Abstract
Seven previously unreported daphnane-type diterpene esters named acutilobins A-G, together with 12 known ones, were isolated from EtOAc extract of Daphne acutiloba Rehd. Their structures were elucidated based on the spectroscopic data. The cytotoxic and anti-HIV-1 activities of these daphnane-type diterpene esters were evaluated through bioassays. Fourteen of these isolates exhibited definite cytotoxic activities against the five human tumor cell lines HL-60, SMMC-7721, A-549, MCF-7, and SW480. Additionally, anti-HIV-1 activities were observed in 13 daphnane-type diterpene esters, among which acutilobins A-G exhibited significant anti-HIV-1 activities with EC₅₀ below 1.5 nM and SI over 10,000. Particularly, genkwanineVIII showed the strongest activity with EC₅₀ 0.17 nM and SI 187,010.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / isolation & purification
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Anti-HIV Agents / pharmacology*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / isolation & purification
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Daphne / chemistry*
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Diterpenes / chemistry
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Diterpenes / isolation & purification
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Diterpenes / pharmacology*
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Esters / chemistry
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Esters / isolation & purification
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Esters / pharmacology*
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HIV-1 / drug effects*
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HL-60 Cells
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Humans
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Molecular Conformation
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Plant Extracts / chemistry
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Plant Extracts / isolation & purification
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Plant Extracts / pharmacology*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Anti-HIV Agents
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Antineoplastic Agents
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Diterpenes
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Esters
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Plant Extracts
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mezerein