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Synthesis, structure-activity relationships, and mechanism of action of anti-HIV-1 lamellarin α 20-sulfate analogues.

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Title: Synthesis, structure-activity relationships, and mechanism of action of anti-HIV-1 lamellarin α 20-sulfate analogues.
Authors: Kamiyama, Haruka / Kubo, Yoshinao / Sato, Hironori / Yamamoto, Naoki / Fukuda, Tsutomu / Ishibashi, Fumito / Iwao, Masatomo
Issue Date: 15-Dec-2011
Publisher: Elsevier BV
Citation: Bioorganic & Medicinal Chemistry, 19(24), pp.7541-7550; 2011
Abstract: Lamellarin α and six different types of lamellarin α 20-sulfate analogues were synthesized and their structure-activity relationships were investigated using a single round HIV-1 vector infection assay. All lamellarin sulfates having pentacyclic lamellarin core exhibited anti-HIV-1 activity at a 10μM concentration range regardless of the number and position of the sulfate group. On the other hand, non-sulfated lamellarin α and ring-opened lamellarin sulfate analogues did not affect HIV-1 vector infection in similar concentrations. The lamellarin sulfates utilized in this study did not exhibit unfavorable cytotoxic effect under the concentrations tested (IC(50)>100μM). Confocal laser scanning microscopic analysis indicated that hydrophilic lamellarin sulfates were hardly incorporated in the cell. HIV-1 Env-mediated cell-cell fusion was suppressed by lamellarin sulfates. These results suggested that lamellarin sulfates have a novel anti-HIV-1 activity besides the previously reported integrase activity inhibition, possibly at a viral entry step of HIV-1 replication.
URI: http://hdl.handle.net/10069/26755
ISSN: 09680896
DOI: 10.1016/j.bmc.2011.10.030
PubMed ID: 22071527
Rights: Copyright © 2011 Elsevier Ltd. All rights reserved.
Type: Journal Article
Text Version: author
Appears in Collections:Articles in academic journal

Citable URI : http://hdl.handle.net/10069/26755

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