摘要
人工合成两种半乳糖多聚赖氨酸导向配体，与荧光素标记的互补于ＨＢＶｍＲＮＡ多聚腺苷酸信号部分的２１－聚反义硫代脱氧核苷酸（ＡＳＯＤＮ）电性结合，与２．２．１５细胞共同孵育，４０ｍｉｎ后配体组对ＨＢｓＡｇ和ＨＢｅＡｇ的抑制率为４１％～４７％和２８％～３１％，单纯ＡＳＯＤＮ组为１１％和５％；３ｄ后配体组为８８％～８９％和７１％～７４％，单纯组为６４％和５３％。经流式细胞分析，配体组使２．２．１５细胞荧光染色率达７５．３％和８３．８％；单纯组为２４．３％。结果表明，两种人工配体均具有良好的导向ＡＳＯＤＮ入肝细胞的功能，且可以明显提高ＡＳＯＤＮ抗ＨＢＶ的活性。
Two kinds of galactose terminal glyco poly L lysine were synthesized, which could bind ASODN and were fluorecein labelled and complementary to polyadenylation signal of HBV mRNA. After incubated with 2.2.15 cells for 40 minutes, the inhibitory rate on HBsAg and HBeAg production was 41%～47%, 28%～31% in modified group, and was 11% and 5% in non modified group. After incubated for 3 days, it was 88%～89% and 71%～74% in modified group, and was 64% and 53% in non modified group. The rate of cell fluorecent staining detected by flow cytometric analysis was 75.3% and 83.8% in modified groups while it was only 24.3% in non modified group. These data indicate that the synthesized ligands can delivery ASODN to liver cells, and are effective in improving the anti HBV activity of ASODN in vitro.
出处
《解放军医学杂志》
CSCD
北大核心
1996年第3期196-198,共3页
Medical Journal of Chinese People's Liberation Army
基金
总后卫生部"八五"招标课题资助
国家自然科学基金
关键词
乙型肝炎
药物疗法
反义寡核苷酸
半乳糖
hepatitis B virus
antisense oligodeoxynucleotides
asialoglycoprotein receptor
therapy
