• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.23 no.2
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• pp.69-80
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• 2010

Objective : The purpose of this study was to compare anti-Inflammation and anti-oxidation of Jeondo-San(JDS) extracted with two kinds of solvents, ethanol and water. Methods : Two kinds of JDS extractions were prepared 20, 50, $100\;{\mu}g/mg$. The Cytotoxicity was measured by MTT assay in Raw 264.7 cell. The anti-inflammation effects were measured by inhibitory efficacy on $PGE_2$, NO, TNF-$\alpha$, COX-2 and iNOS in Raw 264.7 cell. The anti-oxidation effects were measured by ROS inhibitory efficacy, intracellular GSH synthesis and DPPH Radical scavenging in HaCaT cell. Results : 1. All of JDS extraction groups had no cytotoxicity in Raw 264.7 cell. 2. All of JDS extraction groups showed significantly inhibitory effect on production of $PGE_2$. Inhibitory efficacy increased in accodance with concentration. 3. All of JDS extraction groups showed significantly inhibitory effect on production of NO. Inhibitory efficacy increased in accodance with concentration. 4. All of JDS extraction groups did not show significantly inhibitory effect on production of TNF-$\alpha$. 5. $100\;{\mu}g/ml$ JDS extracted with ethanol and $50\;{\mu}g/ml$, $100\;{\mu}g/ml$ JDS extracted with water showed inhibitory effect on iNOS expression. 6. All of JDS extraction groups showed significantly inhibitory effect on production of ROS. Inhibitory efficacy increased in accodance with concentration. Ethanol extractions were better than water extractions. 7. $100\;{\mu}g/ml$ JDS extracted with ethanol only produced GSH of $32{\pm}5.2%$. 8. All of JDS extraction groups showed significantly scavenging effect of DPPH radicals. Inhibitory efficacy increased in accodance with concentration. Ethanol extractions were better than water extractions. Conclusion : Two kinds of JDS extractions have not cytotoxicity and inhibit production of NO. JDS extracted with water was effective in anti-inflammation, JDS extracted with ethanol was effective in anti-oxidation.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.97.3-98
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• 2003

The inhibitory effects of tetrahydropapaverine on serotonin biosynthesis in serotonin-producing murine mastocytoma P815 cells were investigated. Tetrahydropapaverine at concentration ranges of 5-20 M decreased serotonin content in a concentration-dependent manner in P815 cells and showed 42.1 % inhibition of serotonin content at 5.0 M for 24 hr. The value of 50 % inhibitory concentration, IC$\sub$50/, of tetrahydropapaverine was 6.2 M. Under these conditions, tryptophan hydroxylase (EC 1.14.16.4, TPH), was inhibited for 24-36 hr after treatment with tetrahydropapaverine in P815 cells(49.1 % inhibition at 7.5 M). (omitted)

• Proceedings of the SCSK Conference
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• 2003.09b
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• pp.479-479
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• 2003

We investigated the tyrosinase inhibitory effect using whitening materials such as arbutin, ethyl ascorbyl ether, glabridin, kojic acid, magnesium ascorbyl phosphate and ascorbic acid. Tyrosinase inhibition rate were determined varying the enzyme concentration, reaction time, reaction temperature and pH. The optimal conditions to measure the inhibitory efficacy were as follows. : enzyme concentration 1,500 or 2,000IU/mL, reaction time 15min(for the enzyme concentration 1,500 IU/mL) and l0min(for the enzyme concentration 2,000IU/mL), reation temperature 42$^{\circ}C$, pH 6.5. Under these conditions $IC_{50}$/ of arbutin, ethyl ascorbyl ether, glabridin, kojic acid, magnesium ascorbyl phosphate and ascorbic acid were calculated. In the case of magnesium ascorbyl phosphate, the inhibitory effect of tyrosinase was very low and the $IC_{50}$/ of magnesium ascorbyl phosphate could not be calculated. Other five materials showed good inhibitory effect of tyrosinase and can be used for the whitening materials.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.22 no.2
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• pp.193-200
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• 1996

In eastern Asian region, cosmetic preparations containing the molecues possessing the whitening activity are promising. In this study, 100 plant extracts were screened in order to elucidate the whitening effects using in vitro tyrosinase assay and DOPA autooxidation. Several plant extracts such as Morus alba, Glycyrrhiza glabra showed the inhibitory activity (>50%) against mushroom tyrosinase at the concentration 333$mu extrm{m}$/ml. And plant extracts including Morus alba and Bupleurum falcatum showed the inhibitory activity (>50%) at the concentration of 500($\mu\textrm{g}$/ml against DOPA autooxidation. The IC50 values of the several extracts were also found.

• Archives of Pharmacal Research
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• v.18 no.2
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• pp.105-112
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• 1995

In ordedr to gain insight into the mechanisms byl which erythropoietin promotes erythropoiesis, effects of various inhibitors on the erythropoietin-propmoted differentiation of erythroid progenitor cells and on the erythroid progenitor cells and on the erythropoietin-promoted $Ca^{++}$ uptake in the progenitor cells were determined, and the relationship between the inhibitory activity of each inhibitor cells were determined, and he relationship between the inhibitory activity of each inhibitor toward the differentiation and channel blocker (varapamil), a $Ca^{++}$ chelator (EDTA) and a protein kinase C inhibitor (stauroporine). All of these agents inhibited both the erythropoietin-mediated differentiation of the erythroid progenitor cells, as determined by the incroporation of $^{59}Fe$ into heme, and $Ca^{++}$ uptake in a concentrtion dependent manner. In the cases of varapamil and EDTA, the half-miximal inhibitory concentration $(IC_{50})$ values for differentiation of the progenitor cells may be theconsequence of the inhibition of the $Ca^{++}$ uptake in a concentration dependent manner. In the cases of varapamil and EDTA, the half-miximal inhibitory concentration dependent manner. In the cases of verapamil and EDTA, the half-miximal inhibitory concentration $(IC_{50})$ values for differentiation of the progenitor cells may be the consequence of the inhibition of the $Ca^{++}$ uptake by the inhibitor. On the other hand, in the cases of genistein and stauroporine, the $IC_{50}$ values for inhibition of differentitation were significantly different from that for inhibition of $Ca^{++}$uptake. These results suggest that the mechanism of inhibition of differentiation by these two inhibitors in complex. However, taken all together, the above results support the proposition that $Ca^{++}$ uptake may play a role in the erythropoietin-mediated differentiation of erythoid progenitor cells.

• Mycobiology
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• v.51 no.1
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• pp.60-66
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• 2023

In this study, the α-amylase inhibitory activity, α-glucosidase inhibitory activity, pancreatic lipase inhibitory activity, and Xanthine Oxidase inhibitory activity of the fruiting body extracts of 5 varieties of Agaricus bisporus (AB) were confirmed. First, the α-amylase inhibitory activity of AB12, AB13, AB18, AB34, and AB40 methanol extracts was lower than that of acarbose, a positive control, in all concentration ranges. The α-glucosidase inhibitory activity of the AB40, AB13, and AB12 methanol extracts at the extract concentration of 1.0 mg/mL was 80.5%, 81.3%, and 78.5%, respectively, similar to that of acarbose, a positive control. The pancreatic lipase inhibitory activity of the methanol extract of Agaricus bisporus fruiting body was significantly lower than that of the positive control orlistat in the concentration range of 50~1.000 (mg/mL). The Xanthine Oxidase inhibitory activity was 0.5~8.0 mg/mL of each extract, which was significantly lower than that of the positive control allopurinol in the same concentration range. However, the Xanthine Oxidase inhibitory activity of AB13 and AB40 at 8.0 mg/mL was about 70%, which was higher than that of other mushrooms. In conclusion, five kinds of Agaricus bisporus fruiting bodies seem to have inhibitory effects on enzymes such as α-amylase, α-glucosidase, pancreatic lipase, and Xanthine Oxidase that degrade starch and protein. In particular, it has an inhibitory effect and a reduction effect on xanthine oxidase that causes gout, so it is expected that it can be developed and used as a food or health supplement with health functional properties through future research.

• Korean Journal of Pharmacognosy
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• v.42 no.4
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• pp.323-328
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• 2011

We investigated antioxidative activity, tyrosinase inhibitory activity, and melanin production inhibitory activity of the methanol extract of Paeoniae Radix and its fractions. The total polyphenol content of the extract was 73.45 mg/g, and content of the ethyl acetate fraction was 514.50 mg/g as the highest content of fractions. In DPPH radical scavenging ability, $SC_{50}$ values of the ethyl acetate was 3.86 ${\mu}g/ml$ as a result of greater activity in the positive control (ascorbic acid). Moreover, tyrosinase inhibitory activity of the ethyl acetate fraction showed higher activity than arbutin used as a positive control. In the cytotoxicity measurement by MTT assay, the extract and fractions were exhibited cell viabilities of 76.96~157.26% against Raw 264.7 and B16F10 cell in concentration of 10~100 ${\mu}g/ml$. In nontoxic concentration range, the ethyl acetate fraction showed strong melanin production inhibitory effect in ${\alpha}$-melanocyte stimulating hormone (${\alpha}$-MSH)-stimulated B16F10 cell. As a result, the ethyl acetate fraction of the methanol extract from Paeoniae Radix could be applicable to functional materials for skin-whitening agents.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.4 no.4
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• pp.366-371
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• 2003

Biological efficacy assays, including antimicrobial, tyrosinase inhibition and anticancer activities of Chlorella hydrolysate, were carried out. In tyrosinase inhibition assay of Chlorella hydrolysate, $IC_{50}$(inhibitory concentration) was measured as 12%. Chlorella hydrolysate showed high anti-lung cancer activity of 88.2% at a concentration of 0.15%.

• Journal of the Korean Chemical Society
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• v.64 no.2
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• pp.79-83
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• 2020

A novel pharmacophore with epinastine (1) and NSAID moieties (2-5) was designed by molecular hybridization approach. The hybrid compounds 6-9 were synthesized by EDCI/HOBt or HATU-mediated coupling of 1 with salicylic acid (2), mefenamic acid (3), indomethacin (4) and naproxen (5), respectively, and were assessed for their inhibitory effect against NO production in LPS-induced RAW-264.7 macrophages in vitro. The Hybrids were found to exhibit significant NO production inhibitory effects with half-maximal inhibitory concentration (IC₅₀) values ranging in between 15.96 ± 1.32 and 36.68 ± 2.53 μM and were non-cytotoxic to macrophages. Comparing the inhibition concentration (IC₅₀), cytotoxicity concentration (CC₅₀) and in vitro efficacy index (iEI), 6 (IC₅₀ = 17.97 ± 1.92 μM; iEI = 11.13) and 9 (IC₅₀ = 15.96 ± 1.32 μM; iEI = 12.53) were better suited than other hybrids as well as their parent compound. Our findings signify that hybrids 6 and 9 may serve as platforms for continued investigations for the development of more efficient anti-inflammatory agents.

• Biomolecules & Therapeutics
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• v.9 no.3
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• pp.183-187
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• 2001

Nitric oxide (NO) produced in large amounts by the inducible nitric oxide synthase (iNOS) is known to be responsible for the vasodilation and hypotension observed in septic shock and inflammation. The inhibitors of iNOS, thus, may be useful candidate for the treatment of inflammatory diseases accompanied by the overproduction of NO. We prepared alcoholic extracts of Chinese medicinal plants and screened their inhibitory activity against NO production in lipopolysaccharide (LPS)-activated macrophages. Among the 80 kinds of extracts of herbal drugs, 15 extracts showed potent inhibitory activity of NO production above 80% at the concentration o$50\mu\textrm{g}/ml$. These potent extracts showed dose dependent inhibition of NO production of LPS-activated macrophages at the concentration of 50, 30,$10\mu\textrm{g}/ml$. Especially, Rhus chinensis, Senecio scandens and Wikstroemia indica showed most potent inhibition above 50% at the concentration of $10\mu\textrm{g}/ml$. These plants are promising candidates for the study of the activity-guided purification of active compounds and would be useful for the treatment of inflammatory diseases and endotoxemia accompanying the overproduction of NO.