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Organic Letters Sep 2023An unusual secomeroterpenoid, dysambiol (), was isolated from a sp. marine sponge collected from the South China Sea. Dysambiol features an unprecedented...
An unusual secomeroterpenoid, dysambiol (), was isolated from a sp. marine sponge collected from the South China Sea. Dysambiol features an unprecedented secomeroterpene scaffold with a rare lactone bridge. The structure of was determined by extensive spectroscopic analysis, Mosher's method, and electronic circular dichroism calculation. Dysambiol displayed potent anti-inflammatory activity in LPS-induced Raw 264.7 macrophages by regulating the NF-κB/MPAK signaling pathway.
Topics: Animals; Dysidea; Porifera; Anti-Inflammatory Agents; China; Circular Dichroism
PubMed: 37610094
DOI: 10.1021/acs.orglett.3c02409 -
Journal of Medicinal Chemistry Aug 2023Dual-specificity, tyrosine phosphorylation-regulated kinases (DYRKs) and cdc2-like kinases (CLKs) recently attracted attention due to their central involvement in...
Dual-specificity, tyrosine phosphorylation-regulated kinases (DYRKs) and cdc2-like kinases (CLKs) recently attracted attention due to their central involvement in various pathologies. We here describe a family of DYRK/CLK inhibitors derived from Leucettines and the marine natural product Leucettamine B. Forty-five 2-functionalized 2-aminoimidazolin-4-ones bearing a fused [6 + 5]-heteroarylmethylene were synthesized. Benzothiazol-6-ylmethylene was selected as the most potent residue among 15 different heteroarylmethylenes. 186 2-substituted 2-aminoimidazolin-4-ones bearing a benzothiazol-6-ylmethylene, collectively named Leucettinibs, were synthesized and extensively characterized. Subnanomolar IC (0.5-20 nM on DYRK1A) inhibitors were identified and one Leucettinib was modeled in DYRK1A and co-crystallized with CLK1 and the weaker inhibited off-target CSNK2A1. Kinase-inactive isomers of Leucettinibs (>3-10 μM on DYRK1A), named iso-Leucettinibs, were synthesized and characterized as suitable negative control compounds for functional experiments. Leucettinibs, but not iso-Leucettinibs, inhibit the phosphorylation of DYRK1A substrates in cells. Leucettinibs provide new research tools and potential leads for further optimization toward therapeutic drug candidates.
Topics: Animals; Phosphorylation; Imidazoles; Porifera; Protein Kinase Inhibitors
PubMed: 37487467
DOI: 10.1021/acs.jmedchem.3c00884 -
Journal of Structural Biology Dec 2023The widespread decline of shallow-water coral reefs has fueled interest in assessing whether mesophotic reefs can act as refugia replenishing deteriorated shallower...
The widespread decline of shallow-water coral reefs has fueled interest in assessing whether mesophotic reefs can act as refugia replenishing deteriorated shallower reefs through larval exchange. Here we explore the morphological and molecular basis facilitating survival of planulae and adults of the coral Porites astreoides (Lamarck, 1816; Hexacorallia: Poritidae) along the vertical depth gradient in Bermuda. We found differences in micro-skeletal features such as bigger calyxes and coarser surface of the skeletal spines in shallow corals. Yet, tomographic reconstructions reveal an analogous mineral distribution between shallow and mesophotic adults, pointing to similar skeleton growth dynamics. Our study reveals patterns of host genetic connectivity and minimal symbiont depth-zonation across a broader depth range than previously known for this species in Bermuda. Transcriptional variations across life stages showed different regulation of metabolism and stress response functions, unraveling molecular responses to environmental conditions at different depths. Overall, these findings increase our understanding of coral acclimatory capability across broad vertical gradients, ultimately allowing better evaluation of the refugia potential of mesophotic reefs.
Topics: Animals; Anthozoa; Bermuda; Coral Reefs; Water; Porifera; Ecosystem
PubMed: 37832837
DOI: 10.1016/j.jsb.2023.108036 -
Frontiers in Neural Circuits 2023Interkingdom signalling within a holobiont allows host and symbionts to communicate and to regulate each other's physiological and developmental states. Here we show...
Interkingdom signalling within a holobiont allows host and symbionts to communicate and to regulate each other's physiological and developmental states. Here we show that a suite of signalling molecules that function as neurotransmitters and neuromodulators in most animals with nervous systems, specifically dopamine and trace amines, are produced exclusively by the bacterial symbionts of the demosponge . Although sponges do not possess a nervous system, expresses rhodopsin class G-protein-coupled receptors that are structurally similar to dopamine and trace amine receptors. When sponge larvae, which express these receptors, are exposed to agonists and antagonists of bilaterian dopamine and trace amine receptors, we observe marked changes in larval phototactic swimming behaviour, consistent with the sponge being competent to recognise and respond to symbiont-derived trace amine signals. These results indicate that monoamines synthesised by bacterial symbionts may be able to influence the physiology of the host sponge.
Topics: Animals; Dopamine; Porifera; Amines; Neurotransmitter Agents; Communication
PubMed: 37841893
DOI: 10.3389/fncir.2023.1250694 -
Journal of the Mechanical Behavior of... Jul 2024Recently, the replication of biological microstructures has garnered significant attention due to their superior flexural strength and toughness, coupled with...
Recently, the replication of biological microstructures has garnered significant attention due to their superior flexural strength and toughness, coupled with lightweight structures. Among the most intriguing biological microstructures renowned for their flexural strength are those found in the Euplectella Aspergillum (EA) marine sponges. The remarkable strength of this sponge is attributed to its complex microstructure, which consists of concentric cylindrical layers known as spicules with organic interlayers. These features effectively impede large crack propagation, imparting extraordinary mechanical properties. However, there have been limited studies aimed at mimicking the spicule microstructure. In this study, structures inspired by spicules were designed and fabricated using the stereolithography (SLA) 3D printing technique. The mechanical properties of concentric cylindrical structures (CCSs) inspired by the spicule microstructure were evaluated, considering factors such as the wall thickness of the cylinders, the number of layers, and core diameter, all of which significantly affect the mechanical response. These results were compared with those obtained from solid rods used as solid samples. The findings indicated that CCSs with five layers or fewer exhibited a flexural strength close to or higher than that of solid rods. Particularly, samples with 4 and 5 cylindrical layers displayed architecture similar to natural spicules. Moreover, in all CCSs, the absorbed energy was at least 3-4 times higher than solid rods. Conversely, CCSs with a cylinder wall thickness of 0.65 mm exhibited a more brittle behavior under the 3-point bending test than those with 0.35 mm and 0.5 mm wall thicknesses. CCSs demonstrated greater resistance to failure, displaying different crack propagation patterns and shear stress distributions under the bending test compared to solid rods. These results underscore that replicating the structure of spicules and producing structures with concentric cylindrical layers can transform a brittle structure into a more flexible one, particularly in load-bearing applications.
Topics: Printing, Three-Dimensional; Porifera; Animals; Stereolithography; Biomimetic Materials; Mechanical Phenomena; Materials Testing
PubMed: 38640693
DOI: 10.1016/j.jmbbm.2024.106555 -
Ecology and Evolution Aug 2023The molluscan feeding structure is the radula, a chitinous membrane with teeth, which are highly adapted to the food and the substrate to which the food is attached. In...
The molluscan feeding structure is the radula, a chitinous membrane with teeth, which are highly adapted to the food and the substrate to which the food is attached. In Polyplacophora and Patellogastropoda, the handling of hard ingesta can be facilitated by high content of chemical compounds containing Fe or Si in the tooth cusps. Other taxa, however, possess teeth that are less mineralized, even though animals have to avoid structural failure or high wear during feeding as well. Here, we investigated the gastropod , feeding on hard Foraminifera, diatoms and Porifera. Tooth morphologies and wear were documented by scanning electron microscopy and their mechanical properties were tested by nanoindentation. We determined that gradients of hard- and stiffness run along each tooth, decreasing from cusp to basis. We also found that inner lateral teeth were harder and stiffer than the outer ones. These findings allowed us to propose hypotheses about the radula-ingesta interaction. In search for the origins of the gradients, teeth were visualized using confocal laser scanning microscopy, to determine the degree of tanning, and analyzed with energy-dispersive X-ray spectroscopy, to test the elemental composition. We found that the mechanical gradients did not have their origins in the elemental content, as the teeth did not contain high proportions of metals or other minerals. This indicates that their origin might be the degree of tanning. However, in the tooth surfaces that interact with the ingesta high Si and Ca contents were determined, which is likely an adaptation to reduce wear.
PubMed: 37589038
DOI: 10.1002/ece3.10332 -
Phytochemistry Dec 2023Six undescribed chlorinated sesquiterpene carbamates, aaptocarbamates A-F, and a chlorinated tris-norsesquiterpene carbamate, aaptocarbamate G, were isolated from the...
Six undescribed chlorinated sesquiterpene carbamates, aaptocarbamates A-F, and a chlorinated tris-norsesquiterpene carbamate, aaptocarbamate G, were isolated from the marine sponge Aaptos sp. collected in Indonesia. Aaptocarbamates D-F and G possess tetrahydrofurans and a tetrahydrofuranone, respectively. The relative configurations of the tetrahydrofuran units were determined by the NOE correlations and DFT-based calculation of the C chemical shifts. This is the first time that chlorinated terpene carbamates have been reported from natural sources. Various aaptamine derivatives have been reported from the Aaptos sponges so far, the isolation of chlorinated terpene carbamates is very rare. Aaptocarbamates A, B, and D showed 60% inhibition of the RANKL-induced formation of multinucleated osteoclasts in RAW264 macrophages at 20 μM.
Topics: Animals; Terpenes; Carbamates; Porifera
PubMed: 37769957
DOI: 10.1016/j.phytochem.2023.113872 -
Zootaxa Jul 2023California's network of marine protected areas was created to protect the diversity and abundance of native marine life, but the status of some taxa is very poorly...
California's network of marine protected areas was created to protect the diversity and abundance of native marine life, but the status of some taxa is very poorly known. Here we describe the sponges (phylum Porifera) from the Carmel Pinnacles State Marine Reserve, as assessed by a SCUBA-based survey in shallow waters. Of the 29 sponge species documented, 12 (41%) of them were previously unknown. Using a combination of underwater photography, DNA sequencing, and morphological taxonomy, we greatly improve our understanding of the status and distribution of previously described species and formally describe the new species as Hymedesmia promina sp. nov., Phorbas nebulosus sp. nov., Clathria unoriginalis sp. nov., Clathria rumsena sp. nov., Megaciella sanctuarium sp. nov., Mycale lobos sp. nov., Xestospongia ursa sp. nov., Haliclona melissae sp. nov., Halichondria loma sp. nov., Hymeniacidon fusiformis sp. nov., Scopalina carmela sp. nov., and Obruta collector gen. nov., sp. nov. An additional species, Lissodendoryx topsenti (de Laubenfels 1930), is moved to Hemimycale, and H. polyboletus comb. nov., nom. nov. is created due to preoccupation by H. topsenti (Burton, 1929). Several of the new species appear to be rare and/or have very restricted distributions, as they were not found at comparative survey sites outside of Carmel Bay. These results illustrate the potential of qualitative presence/absence systematic surveys of understudied taxa to discover and document substantial novel diversity.
PubMed: 37518391
DOI: 10.11646/zootaxa.5318.2.1 -
Scientific Reports Sep 2023The widespread use of synthetic pesticides has resulted in a number of issues, including a rise in insecticide-resistant organisms, environmental degradation, and a...
The widespread use of synthetic pesticides has resulted in a number of issues, including a rise in insecticide-resistant organisms, environmental degradation, and a hazard to human health. As a result, new microbial derived insecticides that are safe for human health and the environment are urgently needed. In this study, rhamnolipid biosurfactants produced from Enterobacter cloacae SJ2 was used to evaluate the toxicity towards mosquito larvae (Culex quinquefasciatus) and termites (Odontotermes obesus). Results showed dose dependent mortality rate was observed between the treatments. The 48 h LC (median lethal concentration) values of the biosurfactant were determined for termite and mosquito larvae following the non-linear regression curve fit method. Results showed larvicidal activity and anti-termite activity of biosurfactants with 48 h LC value (95% confidence interval) of 26.49 mg/L (25.40 to 27.57) and 33.43 mg/L (31.09 to 35.68), respectively. According to a histopathological investigation, the biosurfactant treatment caused substantial tissue damage in cellular organelles of larvae and termites. The findings of this study suggest that the microbial biosurfactant produced by E. cloacae SJ2 is an excellent and potentially effective agent for controlling Cx. quinquefasciatus and O. obesus.
Topics: Humans; Animals; Enterobacter cloacae; Porifera; Cloaca; Culex; Culicidae; Insecticides; Isoptera; Larva
PubMed: 37704703
DOI: 10.1038/s41598-023-42475-6 -
Current Microbiology Oct 2023The disbalance of vaginal eubiotic microbiota can lead to overgrowth of Candida species and bacteria responsible for aerobic vaginitis, activating inflammatory pathways....
The disbalance of vaginal eubiotic microbiota can lead to overgrowth of Candida species and bacteria responsible for aerobic vaginitis, activating inflammatory pathways. The presence of Trichomonas vaginalis, a sexually transmitted protozoan pathogen, can be a predisposing factor for disordering the growth of bacterial/fungal pathogenic species due to the increase in pH and reduction of eubiotic microbiota. Herein, we evaluated the effects of the potent trichomonacidal compound, copper(II)-1,10-phenanthroline-5,6-dione (Cu-phendione), against pathogens responsible for candidiasis and aerobic vaginitis. Cu-phendione showed antimicrobial activity against Candida albicans, non-albicans Candida species (C. glabrata, C. krusei, C. parapsilosis, and C. tropicalis) and Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus, Enterococcus faecalis, and Streptococcus agalactiae) bacteria. Moreover, Cu-phendione was able to interfere with the fungal biofilm formation. These results highlight the antimicrobial potential of Cu-phendione against bacterial and fungal strains of vaginitis-causing infectious agents.
Topics: Animals; Female; Humans; Copper; Dysbiosis; Anti-Infective Agents; Bacteria; Candida; Candida glabrata; Porifera; Vaginitis; Microbiota; Biofilms
PubMed: 37870614
DOI: 10.1007/s00284-023-03500-z