• The Korean Journal of Pharmacology
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• v.29 no.2
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• pp.245-252
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• 1993

Amiloride is a potassium sparing duretic which specifically inhibits $Na{^+}$ channels. In the present study, we investigated the possible interaction of amiloride with $A_1$ adenosine receptors-adenylyl cyclase system in crude adipocytic plasma membrane fractions prepared from Sprague-Dawley rats. When the function of $G_i$ protein (inhibitory guanine nucleotide binding protein) was assessed by determining the effects of GTP on isoproterenol-stimulated adenylyl cyclase activity, the inhibitory effect of high concentrations of GTP was not observed in the presence of amiloride. In contrast, the adenosine receptor-mediated inhibition of the enzyme activity, as determined empolying 2-chloroadenosine, was either unchanged or even more enhanced by amiloride depending on the concentrations of 2-chloroadenosine. Thus, it appears that GTP- and receptor-mediated inhibitory function of $G_{i}$ proteins can be separated from one another. Receptor-mediated function of $G_{s}$ protein did not appear to be significantly affected by amiloride, since the inhibition of isoproterenol-stimulated adenylyl cyclase activity by propranolol under the same conditions was not significantly altered by amiloride. The enhancement of 2-chloroadenosine-mediated inhibition of adenylyl cyclase by amiloride was maintained in the presence of 150 mM NaCl. In summary, these results suggest that amiloride interacts both with $A_{l}$ adenosine receptors and with $G_i$ proteins in adipocytic membranes. Its binding to the $A_1$ adenosine receptors appears to facilitate the coupling of the receptors with $G_i$ proteins thereby enhancing the inhibition of isoproterenol-stimulated adenylyl cyclase activity by $A_1$ adenosine agonist, and the direct interaction with $G_i$ proteins appears to remove the GTP-dependent inhibitory effect on adenylyl cyclase activity.

• Korean Journal of Microbiology
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• v.37 no.2
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• pp.151-157
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• 2001

This study was conducted to select lactic acid bacteria which possess potential inhibitory effect on Helicobacter pylori, and to make feasibility test of fermented milk products using them. In order to select lactic acid bacteria specifically inhibiting the growth of H. pylori, antibacterial activity using paper disk method, adherence ability to Caco-2 cell inhibitory effect on urease activity of H. pylori, and milk fermentation feasibility were measured. Among 45 strains of lactic acid bacteria tested, 28 strains showed clear zone and Lactobacillus gasseri MK-03 showed the largest clear zone. Caco-2 cell adherence by lactic acid bacteria and inhibitory effect of them on H. pylori adherence were also evaluated. Of 28 strains tested, 18 strains appeared to be effective on adherence to Caco-2 cell, and especially Bifidobacterium longum MK-26 was found to be superior to others. When Bif. longum MK-26 and H. pylori were reacted with Caco-2 cell 2hrs before, adherence percentage of H. pylori decreased from 0.105% to 0.004%. To investigate inhibitory effect of lactic acid bacteria-derived supernatant on urease activity of H. pylori, pH-adjusted fermented supernatant(pH-4.4) was assessed by co-cultivation method. There of Lb. acidophilus MK-07-derived supernatant showed the most inhibitory effect on urease activity of H. pylori. Considering milk fermentation ability of selected 3 strains, they were comparably feasible to fermented milk products. Consequently, Lb. gasseri MK-03, Lb. acidophilus MK-07, and Bif. longum MK-26 were selected to specifically inhibit the growth of H. pylori, by antibacterial activity, inhibition of urease activity, and inhibition of Caco-2 cell adherence, respectively.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.23 no.3
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• pp.115-121
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• 1997

To identify inhibitors of melanogenesis, we compared the effects of 5 compounds on mushroom tyrosinase, human melanocytic tyrosinase activity and melanin content. The cytotoxicyty of the components were also tested on cultured human melanoctes. Kojic acid showed marked inhibitory effect both on mushroom and human tyrosinase activity. This action of kijic acid is stronger than that of ascorbic acid. Arbutin inhibited human tyrosinase activity of cultured melanocytes although it had slightly inhibitory effect on mushroom tyrosinase activity. Azelaic acid had no effect on human tyrosinase activity. Melanin production was inhibited significantly by kojic acid and tranexamic acid. MTT assay showed that all of the compounds were non-cytotoxic to melanocytes at the concentrations tested. These results suggest that the effect of kojic acid on cultured meanocytes involve inhibition of tyrosinase activity and melanogenesis without affection the cell number.

• The Korean Journal of Physiology
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• v.10 no.2
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• pp.1-10
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• 1976

The action of acetylcholine on the sodium plus potassium activated ATPase activity in the rabbit red cell membrane has been investigated and the experiments were also designed to determine the mechanism of action of acetylcholine on the ATPase activity. The following results were observed. 1. The activity of the NaK ATPase from red cell membrane is inhibited by acetylcholine. 2. The ratio of inhibition of NaK ATPase by acetylcholine is decreased by raising the potassium concentration, and is increased by raising the sodium concentration. 3. The ATPase activity is increased by small amounts of calcium but inhibited by larger amounts. The ratio of inhibition of the enzyme by acetylcholine is increased by raising the calcium concentration. 4. The inhibitory action of acetylcholine on the NaK ATPase activity was not related to the sulfhydryl group of cysteine, the hydroxyl group of threonine, or the carboxyl group of aspartic acid. 5. The inhibitory action of acetylcholine on the ATPase activity is due to amino group of the enzyme of NaK ATPase.

• Journal of Environmental Health Sciences
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• v.21 no.1
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• pp.74-77
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• 1995

The insecticidal and antibacterial activity of new synthesized carbamate derivatives(8-Hydroxy-5-chloroquinolyl-N-methylcarbamate(I), 8-Hydroxy-5-chloroquinolyl-N-ethylcarbamate(II)) was examined using 0.2 w/v% acetone solutiolas and 50 r/ml~1000 r/m N,N'-dimethylformamide-$H_2O$(2:3) solutions of each compounds, respectively. 1) Two carbamates exerted insecticidal effects on Sogata furcifera HORVATH, Delphacodes Striatella FAUEN, Whereas no significant effects were observed on the Nilaparvate lugens STAL, Inazuma dorasails MOISCHIULSKY and Nephateffix apicalis Cincticeps UHLER. 2) These compounds exhibited growth-inhibitory activity against Staphylococcus aureus, Salmonella paratyphi A, Shigella dysenteriae 1a, Escherichia coli NL 1401,at the concentration range of 100~500 r/ml in general.

• The Korean Journal of Food And Nutrition
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• v.34 no.2
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• pp.181-186
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• 2021

Antioxidant properties and antioxidant activities were analyzed for water extracts and 50% and 70% ethanol extracts of the leaf of Angelica gigas Nakai. The polyphenol and flavonoid contents in water, 50%, and 70% ethanol extract of the leaf of Angelica gigas Nakai, it was found that the polyphenol contents were 18.75 mg GAE/g, 28.95 mg GAE/g, and 34.73 mg GAE/g, respectively, and flavonoid contents were respectively. The DPPH IC50 scavenging activity was 45.84 mg/mL, 36.44 mg/mL, 19.11 mg/mL, respectively, and theABTS+ radical scavenging ability (1 mg/mL) was 28.73%, 22.79%, and 12.70%, respectively. Tyrosinase inhibitory activity, 70% ethanol extract, 50% ethanol extract, and water extract 33.14%, and 4.53%, respectively. Nitrite scavenging activity, 70% ethanol extract, 50% ethanol extract, and water extract were in the order of 1 mg/mL scavenging activity, 36.43%, 34.80%, and 18.85%, respectively.

• Journal of Dairy Science and Biotechnology
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• v.22 no.2
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• pp.99-106
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• 2004

Tumor cell proliferation inhibitory, antioxidative activities and glutathione content were analyzed in a variety of spore forming lactic acid bacteria. Tumor cell proliferation inhibitory activity varied widely depending upon the strains of spore forming lactic acid bacteria and the types of carcinoma cell lines(0${\simn}$56.7%), Bacillus coagulans KTCC3625 has shown a marked antipro-liferative effect against the carcinoma cells and NCL-H1299 human lymphoma cell line tended to be least affected by the spore forming lactic acid bacterial cell extracts. Antioxidative activity analyzed in the lipid peroxidation occurred in all the test strains varied on the strains(5.0 to 52.0%) an extensively high degree of antioxidative activity was demonstrated by three strains of Bacillus coagulans KTCC3625, Bacillus coagulans KTCC1015 and Lactobacillus sporogens CU 815. Concentrations of glutathione were highest in a strain of Lactobacillus sporogenes CU 815 followed by Sporo-lactobacillus inulinus ATCC13538 (5.34 to 8.19 mol/g). Spearmans' rank correlation quotient between cellular GSH levels and linoleic acid peroxidation inhibitory effects of the spore forming lactic acid bacteria revealed highly significant correlation quotient of 0.78. Spearmans' rank correlation quotient between the Caski human cervix carcinoma cell proliferation inhibitory activity and the linoleic acid peroxidation inhibitory effects of the spore forming lactic acid bacteria and that between Caski carcinoma cell proliferation inhibitory activity and the cellular GSH levels were shown to be 0.29 and 0.32,respectively, which means an insignificant positive correlation however.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.44 no.1
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• pp.8-17
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• 2011

To identify and examine the distribution of proteolytic inhibitory activity in crude extracts from fish eggs, and to determine the applicability of these protease inhibitors as anti-degradation agents in surimi-based products and fish meat, we compared the inhibitory activities of various extracts from fish eggs to those of commercial proteases, such as trypsin and papain. We used the optimal conditions for the screening of trypsin activity: 30 ug/uL of 0.1% trypsin and 0.6 mM Na-benzoyl-L-arginine-p-nitroanilide (BAPNA) with a pH of 8.0 at $40^{\circ}C$ for 60 min. The activities of papain and four commercial proteases were investigated after mixing with 100 ug/uL enzymes and 0.3% casein with a pH of 8.0 at $40^{\circ}C$ for 60 min. We performed a screening assay to detect the inhibitory activity (%) of crude extracts from eight species of fish eggs against the target proteases trypsin and papain. The assay revealed a wide distribution of trypsin and papain inhibitors in fish eggs. The specific inhibitory activities (11.6.28.6 U/mg) of crude extracts from fish eggs against trypsin and BAPNA substrate were higher than that (0.64 U/mg) of egg whites, used as a commercial inhibitor. The inhibitory activities of crude extracts from fish eggs against trypsin, and of egg whites against casein substrate (1.94.4.51 U/mg), were higher than those of papain (0.24.1.57 U/mg) and commercial protease (0.04.0.32 U/mg). The extracts from fish eggs were rich in protease inhibitors that exhibited strong inhibitory activity against trypsin, a serine protease, and papain, a cysteine protease.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2018.10a
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• pp.116-116
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• 2018

Bioconversion, the enzymatic process by microorganism on organic precursor to desired products. The natural extract is converted into a form that can be easily absorbed into the skin, while scaling up of to higher quantity is possible. Selection of naturally processed raw material rather than chemically processed is preferred. Therefore, fermentation was carried out by mixing Rubus coreanus Miquel, soybean, Zanthoxylum schinifolium as bioconverting materials, the possibility of inflammation, whitening material were checked. In this study, useful microorganisms were isolated from various salted fish, and 16S rDNA sequence was analyzed to confirm their genetic characteristics. Combining the three natural materials using bioconversion technology to study their activity before and after fermentation. To evaluate the antioxidant activity and the active ingredient content the DPPH radical scavenging activity and the total polyphenol content were examined. Raw 264.7 cells were used to evaluate MTT assay, NO and $TNF-{\alpha}$ production inhibitory activity. Also, to evaluate the whitening activity, tyrosinase inhibitory activity and melanin formation inhibitory activity were measured using B16F10 cells. In total 34 strains were obtained from various salted fish. The effective strains useful for the bioconversion process, showed that DPPH radical scavenging ability and polyphenol content were increased in the two kinds of microbial treatment groups compared to the untreated group. 16S rDNA sequencing analysis of the strains showed excellent in Pediococcus pentosaceus B1 in comparison. An increase of up-to 156% in anti-oxidative activity and 141% in polyphenol content was observed after bioconversion. In addition, after mixed fermentation the toxidty of Raw 264.7 and B16F10 cells tended to decrease and a significant increase was observed in anti-inflammatory activity as well. Also, tyrosinase activity and melanin significantly. synthesis decreased significantly.

• Korean Journal of Food Science and Technology
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• v.29 no.2
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• pp.194-197
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• 1997

Dopamine ${\beta}-hydroxylase\;(DBH)$ catalyses the enzymatic reaction of dopamine to norepinephrine. For the purpose of screening DBH inhibitory activity from edible mushrooms, Ganoderma lucidum, Agaricus bisporus and Lentinus edodes were examined by tracing inhibitory activities against bovine adrenal DBH, utilizing tyramine as a substrate. Among the three edible mushrooms tested, Ganoderma lucidum showed potent enzyme inhibitory activilies above 100% against DBH in chloroform fraction. Lentinus edodes and Agaricus bisporus showed inhibitory activities in ethylacetate fraction on 79.7% and 64.7%, respectively. Each solvent fraction of these mushrooms were assessed in the aspects of their inhibitory activities against DBH, and their $IC_{50}$ values were calculated. $IC_{50}$ value of chloroform fraction of Ganoderma lucidum was $1.60{\times}10^{-4}\;g$, and those of ethylacetate fractions of Agaricus bisporus and Lentinus edodes were $5.50{\times}10^{-4}\;g\;and\;2.35{\times}10^{-4}\;g$, respectively.