• Title/Summary/Keyword: Inhibitory Activity

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Anti-Inflammatory Effects of N1-Benzyl-4-Methylbenzene-1,2-Diamine (JSH-21) Analogs on Nitric Oxide Production and Nuclear Factor-kappa B Transcriptional Activity in Lipopolysaccharide-Stimulated Macrophages RAW 264.7

  • Min, Kyung-Rak;Shin, Hyun-Mo;Lee, Jee-Hyun;Kim, Byung-Hak;Chung, Eun-Yong;Jung, Sang-Hun;Kim , Young-Soo
    • Archives of Pharmacal Research
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    • v.27 no.10
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    • pp.1053-1059
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    • 2004
  • $N^1$-Benzyl-4-methylbenzene-1,2-diamine (JSH-21) and its analogs were chemically synthesized and their anti-inflammatory potentials investigated. JSH-21 inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 in a dose-dependent manner, with an $IC_{50}$ value of 9.2 ${\mu}M$, where pyrrolidine dithiocarbamate and parthenolide as positive controls exhibited $IC_{50}$ values of 29.3 and 3.6 ${\mu}M$, respectively. The inhibitory effect of JSH-21 on the NO production was attributable to its down-regulatory action on LPS-inducible NO synthase (iNOS), which was documented by iNOS promoter activity. In the mechanism of the anti-inflammatory action, JSH-21 exhibited inhibitory effects on LPS-induced DNA binding activity and transcriptional activity of nuclear factor-kappa B (NF-$_KB$). Structural analogs of JSH-21 also inhibited both the LPS-induced NO production and NF-$_KB$). transcriptional activity, where diamine substitution at positions 1 and 2 of JSH-21 seems to play an important role in the anti-inflammatory activity.

Inhibitory Effects of Marine Algae Extract on Adipocyte Differentiation and Pancreatic Lipase Activity

  • Kim, Eun-Sil;Lee, Kyoung-Jin;Oh, Kyoung-Hee;Ahn, Jong-Hoon;Kim, Seon-Beom;Liu, Qing;Hwang, Bang-Yeon;Lee, Mi-Kyeong
    • Natural Product Sciences
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    • v.18 no.3
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    • pp.153-157
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    • 2012
  • Obesity, which is characterized by excessive fat accumulation in adipose tissues, occurs by fat absorption by lipase and sequential fat accumulation in adipocyte through adipocyte differentiation. Thus, inhibition of pancreatic lipase activity and adipocyte differentiation would be crucial for the prevention and progression of obesity. In the present study, we attempted to evaluate anti-adipogenic activity of several algae extracts employing preadipocytes cell line, 3T3-L1 as an in vitro assay system. The effects on pancreatic lipase activity in vitro were also evaluated. Total methanolic extracts of Cladophora wrightiana and Costaria costata showed significant inhibitory activity on adipocyte differentiation as assessed by measuring fat accumulation using Oil Red O staining. Related to pancreatic lipase, C. wrightiana and Padina arborescens showed significant inhibition. Further fractionation of C. wrightiana, which showed the most potent activity, suggested that $CHCl_3$ and n-BuOH fraction are responsible for adipocyte differentiation inhibition, whereas n-BuOH and $H_2O$ fraction for pancreatic lipase inhibition. Our study also demonstrated that n-BuOH fraction was effective both in early and middle stage of differentiation whereas $CHCl_3$ fraction was effective only in early stage of differentiation. Taken together, algae might be new candidates in the development of obesity treatment.

III. Investigation on Allelopathic Effect from Various Crosses of Rice Cultivars (III. 벼 교잡종의 Allelopathy 효과 구명)

  • Lee, Jae-Hyun;Shin, Dong-Hyun;Lee, In-Jung;Kim, Kil-Ung
    • Current Research on Agriculture and Life Sciences
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    • v.20
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    • pp.65-70
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    • 2002
  • This study was conducted to investigate allelopathic potential of various crosses of rice cultivars using their inhibitory effect on barnyardgrass growth under field conditions, and to determine PAL activity and phenolic compounds involved in phenylpropanoid pathway from selected crosses of rice cultivars. Under field conditions, Kouketsumochi, Woo co chin yu possessed higher allelopathic potential inhibiting over 90% of barnyardgrass growth. Crosses of Kouketsumochi/Woo co chin yu, Dongjinbeyo/Kouketsumochi, Dongjinbeyo/Woo co chin yu showed over 80% inhibitory effects on barnyardgrass growth. The highest PAL activity, $63.46{\mu}kats/kg$ proteins was detected in Kouketsumochi which is the most important enzyme in phenylpropanoid pathway and also higher PAL activity in crosses with Kouketsumochi. Content of cinnamate was $2.64{\mu}g/g$ f.w. in Kouketsumochi which was 2 to 5 times higher than other rice cultivars tested, indicating that higher PAL activity resulted in more cinnamate. The similar trends in cinnamate content and PAL activity were observed in crosses of rice cultivars with Kouketsumochi.

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Antioxidant and Antimicrobial Activity of Rosa multiflora Thunberg Fruits Extracts

  • Cho, Young-Je
    • Current Research on Agriculture and Life Sciences
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    • v.31 no.3
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    • pp.170-176
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    • 2013
  • In this study, we selected some material to have potential bioactivity from natural plants, confirmed as basic data for industrializing and tried to develope the food materials using them. DPPH, ABTS, antioxidant protection factor, TBARs and antimicrobial activity of extracts from Rosa multiflora Thunberg fruits were determined. The total phenolics extracted from Rosa multiflora were 12.08, 11.82, 11.1 and 12.6 mg/g when using water, 70% ethanol, 70% methanol and 70% acetone as the solvent, respectively. The optimum conditions for extracting the phenolic compounds were 70% ethanol over for 12 hrs(11.82 mg/g). The electron donating ability and inhibition rate on ABTS of the 70% ethanol extracts were 97% and 92.2%, respectively while the antioxidant protection factor(PF) of the water extracts and 70% ethanol extracts were 1.79 and 1.34 PF, respectively. The TBAR (thiobarbituric acid reactive substance) value were $1.3{\mu}M$ for the control and $0.15{\mu}M$ for the 70% ethanol extracts. The inhibitory activity against ${\alpha}$-amylase was 26% for the 70% ethanol extracts. The 70% ethanol extracts from Rosa multiflora Thunberg fruits exhibited antimicrobial activity against H. pylori, S. epidermidis, S. aureusand and E. coli with clear zone diameters of 14, 25, 14 and 13 mm, respectively when using $200{\mu}g/mL$ of the phenolic compounds. An HPLC analysis identified 6 major phenolic metabolites in the Rosa multiflora Thunberg fruits extracts: rosmarinic acid, caffeic acid, chlorogenic acid, courmaric acid, protocatechuic acid and quercetin. In particular, the content of rosmarinic acid was the highest in the 70% ethanol extracts. Therefore these results indicate that 70% ethanol extracts from Rosa multiflora Thunberg fruits can be useful as a natural antioxidant and in functional foods.

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Comparison of phytochemical composition and physiological activity of 'Hongsan' and 'Hansan', a new variety of garlic (마늘 신품종 홍산과 한산의 식물화학적 구성 및 생리활성 비교)

  • Kim, Ju-Sung;Ra, Jong Hwan
    • Korean Journal of Food Science and Technology
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    • v.51 no.2
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    • pp.147-151
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    • 2019
  • This study was performed to investigate the physiological activity of Hongsan garlic and Hansan garlic, which were registered in the plant breeders' right in 2016. The content of mineral components, except sodium and sulfur ingredients, was found to be high in Hansan garlic. In addition, organic sulfur components were high in Hansan garlic. Moreover, the total soluble solid content, reducing sugar content, and alpha glucosidase inhibitory activity were high in Hansan garlic. Acidity, pH, total phenol, and flavonoid content were high in Hongsan garlic. Both varieties showed higher inhibitory activity to gram-positive bacteria than to gram-negative bacteria. The antimicrobial activity of Hongsan garlic was slightly higher than that of Hansan garlic. These results are expected to provide useful information to farmers who grow the above garlic varieties.

Comparison of Antioxidant and Physiological Activities in Various Solvent Extracts of Ixeris repens (갯씀바귀(Ixeris repens) 추출물의 항산화성 및 생리활성)

  • Kim, Joo-Sung;Lee, Yeon-Ji;Kim, Ji-Youn;Choi, Ji-Won;You, Sun-Jae;Kim, Yong-Tae
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.54 no.5
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    • pp.742-750
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    • 2021
  • Ixeris repens is a type of halophyte that grows in high salinity sands found in coastal sand dunes and sandy shores. This study was conducted to investigate the contents, antioxidant potency, and physiological activities of I. repens. In analyses of general composition, carbohydrate, protein, ash, and moisture content were 57.42%, 10.48%, 11.99% and 10.29%, respectively. Potassium, calcium, sodium, and magnesium were its most prevalent minerals. The solvents used to extract I. repens were 70% ethanol, 80% methanol, and distilled water. Among the resultant extracts, ethanol and methanol extracts displayed higher total polyphenol and flavonoid contents than the water extract. ABTS (IC50, 0.12 mg/mL) and FRAP (0.77 mM) radical scavenging activity were highest in the water extract, while methanol extract exhibited the strongest DPPH radical scavenging activity (IC50, 1.32 mg/mL), NO scavenging activity (IC50, 4.10 mg/mL), and reducing power (EC50, 0.14 mg/mL). Tyrosinase, elastase, and α-glucosidase inhibitory activities were highest in the ethanol extract. The ethanol extract also possessed the most potent acetylcholinesterase inhibitory activity. These results indicate that I. repens may be useful as an antioxidant, and a functional substance in food and pharmaceutical materials.

Vaccinium oldhamii Stems Inhibit Pro-inflammatory Response and Osteoclastogenesis through Inhibition of NF-κB and MAPK/ATF2 Signaling Activation in LPS-stimulated RAW264.7 Cells

  • Park, Su Bin;Kim, Ha Na;Kim, Jeong Dong;Jeong, Jin Boo
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2019.10a
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    • pp.67-67
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    • 2019
  • Vaccinium oldhamii (V. oldhamii) has been reported to exert a variety of the pharmacological properties such as anti-oxidant activity, anti-cancer activity, and inhibitory activity of ${\alpha}$-amylase and acetylcholinesterase. However, the anti-inflammatory activity of V. oldhamii has not been studied. In this study, we aimed to investigate anti-inflammatory activity of the stem extracts from V. oldhamii, and to elucidate the potential mechanisms in LPS-stimulated RAW264.7 cells. Among VOS, VOL and VOF, the inhibitory effect of NO and PGE2 production induced by LPS was highest in VOS treatment. Thus, VOS was selected for the further study. VOS dose-dependently blocked LPS-induced NO and PGE2 production by inhibiting iNOS and COX-2 expression, respectively. VOS inhibited the expression of pro-inflammatory cytokines such as $IL-1{\beta}$, IL-6 and $TNF-{\alpha}$. In addition, VOS suppressed TRAP activity and attenuated the expression of the osteoclast-specific genes such as NFATc1, c-FOS, TRAP, MMP-9, cathepsin K, CA2, OSCAR and ATPv06d2. VOS inhibited LPS-induced $NF-{\kappa}B$ signaling activation through blocking $I{\kappa}B-{\alpha}$ degradation and p65 nuclear accumulation. VOS inhibited MAPK signaling activation by attenuating the phosphorylation of ERK1/2, p38 and JNK. Furthermore, VOS inhibited ATF2 phosphorylation and blocked ATF2 nuclear accumulation. From these findings, VOS has potential to be a candidate for the development of chemopreventive or therapeutic agents for the inflammatory diseases.

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Inhibitory Effect of Osteoclastogenesis and Estradiol Activity of Myelophycus simplex Extract (바위수염 추출물의 파골세포 분화 억제 및 에스트라디올 활성 평가)

  • Ha, Hyun Joo;Lim, Hyung Jin;Kim, Min Gyeong;Bak, Seon Gyeong;Rho, Mun-Chual;Cheong, Sun Hee;Lee, Seung-Jae;Lee, Sang-Hoon
    • Journal of Marine Bioscience and Biotechnology
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    • v.12 no.2
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    • pp.75-80
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    • 2020
  • In the present study, the estrogenic activity and anti-osteoclastogenic activity of the Myelophycus simplex extract were evaluated using T47D-Kbluc cells and bone marrow-derived macrophages (BMMs). As a result of the measurement of the estrogenic activity in the T47D-Kbluc cell line, the Myelophycus simplex extract showed increased estrogenic activity in a dose-dependent manner in association with its concentration. To confirm the regulatory effect of the Myelophycus simplex extract on the estrogen-responsive gene, the Myelophycus simplex extract showed a similar tendency to estradiol: the expression of estrogen receptor 1 (ESR1) was significantly decreased while the expression of estrogen receptor 2 (ESR2) was increased. Furthermore, the Myelophycus simplex extract exhibited an inhibitory effect on osteoclast differentiation. In conclusion, these Myelophycus simplex extracts might be regarded as candidates for further studies or the development of functional food products or medicine to prevent or avoid postmenopausal symptoms for women.

Development of Antibacterial Using Several Wild Flowers (야생화를 이용한 살균제 개발)

  • Jung, J.H.;Park, N.B.
    • Journal of Practical Agriculture & Fisheries Research
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    • v.21 no.1
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    • pp.71-80
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    • 2019
  • We have been experimenting for industrialize four kinds of wildflowers(Smilax china, Saururus chinensis, Houttuynia cordata and Zizania caduciflora) which are used for Korean medicinal plants for a long time as Korean resources plants. Smilax china, Saururus chinensis, Houttuynia cordata was used for roots and Zizania caduciflora used for leaves. Extraction was carried out in 50% ethyl alcohol, which was concentrated by freezing the material and then injected at a low concentration of 100ppm. The results of the study on the antibacterial potential activity and antifungal potential activity using the four wildflowers strains were as follows. 1. The results of the sterilization and antibacterial potential activity and antifungal potential activity were as follows. Houttuynia cordata showed good inhibitory effect for Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa. The inhibitory power of Zizania caduciflora was proved to some extent. However, other cultivars showed little antibacterial and antifungal activity. 2. The antifungal potential activity against Candida albicans, Aspergillus niger, Aspergillus fumigatus, and Cryptococcus neoformans was small but some inhibition against Candida albicans was confirmed. There was no inhibition of other fungi potential at all.

Antioxidant activity and MMP-1 inhibitory activity of Panax Ginseng Sprout Extracts (새싹인삼 추출물의 항산화 활성 및 MMP-1 저해 활성 )

  • Min-Jung Kim;Ye-Jin Yang;Ju-Hye Yang;Won-Yung Lee;Woo-Hyun Kim;Jae-Nam Lee;Kwang-Il Park
    • Herbal Formula Science
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    • v.32 no.1
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    • pp.83-90
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    • 2024
  • Objectives : As a substitute for high-price ginseng, this study attempted to examine a possibility of the ferment extract of Panax ginseng sprout whether leaves and roots can be used together as a cosmetic ingredient with anti-oxidative and wrinkle-care effects. Methods : In terms of a test method, antioxidant activities were confirmed through total polyphenol contents, total flavonoid contents, DPPH radical scavenging activity and ABTS radical scavenging activity using the Panax ginseng sprout. In addition, to assess wrinkle-care effectiveness, the cytotoxicity of the extract was analyzed through MTT assay, and inhibition of collagenase activity in the cells was tested using the Panax ginseng sprout fermented by Saccharomyces cerevisiae. Resuits : The content of polyphenols and flavonoids in natural plants was highest in Panax Ginseng Sprout Extract at 100℃, which also demonstrated high DPPH, ABTS radical scavenging activity. MTT assay demonstrated that the Panax Ginseng Sprout Ferment Extract did not have a cytotoxic effect in CCD-986SK cell. Also, Panax Ginseng Sprout Ferment Extract was found to inhibit MMP-1 expression by 51.85±6.09% at a concentration of 10%. Conclusions : Therefore, this study has confirmed a possibility of Panax ginseng sprout ferment extract as a cosmetic ingredient with MMP-1-inhibitory effects.