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Gagunins A–G, seven new diterpenoids were isolated from the sponge Phorbas sp. collected from Gagu-Do, Korea. The carbon skeleton of these highly oxygenated metabolites was determined to be an unusual 10,13-bis-epi-homoverrucosane on the basis of combined chemical and spectral methods. Stereochemical assignments of these diterpenoids were accomplished by extensive ROESY and 1D NOESY experiments. The novel compounds exhibited significant cytotoxicity with values ranging from 0.03 to 51 μg/mL, toward a human leukemia cell-line (K-562). [Copyright &y& Elsevier]

Paralytic shellfish toxins (PSTs) are potent neurotoxins produced by certain microalgae, particularly dinoflagellates, and they can accumulate in shellfish in coastal seawater and thus pose significant health risks to humans. To explore the relationship between toxicity and PST profiles in seawater and mussels, the spatiotemporal variations in PST concentrations and profiles were investigated along the southern coast of Korea under peak PST levels during spring. Seawater and mussel samples were collected biweekly from multiple stations, and the toxin concentrations in the samples were measured. Moreover, the dinoflagellate community composition was analyzed using next-generation sequencing to identify potential PST-producing species. The PST concentrations and toxin profiles showed substantial spatiotemporal variability, with GTX1 and GTX4 representing the dominant toxins in both samples, and C1/2 tending to be higher in seawater. Alexandrium species were identified as the primary sources of PSTs. Environmental factors such as water temperature and salinity influenced PST production. This study demonstrates that variability in the amount and composition of PSTs is due to intricate ecological interactions. To mitigate shellfish poisoning, continuous monitoring must be conducted to gain a deeper understanding of these interactions. [ABSTRACT FROM AUTHOR]

Copepods are a major component of metazooplankton and important prey for fish and invertebrates such as crabs, shrimps, and flatworms. Certain bloom-forming dinoflagellates can kill copepods, but there is little research on the interactions between copepods and the bloom-forming dinoflagellates Karenia bicuneiformis and K. selliformis. In this study, the survival and ingestion rates of the calanoid copepod Acartia hongi feeding on K. bicuneiformis and K. selliformis were determined as a function of prey concentration. On day 2, the survival of A. hongi incubated with K. bicuneiformis was 90–100% at all the tested prey concentrations, while that with K. selliformis was 0–20% at ≥ 582 ng C mL−1. Compared to other harmful dinoflagellates from the literature, K. bicuneiformis caused low mortality of Acartia; however, K. selliformis caused almost the highest mortality at similar dinoflagellate concentrations. With increasing mean prey concentration, the ingestion rates of A. hongi feeding on K. bicuneiformis increased on day 1, but those on K. selliformis did not increase. Acartia hongi stopped feeding on K. bicuneiformis at mean prey concentrations of ≥ 341 ng C mL−1 and K. selliformis at all prey concentrations on day 2. At the prey concentration of 1000 ng C mL−1, the ingestion rate of A. hongi feeding on K. bicuneiformis was moderate among the rates of Acartia spp. feeding on harmful dinoflagellates; however, that on K. selliformis was the lowest. These results indicate that K. bicuneiformis and K. selliformis differentially affect the survival and ingestion rates of A. hongi. [ABSTRACT FROM AUTHOR]

Suaeda glauca, a halophyte in the Amaranthaceae family, exhibits remarkable resilience to high salt and alkali stresses despite the absence of salt glands or vesicles in its leaves. While there is growing pharmacological interest in S. glauca, research on its secondary metabolites remains limited. In this study, chemical constituents of the aerial parts of S. glauca were identified using 1D- and 2D-NMR experiments, and its biological activity concerning hair loss was newly reported. Eight compounds, including alkaloids (1~3), flavonoids (4~6), and phenolics (7 and 8), were isolated. The compounds, except the flavonoids, were isolated for the first time from S. glauca. In the HPLC chromatogram, quercetin-3-O-β-d-glucoside, kaempferol-3-O-β-d-glucoside, and kaempferol were identified as major constituents in the extract of S. glauca. Additionally, the therapeutic potential of the extract of S. glauca and the isolated compounds 1~8 on the expressions of VEGF and IGF-1, as well as the regulation of Wnt/β-catenin signaling, were evaluated in human follicle dermal papilla cells (HFDPCs) and human umbilical vein endothelial cells (HUVECs). Among the eight compounds, compound 4 was the most potent in terms of increasing the expression of VEGF and IGF-1 and the regulation of Wnt/β-catenin. These findings suggest that S. glauca extract and its compounds are potential new candidates for preventing or treating hair loss. [ABSTRACT FROM AUTHOR]

Background: In traditional folk medicine, Limonium tetragonum is used in the treatment of uterine hemorrhage, tinnitus, and oligomenorrhea. Objective: This study aimed to identify the therapeutic effect of L. tetragonum EtOAc extract (EALT) on liver of mice with chronic alcohol poisoning. Materials and Methods: C57BL/6J mice were administered 100 mg/kg of EALT with a single binge ethanol/Lieber-DeCarli liquid diet for 8 weeks. Results: The chronic-binge ethanol diet induced a significant increase in liver marker enzyme activities. Coadministration of EALT reversed the elevation of serum total cholesterol and triglyceride as well as aspartate aminotransferase and alanine aminotransferase due to chronic alcohol consumption. Histologic findings including markedly attenuated fat accumulation in hepatocytes were observed in EALT-treated mice. EALT supplementation prevented alcoholic liver injury through attenuation of inflammatory mediators such as toll-like receptor-4, cytochrome P4502E1, and cyclooxygenase-2, and inflammatory cytokine interleukin-6. Conclusion: Results provided direct experimental evidence for the hepatoprotective effect of EALT in the NIAAA mouse model. Therapeutic attempts with the L. tetragonum extract might be useful in the management of alcoholic liver disease. [ABSTRACT FROM AUTHOR]

There were five sesquiterpene lactones, belonging to the eudesmanolide class, isolated from the halophyte Sonchus brachyotus DC. The structures of the compounds were determined using spectroscopic methods, including 1D and 2D NMR spectra, MS data, and optical rotation values. Compounds 4 and 5 were characterized by the position of p-hydroxyphenylacetyl group in the sugar moiety. In the evaluation of anti-inflammatory effects on LPS-activated RAW264.7 macrophages, compound 1, 5α,6βH-eudesma-3,11(13)-dien-12,6α-olide, potently suppressed the expression of iNOS and COS-2, as well as the production of TNF-α, IL-6, and IL-10. Treatment of 1 regulates the Nrf2/HO-1 pathway. [ABSTRACT FROM AUTHOR]

Lithium metal batteries (LMBs) have the potential to deliver a greater specific capacity than any commercially used lithium battery. However, excessive dendrite growth and low Coulombic efficiencies (CEs) are major hurdles preventing the commercialization of LMBs. In this study, two different salts, lithium difluorophosphate (LiDFP) and lithium bis(trifluoromethanesulfonyl)imide (LiTFSI), are chosen for use in concentrated electrolytic systems. By mixing salts with vastly different cation–anion interaction energies, the ion solvation structures in the electrolyte can be modulated to enhance the physical/electrochemical properties and suppress Li dendrite growth in LMBs. Among the investigated electrolyte systems, 2.2 m LiDFP + 1.23 m LiTFSI in 1,2‐dimethoxyethane is proposed as a highly promising electrolyte system because of its high conductivity (6.57 mS cm−1), CE (98.3%), and the formation of an extremely stable solid–electrolyte interface layer. The bisalt electrolyte presented herein, as well as the associated concepts, provide a new avenue toward commercial LMBs. [ABSTRACT FROM AUTHOR]

Black-fruited chokeberries (Aronia melanocarpa), growing mainly in the Central and Eastern European countries, have health benefits due to the high concentrations of polyphenolic compounds. However, a strong bitter taste of chokeberries limits its usage as functional food. We hypothesized that the fermented A. melanocarpa with a reduced bitter taste would improve insulin sensitivity and/or ameliorate weight gain induced by high-fat diet (HFD) in male C57BL/6J mice. The mice were administered with HFD together with the 100 mg/kg of natural A. melanocarpa (T1) or the fermented A. melanocarpa (T2) for 8 weeks. The treatment with T2 (100 mg/kg body weight, p.o.) markedly attenuated the weight gain and the increase in serum triglyceride level induced by HFD. The T2-treated group had better glucose tolerance and higher insulin sensitivity as measured by oral glucose tolerance test and intraperitoneal insulin tolerance test in comparison to the T1-treated group. Phytochemical analysis revealed that the main constituents of T2 were cyanidin-3-xyloside and 1-(3′,4′-dihydroxycinnamoyl)cyclopenta-2,3-diol, and the content of cyanidin glycosides (3-glucoside, 3-xyloside) was significantly reduced during the fermentation process. From the above results, we postulated that antiobesity effect of black chokeberry was not closely correlated with the cyanidin content. Fermented chokeberry might be a viable dietary supplement rich in bioactive compounds useful in preventing obesity. [ABSTRACT FROM AUTHOR]

Thecadinium kofoidiiis a marine sand-dwelling dinoflagellate that sometimes forms dense blooms. This species was previously thought to be an exclusively autotrophic dinoflagellate, and its mixotrophic ability has not been explored yet. By investigating its ecophysiology, its trophic mode should be revealed. We explored the mixotrophic ability ofT. kofoidiiby examining its protoplasm under light and transmission electron microscopes with diverse algal prey species. Furthermore, the feeding mechanism ofT. kofoidiiand prey species on which it feeds were investigated. In addition, the growth and ingestion rates ofT. kofoidiias a function of prey concentration were determined when feeding on the benthic cryptophyteRhodomonas salina.Thecadinium kofoidiiwas able to feed onR. salinaand the dinoflagellateSymbiodinium voratum, which had equivalent spherical diameters (ESDs) ≤ 10.1 µm, while it did not feed on the benthic dinoflagellatesLevanderina fissa,Prorocentrum concavumorOstreopsiscf.ovata, which had ESDs ≥ 15 µm.Thecadinium kofoidiifed on the edible prey cells using the peduncle. The maximum ingestion rate ofT. kofoidiionR. salinawas 1.3 cells predator−1d−1. However, feeding onR. salinadid not significantly increase the growth rate ofT. kofoidii. The low ingestion rate ofT. kofoidiionR. salinamay have partially resulted in the lack of significant increase in its growth rate due to mixotrophy. The present study discovered predator–prey relationships betweenT. kofoidiiandR. salinaandS. voratum, which may change our view of the energy flow and carbon cycling in marine benthic food webs. [ABSTRACT FROM PUBLISHER]

The article discusses the results of studies analyzing the bioactive constituents of marine-derived microorganisms. It details the discovery that a crude extract from a small-scale culture of the marine-mudflat-derived fungus Paecilomyces formosus displayed radical-scavenging activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and in vitro antimicrobial activity against methicillin- and multidrug-resistant Staphylococcus aureus (MRSA and MDRSA).

Cryptophytes are ubiquitous and one of the major phototrophic components in marine plankton communities. They often cause red tides in the waters of many countries. Understanding the bloom dynamics of cryptophytes is, therefore, of great importance. A critical step in this understanding is unveiling their trophic modes. Prior to this study, several freshwater cryptophyte species and marine Cryptomonas sp. and Geminifera cryophila were revealed to be mixotrophic. The trophic mode of the common marine cryptophyte species, Teleaulax amphioxeia has not been investigated yet. Thus, to explore the mixotrophic ability of T. amphioxeia by assessing the types of prey species that this species is able to feed on, the protoplasms of T. amphioxeia cells were carefully examined under an epifluorescence microscope and a transmission electron microscope after adding each of the diverse prey species. Furthermore, T. amphioxeia ingestion rates heterotrophic bacteria and the cyanobacterium Synechococcus sp. were measured as a function of prey concentration. Moreover, the feeding of natural populations of cryptophytes on natural populations of heterotrophic bacteria was assessed in Masan Bay in April 2006. This study reported for the first time, to our knowledge, that T. amphioxeia is a mixotrophic species. Among the prey organisms offered, T. amphioxeia fed only on heterotrophic bacteria and Synechococcus sp. The ingestion rates of T. amphioxeia on heterotrophic bacteria or Synechococcus sp. rapidly increased with increasing prey concentrations up to 8.6 × 10 6 cells ml −1 , but slowly at higher prey concentrations. The maximum ingestion rates of T. amphioxeia on heterotrophic bacteria and Synechococcus sp. reached 0.7 and 0.3 cells predator −1  h −1 , respectively. During the field experiments, the ingestion rates and grazing coefficients of cryptophytes on natural populations of heterotrophic bacteria were 0.3–8.3 cells predator −1 h −1 and 0.012–0.033 d −1 , respectively. Marine cryptophytes, including T. amphioxeia, are known to be favorite prey species for many mixotrophic and heterotrophic dinoflagellates and ciliates. Cryptophytes, therefore, likely play important roles in marine food webs and may exert a considerable potential grazing impact on the populations of marine bacteria. [ABSTRACT FROM AUTHOR]

Despite the nutritional and medicinal values of Allium hookeri, its unique flavor (onion or garlic taste and smell) coming from sulfur containing compounds limits its usage as functional food. For comparative study, A. hookeri roots were prepared under two different drying conditions, namely, low-temperature drying that minimizes the volatilization of sulfur components and hot-air drying that minimizes the garlic odor and spicy taste of A. hookeri. In GC/MS olfactory system, the odorous chemicals and organosulfur compounds such as diallyl trisulfide, dimethyl trisulfide, and dipropyl trisulfide were significantly decreased in hot-air drying compared to low-temperature drying. The spiciness and saltiness taste were noticeably reduced, while sourness, sweetness, and umami taste were significantly increased in hot-air dried A. hookeri according to electronic tongue. Although the content of volatile sulfur components was present at lower level, the administration of hot-air dried A. hookeri extract (100 mg/kg p.o.) apparently prevented the body weight gain and improved insulin resistance in C57BL/6J obese mice receiving high fat diet. Results suggested that the hot-air dried A. hookeri possessing better taste and odor might be available as functional crop and bioactive diet supplement for the prevention and/or treatment of obesity. [ABSTRACT FROM AUTHOR]

Blooms caused by some species belonging to the dinoflagellate genus Alexandrium are known to cause large-scale mortality of fish. Thus, the dynamics of these species is important and of concern to scientists, officials, and people in the aquaculture industry. To understand the dynamics of such species, their growth and mortality due to predation need to be assessed. The newly described dinoflagellate Alexandrium pohangense is known to grow slowly, with a maximum autotrophic growth rate of 0.1 d −1 . Thus, it may not form bloom patches if its mortality due to predation is high. Therefore, to explore the mortality of A. pohangense due to predation, feeding on this species by the common heterotrophic dinoflagellates Gyrodinium dominans, Gyrodinium moestrupii, Luciella masanensis, Noctiluca scintillans, Oxyrrhis marina, Oblea rotunda, Polykrikos kofoidii , and Pfiesteria piscicida , as well as by the ciliate Tiarina fusus , was examined. None of these potential predators was able to feed on A. pohangense . In contrast, these potential predators were killed and their bodies were dissolved when incubated with A. pohangense cells or cell-free culture filtrates. The survival of G. moestrupii, O. marina, P. kofoidii , and T. fusus on incubation with 10 cells ml −1 of A. pohangense was 20–60%, while that at the equivalent culture filtrates was 20–70%. With increasing A. pohangense cell-concentration (up to 1000 cells ml −1 or equivalent culture filtrates), the survival rate of G. moestrupii, O. marina, P. kofoidii , and T. fusus rapidly decreased. The lethal concentration (LC 50 ) for G. moestrupii, O. marina, P. kofoidii , and T. fusus at the elapsed time of 24 h with A. pohangense cells (cultures of 11.4, 13.3, 1.6, and 3.3 cells ml −1 , respectively) was lower than that with A. pohangense filtrates (culture filtrates of 35.5, 30.6, 5.5, and 5.0 cells ml −1 , respectively). Furthermore, most of the ciliates and heterotrophic dinoflagellates in the water collected from the coast of Tongyoung, Korea, were killed when incubated with cultures of 1000 A. pohangense cells ml −1 and equivalent culture filtrates. The relatively slow growing A. pohangense may form blooms by reducing mortality due to predation through killing potential protist predators. [ABSTRACT FROM AUTHOR]

The article talks about a Diol Ester derivative of Dinophysistoxin-1 obtained from Prorocentrum found in South Korea. It adds that marine dinoflagellates may cause food poisoning and contains toxins such as okadaic acid (OA), pectenotoxin-2 (PTX-2) and dinophysistoxin-1 (DTX-1). The methanolic extract of Prorocentrum lima shows cytotoxicity which is shown by liquid chromatography-mass spectometry (LC-MS).

AcuminolideA (1), along with pectenotoxin II (PTX-2),dinophysistoxin I (DTX-1), okadaic acid (OA), and 7-epi-PTX-2 secoacid, was isolated from a large-scalecultivation of the dinoflagellate Dinophysis acuminata. The new 33-membered macrolide 1was characterizedby detailed analysis of 2D NMR and MS data. Its relative stereochemistrywas elucidated on the basis of ROESY correlations and J-based analysis. In contrast to the other well-known toxins thatwere isolated, 1showed no cytotoxicity against fourcancer cell lines but caused potent stimulation of actomyosin ATPaseactivity. [ABSTRACT FROM AUTHOR]

Abstract: Ostreol A was isolated from cultures of the epiphytic dinoflagellate Ostreopsis cf. ovata from the coastal waters of Jeju Island, Korea. The compound, a non-palytoxin derivative, has a polyhydroxy chain ending with the primary amino group and contains an amide bond, along with two tetrahydropyran rings in the chain. Its chemical structure was elucidated by nuclear magnetic resonance (NMR) spectroscopy methods and confirmed by mass analysis. The compound exhibited significant cytotoxicity in the brine shrimp lethality test at a concentration of 0.9μg/mL. [Copyright &y& Elsevier]

Ten ceramides and four cerebrosides were extracted from the starfish Distolasterias nipon by solvent extraction, silica gel column chromatography and reversed-phase high-performance liquid chromatography. Structural identification was conducted using tandem mass spectrometry of monosodiated ions desorbed by fast atom bombardment. The complete structures of four cerebrosides were determined by a previously reported method. The high-energy collision-induced dissociation (CID) spectral characteristics of ceramides with various structures depend on the number and positions of double bonds on both the N-acyl and sphingoid chains, the presence of a hydroxyl group or a double bond at the C-4 position of the sphingoid chain and the presence of an α-hydroxy group on the N-acyl chain. The high-energy CID of the monosodiated ion, [M+Na]+, of each ceramide molecular species generated abundant ions, providing information on the composition of the fatty acyl chains and sphingoid long-chain bases. Each homologous ion series along the fatty acyl group and aliphatic chain of the sphingoid base was used for locating the double-bond positions of both chains and hydroxyl groups on the sphingoid base chain. The double-bond positions were also confirmed by the m/z values of abundant allylic even- and odd-electron ions, and the intensity ratio of the T ion peak relative to the O ion peak. This technique could determine the complete structures of ceramides and cerebrosides in an extract mixture and has great potential for determining other sphingolipids isolated from various biological sources. Copyright © 2013 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

Densanins A (1) and B (2) were isolated from the sponge Haliclona densaspicula. On the basis of spectral data and the Mosher ester method, the complete structures were characterized as hexacyclic diamine alkaloids, which were probably derived from 3-alkylpyridine. Compounds 1and 2showed relatively potent inhibitory effects on lipopolysaccharide-induced nitric oxide production in BV2 microglial cells with IC50values of 1.05 and 2.14 μM, respectively. [ABSTRACT FROM AUTHOR]

The green alga Spirogyra varians accumulated antioxidative compounds in response to cold stress. When the algae were transferred from 20°C to 4°C, the amount of phenolic contents and flavonoids in the cell increased 17 times and 30 times, respectively, in 2 months. At this time, the radical scavenging activity of the methanolic extract of S. varians was 238 times higher than that of initial culture. To identify the responsible antioxidants, the methanolic extract was obtained from the algae grown at 4°C. HPLC analysis of the extract showed six compounds newly produced or increased over time. Four of the compounds were successfully purified, and the structures were identified using H NMR spectroscopy. The compounds were galloyl derivatives-methyl gallate, 1- O-Galloyl-β- d-glucose, 1,2,3,6-tetra- O-Galloyl-β- d-glucose and 1,2,3,4,6-penta- O-Galloyl-β- d-glucose which are intermediates of the shikimate pathway. [ABSTRACT FROM AUTHOR]

Abstract: Osteoporosis arises from an imbalance between osteoblastic bone formation and osteoclastic bone resorption. In this study, we screened molecules from marine natural products that stimulate osteoblast differentiation. We found that phorbaketal A significantly stimulates osteoblast differentiation in mesenchymal cells. Increased interaction of TAZ and Runx2 stimulated phorbaketal A-induced expression of osteoblastic marker genes. The activation of ERK was important for the stimulation of differentiation because an inhibitor of ERK blocked phorbaketal A-induced osteogenic differentiation. Taken together, the results showed that phorbaketal A stimulates TAZ-mediated osteoblast differentiation through the activation of ERK. Structured summary of protein interactions: TAZ physically interacts with RUNX2 by pull down (View interaction) [Copyright &y& Elsevier]

Abstract: The gene (Ta0298) encoding a putative α-glucosidase from hyperthermophilic archaeon Thermoplasma acidophilum (AglA) was cloned and expressed in Escherichia coli. Gel filtration chromatography of the purified enzyme indicated that the native form was a pentamer with strong maltose (α-1,4 linkage)-hydrolyzing activity. AglA was optimally active at pH 5–6 and 80°C and had a half-life of 16.8h and 1.4h at 80°C and 85°C, respectively. The enzyme also hydrolyzes kojibiose (α-1,2), nigerose (α-1,3), and isomaltose (α-1,6) to a lesser extent. Analysis of the reaction with maltooligosaccharides and panose as substrates show that AglA specifically liberates glucose from the non-reducing end indicating that it is typical of a glycoside hydrolase family 31 (GH31) α-glucosidase. Kinetic analyses revealed that the hydrolytic activity of AglA was greatly affected by the chain length of the substrate and the regiospecificity of the glucosidic linkages. The enzyme showed highest specificity for maltose and decreasing values of catalytic efficiency (k cat/K m) toward higher maltooligosaccahrides, although these still serve as substrates. The inhibition profile of AglA toward aesculin was revealed to be a mixed type of noncompetitive inhibition with a K i value of 4.30μM and of 12.5μM, whereas that toward acarbose showed a competitive inhibition pattern with a K i of 2.99μM. Structural analyses of two arbutin transglucosylation products using NMR indicated that the glucose unit of maltose was transferred to the C-3 and C-6 position in the glucose moiety of arbutin. [Copyright &y& Elsevier]

• HPLC with evaporative light scattering detector for krill oil phospholipid analysis. • Developed method validated based on the ICH validation of analytical procedures. • HPLC-ELSD and 31P NMR analyses results in agreement. • HPLC-ELSD method alternative for 31P NMR technique in phospholipid analysis. A method wherein a high-performance liquid chromatography (HPLC) system is combined with an evaporative light scattering detector (ELSD) was developed and validated as an alternative to the official phosphorous-31 nuclear magnetic resonance (31P NMR) technique to analyze phospholipids in krill oil. A quadratic calibration curve with a good correlation coefficient (>0.999) in the 100–1000 μg mL−1 range was obtained for each phospholipid. The limit of detection (2–7.5 μg mL−1) of the designed assay for the phospholipids in krill oil was good, and the accuracy (99.6–101.0 %) was excellent. The relative standard deviations for repeatability (<1%) and intermediate precision (2.3 %–6.9 %) were acceptable. The results of the developed HPLC-ELSD method applied to krill oil samples were in agreement with those of 31P NMR spectroscopy. Moreover, statistical comparison indicated no significant difference between two methods. Thus, the HPLC-ELSD method can be applied for analyzing the phospholipid composition of krill oil. [ABSTRACT FROM AUTHOR]

Curcumin and some of its derivatives were known as in vivo inhibitors of angiogenesis. In present study, a novel curcumin derivative, named hydrazinocurcumin (HC) was synthesized and examined for its biological activities. HC potently inhibited the proliferation of bovine aortic endothelial cells (BAECs) at a nanomolar concentration (IC50=520 nM) without cytotoxicity. In vivo and in vitro angiogenesis experiments showed HC as a new candidate for anti-angiogenic agent. [Copyright &y& Elsevier]

Curcumin and some of its derivatives were known as in vivo inhibitors of angiogenesis. In present study, a novel curcumin derivative, named hydrazinocurcumin (HC) was synthesized and examined for its biological activities. HC potently inhibited the proliferation of bovine aortic endothelial cells (BAECs) at a nanomolar concentration (IC50=520 nM) without cytotoxicity. In vivo and in vitro angiogenesis experiments showed HC as a new candidate for anti-angiogenic agent. © 2002 Elsevier Science. All rights reserved. [Copyright &y& Elsevier]

Densazalin, a polycyclic alkaloid, was isolated from the marine sponge Haliclona densaspicula collected in Korea. The complete structure of the compound was determined by spectroscopic methods, including 1D and 2D nuclear magnetic resonance techniques, high-resolution mass spectrometry, and comparison of the calculated and measured electronic circular dichroism spectra. Densazalin possesses a unique 5,11-diazatricyclo[7.3.1.02,7]tridecan-2,4,6-triene moiety, which is connected by two linear carbon chains. This compound was derived from the biogenetic precursor bis-1,3-dialkylpyridnium. Densazalin exhibited cytotoxic activity on two human tumor cell lines (AGS and HepG2) in the Cell Counting Kit-8 (CCK-8) bioassay, with IC50 values ranging from 15.5 to 18.4 μM. [ABSTRACT FROM AUTHOR]

Keywords: bisalt electrolytes; concentrated electrolytes; high ionic conductivity; lithium dendrites; lithium metal batteries; preferential ionic interactions EN bisalt electrolytes concentrated electrolytes high ionic conductivity lithium dendrites lithium metal batteries preferential ionic interactions 1 1 1 03/22/21 20210318 NES 210318 In article number 2003520, Kyungwon Kwak, Kyung-Koo Lee and co-workers design a concentrated bisalt electrolyte for lithium metal batteries. Lithium Metal Batteries: Synergistic Effects on Lithium Metal Batteries by Preferential Ionic Interactions in Concentrated Bisalt Electrolytes (Adv. Bisalt electrolytes, concentrated electrolytes, high ionic conductivity, lithium dendrites, lithium metal batteries, preferential ionic interactions. [Extracted from the article]

Turbinaria ornata is a tropical brown algae (seaweed) known to have anti-inflammatory properties. In this study, we analyzed T. ornata extract (TOE) using liquid chromatography quadrupole time of flight mass spectrometry (LC-QTOF-MS) and nuclear magnetic resonance (NMR) and evaluated the in vivo efficacy of TOE against dextran sulfate sodium-induced chronic colitis in C57BL/6 mice. The bioactive fraction of TOE was administered orally daily for 6 weeks to mice under different treatments normal, colitis, and colitis + conventional drug (5-aminosalicylic acid, 5-ASA). Regarding clinical manifestation, the disease activity index and colon length of the colitis + TOE group were significantly reduced compared to those of the colitis group. The results of myeloperoxidase activity and histopathological examination showed similar results. Western blot analysis of colon tissues revealed that cyclooxygenase-2, tumor necrosis factor alpha (TNF-α), and phosphorylated signal transducer and activator of transcription-3 (p-STAT3) were significantly decreased in the colitis + 5-ASA group, whereas forkhead box P3 (FOXP3) was increased. qPCR results showed changes in T cell subsets; the administration of TOE upregulated regulatory T cell (Treg) expression, although T helper 17 cell (Th17) expression did not change significantly. Interestingly, the colitis + TOE group showed high levels of both Th1 and Th2 transcription factors, but the secreted cytokine interferon (IFN)-γ and interleukin (IL)-4 remained unchanged and somewhat reduced. Additionally, TNF-α gene expression was significantly reduced in the colitis + TOE group. IL-6 mRNA levels were also decreased, although not significantly. Four compounds were structurally elucidated using 1D- and 2D-NMR spectroscopy, and five compounds were fully identified or tentatively characterized using LC-QTOF-MS. In conclusion, TOE could alleviate chronic colitis via upregulation of Foxp3+ Treg cells and production of the anti-inflammatory cytokine IL-10, which directly inhibits macrophages and pro-inflammatory cytokine synthesis, leading to reduced colitis. [ABSTRACT FROM AUTHOR]

Prorocentrolide and its analogs, the novel naturally derived antitumor agents, have recently been identified in the dinoflagellate Prorocentrum lima. In the current study, the underlying inhibitory mechanisms of 4-hydroxyprorocentrolide (1) and prorocentrolide C (2) on the proliferation of human carcinoma cells were determined. 1 and 2 arrested the cell cycle at the S phase in A549 cells and G2/M phase in HT-29 cells, leading to apoptotic cell death, as determined using fluorescence-activated cell sorting analysis with Annexin V/PI double staining. Apoptosis induced by these compounds was associated with alterations in the expression of cell cycle-regulating proteins (cyclin D1, cyclin E1, CDK2, and CDK4), as well as alterations in the levels of apoptosis-related proteins (PPAR, Bcl-2, Bcl-xl, and survivin). These findings provide new insights into the antitumor mechanisms of 4-hydroxyprorocentrolide and prorocentrolide C and a basis for future investigations assessing prorocentrolide analogs as prospective therapeutic drugs. [ABSTRACT FROM AUTHOR]

Crohn's disease (CD) and ulcerative colitis (UC), collectively referred to as inflammatory bowel disease (IBD), are autoimmune diseases characterized by chronic inflammation within the gastrointestinal tract. Debromohymenialdisine is an active pyrrole alkaloid that is well known to serve as a stable and effective inhibitor of Chk2. In the present study, we attempted to investigate the anti-inflammatory properties of (10Z)-debromohymenialdisine (1) isolated from marine sponge Stylissa species using an intestinal in vitro model with a transwell co-culture system. The treatment with 1 attenuated the production and gene expression of lipopolysaccharide (LPS)-induced Interleukin (IL)-6, IL-1β, prostaglandin E2 (PGE2), and tumor necrosis factor-α in co-cultured THP-1 macrophages at a concentration range of 1–5 μM. The protein expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 were down-regulated in response to the inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-kB) translocation into the nucleus in cells. In addition, we observed that 1 markedly promoted the nuclear translocation of nuclear factor erythroid 2 related factor 2 (Nrf2) and subsequent increase of heme oxygenase-1 (HO-1) expression. These findings suggest the potential use of 1 as a pharmaceutical lead in the treatment of inflammation-related diseases including IBD. [ABSTRACT FROM AUTHOR]