• Journal of the Korean Chemical Society
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• v.57 no.2
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• pp.234-240
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• 2013

The synthesis of title compounds were accomplished by synthetic sequence shown in Scheme 1. Chalcones on cyclocondensation with thiourea in ethanol and potassium hydroxide under reflux yielded the respective dihydropyramidin-2(1H)-thiones. Each of the dihydropyrimidin thiones was, then subjected to the Mannich condensation in alkaline medium using three different secondary amines, viz., dimethylamine, diethylamine and morpholine to obtain a new series of S-Mannich bases. All the synthesised compounds ($C_1-C_{15}$) were evaluated for their antiulcer and antibacterial activities. Compounds $C_4$, $C_5$, $C_6$, $C_{14}$ and $C_{15}$ exhibited relatively more potent antiulcer activity but not comparable to the standard; Omeprazole, while $C_1$, $C_2$, $C_3$ and $C_{13}$ were moderate in activity at 100 mg/kg p.o. All the compounds ($C_1-C_{15}$) showed mild to moderate activity against both Gram-positive (S.aureus, L.delbrueckii) and Gram-negative (P.vulgaris, E.coli) bacteria. Amongst the compounds tested, only $C_6$, $C_9$, $C_{12}$ and $C_{15}$ were found to be potent.

• Proceedings of the Korean Society of Dyers and Finishers Conference
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• 2012.03a
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• pp.122-122
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• 2012

The aims of this study were to examine the efficacy of phytochemical compounds of colorants as anti-oxidant agent. The bioactive properties of natural colorants were studied by total phenolic contents, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging and anti-bacterial activity in Escherichial coli. The concentration ($IC_{50}$) of various extracts from colorants required to exert 50% reducing effect on DPPH radical were found to be 0.007-4 mg/ml. Especially, the gallnut (Schlectendalia Chinensis) displayed remarkable effect of DPPH as compared to positive control ascorbic acid. The total phenolic contents (TPC) and restraint of E coli. also analyzed. It was found that gallnut extracts effectively inhibited DPPH radical at a concentration below 0.01 mg/ml. Natural colorant extracts could be of good resources as anti-oxidant and anti-bacterial agents. The results suggest that our study may contribute to the development of natural and functional materials with potential application to reduce oxidative damage.

• YAKHAK HOEJI
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• v.53 no.6
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• pp.303-313
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• 2009

Traditionally, Cham dang-gui (Angelica gigas Nakai) is one of the most popular herbal medicines in Asian countries including Korea. A. gigas has been used as a functional food product for treatment anemia, women's health care, a sedative, an anodyne or a tonic agent. Decursin and decursinol angelate isolated from the roots of A. gigas are pyranocoumarin compounds. Recently, as the global herbal medication market is increasing, investigations about pharmacological effects of decursin and decursinol angelate are rapidly increasing. We summarized previous studies about pharmacological effects of decursin and decursinol angelate, and reviewed relation with pharmacological effects of decursin and decursinol angelate on human disorder, focused on the approach for new drug development. Pharmacological effects of decursin and decursinol angelate were classified as anti-tumor activity, anti-bacterial activity, improvements of the circulating system, inhibition of cytochrome P-450 activity, anti-inflammation activity, anti-oxidant activity and cognitive-enhancing activites. The activity of A. gigas with improvement of the circulating system may have wide therapeutic potential for circulatory diseases, including diabetes, hyperlipidemia and atherosclerosis. Also, anti-inflammation activity A. gigas may be beneficial for the treatment and prevention of asthma, atopic dermatitis and rheumatism arthritis. This relation could potentially lead to the development of herbal new drugs. In order to development a new drug containing decursin and decursinol angelate, it is also necessary to consider the safety profile, and the information in this review would contribute to development a new drug from herbal medicine.

• Journal of Microbiology and Biotechnology
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• v.28 no.5
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• pp.697-706
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• 2018

Lactobacillus pentosus K1-23 was selected from among 25 lactic acid bacterial strains owing to its high inhibitory activity against several pathogenic bacteria, including Escherichia coli, Salmonella typhimurium, S. gallinarum, Staphylococcus aureus, Pseudomonas aeruginosa, Clostridium perfringens, and Listeria monocytogenes. Additionally, among 13 strains of Aureobasidium spp., A. pullulans NRRL 58012 was shown to produce the highest amount of ${\beta}$-glucan ($15.45{\pm}0.07%$) and was selected. Next, the optimal conditions for a solid-phase mixed culture with these two different microorganisms (one bacterium and one yeast) were determined. The optimal inoculum sizes for L. pentosus and A. pullulans were 1% and 5%, respectively. The appropriate inoculation time for L. pentosus K1-23 was 3 days after the inoculation of A. pullulans to initiate fermentation. The addition of 0.5% corn steep powder and 0.1% $FeSO_4$ to the basal medium resulted in the increased production of lactic acid bacterial cells and ${\beta}$-glucan. The following optimal conditions for solid-phase mixed culture were also statistically determined by using the response surface method: $37.84^{\circ}C$, pH 5.25, moisture content of 60.82%, and culture time of 6.08 days for L. pentosus; and $24.11^{\circ}C$, pH 5.65, moisture content of 60.08%, and culture time of 5.71 days for A. pullulans. Using the predicted optimal conditions, the experimental production values of L. pentosus cells and ${\beta}$-glucan were $3.15{\pm}0.10{\times}10^8CFU/g$ and $13.41{\pm}0.04%$, respectively. This mixed culture may function as a highly efficient antibiotic substitute based on the combined action of its anti-pathogenic bacterial and immune-enhancing activities.

• IMMUNE NETWORK
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• v.3 no.1
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• pp.23-28
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• 2003

Background: Intracellular antibody specific to hepatitis B virus X protein (HBx) might be useful for studying the role of HBx in hepatocellular carcinogenesis and HBV replication. Methods: With variable region genes for H7 monoclonal anti-HBx Ab, we constructed a vector for bacterial expression of single chain Ab (scFv) and a vector for eukaryotic cell expression of it. The expression of H7 scFv and its binding activity against HBx was examined by immunoblotting and immunofluorescence microscopy. Results: H7 scFv expressed in bacterial cells retained reactivity to HBx. We demonstrated its intracytoplasmic expression in CosM6 eukaryotic cells. Conclusion: This is the first study showing the expression of intracellular anti-HBx Ab in eukaryotic cells. H7 scFv may be a good tool to study the function of HBx in HBV infection.

• International Journal of Clinical Preventive Dentistry
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• v.14 no.4
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• pp.216-221
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• 2018

Objective: In this study, we tried to investigate the antimicrobial activity of natural herbaceous plant-derived essential oils against oral disease-causing bacterial strains and establish the scientific evidences to apply them to the dentifrice, mouthwash, and other uses. Methods: We used the disk diffusion method with 23 types of 100% natural essential oils to verify the antimicrobial effect against Streptococcus mutans, Porphyromonas gingivalis, and Lactobacillus rhamnosus. After adhering to the surface of the plate culture medium, $20{\mu}l$ of the essential oil was prepared, and the diameter of the transparent ring was measured after incubation for 24 hours. All the experiments were repeated three times. Results: Among 23 types of oils, 13 were effective against all three strains: myrrh, ginger, basil, carrot seed, tea tree, patchouli, ylang ylang, cypress, lemongrass, cinnamon, peppermint, lavender, and eucalryptus. Seventeen oils were effective against S. mutans, and myrrh, basil, and carrot seed showed high antimicrobial activity. Eighteen oils were effective against P. gingivalis, and tea tree, carrot seed, and cinnamons showed high antimicrobial activity. Sixteen oils were effective against L. rhamnosus, and carrot seed and peppermint cinnamon showed high antimicrobial activity. Conclusion: Consequently, 13 essential oils showed the antimicrobial activity against three bacterial strains, which indicates these essential oils might be used as the effective materials to suppress the growth of oral-disease inducing microorganisms. Moreover, essential oils that have been analyzed activities in this study will be mixed up within the constant range and analyzed their antimicrobial effects to examine the synergistic activity among them.

• Journal of Microbiology and Biotechnology
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• v.24 no.10
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• pp.1438-1444
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• 2014

Lactic acid bacteria (LAB) are probiotics that provide numerous beneficial effects on the host body, especially on the intestine. Combining several strains of LAB, we prepared a formulation containing four different LAB and studied its anti-inflammatory activity both in vitro and in vivo. The formulation significantly reduced NO production from RAW 264.7 cells treated with bacterial lipopolysaccharide, indicating that the formulation might include anti-inflammatory activity. The formulation also suppressed inflammatory change induced by trinitrobenzene sulfonic acid (TNBS) in mice, where oral or rectal administration of the formulation protected the colon tissue from the damage by TNBS. Expressions of the IL-6 and FasL genes appeared to be down-regulated by the formulation in TNBS-treated colon tissues, suggesting that the suppression of those genes may be involved in the anti-inflammatory activity of the formulation.

• Natural Product Sciences
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• v.29 no.2
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• pp.59-66
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• 2023

The anti-melanogenic activity of 259 actinomycete strains was tested, and based on the results for the inhibition of mushroom tyrosinase activity and the reduction in melanin content, Micromonospora sp. JCS1 and JCS7 were selected as the strains with the highest anti-melanogenic potential. The activity-guided fractionation of extracts from JCS1 and JCS7 led to the isolation of the dipeptides cyclo(ʟ-Phenyl alanine (Phe)-ʟ-Proline (Pro)) (1) and cyclo(ʟ-Tryptophan (Trp)-ʟ-Proline (Pro)) (2). These two compounds were tested for their inhibition of mushroom tyrosinase by monitoring ʟ-DOPA levels and melanin production. Cyclo(ʟ-Phe-ʟ-Pro) (1) and cyclo(ʟ-Trp-ʟ-Pro) (2) were thus confirmed to have the potential for use in functional whitening cosmetics containing actinomycete-derived secondary metabolites.

• Korean Journal of Plant Resources
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• v.32 no.6
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• pp.669-676
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• 2019

Zanthoxylum piperitum D.C. (ZP) peels has been used as a natural spice and herb medicine for hypertension reduction, for strokes, and for its anti-bacterial and anti-oxidant activity. However, the anti-inflammatory mechanisms employed by ZP have yet to be completely understood. In this study, we elucidate the anti-inflammatory mechanism of ZP in lipopolysaccharide (LPS)-induced RAW264.7 cells. We evaluated the effects of ZP in LPS-induced levels of inflammatory cytokines, prostaglandin E₂ (PGE₂), and caspase-1 using ELISA. The expression levels of inflammatory-related genes, including cyclooxygenase (COX)-2 and inducible nitric oxide synthase (iNOS), were assayed by Western blot analysis. We elucidated the effect of ZP on nuclear factor (NF)-κB activation by means of a luciferase activity assay. The findings of this study demonstrated that ZP inhibited the production of inflammatory cytokine and PGE₂ and inhibited the increased levels of COX-2 and iNOS caused by LPS. Additionally, we showed that the anti-inflammatory effect of ZP arises by suppressing the activation of NF-κB and caspase-1 in LPS- induced RAW264.7 cells. These results provide novel insights into the pharmacological actions of ZP as a potential candidate for development of new drugs to treat inflammatory diseases.

• Journal of Korean society of Dental Hygiene
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• v.18 no.4
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• pp.423-432
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• 2018

Objectives: Calcium hydroxide, a root canal temporary sealer, has long been used and it has anti-bacterial and anti-inflammatory activity. To investigate the properties of a newly developed calcium hydroxide paste comprising silicon-substituted hydroxyapatite (Si-HA), we examined the anti-inflammatory activity of the new calcium hydroxide paste in RAW 264.7 macrophages stimulated by lipopolysaccharide (LPS), which causes infection of the root canal. Methods: The test materials, including Calcipex II as control group and the newly developed TRC paste, were extracted from cell culture media and then diluted for experiment. In LPS-stimulated RAW 264.7 cells, the cytotoxicity and nitric oxide (NO) production of test materials were measured by MTT assay and Griess reagents, respectively. Also, the expression of the inducible nitric oxide synthase (iNOS) was assessed by western blotting. Results: The IC50 values of Calcipex II and TRC paste were $17.6mg/m{\ell}$ and $13.5mg/m{\ell}$, respectively. The level of NO, increased by LPS, was dose-dependently inhibited more by TRC paste than Calcipex II treatment. In addition, iNOS expression was decreased by 71% and 92% at concentrations of $2mg/m{\ell}$ and $20mg/m{\ell}$ of TRC paste, respectively. Conclusions: We demonstrated that the Si-HA calcium hydroxide paste has a slightly improved anti-inflammatory property and further studies are needed before clinical recommendations are proposed.