• Title/Summary/Keyword: like activity

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Synthesis and Antiproliferative Potency within Anticonvulsant of Novel Bichalcone Derivatives

  • Mansour, Eman;El-Badry, Yaser A.;El-Tokhy, Afaf;Ayyad, Rezed;Abd-Rabou, Ahmed A.
    • Journal of the Korean Chemical Society
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    • v.64 no.1
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    • pp.7-18
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    • 2020
  • An efficient and facile procedure has been developed for the synthesis of novel bichalcone derivatives (4a, 4b). The key step contains the solvent-free aldol synthesis of bichalcones based on quinones. Bichalcones (4a, 4b) were used as precursors for the synthesis of some interesting heterocyclic compounds like, diazepines (5a, 5b), pyrazolo-pyrimidines (7a, 7b), and pyrazoline derivatives (8a, 8b). Moreover, new thioxopyrimidine derivatives (9a, 9b) were furnished and used as a functionalizing agent to produce the triazole-pyrimidines (11, 12) and the carbonitrile derivative (14). All the synthesized compounds were fully characterized using physical and spectral data like, FT-IR, 1H NMR, 13C NMR, and MS. Bichalcones (4a, 4b) and diazepines (5a, 5b) were screened for their anticonvulsant activity, where compounds (4a, 5a, and 5b) revealed potent anticonvulsant activity compared to diazepam. On the other hand, some of the prepared compounds were screened for their antiproliferative activity and they showed significant cytotoxic effects on most of the cancer cell lines with regard to broad spectrum antitumor activity.

Study on the Development of Cosmetic Emulsion Cream for Patients with Atopic Dermatitis using Scutellaria Baicalensis (황금(黃芩)을 이용한 아토피성 피부용 한방화장품 제형화에 관한 연구)

  • Park, Chan-Ik
    • The Korea Journal of Herbology
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    • v.21 no.2
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    • pp.47-53
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    • 2006
  • Objectives : This study was conducted to determine if Scutellaria baicalensis can be used in cosmetic emulsion cream for patients with atopic dermatitis. Methods : Scutellaria baicalensis extract was obtained with the use of butylene glycol through the pressurized solvent extraction(PSE). The antioxidative activity was assessed through SOD-like activity measurement and skin irritating potential was tested using human patch test. Antimicrobial activity was measured by the clear zone formed against Staphylococcus aureus and Escherichia coli and the rheological effects on the emulsion creams were examined using oscillation test. Results : The SOD-like activity increased dose-dependently and was about 90% at 1,000ppm of Scutellaria baicalesis extract. And Scutellaria baicalensis extract did not show any potential to be irritating to the human skin, but it could not be used as an antimicrobial agent for its poor antimicrobial activity against Staphylococcus aureus. The complex modulus decreased by 1,000 pascals and the loss angle also decreased by 20% with the addition of Scutellaria baicalensis extract into the cosmetic emulsion creams, that is, the extract can confer more elastic property on the vehicle. Conclusion : From those results, Scutellaria baicalensis extract can be effectively used as an antioxidant and reinforces the elastic skincare film formed by the application of cream for patients with atopic dermatitis.

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Antioxidative Activity of Solvent Fraction from Taraxacum officinale (민들레 용매분획물의 항산화 활성)

  • Lee, Youn Ri
    • The Korean Journal of Food And Nutrition
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    • v.35 no.4
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    • pp.276-281
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    • 2022
  • Antioxidant activities and α-glucosidase inhibitory activities of Taraxacum officinale solvent fractions were measured. Extraction yields (relative to raw material) of 50% ethanol, hexane, ethyl acetate, butanol, and water were found to be 10.29, 2.61, 5.54, 2.15, and 0.96%, respectively. Polyphenol and flavonoid contents were high in ethyl acetate extract of Taraxacum officinale at 56.88 mg gallic acid/g and 33.27 mg gallic acid/g, respectively. DPPH, hydroxyl radical scavenging activity, and SOD-like activity measurement (IC50%) of Taraxacum officinale 50% ethanol extract, hexane, butanol, ethyl acetate, and water fractions were 22.64, 18.65, 10.29, 20.81, 20.46 mg/mL, 24.68, 10.69, respectively. It was found to be 9.66, 15.81, 13.77 mg/mL, 32.84, 17.09, 12.73, 33.63, and 33.91 mg/mL, and was high in the ethyl acetate layer. Results showed that α-glucosidase inhibitory activities of Taraxacum officinale solvent fraction were 25.75, 15.93, 35.87, 15.96, and 2.88% for 50% ethanol extract, hexane, butanol, ethyl acetate, and water fractions, respectively.

Nitrite Scavenging and Superoxide Dismutase-like Activities of Herbs, Spices and Curries (향신료 및 Curry의 Nitrite 분해와 Superoxide Dismutase 유사활성)

  • Kim, Jin-Hyun;Park, Ki-Moon
    • Korean Journal of Food Science and Technology
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    • v.32 no.3
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    • pp.706-712
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    • 2000
  • The superoxide dismutase(SOD)-like activities for 26 kinds of herbs and spices and 10 kinds of instant curry products were determined by measuring their abilites to reduce nitroblue tetrazolium. All samples showed the SOD-like activities. Rosemary, cassia, tarragon, allspice, oregano, bay leaves, basil, marjoram, thyme and star anise had higher activities than $10^5\;unit/g$ and clove had highest activity of $232,143{\pm}19.989\;unit/g$. The SOD-like activities for 10 kinds of instant curry products were in the range of $400{\sim}700\;unit/g$ when measured after heat treatment at $100^{\circ}C$ for 10 min. The water extracts of spices, herbs and curries were obtained by heat treatments of $25^{\circ}C$ for 60 min or $100^{\circ}C$ for 10 min, and their nitrite scavenging activity was measured at different pH conditions(1.2, 4.2 or 6.0). The nitrite scavenging activities were higher at acidic pH. However, the effects were not different from two heat treatments. The water extracts from cassia, bay leaves, allspices, oregano, staranise, rosemary, clove and tarragan had high nitrite scavenging activity(>90%) when they were measured at pH 1.2, and those from clove was highest $(97.58{\pm}0.88%)$. The pure curry used as raw materials for instant curry products had the nitrite scavenging activity in the range of $50{\sim}60%$ at pH 1.2 and the activity was not changed during the aging period$(0{\sim}12weeks)$. The ten brands of instant curry products had the nitrite scavenging activities of $12{\sim}28%$ at pH 1.2

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Evaluations on Antioxidant Effect of Methanol Extract from Immature Cotton Boll (미성숙 목화다래 메탄올 추출물의 항산화 효능 평가)

  • Park, Hee-Jeong;Lee, Ki-Young
    • Korean Journal of Plant Resources
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    • v.26 no.4
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    • pp.426-432
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    • 2013
  • The results of the content of total polyphenol and flavonoid, DPPH (1-1-diphenyl-2-picryl-hydrazyl) radical scavenging activity, ABTS [2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)] radical scavenging activity, nitrite scavenging activity and SOD-like activity of methanol extracts from immature cotton boll are follows. The contents of total polyphenol and flavonoid compound were higher in small size cotton boll, and DPPH and ABTS radical scavenging activity also showed a relatively high activity in the small size. These results indicate that there is a correlation between phenol content and DPPH radical scavenging, ABTS radical scavenging. The test concentrations of immature cotton boll extract for measuring DPPH and ABTS radical scavenging activities were set as 1.25, 2.5, 5, 10 and 20 mg/ml. Immature cotton boll has high radical scavenging activity at the concentration of 1.25~20 mg/ml and the result showed a tendency to increase in a concentration-dependent. The nitrite scavenging activity showed high activity in the pH 1.2, and the result in the pH 4.2 showed progressively less active, and in the pH 6.0 near neutral was confirmed that does not affect the nitrite scavenging. In addition, SOD-like activity showed somewhat lower activity compared with ascorbic acid, but tended to be higher when compared with the results of the other natural substances. Through this experiment, we confirmed that immature cotton boll was excellent antioxidant activity. Therefore, it is demonstrated that the cotton suggest the possibility of development of new material for cosmetic product or functional food in the future, and is expected to make a greater usability.

Study on the Antioxidant Activity of the Extracts from the Lepista nuda (민자주방망이버섯(Lepista nuda)의 항산화성에 관한 연구)

  • Lee, Yang-Suk;Park, Dong-Cheol;Joo, Eun-Yong;Shin, Seung-Ryeul;Kim, Nam-Woo
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.34 no.7
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    • pp.942-947
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    • 2005
  • This study was investigated to analyze the effect of extracts from the Lepista nuda, on the antioxidant activity to form a part of studies on the functional materials of L. nuda. Antioxidant activity of L. nuda extracts was evaluated by measuring the electron-donating ability (EDA), the superoxide dismutase (SOD)-like activity, and the nitrite-scavenging ability. The EDAs of water and ethanol extracts at the concentration of 1,000 ppm by the rotary heating method from L. nuda were $60.47\%$ and $60.13\%$, respectively and those of water and ethanol extracts by microwave-assisted method were $87.73\%$ and $84.84\%$, respectively. The measurements of SOD-like activity were in the range of $24.58\%\~42.03\%$ at 1,000 ppm. EDA and SOD were increased with the concentrations of extracts. The nitrite-scavenging ability at the concentration of 1,000 ppm was the highest and $29.77\%$ at pH 1.2, and was decreased with an increment of pH value. These results indicated that microwave­assisted water extract from L. nuda showed the highest activities on the EDA and nitrate-scavenging ability, while the rotary heating ethanol extract had the highest effect on the SOD-like activity.

Study on the Immunomodulatory Effects of Ellagic Acid and their Mechanisms Related to Toll-like Receptor 4 in Macrophages (Ellagic acid가 대식세포의 면역조절작용에 미치는 영향과 Toll-like receptor 4 관련 작용기전 연구)

  • NamKoong, Seung;Kim, Ye-Jin;Kim, Taeseong;Sohn, Eun-Hwa
    • Korean Journal of Plant Resources
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    • v.25 no.5
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    • pp.561-567
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    • 2012
  • Ellagic acid (EA) is a phenolic compound in fruits and nuts including raspberries, strawberries, grapes and walnuts. Previous studies have indicated that EA possesses antioxidant activity, growth-inhibition and apoptosis-promoting activity in cancer cells. However, macrophage mediated cytotoxicity and immunomodulating effects on cancer cells have not been clarified. In the present study, we show that EA increased effects on macrophage mediated tumoricidal activity and NO production without direct tumor cell cytotoxicity. To further determine whether TLR4 (toll like receptor 4) is involved in anti-tumor activity, cells were treated TLR4 signaling inhibitor, CLI-095 in the presence of EA. CLI-095 treatment partially reduced macrophage-mediated tumoridial activity. EA also has inhibitory effects of NO production induced by LPS, whereas phagocytic activity was not changed. These results suggest that EA induces macrophage mediated tumoricidal activity which is partially related to TLR4 signaling and has a potential adjuvant in cancer therapy.

Study of Deep Ground Sea-Like Water on Antioxidant Activity and the Immune Response in RAW264.7 Macrophages. (천연 암반 심해수의 항산화 활성 및 면역반응에 대한 연구)

  • Kim, Yu-Jung;Jung, Il-Sun;Song, Hyo-Ju;Choi, Eun-Young;Choi, In-Soon;Choi, Young-Ju
    • Journal of Life Science
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    • v.18 no.3
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    • pp.329-335
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    • 2008
  • Korean Deep ground sea-like water (KDSW) has a similar mineral composition with deep sea water. KDSW has demonstrated its usefulness and attracted in the medical fields. KDSW and Danasoo (desalted deep ground sea-like water) intake improve antioxidant, antidiabetic activity and immunity. Antioxidant activities of KDSW and Dnansoo were measured by using 2,2-diphenyl-l-picryl-hydrazyl (DPPH) free radical, superoxide dismutase-like activity (SODA) and photochemiluminescence (PCL). DPPH radical scavenging and SOD-like activities of KDSW and Danasoo were remarkably increased in a dose-dependent manner. Antioxidant activities of KDSW and Danasoo 85.32 and 14.02 nmol of ascorbic acid equivalent/ml KDSW and Danasoo, respectively, using the PCL method. Lipopolysaccharide (LPS)-induced nitric oxide (NO) production in macrophages RAW264.7 cells was inhibited up to 30% by treatment with Danasoo (20%). NO is synthesized by the enzyme of nitric oxide synthase (NOS) and plays an important role tumor growth and angiogenesis. The anticancer effects of Danasoo on human gastric and lung cancer cells was performed by levels of inducible nitric oxide synthase (iNOS). Danasoo significantly reduced iNOS expression of human gastric cancer (SNU-l) and lung carcinoma (A549). The serum glucose level was significantly reduced by Danasoo (20%) diet in streptozotocin (STZ)-induced diabetic rats. These result suggest that KDSW has excellent biological activities and thus it has great potential as a source for natural health products.

Free Radical Scavenging Activities of Chitosan Oligosaccharides Produced by Bioreactor

  • Park, Pyo-Jam;Byun, Hee-Guk;Kim, Se-Kwon
    • Proceedings of the Korean Society of Fisheries Technology Conference
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    • 2001.10a
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    • pp.241-242
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    • 2001
  • Chitosan, a deacetylated derivative of chitin, is one of the abundant resources, and its biological properties such as antibactierial activity, hypocholesterolemic activity, and hypertensive action are remarked. However, increasing attention has recently been yen to converting chitosan to its oligosaccharides because they possess various functional properties like antitumor activity, immune-enhancing effects, enhancing protective effects against infection with some pathogens in mice, antifungal activity, and antimicrobial activity (Jeon et al., 2001). (omitted)

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Rheumatoid Fibroblast-like Synoviocytes Downregulate Foxp3 Expression by Regulatory T Cells Via GITRL/GITR Interaction

  • Kim, Sung Hoon;Youn, Jeehee
    • IMMUNE NETWORK
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    • v.12 no.5
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    • pp.217-221
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    • 2012
  • Fibroblast-like synoviocytes (FLS) colocalize with leukocyte infiltrates in rheumatoid synovia. Proinflammatory leukocytes are known to amplify inflammation by signaling to FLS, but crosstalk between FLS and regulatory T cells (Tregs) remains uncharacterized. To address this possibility, we cocultured FLS lines derived from arthritic mice with Tregs. FLS that expressed the ligand for glucocorticoid-induced TNF receptor family-related gene (GITR) decreased expression of Foxp3 and GITR in Tregs in a contact-dependent manner. This effect was abolished by blocking antibody to GITR. On the other hand, the Tregs caused the FLS to increase IL-6 production. These results demonstrate that inflamed FLS license Tregs to downregulate Foxp3 expression via the GITRL/GITR interaction while the Tregs induce the FLS to increase their production of IL-6. Our findings suggest that the interaction between FLS and Tregs dampens the anti-inflammatory activity of Tregs and amplifies the proinflammatory activity of FLS, thereby exacerbating inflammatory arthritis.