Cisplatin is an effective drug for treating various cancer types. However, it is highly toxic for both healthy and tumor cells. Therefore, there is a need to reduce its therapeutic dose and increase targeted bioavailability. One of the ways to achieve this could be the coating of cisplatin with polysaccharides and specific carriers for targeted delivery. Nucleic acid aptamers could be used as carriers for the specific delivery of medicine to cancer cells. Cisplatin-arabinogalactan-aptamer (Cis-AG-Ap) conjugate was synthesized based on Cis-dichlorodiammineplatinum, Siberian larch arabinogalactan, and aptamer AS-42 specific to heat-shock proteins (HSP) 71 kDa (Hspa8) and HSP 90-beta (Hsp90ab1). The antitumor effect was estimated using ascites and metastatic Ehrlich tumor models. Cis-AG-Ap toxicity was assessed by blood biochemistry on healthy mice. Here, we demonstrated enhanced anticancer activity of Cis-AG-Ap and its specific accumulation in tumor foci. It was shown that targeted delivery allowed a 15-fold reduction in the therapeutic dose of cisplatin and its toxicity. Cis-AG-Ap sufficiently suppressed the growth of Ehrlich's ascites carcinoma, the mass and extent of tumor metastasis in vivo. Arabinogalactan and the aptamers promoted cisplatin efficiency by enhancing its bioavailability. The described strategy could be very promising for targeted anticancer therapy.

中文翻译：

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核酸适配体提高顺铂-阿拉伯半乳聚糖偶联物的体内抗癌效率并降低其毒性

顺铂是治疗多种癌症的有效药物。然而，它对健康细胞和肿瘤细胞都具有剧毒。因此，需要降低其治疗剂量并提高靶向生物利用度。实现这一目标的方法之一可能是用多糖和特定载体包被顺铂以进行靶向递送。核酸适体可用作将药物特异性递送至癌细胞的载体。顺铂-阿拉伯半乳聚糖-适体 (Cis-AG-Ap) 偶联物​​是基于顺式-二氯二氨铂、西伯利亚落叶松阿拉伯半乳聚糖和热休克蛋白 (HSP) 71 kDa (Hspa8) 和 HSP 90-β (HSP 90-beta) 特异性适体 AS-42 合成的热休克蛋白 90ab1)。使用腹水和转移性艾氏肿瘤模型评估抗肿瘤作用。顺式-AG-Ap 毒性通过血液生化对健康小鼠进行评估。在这里，我们证明了 Cis-AG-Ap 的增强抗癌活性及其在肿瘤灶中的特异性积累。结果表明，靶向递送可使顺铂的治疗剂量及其毒性降低 15 倍。Cis-AG-Ap充分抑制艾氏腹水癌的生长、肿瘤转移的质量和范围体内。阿拉伯半乳聚糖和适体通过提高顺铂的生物利用度来提高顺铂的效率。所描述的策略对于靶向抗癌治疗可能非常有前途。