• Title/Summary/Keyword: Inhibitory Activity

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Tyrosinase Inhibitory Phenolic Constituents of Smilax china Leaves (청미래덩굴 잎의 페놀성 성분 및 Tyrosinase 저해 활성)

  • Kim, Sang Hyun;Ahn, Jong Hoon;Jeong, Ji Yeon;Kim, Seon Beom;Jo, Yang Hee;Hwang, Bang Yeon;Lee, Mi Kyeong
    • Korean Journal of Pharmacognosy
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    • v.44 no.3
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    • pp.220-223
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    • 2013
  • In the course of screening tyrosinase inhibitory activity, total methanolic extract and EtOAc-soluble fraction of Smilax china leaves showed significant inhibitory activity. Further fractionation and isolation of the EtOAc-soluble fraction resulted in 12 phenolic compounds, which were identified as 4-hydroxybenzoic acid (1), 3,4-dihydroxybenzaldehyde (2), 3,4-dihydroxybenzoic acid (3), 3,4-dihydroxyacetophenone (4), 3-hydroxy-4-methoxy benzoic acid (5), trans-p-hydroxycinnamic acid (6), cis-p-hydroxycinnamic acid (7), trans-resveratrol (8), cis-resveratrol (9), dihydroresveratrol (10), moracin M (11) and kaempferol (12). Compounds 1-11 were first reported from this plant. Among the isolated compounds, compounds 2, 8, 9 and 12 showed strong inhibition on tyrosinase activity.

Tyrosinase Inhibition Activity of Some Herbal Drugs (수종 생약의 티로시나제 억제효과)

  • Park, Jeong-Hill;Shin, Young-Geun;Shin, Un-Kyung;Baek, Sun-Kyung;Lee, Seung-Ki;Chung, Myung-Hee;Park, Young-In
    • YAKHAK HOEJI
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    • v.41 no.4
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    • pp.518-523
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    • 1997
  • To isolate biologically active compounds which exhibit tyrosinase inhibition activity and ultimately express skin whitening effect, 14 oriental herbal drugs were screened in ter ms of tyrosinase inhibition. For this purpose, in vitro enzyme assay system for tyrosinase, so called Pomerantz method with some modifications has been established. Crude methanolic extracts from 14 herbal drugs were made and examined for their inhibitory activity against tyrosinase. Those extracts from Cnidii Rhizoma, Arecae Semen, Caryophylli Flos, and Ephedrae Herba showed strong inhibitory activities on mushroom tyrosinase. Therefore, crude methanolic extracts from those 4 herbal drugs were further fractionated using ether, butanol and water. respectively. The ether and n-butanol extracts from Arecae Semen and the n-butanol and water extracts from Caryophylli Flos, respectively, showed relatively strong tyrosinase inhibitory activity compared to arbutin.

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Antioxidant and Cholinesterase Inhibitory Activities of Antarctic Krill Eupausia superba

  • Yoon, Na-Young;Xie, Chengliang;Shim, Kil-Bo;Kim, Yeon-Kye;Lee, Doo-Seog;Yoon, Ho-Dong
    • Fisheries and Aquatic Sciences
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    • v.14 no.4
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    • pp.289-293
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    • 2011
  • The antioxidant and cholinesterase inhibitory activities of methanol, pretanol, and acetone extracts of Eupausia superba were investigated and their bioactivities compared. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis[3-ethylbenzthiazoline-6-sulfonic acid] ($ABTS^+$) radical-scavenging activities and reducing power assays were used to determine antioxidant activities, and Ellman's colorimetric methods were applied to evaluate cholinesterase inhibitory activity. Although all extracts were positive, Acetone extract of E. superba showed the highest activities. However, these showed moderate or no inhibitory activity against butyrylcholinesterase. Moreover, the total carotenoid contents of the organic solvent extracts followed the same order as their antioxidant and acetylcholinesterase inhibitory activities. These results suggest that E. superba is a potential source of natural antioxidants and cholinesterase inhibitors.

Structural Features of Polyphenolic Compounds in Their NO Inhibitory Activities

  • Kim, Byung-Hun;Lee, Yong-Gyu;Kim, Tae-Woong;Cho, Jae-Youl
    • Biomolecules & Therapeutics
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    • v.17 no.1
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    • pp.79-85
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    • 2009
  • Polyphenolic compounds are reported to have various pharmacological activities such as anti-oxidative, anti-cancerous, anti-inflammatory and anti-aging effects. Although numerous papers explore their functional roles in many different cellular actions, not many studies handle their structural features in anti-inflammatory responses. In this study, therefore, we examined structural role of substituted transstilbenes in their NO inhibitory and NF-${\kappa}B$ suppressive activities. Of 10 compounds tested, 4 compounds (cinnamic acid, resveratrol, piceatannol and curcumin) displayed NO inhibitory activities in a dose-dependent manner. Similarly, these compounds blocked LPS-induced cytotoxicity of RAW264.7 cells. All NO inhibitory compounds also inhibited $I{\kappa}B{\alpha}$ phosphorylation, a hallmark for NF-${\kappa}B$ activation. However, these inhibitory compounds exhibited distinct suppressive pattern in tumor necrosis factor (TNF)-${\alpha}$- or phorbol-12-myristate-13-acetate (PMA)-induced NF-${\kappa}B$ and AP-1 activation. According to structure-activity relationship study, polarity and size of ring B seem to be important for diminishing NO production. Therefore, our data suggest that substituted trans-stilbenes can be developed as novel anti-inflammatory drug or further developed as lead compounds for another improvement.

Storage Stability of the Synthetic Angiotensin Converting Enzyme (ACE) Inhibitory Peptides Separated from Beef Sarcoplasmic Protein Extracts at Different pH, Temperature, and Gastric Digestion

  • Jang, Ae-Ra;Jo, Cheo-Run;Lee, Moo-Ha
    • Food Science and Biotechnology
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    • v.16 no.4
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    • pp.572-575
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    • 2007
  • The angiontensin converting enzyme (ACE) inhibitory peptides were separated from beef sarcoplasmic protein extract and their amino acid sequences were identified as GFHI, DFHINQ, FHG, and GLSDGEWQ. The 4 peptides were synthesized in a laboratory and the ACE inhibitory activities of pep tides was measured after 2 months of storage at $4^{\circ}C$ under different pH conditions (6.0, 6.5, 7.0, 7.5, and 8.0) and the exposure of different temperatures (70, 80, 90, and $100^{\circ}C$) for 20 min to evaluate industrial use. No significant difference was detected by pH and temperature abuse for 20 min during storage. When the synthetic peptides were digested by pepsin, trypsin, and chymotrypsin, the ACE inhibitory activity was not changed. These results indicated that the 4 synthetic peptides with ACE inhibitory activity were pH-stable, heat-stable, and resistant to proteinases in gastro-intestinal tracts. Therefore, those 4 peptides can be used as a source for functional food product with various applications.

Inhibitory Effect of 7-O-butyl Naringenin on Growth of Helicobacter pylori ATCC 26695

  • Kim, Kee-Tae;Moon, Sun-Hee;Yeo, Eun-Ju;Park, Yong-Sun;Han, Ye-Sun;Nah, Seung-Yeol;Lee, Na-Gyong;Paik, Hyun-Dong
    • Food Science and Biotechnology
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    • v.15 no.3
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    • pp.466-468
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    • 2006
  • The antimicrobial effect of a novel flavonoid (7-O-butyl naringenin) on Helicobacter pylori ATCC 26695 and its inhibitory effects on the urease activity of the strain were evaluated by comparing with quercetin and naringenin. H. pylori was cultured with brain heart infusion supplemented with 5% horse serum at $37^{\circ}C$ under 10% $CO_2$ atmosphere and the inhibitory effects of flavonoids against the strain were detected using micro-plate methods. During 12 hr of incubation time, the optical densities of phenol red reduced (pink color) in the urea broth by producing ammonia were detected at 560 nm with a spectrophotometer. The results indicated that both quercetin and 7-O-butyl naringenin were effective against the growth of H. pylori. Moreover, inhibitory effect of 7-O-butyl naringenin on the growth of H. pylori was about two-fold higher than quercetin at the same concentration. With regard to H. pylori urease activity, 7-O-butyl naringenin had a greater inhibitory effect than did naringenin or quercetin at the same concentration.

Inhibitory Activitv of (1,3-Dioxolan-2-yl and Dioxan-2-yl)methylaminium Derivatives against Acetylcholinesterase (Acetylcholinesterase에 대한 (1,3-Dioxolan-2-yl 및 Dioxan-2-yl)methylaminium유도체의 저해 작용)

  • Phi, Taek-San;Kim, Yun-Bae;Kim, Jee-Cheon;Cho, Young;Sok, Dai-Eun;Cha, Seung-Hee;Seo, Won-Jun
    • YAKHAK HOEJI
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    • v.38 no.5
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    • pp.511-515
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    • 1994
  • We examined the inhibitory activity of (1,3-dioxolan-2-yl and 1,3-dioxan-2-yl)methylaminium derivatives(A; 1-8) against acetylcholinesterase. Derivatives of six-membered 1,3-dioxane exhibited more potent inhibitory effect than corresponding 5-membered 1,3-dioxolanes. The presence of methyl group at C4 position of dioxane ring was effective to increase the inhibitory potency of heterocyclic analogues. The activity of N-phenacyl-aminiums was greater than that of N,N,N-trimethyl-aminiums. In general, the terminal methyl group on 1,3-dioxane ring and the phenacyl group in ammonium compound A were assumed to be important factors to enhance the inhibitory action.

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Inhibitory effect of Fucofuroeckol-A from Eisenia bicyclis on tyrosinase activity and melanin biosynthesis in murine melanoma B16F10 cells

  • Shim, Kil Bo;Yoon, Na Young
    • Fisheries and Aquatic Sciences
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    • v.21 no.11
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    • pp.35.1-35.7
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    • 2018
  • Background: The aim of this study was to investigate the in vitro inhibitory effects of Fucofuroeckol-A isolated from Eisenia bicyclis against tyrosinase activity and 3-isobutyl-1-methylxanthine (IBMX)-induced melanin biosynthesis in B16F10 melanoma cells. Result: Among the ethanolic (EtOH) extract of E. bicyclis and its organic solvent fractions, the ethyl acetate (EtOAc) soluble fraction showed a noticeable inhibitory effect on mushroom tyrosinase with an $IC_{50}$ value of $37.6{\pm}0.1{\mu}g/mL$. Repeated column chromatography of the active EtOAc fraction resulted in the isolation of Fucofuroeckol-A. It evidenced more potent tyrosinase inhibitory effect with an $IC_{50}$ value of $11.4{\pm}1.4{\mu}M$ than arbutin ($IC_{50}=1076.6{\pm}44.3{\mu}M$), which was used as a positive control. Lineweaver-Burk plots suggest that Fucofuroeckol-A plays as a noncompetitive inhibitor against tyrosinase. Furthermore, we have evaluated the inhibitory effects of Fucofuroeckol-A on IBMX-induced melanin formation in B16F10 melanoma cells. Fucofuroeckol-A ($12.5-100{\mu}M$) exhibited a significant inhibition of melanin production in the melanoma cells. Conclusion: In the present study, we suggested that Fucofuroeckol-A might prove possibility as a novel inhibitor of melanin biosynthesis in cosmetic applications.

BIOLOGICAL EFFECT OF MAGNOLIA AND GINKGO BILOBA EXTRACT TO THE ANTIMICROBIAL, ANTIINFLAMMATORY AND CELLULAR ACTIVITY (후박 및 은행잎 추출물의 향균, 향염 및 세포활성도에 미치는 영향)

  • Chung, Chong-Pyuong;Ku, Young;Bae, Ki-Hwan
    • Journal of Periodontal and Implant Science
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    • v.25 no.3
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    • pp.478-486
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    • 1995
  • Periodontal therapy for treatment of periodontitis involves the elimination of bacterial plaque and elimination of the anatomic defects by regenerative procedure. The purpose of this study was to evaluate on the biological effect of magnolia and Ginkgo biloba extract to the antimicrobial, antiinflammatory and cellular activity. Antimicrobial assay was performed with the diffusion method of the extract by measuring of growth inhibitory zone of B. cereus from blood agar plate. Effect of the extract to cellular activity of gingival fibroblast were examined using MTT method and measured the result with optical density on 570nm by ELISA reader. Inhibitory effects of $PGE_2$ production from gingival fibroblast was performed with the addition of $IL-l{\beta}$ and the extract to the well and examined to the product of $PGE_2$ from cell by ELISA reader. In vivo anti-inflammatory effect was performed with injection examined with clinically and histologically for their extent of mecrosis and inflammation. Antimicrobial activity of Magnolia extract showed significantly higher activity than that of control. However, GBE did not showed significant activity to compare with control, and mixture of Magnolia and GBE extract showed significantly higher activity than that of control. The effect of cellular activity to gingival fibroblast showed no significant differences of between control and Magnolia extract. However, GBE showed significantly higher rate of cellular activity to compare with control and even to PDGF-BB, and also showed same degree of cellular activity even though mixed with Magnolia extract. The inhibitory effect of $PGE_2$ production showed significantly reduction of $PGE_2$ production to compare with control, but its inhibitory effect was not much strong to compare with Indomethacin. In vivo, antiinflammatory effect of Magnolia extract to P. gingivalis injection of Hamster buccal check showed significantly reduction of inflammatory cell infiltration and tissue necrosis, but GBE showed no effect on the inhibition of inflammatory process. These results suggested that Magnolia and GBE extract possessed different kind of biological activity and also can be compensated on their activity with each other for elimination of bacterial plaque and anatonical defect.

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Physiological Activities of Hot Water Extracts from Ecklonia cava Kjellman (감태 열수 추출물의 생리활성)

  • Cho, Eun-Kyung;Choi, Young-Ju
    • Journal of Life Science
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    • v.20 no.11
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    • pp.1675-1682
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    • 2010
  • The biological activity of hot water extract from Ecklonia cava Kjellman (ECE) was investigated to assess antioxidative, anti-skin aging, and nitrite scavenging abilities, as well as alcohol metabolizing activities. Antioxidant activity of ECE was measured by using 2,2-diphenyl-1-picryl-hydrazyl (DPPH) radical scavenging activity and superoxide dismutase (SOD)-like activity. DPPH radical scavenging activity and SOD-like activity of ECE increased in a remarkably dose-dependent manner, and were about 91.4% and 75% at 1 mg/ml, respectively. The xanthine oxidase inhibitory activity was indicated to be about 70% at 1 mg/ml of ECE. Nitrite scavenging ability of ECE showed to be 93.6% at 1 mg/ml and pH 1.2. The influence of ECE on alcohol metabolism was demonstrated through the generating activity of reduced-nicotinamide adenine dinucleotide (NADH) by alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH). The facilitating rate of ADH and ALDH activity by ECE was 167.2% and 334% at 10 mg/ml, respectively. In addition, tyrosinase and elastase inhibitory activities of ECE were 58% and 72% at 10 mg/ml, respectively. These results indicated that ECE has valuable biological attributes owing to its antioxidant, nitrite scavenging, alcohol metabolizing, and elastase and tyrosinase inhibitory activities.