• Natural Product Sciences
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• v.19 no.1
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• pp.8-14
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• 2013

The inhibitory effect and the structure-activity relationships of luteolin and its related derivatives isolated from Taraxacum mongolicum against MAO activities were investigated. The activity-guided isolation of extract from Taraxacum mongolicum led to the isolation of three flavonoids, luteolin, diosmetin, and luteolin-7-glucoside, a polyphenol, chlorogenic acid, a tyrosine and a uridine. The inhibitory activities of luteolin and its related derivatives against MAOs activities are dependent on their molecular structures. The presence of the phenolic hydroxy group at para-position is the active site for MAO-A inhibition as well as of MAO-B. The methoxy group has no potential on MAO-A inhibition. An additional phenolic hydroxy group at the ortho-position alleviates about 4-fold MAO-A inhibitory activity of phenolic hydroxy group at para-position. A carboxylic group seems to be critical for DBH inhibition and has no effects on MAO.

• Microbiology and Biotechnology Letters
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• v.27 no.1
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• pp.8-14
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• 1999

This study was developed to evaluate the growth inhibition effects of cell wall components of Enterococcus faecalis 2B4-1 obtained from feces of neonates against tumor cell lines. Polysaccharide fraction (PS) shown sensitive growth inhibition effect in the cell wall components was isolated and characterized. In growth inhibition effects, residue fractin of whole cell was shown sensitive level of percent survival about 30% when administrated at ehe concentration of 100${\mu}$g/ml, and that was more effective than that of supernatant fraction against the tumor cell lines, SNU-1, 3LL, FARROW and HEC-1-B. Sensitive growth inhibition effects against SNU-1, FARROW and HEC-1-B were performed by whole cell (WC) fraction from Ent. faecalis 2B4-1. Cytoplasm fractin (CP) of WC was shown non-inhibition effect, however, the other part of WC, precipitate of disrupted cell (PD), was sensitive against the tumor cell line mentioned above. Followed by separation to peptidoglycan fraction (PG) and polysaccharide fraction (PS) were all sensitive which the latter was shown more sensitive percent survival than the former. Composed sugars of polysaccharide fraction were determined to D-glucose, L-rhamnose and D-glucosamine, and the rate fo composition was calculated to about 1:1:1 by the data of elemental analysis, IR, TLC and HPLC.

• Weed & Turfgrass Science
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• v.2 no.1
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• pp.70-75
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• 2013

Seven medicinal plant extracts were tested for antifungal activities against six species of the major turfgrass pathogenic fungi (Colletotrichum graminicola, Pythium spp., Rhizoctonia cerealis, Rhizoctonia solani AG1-1, Rhizoctonia solani AG2-2, and Sclerotinia homoeocarpa) using paper disk diffusion method. Three medicinal plant extracts, including Pinus densiflora showed antifungal activities. In suppression of mycelium growth test, on medium adding P. densiflora extract showed that inhibition rate of mycelium growth were above 80% in 10 mg/10 ml concentration of the extract. The inhibition rate of Pythium spp. was 100% and C. graminicola was 84.3% in 10 mg/10 ml concentrations of P. densiflora extract, respectively. In particularly, the inhibition rate of Pythium spp. was 89.5% in 2 mg/10 ml concentrations of P. densiflora extract. As a result, P. densiflora extract showed high antifungal activity to Pythium spp. and C. graminicola of the turfgrass pathogen in in vitro test.

• Applied Chemistry for Engineering
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• v.10 no.1
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• pp.6-11
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• 1999

Dialkylamine (di-)nitrobenzoates as vapor corrosion inhibitor were synthesized with dialkylamines and (di-)nitrobenzoic acids. The compounds were analyzed by elemental analyzer, FT-IR and $^1H$-NMR spectrophotometer. Corrosion inhibition of synthetic compounds and additives [$(NH_4)_2CO_3$, $NaHCO_3$] against ferrous and non-ferrous metal was investigated by potentiostatic method [1% (w/v) corrosion inhibitor in 1M $Na_2SO_4$ aqueous solution] respectively. For corrosion inhibition of ferrous metal, dialkylamine 4-nitrobenzoates were better inhibitor than dialkylamine 3, 5-dinitrobenzoates, the passivating current density ($i_p$) of dialkylamine 4-nitrobenzoate was shown $4.78mA/cm^2$. While, for non-ferrous metal, dialkylamine 3, 5-dinitrobenzoates were better, those of dipropylamine 3, 5-dinitrobenzoate and hexamethyleneimine 3, 5-dinitrobenzoate were shown 36 and $37mA/cm^2$. Additive effect of $(NH_4)_2CO_3$ and $NaHCO_3$ for corrosion inhibition of ferrous metal was excellent but that of non-ferrous metal was not. Optimum ratios of diethylamine 4-nitrobenzoate with $(NH_4)_2CO_3$ and $NaHCO_3$ were 4 : 6 and 5 : 5 (V/V), and passivating current densities ($i_p$) of the mixtures were shown 0.26 and $0.85mA/cm^2$, respectively.

• Bulletin of the Korean Chemical Society
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• v.33 no.9
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• pp.3004-3008
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• 2012

Small molecule conjugated peptides were prepared by solid-phase synthesis as potential novel whitening agents, and their melanogenesis inhibitory activities were investigated. The conjugated small molecules were well-known materials as tyrosinase inhibitors, and peptides were selected from the sequences that are known to antagonize melanocortin receptor 1 (MC1R). Most of small molecules-peptide conjugates showed superior melanin inhibition activity to kojic acid and arbutin. Among these, almost all compounds have -AR- sequence. From this study, we concluded that the small molecule conjugated peptides containing -AR- sequence have melanogenesis inhibitory activities and have potential to be used as novel whitening agents.

• Journal of Marine Bioscience and Biotechnology
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• v.10 no.2
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• pp.83-90
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• 2018

Ultraviolet (UV) radiation causes inflammation and matrix metalloproteinase (MMP) over-expression and extra cellular matrix depletion, leading to skin photo-aging such as wrinkle formation, dryness, and sagging. In this study, we demonstrated that pretreatment with the hexane extract of microalgae protects UVB mediated cell damages. The results of clinical study showed that Microalgal Oil treated group reduced wrinkle and improve elasticity. All these results suggest Microalgal Oil may be useful as new photo-aging cosmetics for protection against UV induced activity.

• Applied Biological Chemistry
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• v.51 no.3
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• pp.171-176
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• 2008

The comparative molecular similarity indices analysis (CoMSIA) models between 3${\beta}$-Hydroxy-12-oleanen-28-oic acid (1-30) analogues as substrate molecule and their inhibitory activities ($pI_{50}$) against protein tyrosine phosphatase (PTP)-1B were derived and discussed quantitatively. Listing in order, the CoMFA>CoMSIA${\geq}$HQSAR>2D-QSAR model, these QSAR models had the better statistical values. The optimized CoMSIA F1 model at grid 3.0${\AA}$ had the best predictability and fitness ($q^2$=0.754 and $r^2$=0.976) by field fit alignment. The order of contribution ratio (%) of CoMSIA fields concerning the inhibitory activities was a H-bond acceptor (48.9%), steric field (25.8%) and hydrophobic field (25.4%), respectively. Therefore, the inhibitory activities of substrate molecules against PTP-1B were dependent upon H-bond acceptor field (A) of $R_4$-group. From the analytical results of CoMSIA contour maps, oleanolic acid derivatives will have better inhibition activities if $R_1$ group has H-bond acceptor disfavor, $R_3$group has steric disfavor and $R_4$ group has steric, hydrophobic, H-bond favor.

• Biomolecules & Therapeutics
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• v.26 no.3
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• pp.274-281
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• 2018

A previous study in humans demonstrated the sustained inhibitory effects of donepezil on acetylcholinesterase (AChE) activity; however, the effective concentration of donepezil in humans and animals is unclear. This study aimed to characterize the effective concentration of donepezil on AChE inhibition and impaired learning and memory in rodents. A pharmacokinetic study of donepezil showed a mean peak plasma concentration of donepezil after oral treatment (3 and 10 mg/kg) of approximately $1.2{\pm}0.4h$ and $1.4{\pm}0.5h$, respectively; absolute bioavailability was calculated as 3.6%. Further, AChE activity was inhibited by increasing plasma concentrations of donepezil, and a maximum inhibition of $31.5{\pm}5.7%$ was observed after donepezil treatment in hairless rats. Plasma AChE activity was negatively correlated with plasma donepezil concentration. The pharmacological effects of donepezil are dependent upon its concentration and AChE activity; therefore, we assessed the effects of donepezil on learning and memory using a Y-maze in mice. Donepezil treatment (3 mg/kg) significantly prevented the progression of scopolamine-induced memory impairment in mice. As the concentration of donepezil in the brain increased, the recovery of spontaneous alternations also improved; maximal improvement was observed at $46.5{\pm}3.5ng/g$ in the brain. In conclusion, our findings suggest that the AChE inhibitory activity and pharmacological effects of donepezil can be predicted by the concentration of donepezil. Further, $46.5{\pm}3.5ng/g$ donepezil is an efficacious target concentration in the brain for treating learning and memory impairment in rodents.

• Preventive Nutrition and Food Science
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• v.4 no.1
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• pp.70-74
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• 1999

The primary objective of these studies was to screen the materials showing inhibitions of HMG-CoA reductase in vitro. The secondary objective was to determine the effect of garlic, lovastatin and copper on cholesterol concentrations in plasma. liver and brease muscle of pullets. In experiment 1, the degree of inhibition of the selective samples on HMG-CoA reductase activity was determined in vitro. The inhibition rate of water soluble garlic extracts, lovastatin and copper to HMG-coA reductase activity were 51.3%, 87.5%, and 82.0% respectively . In experiment 2, control diet (basal diet), garlic powder (3% in diet) , lovastatin (300mg/kg of diet) and copper(200mg/kg of diet) were fed to pullets in order to investigate the changes of cholesterol concentration in plasma and tissues. Plasma total cholesterol , and LDL-cholesterol were significantly reduced in pullets fed a diet containing 3 % garlic powder. However, coper significantly increased total cholesterol compared to controls and lovastatin did not affect plasma chholesterol concentration . Total cholesterol inlover and breast muscle inpullets were not affectedb y adding cholesterol lowering materials to the diets. The data suggests that it is not easy for HMG-CoA reductase inhibitors to reduce cholesterol levels in the body due to complication in cholestrol metabolism . However, garlic administration can lower the levels of plasma cholesterol in pullets.

• Bulletin of the Korean Chemical Society
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• v.15 no.5
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• pp.394-399
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• 1994

The catalytic mechanism of malonyl-CoA synthetase from Rhizobium trifolii was investigated by the steady state kinetics and intermediate identification. Initial velocity studies and the product inhibition studies with AMP and PPi strongly suggested ordered Bi Uni Uni Bi Ping-Pong Ter Ter system as the most probable steady state kinetic mechanism of malonyl-CoA synthetase. Michaelis constants were $0.17{\pm}0.04 {\mu}M,\;0.24{\pm}0.18 {\mu}M\;and\;0.045{\pm}0.26 {\mu}$M for ATP, malonate and CoA, respectively. The TLC analysis of the $^{32}P-labelled$ products in reaction mixture containing $[{\gamma}-^{32}P]$ ATP in the absence of CoA showed that PPi was produced after the sequential addition of ATP and malonate. Formation of malonyl-AMP, suggested as an intermediate in the kinetically deduced mechanism, was confirmed by the analysis of $^{31}P-NMR$ spectra of AMP product isolated from the $^{18}O$ transfer experiment using $[^{18}O]$malonate. Two resonances were observed, corresponding to AMP labelled with zero and one atom of $^{18}O$, indicating that one atom of $^{18}O$ transferred from $[^{18}O]$malonate to AMP through the formation of malonyl-AMP. Formation of malonyl-AMP was also confirmed through the TLC analysis of reaction mixture containing $[{\alpha}-^{32}P]$ATP. These results strongly support the ordered Bi Uni Uni Bi Ping-Pong Ter Ter mechanism deduced from the initial velocity and product inhibition studies.