• Natural Product Sciences
• /
• 제18권1호
• /
• pp.8-12
• /
• 2012

An anacardic acid analog (1) was isolated from the fungus Paecilomyces variotii which was derived from the giant jellyfish Nemopilema nomurai. Compound 1 was isolated from a natural source for the first time and was evaluated for antibacterial activity against human and marine pathogens, including MDR (multidrugresistant) strains. Compound 1 exhibited mild antibacterial activity against Escherichia coli DC 2, Streptococcus iniae, and methicillin-resistant Staphylococcus aureus 3089 (MRSA).

• Natural Product Sciences
• /
• 제19권1호
• /
• pp.61-65
• /
• 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
• /
• 제21권4호
• /
• pp.231-236
• /
• 2015

Two new azaphilone derivatives containing 1,3-dioxolane moiety, penidioxolanes A (1) and B (2), were isolated from marine-derived fungus Penicillium sp. KCB12C078, together with four known compounds (3-6) by chemical investigation. Compounds 1 - 6 were isolated by combination of silica gel, ODS column chromatography and preparative HPLC. Their structures were determined by analysis of spectroscopic data including 1D-, 2D-NMR, and MS techniques. The isolates were evaluated against cancer cell growth inhibition effects and antimicrobial activity.

• Natural Product Sciences
• /
• 제22권3호
• /
• pp.216-219
• /
• 2016

The microbial transformation of anthranilic acid (1) by the marine-mudflat-derived fungus Thielavia sp. produced an antibacterial polycyclic quinazoline alkaloid, thielaviazoline (2). The stereostructure of the metabolite was assigned based on detailed spectroscopic data analyses including comparison of the NMR ($^1H$ and $^{13}C$) data with those of reported compound (2). Compound 2 displayed in vitro antimicrobial activity against methicillin-resistant and multidrug-resistant Staphylococcus aureus (MRSA and MDRSA), with minimum inhibitory concentrations (MICs) of 6.25 and $12.5{\mu}g/mL$, respectively. Compound 2 also showed potent radical-scavenging activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) with an $IC_{50}$ of $11{\mu}M$, which was more active than the positive control, L-ascorbic acid ($IC_{50}$, $20.0{\mu}M$).

• Bulletin of the Korean Chemical Society
• /
• 제30권1호
• /
• pp.188-192
• /
• 2009

New $\alpha$-pyrones (1 and 2) and cyclohexenones (13 and 14) were isolated along with known analogues (3, 5−12) from the ethyl acetate extract of the whole broth of the fungus Paecilomyces lilacinus, a strain derived from a marine sponge Petrosia sp. Their structures were established by interpretation of 1D and 2D NMR, and FABMS data. It is interesting to isolate cyclohexenone derivatives from the genus Paecilomyces (family Trichocomaceae, order Eurotiales), since these cyclohexenones were previously reported only from far distinct genera, Phoma and Alternaria (family Pleosporaceae, order Pleosporales). Compounds 6, 7, and 9 were evaluated for cytotoxicity against a small panel of human solid tumor cell lines. Their cytotoxicity was insignificant upto a concentration of 30 ${\mu}g/mL$.

• Journal of Microbiology and Biotechnology
• /
• 제29권4호
• /
• pp.587-595
• /
• 2019

Pharmacological research on (CHA), a marine-derived quinazolinone alkaloid with significant cytotoxic activity, is restricted by low yields and is a problem that needs to be settled urgently. In this work, the selection of additional nitrogen sources and the optimization of additional concentrations and longer fermentation times using ammonium acetate, were investigated. CHA production was optimized to 62.1 mg/l with the addition of 50 mM ammonium acetate at 120 h of the fermentation in the shaker flask. This feeding strategy significantly increased 3-deoxy-arabino-heptulosonate-7-phosphate synthase activity and transcript levels of critical genes (laeA, dahp, and trpC) in the shikimate pathway compared with the non-treatment group. In addition, the selection of the feeding rate (0.01 and $0.03g/l{\cdot}h$) was investigated in a 5-L bioreactor. As a result, CHA production was increased by 57.9 mg/l with a $0.01g/l{\cdot}h$ ammonium acetate feeding rate. This work shows that the strategy of ammonium acetate supplementation had an effective role in improving CHA production by Aspergillus fumigatus CY018. It also shows that this strategy could serve as an important example of large-scale fermentation of a marine fungus in submerged culture.

• Natural Product Sciences
• /
• 제21권4호
• /
• pp.240-247
• /
• 2015

Viridicatol (1) has previously been isolated from the extract of the marine-derived fungus Penicillium sp. SF-5295. In the course of further biological evaluation of this quinolone alkaloid, anti-inflammatory effect of 1 in RAW264.7 and BV2 cells stimulated with lipopolysaccharide (LPS) was observed. In this study, our data indicated that 1 suppressed the expression of well-known pro-inflammatory mediators such as inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2, and consequently inhibited the production of iNOS-derived nitric oxide (NO) and COX-2-derived prostaglandin E2 ($PGE_2$) in LPS stimulated RAW264.7 and BV2 cells. Compound 1 also reduced mRNA expression of pro-inflammatory cytokines such as $interleukin-1{\beta}$ ($IL-1{\beta}$), interleukin-6 (IL-6), and tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$). In the further evaluation of the mechanisms of these anti-inflammatory effects, 1 was shown to inhibit nuclear factor-kappa B ($NF-{\kappa}B$) pathway in LPS-stimulated RAW264.7 and BV2 cells. Compound 1 blocked the phosphorylation and degradation of inhibitor kappa B $(I{\kappa}B)-{\alpha}$ in the cytoplasm, and suppressed the translocation of $NF-{\kappa}B$ p65 and p50 heterodimer in nucleus. In addition, viridicatol (1) attenuated the DNA-binding activity of $NF-{\kappa}B$ in LPS-stimulated RAW264.7 and BV2 cells.

• Journal of Microbiology and Biotechnology
• /
• 제19권7호
• /
• pp.675-680
• /
• 2009

There is considerable interest in the isolation of potent radical scavenging compounds from natural resources to treat diseases involving oxidative stress. In this report, four new fungal metabolites including one new bisdihydroanthracenone derivative (1, eurorubrin), two new seco-anthraquinone derivatives [3, 2-O-methyl-9-dehydroxyeurotinone and 4, 2-O-methyl-4-O-(${\alpha}$-D-ribofuranosyl)-9-dehydroxyeurotinone], and one new anthraquinone glycoside [6,3-O-(${\alpha}$-D-ribofuranosyl)-questin], were isolated and identified from Eurotium rubrum, an endophytic fungal strain that was isolated from the inner tissue of the stem of the marine mangrove plant Hibiscus tiliaceus. In addition, three known compounds including asperflavin (2), 2-0-methyleurotinone (5), and questin (7) were also isolated and identified. Their structures were elucidated on the basis of spectroscopic analysis. All of the isolated compounds were evaluated for 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity.

• Natural Product Sciences
• /
• 제11권3호
• /
• pp.136-138
• /
• 2005

Bioassay-guided fractionation of an organic extract of the broth from the marine-derived fungus of the genus Aspergillus led to the isolation of the polyketides, (+)-epoxydon (1), (+)-epoxydon monoacetate (2), gentisyl alcohol (3), 3-chlorogentisyl alcohol (4), and methylhydroquinone (5). Compounds 1-5 showed a potent antibacterial activity against the methicillin-resistant and multidrug-resistant Staphylococcus aureus (MRSA and MDRSA) with MIC (minimum inhibitory concentration) values of 12.5, 12.5, 12.5, 50.0, and $6.2\;{\mu}g/mL$, respectively. Compounds 1-4 also exhibited a significant radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH) with $IC_{50}$ values of 6.0, 15.0, 7.0, and $1.0\;{\mu}M$, respectively.

• Journal of Microbiology and Biotechnology
• /
• 제24권10호
• /
• pp.1346-1353
• /
• 2014

In the present study, an anthraquinone derivative, questinol was successfully isolated from the broth extract of the marine-derived fungus Eurotium amstelodami for the first time. The structure of questinol was determined based on the analysis of the MS and NMR spectral data as well as comparison of those data with the published data. Moreover, the anti-inflammatory effect of questinol in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells was investigated. The results showed that questinol did not exhibit cytotoxicity in LPS-stimulated RAW 264.7 cells up to $200{\mu}M$. Questinol could significantly inhibit NO and $PGE_2$ production at indicated concentrations. Questinol was also found to inhibit the production of pro-inflammatory cytokines, including TNF-${\alpha}$, IL-1${\beta}$, and IL-6. Furthermore, the western blot analysis showed that questinol suppressed the expression level of iNOS in a dose-dependent manner. However, questinol could slightly inhibit the expression of COX-2 at the concentration of $200{\mu}M$. Therefore, our study suggests that questinol might be selected as a promising agent for the prevention and therapy of inflammatory disease.