• 한국응용곤충학회지
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• 제31권2호
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• pp.122-132
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• 1992

신규화합물의 in Vitro AChE 저해력을 평가하기 위한 저해시험법의 확립을 목적으로 실험을여 다음과 같은 결과를 얻었다. {TEX}$I_{50}${/TEX} 산출이 가능한 고정시간 저해시험(fixed time inhibition test)의 경우, DFP, DDVP 및 paraoxon과 같은 대표적 AChE 저해제의 저해력 평가에 적당한 저해시간은 10분 정도로 조사되었으며, 10분간의 저해조건하에서 ester group을 보유한 신규화합물의 저해여부 및 정도의 평가에 효과적인 시험농도는 10$\mu$M 수준으로 판정되었으나 다른 화합물의 경우에는 보다 높은 농도로부터 단계적 저해시험이 필요한 것으로 보였다. {TEX}$K_{d}${/TEX}, {TEX}$k_{3}${/TEX} 및 {TEX}$k_{i}${/TEX}와 같은 저해상수의 산출을 위한 경시적 저해시험(Progressive inhibition test)에 있어서, 본 실험의 장시간 저해(0.8~13.3분)와 낮은 저해제농도(1$\times${TEX}$10^{-9}${/TEX}~2$\times${TEX}$10^{-6}${/TEX}M)의 조건하에서는 극히 낮은 {TEX}$K_{d}${/TEX}(1.3$\times${TEX}$10^-{8}${/TEX}~5.6$\times${TEX}$10^{-7}${/TEX}M) 및 {TEX}$K_{3}${/TEX}(0.21~{TEX}$0.27min^{-1}${/TEX})가 관찰되었으나 저해제간의 저해독성 조사에는 충분한 타당성을 가지는 것으로 조사되었다. 또한 DFP, paraoxon 및 신규화합물인 KH501간의 현격한 저해력 차이는 {TEX}$K_{d}${/TEX}의 차이 즉, 저해제와 AChE간의 친화력 차이에 기인된 것으로 판명되었다. 따라서 AntiChE 스크리닝에 있어서 1차단계에서는 고정시간 저해법을 통하여 산출된 {TEX}$I_{50}${/TEX}를 바탕으로 하여 저해력 유무 및 정도를 파악하고, 1차단계에서 고도의 AChE 저해력이 인정된 신규 화합물을 대상으로 2차단계인 경시적 저해법을 이용하여 저해양상 및 특성을 조사하는 것이 합리적인 체계일 것으로 생각되어진다.

• 대한환경공학회지
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• 제22권11호
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• pp.2037-2046
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• 2000

산성 혹은 염기성 pH가 활성슬러지 공정에 미치는 저해 작용은 비경쟁적 저해 동력학(noncompetitive inhibition kinetics)을 따르는 것으로 알려져 있으나, pH를 저해 물질의 농도항으로 정량화하기 어렵기 때문에 실질적으로 비경쟁적 저해 동력학식(noncompetitive inhibition kinetic equation)으로 해석하기 어렵다. 따라서 pH에 의한 저해 작용을 기술하는 경험식들이 여러 연구자들에 의해 개발되어 왔는데, 이들은 주로 산성 조건에 대해서만 적용 가능한 것들이다. 본 연구에서는 의사독성농도(pseudo toxic concentration, $C_{PT}$) 개념을 이용하여 pH가 활성슬러지 공정에 미치는 저해 영향을 정량화하는 기법을 개발하였고, 기존에 알려진 모델들과 비교하였다. 그 결과 $C_{PT}$ 개념을 이용한 모델은 넓은 범위의 pH에 대해 최대비성장속도(${\mu}_{max}$)의 감소를 비교적 정확하게 예측할 수 있었고, 같은 동력학식을 이용하여 산성 조건뿐만 아니라 염기성 조건에 대해서도 적용 가능한 것으로 나타났다. 또한 저해계수(inhibition coefficient. $K_I$)의 추정이 간단하다는 장점이 있다.

• Journal of the Korean Academy of Child and Adolescent Psychiatry
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• 제15권1호
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• pp.82-90
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• 2004

목 적：본 연구에서는 주의력 결핍과잉행동장애 아동을 대상으로 주요 3가지 실행기능 영역인 억제능력, 작업기억, 그리고 계획능력 면에서 정상아동과의 수행차이를 비교 분석하였으며, 실행기능 수행에 영향을 미치는 나이와 지능을 통제하여 고찰하였다. 또한 억제통제능력을 인지억제와 행동억제로 구분하여 수행을 비교연구 하였다. 방 법：대상은 주의력결핍과잉행동장애로 진단된 아동 25명으로 연령범위는 7세에서 12세였고, 비교집단은 동일연령의 정상 아동 25명이였다. 모든 아동들에게 개별적으로 지능검사와 실행기능 검사(고노고, 스트룹 간섭과제, 하노이탑, 숫자검사)를 실시하였으며, 나이와 지능을 공변인으로 한 공변량 분석을 하였다. 결 과：지능에서 ADHD아동과 정상아동간에 유의미한 차이를 보였으며, 나이는 각 실행기능 검사와 유의미한 상관을 보였다. ADHD아동은 정상아동에 비해서 억제능력과 작업기억에서 유의미하게 저조한 수행을 보였다. 하지만, 지능과 나이를 통제했을 경우, 작업기억과 계획능력에서는 수행차이가 없었다. 논 의：ADHD아동은 전반적인 실행기능에서 손상을 보이는 것이 아니라 억제능력(인지억제와 행동억제)에 어려움이 있으며, 억제능력이 ADHD의 주요결함임을 시사해준다. 이와 같은 결론은 치료적 개입시 인지억제 및 행동억제에 중점을 둔 치료방법이 필요함을 시사해준다.

• 한국연초학회지
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• 제9권2호
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• pp.69-75
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• 1987

Nicotine, the main alkaloid of tobacco, showed different effect according to the enzyme. Among investigated enzymes, protease was inactivated remarkably by nicotine and the mode of inhibition was examined. $\alpha$-amylase and $\beta$-amylase were not affected, and cellulase and glucoamylase were inactivated partially when the concentration of it was over 1.0% , but protease was inhibited powerfully by nicotine The inhibition of protease by nicotine was performed almost in the initial stage of reaction, and was not so much affected by temperature, and was reversible. The inhibition type of protease by nicotine appeared as a Mixed-type inhibition.

• 약학회지
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• 제44권3호
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• pp.279-282
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• 2000

The inhibition mode of S-hydroxy-2-phenylalanylaminomethyl-4-pyron ($IC_{50}=24.6{\;}{\mu}M$) on mushroom tyrosinase was investigated using L-tyrosine as a substrate. This inhibitor is the kojic acid derivative, where the C-7 hydroxyl of kojic acid was replaced by amino group and coupled to the carboxyl of L-phenylalanine. The kinetic data obtained show a competitive inhibition pattern.

• 약학회지
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• 제47권3호
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• pp.125-129
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• 2003

A series of 2-phenyl-5-nitrobenzimidazoles substituted at the para positon of the 2-phenyl moiety was synthesized ＆ evaluated for their activity to inhibit topoisomerase I. The structure-activity relationship study revealed that neither the electronic nor lipophilic parameters were related to the topoisomerase I inhibition. A strict spatial requirement seems to be present for retention of topoisomerase I inhibition activity.

• Archives of Pharmacal Research
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• 제10권1호
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• pp.50-59
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• 1987

(E)-2-Phenylcyclopropylamine ((E)-TCP), (Z)-2-Phenylacyclopropylamine ((Z)-TCP), (E)-1-methyl-2-phenylcyclopropylamine ((E)-MTCP), and (Z)-1-methyl-2-phenylcyclopropylamine ((Z)-MTCP) were synthesized and used to determine to what extent 1-methylsubstitution and stereochemistry of 2-phenycyclopropylamines affect inhibition of monoamine oxidase (MAO). Inhibition of rat brain mitochondrial MAO-A and B by the compounds were measured using serotonin and benzylamine as the substrate, respectively and $IC_{50}$ values obtianed with 95% confidence limits by the method of computation. For the inhibition of MAO-A, (E)-MTPC ($IC_{50}$ = 6.2 * $10^{-8}$M) was found to be 37 times more potent than (Z)-MTCP ($IC_{50}$ = 7.8 * $10^{-8}$M), was 7 times more potent than (Z)-MTCP($IC_{50}$= 4.7 * $10^{-7}$M) and (E)-TCP($IC_{50}$ =7.8 * $10^{-8}$M),0.6 times as potent as (Z)- TCP ($IC_{50}$ = 4.4 * $10^{-8}$M). The results suggested that while without 1-methyl group, potency of a (Z)-isomer was comparable to that of (E)-isomer, the methyl group in its (Z)-position was very unfavorable to the inhibition of MAO and that in its (E)-position, the methyl group contributed positively to the potency as found by the fact that (E)-MTCP was 1-5 times more potent than (E)-TCP. In view of the selective inhibition of MAO-A- or B over MAO-A and 1-methyl substitution as well as the stereochemical factors did not significantly influence the selectivity.

• 대한본초학회지
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• 제26권1호
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• pp.111-117
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• 2011

Objectives : The present study was designed to investigate effects of mixed extract from korean medicinal herbs (MIX) on oxidation/reduction reaction-related and aging-related enzyme in vitro. Methods : We performed MTT assay, collagenase inhibition assay, elastase inhibition assay, tyrosinase inhibition assay, DPPH free radical scavenging assay, SOD-like activity and xanthine oxidase inhibition assay. Results : Recently, many studies have reported that elastin is also involved in inhibiting or repairing wrinkle formation, although collagen is a major factor in the skin wrinkle formation. The MIX showed 97% inhibition of collagenase activity, and 64% inhibition of elastase activity at 1 mg/ml concentration of MIX, next only to positive control, which indicate good efficacy for anti-wrinkle ingredient. Also it's treatment showed 34% inhibition of tyrosinase activity, to relate whitening effect, at the same dose of MIX. Antioxidant activities were determined by DPPH radical scavenging, xanthine oxidase (XO) inhibiting activity and SOD-like activity. Also these scavenging, XO-inhibiting and SOD-like activities were measured in 91%, 80%, and 63% inhibition, respectively, at a treated dose of 1 mg/ml, compare to control. Conclusions : These results suggest that possibility of mixed korean medicinal herbs as a functional ingredient for anti-wrinkle and whitening, anti-oxidation and anti-aging cosmetic formula.

• Natural Product Sciences
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• 제22권3호
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• pp.193-200
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• 2016

This study describes the anti-inflammatory, anti-oxidant, and melanogenesis inhibition activities of methanol extract and various organic solvent fractions of Arecae Pericarpium. We examined the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, 1,1-diphenyl-2-picrylhydrazine (DPPH) scavenging activity, mushroom tyrosinase inhibition activity and melanin contents. The study showed that, among all tested fractions, methylene chloride fraction showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells ($IC_{50}$ value $8.89{\mu}g/mL$) and DPPH radical scavenging activity ($EC_{50}$ value $21.39{\mu}g/mL$). Methylene chloride and ethyl acetate fractions similarly inhibited mushroom tyrosinase activity. Methanol extract exhibited strongest reduction of melanin content in B16F10 melanoma cells. Based on the bioactivity assay results, methylene chloride and ethyl acetate fractions were further separated. Eight phenolic compounds were isolated, which are dimeric syringol (1), catechol (2), 4-hydroxybenzaldehyde (3), vanillin (4), 4-hydroxyacetophenone (5), apocynin (6), protocatechuic acid (7) and 4-hydroxybenzoic acid (8). Among the isolated compounds tested, catechol showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells. Catechol also showed the concentration-dependent NF-${\kappa}B$ inhibition activity. Arecae Pericarpium might have potentials to be developed as anti-inflammatory agent or dermatological product for skin-whitening agent.

• 대한본초학회지
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• 제27권5호
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• pp.65-75
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• 2012

Objectives : Cosmeceutical activities such as anti-oxidative and anti-aging effects of the Doinseunguitang and its composition, a traditional prescription, were evaluated. Methods : We performed MTT assay, melanin synthesis inhibition assay, DPPH free radical scavenging assay, SOD-like activity, xanthine oxidase inhibition assay, astringent activity assay, tyrosinase inhibition assay, elastase and collagenase inhibition assay. Results : The results were obtained as follows : DPPH free radical scavenging of water extract Doinseunguitang (DISG) and ethanol extract DISG was 60% and 50% at 1,000 ppm. Xanthine oxidase inhibition effect of ethanol extract showed more than 80% at 500 ppm. Tyrosinase inhibition and inhibition melanin synthesis activities were measured in 40% and 50% at 1,000 ppm and 100 ppm. Elastase and collagenase inhibition rate of ethanol extracts DISG 40% and 80% at 1,000 ppm. It was concluded that compositive ingredients (Persicae Seman, Glycyrrhizae Radix, Cinnamomi Ramulus, Rhei Rhizoma) influenced the most results. Conclusions : The results indicated that, ethanol extract which is superior in its anti-oxidative and anti-aging effects is useful to be applied in herbal cosmetic industry.