• Journal of the korean academy of Pediatric Dentistry
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• v.25 no.1
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• pp.116-126
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• 1998

Numerous chemical agents have been developed to reduce the activity of cariogenic bacteria. Of these, chlorhexidine is acknowledged as the most effective. Gel and mouthrinse have been the traditional method of its application in the mouth. It has been reported that chlorhexidine varnish has prolonged inhibitory effect on the number of streptococcus mutans in saliva and plaque. Recently, chlorhexidine varnish and polyurethane sealant have been developed to promote prolonged anticariogenic effect of chlorhexidine. Products containing 10% chlorhexidine varnish and polyurethane sealant have been developed to prevent caries by reducing the number of streptococcus mutans in the oral cavity. The purpose of this study is to investigate the inhibitory effect of chlorhexidine varnish and polyurethane sealant on streptococcus mutans in the primary dentition. Children with primary dentition containing no active carious lesion were divided into two groups. To the experimental group (n=11), chlorhexidine varnish and polyurethane sealant ($Chlorzoin^{(R)}$, Knowell Therapeutic Technologies, Inc. Canada.) was applied once a week for four weeks according to the manufacturer's instruction. Only oral prophylaxis was performed on the control group(n=7). Caries activity was measured after using $Cariescreen^{(R)}$SM (Knowell Therapeutic Technologies, Inc. Canada,) to incubate streptococcus mutans before and 5, 12, 24 weeks after initial varnish application. The following results were observed.; 1. There was statistically significant decrease in the number of streptococcus mutans in the experimental group for 5 weeks(P<0.01), 12 weeks(P<0.05) after the initial application. but, by 24 weeks significant difference had disappeared. 2. As the inhibitory effect of chlorhexidine varnish and polyurethane sealant application is not everlasting, reapplication at 12-24 weeks should be needed.

• Preventive Nutrition and Food Science
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• v.10 no.4
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• pp.349-352
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• 2005

The growth inhibitory effect of wheat grain, fermented wheat grain products, red pepper powder and kochujang was examined in AGS human gastric adenocarcinoma cells. The kochujang samples were prepared by mixing red pepper powder and each fermented wheat grain products, such as first fermented wheat grain (FFWG), second fermented wheat grain (SFWG) and final fermented wheat grain (FiFWG). The methanol extract of FiFWG showed the highest growth inhibitory effects. In order to investigate the effects of fermented wheat grain products at each stage of fermentation on anticancer activity, the kochujang prepared with red pepper powder and each of FFWG, SFWG and FiFWG were fermented until reaching pH 5.1. The kochujang adjusted to pH 5.1 by fermentation increased the growth inhibitory effect; however, the kochujang prepared with FiFWG showed the highest effect. Increased fermentation time increased the growth inhibitory effect of kochujang when prepared with FiFWG. These results suggested that the anticancer effect of the kochujang on the gastric cancer cells was affected by the fermentation periods of the wheat grains. The well-fermented end products of the wheat grains seem to be one of the major components that showed anticancer activity of kochujang.

• The Journal of Korean Obstetrics and Gynecology
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• v.25 no.2
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• pp.1-11
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• 2012

Objectives: This study was conducted to evaluate the inhibitory effect of Melia Fructus extract on osteoclast differentiation. Methods: MTT-assay was performed to estimate cytotoxicity of Melia Fructus extract in BMMs stimulated with M-CSF. TRAP staining, TRAP activity and Real-time PCR were performed to know the inhibitory effect on osteoclast differentiation. Actin ring formation were analysed to observe the effect of Melia Fructus extract. Results: Melia Fructus extract decreased the number of TRAP positive cells and the expression of NFATc1 gene, c-Fos gene, TRAP and OSCAR in BMMs stimulated with RANKL. Melia Fructus extract has no cytotoxicity at the concentration used in this study. Melia Fructus extract restrained the formation of actin ring. Melia Fructus inhibited NF-${\kappa}B$ activity by inducing degradation of p-$IkB{\alpha}$. Conclusions: Melia Fructus has the inhibitory effect of osteocalst differentiation and bone resorption. Further studies are needed to treat osteoporosis by herbal medicine containing Melia Fructus.

• Journal of the Korean Society of Food Science and Nutrition
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• v.36 no.12
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• pp.1511-1516
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• 2007

To assess a potential possibility of Eucommia ulmoides (EU) as a functional food, anti-hypertensive materials of EU were isolated by silica gel column, thin layer and reverse phase column chromatographies, and then ACE (angiotensin-converting emzyme) inhibitory activities of different parts (leaf, bark, and stem) were investigated. The isolated compound, 8A, was pinoresinol-4,4'-di-O-${\beta}$-D-glucoside (below PDG) originating from Eucommial Cortex and its purity was 95.64%. Of all the samples tested, PDG in raw bark and roasted bark was the highest level at 135.13 mg% and 163.67 mg%, respectively. In ACE inhibitory activity at 10 mg/mL of EU extracts, roasted leaf, raw bark, and roasted bark were 77.56%, 75.73%, and 75.73%, respectively. ACE activities at 1 mg/mL were shown to be 91.87% for PDG, 97.06% for $Enalapril^{(R)}$, and 90.32% for $Captopril^{(R)}$.

• Journal of Microbiology and Biotechnology
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• v.31 no.7
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• pp.1022-1027
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• 2021

Three compounds were isolated from marine-derived Streptomyces sp. CNQ-031, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase (BACE-1) were evaluated. Compound 1 (5,7-dihydroxy-2-isopropyl-4H-chromen-4-one) was a potent and selective inhibitor of MAO-A, with a 50% inhibitory concentration (IC₅₀) of 2.70 µM and a selectivity index (SI) of 10.0 versus MAO-B. Compound 2 [5,7-dihydroxy-2-(1-methylpropyl)-4H-chromen-4-one] was a potent and low-selective inhibitor of MAO-B, with an IC₅₀ of 3.42 µM and an SI value of 2.02 versus MAO-A. Compound 3 (1-methoxyphenazine) did not inhibit MAO-A or MAO-B. All three compounds showed little inhibitory activity against AChE, BChE, and BACE-1. The K_i value of compound 1 for MAO-A was 0.94 ± 0.28 µM, and the K_i values of compound 2 for MAO-A and MAO-B were 3.57 ± 0.60 and 1.89 ± 0.014 µM, respectively, with competitive inhibition. The 1-methylpropyl group in compound 2 increased the MAO-B inhibitory activity compared with the isopropyl group in compound 1. Inhibition of MAO-A and MAO-B by compounds 1 and 2 was recovered by dialysis experiments. These results suggest that compounds 1 and 2 are reversible, competitive inhibitors of MAOs and can be considered potential therapies for neurological disorders such as depression and Alzheimer's disease.

• The Korea Journal of Herbology
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• v.33 no.4
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• pp.95-100
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• 2018

Objectives : Ligustri Fructus has been used since ancient times as a medicinal usages in folk medicines against antitumor purpose. Many biological active constituents have been identified from this biomass such as several terpenoids and lignans. In current study, the properties of antioxidant and anti-diabetic complications using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)($ABTS^+$) radicals scavenging, and advanced glycation end products (AGEs) inhibition assays were evaluated by different extraction methods of Ligustri Fructus. Methods : In present continuing research for development of bioactive natural ingredients, antioxidant and AGEs formation inhibitory capacities of Ligustri Fructus extracts using different organic solvents were prepared and the biological potentials were investigated using in vitro bioassays. Antioxidant properties were evaluated employing radical scavenging assays using DPPH and $ABTS^+$ radicals. In addition, the anti-diabetic complications effects of Ligustri Fructus extracts were tested via AGEs formation inhibitory assay. The total phenolic contents were determined using a spectrophotometric method. Results : All the tested extracts exhibited dose-dependent radical scavenging and AGEs formation inhibitory activities. Among the tested samples, hot water extract of Ligustri Fructus was showed the most potent activity with $IC_{50}$ value of $494.8{\pm}6.7{\mu}g/m{\ell}$ against DPPH radical scavenging assay. Also, $ABTS^+$ radical scavenging activity of hot water extract was higher than those of other extracts. In addition, AGEs formation inhibitory effects of each extacts and total phenolic contents were evaluated. Conclusions : These results suggested that Ligustri Fructus can be considered as a new effective source of natural antioxidant and anti-diabetic complications resources.

• The Korea Journal of Herbology
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• v.32 no.6
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• pp.1-7
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• 2017

Objectives : The heartwood of Sappan Lignum has been used since ancient times as an ingredient in folk medicines against anti-bacterial and anti-anemia purposes. Many bioactive constituents have been derived from this biomass such as chalcones and homoisoflavonoids. In the current investigation, the antioxidant and anti-diabetic properties using DPPH and $ABTS^+$ radicals scavenging, ${\alpha}-glucosidase$, and advanced glycation end products (AGEs) inhibition assays were evaluated by different extraction methods of Sappan Lignum. Methods : In our continuing investigation for bioactive natural ingredients, the antioxidant and ${\alpha}-glucosidase$ inhibitory properties of Sappan Lignum extracts were prepared from different extraction methods and the biological efficacies were investigated in vitro. The antioxidant properties were evaluated employing radical scavenging assays using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) ($ABTS^+$) radicals. In addition, the anti-diabetic effects of Sappan Lignum extracts were tested via ${\alpha}-glucosidase$ and AGEs formation inhibitory assay. The total phenolic contents were determined using a spectrophotometric method. Results : All the tested samples showed dose-dependent radical scavenging and ${\alpha}-glucosidase$ inhibitory activities. Among the tested extracts, the 80% methanolic extract of Sappan Lignum was showed the most potent activity with an $IC_{50}$ value of $82.3{\pm}1.7{\mu}g/m{\ell}$ against DPPH radical scavenging assay. While, $ABTS^+$ radical scavenging activity of 80% methanolic extract was higher than those of other extracts. Also, ${\alpha}-glucosidase$ inhibitory and AGEs formation effects of each extacts and total phenolic contents were evaluated. Conclusions : These results suggested that Sappan Lignum can be considered as a new effective source of natural antioxidant and anti-diabetic materials.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.34 no.2
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• pp.164-172
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• 2001

The angiotensin-I converting enzyme (ACE) inhibitors from laver hydrolysate was isolated. Among the 13 kinds of proteases, Maxazyme NNP was most effective for preparing the high ACE inhibitory compound. In extraction conditions of ACE inhibitory peptide from laver hydrolysate, ACE inhibitory activity of hydrolysate treated with diethylether for decolorization and that of $70\%$ ethanol soluble fraction among the different ethanol concentrations were higher than other preparations. Low molecular fraction less than 3,000 dalton of layer hydrolysate separated by ultrafiltration had the highest ACE inhibitory activity, for further separation of ACE inhibitory peptide from laver hydrolysate, gel filtration chromatography (Sephadex G-25), reverse-phase HPLC (ODS & Vydac C-18) and gel permeation chromatography (Superdex Peptide HR) were performed. The molecular mass of the ACE inhibitory peptide fractions of gel permeation chromatography determined by electrospray-mass spectrometer were 413.48 (S1O2V2V1P),346.86 (S1O2V2V2P) and 320.32 (S2O6V3V1P) dalton and their amino acid sequence were Val-Gln-Gly-Asn, Thr-Glu-Thr and Phe-Arg, respectively.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.795-800
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• 2002

6,7-Bis-[S-(aryl)thio]-5,8-quinolinediones 4 and 5 were synthesized by the substitution of 6,7-dichloro-5,8-quinolinediones with appropriate arylthiols. Their antifungal activity were tested in vitro for their growth inhibitory activities against pathogenic fungi in comparison with flucytosine. The antifungal activities were significantly improved by S-(aryl)thio moieties of the compounds 4 and 5. The all tested compounds 4 and 5 showed generally good activities against C. albicans and A. niger ranging from 0.8 to 25 $\mu\textrm{g}$/ml. Among them, compounds 4d-4h and 5a-5c exhibited also good activities against C. krusei and C. tropicalis. The activities of compounds 4j and 4I were comparable to those of flucytosine against all tested fungi.

• Natural Product Sciences
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• v.14 no.2
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• pp.143-146
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• 2008

Protein tyrosine phosphatase 1B (PTP1B) is emerging as a potential therapeutic target for the treatment of type-2 diabetes and obesity. To search for new types of PTP1B inhibitors, we have undertaken in vitro enzyme assay for some anthraquinones and stilbenes isolated from plants. Of the anthraquinones tested, physcion (1), 1-O-methylemodin (2), and emodin (3) showed high activities, with $IC_{50}$ values of 7.6, 7.0, and $3.8{\mu}g/mL$, respectively, while the anthraquinone glycosides, physcion-8-O-${\beta}$-D-glucopyranoside (4) and emodin-8- O-${\beta}$-D-glucopyranoside (5), were less active than their aglycones. All the stilbenens (6 - 15) slightly inhibited PTP1B activity at high concentration of $30{\mu}g/mL$. Our findings suggest that the hypoglycemic effect of anthraquinones may be associated with their PTP1B inhibitory activity.