• 생명과학회지
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• 제15권5호
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• pp.796-801
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• 2005

국내산 산죽잎을 methanol로 추출하여 천연 항산화제로서의 이용성을 조사하기 위하여 여러 방법으로 항산화 활성을 측정하고 안정성에 대해 조사하였다. 산죽잎 메탄올 추출물은 0.1 mg/l에서 0.8mg/ml의 범위에서 농도 의존적으로 항산화활성이 증가하였다. 산죽잎 메탄올추출물은 DPPH radical 소거능에 대한 $IC_{50}$ 값은 $583{\mu}g/ml$, SOD 유사활성능에 대한 $IC_{50}$값은 $800{\mu}g/ml$, hydrogen peroxide 소거능에 대한 $IC_{50}$값은 $38{\mug}/ml$이 었으며 대조구로 사용한 BHT의 각각 의 $IC_{50}$값은 $271{\mu}g/ml,{\;}680{\mu}g/ml,{\;}30{\mu}g/ml$이었다. 산죽잎 메탄올추출물의 자동산화 억제능은 상기 농도 범위에서 $55\∼60\%$의 억제효과를 나타내었다. 산죽잎 메탄올추출물의 pH 안정성은 pH 6에서 안정하였으나 산성이나 알카리성으로 갈수록 pH 안정성은 떨어졌다. 산죽잎 메탄올추출물의 열안정성은 $0^{\circ}C$에서 $120^{\circ}C$의 온도범위에서 $80\%$ 이상의 항산화능을 유지하였다.

• Natural Product Sciences
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• 제5권3호
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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.

• 대한화학회지
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• 제43권4호
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• pp.461-468
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• 1999

Acetolactate synthase (ALS)는 가지를 가진 필수아미노산 Val, Leu, Ile의 생합성 과정에서 공통적으로 작용하는 효소이다. ALS는 서로 구조적 유사성이 없는triazolopyrimidine, imidazolinone,sulfonylurea, 그리고 pyrimidyl-oxy-benzoate 제초제들의 공통적인 작용 표적이다. 보리로부터 부분 정제한 ALS를 이용하여 새로이 합성한 triazolopyrimidine sulfonamide 유도체들의 저해 활성을 측정하였다. 활성을 가진 유도체들의 $IC_{50}$ 값은 0.5nM∼8${\mu}M$ 범위였으며, 그 중에서 탁월한 저해 활성을 갖는 것은 TP1과TP2 유도체로 $IC_{50}$ 값은 각각 0.5 nM과 1.6 nM이였다. 이 저해제들은 기존의 상품화된 제초제인 Metosulam ($IC_{50}$;3.6 nM), Flumetsulam ($IC_{50}$;126 nM), 그리고 Cadre ($IC_{50};4 {\mu}M$)에 비해 보리 ALS에 대한 저해 활성이 보다 우수하였다. 보리 ALS에 대한 TP2의 저해 활성은 반응시간이 증가함에 따라 증가하였고, 혼합형 저해 유형을 보였다. TP2와 imidazolinone 계열의 제초제인 Cadre, 그리고 되먹임(feedback) 저해제인 Leu에 대한 이중저해 (dual inhibition) 실험 결과 TP2와 Cadre의 경우는 평행한 반응속도론적 형태가 그러나 TP2와 Leu의 경우는 한 점에서 만나는 반응속도론적 헝태가 얻어졌다. 이는 TP2와 Cadre의 결합 부위가 최소한 부분적으로 중복되고 있음을 시사한다. Cys 잔기에 대한 화학적 변형은 TP2와 Cadre의 결합에는 영향을 미치지 않으나, Leu의 결합에는 영향을 미쳤다.

• 한방안이비인후피부과학회지
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• 제20권1호통권32호
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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.

• 생약학회지
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• 제44권4호
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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.

• 한국환경농학회지
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• 제7권2호
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• pp.117-123
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• 1988

본 연구에서는 diazinon과 carbofuran의 송사리와 미꾸리에 대한 선택적 어독성 기작을 규명코자 뇌와 몸체에서 acetylcholinesterase(AchE)를 추출하여 활성을 측정하였다. 또 농약에 의한 효소의 활성저해도(IC50)를 측정하였으며 이를 급성 어독성 실험에서 얻어진 LC5O값과 비교하였는데 그 결과는 다음과 같았다. 송사리의 AchE의 활성은 미꾸리의 활성보다 2배 높았고, diazinon과 carbofuran의 선택적 독성은 diazinon의 대사산물인 diazoxon의 두 어종에 대한 IC50 값이 미꾸리가 송사리보다 4배 낮고, carbofuran의 IC50값은 송사리가 미꾸리보다 약 3.4배 낮으므로,IC50 값에 의하여 부분적으로는 설명될 수 있었다. 따라서 AchE을 이용하여 유기인계 및 카바메이트계 농약의 독성을 검색하는데 있어 동일농약인 경우 어종간의 감수성을 부분적으로 설명할 수 있기 때문에 농약의 독성을 1차적으로 검색할 수 있는 수단이 될 것으로 사료된다. 그러나 위의 방법이 본격적으로 사용될 수 있기 위해서는 농약의 종류와 어종을 다양화한 실험과 흡수, 체내에서의 대사 등에 관한 연구를 통하여 급성 독성 현상과 AchE의 저해도와의 관계가 먼저 정리되어야 할 것으로 본다.

• 대한의생명과학회지
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• 제11권4호
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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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• 제8권3호
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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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• 제3권1호
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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.

• 한국식품과학회지
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• 제39권6호
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• pp.669-675
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• 2007

본 연구자들은 Cumin(Cuminum cymium L.) seed로부터 정제한 $2-hydroxyethyl-{\beta}-undecenate$의 항치주염 활성을 사람의 백혈구를 이용하여 염증 매개물질 $LTB_4$ 및 PGs의 생성 효소인 5-lipoxygenase와 cyclooxygenase, 및 조직파괴 효소인 collagenase와 elastase의 저해 효과를 규명하여 다음과 같은 결론을 얻었다. HPS의 항치주염 활성을 사람의 백혈구를 이용하여 염증 매개물질 $LTB_4$ 및 PGs의 생성 효소인 5-lipoxygenase와 cyclooxygenase 및 조직파괴효소인 collagenase와 elastase의 저해효과를 규명한 결과, HPS은 $5\;{\times}\;10^{-2}\;M$ 첨가 시 97%의 PMNL로부터 $LTB_4$ 생합성이 저해되었으며 이때 $IC_{50}$ 값은 $2\;{\times}\;10^{-4}\;M$ 이었다. 균질화된 사람의 PMNL 5-lipoxygenase 및 시판 정제 5-lipoxygenase 활성에 대한 HPS의 저해 효과는 $5\;{\times}\;10^{-2}\;M$첨가 시 92%의 효소 활성이 저해되었다. 또한 효소 활성에 대한 $IC_{50}$ 값은 $2.5\;{\times}\;10^{-4}\;M$이었으며, 정제 5-lipoxygenase에 대한 $IC_{50}$ 값은 $2.3\;{\times}\;10^{-4}\;M$이었다. 또한 백혈구 COX 활성에 대한 $IC_{50}$ 값은 $5.1\;{\times}\;10^{-4}\;M$이었고, 정제 COX에 대한 $IC_{50}$ 값은 $2.3\;{\times}\;10^{-4}\;M$이었으며, 백혈구 collagenase 활성에 대한 $IC_{50}$ 값은 $2\;{\times}\;10^{-3}\;M$이었고 정제 collagenase에 대한 $IC_{50}$ 값은 $5\;{\times}\;10^{-2}\;M$이었다. 백혈구 elastase의 경우 $5\;{\times}\;10^{-2}\;M$ 첨가 시 66%의 활성이 저해된 반면 정제 elastase의 경우 $5\;{\times}\;10^{-2}\;M$ 첨가 시 25%의 효소 활성이 저해되었다. 또한 백혈구 elastase 활성에 대한 $IC_{50}$ 값은 $7.5\;{\times}\;10^{-3}\;M$이었다. 인체 치은세포에 대한 독성 시험 결과 $5\;{\times}\;10^{-2}\;M$의 HPS 첨가시 세포의 활성은 배양 2일째 47.83%로 나타났으며, $1\;{\times}\;10^{-2}\;M$의 HPS 첨가시에도 68.53%로 나타나 비교적 세포독성이 강한 것으로 나타났다.