Marine Sponge Extracts Research Articles

Unravelling the protective effects of peptide isolated from marine sponge extract MS01 against SH-SY5Y cell line and its in-silico pharmacokinetic analysis

Parkinson's disease (PD) is characterised by developing postural instability, resting seizures, tremors, and a movement problem coupled with stiffness. All the available drugs can improve motor function considerably, but they can also have negative side effects, especially if the problem gets worse. The structure-activity relation was performed in the DISCOVERY STUDIO V2.5.5 pharmacophore model using the HypoGen algorithm for a training set of 15 compounds. Here, xenin peptide fits well with a least cost difference and a fit value of 10.46, indicating a favourable pharmacological characteristic. Therefore, we tried applying gene network analysis in cytoHubba to find the hub gene for PD in Danio rerio and Homo sapiens, as zebrafish and humans share many disease proteins and processes. Molecular docking studies for the hub gene polyubiquitin B from Danio rerio and Parkin from Homo sapiens, as well as the peptide xenin obtained from the marine sponge extract MS01 was performed. The peptide exhibits a substantial binding affinity with the receptor UBB through 8 and PRKN through 4 intermolecular hydrogen bonds in their bonded and non-bonded interactions, although it has little effect on the protein structure, according to simulation studies and dynamical free energy calculations. The protein structure has also been stabilised in terms of energy, secondary structure, and flexibility by the peptide binding. In addition to in-silico analysis the extract was tested in-vitro on SH-SY5Y cells for its effectiveness against ROS and cell viability, which proved its qualitative effect.

Chemical Component Analysis of Marine Sponge Extract of Potentially Medicinal Based on Solvent Differences

Tracing and characterizing marine natural materials with special medicinal abilities is important to obtain new materials to enrich the diversity of drugs to treat particular diseases. The identification of the chemical components of sponges is interesting, considering the uniqueness and several other abilities possessed by sponges that are thought to have medicinal potential. Searching for chemical components in sponge extracts is suspected to contain secondary metabolic substances with medicinal potential. The study aimed to identify the chemical components of sponge extract with potential medicinal value based on differences in solvents. The first extract on the sponge Clathria (Thalysias) reinwardti Sp.1 (CTR) by maceration method using semi-polar solvents (methanol). The second extraction uses a separating funnel with two types of non-polar solvents (diethyl-ether and n-hexane). The chemical components of the three extracts were analyzed using a gas chromatography-mass spectrophotometer instrument. The identified chemical components of sponge extract generally belong to the class of free fatty acids and cholesterol. Investigation of identified compounds with medicinal value chemical components, for example, Cholestan-3.alpha.-ol, Ergosta-5, Hexadecanoic acid, 1-(2,6-Dichlorophenyl)-2-indolinone and Pyridine-3-carboxamide. Searching for chemical components with medicinal potential from sponge extracts is novelty research based on differences in solvents, a new method. Complementing the data from this research, it is necessary to carry out further and specific searches related to chemical components with medicinal properties, which can be carried out by chromatographic fractionation and testing the activity of the extract against bacteria. pathogens and parasitic fungi.

In vitro antioxidant, antidiabetic, and in silico docking studies on diabetic wound healing potential of identified compounds of methanolic extract of marine sponge, Agelas clathrodes (Schmidt, 1870) by GC-MS and LC-MS analysis

In vitro antioxidant, antidiabetic, and in silico docking studies on diabetic wound healing potential of identified compounds of methanolic extract of marine sponge, Agelas clathrodes (Schmidt, 1870) by GC-MS and LC-MS analysis

Anti-inflammatory and antioxidant properties of Agelas sp., Ircinia sp., and Aaptos suberitoides

Reactive oxygen species (ROS) and cyclooxygenase-2 (COX-2) can be therapeutic targets for inflammatory diseases. COX-2 expression which can be triggered by ROS might consequently promote inflammation. Inhibition of ROS by the antioxidant, however, may prevent or decrease the expression of COX-2. In this study, the antioxidant and anti-inflammatory properties of the hexane (H), dichloromethane (DCM), and methanol-water (MW) extracts of marine sponges Agelas sp. (Asp), Ircinia sp. (Isp), and Aaptos suberitoides (As) were determined. The correlation between their antioxidant properties and ability to inhibit COX enzymes was also established. The MW extracts of the marine sponges and the AsDCM contain a significant (p<0>50% of the COX-2 and gave a selectivity index (COX-2/COX-1) >1.0. This suggests that the extracts can be sources of compounds with promising and selective inhibitory properties against COX-2. Correlation analysis further showed a positive linear correlation between the extracts’ inhibitory activity against the COX enzymes and their TPC, reducing power, and DPPH radical scavenging activity. Thus, the antioxidant activity of the extracts may have influenced their anti-inflammatory property via COX inhibition.

Marine Natural Compound (Neviotin A) Displays Anticancer Efficacy by Triggering Transcriptomic Alterations and Cell Death in MCF-7 Cells.

We investigated the anticancer mechanism of a chloroform extract of marine sponge (Haliclona fascigera) (sample C) in human breast adenocarcinoma (MCF-7) cells. Viability analysis using MTT and neutral red uptake (NRU) assays showed that sample C exposure decreased the proliferation of cells. Flow cytometric data exhibited reactive oxygen species (ROS), nitric oxide (NO), dysfunction of mitochondrial potential, and apoptosis in sample C-treated MCF-7 cells. A qPCR array of sample C-treated MCF-7 cells showed crosstalk between different pathways of apoptosis, especially BIRC5, BCL2L2, and TNFRSF1A genes. Immunofluorescence analysis affirmed the localization of p53, bax, bcl2, MAPKPK2, PARP-1, and caspase-3 proteins in exposed cells. Bioassay-guided fractionation of sample C revealed Neviotin A as the most active compound triggering maximum cell death in MCF-7, indicating its pharmacological potency for the development of a drug for the treatment of human breast cancer.

Antiproliferative and pro-apoptotic effects on cancer cell line HCT116 using marine sponge Tedania species collected from Kalangahan, Lugait, Misamis Oriental, Philippines

Cancer is a major cause of mortality worldwide, and marine sponges have emerged as potential sources of anticancer agents. In this study, we investigated the antiproliferative and pro-apoptotic effects of a marine sponge extract from Tedania sp. against the human colorectal carcinoma cell line (HCT116) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and Caspase-Glo® 3/7 assays. The extract was prepared using a polar solvent mixture of ethanol:water, and was subjected to reversed-phase flash chromatography consisiting of water(W), acetonitrile(ACN), and ethyl acetate(EA) gradient eluent, yielding 16 Fraction. Treatment of HCT116 cells with Fractions 1-16 showed that only Fraction 16, consisting of 100�, exhibited significant (p<0.05) cytotoxic activity with the lowest viability of 90.9% compared to the negative control. Furthermore, Fraction 9, consisting of 20:80 W and ACN, showed a significantly (p<0.05) highest fold change (FC) value of 2.89 indicating an almost threefold increase in caspase-3/7 activity. These results demonstrate that the Tedania sp. extract has promising antiproliferative and pro-apoptotic effects against HCT116 cell lines, indicating its potential as an anticancer agent.

WITHDRAWN: Revealing the neuroprotection and neurodegeneration efficacy of marine sponge extract in Parkinson's disease using gene expression and molecular docking

Parkinson's disease is one of the most prevalent neurological conditions (PD). The pathogenesis of PD was thought to involve mitochondrial dysfunction and oxidative stress. In this study, PD was induced in zebrafish models, and the effectiveness of MS01 sponge extract in neuroprotective effects was assessed. In zebrafish models, rotenone and MS01-mixed pellets were fed, tested for sensitivity and motor function, and euthanized. Histopathology and confocal images of the zebrafish brain were then analyzed for the expression of the PINK1 and Parkin genes. Gene expression study showed MS01 was effective against neurodegeneration at a dose-dependent concentration. The compound xenin identified by LC-MS/MS analysis was selected for in silico studies. Using molecular docking and modeling techniques, the gene expression of PINK1 and Parkin were also investigated. The analysis showed binding of the xenin peptide to the PINK1-Ubiquitin complex may enhance the stability of the complex and increase the production of Parkin, which reduces Parkinson's disease symptoms (PD). This demonstrates the neuroprotective effects of the xenin peptide.

Use of the Allium cepa Model to Assess the Cytogenotoxicity of Luffariella herdmani Marine Sponge Extract.

Marine sponge extracts are known to contain potentially toxic compounds that have biological activities of possible pharmacological interest. Thus, it is vital that biological models are used for the preliminary toxicity screening of such extracts. The present study reports the use of Allium cepa, a low-cost plant-based in vivo model, to assess the cytotoxicity and genotoxicity of Luffariella herdmani marine sponge crude extract (SCE). Pre-germinated onion bulbs, exposed for 96hours to different concentrations of SCE (ranging from 0.3125 to 20μg/ml), were used to determine general cytotoxicity. Root length as well as morphological abnormalities were recorded. Genotoxicity was assessed by exposing the root tips to SCE (0.3125-20μg/ml) and the appropriate controls for 48hours, and then staining with acetocarmine. The Mitotic Index (MI), Mitotic Phase Indices (MPIs) and chromosomal aberrations were evaluated and recorded. SCE inhibited A. cepa root growth (EC50 = 10.34μg/ml) and elicited a mitodepressive effect (LC50 = 1.95μg/ml) in a dose-dependent and significant manner. In addition, macroscopic alterations as well as chromosomal aberrations were detected. Overall, our findings indicate that L. herdmani crude extract exhibits cytotoxic and genotoxic activity, suggesting that it might contain substances with anti-proliferative/anticancer potential that could be subject to further characterisation.

A New Tetracyclic Bromopyrrole-Imidazole Derivative through Direct Chemical Diversification of Substances Present in Natural Product Extract from Marine Sponge Petrosia (Strongylophora) sp.

Chemical diversification of substances present in natural product extracts can lead to a number of natural product-like compounds with a better chance of desirable bioactivities. The aim of this work was to discover unprecedented chemical conversion and produce new compounds through a one-step reaction of substances present in the extracts of marine sponges. In this report, a new unnatural tetracyclic bromopyrrole-imidazole derivative, rac-6-OEt-cylindradine A (1), was created from a chemically diversified extract of the sponge Petrosia (Strongylophora) sp. We also confirmed that 1 originated from naturally occurring (-)-cylindradine A (2) via a new reaction pattern. Moreover, (-)-dibromophakellin (3) and 4,5-dibromopyrrole-2-carboxylic acid (4), as well as 2, were reported herein for the first time in this genus. Studies on the possible reaction mechanism and bioactivities were also conducted. The results indicate that the direct chemical diversification of substances present in natural product extracts can be a speedy and useful strategy for the discovery of new compounds.

Antimicrobial and cytotoxic effects of marine sponge extracts Agelas clathrodes, Desmapsamma anchorata and Verongula rigida from a Caribbean Island.

Although marine sponges are known for their antimicrobial, antifungal and cytotoxic activity, very few studies have been carried out on endemic species of Martinique. Martinique is part of the Agoa Sanctuary, a marine protected area that includes the exclusive economic zones (EEZ) of the French Caribbean islands, making it an abundant source of marine species. To highlight the potential of this area for the discovery of marine biomolecules with antipathogenic and antitumor activities, we tested the aqueous and ethanolic extracts of sponge species Agelas clathrodes, Desmapsamma anchorata and Verongula rigida. Five bacterial strains: Bacillus cereus (CIP 78.3), Escherichia coli (CIP 54.127), Pseudomonas aeruginosa (CIP A22), Staphylococcus aureus (CIP 67.8) and Staphylococcus saprophyticus (CIP 76125) were evaluated, as well as four tumor cell lines: breast cancer (MDA-MB231), glioblastoma (RES259) and leukemia (MOLM14 and HL-60). Antimicrobial activity was evaluated using the disc diffusion technique by determining the minimum inhibitory and minimum bactericidal concentrations. Tumor cytotoxic activity was determined in vitro by defining the minimum concentration of extracts that would inhibit cell growth. Ethanolic extracts of Agelas clathrodes were bactericidal for Staphylococcus aureus and Staphylococcus saprophyticus strains, as well as strongly cytotoxic (IC50 < 20 µg/mL) on all cancer cell lines. Verongula rigida also showed strong cytotoxic activity on cell lines but no antimicrobial activity. These results are innovative for this species on these bacterial lines, highlighting the potential of sponge extracts from this area as bioactive compounds sources.

Therapeutically Active Marine Sponge Isolated from Rameshwaram Thoppu Kaadu Theevu against MDR Pathogen Lactobacillus acidophilus Isolated from Childhood Caries

Dental illness is a foremost health problem upsetting childhood, and this action severely causes sickness which is caused by emerging pathogen Lactobacillusacidophilus. So plaque samples were collected from diverse dental clinics around Tirupur Dt. In this study, 20 MDR isolates were isolated and identified by biochemical analysis. Additionally, the decay pathogen Lactobacillus acidophilus was assayed against Levofloxacin, Moxifloxacin, Clindamycin, Vancomycin, Ampicillin, Chloramphenicol, Tetracycline and Novobiocin. Among these strains 0%, 0%, 26%, 34%, 22%, 2%, 16%, 16% and 6% were found to exhibit resistance to four groups of antibiotics. Currently, the extension of resistance to contemporary antimicrobials has demand to search for innovative anti-therapeutic agent. Moreover, several studies mostly deal with marine sponge to explore the therapeutic drug and this potential role in the manufacture of metabolites is becoming a driving area for exploring a rich source of novel compounds that are of prospective interest to mankind for diagnosis of tooth decay. Different concentration of sponge 50μg, 100μg, and 150μg were prepared with DMSO, and well diffusion assay was used. The result indicated that the maximum and minimum inhibition of 22 mm and 16 mm was observed against the isolate LAVG07 and LAVG08. This research proved that the marine sponge extract shows the prominent antimicrobial activity against decay causing organism and it may be broadcast to be a successful approach to come to blow promising multi challenging clinical drugs in the future.

New Metabolites from the Marine Sponge Scopalina hapalia Collected in Mayotte Lagoon.

The biological screening of 44 marine sponge extracts for the research of bioactive molecules, with potential application in the treatment of age-related diseases (cancer and Alzheimer’s disease) and skin aging, resulted in the selection of Scopalina hapalia extract for chemical study. As no reports of secondary metabolites of S. hapalia were found in the literature, we undertook this research to further extend current knowledge of Scopalina chemistry. The investigation of this species led to the discovery of four new compounds: two butenolides sinularone J (1) and sinularone K (2), one phospholipid 1-O-octadecyl-2-pentanoyl-sn-glycero-3-phosphocholine (3) and one lysophospholipid 1-O-(3-methoxy-tetradecanoyl)-sn-glycero-3-phosphocholine (4) alongside with known lysophospholipids (5 and 6), alkylglycerols (7–10), epidioxysterols (11 and 12) and diketopiperazines (13 and 14). The structure elucidation of the new metabolites (1–4) was determined by detailed spectroscopic analysis, including 1D and 2D NMR as well as mass spectrometry. Molecular networking was also explored to complement classical investigation and unravel the chemical classes within this species. GNPS analysis provided further information on potential metabolites with additional bioactive natural compounds predicted.

Metataxanomic, bioactivity and microbiome analysis of Red Sea marine sponges from Egypt.

Red Sea marine sponges (phylum Porifera) and associated microorganisms harbor a wide range of microorganisms, which are considered an essential source of bioactive products. In this study, we screened both the crude extracts of Red Sea marine sponges and their associated bacterial extract for antimicrobial activity and antiviral activity. Molecular characterization of bioactive producers was performed using16S rRNA sequencing, in addition to metagenomic analysis of three representative sponges utilizing the 16S rRNA gene V3-V4 region sequencing in two different seasons. Twelve samples were collected from five different sponge species by scuba diving, and all the crude extracts of sponges showed antimicrobial activity except Negombata corticata. Moreover, 84 out of 110 bacterial isolates extracts demonstrated antimicrobial activity against at least one tested microorganism. These results revealed the bioactivity and biodiversity of the Red Sea marine invertebrates-associated bacteria. It was found that the bioactive isolates belong to several bacterial groups. The bacterial communities of Negombata magnifica, Negombata corticata, and Siphonochalina siphonella were shown with great diversity and differences in the bacterial percentage, diversity, and unique community composition at different seasons in each sponge species. Unique microenvironment for each sponge species may be linked to the production of specific bioactive product.

CYTOTOXIC ACTIVITY OF ETHANOL EXTRACT Petrosia sp. IN VITRO AGAINST CANCER CELLS HeLa

Cervical cancer is one of the highest causes of death in Indonesian women caused by mutations of normal cervical cells turning into abnormal cells. Treatment of cervical cancer causes significant side effects with a relatively long treatment period, so many researchers are exploring various natural ingredients from marine ecosystems as candidates for anticancer drugs. One of them is the sea sponge Petrosia sp. containing various secondary metabolites, one of which is an alkaloid that has a cytotoxic effect on cancer cell lines. This study aims to determine the cytotoxic activity of the ethanol extract of Petrosia sp. in HeLa cervical cancer cells. The ethanol extract of Petrosia sp. obtained by maceration using 96% ethanol and obtained extract as much as 55.9 g and yield value of 2.94%. Cytotoxic activity test was carried out in vitro using the Presto Blue method with varying concentrations of ethanol extract 7.81 ppm; 15.62 ppm; 31.25 ppm; 62.5 ppm; 125 ppm; 250 ppm; 500 ppm; and 1000 ppm. The cytotoxic parameter used was IC50 which was determined using the GraphPad Prism software version 5. The IC50 value of the marine sponge extract Petrosia sp. of 97.20 ppm or 97.20 g/ml with an active category as cervical anticancer.&#x0D; Cervical cancer is one of the highest causes of death in Indonesian women caused by mutations of normal cervical cells turning into abnormal cells. Treatment of cervical cancer causes significant side effects with a relatively long treatment period, so many researchers are exploring various natural ingredients from marine ecosystems as candidates for anticancer drugs. One of them is the sea sponge Petrosia sp. containing various secondary metabolites, one of which is an alkaloid that has a cytotoxic effect on cancer cell lines. This study aims to determine the cytotoxic activity of the ethanol extract of Petrosia sp. in HeLa cervical cancer cells. The ethanol extract of Petrosia sp. obtained by maceration using 96% ethanol and obtained extract as much as 55.9 g and yield value of 2.94%. Cytotoxic activity test was carried out in vitro using the Presto Blue method with varying concentrations of ethanol extract 7.81 ppm; 15.62 ppm; 31.25 ppm; 62.5 ppm; 125 ppm; 250 ppm; 500 ppm; and 1000 ppm. The cytotoxic parameter used was IC50 which was determined using the GraphPad Prism software version 5. The IC50 value of the marine sponge extract Petrosia sp. of 97.20 ppm or 97.20 g/ml with an active category as cervical anticancer.

Zoo-chemical profiling, in vivo toxicity, and in vitro anti-inflammatory properties of Luffariella herdmani marine sponge extract

Zoo-chemical profiling, in vivo toxicity, and in vitro anti-inflammatory properties of Luffariella herdmani marine sponge extract

Sycosterol A, an α-Synuclein Inhibitory Sterol from the Australian Ascidian Sycozoa cerebriformis.

During a recent biodiscovery study to identify new α-synuclein (α-syn) aggregation inhibitors, we screened 29 Australian marine sponge and ascidian extracts in an MS binding assay. This resulted in an extract from the ascidian Sycozoa cerebriformis showing activity toward α-syn. The bioassay and MS guided isolation process led to the identification of one new polyoxygenated sterol sulfate, sycosterol A (1). The structure of this low-yielding steroid was elucidated from HRMS and NMR analysis. Sycosterol A displayed moderate antiaggregation activity with 46.2% (±1.8) inhibition when screened against α-syn at a 5:1 (sycosterol A:α-syn) molar ratio. The α-syn antiaggregation activity displayed by 1 and the recent discovery of similar sterols with α-syn antiaggregation activity and potent antiprion activity suggest this unique class may be useful antineurodegenerative compounds.

Pyrrolactams from Marine Sponge Stylissa massa Collected from Myanmar and Their Anti-Vpr Activities.

A new brominated pyrrolactam stylissaol A (1) together with four known analogues, 2-bromoaldisine, aldisine, spongiacidin D, and Z-hymenialdisine, were isolated from the EtOAc extract of marine sponge Stylissa massa collected in Myanmar. The absolute configuration at C-10 of 1 was determined as R by the electronic circular dichroism (ECD) data. Among the isolated compounds, 2-bromoaldisine showed anti-Viral Protein R (Vpr) activity against TREx-HeLa-Vpr cells with an effective dose of 10 µM and its potency was comparable to that of positive control damnacanthal.

ANTIOXIDANT ACTIVITY OF METHANOL EXTRACT NATUNA MARINE SPONGE (PORIFERA) WITH DPPH METHODE

Objective: Natuna sponge is a marine animal that contains a wide range of secondary metabolites that can be utilized in the field of pharmacy. The research aims to test the phytochemical content and antioxidant activity of the Natuna methanol marine sponge extract. Sample extraction is done by the maceration method with methanol solvent.&#x0D; Methods: Phytochemical tests include alkaloid testing, flavonoids, steroids, saponins, and tannins. Test antioxidant activity using the immersion DPPH method (1.1-diphenyl-2-picryl hydroxyl) measured absorption at a wavelength of 517 nm.&#x0D; Results: The phytochemical test results showing the sponge of Natuna contain secondary metabolites including alkaloids, flavonoids, steroids, saponins, and tannins.&#x0D; Conclusion: This Natuna sponge methanol extract has an antioxidant activity that is very strong with an IC50 value of 52.91 ppm, and the comparator used is Vitamin C with an IC50 value of 43,51 ppm.

Neuroprotective and anti-inflammatory activity of marine sponge extract and HPLC profiling of its components

해면동물은 강력한 세포독성을 나타내는 함유성분으로 의약후 보물질 탐색의 중요한 소재로 이용되고 있으나 최근 해양생태계 보전에 관심이 높아짐에 따라 해면동물 확보는 더욱 어려움을 겪고 있다. 이러한 경향에 대응하고 해양 천연물연구의 활성화를 위한 해양생물자원 데이터베이스 구축을 위하여 181개 해면동물 추출물에 대한 HPLC 프로파일을 생성하고 항염증 및 신경세포보호 활성을 탐색하였다. 이를 통하여 해면동물 추출물간의 HPLC를 통한 함유성분에 따른 클러스터링이 가능하였고 또한 각각 17개, 14개 시료에서 항염증 활성과 신경세포보호활성이 확인되었다. 이와 같은 연구는 해면동물을 포함한 해양생물자원에서의 효과적인 생리활성 탐색에 도움이 될 것이라고 판단한다.

New from Old: Thorectandrin Alkaloids in a Southern Australian Marine Sponge, Thorectandra choanoides (CMB-01889)

Thorectandra choanoides (CMB-01889) was prioritized as a source of promising new chemistry from a library of 960 southern Australian marine sponge extracts, using a global natural products social (GNPS) molecular networking approach. The sponge was collected at a depth of 45 m. Chemical fractionation followed by detailed spectroscopic analysis led to the discovery of a new tryptophan-derived alkaloid, thorectandrin A (1), with the GNPS cluster revealing a halo of related alkaloids 1a–1n. In considering biosynthetic origins, we propose that Thorectandra choanoides (CMB-01889) produces four well-known alkaloids, 6-bromo-1′,8-dihydroaplysinopsin (2), 6-bromoaplysinopsin (3), aplysinopsin (4), and 1′,8-dihydroaplysinopsin (10), all of which are susceptible to processing by a putative indoleamine 2,3-dioxygenase-like (IDO) enzyme to 1a–1n. Where the 1′,8-dihydroalkaloids 2 and 10 are fully transformed to stable ring-opened thorectandrins 1 and 1a–1b, and 1h–1j, respectively, the conjugated precursors 3 and 4 are transformed to highly reactive Michael acceptors that during extraction and handling undergo complete transformation to artifacts 1c–1g, and 1k–1n, respectively. Knowledge of the susceptibility of aplysinopsins as substrates for IDOs, and the relative reactivity of Michael acceptor transformation products, informs our understanding of the pharmaceutical potential of this vintage marine pharmacophore. For example, the cancer tissue specificity of IDOs could be exploited for an immunotherapeutic response, with aplysinopsins transforming in situ to Michael acceptor thorectandrins, which covalently bind and inhibit the enzyme.