• Title/Summary/Keyword: Inhibitory Activity

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NF-${\kappa}B$ Inhibitory Activities of Phenolic and Lignan Components from the Stems of Acanthopanax divaricatus var. albeofructus

  • Sun, Ya Nan;Li, Wei;Song, Seok Bean;Yan, Xi Tao;Yang, Seo Young;Kim, Young Ho
    • Natural Product Sciences
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    • v.20 no.4
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    • pp.232-236
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    • 2014
  • Acanthopanax divaricatus var. albeofructus (ADA) is commonly ingested as a traditional medicine or as a component of a health drink in Korea. In this phytochemical study, nine phenolics (1 - 9) and three lignans (10 - 12) were isolated from the MeOH extract of the stems of ADA. Chemical structures were elucidated by comparing spectroscopic data with reported values. Nuclear factor kappa B ($NF-{\kappa}B$) inhibitory activity of the isolated compounds was evaluated using an $NF-{\kappa}B$ luciferase assay in HepG2 cells. Among them, compounds 1, 3 - 8, and 11 showed significant inhibitory effects on $TNF{\alpha}$-induced $NF-{\kappa}B$ transcriptional activity in a dosedependent manner, with $IC_{50}$ values ranging from 13.25 to $37.36{\mu}M$. Further studies on potential anti-inflammatory effects and the benefits of phenolic and lignan components from ADA are warranted.

Anti-inflammatory Activity of Flavonoids from Populus davidiana

  • Zhang, XinFeng;Hung, Tran Manh;Phuong, Phuong Thien;Ngoc, Tran Minh;Min, Byung-Sun;Song, Kyung-Sik;Seong, Yeon-Hee;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • v.29 no.12
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    • pp.1102-1108
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    • 2006
  • An in vitro bioassay-guide revealed that the methanol (MeOH) extract of the stem bark of Populus davidiana showed considerable inhibitory activity against cyclooxygenase (COX-1, COX-2). Continuous phytochemical study of the MeOH extract of this plant led to the isolation of ten flavonoids; sakuranetin (1), rhamnocitrin (2), 7-O-methylaromadendrin (3), naringenin (4), eriodictyol (5), aromadendrin (6), kaempferol (7), neosakuranin (8), sakuranin (9) and sakurenetin-5,4'-di-${\beta}$-D-glucopyranoside (10). Their structures were identified on the basis of their physicochemical and spectroscopic analyses. The isolated compounds, 1-10, were tested for their inhibitory activities against COX-1 and COX-2. Compound 7 was found to have potent inhibitory effect on COX-1 and a moderate effect on COX-2, meanwhile, compounds 1-6 showed moderate inhibition against COX-1 only. Moreover, compounds 5-8 exhibited suppressive effects on xanthine oxidase (XO). These results may explain, in part, the traditional uses of P. davidiana in ethnomedicine.

Synthesis and Inhibitory Activity on NF-${\kappa}B$ Activation of Chroman-2-carboxylic Acid N-Heteroarylamide Derivatives (크로만-2-카르복실산 N-헤테로아릴아마이드 유도체 합성 및 NF-${\kappa}B$ 저해 활성)

  • Yi, Won-Hui;Kwak, Jae-Hwan;Han, Sang-Bae;Kim, Young-Soo;Jung, Jae-Kyung;Lee, Hee-Soon
    • YAKHAK HOEJI
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    • v.56 no.3
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    • pp.186-190
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    • 2012
  • Nuclear factor-${\kappa}B$ (NF-${\kappa}B$) has been considered as one of the major targets for therapeutic agents of diverse human diseases. In the previous studies, 6-hydroxy-7-methoxychroman-2-carboxylic acid N-phenylamide (KL-1156) and chroman-2-carboxylic acid N-(4-chlorophenyl)amide were identified as good inhibitors of NF-${\kappa}B$ activation. In this continuous study, we describe the synthesis and NF-${\kappa}B$ inhibitory activities of chroman derivatives containing N-heteroaryl groups for exploration of SAR (structure-activity relationship). In addition, inhibitory effects of cell proliferation are evaluated against human cancer cell lines (NCI-H23 and PC-3).

Comparison of the Scrophulariae Radix of Gyeongbuk's with that of Chinese: Content of Harpagoside and Inhibitory Effect of Nitric Oxide (경북산 현삼과 중국산 현삼의 비교: Harpagoside 함량 및 Nitric Oxide 저해활성)

  • Zhang, Hai-Yan;Kim, Geum-Jin;Hwang, In-Hyun;Cho, Hi-Jae;Lee, Seung-Ho;Na, Min-Kyun
    • Korean Journal of Pharmacognosy
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    • v.42 no.1
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    • pp.15-21
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    • 2011
  • Scrophulariae Radix (Scrophulariaceae) has been traditionally used to treat pharyngitis, laryngitis, tonsillitis, fever, and edema. To compare the quality of the Scrophulariae Radix produced from Gyeongbuk with that from China, a quantitative analysis on the major component, E-harpagoside, was performed by reversed-phase HPLC, and a relative inhibitory activity of nitric oxide (NO) was assayed in the Raw 264.7 cells. Using a Luna $C_{18}$(2) column, we carried out quantitative analysis with a gradient of 0.1% phosphoric acid in water and acetonitrile. Our results demonstrated that the content of E-harpagoside in Gyeongbuk's Scrophulariae Radix were three times higher than that of Chinese. Moreover, the inhibitory activity of Scrophulariae Radix of Gyeongbuk's in the lipopolysaccharide (LPS)-induced NO production was higher than that of Chinese.

Studies on the Antimutagenicity of extract from Barley (Hordeum vulgare) (보리(Hordeum vulgare) 추출물의 항변이원성)

  • 이은주;구성자
    • Korean journal of food and cookery science
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    • v.14 no.5
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    • pp.468-474
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    • 1998
  • This study was performed to determine the effects of antimutagenicity from Barley (Hordeum vulgare). In Salmonella typhimurium reversion assay (In vitro test), the extract of Barley (Hordeum vulgare) inhibited mutagenic activity of 4-NQO and Trp-p-1 with 59 mix. in Salmonella typhimurium TA98 and TA100. In Micronucleus test (In vivo test), the methanol extract of Barley (Hordeum vulgare) inhibited micronucleus formation in bone marrow by cyclophosphamide. The $\beta$-glucan of Barley (Hordeum vulgare) showed inhibitory effects of 59-77% in mutagenic activity of 4-NQO by Salmonella typhimurium TA100. The mutagenicity of Trp-p-1 with S9 mix. by Salmonella typhimurium TA98 showed inhibitory effects of 24-56%. The methanl extract (M) was fractionated with ether (MI), ethylacetate (M2), buthanol (M3) and water (M4). The Antimutagenicity of Trp-p-1 with 59 mix. by Salmonella typhimurium TA98 in Barley fraction showed the following: methanol extract (99.58%)>ether fraction (98.05%)>buthanol fraction (56.90%)>water fraction (56.72%)>ethyl acetate fraction (28.72%). Among them, ether fraction in TA 98 showed strong antimutagenicity effects (85.56%, 98.05%) against mutation induced by 4-NQO and Trp-p-1. As concentration of the methanol extract increased (1.25~5 g/kg/10 cc), micronucleus formation in bone marrow by chemical mutagen (CP) showed inhibitory effects of 50% (p< 0.05).

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Inhibitory Components from Glycosmis stenocarpa on Pepper Mild Mottle Virus

  • Kim, Jang Hoon;Yoon, Ju-Yeon;Kwon, Sun Jung;Cho, In Sook;Nguyen, Manh Cuong;Choi, Seung-Kook;Kim, Young Ho;Choi, Gug Seoun
    • Journal of Microbiology and Biotechnology
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    • v.26 no.12
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    • pp.2138-2140
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    • 2016
  • The goal of this study was to identify a source of natural plant compounds with inhibitory activity against pepper mild mottle virus (PMMoV). We showed, using a half-leaf assay, that murrayafoline-A (1) and isomahanine (2) isolated from the aerial parts of Glycosmis stenocarpa have inhibitory activity against PMMoV through curative, inactivation, and protection effects. Using a leaf-disk assay, we confirmed that 2 inhibited virus replication in Nicotiana benthamiana. Using electron microscopy, we found that a mixture of the virus with 2 resulted in damage to the rod-shaped virus.

Evaluation of ${\mu}$-Calpain Inhibitory Activity of Korean Indigenous Marine Organism Extracts

  • Lee, Yoo-Jin;Lee, Eun-Young;Han, Ah-Reum;Song, Jun-Im;Kwon, Young-Joo;Seo, Eun-Kyoung
    • Natural Product Sciences
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    • v.18 no.2
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    • pp.102-105
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    • 2012
  • Marine organism extracts were prepared from 26 species of Korean indigenous marine organisms, including 25 species belonging in class Anthozoa of phylum Cnidaria and a species belonging to subphylum Urochordata of phylum Chordata, and screened their inhibitory effects against ${\mu}$-calpain. As a result, the thirteen extracts were found to be active in the criteria of $IC_{50}$ < 100 ${\mu}g/ml$. Among them, the MeOH extracts of Plexauroides praelonga and Alveopora japonica showed remarkable ${\mu}$-calpain inhibitory activity with $IC_{50}$ values of $4.62{\pm}0.22$ and $4.82{\pm}0.07{\mu}g/ml$, respectively. In addition, chemical investigation of A. japonica led to the isolation of an active compound, hexadecyl tetradecanoate, as a selective cathepsin B inhibitor ($IC_{50}=9.05{\pm}2.45{\mu}M$). This compound was isolated as constituent of A. japonica for the first time in the present study.

The Biological Activity of Deer Antler Extract in vitro (In vitro에 의한 녹용 추출물의 생리 활성 효과)

  • Lee, Kyung-Ae;Chung, Hae-Young
    • The Korean Journal of Food And Nutrition
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    • v.20 no.2
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    • pp.114-119
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    • 2007
  • Our research objective was to examine the in vitro biological activity of deer antler(Nogyong in Korean) extract, including the antioxidative, nitrite scavenging, and tyrosinase inhibitory effects, as well as the antithrombotic, and angiotensin I converting enzyme(ACE) inhibitory activities. The carbohydrate, protein, fat, and mineral contents of the deer antler were 7.6%, 65.3%, 3.2% and 23.9%, respectively. The electron donating ability(EDA) by the reduction of 2,2'-diphenyl-1-picrylhydrazyl(DPPH) was 67.1%, and the inhibition rate of lipid peroxidation by the thiocyanate method using linoleic acid was 92.1% in 100 mg/ml of extract. The nitrite scavenging effects were pH dependent, and were highest at pH 1.2 and lowest at pH 6.0. The sample inhibition rate against tyrosinase was above 64.0%. The platelet aggregation induced by ADP(adenosine-5'diphosphate) was inhibited up to 51.7%, and the inhibitory effect was dependent on the sample concentration. Lastly, the inhibition rate of ACE was 47.5% in 100 mg/ml of deer antler extract.

Physiological Activities of Saccharified Cherry Tomato Gruel Containing Different Levels of Cherry Tomato Puree (방울토마토 첨가량을 달리한 당화 방울토마토죽의 항산화 및 ACE 저해 효과)

  • Kim, Jin Sook;Kim, Ja Young;Chang, Young Eun
    • Korean journal of food and cookery science
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    • v.28 no.6
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    • pp.773-779
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    • 2012
  • This study was conducted to investigate the physiological activities of saccharified cherry tomato gruel containing different levels(0, 15, 30, and 45%) of cherry tomato puree. The total phenolic compound and flavonoids contents of saccharified cherry tomato gruel with cherry tomato puree were 1.73-5.09 mg/g and 0.28-7.01 mg/g, respectively. DPPH radical scavenging activities of saccharified cherry tomato gruel with cherry tomato puree were 8.67-92.58%, respectively. The ABTS radical scavenging activities of saccharified cherry tomato gruel with cherry tomato puree ranged from 6.02 to 61.59%. The ACE inhibitory activity of cherry tomato rice gruel increased with cherry tomato puree showed a range of 38.85-62.15%, respectively. With increasing additions of cherry tomato puree, the total phenolic compound and flavonoid contents, DPPH and ABTS radical scavenging activities and, ACE inhibitory activities were increased significantly (p<0.05). In conclusion, saccharified cherry tomato gruel could be used as a gruel processing method to in order to increase the functional values of gruels.

Antibacterial Activities of Essential Oil from Zanthoxylum schinifolium Against Food-Borne Pathogens (산초 정유성분의 식중독균에 대한 항균 활성)

  • Jang, Mi-Ran;Seo, Ji-Eun;Lee, Je-Hyuk;Kim, Gun-Hee
    • Korean journal of food and cookery science
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    • v.26 no.2
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    • pp.206-213
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    • 2010
  • In this study, the antibacterial activities of essential oil from Zanthoxylum schinifolium against four Gram-positive bacteria and six Gram-negative bacteria were investigated. The antibacterial activity of the oils was determined using the agar-well diffusion assay, MIC (minimum inhibitory concentration) and MBC (minimum bactericidal concentration). In particular, essential oil from Z. schinifolium showed higher antibacterial activity against Gram-positive bacteria than against Gram-negative bacteria. Essential oil from Z. schinifolium displayed large inhibition zones especially against Bacillus cereus (31 mm). At concentrations between 0 and $20\;{\mu}g/mL$ the oils showed an antibacterial effect against both Gram-negative and Gram-positive bacteria. The minimum inhibitory concentration (MIC) values against nine bacteria ranged from 1.25 to $5\;{\mu}g/mL$. The minimum bactericidal concentration (MBC) values against eight bacterial ranged from 2.5 to $20\;{\mu}g/mL$, except Shigella sonnei. Furthermore, our finding on the antibacterial activities of essential oils from Zanthoxylum schinifolium validated the use of this plant for medical purposes.