• Journal of Microbiology and Biotechnology
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• v.9 no.1
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• pp.119-121
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• 1999

Tumor cell interaction with the extracellular matrix is defined as the critical event of tumor invasion that signals the initiation of a metastatic cascade. Sesquicillin has been identified as an inhibitor of melanoma cell adhesion to the components of the extracellular matrix (ECM) in cultured broth of fungal strain F60063. Sesquicillin strongly inhibited the adhesion of B16 melanoma cells to laminin, fibronectin, and typeIV collagen. It also inhibited B16 melanoma cell invasion of reconstituted basement membrane Matrigel in vitro in a dose-dependent manner. These results suggest that sesquicillin is a new class of nonpeptidic ECM adhesion inhibitor having anti-invasive activity.

• Mass Spectrometry Letters
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• v.9 no.1
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• pp.37-40
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• 2018

Farinomalein is a maleimide-bearing compound well known for its anti-fungal activity. In the present study, synthesis of farinomalein is achieved via Stobbe condensation followed by Haval-Argade contrathermodynamic rearrangement. Kinetically driven Stobbe condensation followed by condensation with beta-alanine reveals formation of two isomers of farinomalein. This article describes application of LC-MS/MS in structure elucidation of farinomalein 1 and its isomers 2 and 3 encountered in its synthesis. The proposed distinct fragmentation pathway is supported by rational organic reaction mechanism. These fragmentation pathways are significant for analytical method development of farinomalein in near future. The structures of farinomalein 1 and its isomers 2 and 3 have been assigned undisputedly.

• Journal of fish pathology
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• v.23 no.1
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• pp.137-143
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• 2010

Hot water extracts of 5 herbs were tested in-vitro for anti-bacterial, anti-fungal, anti-parasitical effects for possible use against fish diseases. Skullcap, Scutellaria baicalensis, was the most effective herb in these 5. The effects of skullcap in cultured flounder were examined for various physiological responses and bacterial disease-prevention follow as feeding skullcap absorbed diet for 4, 8, 12weeks. There were not any significant effects in physiological responses, except beneficial action of growth promotion. No definitive preventive activity was observed with experimental feeding of the extract against infected flounder. As we could not confirm in-vivo antibacterial effects of skullcap in flounder despite its in-vitro efficacy, further studies are needed to define the in-vivo efficacy.

• Natural Product Sciences
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• v.21 no.4
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• pp.240-247
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• 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
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• v.30 no.4
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• pp.571-582
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• 2020

Quorum sensing (QS)-mediated infections cause severe diseases in human beings. The control of infectious diseases by inhibiting QS using antipathogenic drugs is a promising approach as antibiotics are proving inefficient in treating these diseases. Marine fungal (Pestalotiopsis sydowiana PPR) extract was found to possess effective antipathogenic characteristics. The minimum inhibitory concentration (MIC) of the fungal extract against test pathogen Pseudomonas aeruginosa PAO1 was 1,000 ㎍/ml. Sub-MIC concentrations (250 and 500 ㎍/ml) of fungal extract reduced QS-regulated virulence phenotypes such as the production of pyocyanin, chitinase, protease, elastase, and staphylolytic activity in P. aeruginosa PAO1 by 84.15%, 73.15%, 67.37%, 62.37%, and 33.65%, respectively. Moreover, it also reduced the production of exopolysaccharides (74.99%), rhamnolipids (68.01%), and alginate (54.98%), and inhibited the biofilm formation of the bacteria by 90.54%. In silico analysis revealed that the metabolite of P. sydowiana PPR binds to the bacterial QS receptor proteins (LasR and RhlR) similar to their respective natural signaling molecules. Cyclo(-Leu-Pro) (CLP) and 4-Hydroxyphenylacetamide (4-HPA) were identified as potent bioactive compounds among the metabolites of P. sydowiana PPR using in silico approaches. The MIC values of CLP and 4-HPA against P. aeruginosa PAO1 were determined as 250 and 125 ㎍/ml, respectively. All the antivirulence assays were conducted at sub-MIC concentrations of CLP (125 ㎍/ml) and 4-HPA (62.5 ㎍/ml), which resulted in marked reduction in all the investigated virulence factors. This was further supported by gene expression studies. The findings suggest that the metabolites of P. sydowiana PPR can be employed as promising QS inhibitors that target pathogenic bacteria.

• Korean Journal Plant Pathology
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• v.10 no.3
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• pp.151-156
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• 1994

Pseudomonas fluorescens produces the antibiotic, 2,4-diacetylphloroglucinol (Phl), which promotes plant growth by inhibiting bacteria and fungi. Cosmids (genomic library) were mobilized into Phl-nonproducing mutants through the triparental matings with pRK2013 as the helper plasmid at the frequency of 8.37$\times$10-4. Complemented mutants that showed antibiotic activity were selected among about 2,000 transconjugants. The complemented mutants were confirmed by acquired drug resistances (kanamycin and tetracycline). The antibiotic substances of wild type and complemented mutants showed the most excellent anti-bacterial activity. Inhibitory effects of complemented P. fluorescens against phytopathogenic fungi were equal to the parental strain. Complemented mutant and wild type of P. fluorescens were causal microbes of fungal morphological abnormalities. Complemented mutants in potato dextrose agar supplemented with bromothymol blue also showed restoration of glucose utilization as wild type. Plasmids of complemented mutants were isolated from transconjugant sand transformed into competent cells of E. coli DH5$\alpha$. The plamid DNA was reisolated from transformed E. coli DH5$\alpha$.

• Archives of Pharmacal Research
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• v.28 no.11
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• pp.1205-1212
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• 2005

2-Thiouracil-5-sulphonic acid N-(4-acetylphenyl) Amide (1) was reacted with a series of aromatic aldehydes giving chalcones 2 (Claisen-Schemidt reaction), some of these chalcones were reacted with urea and thiourea giving pyrimidine-2-one and pyrimidine-2 thione derivatives respectively of the type 3a,b and 4a,b. In addition many chalcones were reacted with hydroxylamine hydrochloride giving isoxazoline derivatives 5a,b. They could also reacted with phenylhydrazine to give pyrazoline derivatives 5a,b, chalcones also were reacted withethylcyano acetate and/or malononitryl in pyridine giving pyran derivatives 7a,c and 8a,c. In another pathway chalcones were epoxidised by $H_{2}O_{2}$ giving epoxides 9a,c which in turn were reacted with phenylhydrazine giving 4-hydroxypyrazoline derivatives 10a,c. In another reaction chalcones were reacted with ethylcyanoacetate in presence of amm.acetate giving pyridone derivatives 11a,d which could be prepared also in exellent yield from compound 1 by its reaction with certain aromatic aldehydes and ethylcyanoacetate in presence of ammonium acetate. Finally, compound 1 was reacted with semicarbazide giving semicarbazone intermediate 12 which in turn was reacted with thionyl chloride giving thiadiazole derivative 13. The biological effects of some of the new synthesized compounds were also investigated.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.15 no.9
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• pp.5628-5636
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• 2014

Currently, many countries have an interest in developing cosmetics materials using native plants. In this aspect, there is increasing need to develop cosmetics materials using native plants in our county. In the present study, calluses were induced from Artemisia annua Linne, which was highlighted because of its useful effects, such as anti-cancer, anti-fungal and anti-inflammation. Water and ethanol extractions were performed from the calluses of Artemisia annua Linne. After the mass production of Artemisia annua Linne's calluses, water and ethanol extraction was performed to examine its functional roles in healing wounds and inflammation. The differences in the effective elements were observed in the ethanol extract. The callus showed anti-inflammation activity through the suppression of the inflammation-related gene, COX-2, and ethanol extracts showed their ability to heal wounds. Overall, these results suggest that the extract of Artemisia annua Linne's calluses is a natural and environment-friendly material, and can be used as medical supplies associated with anti-inflammation and healing wounds.

• Journal of Physiology & Pathology in Korean Medicine
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• v.21 no.1
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• pp.243-249
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• 2007

The French paradox has been attributed to the antioxidant properties of flavonoids present in the red wine. Amentoflavone(AF) is a bi-flavonoid compound with anti-fungal and anti-inflammatory activities. We isolated AF from Selaginella tamariscina, and studied its effects on nuclear factor-B(NF-B)-mediated MMP-9 gene expression in RAW264.7 cells. AF blocked the lipopolysaccharide(LPS)-induced expression of MMP-9. Zymographic and immunoblot analyses showed that AF suppressed LPS-induced MMP-9 expression in a dose-dependent manner. To clarify the mechanistic basis for its inhibition of MMP-9 induction, we examined the effect of AF on the transactivation of MMP-9 gene by luciferase reporter activity using -1.59 kb flanking region. AF potently suppressed the reporter gene activity. This inhibition was characterized by down-regulation of MMP-9, which was transcriptionally regulated at NF-B site and activation protein-1 (AP-1) site in the MMP-9 promoter, two important nuclear transcription factors that are involved in MMP-9 expression. These findings indicate the efficacy of AF in inhibiting MMP-9 expression through the transcription factors NF-B and AP-1 on LPS-induced RAW264.7 cells.

• The Plant Pathology Journal
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• v.37 no.1
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• pp.24-35
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• 2021

Blue mold caused by Penicillium expansum is one of the most significant postharvest diseases of apples. Some microorganisms associated with the surface of ripening apples possess the ability to inhibit the growth of P. expansum. However, the existing literature about their colonization in the stages before ripening is not explored in depth. This study aims to characterize the antagonistic capacity of bacterial populations from five fruit development stages of 'Royal Gala' apples. The results have shown that the density of the bacterial populations decreases throughout the ripening stages of fruit (from 1.0 × 105 to 1.1 × 101 cfu/㎠). A total of 25 bacterial morphotypes (corresponding to five genera identified by 16S RNA) were differentiated in which Bacillus stood out as a predominant genus. In the in vitro antagonism tests, 10 Bacillus strains (40%) inhibited the mycelial growth of P. expansum from 30.1% to 60.1%, while in fruit bioassays, the same strains reduced the fruit rot ranging from 12% to 66%. Moreover, the bacterial strains with antagonistic activity increased in the ripening fruit stage. B. subtilis subsp. spiziennii M24 obtained the highest antagonistic activity (66.9% of rot reduction). The matrix-assisted laser desorption ionization-time of flight mass spectrometry analysis revealed that bacteria with antagonistic activity produce anti-fungal lipopeptides from iturin and fengycin families.