• Molecular & Cellular Toxicology
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• v.1 no.3
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• pp.179-188
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• 2005

To develop the novel anti-allergic drug, many sophoricoside derivatives were synthesized. Among these derivatives, JSH-II-3, VI-3, VII-3, VIII-3, VII-20 and VII-20 (sodium salt) were selected and subjected to high throughput toxicity screening (HTTS) because they revealed strong IL-5 inhibitory activity and limitation of quantity. Single cell gel electrophoresis (Comet) assay, mouse lymphoma thymidine kinase ($tk^{+/-}$) gene assay (MOLY), chromosomal aberration assay in mammalian cells and Ames reverse mutation assay in bacterial system were used as simplified, inexpensive, short-term in vitro screening tests in our laboratory. Through the primary screening using the comet assay, we could choose the first candidates of sophoricoside derivatives with no genotoxic potentials as JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt). Also JSH-VII-3, VII-20 and VII-20 (sodium salt) are non-mutagenic in MOLY assay, while JSH-II-3 is mutagenic at high concentration with the presence of metabolic activation system in both comet assay and MOLY assay. The selected derivatives (JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt) are not mutagenic in S. typhimurium TA98 and TA100 strains both in the presence and absence of metabolic activation. From results of chromosomal aberration assay, 6 h treatment of JSH-VI-3, VII-3 and VII-20 (sodium salt) were not revealed clastogenicity both in the presence and absence of S-9 mixture. Therefore, we suggests that JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt), as the optimal candidates with both no genotoxic potential and IL-5 inhibitory effects must be chosen. To process the development into new anti-inflammatory drug of these derivatives, further investigation will need.

• Journal of the Korean Crystal Growth and Crystal Technology
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• v.25 no.5
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• pp.212-217
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• 2015

Ships and marine structures have a lot of problems in their high maintenance and operating cost by biofouling. A biofouling occurrs by the adhesion of marine microorganism, algae and bacteria. In this study, the aim is to prevent or to reduce the biofouling phenomena through silver nano-particle coating on artificial light-weight aggregates and geopolymer. The antibacterial activity on them is tested according to ASTM E2149-2013a. The test results showed, it is estimated that silver nano-particles removed 99.99 % of bacteria. Specimens were set up in the sea side of field test area in Korea Institute of Ocean Science and Technology (KIOST) and have been observed for five months. The anti-biofouling effect and difference in weight change rate have been detected two months later after the installation. Because silver nanoparticles inhibit bacterial growth and kill the cells by destroying bacterial membranes, silver nano-particle coating on artificial lightweight aggregates is a well-suited and eco-friendly method for preventing biofouling in the sea up to 5 months.

• Journal of Veterinary Science
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• v.24 no.2
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• pp.20.1-20.13
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• 2023

Background: As Actinobacillus pleuropneumonniae (APP) infection causes considerable losses in the pig industry, there is a growing need to develop effective therapeutic interventions that leverage host immune defense mechanisms to combat these pathogens. Objectives: To demonstrate the role of microRNA (miR)-127 in controlling bacterial infection against APP. Moreover, to investigate a signaling pathway in macrophages that controls the production of anti-microbial peptides. Methods: Firstly, we evaluated the effect of miR-127 on APP-infected pigs by cell count/enzyme-linked immunosorbent assay (ELISA). Then the impact of miR-127 on immune cells was detected. The cytokines tumor necrosis factor (TNF)-α and interleukin (IL)-6 were evaluated by ELISA. The expression of cytokines (anti-microbial peptides [AMPs]) was assessed using quantitative polymerase chain reaction. The expression level of IL-6, TNF-α and p-P65 were analyzed by western blot. The expression of p65 in the immune cells was investigated by immunofluorescence. Results: miR-127 showed a protective effect on APP-infected macrophage. Moreover, the protective effect might depend on its regulation of macrophage bactericidal activity and the generation of IL-22, IL-17 and AMPs by targeting sphingosine-1-phosphate receptor3 (SIPR3), the element involved in the Toll-like receptor (TLR) cascades. Conclusions: Together, we identify that miR-127 is a regulator of S1PR3 and then regulates TLR/nuclear factor-κB signaling in macrophages with anti-bacterial acticity, and it might be a potential target for treating inflammatory diseases caused by APP.

• Journal of Pharmaceutical Investigation
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• v.36 no.6
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• pp.371-375
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• 2006

Neomycin coupled to a polymer matrix via a metal linker was prepared and evaluated for prolonging antibacterial activity. Microcrystallized cellulose was chemically modified to cellulose xanthate(MCX) to afford metal binding sites. MCX was treated with Cu(II), Fe(III) or Zn(II) followed by reaction with neomycin (Ne). The release of Ne from MCX-Zn(II)-Ne was investigated and its activity duration was measured by ditch plate method. The amount of metal bound to MCX was 0.36 mmol/g matrix, 0.26 mmol/g matrix and 0.56 mmol/g matrix for Cu(II), Zn(II) and Fe(III), respectively. Ne bound to MCX-metal chelates was 0.006 mmol, 0.07 mmol and 0.01 mmol per g MCX for Cu(II), Zn(II) and Fe(III), respectively. The Ne release from MCX-Zn(II)-Ne was sustained even after seven washes, whereas Ne from MC/Zn(II)/Ne mixture was almost completely released in two washes. Antibacterial activity was prolonged with MCX-Zn(II)-Ne and MCX-Fe(III)-Ne, but not with MCX-Cu(II)-Ne when compared with that of free Ne. Taken together, these results suggest that neomycin coupled to MCX via a proper metal linker has a potential as a polymeric antibacterial agent with sustained activity.

• Biomedical Science Letters
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• v.29 no.3
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• pp.130-136
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• 2023

In this study, the anti-bacterial activity of three medicinal herbs such as Dioscorea batatas, Morus alba, and Tagetes erecta, have been applied in oriental medicine against Escherichia coli and Staphylococcus aureus. The antibacterial activity of Dioscorea batatas ethanol extract (DBEE), Morus alba ethanol extract (MAEE), and Tagetes erecta ethanol extract (TEEE) was analyzed by disk diffusion, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) assays. As a result, three medicinal herbs exhibited antibacterial activity in a dose-dependent manner as well as MAEE and TEEE showed the most potent antibacterial activity followed by disk diffusion assay against E. coli and S. aureus, respectively. MIC against E. coli and S. aureus was 1.6 mg/mL of MAEE and TEEE as well as 0.2 mg/mL of TEEE. MBC against both strains was 5 mg/mL of DBEE and 2.5 mg/mL of TEEE. Consequently, three medicinal herbs in this study showed potent antibacterial activity through the inhibited growth of E. coli and S. aureus, which is considered as a potential candidate for cosmeceutic agents to attenuate the pruritus. In addition, antibacterial and antihistamine effects followed by the extraction solvents should be analyzed in future studies.

• Microbiology and Biotechnology Letters
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• v.49 no.4
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• pp.543-551
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• 2021

Nocardiopsis species produce bioactive compounds, such as antimicrobial and anti-cancer agents and toxins. However, no reports have described their anti-inflammatory and anti-fibrotic effects during nasal polyp (NP) formation. In this study, we investigated whether marine-derived bacterial Nocardiopsis sp. 13G027 exerts anti-inflammatory and anti-fibrotic effects on lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages and transforming growth factor (TGF)-β1-induced NP-derived fibroblasts (NPDFs). Nitric oxide (NO) and prostaglandin E₂ (PGE₂) levels were analyzed. Extract from Nocardiopsis sp. 13G027 significantly inhibited the upregulation of NO and PGE₂ in LPS-activated RAW 264.7 macrophages. The expression of mitogen-activated protein kinases (MAPKs) and protein kinase B (Akt/PKB) in LPS-induced RAW 264.7 macrophages was evaluated; smooth muscle alpha-actin (α-SMA), collagen type I (Col-1), and fibronectin also phosphorylated small mothers against decapentaplegic (SMAD) 2 and 3 in TGF-β1-stimulated NPDFs. The Nocardiopsis sp. 13G027 extract suppressed the phosphorylation of MAPKs and Akt and the DNA-binding activity of activator protein 1 (AP-1). The expression of pro-fibrotic components such as α-SMA, Col-1, fibronectin, and SMAD2/3 was inhibited in TGF-β1-exposed NPDFs. These findings suggest that Nocardiopsis sp. 13G027 has the potential to treat inflammatory disorders, such as NP formation.

• KSBB Journal
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• v.24 no.4
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• pp.347-352
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• 2009

Ethanol extract (1.0 wt%) of Scutellaria baicalensis $G_{EORGE}$ practically satisfied CTFA (The cosmetics, Toiletry, and Fragrance Association) standard in its antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans which were inoculated in skin toner and skin lotion. At concentrations of the extract less than 1.0 wt% the survival rate was the best for S. aureus and the worst for P. aeruginosa. The antimicrobial effect seems to be due to the damage to the bacterial cell wall as evidenced by the images of a Field Emission-Scanning Electron Microscope. The extract also showed a high anti-oxidant effect, and superoxide dismutase (SOD)-like activity reached 80% at 1,000 ppm. These findings suggest that the extract of Scutellaria baicalensis $G_{EORGE}$ is applicable to cosmetics as a natural preservative and an anti-oxidant.

• YAKHAK HOEJI
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• v.50 no.6
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• pp.345-350
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• 2006

The pharmacological properties of ginseng are mainly attributed to ginsenosides, the active constituents that are found in the extracts of different species of ginseng. Lately; the studies on ginsenosides are mainly focused on IH-901, a major intestinal bacterial metabolite of ginsenosides. In this study; we examined the anti-diabetic activity of IH-901 in C57BU61 db/db mice model. IH-901 was administrated orally at a dose of 20 mg/kg for 5 weeks. During the experimental period, body weight and blood glucose levels were measured every week. After 5 weeks, db/db mice were sacrificed and diabetic parameters were analyzed. IH-901 treated group showed a significant decrease in fasting blood glucose levels (from 10.5 mM to 9.4 mM), insulin resistance index (from 163.6 to 100.2) and triglyceride levels (from 115.3 to 70.1) compared to the diabetic control. In Pancreatic islets morphology; IH-901 treated group revealed much less infltrated mononuclear cells, indicating that IH-901 recovered ${\beta}$-cell damage due to hyperglycemia. In addition, IH-901 upregulated expressions of glucose transporter 4 (GLUT4) and PPAR-${\gamma}$ in skeletal muscle and adipose tissue, respectively. Taken together IH-901might be a potential anti-hyperglycemic agent with insulin sensitizing effect.

• Molecules and Cells
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• v.42 no.11
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• pp.755-762
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• 2019

Despite decades of research into colorectal cancer (CRC), there is an ongoing need for treatments that are more effective and safer than those currently available. Lactic acid bacteria (LAB) show beneficial effects in the context of several diseases, including CRC, and are generally regarded as safe. Here, we isolated a Lactobacillus rhamnosus (LR)-derived therapeutic protein, p8, which suppressed CRC proliferation. We found that p8 translocated specifically to the cytosol of DLD-1 cells. Moreover, p8 down-regulated expression of Cyclin B1 and Cdk1, both of which are required for cell cycle progression. We confirmed that p8 exerted strong anti-proliferative activity in a mouse CRC xenograft model. Intraperitoneal injection of recombinant p8 (r-p8) led to a significant reduction (up to 59%) in tumor mass when compared with controls. In recent years, bacterial drug delivery systems (DDSs) have proven to be effective therapeutic agents for acute colitis. Therefore, we aimed to use such systems, particularly LAB, to generate the valuable therapeutic proteins to treat CRC. To this end, we developed a gene expression cassette capable of inducing secretion of large amounts of p8 protein from Pediococcus pentosaceus SL4 (PP). We then confirmed that this protein (PP-p8) exerted anti-proliferative activity in a mouse CRC xenograft model. Oral administration of PP-p8 DDS led to a marked reduction in tumor mass (up to 64%) compared with controls. The PP-p8 DDS using LAB described herein has advantages over other therapeutics; these advantages include improved safety (the protein is a probiotic), cost-free purification, and specific targeting of CRC cells.

• Microbiology and Biotechnology Letters
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• v.36 no.1
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• pp.82-85
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• 2008

Hyungbangjihwang-Tang (HT), an Oriental herbal formula, has been known to play a role which helps to recover vigor of human in the Orient. In this study, antibacterial substance (HTI) was purified from the ethyl-acetate extracts of HT by using $SiO_2$ column chromatography and HPLC, and the antibacterial effects of HTI were investigated. By using the CLSI broth micro-dilution assay, the activity of HTI was evaluated against human pathogenic Gram-positive and Gram-negative bacterial strains including the clinical isolates of methicillin-resistant Staphylococcus aureus. The results demonstrated that HTI showed broad spectrum antibacterial activities against all bacterial strains tested. In conclusion, HTI is an interesting new molecule for its potential in anti-infective drug discovery and for future studies on activity-structure relationship through analysis of its chemical structure.