• Title/Summary/Keyword: Inhibitory Activity

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Antioxidant and Xanthine Oxidase Inhibitory Activities of Hot Water Extracts of Medicinal Herbs (한약재 열수추출물의 항산화 활성 및 Xanthine Oxidase 저해 활성)

  • Shin, Yu-Jin;Hwang, Jeong-Man;Lee, Seung-Cheol
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.42 no.10
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    • pp.1712-1716
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    • 2013
  • In our study, as many as 29 edible medicinal herbs were selected for testing their ability in the effective treatment of gout based on oriental medicine theory. We extracted each medicinal herb (135 g) with 4 L of distilled water at $100{\sim}105^{\circ}C$ for 210 min. Thereafter, we evaluated both the antioxidant and xanthine oxidase inhibition activities of the extracts obtained. Among all the edible medicinal herbs used in our study, only the extract from Scutellaria baicalensis Georgi (Korean name: hwang-geum) showed (1) the maximum total phenolic content (TPC) (2.25 mg gallic acid equivalent/mL), (2) DPPH radical scavenging activity (94.04%), and (3) xanthine oxidase inhibition activity (87.75%). We also observed that TPC was relatively highly correlated with both the DPPH radical scavenging activity (r=0.63) and xanthine oxidase inhibition activity (r=0.77). Our results suggest that S. baicalensis G. may be a potent antioxidant source for the extraction and development of nutraceuticals that may be utilized for effective treatment of gout.

The Effects of Donepezil, an Acetylcholinesterase Inhibitor, on Impaired Learning and Memory in Rodents

  • Shin, Chang Yell;Kim, Hae-Sun;Cha, Kwang-Ho;Won, Dong Han;Lee, Ji-Yun;Jang, Sun Woo;Sohn, Uy Dong
    • 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.

Identification and Characterization of Fibrinolytic Compound from Cornus officinalis S. et Z (산수유(Cornus officinalis)로부터 혈전용해물질의 확인 및 특성 연구)

  • Kim, Jun-Ho
    • Korean Journal of Plant Resources
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    • v.33 no.4
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    • pp.237-244
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    • 2020
  • The objective of this study was to identify and characterize fibrinolytic compound from Cornus officinalis. Cornus officinalis. Hot water extract was fractionated into hexane, chloroform, ethyl acetate, butanol, and water fractions. Assays for fibrinolytic activity indicated that only the ethyl acetate fraction had significant efficacy at 1.36 plasmin units/mL. Isolation of fibrinolytic compound was carried out on Amberlite IRA-400, Sephadex LH-20 and active charcoal column chromatography. HPLC analysis of the purified fibrinolytic compound showed retention time (RT) same as authentic malic acid. LC / MS / MS in negative mode showed the same peak at m/z 133, confirming that the purified compound was malic acid with a molecular weight 134 Da. The compound showed fibrinolytic activity of 0.69 plasmin units/mL, 14.62% of thrombin inhibitory activity, 6.42% of antioxidative activity, and 17.28% of α-glucosidase inhibitory activity. The purified compound hydrolyzed γ subunits of human fibrinogen. In conclusion, malic acid isolated from Cornus officinalis might have potential to be developed as ingredient for biofunctional foods to prevent cardiovascular diseases.

Inhibitory Effect of Water Extract of Adenophorae Radix on the Melanogenesis (사삼 물 추출액의 멜라닌 형성 억제 효과)

  • Kang Hyun-sung;Lim Hong-jin;Park Min-chul;Lim Kyu-sang;Kim Nam-kwen
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.17 no.1
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    • pp.82-93
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    • 2004
  • Recently many efforts were focused to understanding the mechanical insights of melanogenesis to develop the agents for hyper-pigmentation and hypo-pigmentation. In the melanin biosynthetic pathway, tyrosinase is the rate limiting enzyme, and ${\alpha}$-melanocyte stimulating hormone(MSH) or cAMP-elevating agents stimulate melanogenesis and enhance the melanin synthesis and the tyrosinase activity. The author has analyzed the effects of Radix Trichosanthis on the basal Melanogenic activities of Bl6/F10 mouse melanoma cells, and on the ${\alpha}$-MSH or forskolin-induced melanogenesis. Radix Trichosanthis alone markedly suppressed melanin content and tyrosinase activity in a dose-dependent manner. Pretreatment of the cells with Radix Trichosanthis also suppressed the increase of ${\alpha}$-MSH(10 nM) or forskolin(20 ${\mu}$M)-induced melanin content and tyrosinase activity. The decrease in the tyrosinase activity was paralled by a decrease in the abundance of tyrosinase protein and tyrosinase promoter activity. Pretreatment of the cells with Radix Trichosanthis also inhibited the increase of forskolin(20 ${\mu}$M) induced the amount of tyrosinase protein and tyrosinase promoter activity. The results of DOPA staining revealed that pretreatment of the cells with Radix Trichosanthis showed less intensity than B16 melanoma cells stimulated with ${\alpha}$-MSH or forskolin. These results suggest that Radix Trichosanthis inhibits melanogenesis and abrogates ${\alpha}$-MSH and cAMP-induced melanogenesis in B16 melanoma cells.

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Functional Properties of Korean Atractylodes japonica Koidz (한국산 삽주의 기능성)

  • 강은미;정창호;심기환
    • Food Science and Preservation
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    • v.8 no.1
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    • pp.86-91
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    • 2001
  • To study the availability of the Korean Atractylodes japonica Koidz. as ingredients for functional flood, functional properties of solvent extracts were investigated and the results were followed. Yield was 14.8% by ethanol extraction of fresh Korean A. Japonica and 17.7% by water fraction. Acetone extract and butanol fraction showed stronger activity of the hydrogen donating activities, each of 72.9% and 74.2%, respectively, in fresh Korean A. japonica and methanol extract and butanol fraction showed stronger activity of the nitrite scavenging effects, each of 95.0% and 79.2%. in fresh Korean A. japonica. Among the solvent extacts from fresh Korean a. japonica, extract by methanol showed strong antimicrobial activity in which clear zone showed 20 mm for Bacillus subtilis and 19 mm for Pseudomonas aeruginosa. Butanol fraction derived from methanol extract showed moderate antimicrobial activity : 18 mm clear zone for Bacillus subtilis and Vibrio parahaemolyticus. Minimum inhibitory concentrations of methanol extract and butanol fraction were about 2 mg/disc and 4 mg/disc against gram(+) bacteria and 6 mg/disc against gram(-) bacteria, respectively.

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In Vitro evaluation of lipid accumulation inhibitory effect in 3T3-L1 cell and antioxidant enzyme activity of Codonopsis lanceolata using different solvent fractions

  • Boo, Hee Ock;Park, Jeong Hun;Kim, Hag Hyun;Kwon, Soo Jeong;Lee, Moon Soon
    • Proceedings of the Korean Society of Crop Science Conference
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    • 2017.06a
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    • pp.292-292
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    • 2017
  • This study was conducted to evaluate the effect of anti-obesity and antioxidant enzyme activities in vitro by different solvent fractions from the roots of Codonopsis lanceolata. The cytotoxicity of different solvent fractions of C. lanceolata on 3T3-L1 preadipocytes were evaluated using the MTT assay, the rate of cell survival progressively decreased in a dose-dependent manner. Butyl alcohol fraction at $200{\mu}g/mL$ exhibited a pronounced cytotoxic effect (75.73%) on 3T3-L1 cell comparable to that of the hexane fraction (79.82%), methylene chloride fraction (84.02%), ethyl acetate fraction (87.62%) and DW fraction (86.30%) at the same concentration. The Oil Red O solution was used to determine whether different solvent fractions of C. lanceolata induce adipocyte differentiation in 3T3-L1 preadipocytes. Confluent 3T3-L1 cells were treated with $50{\mu}g/mL$ concentration of solvent fraction extracts from C. lanceolata. Inhibitory degree of lipid accumulation against solvent fraction extracts showed a significant level compared with the control. Both lipid accumulation and adipocyte differentiation showed relatively high effect on methyl chloride fraction. The root extract of C. lanceolata had the highest SOD enzyme activity of 84.5% in ethyl acetate partition layer and while water partition layer of diploid showed the lowest SOD enzyme activity of 57.9%. The activity of CAT, APX and POD showed a significantly higher activity in ethyl acetate partition layer compared with the other fraction. These results suggested that the roots of C. lanceolata may assist in the potential biological activity on anti-obesity and antioxidant capacity.

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Investigation of Antimicrobial Activity of Brown Algae Extracts and the Thermal and pH Effects on Their Activity

  • Lee, So-Young;Kim, Jin-Hee;Song, Eu-Jin;Kim, Koth-Bong-Woo-Ri;Hong, Yong-Ki;Lim, Sung-Mee;Ahn, Dong-Hyun
    • Food Science and Biotechnology
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    • v.18 no.2
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    • pp.506-512
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    • 2009
  • The antimicrobial activity of water and ethanol extracts from 30 species of algae was measured using the agar diffusion method and minimum inhibitory concentration (MIC) test. In agar diffusion method, the 95% ethanol extracts from 12 of the algae showed growth inhibition against the tested microorganisms. In particular, Ishige okamurai, Ecklonia stolonifera, Sargassum siliquastrum, Sargassum thunbergii, Colpomenia bullosa, and Ecklonia cava had strong antibacterial activities against Gram-positive bacteria at 4 mg/mL. In the results of the MIC test, S. siliquastrum showed the most antimicrobial activity, where its MIC values ranged from 0.005 to 0.0075% against Listeria monocytogenes, Clostridium perfringens, and Basillus subtilis. In the thermal stability test, for the ethanol extracts of I. okamurai, E. cava, S. siliquastrum, S. thunbergii, and C. bullosa, the extracts proved to maintain high antimicrobial activities when they were treated at $121^{\circ}C$ for 15 min. In the pH stability test, the antimicrobial activity of the S. siliquastrum ethanol extract was stable from pH 2 to 10, whereas the activity of the other species ethanol extracts were weakened under pH 10 against several microbes.

Antimicrobial Activity and Total Polyphenol Content of Extracts from Artemisia capillaris Thunb· and Artemisia iwayomogi Kitam· Used as Injin (인진(茵蔯)으로 쓰이는 사철쑥과 더위지기 추출물의 항미생물활성 및 total polyphenol함량)

  • Seo, Kyoung-Sun;Yun, Kyeong-Won
    • Korean Journal of Plant Resources
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    • v.24 no.1
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    • pp.10-16
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    • 2011
  • We investigated the antimicrobial activity of ether and ethylacetate fractions from Artemisia capillaris and Artemisia iwayomogi used as Injin. The antimicrobial activity of the ethylacetate fractions from Artemisia capillaris and Artemisia iwayomogi for tested microbes were stronger than those of ether fractions of the two Artemisia plants. The antimicrobial activity of fractions of Artemisia iwayomogi was higher than that of fractions of Artemisia capillaris for the tested microbes. The extracts of young shoots and leaves showed stronger antimicrobial activity than those of young leaves. The range of minimum inhibitory concentrations(MICs) of ethylacetate fractions from the part of Artemisia capillaris and Artemisia iwayomogi were 0.25~2.0 mg/ml. The MICs of ether fractions were showed higher concentration than those of ethylacetate fractions. The fractions of Artemisia iwayomogi showed lower MICs than fractions of Artemisia capillaris. The highest total polyphenol content was found in young shoots and leaves of A. capillaris. The young shoots and leaves of the two kinds of Artemisia plants showed higher content of total polyphenol.

Effects of NaCl and Organic Acids on the Antimicrobial Activity of Chitosan (키토산의 항균활성에 미치는 염화나트륨 및 유기산의 영향)

  • Hong, Yi-Fan;Kim, Hangeun;Bang, Myun-Ho;Kim, Hyun-Su;Kim, Tae-Rack;Park, Yun-Hee;Chung, Dae-Kyun
    • Microbiology and Biotechnology Letters
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    • v.42 no.4
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    • pp.413-416
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    • 2014
  • The antibacterial activity of chitosan against Escherichia coli and Staphylococcus aureus was investigated in the presence of NaCl, acetic acid, lactic acid, and citric acid to assess its potential use as a food preservative. The inhibitory activity of chitosan decreased slightly upon adding NaCl to culture broth containing 100 ppm of chitosan (MW 3,000), while adding acetic acid, lactic acid, or citric acid enhanced the inhibitory activity of chitosan on growing cells. Our results indicate that food components, such as NaCl, acetic acid, lactic acid, and citric acid, can significantly affect the bactericidal activity of chitosan.

Chemical Constituents of the Root of Dystaenia takeshimana and Their Anti-Inflammatory Activity

  • Kim, Ju-Sun;Kim, Jin-Cheul;Shim, Sang-Hee;Lee, Eun-Ju;Jin, Wen-Yi;Bae, Ki-Hwan;Son, Kun-Ho;Kim, Hyun-Pyo;Kang, Sam-Sik;Chang, Hyeun-Wook
    • Archives of Pharmacal Research
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    • v.29 no.8
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    • pp.617-623
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    • 2006
  • In our ongoing search for bioactive compounds originating from the endemic species in Korea, we found that the hexane and EtOAc fractions of the MeOH extract from the root of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5- lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin $D_2\;(PGD_2)$ and leukotriene $C_4\;(LTC_4)$ in mouse bone marrow-derived mast cells. By activity-guided fractionation, five coumarins, viz. psoralen (2), xanthotoxin (3), scopoletin (4), umbelliferone (5), and (+)-marmesin (6), together with ${\beta}-sitosterol$ (1), were isolated from the hexane fraction, and two phenethyl alcohol derivatives, viz. 2-methoxy-2-(4'-hydroxyphenyl)ethanol (7) and 2-hydroxy-2-(4'-hydroxyphenyl)ethanol (8), three flavonoids, viz. apigenin (9), luteolin (10), and cynaroside (11), as well as daucosterol (12) were isolated from the EtOAc fraction using silica gel column chromatography. In addition, D-mannitol (13) was isolated from the BuOH fraction by recrystallization. Two of the coumarins, scopoletin (4) and (+)- marmesin (6), the two phenethyl alcohol derivatives (7, 8) and the three flavonoids (9-11) were isolated for the first time from this plant. Among the compounds isolated from this plant, the five coumarins as well as the three flavonoids showed COX-2/5-LOX dual inhibitory activity. These results suggest that the anti-inflammatory activity of D. takeshimana might in part occur via the inhibition of the generation of eicosanoids.