Inhibition of HIV-1 Reverse Transcriptase and Protease by Phlorotannins from the Brown Alga Ecklonia cava (Pharmacognosy)

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概要

• 論文の詳細を見る

• 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 (IC_<50>, 0.51μM) against HIV-1 RT was comparable to that of nevirapine (IC_<50>, 0.28μM), 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 0.78μM. With respect to the homopolymeric template/primer, (rA)_n(dT)_<15>, 8,8'-bieckol (2) displayed an uncompetitive type of inhibition (K_i, 0.23μM).

• 社団法人日本薬学会の論文
• 2004-04-01

著者

• KIM Tae

  National Institute of Toxicological Research, Korea Food and Drug Administration

• KIM Seung

  National Institute of Toxicological Research, Korea Food and Drug Administration

• KIM Jeong

  Department of Information Electronics Engineering, Ewha Womans University

• Kim J

  Department Of Biological Sciences Institute Of Natural Sciences Sungkyunkwan University

• Kim Nam-gil

  Department Of Mathematics Chosun University

• Kim Nam-gil

  Department Of Aquaculture Gyeongsang National University

• Ahn Mi-jeong

  College Of Pharmacy And Research Institute Of Pharmaceutical Science Seoul National University

• KIM Jinwoong

  College of Pharmacy, Seoul National University

• Kim Tae

  National Institute Of Toxicological Research Korea Food And Drug Administration

• YOON Kee-Dong

  College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University

• MIN So-Young

  College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University

• LEE Ji

  Research Group of Pain and Neuroscience in Vision 2000 Project, East-West Medical Research Institute

• HUH Hoon

  College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University

• Yoon Kee-dong

  College Of Pharmacy And Research Institute Of Pharmaceutical Science Seoul National University

• Kim Jinwoong

  College Of Pharmacy And Research Institute Of Pharmaceutical Science Seoul National University

• Min So-young

  College Of Pharmacy And Research Institute Of Pharmaceutical Science Seoul National University

• Huh Hoon

  College Of Pharmacy And Research Institute Of Pharmaceutical Science Seoul National University

• Kim Jeong

  Department Of Anatomy Wonkwang University School Of Medicine

• Kim Tae

  National Institute Of Advanced Industrial Science And Technology (aist):crest-japan Science And Tech

• Kim S

  National Institute Of Toxicological Research Korea Food And Drug Administration

• Kim Seung

  National Insitute Of Toxicological Research Korea Food And Drug Administration

• Lee Joong-ku

  韓国

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