ZHANG Ling-Xia, WANG Hui-Fen, LI Ke, ZHONG Bo-Hua, LIU Hong and PAN Yong. Experimental Studises Oil Viral Hepatitis Receptor——targeted Drug L——HSA-AraAMP[J]. Virologica Sinica, 1995, 10(4).
Citation: ZHANG Ling-Xia, WANG Hui-Fen, LI Ke, ZHONG Bo-Hua, LIU Hong, PAN Yong. Experimental Studises Oil Viral Hepatitis Receptor——targeted Drug L——HSA-AraAMP .VIROLOGICA SINICA, 1995, 10(4) : 283.

受体导向药物L-HSA-AraAMP的导向性及体外抗病毒效应的研究

  • 观察了用125I标记的受体导向药物──乳糖化人血清白蛋白单磷酸阿糖腺苷(L-HSA-AraAMP,简称交联物)在小鼠体内的分布情况,结果显示在肝肮内含量明显高于其它各脏器,表明药物的肝脏导向性能良好。同时观察到药物具有缓慢释放作用,从而增强了药效。用乙肝病毒DNA转染的肝癌细胞(2.2.15细胞)观察交联药物的抗病毒药效,结果显示交联物与AraAMp具有相似的抗病毒效应。两药对HBsAg的抑制率分别为50%、63%,对HBeAg为62.6%、67.2%。500μg/mlu交联物(其中含AraAMp为31.3μg/ml)与100μg/mlAraAMP对HBVDNA具有相似的抑制作用。两药对HBcAg抑制的选择指数分别大于4.8、1.7。显示交联物比AraAMP,在药效相似情况下可明显减少用量,降低毒性,延长作用时间。

Experimental Studises Oil Viral Hepatitis Receptor——targeted Drug L——HSA-AraAMP

  • Lactosaminated Human Serum Albumin(L-HSA)was,used as a carrier and coupled to Ara-binosied adenine monophospate(AraAMP).The distribution of 125I-labelled L-HSA-AraAMPwere higher in liver than in other organs.Radioactivities of the drug could still be measured atthe 7th dav after injection.The efficacy of targeted drug was determined by analyzing dynamic changes of HBsAg andHBeAg in 2.2.15 cell culture medium by RIA and changes in the replicative intracellular HBVDN A content by Southern blot.The results showed that the targeted drug had significantly in-hibitory ratio of HBsAg and HBeAg which was similar to AraAMP(inhibitory ratfo of HBsAg50%,63%;HBeAg 62.6%,67.2%,respectively).Southern blot test showed the replicativeintermedlates rcDNA and ssDNA were inhibited by AraAMP.The targeted drug had parallel an-ti-H BV DN A reDlicative effectiveness com pared with AraAMP.The values of Si of drugs toHBsAg and HBeAg were detected.

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    Experimental Studises Oil Viral Hepatitis Receptor——targeted Drug L——HSA-AraAMP

    • 1. PLA 302 Hospital,Beijing

    Abstract: Lactosaminated Human Serum Albumin(L-HSA)was,used as a carrier and coupled to Ara-binosied adenine monophospate(AraAMP).The distribution of 125I-labelled L-HSA-AraAMPwere higher in liver than in other organs.Radioactivities of the drug could still be measured atthe 7th dav after injection.The efficacy of targeted drug was determined by analyzing dynamic changes of HBsAg andHBeAg in 2.2.15 cell culture medium by RIA and changes in the replicative intracellular HBVDN A content by Southern blot.The results showed that the targeted drug had significantly in-hibitory ratio of HBsAg and HBeAg which was similar to AraAMP(inhibitory ratfo of HBsAg50%,63%;HBeAg 62.6%,67.2%,respectively).Southern blot test showed the replicativeintermedlates rcDNA and ssDNA were inhibited by AraAMP.The targeted drug had parallel an-ti-H BV DN A reDlicative effectiveness com pared with AraAMP.The values of Si of drugs toHBsAg and HBeAg were detected.

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