• Journal of Marine Bioscience and Biotechnology
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• v.5 no.4
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• pp.33-39
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• 2011

As a rapid and quick bioactive compound evaluation technique, we utilized an automatic system of high throughput screening (HTS) to investigate ${\alpha}$-glucosidase inhibitory efficacy of seaweeds, collected from Jeju Island in Korea. In this study, different extracts with methanol at $20^{\circ}C$ and $70^{\circ}C$ from 23 species of brown seaweeds and 22 species of red seaweeds and 9 species of green seaweeds were subjected to HTS. Of the brown seaweeds tested, Myelophycus simplex (20B3), Ishige sinicola (20B5, 70B5), Colpomenia sinuosa, (20B14, 70B14), Hizikia fusiforme (20B21), Ishige okamurai (70B22) and Ecklonia cava (70B23) showed significantly high ${\alpha}$-glucosidase inhibitory activity with 96.52%, 98.34%, 98.37%, 80.49%, 96.16%, 76.32%, 98.32% and 98.12%. Schizymenia dubyi (20R15), Gelidium amansii (20R16) and Polysiphonia japonica (70R22) amomng the red seaweeds showed remarkable ${\alpha}$-glucosidase inhibitory activity more than 95%. On the other hand, the green seaweeds showed poor ${\alpha}$-glucosidase inhibitory activities (less the10%) at 1 mg/ml.

• KSBB Journal
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• v.25 no.4
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• pp.330-336
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• 2010

In this study, a new compound, 1-(2-hydroxy-3,4,5,6-tetramethoxyphenyl)-1-methoxy-3-phenylpropane; (Jeju-Erythrane) was isolated and identified from the bark of Lindera erythrocarpa Makino. Also, we investigated the effects of Jeju-Erythrane on alpha melanocyte-stimulating hormone (MSH)-induced melanogenesis in mouse B16F10 melanoma cells. The new compound dose dependently inhibited the tyrosinase activity and melanin synthesis in B16F10 cells. The new compound showed inhibitory effect on the Tyrosinase and TRP-1 gene transcription but not on the TRP-2 gene. These results suggest that the new compound of L. erythrocarpa could be used as a functional biomaterial in developing skin whitening agent.

• Applied Biological Chemistry
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• v.46 no.1
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• pp.60-65
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• 2003

MMP-1 inhibitory compounds were isolated from 120 Korean traditional edible plants. UP- 1 activity significantly increased linearly with increasing UVB dose in normal human foreskin fibroblast HS68 cell, showing maximum activity at approximately 35 $mJ/cm^2$, whereas in HaCaT cell, normal human keratinocyte, no increase was observed. Maximum secretion of MMP-1 after UVB treatment occurred around 36-48 k after treatment. MMP-1 inhibitory compound isolated from cold-water fraction of Cataegus pinnatifida Bunge showed the mort potent activity. The MMP-1 inhibitory compound was deduced as a peptide based on the fact that pronase digestion decreased the activity whereas periodate oxidation did not. The most potent UP- 1-inhibitory protein, CP-2Va-2, showing an activity of 88.5% against MMP-1, was isolated through sequential column chromatography on DEAE-Toyopearl 650C, Butyl-Toyopearl 650M, and Bio-Gel P-30. Molecular weight of CP-2Va-2 determined through high performance liquid chromatography and SDS PACE was 19 and 20 kDa. respectively, signifying a monomeric structure.

• Journal of Life Science
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• v.29 no.7
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• pp.755-761
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• 2019

Kojic acid (KA) is produced by Aspergillus oryzae-sort of like mushrooms, which is commonly called as koji in Japan. KA is used as a chelation agent and a preservative preventing oxidative browning of fruits. KA also shows antibacterial and antifungal properties. Because KA stops the production of melanin by inhibiting tyrosinase in the biosynthetic pathway from tyrosine to melanin in skin, it has been applied as a skin lightening ingredient in cosmetics. Since some animal studies have shown that high amounts of KA had side effects such as in liver, kidney, reproductive, cardiovascular, gastrointestinal, respiratory, brain, and nervous system, more efficient KA derivatives are needed to be developed in order to safely apply as a skin lightening ingredient. A series of KA derivatives via conjugated with triazole by click reaction were synthesized and their in vitro tyrosinase inhibitory activities were evaluated. Most of all KA derivatives have shown in moderate tyrosinase inhibitory activities. In case of KA-hybrid compound, 1~3 have shown tyrosinase inhibitory activities about 50~10,000 times more effective tyrosinase inhibitor compared to KA itself. Specifically, the $IC_{50}$ value of KA-hybrid compound, 2 was $0.0044{\pm}0.74{\mu}M$ against tyrosinase. It is about 10,000 times more effective tyrosinase inhibitor compared to KA itself ($IC_{50}=45.2{\pm}4.6{\mu}M$).

• Food Science and Preservation
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• v.24 no.2
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• pp.282-288
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• 2017

This study provided the evidence activity for biological of phenolic compounds from Trachelospermum asiaticum var. intermedium nakaier as a beauty food. The contents of phenolic compounds in water and 70% ethanol extracts were 16.8 mg/g and 38.1 mg/g, respectively. DPPH free radical scavenging activities of water and ethanol extracts at $100{\mu}g/mL$ of phenolic concentration were 80.9% and 83.1%, respectively. ABTS radical decolorization activity was 95.0% in water extracts and 95.8% in ethanol extracts at $200{\mu}g/mL$ phenolic concentration. Antioxidant protection factor (PF) was determined to 2.43 and 2.45 PF in water extracts and ethanol extracts at $100{\mu}g/mL$ phenolic concentration. TBARs of water and ethanol extracts were 89.9% and 89.3% each at $200{\mu}g/mL$ phenolic concentration. The inhibitory effect of ethanol extracts at $200{\mu}g/mL$ phenolic concentration on xanthine oxidase was 50.5%. The inhibitory activity of a-glucosidase was 92.6% in ethanol extracts at $200{\mu}g/mL$ phenolic concentration. As a result, this study will provide valuable information as a functional material with antioxidant activity, inhibitory activities of xanthin oxidase and ${\alpha}-glucosidase$.

• Korean Journal of Organic Agriculture
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• v.22 no.3
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• pp.469-481
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• 2014

IIn vitro antimicrobial and anti-inflammatory activities of nargenicin and its derivatives were investigated. Nargenicin, an unusual macrolide antibiotic with potent anti-MRSA (methicilin-resistant Staphylococcus aureus) activity, was purified from the culture broth of Nocardia sp. CS682. And variety of novel nargenicin derivatives was synthesized from nargenicin. Two compounds (4 and 5) exhibit a broad spectrum of antimicrobial activities against infectious bacteria. The antimicrobial activity of derivatives against fifteen organisms was assessed using the minimum inhibitory concentration (MIC). The MIC values were in the ranges of $0.15{\sim}80{\mu}g/mL$ (w/v) for compound 1 and 2, $5{\sim}80{\mu}g/mL$ (w/v) for compound 3, $1.25{\sim}40{\mu}g/mL$ (w/v) for compound 4, and $1.25{\sim}80{\mu}g/mL$ (w/v) for compound 5, depending on the pathogens studied. In vitro, we investigated cytotoxicity and inhibition of nitric oxide (NO) production of synthesized compounds 1-5 in Raw 264.7 cells. LPS-induced nitric oxide releases were significantly blocked by compound 3, 4 and 5 in a dose-dependent manner. At high concentrations ($5{\mu}g/mL$) compound 5 inhibited the NO production by 95%. Compound 4 inhibited the release of NO in LPS-activated Raw 264.7 cells by 75% at the concentration of $10{\mu}g/mL$. Compound 3 inhibited the release of NO in LPS-activated Raw 264.7 cells by 65% at the concentration of $100{\mu}g/mL$. On the other hand, nargenicin, compound 1 and 2 did not inhibit NO production. These results demonstrated that compound 4 and 5 displayed antimicrobial activity and blocked LPS-induced pro-inflammatory mediators such as NO in macrophages, which might be responsible for its therapeutic application.

• Applied Chemistry for Engineering
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• v.26 no.4
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• pp.470-476
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• 2015

In this study, three dicaffeoylquinic acids (DCQAs) isolated from Gnaphalium affine D. DON. extracts were structurally identified and evaluated for their antioxidant activities, cellular protective effects, and tyrosinase inhibitory activities. The ethyl acetate fraction of G. affine was chromatographed, which yielded 3 DCQA derivatives of 1-3 : 3,5-dicaffoylquinic acid (3,5-DCQA, 1), 4,5-dicaffeoylquinic acid (4,5-DCQA, 2), 1,5-dicaffoylquinic acid (1,5-DCQA, 3). The structure of each compounds was determined using $^1H$ NMR and MS analyses. Compounds of 1-3 showed strong free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activities ($FSC_{50}=3.70$, 5.80, and $5.50{\mu}M$, respectively) compared to those of a commonly used lipophilic antioxidant, (+)-${\alpha}$-tocopherol ($21.90{\mu}M$). Cellular protective effects of 1-3 compounds on the $^1O_2$ sensitized photohemolysis of human erythrocytes were similar to (+)-${\alpha}$-tocopherol. 1-3 compounds also exhibited higher tyrosinase inhibitory effects ($IC_{50}=0.15$, 0.16, and 0.13 mM) compared to arbutin (0.33 mM), known as a skin-whitening agent. These results indicate that three DCQA derivatives may be applied as an antioxidant and a skin whitening agent in food or cosmetic industries.

• Journal of Physiology & Pathology in Korean Medicine
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• v.27 no.1
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• pp.83-91
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• 2013

Pruritus is a unpleasant symptom in the skin that provokes the act of or desire to scratch. Mast cells are important effector cells in allergic reactions such as pruritus and inflammation. The purpose of this study was undertaken to investigate the synergic anti-pruritic and anti-inflammatory effects of Scutellariae Radix (SB) plus Flos Loncerae (FL) extracts in rat peritoneal mast cells (RPMCs), pruritogen-induced scratching mice and 2,4-dinitrofluorobenzene (DNFB)-induced allergic mice. We investigated the effect of SB, FL and SB plus FL extracts on the production of tumor necrosis factor (TNF)-${\alpha}$, interleukin (IL)-$1{\beta}$, and histamine in RPMCs, on the scratching behavior in ICR mice, and skin clinical serverity and inflammatory mediators in DNFB-induced allergic hairless mice. RPMCs stimulated with PMA plus A23187 or compound 48/80 significantly increased TNF-${\alpha}$, IL-$1{\beta}$ or histamine production compared with media control. However, TNF-${\alpha}$ IL-$1{\beta}$ or histamine levels increased by PMA plus A23187 or compound 48/80 treatment were significantly inhibited by SB, FL in a dose-dependent manner. Especially, SB plus FL pretreatment had a synergic inhibitory effects on stimulator-induced cytokines (TNF-${\alpha}$ and IL-$1{\beta}$) and histamine production. Moreover, SB plus FL administration had a synergic inhibitory effects on the scratching behavior induced by pruritogen (compound 48/80, histamine, serotonin, substance P) in ICR mice. Furthermore, SB plus FL administration had a synergic inhibitory effects on skin damage, inflammatory mediators, leukocyte and mast cell infiltration induced by DNFB in hairless mice. These results suggest that SB plus FL administration has a potential use as a medicinal plant for treatment against itching and inflammation-related skin disease.

• Journal of the Korean Society of Food Science and Nutrition
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• v.36 no.2
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• pp.155-162
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• 2007

The purpose of this study is to investigate the anti type I allergic effects and mechanisms of the phyto extract mixture (PEM381) which contains Camellia sinensis (leaf), Psidium guajava (leaf), and Rosa hybrida (flower). PEM381 was tested for its inhibitory effects on arachidonic acid cascade related enzymes (5-lipoxygenase and cyclooxygenase), the mast cell mediated allergic reaction and passive cutaneous anaphylaxis. $IC_{50}$ value of PEM381 against 5-lipoxygenase was $14.11{\pm}0.51ppm$ while that of positive control (nordihy-droguaiaretic acid) was $0.54{\pm}0.08ppm$. PEM381 also exhibited considerable selective inhibition of cyclooxygenase-2. PEM381 could inhibit both degranulation and histamine release in a dose dependent manner from rat peritoneal mast cells activated by compound 48/80. In addition, oral administration of PEM381 showed an inhibitory effect on passive cutaneous anaphylaxis reaction activated by anti-dinitrophenyl IgE antibody in mice. These results suggest that PEM381 may be useful for the prevention and treatment of type Ⅰ allergy related diseases.

• Journal of Microbiology and Biotechnology
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• v.6 no.4
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• pp.245-249
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• 1996

A cytotoxic compound, 8461 was isolated from the culture of Streptomyces sp. strain MCY846 by its cytotoxicity against gastric cancer cell line SNU-l. The IR, UV and NMR spectra of 8461 were identical to those of elaiophylin. This compound showed moderate cytotoxicity against several cell lines and exerted strong inhibitory effect on the synthesis of nitric oxide in the lipopolysaccharide stimulated-Raw 264.7 cells.