title: Anti-HIV-1 activity of phlorotannin derivative 8,4‴-dieckol from Korean brown alga Ecklonia cava.
abstract: 8,4‴-dieckol is a natural product which has been isolated from brown alga, Ecklonia cava. This polyphenolic compound is a phlorotannin derivative with a broad range of bioactivities. Its inhibitory activity on human immunodeficiency virus type-1 (HIV-1) was tested and the results indicated that 8,4‴-dieckol inhibited HIV-1 induced syncytia formation, lytic effects, and viral p24 antigen production at noncytotoxic concentrations. Furthermore, it was found that 8,4‴-dieckol selectively inhibited the activity of HIV-1 reverse trancriptase (RT) enzyme with 91% inhibition ratio at the concentration of 50 μM. HIV-1 entry was also inhibited by 8,4‴-dieckol. According to data from this study, 8,4‴-dieckol is an effective compound against HIV-1 with high potential for further studies. These results suggest that it might be used as a drug candidate for the development of new generation therapeutic agents, although further studies on the mechanism of inhibition should be addressed.
authors.affiliation: a Marine Bioprocess Research Center , Pukyong National University , Busan , Republic of Korea.
authors.forename: Fatih
authors.initials: F
authors.lastname: Karadeniz
authors.forename: Kyong-Hwa
authors.initials: KH
authors.lastname: Kang
authors.forename: Jae W
authors.initials: JW
authors.lastname: Park
authors.forename: Sun-Joo
authors.initials: SJ
authors.lastname: Park
authors.forename: Se-Kwon
authors.initials: SK
authors.lastname: Kim
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology*; D001572:Benzofurans / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D015726:Giant Cells / Q000187:drug effects; D016655:HIV Core Protein p24 / Q000096:biosynthesis; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism / Q000502:physiology; D006801:Humans; D000459:Phaeophyceae / Q000737:chemistry*; D013601:T-Lymphocytes / Q000166:cytology / Q000187:drug effects; D013634:Tannins / Q000737:chemistry*; D053586:Virus Internalization / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D001572:Benzofurans; D016655:HIV Core Protein p24; D013634:Tannins; C503840:dieckol; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase
keywords: 8,4‴-dieckol; Ecklonia cava; HIV-1 RT inhibition; phlorotannin; syncytia