Unravelling the Anti-Inflammatory and Antioxidant Potential of the Marine Sponge Cliona celata from the Portuguese Coastline

Inflammation is a double-edged sword, as it can have both protective effects and harmful consequences, which, combined with oxidative stress (OS), can lead to the development of deathly chronic inflammatory conditions. Over the years, research has evidenced the potential of marine sponges as a source of effective anti-inflammatory therapeutic agents. Within this framework, the purpose of this study was to evaluate the antioxidant and the anti-inflammatory potential of the marine sponge Cliona celata. For this purpose, their organic extracts (C1–C5) and fractions were evaluated concerning their radical scavenging activity through 2,2-diphenyl-1-picrylhydrazyl radical (DPPH), ferric reducing antioxidant power (FRAP), oxygen radical absorbance capacity (ORAC), and anti-inflammatory activity through a (lipopolysaccharides (LPS)-induced inflammation on RAW 264.7 cells) model. Compounds present in the two most active fractions (F5 and F13) of C4 were tentatively identified by gas chromatography coupled to mass spectrometry (GC-MS). Even though samples displayed low antioxidant activity, they presented a high anti-inflammatory capacity in the studied cellular inflammatory model when compared to the anti-inflammatory standard, dexamethasone. GC-MS analysis led to the identification of n-hexadecanoic acid, cis-9-hexadecenal, and 13-octadecenal in fraction F5, while two major compounds, octadecanoic acid and cholesterol, were identified in fraction F13. The developed studies demonstrated the high anti-inflammatory activity of the marine sponge C. celata extracts and fractions, highlighting its potential for further therapeutic applications.

Molecular Networking-Guided Isolation of New Etzionin-Type Diketopiperazine Hydroxamates from the Persian Gulf Sponge Cliona celata

The Persian Gulf is a unique and biologically diverse marine environment dominated by invertebrates. In continuation of our research interest in the chemistry and biological activity of marine sponges from the Persian Gulf, we selected the excavating sponge Cliona celata for detailed metabolome analyses, in vitro bioactivity screening, and chemical isolation studies. A UPLC-MS/MS (MS2) molecular-networking-based dereplication strategy allowed annotation and structural prediction of various diketopiperazines (DKPs) and etzionin-type diketopiperazine hydroxamates (DKPHs) in the crude sponge extract. The molecular-networking-guided isolation approach applied to the crude extract afforded the DKPH etzionin (1) and its two new derivatives, clioetzionin A (2) and clioetzionin B (3). Another new modified DKP (4) was identified by MS/MS analyses but could not be isolated in sufficient quantities to confirm its structure. The chemical characterization of the purified DKPHs 1–3 was performed by a combination of 1D and 2D NMR spectroscopy, HRMS, HRMS/MS, and [α]D analyses. Compounds 1 and 2 exhibited broad antibacterial, antifungal, and anticancer activities, with IC50 values ranging from 19.6 to 159.1 µM. This is the first study investigating the chemical constituents of a C. celata specimen from the Persian Gulf. It is also the first report of full spectroscopic data of etzionin based on extensive spectroscopic analyses.

Larvicidal, Ovicidal, and Repellent Activities of Marine Sponge Cliona celata (Grant) Extracts against Culex quinquefasciatus Say and Aedes aegypti L. (Diptera: Culicidae)

Solvent extracts of marine sponge Cliona celata (Grant) were screened for larvicidal, ovicidal, and repellent properties against the filarial vector Culex quinquefasciatus Say and dengue vector Aedes aegypti L. Larvicidal and ovicidal activities of hexane, ethyl acetate, and methanol extracts were tested in four different concentrations ranging as 62.5, 125, 250, and 500 ppm. Among the three solvent extracts of C. celata, methanol extract showed the highest larvicidal activity at 500 ppm against both mosquito species. The LC50 and LC90 values of C. celata methanol extract were recorded as 95.63 and 242.16 ppm against C. quinquefasciatus larvae and 158.40 and 780.16 ppm against A. aegypti larvae, respectively. Ovicidal activity was high in methanol extract, in which 100% ovicidal activity was recorded in C. quinquefasciatus, and 72% ovicidal activity was recorded in A. aegypti at 500 ppm. The hexane extract was found to be the most effective protectant against the adult mosquitoes of both species. The mean protection time recorded in hexane extract was up to 273 and 165 min at 5 mg/cm2 dosage against C. quinquefasciatus and A. aegypti, respectively. Considering these bioactivities, C. celata could be used to obtain some novel pesticidal molecules.