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Article

Anti-Inflammatory Activity of Monosubstituted Xestoquinone Analogues from the Marine Sponge Neopetrosia compacta

Marine Science Institute, University of the Philippines—Diliman, Velasquez St., UP Diliman, Quezon City 1101, Philippines
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Author to whom correspondence should be addressed.
Academic Editors: Jose M. Prieto and Stanley Omaye
Antioxidants 2022, 11(4), 607; https://doi.org/10.3390/antiox11040607
Received: 25 January 2022 / Revised: 4 March 2022 / Accepted: 16 March 2022 / Published: 22 March 2022
Chronic inflammation is recognized as a contributor to multiple chronic diseases, such as cancer, cardiovascular, and autoimmune disorders. Here, a natural products-initiated discovery of anti-inflammatory agents from marine sponges was undertaken. From the screening of 231 crude extracts, a total of 30 extracts showed anti-inflammatory activity with no direct cytotoxic effects at 50 μg/mL on RAW 264.7 (ATCC®TIB-71™) murine macrophage cells stimulated with 1 μg/mL lipopolysaccharide (LPS). Bioactivity-guided purification of the anti-inflammatory extract from the sponge Neopetrosia compacta led to the isolation of xestoquinone (1), adociaquinone B (2), adociaquinone A (3), 14-hydroxymethylxestoquinone (4), 15-hydroxymethylxestoquinone (5), and an inseparable 2:1 mixture of 14-methoxyxestoquinone and 15-methoxyxestoquinone (6). Compounds 16 caused a concentration-dependent reduction of nitric oxide (NO) production in LPS-stimulated RAW 264.7 cells, with 46 having low micromolar IC50 and acceptable selectivity index. Gene expression analysis using qRT-PCR showed that 1, 5, and 6 downregulated Il1b and Nos2 expression by 2.1- to 14.8-fold relative to the solvent control at 10 μM. Xestoquinone (1) and monosubstituted analogues (46), but not the disubstituted adociaquinones (2 and 3), caused Nrf2 activation in a luciferase reporter MCF7 stable cells. Compounds 5 and 6 caused a modest increase in Nqo1 gene expression at 10 μM. The anti-inflammatory activity of xestoquinone (1) and monosubstituted analogues (46) may, in part, be mediated by Nrf2 activation, leading to attenuation of inflammatory mediators such as IL-1β and NOS2. View Full-Text
Keywords: marine sponge; xestoquinone; anti-inflammatory; Nrf2 activation; natural products marine sponge; xestoquinone; anti-inflammatory; Nrf2 activation; natural products
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MDPI and ACS Style

Susana, S.R.; Salvador-Reyes, L.A. Anti-Inflammatory Activity of Monosubstituted Xestoquinone Analogues from the Marine Sponge Neopetrosia compacta. Antioxidants 2022, 11, 607. https://doi.org/10.3390/antiox11040607

AMA Style

Susana SR, Salvador-Reyes LA. Anti-Inflammatory Activity of Monosubstituted Xestoquinone Analogues from the Marine Sponge Neopetrosia compacta. Antioxidants. 2022; 11(4):607. https://doi.org/10.3390/antiox11040607

Chicago/Turabian Style

Susana, Shalice R., and Lilibeth A. Salvador-Reyes. 2022. "Anti-Inflammatory Activity of Monosubstituted Xestoquinone Analogues from the Marine Sponge Neopetrosia compacta" Antioxidants 11, no. 4: 607. https://doi.org/10.3390/antiox11040607

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