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National Committee on Marine Sciences (NCMS)

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    Anti-inflammatory activity of monosubstituted xestoquinone analogues from the marine sponge Neopetrosia compacta
    Susana, Shalice R.; Salvador-Reyes, Lilibeth A. (MDPI, 2022-03-22)
    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 1–6 caused a concentration-dependent reduction of nitric oxide (NO) production in LPS-stimulated RAW 264.7 cells, with 4–6 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 (4–6), 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 (4–6) may, in part, be mediated by Nrf2 activation, leading to attenuation of inflammatory mediators such as IL-1β and NOS2.
    Samples were collected under gratuitous permit numbers GP-0084-15 and GP-0123-17, issued by the Department of Agriculture of the Philippines. We thank the municipalities of Bolinao, Pangasinan, and Puerto Galera, Oriental Mindoro for permission for sample collection. We acknowledge assistance from Z. L. Malto and DDHP chemical ecology group in obtaining the mass spectrometric data and sample collection, respectively.
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    Comprehensive metabolomics of Philippine Stichopus cf. horrens reveals diverse classes of valuable small molecules for biomedical applications
    Torreno, Vicenzo Paolo M.; Molino, Ralph John Emerson J.; Junio, Hiyas A.; Yu, Eizadora T. (Public Library of Science (PLoS), 2023-12-06)
    Stichopus cf. horrens is an economically important sea cucumber species in Southeast Asia due to their presumed nutritional and medicinal benefits. However, compared to other sea cucumbers such as Apostichopus japonicus, there are no biochemical studies on which compounds contribute to the purported bioactivities of S. cf. horrens. To address this, a high-throughput characterization of the global metabolite profile of the species was performed through LC-MS/MS experiments and utilizing open-access platforms such as GNPS, XCMS, and metaboAnalyst. Bioinformatics-based molecular networking and chemometrics revealed the abundance of phospholipids such as phosphatidylcholines (PCs), phosphatidylethanolamines (PEs), phosphatidylinositols (PIs), and phosphatidylserines (PSs) in the crude samples. Body wall extracts were observed to have higher levels of structural, diacylated PCs, while the viscera have higher relative abundance of single-tail PCs and PEs that could be involved in digestion via nutrient absorption and transport for sea cucumbers. PEs and sphingolipids could also be implicated in the ecological response and morphological transformations of S. cf. horrens in the presence of predatory and other environmental stress. Interestingly, terpenoid glycosides and saponins with reported anti-cancer benefits were significantly localized in the body wall. The sulfated alkanes and sterols present in S. cf. horrens bear similarity to known kairomones and other signaling molecules. All in all, the results provide a baseline metabolomic profile of S. cf. horrens that may further be used for comparative and exploratory studies and suggest the untapped potential of S. cf. horrens as a source of bioactive molecules.
    The authors would like to thank the Marine Invertebrate Ecology Laboratory under Dr. Marie Antonette Juinio-Meñez for the collection and maintenance of animals, and the Mass Spectrometry Facility at the Institute of Chemistry, UP Diliman for instrument use.
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    Genistein and daidzein from a sponge-associated fungus (Family: Microstromataceae) show dose and incubation time-dependent Ca2+ influx activity variation
    Azcuna, Miguel Enrique Ma.; Acyatan, Zildjian; Manzano, Geminne; Yu, Clairecynth; Aliño, Porfirio Alexander M.; Altamia, Marvin; Salvador-Reyes, Lilibeth; Concepcion, Gisela P. (Philippine Association for the Advancement of Science and Technology, 2023-10-31)
    The compounds genistein and daidzein were obtained from the broth culture of a fungus isolated from the Philippine blue sponge Xestospongia sp. Genomic sequencing (18S rRNA) resulted in no exact hits and low sequence similarity (91%) to two species of fungi under the family Microstromataceae: Sympodiomycopsis vantaiensis and Microstromatales sp. Genistein has gained attention in recent years because of its potential to delay the onset of Alzheimer’s disease. This is the first report of genistein and daidzein isolated from a marine-derived fungus. Genistein and daidzein have a wide range of biological activities (e.g., neuroprotective, antimicrobial, anticancer), and this study reports a variation in intracellular [Ca2+] levels in dorsal root ganglion cells (DRGs) post-administration depending on dose and incubation time. An incubation time of 10 min resulted in a block effect, which was evidenced by decreased intracellular [Ca2+] levels. A dose-response was observed as the intensity of intracellular [Ca2+] decreased further at a higher dose. Conversely, an incubation time of 5 min resulted in an increase effect which was evidenced by decreased intracellular [Ca2+] levels. The similarity of these compounds with potent estrogens indicates that estrogen-mediated receptor signaling is the mechanism of action for the increase effect. The block effect, however, could be caused by a variety of factors, such as neurotoxicity or an ER stress response that results in the release of pro- and anti-apoptotic proteins. These findings confirm the ability of genistein to regulate [Ca2+] influx and the expression of apoptosis-related proteins. Further studies should investigate these mechanisms to understand the neuroprotective activities of genistein and daidzein.
    We thank the Drug Discovery and Health Products (DDHP) – Marine Component Project 1 for providing the sponge sample for fungal isolation. We thank Dr. Eizadora Yu of the Institute of Chemistry, University of the Philippines Diliman for providing fungal primers for DNA extraction and obtaining DNA sequences from the fungal sample.