A 4/8 Subtype α-Conotoxin Vt1.27 Inhibits N-Type Calcium Channels With Potent Anti-Allodynic Effect DOI Creative Commons
Shuo Wang, Peter H. Bartels, Cong Zhao

et al.

Frontiers in Pharmacology, Journal Year: 2022, Volume and Issue: 13

Published: April 29, 2022

A novel 4/8 subtype α-conotoxin, Vt1.27 (NCCMFHTCPIDYSRFNC-NH 2 ), was identified from Conus vitulinus in the South China Sea by RACE methods. The peptide synthesized and structurally characterized. Similar to other α-conotoxins that target neuronal nicotinic acetylcholine receptor (nAChR) subtypes, inhibited rat α3β2 nAChR (IC 50 = 1160 nM) inactive at voltage-gated sodium potassium channels sensory neurons. However, high voltage-activated N-type (Ca V 2.2) calcium expressed HEK293T cells with an IC of 398 nM. An alanine scan showed residues Phe 5 , Pro 9 Ile 10 Ser 13 contribute significantly inhibitory activity Vt1.27. molecular dockings indicate inhibits transmembrane region Ca 2.2, which is different ω-conotoxins. Furthermore, exhibited potent anti-allodynic effect partial sciatic nerve injury (PNL) chronic constriction (CCI) pain models nmol/kg level intramuscular injection. threshold elevation groups higher than α-conotoxin Vc1.1 CCI models. These findings expand our knowledge targets potentially provide a potent, for treatment neuropathic pain.

Language: Английский

Marine Demospongiae: A Challenging Treasure of Bioactive Compounds DOI Creative Commons
Roberta Esposito, Serena Federico, Marco Bertolino

et al.

Marine Drugs, Journal Year: 2022, Volume and Issue: 20(4), P. 244 - 244

Published: March 31, 2022

In the last decades, it has been demonstrated that marine organisms are a substantial source of bioactive compounds with possible biotechnological applications. Marine sponges, in particular those belonging to class Demospongiae, have considered among most interesting invertebrates for their potential. this review, attention is devoted natural compounds/extracts isolated from Demospongiae and associated microorganisms important biological activities pharmacological applications such as antiviral, anticancer, antifouling, antimicrobial, antiplasmodial, antifungal antioxidant. The data here presented show sponges an exciting compounds, which worth developing into new drugs, avarol, hydroquinone sponge

Language: Английский

Citations

17
Integration of HPTLC with ATR-FTIR, HRMS and bioquantification for evaluation of antibacterial and antioxidant compounds in marine sponges DOI
Miljan Bigović, Marko Jović, Marko Nikolić

et al.

Journal of Chromatography A, Journal Year: 2025, Volume and Issue: unknown, P. 465967 - 465967

Published: April 1, 2025

Language: Английский

Citations

0
Structure from Motion Photogrammetry as an Effective Nondestructive Technique to Monitor Morphological Plasticity in Benthic Organisms: The Case Study of Sarcotragus foetidus Schmidt, 1862 (Porifera, Demospongiae) in the Portofino MPA DOI Creative Commons
Torcuato Pulido Mantas, Camilla Roveta, Barbara Calcinai

et al.

Diversity, Journal Year: 2024, Volume and Issue: 16(3), P. 175 - 175

Published: March 8, 2024

Porifera are essential components of marine ecosystems, providing valuable ecological functions. Traditional approaches to estimating sponge growth and biomass destructive often not suitable for certain morphologies. The implementation new innovative techniques nondestructive methodologies have allowed a more sustainable approach. In this study, population Sarcotragus foetidus Schmidt, 1982 (Demospongiae, Dictyoceratida, Irciinidae), thriving inside the Portofino Marine Protected Area, was monitored using Structure from Motion photogrammetry over period 6 years, September 2017 October 2023. Of 20 initial individuals, only 12 were still in place during last monitoring, indicating 40% mortality. Through photogrammetry, overall volume change production estimated be 9.24 ± 5.47% year−1 29.52 27.93 g DW year−1, respectively, general decreasing trend between 2021 Signs necrosis observed some potentially related high temperature occurring summer 2022 Considering current climate crisis, long-term monitoring efforts must made better understand dynamics species, has potential versatile tool that will contribute standardization studies.

Language: Английский

Citations

3
Pro-Apoptotic Activity of the Marine Sponge Dactylospongia elegans Metabolites Pelorol and 5-epi-Ilimaquinone on Human 501Mel Melanoma Cells DOI Creative Commons
Sara Carpi, Egeria Scoditti, Beatrice Polini

et al.

Marine Drugs, Journal Year: 2022, Volume and Issue: 20(7), P. 427 - 427

Published: June 28, 2022

The natural environment represents an important source of drugs that originates from the terrestrial and, in minority, marine organisms. Indeed, a largely untapped process drug discovery. Among all organisms, sponges with algae represent richest compounds showing anticancer activity. In this study, two secondary metabolites pelorol (PEL) and 5-epi-ilimaquinone (EPI), purified Dactylospongia elegans were investigated for their anti-melanoma PEL EPI induced cell growth repression 501Mel melanoma cells concentration- time-dependent manner. A cycle block G1 phase by was also observed. Furthermore, significant accumulation DNA histone fragments cytoplasmic fraction, indicating pro-apoptotic effect both compounds. At molecular level, apoptosis through increase BAX expression, confirmed decrease its silencing miR-214-3p anti-apoptotic BCL-2, MCL1, BIRC-5 mRNA attested miRNAs, i.e., miR-193a-3p miR-16-5p. conclusion, our data indicate exert cytotoxicity activity against promoting apoptotic signaling inducing changes miRNA expression downstream effectors. For these reasons could promising lead research.

Language: Английский

Citations

10
Use of the Allium cepa Model to Assess the Cytogenotoxicity of Luffariella herdmani Marine Sponge Extract DOI

Sashini Umasha Kuruppuarachchi,

Uthpala A. Jayawardena, Varuni Karunika Gunathilake

et al.

Alternatives to Laboratory Animals, Journal Year: 2023, Volume and Issue: 51(3), P. 175 - 187

Published: April 26, 2023

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

Language: Английский

Citations

4
Evaluation of In Vitro Cytotoxic Potential of Avarol towards Human Cancer Cell Lines and In Vivo Antitumor Activity in Solid Tumor Models DOI Creative Commons
Tatjana Stanojković, М. В. Филимонова, Nađa Grozdanić

et al.

Molecules, Journal Year: 2022, Volume and Issue: 27(24), P. 9048 - 9048

Published: Dec. 19, 2022

The goal of this study was to determine the activity in vitro and vivo avarol, a sesquiterpene hydroquinone originating from Dysidea avara sponge south Adriatic Sea, against different cancer cell lines two types mouse carcinoma. To investigate cytotoxicity, human cervix adenocarcinoma line (HeLa), colon (LS174), non-small-cell lung carcinoma (A549), normal fetal fibroblast (MRC-5) were used. antitumor investigated transplantable tumors, Ehrlich (EC) cervical (CC-5). effect avarol on survival, which determined by microculture tetrazolium test, confirmed significant potency lines, without selectivity towards MRC-5. highest cytotoxicity exhibited HeLa cells (10.22 ± 0.28 μg/mL). Moreover, potent tumor models determined, as intraperitoneal administration at dose 50 mg/kg resulted inhibition growth mice. After three administrations 29% EC achieved, while case CC-5, 36% achieved after second avarol. Therefore, results indicate that marine sesquiterpenoid could be promising bioactive compound development new anticancer medicine.

Language: Английский

Citations

6
A 4/8 Subtype α-Conotoxin Vt1.27 Inhibits N-Type Calcium Channels With Potent Anti-Allodynic Effect DOI Creative Commons
Shuo Wang, Peter H. Bartels, Cong Zhao

et al.

Frontiers in Pharmacology, Journal Year: 2022, Volume and Issue: 13

Published: April 29, 2022

A novel 4/8 subtype α-conotoxin, Vt1.27 (NCCMFHTCPIDYSRFNC-NH 2 ), was identified from Conus vitulinus in the South China Sea by RACE methods. The peptide synthesized and structurally characterized. Similar to other α-conotoxins that target neuronal nicotinic acetylcholine receptor (nAChR) subtypes, inhibited rat α3β2 nAChR (IC 50 = 1160 nM) inactive at voltage-gated sodium potassium channels sensory neurons. However, high voltage-activated N-type (Ca V 2.2) calcium expressed HEK293T cells with an IC of 398 nM. An alanine scan showed residues Phe 5 , Pro 9 Ile 10 Ser 13 contribute significantly inhibitory activity Vt1.27. molecular dockings indicate inhibits transmembrane region Ca 2.2, which is different ω-conotoxins. Furthermore, exhibited potent anti-allodynic effect partial sciatic nerve injury (PNL) chronic constriction (CCI) pain models nmol/kg level intramuscular injection. threshold elevation groups higher than α-conotoxin Vc1.1 CCI models. These findings expand our knowledge targets potentially provide a potent, for treatment neuropathic pain.

Language: Английский

Citations

1