COX Inhibitory and Cytotoxic Naphthoketal-Bearing Polyketides from Sparticola junci |
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Authors: | Katherine Yasmin M. Garcia,Mark Tristan J. Quimque,Gian Primahana,Andreas Ratzenbö ck,Mark Joseph B. Cano,Jeremiah Francis A. Llaguno,Hans-Martin Dahse,Chayanard Phukhamsakda,Frank Surup,Marc Stadler,Allan Patrick G. Macabeo |
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Abstract: | Axenic fermentation on solid rice of the saprobic fungus Sparticola junci afforded two new highly oxidized naphthalenoid polyketide derivatives, sparticatechol A (1) and sparticolin H (2) along with sparticolin A (3). The structures of 1 and 2 were elucidated on the basis of their NMR and HR-ESIMS spectroscopic data. Assignment of absolute configurations was performed using electronic circular dichroism (ECD) experiments and Time-Dependent Density Functional Theory (TDDFT) calculations. Compounds 1–3 were evaluated for COX inhibitory, antiproliferative, cytotoxic and antimicrobial activities. Compounds 1 and 2 exhibited strong inhibitory activities against COX-1 and COX-2. Molecular docking analysis of 1 conferred favorable binding against COX-2. Sparticolin H (2) and A (3) showed a moderate antiproliferative effect against myelogenous leukemia K-562 cells and weak cytotoxicity against HeLa and mouse fibroblast cells. |
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Keywords: | Sparticola junci structure elucidation ECD-TDDFT COX inhibitory molecular docking antiproliferative cytotoxic |
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