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来自韩国褐藻孔石莼的间苯三酚单宁衍生物8,4‴-二 Eckol的抗HIV-1活性。

Anti-HIV-1 activity of phlorotannin derivative 8,4‴-dieckol from Korean brown alga Ecklonia cava.

作者信息

Karadeniz Fatih, Kang Kyong-Hwa, Park Jae W, Park Sun-Joo, Kim Se-Kwon

机构信息

a Marine Bioprocess Research Center , Pukyong National University , Busan , Republic of Korea.

出版信息

Biosci Biotechnol Biochem. 2014;78(7):1151-8. doi: 10.1080/09168451.2014.923282. Epub 2014 Jun 12.

DOI:10.1080/09168451.2014.923282
PMID:25229850
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.

摘要

8,4‴-二eckol是一种从褐藻海蕴中分离出来的天然产物。这种多酚类化合物是一种具有广泛生物活性的间苯三酚鞣质衍生物。对其抗人类免疫缺陷病毒1型(HIV-1)的活性进行了测试,结果表明,8,4‴-二eckol在无细胞毒性浓度下可抑制HIV-1诱导的合胞体形成、裂解作用以及病毒p24抗原的产生。此外,发现8,4‴-二eckol在50μM浓度下可选择性抑制HIV-1逆转录酶(RT)的活性,抑制率为91%。8,4‴-二eckol还可抑制HIV-1的进入。根据该研究的数据,8,4‴-二eckol是一种抗HIV-1的有效化合物,具有很大的进一步研究潜力。这些结果表明,它可能作为新一代治疗药物开发的候选药物,不过还应进一步研究其抑制机制。

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