• Title/Summary/Keyword: enzyme inhibitory

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Inhibitory Effects on Melanin Production in B16 Melanoma Cells of Fallen Pear (B16F10 Melanoma 세포에서 낙과 배 물 추출물의 멜라닌 생성 저해 효과)

  • Shin, Bo Yeon;Jung, Bo Ram;Jung, Jong Gi;Cho, Seung Sik;Bang, Mi Ae
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.46 no.3
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    • pp.320-326
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    • 2017
  • This study investigated the water extracts of fallen pear (FPWE) on tyrosinase activity and melanogenesis. In the present study, we examined the effects of FPWE on mushroom tyrosinase activity in vitro, B16F10 melanoma cell tyrosinase activity, melanin contents, and expression of melanogenic enzyme proteins such as tyrosinase. An apparent down-regulatory effect on tyrosinase activity was observed when B16F10 cells were incubated with FPWE. Results of melanin assay using B16F10 cells treated with different concentrations (50, 125, and $250{\mu}g/mL$) of FPWE showed a dose-dependent decrease in melanin content. To determine whether or not FPWE indirectly affects tyrosinase activity, we assessed mushroom tyrosinase activity upon treatment with various concentrations (125, 250, 500, and $1,000{\mu}g/mL$) of FPWE. In addition, we investigated changes in the protein level of tyrosinase by using Western blotting. Tyrosinase and microphthalmia-associated transcription factor expression levels in B16F10 melanoma cells were reduced in a dose-dependent manner by FPWE. These results suggest that FPWE reduced melanin formation by inhibition of tyrosinase activity. Therefore, we suggest that FPWE could be used an effective whitening agent for skin.

Anti-oxidative and Anti-inflammatory Activities of Desmodium heterocarpon Extract in RAW 264.7 Cells (RAW 264.7 세포에서 Desmodium heterocarpon 추출물의 항산화 및 항염증 활성)

  • Lee, Su Hyeon;Jin, Kyong-Suk;Son, Yu Ri;Kwon, Hyun Ju;Kim, Byung Woo
    • Journal of Life Science
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    • v.28 no.2
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    • pp.216-222
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    • 2018
  • Desmodium heterocarpon is one of vines belongs to Fabaceae family, mainly distributed in Asian countries such as Korea and Japan. This study was conducted to explore new nutraceutical resources from the plant kingdom possessing biological activities. To fulfill this purpose, the anti-oxidative and anti-inflammatory activities of D. heterocarpon ethanol extract (DHEE) were evaluated by 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging activity assay, reactive oxygen species (ROS) scavenging activity assay, nitric oxide (NO) inhibitory activity assay, and the analysis of related protein expressions by Western blot hybridization. DHEE exhibited potent anti-oxidative activity as confirmed by DPPH radical scavenging capacity against DPPH similar with ascorbic acid, a well-known anti-oxidative agent, used as a positive control. DHEE also effectively suppressed hydrogen peroxide ($H_2O_2$)-induced ROS on RAW 264.7 murine macrophage cells. Furthermore, DHEE induced the expression of the anti-oxidative enzyme heme oxygenase 1 (HO-1), and its upstream transcription factor, nuclear factor-E2-related factor 2 (Nrf2) as a dose dependent manner. DHEE inhibited lipopolysaccharide (LPS) induced nitric oxide (NO) formation as a consequence of inducible NO synthase (iNOS) down regulation. Taken together, these results suggest that DHEE has anti-oxidative and anti-inflammatory activities and thus appears to be useful sources as potential anti-oxidant and anti-inflammatory agents. The identification of active compounds that confer biological activities of DHEE might be needed.

The Efficacy of Saururus chinensis on Cervical Cancer Cells : The Inhibitory Effect on the Function of E6 and E7 Oncogenes of HPV Type 16 (삼백초 추출물의 자궁경부암세포 억제 효능)

  • Chung, Yeon-Gu;Lee, Hae-Sook;Lee, Kyung-Ae;Joung, Ok;Oh, Won-Keun;Kim, Kwang-Dong;Lim, Jong-Seok;Moon, Ja-Young;Cho, Yong-Kweon;Park, Sue-Nie;Yoon, Do-Young
    • YAKHAK HOEJI
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    • v.46 no.6
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    • pp.426-432
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    • 2002
  • Cervical cancer is one of the leading causes of female death from cancer worldwide with about 500,000 deaths per year. A strong association between certain human papilloma viruses (HPV type 16 and 18) and cervical cancer has been well known. An extract of Saururus chinensis, named as PE-46, has been used to investigate whether this agent has the ability of inhibiting the oncogenes E6 and E7 of HPV type 16. PE-46 inhibited the proliferation of human cervical cancer cell lines in a dose response manner. PE-46 also inhibited the in vitro binding of E6 and E6AP which are essential for the binding and degradation of the tumor suppressor p53. In addition, PE-46 inhibited the in vitro binding of E7 and Rb which is essential tumor suppressor for the control of cell cycle. The levels of mRNA for E6 and E7 were also decreased by PE-46. SiHa cells treated with PE-46 induced G0/G1 arrest, resulting in inhibition of growth. Our study showed that the PE-46 can inhibit the cervical carcinomas via both inhibition of bindings between oncogenes and tumor suppressors, and inhibition of G1longrightarrowS transition. PE-46 inhibited the oncogenecity of E6 and E7 of HPV 16 type, thus could be used as a putative modulating agent for the treatment of cervical carcinomas caused by HPV.

Effect of Lidocaine on Utilization of Endogenous Substrates for Contractile Process of Isolated Rat Atria (심근 수축에 쓰여지는 내인성 기질 대사에 대한 Lidocaine의 영향)

  • Ko Kye-Chang
    • The Korean Journal of Pharmacology
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    • v.31 no.1 s.57
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    • pp.53-61
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    • 1995
  • The experiments were performed to determine whether the cardiac depressant action of lidocaine is directly associated with the utilization of endogenous substrates in isolated rat atria, by using citrate and bicarbonate-free medium known as potent inhibitors of phosphofructokinases (PFK) enzyme step. Citrate and bicarbonate-free medium produced negative inotropic action of isolated rat atria incubated in normal Krebs-Ringer bicarbonate glucose medium. Pyruvate and acetate increased the force of contraction of atria depressed by citrate or bicarbonate-free medium, whereas fructose was without effect indicating the inhibitory effect of citrate and bicarbonate-free medium at some point in the glycolytic pathway such as the PFK step in atria. In the absence of exogenous substrate, citrate and bicarbonate-free medium produced a marked depression of the force of substrate-depleted atria indicating that utilization of endogenous substrate above the PFK step, probably cardiac glycogen, is also impaired by citrate or bicarbonate-free medium. Lidocaine produced further depression of the contractile force of atria depressed by citrate. These results argue strongly for an additional mechanism of cardiac depression caused by lidocaine involving the sites below the PFK.

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The effect of L-Ascorbic Acid on the Oxidative Reaction of Lysine in Collagen. (Collagen 분자 중의 lysine 산화반응에 미치는 비타민 C의 영향)

  • 김미향
    • Journal of Life Science
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    • v.14 no.3
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    • pp.478-483
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    • 2004
  • In a model reaction using lysyl oxidase purified partilally from bovine aorta, effect of L-ascorbic acid AsA on the oxidative reaction of lysine in collagen was investigated. Addition of Ash to the reaction mixture under aerobic conditions resulted in the decrease of enzymatic activity. In order to examine the specificity of AsA in the oxidative reaction of lysine, other reductants including A derivatives instead of AsA were added to the reaction mixture. Thiol such as glutathione had no effect on the activities of lysyl oxidase. on the other hand, it was observed that erythorbic acid, which was a stereoisomer of AsA, had the same inhibitory effect on this oxidative reaction as AsA. Moreover, by the addition of 3,4-dihydroxybenzoate, which was structural analog of AsA, the activities decreased in a similar manner to that of AsA. These results indicate that the regulatory effect of AsA on lysyl oxidase is attributed to characteristics of the structure. From the determination of Ash remained in the reaction mixture, it is shown that AsA concentration remarkably decreased by lysyl oxidase of the reaction mixture. It is hypothesized that endiol groups reduces the enzyme-bound $Cu^{+2}$ required for further progress of the reaction, and suggests that AsA regulates specifically the reduction of $Cu^{+2}$ required to oxidize lysyl oxidase. This findings support that AsA has an important regulatory role on the oxidative reaction of lysine and on changes of collagen cross-links with aging.

Effects of Rhynchosia molubilis Saponin on Hepatotoxicity and Pathology (간독성과 병리학적인 면에서 노두 사포닌의 효과)

  • Ha Bae-Jin
    • Journal of Life Science
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    • v.16 no.2 s.75
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    • pp.186-191
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    • 2006
  • This study was carried out to investigate the effects of Rhynchosia molubilis saponin on carbon tetrachloride ($CCl_4$)-induced hepatotoxicity. Sprague-Dawley rats were intraperitoneally administered the Rhynchosia molubilis saponin at 100 mg/kg every day for two weeks, then $CCl_4$ (3.3 ml/kg) was injected into rats. 12 hours later, they were anesthesized with ether and dissected. Rhynchosia molubilis saponin-administered group showed 59.92% and 62.28% of inhibitory effects on aspartate aminotransferase (AST) and alanine aminotransferase (ALT) activities compared to $CCl_4$-treated group (p<0.05). Malonedialdehyde (MDA) levels of Rhynchosia molubilis Saponin-administered and $CCl_4$-treated (RSC) group in liver homogenate and mitochondria were significantly inhibited to 61.83%, 81.11 %, respectively, compared to $CCl_4$-treated group (p<0.05). Superoxide dismutase (SOD) activities of RSC group in liver homogenate and mitochondria were significantly inhibited to 66.53%, 31.04%, respectively, compared to $CCl_4$-treated group (p<0.05). GPx activities of RSC group in liver homogenate and mitochondria were significantly inhibited to 72.74%, 72.68%, respectively, compared to $CCl_4$-treated group (p<0.05). The histological examinations showed that the liver cell necrosis and centrilobular congestion aggregation induced by $CCl_4$ were dearly eliminated by the administration of Rhynchosia molubilis saponin. These results suggest that Rhynchosia molubilis saponin could have the protective effects against hepatotoxicity.

Physiological Activity of Medicinal Plant Extracts (생약재 추출물의 생리활성 효과)

  • Na Gyung-Min;Han Ho-Suk;Ye Su-Hyang;Kim Hyun-Ku
    • Food Science and Preservation
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    • v.11 no.3
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    • pp.388-393
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    • 2004
  • The physiological activity of 5 kinds of medicinal plant extracts were examined. Total polyphenol contents showed the highest value in 50 $\%$ ethanol extracts. Electron donating ability showed the highest value in 50 $\%$ ethanol extracts of Glycyrrhiza uralensis. SOD-like activity showed the highest activity in 50$\%$ ethanol extracts of Glycyrrhiza uralensis. Medicinal plant extracts showed the different nitrite scavenging abilities under the different pH conditions. Medicinal plant extracts showed the highest value in nitrite scavenging ability at pH 1.2. The maximum nitrite scavenging effect was found at pH 1.2 and decreased as pH increased. Angiotensin-converting enzyme inhibitory activity showed the highest value in 50 $\%$ ethanol extracts of dried garlic.

Inhibitory Effect of Aqueous Extract from Lonicera japonica Flower on LPS-induced Inflammatory Mediators in RAW 264.7 Macrophages. (금은화 수용성 추출물의 LPS 유도 염증매개물 억제 효과)

  • Yun, Young-Gab;Kim, Gyu-Min;Lee, Sung-Jun;Ryu, Seong-Hun;Jang, Seon-Il
    • The Korea Journal of Herbology
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    • v.22 no.3
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    • pp.117-125
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    • 2007
  • Objective : Lonicera japonica (Caprifoliaceae) has long been used for treatment of infectious diseases in oriental countries. The aim of this study was to investigative the effect by which the aqueous extract from flower of L. japonica (LJFAE) inhibited the lipopolysaccharide (LPS)-induced inflammatory mediators in murine macrophages, RAW 264.7 cells Methods : The dried flowers of L. japonica were extracted with distilled water at $100^{\circ}C$ for 7 h. The extract was filtered through 0.45 ${\mu}m$ filter, freeze-dried. The dried extract was dissolved in Hank's balanced salt solution (HBSS) and filtered through 0.22 ${\mu}m$ filter before use. Accumulated nitrite, an oxidative product of nitric oxide (NO), was measured in the culture medium by the Griess reaction. The levels of prostaglandin E2 (PGE2), tumor necrosis factor-$\alpha$ (TNF-$\alpha$), interleukin-1$\beta$ (IL-1$\beta$), and IL-6 production, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression were measured by enzyme-linked immunosorbent assay and Western blot analysis. Results: LJFAE (10-400 ${\mu}g$/ml) per se had no cytotoxic effect in unstimulated macrophages, but LJFAE concentration-dependently reduced NO, PGE2, TNF-, IL-l, and IL-6 production and COX-2 activity caused by stimulation of LPS. The levels of iNOS and COX-2 protein expressions were markedly suppressed by the treatment with LJFAE in a concentration dependent manner. Conclusions : These results suggest that LJFAE suppress the NO and PGE2production in macrophages by inhibiting iNOS and COX-2 expression and these properties may contribute to the anti-inflammatory activity of Lonicera japonica.

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Kinetic Modeling of the Enzymatic Hydrolysis of $\alpha$-Cellulose at High Sugar Concentration (순수 섬유소에 대한 고농도 당화공정의 동력학적 모사)

  • 오경근;정용섭홍석인
    • KSBB Journal
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    • v.11 no.2
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    • pp.151-158
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    • 1996
  • For the effective ethanol fermentation, the high concentration of sugar as the substrate of microbial fermentation is required. The most important reason in the inefficient hydrolysis; the easy deactivation of enzyme by temperature or shear stress and the severe inhibition effects of its products. In our work, we comprehended the kinetic characteristics of cellulose and ${\beta}$-glucosidase in the progress of hydrolysis, and observed the potential inhibitory effects of the hydrolyzed products and the deactivation of enzymes. We also tried to present the kinetic model of enzymatic hydrolysis of cellulose, which is applicable to process at the high concentration of sugar. Cellulase and ,${\beta}$-glucosidase exhibit diverse kinetic behaviors. At a level of only 5g/$\ell$ of glucose, the ${\beta}$-glucosidase activity was reduced by more than 70%. This result means that ${\beta}$-glucosldase was the most severely inhibited by glucose. Also at l0g/$\ell$ of cellobiose, the cellulose lost approximately 70% of its activity. ${\beta}$-glucosldase was more sensitive to deactivation than cellulose by about 1.6 times. The comprehensive kinetic model in the range of confidence was obtained and the agreement between the model prediction and the experimental data was reasonably good, testifying to the validity of the model equations used and the associated parameters.

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Physiological activity of Pholiota nameko sp. ethanol extract (맛버섯 에탄올 추출물의 생리활성)

  • Jo, Se-Hyun;Jin, Gyoung-Ean;Yang, Yu;Jung, Kyung-Ju;Yun, Hyung-Sik;Yu, Young-Bok;Park, Ki-Moon
    • Journal of Mushroom
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    • v.8 no.4
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    • pp.142-149
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    • 2010
  • This study was conducted to investigate the physiological activities of the ethanol extracts from 10 different strains of Pholiota nameko. In addition, the ${\beta}$-glucan and polyphenol contents from these strains were also measured. Total polyphenol contents from all the strains were more than 40 mg% with the highest content of $61.50{\pm}0.59$ mg% and ${\beta}$-glucan contents were 30% with the highest content of $37.20{\pm}1.12%$. The highest inhibitory activities on ${\alpha}$-amyloglucosidase activity and nitric oxide production were $13.78{\pm}0.56%$ and $56.59{\pm}7.11%$, respectively. However, ethanol extracts from all the strains have little effects on DPPH radical and nitrite scavenging rates and the activity of angiotensin I converting enzyme. The cytotoxic activity of ethanol extracts from all the strains on A549 cell was shown upto 30% with the highest effect of $47.96{\pm}8.46%$ treated at 1 mg/mL concentration.

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