• Journal of Applied Biological Chemistry
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• 제50권3호
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• pp.115-119
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• 2007

To discover the sources with antioxidant and tyrosinase inhibitory activities in Korean traditional medicines, 10 extract of medicinal plants were screened for their potential to scavenge stable 1,1-diphenyl-2-picryhydrazyl (DPPH) free radical, inhibit hydroxyl radical (${\cdot}OH$), total phenolic content, and inhibition of tyrosinase. The potency of DPPH radical scavenging activity was shown in the extract of Ulmus davidiana var. japonica Nakai that has a greater effect with $IC_{50}$ values of $6.49{\pm}5.43{\mu}g/mL$, than BHA ($IC_{50}=20.99{\pm}0.74{\mu}g/mL$), L-ascorbic acid $(IC_{50}=20.59{\pm}1.06{\mu}g/mL),\;and\;{\alpha}-tocopherol\;(IC_{50}=25.55{\pm}0.26{\mu}g/mL)$ as a positive control. The ${\cdot}OH$ scavenging activities were observed in the plants tested. Acanthopanax senticosus, Cirsium setiders, U. davidiana exhibited scavenging activity of more than 60% at $500{\mu}g/mL$. The scavenging activity(%) of BHA and a-tocopherol were 64.32 and 55.87% at $500{\mu}g/mL$, respectively. The total phenolic content was determined, in order to assess its effect on the extract's antioxidant activity. The total phenoic content of $33.37{\pm}0.52mg/g$ was conformed by methanolic extract of U. davidiana. The U. davidiana and Morus bombycis exhibited tyrosinase inhibitory activity with a $34.28{\pm}1.32\;and\;75.57{\pm}1.10%$, respectively. In particular, M. bombycis has stronger tyrosinase inhibitory activity than albutin with $36.48{\pm}3.56%$ as a positive control. This work showed that the inhibitory abilities of Korean medicinal plants, such as U. davidiana and M. bombycis, on DPPH free radical, inhibit hydroxyl radical (${\cdot}OH$), and inhibition of tyrosinase and total phenolic content, can be useful in the prevention and treatment of free radical-relate disease. Investigations into further isolation of inhibitory principles of U. davidiana and M. bombycis are now in progress.

• 생약학회지
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• 제43권3호
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• pp.231-238
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• 2012

Menthae herba (MH) extracts exhibit anti-inflammatory effects. The purpose of this study was to determine whether the anti-inflammatory effects of MH extracts vary according to the cultivation regions. We performed a comparative analysis of MH extracts by evaluating the production of inflammatory mediators in RAW 264.7 murine macrophage cells and HaCaT human keratinocyte cells. MH extracts obtained from different cultivation regions in Korea and China significantly reduced the production of nitric oxide (NO), prostaglandin $E_2$ ($PGE_2$), and tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) in RAW 264.7 cells stimulated with lipopolysaccharide (LPS). No differences in these inhibitory activities were observed between MH extracts. In HaCaT cells stimulated with TNF-${\alpha}$ and interferon-${\gamma}$ (IFN-${\gamma}$), MH extracts did not inhibit the production of macrophage-derived chemokine (MDC/CCL22), but most extracts reduced the production of the regulated on activation normal T-cell expression and secreted (RANTES/CCL5). We used clustering tree analysis of the MH extracts according to the chromatographic pattern and anti-inflammatory potency of MH extracts. We observed differences in the chromatographic pattern of MH extracts but no difference in anti-inflammatory potency. Our findings suggest that MH extracts from different regions do not show any differences in their pharmacological potency in that MH extracts are used as therapeutic agents to treat inflammatory disorders.

• Bulletin of the Korean Chemical Society
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• 제30권11호
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• pp.2707-2712
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• 2009

5-$HT_{3}$ receptor;5-$HT_{3A}$ receptor channel activity;Novel 5-$HT_{3}$ receptor channel current blockers;Chlorophenyl substituted piperazinylethylaminomethylpyrazoles; The 5-$HT_{3A}$ receptors are one of ligand-gated ion channels and are known to be involved in visceral pain, anxiety, or anticancer agent-induced nausea and vomiting. In present study, we designed novel skeletons based on the developed 5-$HT_{3}$ receptor antagonists and evaluated their effects on 5-$HT_{3A}$ receptor channel currents ($I_{5-HT}$) of a series of pyrazole derivatives having N-chlorophenylpiperazine functionality (6-9). We found that most of N-p-chlorophenyl substituted piperazinyl-pyrazole derivatives (7b, 7c, 7e and 7h) exhibited the high potency for the inhibition of $I_{5-HT}$, whereas the compound without chloride (6) or with m-chlorophenyl group (a serious of 8 and 9) showed the low potency. These result indicate that p-chlorophenyl group is might play an important role for increasing the inhibitory potency on $I_{5-HT}$.

• 대한한방내과학회지
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• 제36권2호
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• pp.165-179
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• 2015

Objectives: This experiment investigated the antimicrobial activity of Hwangryunheadok-tang and extracts of Scutellariae radix , Phellodendri cortex , Coptis rhizome , and Gardenia jasminoides against Salmonella typhimurium . Methods: After spreading S. typhimurium on a bacterial culture medium plate, antimicrobial activity was tested by dripping diluted Hwangryunheadok-tang or extracts of Scutellariae radix , Phellodendri cortex , Coptis rhizome , or Gardenia jasminoides (80 μl, diluted 100, 50, 10, and 1%) onto the plate, followed by culture for 16 to 72 hours. The minimal inhibitory concentration (MIC) was tested by dripping the minimum dilution that showed antimicrobial activity (80, 60, 40, and 20 μl) and measuring the density. The antimicrobial activity of Hwangryunheadok-tang and four extracts showed continuous antibacterial activity against S. typhimurium throughout the experiment. Result: 1. S. typhimurium . (Standard Microorganism, ATCC) 1) The Hwangryunheadok-tang and extracts of Scutellariae radix , Phellodendri cortex , and Coptis rhizome showed antibacterial activity in the undiluted solutions and in 50% dilutions. Gardenia jasminoides extract showed potency only in the undiluted solution. The antimicrobial potency of the undiluted solution was increased when the volume of inoculation was increased, but no difference was noted when the culture time was extended. All the extracts showed antimicrobial potency against S. typhimurium . 2. S. typhimurium isolated from diarrhea patients 1) When compared to the standard microorganism experiment on S. typhimurium , the MICs of the five extracts were increased. However, whereas the antimicrobial potency of doxycycline was lost entirely against bacteria isolated from patients with diarrhea, the antimicrobial potency of all the extracts was diminished but did not disappear. 2) The antimicrobial activity of Hwangryunheadok-tang and four extracts was continuous even when the culture time was extended to 16, 24, and 72 hours. Conclusions: The Hwangryunheadok-tang and four kinds of extracts have antimicrobial activity against S. typhimurium . Comparison of a standard microorganism with S. typhimurium isolated from diarrhea patients showed that the antimicrobial activity of all the extracts was better than that of antibiotics. Further studies should focus on the value and benefits of Hwangryunheadok-tang , and the four kinds of extracts as clinical treatments.

• 한국식품영양과학회지
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• 제21권3호
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• pp.255-262
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• 1992

단백소화율에 미치는 식이 섬유소의 영향에 대하여 알아보기 위해, 채소류(상치, 깻잎, 고추. 다시마)로부터 추출한 식이 섬유소와 시판용 정제 식이 섬유소 (cellulose, pectin, sodium alginate, gum karaya)를 어류 단백질인 말쥐치 단백질(냉동건조육 및 myofibrils)에 첨가 반응시켜, 단백질 의 소화율에 어느 정도 영향을 미치는가에 대해 알아보았다. 각 시료의 중성세제 추출섬유소 (neutral detergent fiber) 함량은 24.21%(고추) 9.75%(다시마)의 범위였고, 산성세제 추출섬유소 (acid detergent fiber) 함량은 20.85%(고추) 11.97%(깻잎)의 범위였으며, 수용성 섬유소 함량은 13.79%(다시마) 4.41%(상치)의 범위였다. 말쥐치 단백질에 대한 식이 섬유소의 반응 비율을 1 : 1 (wt/wt)로 하고, 37$^{\circ}C$에서 2시간 동안 반응시켰을 때. 말쥐치 단백소화율은 정제 식이 섬유소 첨가의 경우, 1.52%(cellulose) 9.97%(pectin)가 감소되었고. 추출한 식이 섬유소 첨가의 경우, 5.15%(고추) 12.36%(다시마)가 감소되었다. 섬유소의 trypsin 활성저해능은 단백소화율이 감소함에 따라 증가하여, ANRC casein에 대한 soybean trypsin inhibitor 22mg/g (cellulose) 61.82mg/g(gum karaya), 49.75mg/g(고추) 171.52mg/g(상치)에 상응하는 것으로 나타났다. 정제 식이 섬유소에 의한 단백분해효소의 활성 변화는 sodium alginate를 제외하고는 거의 없어, 어류 단백소화율의 저하는 식이 섬유소가 단백질에 직접 결합하여 비소화성 물질을 형성한 결과가 주도하리라 생각되었다. 말쥐치 단백질과 섬유소를 반응시킨 것을 효소 가수분해시킨 후에 측정한 유리 필수 아미노산의 함량은 sodium alginate와 다시마 섬유소의 경우 현저하게 저하하였으며(75% 이상), isoleucine과 valine이 크게 영향을 받았다.

• Advances in Traditional Medicine
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• 제7권5호
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• pp.477-484
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• 2008

The present study was aimed at investigating the hypouricemic and xanthine oxidase inhibitory activities of the various fractions of the hydromethanolic extract of the leaves of Coccinia grandis L. Voigt (Cucurbitaceae). The leaves of this species was used in traditional medicinal system for the treatment of gout, rheumatism, jaundice, bronchitis, fever, skin eruptions, wounds, etc. The degree of xanthine oxidase inhibition was determined in vitro by measuring the increase in absorbance at 295 nm associated with uric acid formation. Among the fractions tested, the chloroform fraction exhibited highest potency ($IC_{50}$ $17.8\;{\mu}g/ml$). This was followed by the pet-ether ($IC_{50}$ $29.7\;{\mu}g/ml$), ethyl acetate ($IC_{50}$ $41.2\;{\mu}g/ml$) and residual ($IC_{50}$ $47\;{\mu}g/ml$) fractions. The $IC_{50}$ value of allopurinol was $6.1\;{\mu}g/ml$. In addition, the hypouricemic and hepatic xanthine oxidase (XO)/xanthine dehydrogenase (XDH) inhibitory activities of the fractions were examined in vivo using oxonate (280 mg/kg, i.p.) induced hyperuricemic mice. At a dose of 200 mg/kg orally for 7 days, the pet-ether, chloroform and ethyl acetate fractions produced a significant (P < 0.01) reduction in serum urate level and also inhibited hepatic XO/XDH activities when compared to hyperuricemic mice. These inhibitory effects were weaker than that observed for the standard drug, allopurinol (10 mg/kg, p.o.). Lineweaver-Burk analysis of the enzyme kinetics indicated that the mode of inhibition was of a mixed type. These results suggest that the use of Coccinia grandis leaves for the treatment of gout could be attributed to its XO inhibitory activity.

• Archives of Pharmacal Research
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• 제21권1호
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• pp.6-11
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• 1998

The activities of two types of antiulcer agents against 9 strains of Helicobacter pylori (H. pylori) were determined by the agar dilution method. The antiulcer agents were YJA20379, a newly synthesized proton pump inhibitor developed by Yung-jin Pharmaceutical company, and omeprazole. Both compounds were found to have significant activities against this organism. The MIC values of YJA20379 and omeprazole were 11.7 and $31.25{\mu.g/ml}$ respectively. In addition, the inhibitory potency of both compounds was investigated on H. pylori urease which is believed to be an important colonization and virulence factor in the pathogenesis of gastritis and peptic ulcers. These compounds dose-dependently inhibited urease extracted with distilled water and their $IC_50$ values were $16.4{\times}10^{-5} M and 14.3{\times}10^{-5}M,$ respectively. In addition, a pH-dependent study to determine whether inhibitory potency would be activated by acid condition was performed. It was found that unlike omeprazole, YJA20379 was not affected by acid condition. To determine the inhibition pattern and optimal concentration of substrate, kinetics were evaluated at various pH levels (pH 5.0, 7.0, and 8.5). The data show that YJA20379 noncompetitively inhibited H. pylori urease and $K_M/K_i$values were 0.96 $mM/60{\mu}M (pH 5.0), 0.56 mM/141.5 {\mu}M (pH 7.0)$, and $1.94mM/34{\mu}M (pH 8.5)$, respectively. Based on data obtained, it is concluded that YJA20379 is a significant inhibitor of H. pylori growth and urease and therefore, taking these results into consideration, YJA20379 might be a beneficial therapy for gastritis and peptic ulcers induced by H. pylori.

• 생약학회지
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• 제30권4호
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• pp.413-416
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• 1999

During the screening for inhibitors on nitric oxide (NO) production in LPS-activated murine macrophage, RAW 264.7 cells, two coumarins were isolated from chloroform extract of Ponciri Fructus. They were identified as imperatorin (10), phellopterin (11) on the basis of spectroscopic methods. The $IC_{50}$ values for NO formatiom were about $5.4\;{\um}M$ and $35.0\;{\um}M$, respectively, and then eleven coumarins were tested for the inhibitory effects on NO production in activated macrophages. All the test coumarins inhibited NO production in concentration-dependent manner and furanocoumarins (6-11) showed much more potent inhibitory effect than simple coumarins. Among the compounds examined xanthotoxin (8) was the most potent inhibitors of NO production $(IC_{50}=1.4\;{\mu}M)$. Analysis of the structure-activity relationship among these coumarins led to the conclusion that the substitution of C-5 position in furanocoumarins reduces greatly their inhibitory potency although the substitution of C-8 does not almost affect it.

• 한국연초학회지
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• 제19권2호
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• pp.136-144
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• 1997

Cigarette smoking is known to suppress both 1-methy14-phenyl-155,Ltetrahydropy-ridine (MPTP)-induced parkinsonism and idiopathic Parkinson's disease (PD). However, the precise mechanism underlying its protective action against PD is not clearly elucidated yet. In order to find possible clue on the mechanism of protective action of smoking, we investigated the inhibitory effect of cigarette smoke components on rat brain mitochondria1 monoamine oxidase B (MAO-B), responsible enzyme for the activation of MPTP to its toxic metabolitesr and identified the components having an inhibitory potency on this enzyme from cigarette smoke. Total 31 eligible constituents including nicotine were selected from cigarette smoke condensates via solvents partitioning and silica gel chromatographic separation, and inhibitory potencies of 19 components on MAO-B were determined. Hydroquinone and methylcatechol, the phenolic components, showed the strongest inhibitory potencies on MAO-B activity in the components tested. 3,4-Dihydroxybenzylamino, myosmine and indole in basic fracton, eugenol in phenolic fraction, and farnesol in neutral fraction also inhibited the enzyme activity dose-dependently. Among tobacco alkaloids tested only myosmine was effective for the inhibition of this enzyme. These results suggest that the decrease in MAO-B activity by such components derived from cigarette smoke seems to be related to the suppression of MPTP-induced neurotoxicity and to the less incidence of Parkinson's disease in smokers than in nonsmokers.

• Archives of Pharmacal Research
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• 제25권3호
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• pp.306-312
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• 2002

Aldose reductase, the key enzyme of the polyol pathway, is known to play important roles in the diabetic complication. The inhibitors of aldose reductase, therefore, would be potential agents for the prevention of diabetic complications. To evaluate active principles for the inhibition of aldose reductase from the rhizomes of Belamcanda chinensis, twelve phenolic compounds were isolated and tested for their effects on rat lens aldose reductase. As a result, isoflavones such as tectorigenin, irigenin and their glucosides were found to show a strong aldose reductase inhibition. Tectoridin and tectorigenin, exhibited the highest aldose reductase inhibitory potency, their $IC_{50}$ values, being $1.08{\times}10^{-6}{\;}M{\;}and{\;}1.12{\times}10^{-6}{\;}M$, respectively, for DL-glyceraldehyde as a substrate. Both compounds, when administered orally at 100 mg/kg for 10 consecutive days to streptozotocin-induced diabetic rats, caused a significant inhibition of sorbitol accumulation in the tissues such as lens, sciatic nerves and red blood cells. Tectorigenin showed a stronger inhibitory activity than tectoridin. From these results, it is suggested that tectorigenin is attributed to be a promising compound for the prevention and/or treatment of diabetic complications.