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AHN, Mi-Jeong,YOON, Kee-Dong,MIN, So-Young,LEE, Ji Suk,KIM, Jeong Ha,KIM, Tae Gyun,KIM, Seung Hee,KIM, Nam-Gil,HUH, Hoon,KIM, Jinwoong WHO COLLABORATING CENTRE FOR TRADITIONAL MEDICINE 2004 東西醫學硏究所 論文集 Vol.2004 No.-
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 an 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 (IC_(50), 0.51 μм) against HIV-1 RT was comparable to that of nevirapine (IC_(50), 0.28 μм), 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 μM. 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 μм).