• Fisheries and Aquatic Sciences
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• 제22권12호
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• pp.30.1-30.11
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• 2019

Marine natural products isolated from the sponge Fascaplysinopsis cf reticulata, in French Polynesia, were investigated as an alternative to antibiotics to control pathogens in aquaculture. The overuse of antibiotics in aquaculture is largely considered to be an environmental pollution, because it supports the transfer of antibiotic resistance genes within the aquatic environment. One environmentally friendly alternative to antibiotics is the use of quorum sensing inhibitors (QSIs). Quorum sensing (QS) is a regulatory mechanism in bacteria which control virulence factors through the secretion of autoinducers (AIs), such as acyl-homoserine lactone (AHL) in gram-negative bacteria. Vibrio harveyi QS is controlled through three parallel pathways: HAI-1, AI-2, and CAI-1. Bioassay-guided purification of F. cf reticulata extract was conducted on two bacterial species, i.e., Tenacibaculum maritimum and V. harveyi for antibiotic and QS inhibition bioactivities. Toxicity bioassay of fractions was also evaluated on the freshwater fish Poecilia reticulata and the marine fish Acanthurus triostegus. Cyclohexanic and dichloromethane fractions of F. cf reticulata exhibited QS inhibition on V. harveyi and antibiotic bioactivities on V. harveyi and T. maritimum, respectively. Palauolide (1) and fascaplysin (2) were purified as major molecules from the cyclohexanic and dichloromethane fractions, respectively. Palauolide inhibited QS of V. harveyi through HAI-1 QS pathway at 50 ㎍ ml^-1 (26 μM), while fascaplysin affected the bacterial growth of V. harveyi (50 ㎍ ml^-1) and T. maritimum (0.25 ㎍). The toxicity of fascaplysin-enriched fraction (FEF) was evaluated and exhibited a toxic effect against fish at 50 ㎍ ml^-1. This study demonstrated for the first time the QSI potential of palauolide (1). Future research may assess the toxicity of both the cyclohexanic fraction of the sponge and palauolide (1) on fish, to confirm their potential as alternative to antibiotics in fish farming.

• 해양환경안전학회지
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• 제12권2호
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• pp.81-87
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• 2006

본 연구는 남해안 북만 해역을 대상으로 조류성장잠재력(AGP) 시험을 통하여 H. akashiwo의 성장제한요인을 평가하였다. 영양물질의 첨가 및 미생물과의 동시배양에 의하면 적조발생 단계별 H. akashiwo의 성장은 서로 다른 제한요인에 의하여 영향을 받는 것으로 나타났다. 적조발생 전의 H. akashiwo 성장은 질산질소 $50{\mu}M$과 연산인 $5{\mu}M$을 복합첨가하면 크게 증가하였지만 인산인을 단독 첨가하거나 미생물과 동시 배양하여도 전혀 영향이 없었다. 적조발생 전의 H. akashiwo 성장제한요인은 질산질소로 나타났다. 적조발생시기의 H. akashiwo 성장은 질산질소 $50{\mu}M$ 또는 인산인 $5{\mu}M$을 단독첨가하면 증가하였지만 미량영양물질이나 $vitamin\;B_{12}$을 첨가해도 전혀 영향이 없었다. 적조발생 시기의 H. akashiwo 성장제한요인은 질산질소와 인산인이 동시에 작용하는 것으로 나타났다. 반면에 적조소멸시기의 H. akashiwo 성장은 질산질소와 인산인을 첨가하면 약간 증가하였지만 미생물과 동시 배양하면 현저히 감소하였다. 그러므로 적조 소멸시기의 H. akashiwo 성장제한은 미생물요인에 의한 것으로 평가되었다.

• 한국수산과학회지
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• 제42권6호
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• pp.628-632
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• 2009

In order to estimate acute toxicity of various heavy metals on mysid, Neomysis japonica, the experiments were conducted by renewal bioassay method at $20\pm0.5^{\circ}C$ and $30\pm0.3$ psu salinity. The 96 hr $LC_{50}$ of Neomysis japonica exposed to cadmium, copper, zinc, arsenic, lead and chromium were $90.4\;{\mu}g/L$, $82.3\;{\mu}g/L$, $646.1\;{\mu}g/L$, $1488.5\;{\mu}g/L$, $1758.8\;{\mu}g/L$ and $1609.6\;{\mu}g/L$, respectively, and were ranked in order of toxicity: copper > cadmium > zinc > arsenic > chromium > lead.

• Journal of Microbiology and Biotechnology
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• 제23권9호
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• pp.1206-1211
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• 2013

The selective inhibition of PTP1B has been widely recognized as a potential drug target for the treatment of type 2 diabetes and obesity. In the course of screening for PTP1B inhibitory fungal metabolites, the organic extracts of several fungal species isolated from marine environments were found to exhibit significant inhibitory effects, and the bioassay-guided investigation of these extracts resulted in the isolation of fructigenine A (1), cyclopenol (2), echinulin (3), flavoglaucin (4), and viridicatol (5). The structures of these compounds were determined mainly by analysis of NMR and MS data. These compounds inhibited PTP1B activity with 50% inhibitory concentration values of 10.7, 30.0, 29.4, 13.4, and 64.0 ${\mu}M$, respectively. Furthermore, the kinetic analysis of PTP1B inhibition by compounds 1 and 5 suggested that compound 1 inhibited PTP1B activity in a noncompetitive manner, whereas compound 5 inhibited PTP1B activity in a competitive manner.

• Environmental Analysis Health and Toxicology
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• 제24권4호
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• pp.311-320
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• 2009

The short term (24-hr) and long term (21 days) effects of copper, cadmium, fenbendazole and sulfathiazole on the survival of the Korean fairy shrimp Branchinella kugenumaensis were evaluated. The 24-hr median lethal concentrations ($LC_{50}$) of copper, cadmium, fenbendazole, and sulfathiazole were 39, 512, 182, and 31,818 ${\mu}g/L$, respectively. The toxicity of copper is highest among 4 chemicals used in this study, while sulfathazole the lowest. After the long term (21 days) exposure experiment, the $LC_{50}$ copper, cadmium, fenbendazole, and sulfathiazole were 1.12, 2.1, 0.1, 6.6 ${\mu}g/L$, respectively. The long term effects of antibiotics were highly enhanced while the short-term effects were not strong. The sensitivities of B. kugenumaensis to copper and cadmium were higher than or comparable to those of other freshwater branchiopods (Streptocephalus spp., Thamnocephalus sp.), and far higher than the marine species (Artemia sp.). There were significant effects on the survival of B. kugenumaensis after long term exposure to relatively lower concentrations of copper, cadmium, fenbendazole and sulfathiazole. Therefore, B. kugenumaensis seems quite a good candidate species for the ecotoxicological assessments of freshwater environments.

• Natural Product Sciences
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• 제23권4호
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• pp.274-280
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• 2017

In a search for novel treatments for diabetic complications from natural resources, we found that the ethyl acetate-soluble fraction from the 80% ethanol extract of the leaves of Homonoia riparia has a considerable inhibitory effect on advanced glycation end product (AGE) formation. Bioassay-guided isolation of this fraction resulted in identification of 15 phenolic compounds (1 - 15). These compounds were evaluated in vitro for inhibitory activity against the formation of AGE. The majority of tested compounds, excluding ethyl gallate (15), markedly inhibited AGE formation, with $IC_{50}$ values of $2.2-89.9{\mu}M$, compared with that of the positive control, aminoguanidine ($IC_{50}=962.3{\mu}M$). In addition, the effects of active isolates on the dilation of hyaloid-retinal vessels induced by high glucose (HG) in larval zebrafish was investigated; (-)-epigallocatechin-3-O-gallate (6), corilagin (7), and desmanthine-2 (11) significantly decreased HG-induced dilation of hyaloid-retinal vessels compared with the HG-treated control group.

• Archives of Pharmacal Research
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• 제28권12호
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• pp.1376-1380
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• 2005

In this study, ethanolic extracts from 18 seaweed variants were assessed for hepatoprotective activity against tacrine-induced cytotoxicity in Hep G2 cells. Only one of these, Ecklonia stolonifera Okamura (Laminariaceae), a member of the brown algae, exhibited promising hepatoprotective activity. Bioassay-guided fractionation of the active ethyl acetate (EtOAc) soluble fraction obtained from the ethanolic extract of E. stolonifera, resulted in the isolation of several phlorotannins [phloroglucinol (1), eckstolonol (2), eckol (3), phlorofucofuroeckol A (4), and dieckol (5)]. Compounds 2 and 4 were determined to protect Hep G2 cells against the cytotoxic effects of tacrine, with $EC_{50}$ values of 62.0 and 79.2 $\mu$g/mL, respectively. Silybin, a well characterized hepatoprotective agent, was used as a positive control, and exhibited an $EC_{50}$ value of 50.0 $\mu$g/mL. It has been suggested that the phlorotannins derived from marine brown algae might prove useful sources in the development of novel hepatoprotective agents.

• Journal of Ginseng Research
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• 제21권2호
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• pp.78-84
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• 1997

As a part of our ongoing effort to develop new antineoplastic immunostimulator from natural sources, bioassay-directed fractionationn of polysaccharides from Korean red ginseng was carried out by observing the proliferation of marine spleen cells and the generation of lymphoklne activated killer (LAK) cells. The acidic polysaccharide fractions proliferated spleen cells and generated LAK cells in proportion to their acidity in vitro. The LAK cell which was induced by ginseng showed tumoricidal activity against both NK celt sensitive and insensitive tumor target cells without major histocompatibility (MHC) restriction. Adherent macrophages and CD4+helper T cells were involved in the generation of the LAK cells. The acidic polysaccharide from Korean red ginseng synerglzed with recombinant IL-2 (rIff-2) at lower than 3 U/ml. The optimal doses of the acidic polysaccharide from Korean red ginseng for the proliferation of spleen cells and for the generation of LAK cells were 1 mg/ml and 100 $\mu\textrm{g}$/ml, respectively; this means that the mechanisms for the both activities may be different from each other.

• Natural Product Sciences
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• 제19권1호
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• pp.61-65
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• 2013

A bioassay-guided fractionation of the extract of the fungus Paecilomyces variotii, which was derived from the giant jellyfish Nemopilema nomurai, led to the isolation of antibacterial compounds viriditoxin and its monomeric subunit semi-viriditoxin. Viriditoxin showed significant antibacterial activity against several marine fish and human pathogens including MDR strains. Significant potencies against resistant pathogens such as VRE Enterococcus faecium, VRE Enterococcus faecalis, and MRSA were highly interesting. Viriditoxin also showed notable antibacterial activity against the fish pathogen Streptococcus iniae. Its potency was over 100-fold higher than oxytetracycline which is employed as a general antibiotic for aquaculture.

• Natural Product Sciences
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• 제17권2호
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• pp.100-103
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• 2011

Phytochemical study on the ethanol extract of a Crinum species by bioassay-guided fractionation resulted in the isolation of an active principle, which was determined as parthenin (1) on the basis of physicochemical and spectroscopic analyses. This is the first report on the existence of a sesquiterpenoid from Crinum ensifolium. Compound 1 was found to show strong cytotoxic activity against some cancer cell lines and strongly inhibit NF-${\kappa}$B activity with the $IC_{50}$ value of 1.82 ${\mu}M$.