• Title/Summary/Keyword: Inhibitory Activity

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Screening of Inhibitory Effect of Edible Mushrooms on Tyrosinase and Isolation of Active Component (한국산 식용버섯류의 Tyrosinase 활성 저해 검색 및 그 유효성분 분리)

  • 박영현;장성근
    • Journal of Food Hygiene and Safety
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    • v.12 no.3
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    • pp.195-199
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    • 1997
  • For the purpose of isolation and screening of tyrosinase inhibitory activity from edible mushrooms, Pleurotus ostreatus, Auricularia auricula-Judae, Umbilicaria esculenta, Agaricus bisporus, Flammuline velutipes, Lentinus edodes, Ganoderma lucidum, and Coriouls versicolor were examined by tracing inhibitory activities against tyrosinase, utilizing L-3,4-dihydroxyphenylalanine (L-DOPA) as a substrate. Among the eight edible mushrooms tested, Umbilicaria esculenta showed potent enzyme inhibitory activities above 7804% against tyrosinase in ethylacetate (EtOAc) extracts. Ganoderma lucidum and Agaricus bisporus showed inhibitory activities of 67.3% and 51.5% in water extracts. EtOAc extracts of Umbilicaria esculenta was fractionated from silicagel column chromatography and one fraction showed the most inhibitory activity of 60.9%. The three bands (Rf=0.38, 0.27, 0.19) were isolated from preparative TLC of the fraction for purification and identified as mixtures of orsellinate, methyl orsellinate, methyl lecanorate, and methyl gyrophorate by high pressure liquid chromatography (HPLC), ultravisible spectrophotometer (UV), mass spectrophotometer (Mass), nuclear magnetic resonance spectrometer (NMR).

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Antioxidative Activity and Tyrosinase Inhibition Effect of Ethanol Extract and Its Fractions from the Branch of Rhododendron schlippenbachii (철쭉 가지 에탄올 추출물 및 용매별 분획물의 항산화 활성과 Tyrosinase 저해 활성)

  • Im, Do Youn;Lee, Kyoung In
    • Korean Journal of Medicinal Crop Science
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    • v.21 no.6
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    • pp.439-443
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    • 2013
  • This study was conducted to investigate the antioxidative activity and tyrosinase inhibitory activity of 50% ethanol extract and its fractions from the branch of Rhododendron schlippenbachii. In DPPH radical scavenging ability, butanol and ethyl acetate fractions showed 59.98% and 55.17% of relative activity compared with positive control (ascorbic acid), but the 50% ethanol extract showed relatively low activity. In nitric oxide (NO) scavenging ability, the ethyl acetate and butanol fractions showed 141.80% and 131.55% relative activity compared with ascorbic acid as used for positive control. On the other hand, tyrosinase inhibitory activity of the ethyl acetate and butanol fractions showed about twice higher activity than positive control (arbutin). It means that the ethyl acetate and butanol fractions from the extract of R. schlippenbachii branch has ability for used as effective radical scavenger and tyrosinase inhibitor.

A new Potential Anti-inflammatory Agent

  • Kim, Hee-Kee;Son, Kun-Ho;Chang, Hyeun-Wook;Kang, Sam-Sik;Kim, Hyun-Pyo
    • Archives of Pharmacal Research
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    • v.21 no.4
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    • pp.406-410
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    • 1998
  • Biflavonoid is one of unique classes of naturally-occurring bioflavonoids. Certain biflavonoids including amentoflavone were previously reported to have inhibitory effect on the group 11 phospholipase $A_2$ activity. Amentoflavone was also found to inhibit cyclooxygenase from guinea-pig epidermis without affecting lipoxygenase. In this study, anti-inflammatory and analgesic activities of amentoflavone were evaluated. When amentoflavone was administered intraperitoneally, it showed a potent anti-inflammatory activity as determined by amelioration of croton-oil induced mouse ear edema. It also showed a potent anti-inflammatory activity in the rat carrageenan paw edema model ($ED_{50}$=42 mg/kg) compared to the activity of prednisolone (35 mg/kg) and indomethacin (10 mg/kg). However, amentoflavone did not show a significant inhibitory activity against rat adjuvant-induced arthritis, a chronic inflammatory model. In addition, amentoflavone was found to possess a potent analgesic activity in the acetic acid writhing test ($ED_{50}$=9.6 mg/kg) compared to the activity of indomethacin (3.8 mg/kg). These results suggest that amentoflavone may be a potential lead for a new type of anti-inflammatory agents having dual inhibitory activity of group 11 phospholipase $A_2$ and cyclooxygenase.

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Differential Effects of Tautomycetin and Its Derivatives on Protein Phosphatase Inhibition, Immunosuppressive Function and Antitumor Activity

  • Niu, Mingshan;Sun, Yan;Liu, Bo;Tang, Li;Qiu, Rongguo
    • The Korean Journal of Physiology and Pharmacology
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    • v.16 no.2
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    • pp.145-151
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    • 2012
  • In the present work, we studied the structure-activity relationship (SAR) of tautomycetin (TMC) and its derivatives. Further, we demonstrated the correlation between the immunosuppressive fuction, anticancer activity and protein phosphatase type 1 (PP1) inhibition of TMC and its derivatives. We have prepared some TMC derivatives via combinatorial biosynthesis, isolation from fermentation broth or chemical degradation of TMC. We found that the immunosuppressive activity was correlated with anticancer activity for TMC and its analog compounds, indicating that TMC may home at the same targets for its immunosuppressive and anticancer activities. Interestingly, TMC-F1, TMC-D1 and TMC-D2 all retained significant, albeit reduced PP1 inhibitory activity compared to TMC. However, only TMC-D2 showed immunosuppressive and anticancer activities in studies carried out in cell lines. Moreover, TMC-Chain did not show any significant inhibitory activity towards PP1 but showed strong growth inhibitory effect. This observation implicates that the maleic anhydride moiety of TMC is critical for its phosphatase inhibitory activity whereas the C1-C18 moiety of TMC is essential for the inhibition of tumor cell proliferation. Furthermore, we measured $in$ $vivo$ phosphatase activities of PP1 in MCF-7 cell extracts treated with TMC and its related compounds, and the results indicate that the cytotoxicity of TMC doesn't correlate with its $in$ $vivo$ PP1 inhibition activity. Taken together, our study suggests that the immunosuppressive and anticancer activities of TMC are not due to the inhibition of PP1. Our results provide a novel insight for the elucidation of the underlying molecular mechanisms of TMC's important biological functions.

Inhibitory Effects of Herbal Extracts on Dopa Oxidase Activity of Tyrosinase

  • Shin, Nam-Ho;Lee, Kyong-Soon;Kang, Seh-Hoon;Min, Kyung-Rak;Lee, Seung-Ho;Kim, Young-Soo
    • Natural Product Sciences
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    • v.3 no.2
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    • pp.111-121
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    • 1997
  • Tyrosinase catalyzes the rate-limiting steps in melanin biosynthesis which is involved in skin-coloring and local hyperpigmentation of human beings, and unfavorable darkening of food products, Inhibitory effects on 3,4-dihydroxy-phenylalanine (dopa) oxidase activity of tyrosinase by 594 kinds of herbal extracts prepared from herbal medicines and wild plants in Korea were estimated. Two herbal extracts prepared from radicis cortex of Morus alba and rhizoma of Curcuma longa were selected as those exhibiting potent inhibitory effects on the enzyme activity. These herbal extracts were subjected to sequential fractionations with methylene chloride, ethyl acetate, n-butanol, and polar residue. The inhibitory effects on dopa oxidase activity of tyrosinase were shown in ethyl acetate fraction of Morus alba, and in methylene chloride fraction of Curcuma langa. The ethyl acetate fraction of Marus alba exhibited 50% of inhibition on dopa oxidase activity of tyrosinase at the concentration of 12 ${\mu}g/ml$, and methylene chloride fraction of Curcuma langa at 51 ${\mu}g/ml$.

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Enzymological Evaluation of Bowel Inflammation Inhibitory Activity and Intestinal Microbial Flora Improvement by Enzymatic Hydrolysate of Schizandrae Fructus (오미자 효소가수분해물에 의한 장내 세균총 개선 및 장관 염증 억제 효과의 효소학적 평가)

  • Ryu, Il-Hwan;Kwon, Tae-Oh;Lee, Kang-Soo;Yun, Yong-Gab
    • Korean Journal of Pharmacognosy
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    • v.38 no.4
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    • pp.363-371
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    • 2007
  • Schizandrae Fruits has been used as a traditional Oriental medicine for treatment of many stress-induced diseases. In the present study, we investigated inhibitory activity of enzymatic hydrolysate of Schizandrae fructus (SC-EX) in growth of tested intestinal microorganism and activity of bowel inflammation related enzyme. SC-EX was added to the proteose peptone-yeast extract-fildes (PYF) media to investigation the effect on the growth of type culture of intestinal microorganism. The growth of lactic acid bacteria such as Bifidobacterium species and Lactobacillus species was accelerated by more than 3% concentration of SC-EX. But, growth of harmfulness bacteria such as E.coli, Clostridium sp. Staphylococcus sp. Streptococcus sp. was inhibited by more than 3% concentration of SC-EX. Also, SC-EX was exhibited a concentration-dependent inhibitory activity of the bowel inflammation related enzymes. The SC-EX was showed 76% and 92% inhibitory activity of 5-lipoxygenase and cyclooygenase at 5% additional concentration respectively. Our results indicated that SC-EX may possess improvement effect on the intestinal flora and Anti-inflammatory effect on the bowel.

Inhibition of Experimental Gastric Ulcer by Potato Tubers and the Starch

  • Lee, Jun-Gi;Jin, Jeong-Ho;Lim, Hak-Tae;Choi, Hee-Don;Kim, Hyun-Pyo
    • Natural Product Sciences
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    • v.15 no.3
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    • pp.134-138
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    • 2009
  • In an attempt to establish anti-ulcerogenic activity of potato tubers, inhibitory activity against ethanol- and indomethacin-induced gastric ulcer models in rats was evaluated for the first time. From several varieties of potato tubers including Solanum tuberosum L. cv. Superior (white skin and fresh potato) and two new varieties of (Bora valley and Gogu valley), raw potato juice was prepared and the starch was obtained from each juice by filtration and drying. Upon oral administration to rats, raw potato juice showed more or less inhibitory activity. The starch showed higher and dose-dependent inhibitory activity, suggesting that the active ingredient in raw potato juice may be the starch. Particularly, the starch obtained from the tubers of new potato variety, "Bora valley," with purple color, showed the highest inhibitory activity (62.4% and 37.1% inhibition of ulcer index at 500 mg/kg), while omeprazole (proton pump inhibitor) used as a reference drug showed 74.4% and 75.7% inhibition at 20 mg/kg against ethanol- and indomethacin-induced ulcer formation, respectively. The present study provides a first evidence of anti-ulcerogenicity of raw potato juice and the starch. Especially, the starch from "Bora valley" strongly inhibited ulcer formation in rats. Considering that these are food components, they may be safely used for anti-ulcerogenic nutraceuticals.

Antimicrobial Activity of Elfvingia applanata extract alone and in Combination with Some Antibiotics (Elfvingia applanata 엑스가 수종 항생물질의 항균력에 미치는 병용효과)

  • Kim, Young-So;Rym, Kyo-Hwan;Lee, Chong-Kil;Han, Seong-Sun
    • YAKHAK HOEJI
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    • v.38 no.6
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    • pp.742-748
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    • 1994
  • As part of our search for less toxic antimicrobial agents from natural resources, the carpophores of Elfvingia applanata$(P_{ers}.)K_{ARST}.$ was extracted with hot water. EA, the aqueous extract from the carpophores of E. applanata, was lyophilized and a dark brownish powder was obtained. Antimicrobial activity of EA was tested in vitro against Gram positive and Gram negative bacteria by serial broth dilution method, and the antimicrobial activity was expressed by minimal inhibitory concentration(MIC). Among fourteen species of bacteria tested, the antimicrobial activity of EA was the most potent against Proteus vulgaris showing MIC of 1.250 mg/ml. To investigate the effect of antimicrobial combinations of EA with four kinds of antibiotics(ampicillin, cefazolin, oxytetracycline and chloramphenicol), the fractional inhibitory concentration index(FICI) was determined by checkerboard assay for each strain. The antimicrobial combinations of EA with four kinds of antibiotics resulted in synergism in four instances, but no antagonism was observed. Four instances of synergism were observed when EA was combined with ampicillin against Micrococcus luteus, with cefazolin against Bacillus subtilis, with cefazolin against Micrococcus luteus and with oxytetracycline against Staphylococcus aureus.

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Biological Activities of Low Molecular Weight Substances Fractionated from the Seasoned and Smoked Products of Skipjack Tuna (Euthynus pelamis) (가다랑어 훈연조미제품 유래 저분자물질의 생리활성)

  • LEE Jung Min;CHOI Geun Pyo;WON Moo Ho;KIM Sang Moo
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.38 no.4
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    • pp.219-225
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    • 2005
  • We studied the anticancer, antioxidative, ACE inhibitory, antithrombic, and cerebral ischemia inhibitory activities, of low molecular weight substances fractionated from the seasoned and smoked products of skipjack tuna (Euthynus pelamis). Low molecular weight substances fractionated from the liquid extract of seasoned and smoked skipjack tuna powder showed 7 peaks on gel permeation chromatography. Anticancer activity was the highest at Peak 3 $(54.23%)$ followed by Peak 4 $(41.58\%)$. The potency order of antioxidative activity was the highest at Peak 3 $(94.14\%)$ followed by Peak 2 $(82.07\%)$ and Peak 5 $(81.24\%)$. ACE inhibitory activity was the highest at Peak 3 $(67.27\%)$ followed by Peak 5 $(45.62\%)$. But there was weak anti thrombotic effect (PT and APTT) in the low molecular weight substances of the seasoned and smoked products of skipjack tuna. Cerebral ischemia inhibitory activity was the highest at Peak 3 $(80.0\%)$ followed by Peak 5 $(40.0\%)$.

Studies about Monoamine Oxidase Inhibitory Activities of Korean Green Tea (Teae sinensis L.) Harvested from Different Time and Location

  • Choi, You Jin;Chong, Han-Soo;Kim, Young-Kyoon;Hwang, Keum Hee
    • Natural Product Sciences
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    • v.19 no.4
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    • pp.281-285
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    • 2013
  • This study was designed to investigate the nervous sedative effects of green tea. The sedative effect was evaluated by examination of Monoamine oxidases (MAOs) inhibitory activity in vitro in the brain and liver of rat fed on green tea cultivated and harvested from the different regions and periods. It showed that methanol extracts of green tea inhibited significantly the brain MAO-A activity. Especially late harvested green tea extracts showed potential inhibitory activity. The liver MAO-B activity was also inhibited by all of the green tea extracts with strong intensity. This study confirmed that major compounds of green tea such as catechin, epigallocatechin-3-gallate (EGCG) and L-theanine, which were well known for the main bioactive components in the tea plants, were not associated with the MAO inhibitory activities of green tea. These results suggested that a MAO inhibition activity comes from other minor tea components we have to search in the future.