Abstract
Eight new acyclic manoalide-related sesterterpenes, hippolides A-H (1-8), together with two known manoalide derivatives, (6E)-neomanoalide (9) and (6Z)-neomanoalide (10), were isolated from the South China Sea sponge Hippospongia lachne. The absolute configurations of 1-8 were established by the modified Mosher's method and CD data. Compound 1 exhibited cytotoxicity against A549, HeLa, and HCT-116 cell lines with IC50 values of 5.22×10(-2), 4.80×10(-2), and 9.78 μM, respectively. Compound 1 also showed moderate PTP1B inhibitory activitiy with an IC50 value of 23.81 μM, and compound 2 showed moderate cytotoxicity against the HCT-116 cell line and PTP1B inhibitory activity with IC50 values of 35.13 and 39.67 μM, respectively. In addition, compounds 1 and 5 showed weak anti-inflammatory activity, with IC50 values of 61.97 and 40.35 μM for PKCγ and PKCα, respectively.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / isolation & purification*
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Anti-Inflammatory Agents, Non-Steroidal / 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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China
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Drug Screening Assays, Antitumor
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HCT116 Cells
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HeLa Cells
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Porifera / chemistry*
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Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors*
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Sesterterpenes / chemistry
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Sesterterpenes / isolation & purification*
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Sesterterpenes / pharmacology
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Terpenes / chemistry
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Terpenes / isolation & purification*
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Terpenes / pharmacology
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Antineoplastic Agents
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Sesterterpenes
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Terpenes
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manoalide
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PTPN1 protein, human
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Protein Tyrosine Phosphatase, Non-Receptor Type 1