• Journal of Life Science
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• v.15 no.5 s.72
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• pp.796-801
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• 2005

For usage of natural antioxidants, sanjook (Sasa boreails var. chiisanensis) leaves were extracted with methanol and investigated about its antioxidative activities and stability. It showed that the antioxidant activity of methanol extracts from the leaves of sanjook depend on their concentration within range of 0.1 to 0.8 mg/ml. The methanol extracts from the leaves of sanjook represented $583{\mu}g/ml$ for $IC_{50}$ of DPPH radical scavenging ability, $800{\mu}g/ml$for $IC_{50}$ of SOD-like activity and $38{\mu}g/ml$for $IC_{50}$ of $H_{2} O_{2}$ scavenging ability, while BHT, as a compared substance, was $271{\mu}g/ml$ for $IC_{50}$ of DPPH radical scavenging ability, $680{\mu}g/ml$ for $IC_{50}$ of SOD-like activity and $30{\mu}g/ml$ for $IC_{50}$ of $H_{2} O_{2}$ scavenging ability, respectively. The anti-au-toxidation effect for methanol extracts from the leaves of sajook was $55\∼60\%$ within range of 0.1 to 0.8 mg/ml. The pH stability on methanol extracts from the leaves of sanjook was most stable at pH 6. The more acid or akali it became, the more unstable it turned. The thermostability on methanol extracts from the leaves of sanjook remained above $80\%$ of their DPPH activity at range of $0^{\circ}C{\;}to{\;}120^{\circ}$.

• Natural Product Sciences
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• v.5 no.3
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• pp.113-120
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• 1999

Nitric oxide (NO) is a free radical synthesized from L-arginine by nitric oxide synthase (NOS). It is believed that NO is an important mediator in numerous physiological and inflammatory responses. Particularly, a large amount of NO released from the inducible nitric oxide synthase (iNOS) is mostly associated with inflammatory processes. Overproduction of NO in these processes including sepsis and autoimmune diseases can have deleterious consequences and pathophysiologic relevance. Therefore, for the discovery of new inhibitory agents against iNOS activity, we have evaluated about 100 kinds of natural products after partition into three layers (n-hexane, ethyl acetate and aqueous) from 100% methanol extracts to study inhibitory effects on iNOS activity induced by lipopolysaccharide (LPS) in RAW264.7 cells culture system. As a positive control, curcumin, which is known as an anti-tumor promoter, anti-inflammatory agent as an iNOS inhibitor, was used and showed the dose-dependent inhibitory effect $(IC_{50},\;2.5\;{\mu}g/ml)$. Among tested fractions, the n-hexane fraction of Cimicifuga heracleifolia $(IC_{50}:\;9.65\;{\mu}g/ml)$, Forsythiae fructus $(IC_{50}:\;6.36\;{\mu}g/ml)$, Saposhnikovia divaricata $(IC_{50}:\;5.92\;{\mu}g/ml)$, and the ethyl acetate fraction of Chrysanthemum sibiricum $(IC_{50}:\;2.56\;{\mu}g/ml)$, Gastrodia elata $(IC_{50}:\;3.46\;{\mu}g/ml)$, and the aqueous fraction of Dianthus chinensis $(IC_{50}:\;6.73\;{\mu}g/ml)$, Euonymus alatus $(IC_{50}:\;6.78\;{\mu}g/ml)$, Mechania urticifoloria $(IC_{50}:\;8.01\;{\mu}g/ml)$ showed strong inhibitory activity against LPS-stimulated iNOS. Especially, the ethyl acetate fraction of Chrysanthemum sibiricum $(IC_{50}:\;2.56\;{\mu}g/ml)$, which exhibited the strongest inhibition against iNOS, was fractionated with silica-gel column chromatography. These subfractions exhibited dose-dependent inhibition against iNOS activity in the range of $2.59-5.6\;{\mu}g/ml$ except for fraction No. 3, 4, 5, 6, 8, 9, and 16. Our study shows that Chrysanthemum sibiricum has the strongest inhibitory effect against iNOS activity and has similar effect to curcumin. Therefore, further studies for the identification of active principles from Chrysanthemum sibiricum and investigation for the mechanism of the inhibition of iNOS by active principles will be performed.

• Journal of the Korean Chemical Society
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• v.43 no.4
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• pp.461-468
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• 1999

Acetolactate synthase (ALS) catalyzes the first common reaction in the biosynthesis of branched-chain amino acids, valine, leucine, and isoleucine. ALS is the common target of several classes of structurally diverse herbicides, the triazolopyrimidines, the imidazolinones, the sulfonylureas, and pyrimidyl-oxy-benzoates. We examined ihibitory activities of newly synthesized triazolopyrimidine sulfonamide derivatives using partially purified ALS from barley. $IC_{50}$ values for the active derivatives are 0.5nM∼8$\mu$M. Among them TP1 and TP2 are the most potent ALS inhibitors with $IC_{50}$ values of 0.5nM and 1.6nM, respectively. These inhibitors are more potent in the inhibition of barley ALS than commercial herbicides, Metosulam ($IC_{50}$;3.6 nM), Flumetsulam ($IC_{50}$;126 nM), and Cadre ($IC_{50};4 {\mu}M$). The progress curves for inhibition of ALS by TP2 showed that the amount of inhibition increases with time. The inhibition of ALS by TP2 was mixed-type inhibition with respect to pyruvate. Dual inhibition analyses of TP2 versus an imidazolinone, Cadre, and Leu showed parallel and intercepting kinetic pattern, respectively. The results suggest that TP2 binds to ALS competively with Cadre but not with Leu. Chemical modification of cysteinly residues in ALS decreased the sensitivity of ALS to Leu, while the modification did not affect the sensitivity of ALS to TP2 and Cadre.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.20 no.1 s.32
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• pp.115-129
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• 2007

Objectives : This study was carried out to evaluate anti-oxidative, anti-microbial and anti-cancer effect for clinical application of Bibangtalmyungsan (BTS) Results : 1. The oxidative effects were measured by polyphenol, DPPH radical scavenging activity. BTS water extract was showed more effective than ethanol extract and also various solvent fractions from BTS water extract showed effective in the following order : ethyl acetate fraction > butanol fraction > hexane fraction ${\fallingdotseq}$ chloroform fraction ${\fallingdotseq}$ aqueous fraction 2. The results of anti-microbial effects were as follows. 1) Antibacterial activities of BTS extracts against Gram's negative and positive bacteria were ineffective 2) Antifungal activities of the BTS extracts against Aspergillus spp. , Trichohyton mentagrophyte KTCC 1077 were not effective. 3. The result of anti-cancer effects were as followings: 1) BTS ethanol extract was more effective than water extract against Caco-2, Calu-6, but it had cytotoxic effect against NIH3T3. 2) On the Caco-2, effective only in ethyl acetate $fraction(IC_{50}:$ 35.81 ${\mu}g/ml)$. 3) On the Calu-6, the most effective in ethyl acetate $fraction(IC_{50}:$ 189.65 ${\mu}g/ml)$ and effective In butanol $fraction(IC_{50}:$ 299.74 ${\mu}g/ml)$ and hexane $fraction(IC_{50}:$ 345.13 ${\mu}g/ml)$ 4) On the SUN-601, $IC_{50}$ value was within 80 ${\mu}g/ml$ in ethyl acetate fraction and hexane fraction. 5) On the HCT-1l6, the most effective in ethyl acetate $fraction(IC_{50}:$ 82.94 ${\mu}g/ml)$ and effective in hexane $fraction(IC_{50}:$ 374.56 ${\mu}g/ml)$. 6) On the AML-2/WT, the most effective in ethyl acetate $fraction(IC_{50}:$ 41.44 ${\mu}g/ml)$ and effective In hexane $fraction(IC_{50}:$ 303.01 ${\mu}g/ml)$. 7) On the NIH3T3, effective only in ethyl acetate $fraction(IC_{50}:$ 203.42 ${\mu}g/ml)$, but it was more ineffective than other cancer cells. Conclusion : These result suggest that BTS has antioxidative, antifungal activities and cytotoxic effects against Caco-2, Calu-6, SUN-601, HCT-116, AML-2/WT and NIH3T3, especially ethyl acetate fraction from water extract has more effective in antioxidative and anticancer effects.

• Korean Journal of Pharmacognosy
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• v.44 no.4
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• pp.372-378
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• 2013

In this study, the inhibitory effect on advanced glycation end products (AGEs) formation of 43 Korean herbal medicines has been evaluated. Among them, 16 Korean herbal medicines were showed to have significant effect ($IC_{50}$; <50 ${\mu}g/ml$) compared to positive reference, aminoguandine ($IC_{50}$: $76.47{\pm}4.81{\mu}g/ml$). Especially, five herbal medicines, Rubus coreanus (leaves, $IC_{50}$: $4.49{\pm}0.03{\mu}g/ml$), Rubus coreanus (twigs, $IC_{50}$: $3.80{\pm}0.34{\mu}g/ml$), Ampleopsis brevipedunculata (stems, $IC_{50}$: $7.43{\pm}0.09{\mu}g/ml$), Lindera erythrocarpa (leave, $IC_{50}$: $8.14{\pm}0.20{\mu}g/ml$), and Lindera erythrocarpa (stems, $IC_{50}$: $3.69{\pm}0.14{\mu}g/ml$) showed more potent inhibitory activity (approximately 9-20 fold) than the positive control aminoguanidine.

• Korean Journal of Environmental Agriculture
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• v.7 no.2
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• pp.117-123
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• 1988

This study was initiated to understand the mechanism of selective toxicity of diazinon and carbofuran to killifish and loach. Conventional LC50 was calculated from fish test. IC50 with acetylcholinesterase activity was estimated using whole body and wet brain homogenate of the two fish species. Acetylcholinesterase activity of killifish was approximately twice as high as that of loach. The selective toxicity of diazinon to killifish and loach was partly (14 : 4) explained by the IC50 of diazoxon, a toxic metabolite of diazinon. IC50 of carbofuran also partly (14 : 3.4) contributed to the selectivity. These result suggested that the enzymatic method might be utilized as a screening tool for the chemicals affecting fish species of environmental concern with certain limitations which should be overcome in future studies.

• Biomedical Science Letters
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• v.11 no.4
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• pp.517-523
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• 2005

The purpose of this study was to determine the effect of rat intestinal a-glucosidase inhibitor; methanol $(80\%)$, ethanol $(80\%)$ and water extract of Schizandra chinensis in Korea (KS: Schizandra chinensis in Korea) and China (CS: Schizandra chinensis in China). When the final concentration was 1 mg/ml for each sample (KS and CS), methanol extract of KS ($IC_{50}$ 1.62 mg/ml) showed $46.8\%$, ethanol extract of KS ($IC_{50}$ 1.48 mg/ml) showed $47.4\%$, water extract of KS ($IC_{50}$ 1.72 mg/ml) showed $46.3\%$ and methanol extract of CS ($IC_{50}$ 8.35 mg/ml) showed $13.3\%$, ethanol extract of CS ($IC_{50}$ 8.05 mg/lml) showed $16\%$, water extract of CS ($IC_{50}$ 8.37 mg/ml) showed $11.54\%$ of inhibitor for p-nitrophenyl $\alpha-D-glucopyranoside$ (pNPG) $\alpha-glcosidase$ activity, respectively. And the contents of total phenol, flavonoid of Schizandra chinensis were measured. When the final concentration was 1mg/ml for each sample (KS and CS), total phenol and flavonoid in KS were higher than CS, respectively. The order superoxide dismutase (SOD) activity $IC_{50}$ values of each solvent extracts of KS were: 2.006 mg/ml methanol extract, 2.304 mg/ml ethanol extract and 2.5 mg/ml water extract, which were higher than that of each solvent extracts CS as: 2.881 mg/ml methanol extract, 3.085 mg/ml ethanol extract and 3.190 mg/ml water extract.

• International Journal of Advanced Culture Technology
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• v.8 no.3
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• pp.231-240
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• 2020

In this paper, we present to evaluate physiological activity of Asparagopsis armata extraction. After extraction with Asparagopsis armata using hydrothermal and supercritical carbon dioxide, various physiological activities were examined. The total concentration of polyphenol compounds was determined to be 18.85 mg/g of hydrothermal Asparagopsis armata extraction and 14.74 mg/g of supercritical Asparagopsis armata extraction. In DPPH radical scavenging assay, ascorbic acid was used as positive antioxidant control. In ABTS radical scavenging assay, ascorbic acid was used as positive antioxidant control. The percentage of inhibition and IC50 were measured. The IC50 of Asparagopsis armata extraction is 261.44ppm and the IC50 of supercritical Asparagopsis armata extraction is 153.98 ppm. The elastase inhibitory assay showed concentration dependence and the IC50 of hydrothermal Asparagopsis armata extraction is 3387 ppm and the IC50 of supercritical Asparagopsis armata extraction is higher than 2500 ppm. In mushroom tyrosinase inhibition experiments, tyrosinase inhibition's IC50 of supercritical Asparagopsis armata extraction was 248.06. In the SOD-like experiments, the concentration-dependent results were showed and IC50 of hydrothermal Asparagopsis armata extraction is 845.29 ppm. In the antimicrobial experiments, maximum clear zones of supercritical Asparagopsis armata extraction represented 23.00 mm in Propionibacterium acnes. In the other hand, in experiments with the same conditions, hydrothermal Asparagopsis armata extraction had no effect in all strains.

• Natural Product Sciences
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• v.3 no.1
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• pp.29-37
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• 1997

Protein Kinase C (PKC) is generally believed to play a central role in signal transduction, cellular growth control, gene expression, and tumor promotion. And it has been suggested that inhibitors of PKC might play important roles for the prevention and treatment of cancer. In order to investigate the possible inhibitors of PKC from natural products, PKC receptor binding assay was performed using bovine brain particulate as a source of PKC and the amount of $[^3H]Phorbol$ 12,13-dibutyrate (PDBu) bound to PKC was measured in the presence of test materials. Total methanol extracts from 100 kinds of natural products were partitioned into 3 fractions (n-hexane, ethyl acetate and aqueous layer) and their binding ability to the regulatory domain of PKC was evaluated. The ethyl acetate fractions of Morus alba $(roots,\;IC_{50}:\;156.6\;{\mu}g/ml)$, Rehmannia glutinosa $(roots,\;IC_{50}:\;134.3\;{\mu}g/ml)$, Lysimachia foenum-graecum $(roots,\;IC_{50}:\;167.8\;{\mu}g/ml)$, Polygonum cuspidata $(roots,\;IC_{50}:\;157.3\;{\mu}g/ml)$, Cnidium officinale $(aerial\;parts,\;IC_{50}:\;145.2\;{\mu}g/ml)$, and the hexane $(IC_{50}:\;179.3\;{\mu}g/ml)$ and the EtOAc fraction of Symplocarpus nipponicus $(roots,\;IC_{50}:\;155.9\;{\mu}g/ml)$ showed inhibitory activity of $[^3H]PDBu$ binding to PKC.

• Korean Journal of Food Science and Technology
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• v.39 no.6
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• pp.669-675
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• 2007

The present study was conducted to explore the anti-inflammatory action of $2-hydroxyethyl-{\beta}-undecenate$ (HPS) purified from Cumin (Cuminum cymium L.) seed against periodontitis. From the study in which human leukocyte was employed to detect the inhibiting effects of 5-lipokygenase and cyclooxygenase, enzymes generating carriers of infection like $LTB_4$ and PGs, as well as of collagenase and elastase, organ-destroying enzymes, following conclusions could be drawn: HPS was found to inhibit leukotrien $B_4$ biosynthesis by stimulating more than 97% of human polymorphonuclear leukocyte (PMNL) with addition of $5\;{\times}\;10^{-2}\;M$ when $IC_{50}$ was set at $2\;{\times}\;10^{-4}\;M$. Ninety-two percent of enzyme activation turned out to be inhibited when $5\;{\times}\;10^{-2}\;M$ was added in a test to prove inhibiting effects of HPS against activation of PMNL 5-lipoxygenase from homogeneous humans and purified 5-lipoxygenase on the market. Besides, $IC_{50}$ for enzyme activation was valued at $2.5\;{\times}\;10^{-4}\;M$, while the value of $IC_{50}$ for purified 5-lipoxygenase was $2.3\;{\times}\;10^{-4}\;M$. The $IC_{50}$ values of COX-activated leukocyte and purified collagenase were $5.1\;{\times}\;10^{-4}\;M$ and $2.3\;{\times}\;10^{-4}\;M$, respectively. Moreover, the value of $IC_{50}$ for activation of leukocyte collagenase was $2\;{\times}\;10^{-3}\;M$, whereas that for purified collagenase was $5\;{\times}\;10^{-2}\;M$. In case of leukocyte elastase, addition of $5\;{\times}\;10^{-2}\;M$ inhibited its activation by 66%. In case of purified one, however, activation of enzyme was inhibited by 25% with addition of $5\;{\times}\;10^{-2}\;M$. Furthermore, the $IC_{50}$ value for activation of leukocyte elastase was revealed to be $7.5\;{\times}\;10^{-3}\;M$. From the virulence test with human gingiva cell, it was shown that, on the second day of cultivation, 47.83% of the cell had been activated when HPS was added by $5\;{\times}\;10^{-2}\;M$. Even the addition of HPS by $1\;{\times}\;10^{-2}\;M$ featured 68.53% of cell activation, suggesting relatively strong toxicity of the substance against gingiva cell.