免疫刺激情况。所有评估的硫代磷酸酯寡脱氧核苷酸均诱导了脾肿大和B淋巴细胞增殖。脾肿大和B淋巴细胞增殖随寡脱氧核苷酸的剂量或浓度增加而增加。脾肿大似乎至少部分是由于B淋巴细胞增殖受到刺激所致。不同的寡脱氧核苷酸在免疫刺激的程度或效力方面存在差异。所测试的寡脱氧核苷酸在体外B淋巴细胞增殖和脾肿大方面的效力排序相关性良好。已证明特定的寡脱氧核苷酸序列基序或回文结构会影响体外细胞增殖。在硫代磷酸酯寡脱氧核苷酸序列中包含5'-AACGTT-3'回文结构可显著增强效力。虽然单独包含此回文结构或CpG基序可能有助于免疫刺激,但这些回文结构和基序显然不是免疫刺激所需的唯一因素。几种不含CpG基序的硫代磷酸酯寡脱氧核苷酸仍能在小鼠中诱导免疫刺激。硫代磷酸酯寡脱氧核苷酸诱导的免疫刺激是这类化合物的一种作用,啮齿动物对此类化合物极为敏感。