• The Korean Journal of Physiology and Pharmacology
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• v.18 no.1
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• pp.33-39
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• 2014

Shepherd's purse, Capsella bursa-pastoris (L.) Medik., has been considered a health food for centuries in Asia and is known to contain the isothiocyanate compound sulforaphane. In this study, we evaluated the anti-inflammatory and antibacterial properties of a sulforaphane-containing solution (SCS) isolated from shepherd's purse. SCS had significant anti-inflammatory activity indicated by the decreased levels of nitric oxide (NO), cytokines (interleukin $1{\beta}$ [IL-$1{\beta}$], IL-6, and IL-10), and prostaglandin $E_2$ ($PGE_2$) in lipopolysaccharide-stimulated RAW 264.7 murine macrophages. In addition, SCS decreased the inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) levels, which confirmed the anti- inflammatory activity of SCS. Further, SCS inhibited vancomycin-resistant enterococci (VRE) and Bacillus anthracis. The minimal inhibitory concentration was $250{\mu}g/ml$ for VRE and $1,000{\mu}g/ml$ for B. anthracis. Taken together, these data indicate that SCS has potential anti-inflammatory and anti-superbacterial properties, and thus it can be used as a functional food or pharmaceutical.

• Archives of Pharmacal Research
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• v.20 no.4
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• pp.358-362
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• 1997

Metabolite identification and urinary and biliary excretion of the new fluoroquinolone antibacterial agent DW116 [1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1 -piperazinyl)-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid, hydrochloride] after oral administration have been studied in Sprague-Dawley rats. The excretion kinetics were monoexponential. Most of the drug was eliminated via the hepatic and renal routes. Mean renal clearance of DW116 was 73.4 ml/hr/kg and mean biliary clearance was 83.8 ml/hr/kg. The major metabolite excreted in the bile was identified as the glucuronide ester of the parent drug using base-hydrolysis of the conjugate metabolite followed by co-HPLC with standard compound, $^{19}$ F-NMR and LC-MS methods. The glucuronide conjugate was also found in urine. The mean urinary recoveries of free and total (free plus glucuronide ester) DW116 were $28.6{\pm}2.7% $and $36.4{\pm}1.8%$ of the administered dose and the corresponding biliary recoveries were $14.4{\pm} 5.5%$ and $37.0{\pm}7.6%$, respectively.

• Journal of Oral Medicine and Pain
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• v.33 no.2
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• pp.105-110
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• 2008

Baicalin is a flavonoid compound isolated from the medicinal plant Scutellaria baicalensis. It is known to affect multiple biological functions, including of antibacterial, anti-viral, anti-inflammatory and analgesic effects. Baicalin can inhibit nuclear factor-kappaB activation. It has been reported that some flavonoids possess the effects of bone metabolism. The present study was undertaken to determine the possible cellular mechanism of action of baicalin in osteoblasts. The effects on the osteoblast were determined by measuring cell proliferation, cell viability, alkaline phosphatase activity, and osteoprotegerin secretion. Baicalin has no effect on the osteoblastic cell proliferation and cell viability. Baicalin treatment showed increase in alkaline phosphatase activity and osteoprotegerin secretion of osteoblasts. Thus, baicalin may be a regulatory protein within the bone.

• Bulletin of the Korean Chemical Society
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• v.32 no.9
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• pp.3219-3222
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• 2011

Three types of ${\beta}$-ketoacyl acyl carrier protein synthase (KAS) are important for overcoming the bacterial resistance problem. Recently, we reported the discovery of a antimicrobial flavonoid, YKAF01 (3,6-dihydroxyflavone), which exhibits antibacterial activity against Gram-positive bacteria through inhibition of ${\beta}$-ketoacyl acyl carrier protein synthase III (KAS III). In this report, we suggested that YKAF01 can be an inhibitor ${\beta}$-ketoacyl acyl carrier protein synthase I (KAS I) with dual inhibitory activity for KAS I as well as KAS III. KAS I is related to the elongation of unsaturated fatty acids in bacterial fatty acid synthesis and can be a good therapeutic target of designing novel antibiotics. We performed docking study of Escherichia coli KAS I (ecKAS I) and YKAF01, and determined their binding model. YKAF01 binds to KAS I with high binding affinity ($2.12{\times}10^6$) and exhibited an antimicrobial activity against the multidrug-resistant E. coli with minimal inhibitory concentration (MIC) value of 512 ${\mu}g$/mL. Further optimization of this compound will be carried out to improve its antimicrobial activity and membrane permeability against bacterial cell membrane.

• Fisheries and Aquatic Sciences
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• v.19 no.10
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• pp.42.1-42.10
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• 2016

The objectives of this study were to identify the histamine-forming bacteria and bacteriocin- producing lactic acid bacteria (LAB) isolated from Myeolchi-jeot according to sequence analysis of the 16S rRNA gene, to evaluate the inhibitory effects of the bacteriocin on the growth and histamine accumulation of histamine-forming bacteria, and to assess the physico-chemical properties of the bacteriocin. Based on 16S rRNA gene sequences, histamine-forming bacteria were identified as Bacillus licheniformis MCH01, Serratia marcescens MCH02, Staphylococcus xylosus MCH03, Aeromonas hydrophila MCH04, and Morganella morganii MCH05. The five LAB strains identified as Pediococcus acidilactici MCL11, Leuconostoc mesenteroides MCL12, Enterococcus faecium MCL13, Lactobacillus sakei MCL14, and Lactobacillus acidophilus MCL15 were found to produce an antibacterial compound with inhibitory activity against the tested histamine-producing bacteria. The inhibitory activity of these bacteriocins obtained from the five LAB remained stable after incubation at pH 4.0-8.0 and heating for 10 min at $80^{\circ}C$; however, the bacteriocin activity was destroyed after treatment with papain, pepsin, proteinase K, ${\alpha}$-chymotrypsin, or trypsin. Meanwhile, these bacteriocins produced by the tested LAB strains also exhibited histamine-degradation ability. Therefore, these antimicrobial substances may play a role in inhibiting histamine formation in the fermented fish products and preventing seafood-related food-borne disease caused by bacterially generated histamine.

• International Journal of Oral Biology
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• v.33 no.4
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• pp.213-216
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• 2008

Continentalic acid (CA, (-)-pimara-8(14), 15-diene-19-oic acid) was isolated from the roots of Aralia cordata (Araliaceae) using bioassay-guided fractionation of a crude chloroform extract. The antibacterial activity of CA against Enterococcus faecalis and Enterococcus gallinarium was estimated by determining minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs). CA exhibited potent activity against standard vancomycin-resistant enterococci (VRE) and vancomycin-susceptible enterococci (VSE), with MICs and MBCs values between 4 and $8{\mu}g/mL$ and 4 and $16{\mu}g/mL$, respectively. This compound exhibited potent activity against strains of VRE, which are highly resistant to clinically useful antibiotics. These findings suggest that continentalic acid may be useful in controlling enterococcal infection.

• Food Science and Biotechnology
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• v.14 no.5
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• pp.685-688
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• 2005

Antibacterial and antiplatelet activities of Acorus gramineus rhizome-derived asaronaldehyde and asaron were analyzed using platelet aggregometer and six human intestinal bacteria. Active constituent of A. gramineus rhizome was isolated and characterized as asaronaldehyde by spectral analyses. At 2 and 1 mg/disk, asaronaldehyde exhibited strong inhibition of Clostridium perfringens and C. difficile without adverse effects on growth of beneficial bacteria such as Bifidobacterium bifidum, Lactobacillus acidophilus, and L. casei. Asaron also revealed moderate growth inhibition against C. perfringens and C. difficile at 2 mg/disk, no growth-inhibiting activity was observed on B. bifidum, L. acidophilus, L. casei, and E. coli. At 50% inhibitory concentration ($IC_{50}$) value, asaronaldehyde was effective in inhibiting platelet aggregation induced by collagen ($IC_{50}$, $27.6\;{\mu}M$) and arachidonic acid ($IC_{50}$, $53.7\;{\mu}M$). These results suggest asaronaldehyde may be useful as lead compound for inhibiting platelet aggregation induced by collagen and arachidonic acid.

• Korean journal of food and cookery science
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• v.30 no.5
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• pp.642-649
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• 2014

We investigated the antioxidant and physicochemical qualities as well as the sensory characteristics, and microbial safety of sunsik containing varied amounts of AF-343, which can help add moisture to the skin and relieve the symptoms of atopic dermatitis. Samples did not show significant differences in pH measurements, but the pH had a tendency to increase with tendencies as increased amounts of AF-343. The total phenolic compound contents and DPPH radical scavenging activity, indicators of biologically active ingredients such as antioxidant, anticancer and antibacterial activity, significantly increased as the amounts of AF-343 increased (p<0.05). In an acceptance test, the samples did not show significant differences, however samples with the 750 mg AF-343 received the highest scores out of all the samples in overall acceptance. All samples were confirmed as microbially safe according to the food code applied to food manufacturers. Aerobic plate counts of the control group were 1.60 log CFU/g, while those of samples with 750 mg AF-343 were 1.70 log CFU/g. E. coli. Pathogenic microorganisms tests were either negative or not detected in all samples.

• Food Science and Biotechnology
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• v.16 no.4
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• pp.537-542
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• 2007

Sophora flavescens AITON (Leguminosae) is a typical traditional Korean medical herb considered to exhibit antibacterial, anti-inflammatory, and antipyretic effects, and is also used for the treatment of skin and mucosal ulcers, sores, diarrhea, gastrointestinal hemorrhage, arrhythmia, and eczema. In this study, the compound sophoraflavanone G was isolated from the dried roots of S. flavescens by bioassay-guided fractionation. We then investigated the effects of various concentrations of sophoraflavanone G on cell viability and the induction of apoptosis in KB cells after an incubation of 24 hr. The results were determined by the following methods: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-terazolium bromide (MTT) assay, Hoechst-33258 dye staining, flow cytometry (cell cycle), and Western blotting for caspase-3 and poly (ADP-ribose) polymerase (PARP). We found sophoraflavanone G induced the apoptosis of KB cells in a dose-dependent manner that was verified by DNA fragmentation, apoptotic bodies, the sub-G1 ratio, caspase-3 activity, and cleavage of PARP. These results suggest that sophoraflavanone G has potent anti-proliferative effects on human oral epidermoid carcinoma cells, with the induction of apoptosis.

• Journal of Pharmaceutical Investigation
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• v.12 no.1
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• pp.1-11
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• 1982

Silver sulfadiazine has been introduced to replace silver nitrate in the topical treatment of extensive burns and this drug exerts a prominent antibacterial action against Pseudomonas aeruginosa. The compound is painless upon application and insufficient sulfadiazine is absorbed to cause crystalluria. The primary purpose of the study was to clarify the antimicrobial action of zinc sulfadiazine ointment in comparison with silver sulfadiazine ointment as well as the pharmaceutical properties of the zinc sulfadiazine preparations. The results are summerized as followings: 1) The optimum ratio of two substrate compounds for the synthesis of zinc sulfadiazine are 2 moles of sulfadiazine and 1 mole of zinc sulfate at pH 6.0. 2) The stability of zinc sulfadiazine ointment preparation by using polyethylene glycol base, Beeler's base or polyoxyl 40 stearate base was more stable than that of silver sulfadiazine preparations. 3) The antimicrobial action of zinc sulfadiazine exhibits a stronger antimicrobial activity than that of sulfadiazine against Staphylococcus aureus but the opposite is true against Pseudomonas aeruginosa.