文章基本信息

标题：Inhibition of HIV-1 Reverse Transcriptase and Protease by Phlorotannins from the Brown Alga Ecklonia cava
本地全文：下载
作者：Mi-Jeong Ahn ; Kee-Dong Yoon ; So-Young Min 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2004
卷号：27
期号：4
页码：544-547
DOI：10.1248/bpb.27.544
出版社：The Pharmaceutical Society of Japan
摘要：The bioassay-directed isolation of a marine brown alga, Ecklonia cava , afforded four phlorotannin derivatives, eckol (1), 8,8′-bieckol (2), 8,4′′′-dieckol (3), and phlorofucofuroeckol A (4). Among these compounds, 2 and 3 exhibited an inhibitory effect on human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) and protease. Specifically, they inhibited the RT more potently than the protease. The inhibitory activity of compound 2 (IC₅₀, 0.51 μ M ) against HIV-1 RT was comparable to that of nevirapine (IC₅₀, 0.28 μ M ), a reference compound. An enzyme kinetic assay showed that this compound inhibited the RNA-dependent DNA synthesis activity of HIV-1 RT noncompetitively against dUTP/dTTP with a K _i value of 0.78 μ M . With respect to the homopolymeric template/primer, (rA)_n(dT)₁₅, 8,8′-bieckol (2) displayed an uncompetitive type of inhibition ( K _i, 0.23 μ M ).
关键词：Ecklonia cava;8,8′-bieckol;8,4′′′-dieckol;HIV-1 reverse transcriptase;noncompetitive inhibition;protease