• Title/Summary/Keyword: Inhibitory Activity

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Synthesis of Mefenamic Acid Derivatives and Antioxidative and Anticoagulant Activities

  • Cha, Bae-Cheon
    • Biomolecules & Therapeutics
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    • v.8 no.4
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    • pp.349-353
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    • 2000
  • Mefenamic acid has been widely used as clinical drug for anti-inflammatory and analgesic. This drug was known to non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen and indomethacin. Although the drugs which comprise this group are of diverse chemical structures, they all share the antipyretic, analgesic and anti-inflammatory actions which are characteristic of aspirin. Action of this drugs is caused by inhibitory effect of biosynthesis of prostaglandin that are synthesized from arachidonic acid via the endoperoxide biosynthesis pathway, the initial step of which is catalysed by cyclooxygenase. Mefenamic acid has more potent inhibitory action of prostaglandin biosynthesis than aspirin. Therefore, mefenamic acid is expected to have anticoagulant activity as aspirin-like drugs. This study was carried out to investigate the sinthesis of mefenamic acid derivatives from mefenamic acid and aromatic compound of antioxidant and its antioxidative and anticoagulant activities. Synthesis of mefenamic acid derivatives was conformed by conjugation as using esterification method. Biological activities was examined using effect of anticoagulant on bleeding time and effect of antioxidant by TBA method. As a result, SJ-202 showed strong antioxidative activity and anticoagulant activity among tested 4 compounds and exhibited similar activity to aspirin at anticoagulant activity.

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Purification, Chemical Composition, and in vitro Antioxidant Activity of Two Protein-bound Polysaccharides from Rapeseed Meal

  • Sun, Han-Ju;Jiang, Shaotong;Zi, Mingyang;Qi, Ding
    • Food Science and Biotechnology
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    • v.18 no.6
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    • pp.1386-1391
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    • 2009
  • Crude polysaccharides from rapeseed meal (PRM) were extracted with 0.3% NaOH aqueous solution, followed by further purifications and 2 fractions, namely PRM1 and PRM2, were separated with a DEAE-cellulose DE-52 column. Their primary compositions were analysed and antioxidant activity was determined, including scavenging activity toward superoxide anion radicals, hydroxyl radicals, and nitric oxide radicals, reducing power, and inhibitory effects against the microsomal lipid peroxidation, compared to that of L-ascorbic acid. The results indicated that PRM1 and PRM2 exhibited not only good reducing power and inhibitory effects on the microsomal lipid peroxidation, but also strong scavenging activity toward superoxide anion radicals, nitric oxide radicals, and hydroxyl radicals. In addition, positive correlations were also observed between the superoxide anion radical scavenging activity and the protein contents of the polysaccharides, and the reducing power and the sulfate contents. These findings thus clearly suggest the polysaccharides possess direct and potent antioxidant activity.

Antioxidant and Antidiabetic Activities of Extracts from Quercus serrata Thunb and Q. acutissima Carruther (도토리(Quercus serrata Thunb)와 상수리(Quercus acutissima Carruther) 추출물의 항산화와 항당뇨 활성 연구)

  • Chu, Ji-Hye;Choi, Jin-Hee
    • Journal of the Korean Society of Food Culture
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    • v.36 no.5
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    • pp.522-529
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    • 2021
  • This study was conducted to analyze the antioxidant and antidiabetic activities of acorns according to the types of Quercus serrata Thunb (QST) and Q. acutissima Carruther (QAC). The total polyphenol contents of the extracts from QST and QAC were 220.59 and 320.96 mg GAE/g, respectively. The content of total polyphenol of QAC was higher than that of QAC (p<0.001). DPPH (2,2 Diphenyl 1 picrylhydrazyl) radical scavenging activity, reducing power and superoxide dismutase (SOD)-like activity were increased in a concentration-dependent manner by both acorn extracts, and QAC showed high activity in all antioxidant experiments (p<0.05). The inhibitory activities of α-glucosidase and α-amylase were also increased in a concentration-dependent manner, and QAC showed higher inhibitory activity than QST (p<0.05). Our study indicates that QST and QAC are functional food materials with high antioxidant and antidiabetic activities. In addition, QAC has a higher physiological activity than QST.

Taste, Nutritional and Functional Characterizations of Commercial Seasoned Sea Squirt Halocynthia roretzi (시판 조미 멍게(Halocynthia roretzi)의 맛, 영양 및 건강기능 특성)

  • Heu, Min Soo;Kim, Ji Hye;Kim, Min Ji;Lee, Ji Sun;Kim, Ki Hyun;Kim, Hyeon Jeong;Kim, Jin-Soo
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.46 no.1
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    • pp.18-26
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    • 2013
  • This study examined the taste, nutritional and functional characterizations of commercial seasoned sea squirt Halocynthia roretzi (CSS). Total taste values of CSS ranged from 7.6 to 69.5 and the major free amino acids were glutamic acid and aspartic acid. Total contents of amino acids in CSS ranged from 5.91 to 7.59 g/100 g and the major amino acids were also glutamic acid and aspartic acid. When taking 100 g of CSS, the minerals that could be expected to have functional health effects (minerals whose levels were above 10% of the recommended daily requirements) were P, Mg and Fe. Other minerals were also present in non-negligible quantities. In terms of the functional properties of CSS, ACE inhibitory activity was 21.2-37.1%, antioxidative activity was 55.4-90.4%, xanthine oxidase inhibitory activity was 52.9-76.6% and ${\alpha}$-glucosidase inhibitory activity was 0-32%. Antimicrobial activity against Vibrio parahaemolyticus was not detected, but activity against Staphylococcus aureus, groups such as KB, GG, CY, DN, HC and KH, and against Escherichia coli groups such as SF, WD, KB and GG, was detected.

Alaternin and Emodin with Hydroxyl Radical inhibitory and/or Scavenging Activities and Hepatoprotective Activity on Tacrine-Induced Cytotoxicity in HepG2 Cells

  • Jung, Hyun-Ah;Chung, Hae-Young;Takaka, Yokezawa;Kim, Youn-Chul;Hyun, Sook-Kyung;Choi, Jae-Sue
    • Archives of Pharmacal Research
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    • v.27 no.9
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    • pp.947-953
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    • 2004
  • The antioxidative and hepatoprotective potentials of two anthraquinones, alaternin (2-hydroxy-emodin) and emodin, to scavenge and/or inhibit hydroxyl radicals generated by the Fenton reaction and to protect tacrine-induced cytotoxicity in human liver derived HepG2 cells were evaluated, respectively. The inhibitory activity on hydroxyl radical generated in a cell-free chemical system (FeSO$_4$/$H_2O$$_2$) was investigated by a fluorescence spectrophotometer using a highly fluorescent probe, 2$^1$,7$^1$-dichlorofluorescein. The hydroxyl radical scavenging activity was determined by electron spin resonance spectroscopy using 5,5-dimethy-1-pyrroline-N-oxide as hydroxyl radicals trapping agents. Tacrine-induced HepG2 cell toxicity was determined by a 3-[4,5-dimethylthiazole-2yl]-2,5-diphenyltertrazolium bromide assay. Although the scavenging activity of alaternin on hydroxyl radical was similar to that of emodin in dose-dependent pat-terns, the inhibitory activity exhibited by the former on hydroxyl radical generation was stron-ger than that of the latter, with $IC_{50}$/ values of 3.05$\pm$0.26 $\mu$M and 13.29$\pm$3.20 $\mu$M, respectively. In addition, the two anthraquinones, alaternin and emodin showed their hepatoprotective activ-ities on tacrine-induced cytotoxicity, and the EC$_{50}$ values were 4.02 11M and 2.37 $\mu$M, respec-tively. Silymarin, an antihepatotoxic agent used as a positive control exhibited the EC$_{50}$ value of 2.00 $\mu$M. These results demonstrated that both alaternin and emodin had the simultaneous antioxidant and hepatoprotective activities.ies.

Inhibitory effects of Arisaematis rhizoma(天南星) on cell proliferation in HeLa cell (천남성(天南星)이 HeLa Cell의 증식억제(增殖抑制)와 apoptosis에 미치는 영향(影響))

  • Cho, Jung-Hoon;Jang, Jun-Bock;Lee, Kyung-Sub;Bae, Woo-Jin
    • The Journal of Korean Obstetrics and Gynecology
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    • v.19 no.3
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    • pp.25-40
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    • 2006
  • Purpose : This study was undertaken to evaluate the inhibitory effects of Arisaematis rhizoma on the cell proliferation in HeLa cells. Methods : The cultured cell after treatment in the different duration in 24, 48, 72 hours with solution of 1%. 5%, 10% Arisaematis rhizoma was quantified by trypan blue exclusin method. The control group was treated with 2% FBS in the different duration in 24, 48, 72 hours. We examined DNA of activated caspase by FACS analysis, caspase-3 activity, DNA fragmentation by DNA laddering, activity of HeLa Cells by the XTT assay, activity of MAP kinase by RT-PCR analysis. Results : After 72 hours culture, the growth activities of 1%, 5%, 10% Arisaematis rhizoma-treated Hela cell were significantly reduced with control group, respectively. After 24 hours culture, the ratio of cells showing caspase activity by FACS analysis were increased in 1%, 5%, 10% Arisaematis rhizoma-treated Hela cell. It were also increased in 48 hours culture of 10% and 72 hours culture of 5%, 10% Arisaematis rhizoma-treated Hela cell. In 24, 48 and 72 hours culture, DNA fragmentations of 5%, 10% Arisaematis rhizoma-treated Hela cell were obviously observed. These results meaned that Arisaematis rhizoma induces apoptosis of HeLa cells. It was supported by increased caspase-3 activity and decreased MAP kinase activity according to time periods and concentrations of Arisaematis rhizoma solution. Conclusion : The study shows that Arisaematis rhizoma has inhibitory effect on cell proliferation and induction capacity of apoptosis of human cevical carcinoma cell line, HeLa cells, in vitro. These results suggest that Arisaematis rhizoma should be useful for treatment of human cevical carcinoma.

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Development and Evaluation of the Herbal Medicine for Hair Growth-promoting Activity (발모 향상을 위한 한약재의 개발 및 효과 확인)

  • Choi, Sunkyung;Cho, Namjoon;Kim, Kee K.
    • KSBB Journal
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    • v.31 no.4
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    • pp.237-245
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    • 2016
  • Hair loss affects both men and women of all ages and often significantly affects social and psychologic health. Recent therapeutic approach for hair loss such as finasteride and minoxidil focused on regulation of hormonal system blood flow. However, long-term use of these drugs caused adverse effects. To develop herbal medicine for therapeutic effect on hair growth, here we screened the 10 medicinal herbs (Red ginseng, Licorice, Ulmus, Barberry root, Lycium root, Rehmanniae radix crudus, Sophora root, Sweet flag, Polygala root, Achyranthes) based on oriental medicine literature. We measured cytotoxicity, anti-oxidant activity, and $5-{\alpha}$ reductase inhibitory effect of the herbal medicine on human dermal papilla (DP) cells to investigate therapeutic effect of the herbal medicine. Treatment of the 1% herbal medicine did not show any cytotoxic effects, and cell growth was increased by treatment of the 0.1% herbal medicine. In addition, the herbal medicine showed stronger antioxidant activity than resveratrol and comparable inhibitory activity of $5-{\alpha}$ reductase with finasteride. Furthermore, when applied to in vivo mouse model, we also observed increases in the number and length of hair of the herbal medicine-treated group. These results suggest that the herbal medicine promotes hair growth by its antioxidant activity and inhibitory activity of $5-{\alpha}$ reductase and might therefore be a promising hair growth-promoting agent.

Antioxidant and Anticholinesterase Potential of Two Nigerian Bitter Yams Using a Simulated Gastrointestinal Digestion Model and Conventional Extraction

  • Salawu, Sule Ola;Ajiboye, Praise Blessing;Akindahunsi, Akintunde Afolabi;Boligon, Aline Augusti
    • Preventive Nutrition and Food Science
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    • v.22 no.2
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    • pp.107-117
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    • 2017
  • The purpose of this study was to evaluate the antioxidant and anticholinesterase activities of yellow and white bitter yams from South Western Nigeria using methanolic extraction and simulated gastrointestinal digestion models. The phenolic compounds in the bitter yam varieties were evaluated by high performance liquid chromatography with a diode array detector (HPLC-DAD). The total phenolic content of the bitter yams was measured by the Folin-Ciocalteu method, reductive potential by assessing the ability of the bitter yam to reduce $FeCl_3$ solution, and the antioxidant activities were determined by the 2,2-diphenyl-1-picrylhydrazyl radical ($DPPH^{\cdot}$) scavenging activity, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation ($ABTS^{{\cdot}+}$) scavenging activity, nitric oxide radical ($NO^{\cdot}$) scavenging ability, hydroxyl radical scavenging ability, and ability to inhibit $Fe^{2+}$-induced lipid oxidation. The HPLC-DAD analysis revealed the presence of some phenolic compounds in the studied bitter yam varieties, with varying degree of quantitative changes after cooking. The antioxidant indices (total phenolic content, total flavonoid content, reducing power, $DPPH^{\cdot}$ scavenging activity, $ABTS^{{\cdot}+}$ scavenging activity, and $NO^{\cdot}$ scavenging activity) were higher in the simulated gastrointestinal digestion model compared to the methanolic extract, with the in vitro digested cooked white bitter yam ranking higher. Similarly, the in vitro digested yams had a higher inhibitory action against lipid oxidation compared to the methanolic extracts, with the cooked white bitter yam ranking high. The methanolic extracts and in vitro enzyme digests showed no acetylcholinesterase inhibitory abilities, while methanolic extracts and the in vitro enzyme digest displayed some level of butyrylcholinesterase inhibitory activities. Therefore the studied bitter yams could be considered as possible health supplements.

Anti-glycation Activities from Various Agricultural Products (단백질 glycation 저해효과가 있는 식품소재)

  • Choi, Hee-Don;Choi, In-Wook;Kim, Yoon-Sook
    • Korean Journal of Food Science and Technology
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    • v.39 no.4
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    • pp.458-463
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    • 2007
  • The ethanolic extracts of 83 kinds of agricultural products, including cereals, vegetables, and Chinese herbs, were tested for their inhibitory activities on protein cross-linking using the $[^{14}C]$-N-formyl-lysine incorporation method. Most of the extracts inhibited, but some extracts accelerated, the cross-linking of protein. Of those items with relatively high activities, we selected 20 samples to test for activity against AGE fonnation using the fluorophotometric method. The ethanol extract of buckwheat that was genninated for 1 day (GB-01) was detennined to have the highest activity with both methods. The ethanol extract of GB-01 was further fractionated by organic solvents, including chloroform, ethyl acetate, butanol, and water, in order of increasing polarity. The fraction that was extracted with ethyl acetate presented the highest protein glycation inhibitory activity (95.2% inhibition at the 100 ug/mL addition level). Polyphenol content analysis by HPLC showed that the amounts of rutin and quercetin were increased with the separation procedures. Finally, there was a significant relationship between activity and polyphenol content in the partially purified samples (p<0.05).

Study on Antitumor Activity and Immunomodulatory effects of Seoleosojong-tang (활어소종탕이 항종역반응에 미치는 영향)

  • Son Ki Jeong;Park Yang Chun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.1
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    • pp.137-147
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    • 2004
  • In order to evaluate the antitumor activity and immunomodulatory effects of Seoleosojong-tang(SST), studies were done. We measured the cytotoxic activity for various kinds of cancer cells, inhibitory effect on activity of DNA topoisomerase I, cell adhesion to complex extracellular matrix, survival time in ICR bearing S-180, pulmonary colonization and histological changes of lung in C57BL/6 injected i.v. with B16-F10, CAM assay, expression of CD4/sup +/, CD8/sup +/, B220/sup +/, cytokine gene in spleen cell. The results were obtained as follows: 1. In cytotoxicity against A549, HT1080, 816-F10, NCL-H661 was showed cytotoxicity as compared with control. 2. The inhibitory effect on adhesion of A549, 816-F10 to complex extracellular matrix was over 40% at 100 ㎍/㎖ of SST. 3. In DNA topoisomerase I assay, SST has inhibitory effect. 4. The T/C% was 120.8 in SST treated group in S-180 bearing ICR mice. 5. In pulmonary colonization assay, a number of colonies were decreased significantly and histological changes were showed that infiltration area of cancer cells were inhibited effectively in SST treated group. 6. In CAM Assay, SST has antiangiogenic effect. 7. On the expression of positive cell to CD4/sup +/, CD8/sup +/ and 8220/sup +/ in spleen cells, CD4/sup +/ cells were increased significantly in SST treated group. 8. Effect of SST on IL-1β gene expression in splenic cell was significantly increased as function of whole concentration. 9. The gene expression of IL-4, IL-6, IL-10, IL-12, IFN-γ, TNF-α were increased in SST treated group. From above results SST could be usefully applied for antitumor activity and immunomodulatory effects, but further research of SST should be required.