• Natural Product Sciences
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• 제24권1호
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• pp.59-65
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• 2018

An isoform of NADPH oxidase (NOX), NOX2 is a superoxide-generating enzyme involved in diverse pathophysiological events. Although its potential as a therapeutic target has been validated, there is no clinically available inhibitor. Herein, NOX2-inhibitory activity was screened with the constituents isolated from Schisandra chinensis, which has been reported to have antioxidant and reactive oxygen species (ROS)-scavenging effects. Among the partitions prepared from crude methanolic extract, a chloroform-soluble partition showed the highest NOX2-inhibitory activity in PLB-985 cell-based NOX2 assay. A total of twenty nine compounds (1 - 29) were identified from the chloroform fraction, including two first isolated compounds; dimethyl-malate (25) and 2-(2-hydroxyacetyl) furan (27) from this plants. Of these constituents, two compounds (gomisin T, and pregomisin) exhibited an NOX2-inhibitory effect with the $IC_{50}$ of $9.4{\pm}3.6$, and $62.9{\pm}11.3{\mu}M$, respectively. They are confirmed not to be nonspecific superoxide scavengers in a counter assay using a xanthine-xanthine oxidase system. These findings suggest the potential application of gomisin T (6) and other constituents of S. chinensis to inhibit NOX2.

• 생명과학회지
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• 제16권5호
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• pp.866-869
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• 2006

감자 polyphenol oxidase에 대한 솔잎 추출물의 저해효과가 조사 되었다. 솔잎 추출물은 anti-browning agents인 potassium sorbate나 citric acid보다도 더 강한 저해효과 를 나타냈으며 pH 7.0-8.0 사이에서 가장 강력한 저해효과가 있음을 알 수 있었다. 또한 반응시간이 증가 할수록 감자 polyphenol oxidase 활성은 현저하게 저해 되었으며 솔잎 추출물은 감자 polyphenol oxidase에 대해 비경쟁적인 저해를 하는 것으로 나타났다. 솔잎 추출물은 $100^{\circ}C$ 에서 10분간 열처리시에도 안정 하였으며 pH 2.0, 3.0, 4.0에서 3시간 처리시에도 여전히 감자 polyphenol oxidase 에 대한 저해효과를 보유하고 있어서 산과, 열에 비교적 안정한 물질임을 알 수 있었다.

• 한국수산과학회지
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• 제57권3호
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• pp.209-215
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• 2024

Ishige foliacea belongs to class Phaeophyceae and family Ishigeaceae. This study investigated the physiological activities of the Korean marine algae I. foliacea. Its solvent extracts were prepared with 70% ethanol, 80% methanol, and distilled water. The ethanol and methanol extracts had higher α-glucosidase (half-maximal inhibitory concentration, IC₅₀: 0.67-0.73 mg/mL), xanthine oxidase (IC₅₀: 0.25-0.28 mg/mL), and angiotensin-converting enzyme (IC₅₀: 25.29-38.28 ㎍/mL) inhibitory activities than those of the water extract. The ethanol and methanol extracts possessed high acetylcholinesterase inhibitory activity (IC₅₀: 0.78c0.97 mg/mL). Conversely, the water extract exhibited the highest β-secretase inhibitory activity (IC₅₀: 0.48 mg/mL). These results indicate that I. foliacea may be useful as a functional substance in food and pharmaceuticals with anti-diabetic, anti-gout, anti-hypertension, and anti-dementia properties.

• 한국축산식품학회지
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• 제26권4호
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• pp.511-516
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• 2006

발효 소시지의 제조에 starter로 사용한 균주를 선발하기 위해 각 유산균 균주들의 ACE 저해 활성, 콜레스테롤 흡착능력, 발효 육제품 저장 중 S. aureus에 대한 저해 황성을 평가하였다. ACE 저해 활성은 L. plantarum L167이 가장 우수하였고(58.75%), 콜레스테롤 흡착 능력이 우수한 균주로는 L. plantarum L155를 선발하였다. 박테리오신을 생산하는 P. damnosus를 starter로 이용하여 제조한 발효 소시지에 S. aureus를 접종하여 상온 저장 중 생균수를 측정한 결과 저장 35일째에 대조구에 비하여 1 log의 균수 감소 효과가 나타났다.

• 대한화장품학회지
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• 제37권2호
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• pp.161-169
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• 2011

본 연구에서는 발모 소재 개발을 위하여 한방복합처방단의 효소처리에 의한 발모 및 흑모 관련 생리활성을 알아보았다. 효소 처리된 한방 복합 처방단의 자유라디칼 소거활성과 superoxide dismutase 유사활성을 알아보았으며, lipoxygenase 활성 저해효과, $5{\alpha}$-reductase 활성 저해효과 및 멜라닌 생성 촉진효과를 확인하였다. 또한, 인체 피부 일차 자극시험 결과 자극이 없는 저자극으로 나타났다. 이로써, 효소 처리된 한방 복합 처방단은 피부자극 없이 모발제품의 기능성 원료로서 큰 가능성을 가지고 있는 것으로 판단된다.

• Archives of Pharmacal Research
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• 제27권2호
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• pp.199-205
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• 2004

Cytochrome P450 (P450) 1 enzymes such as P450 1A1, 1A2, and 181 are known to be involved in the oxidative metabolism of various procarcinogens and are regarded as important target enzymes for cancer chemoprevention. Previously, several hydroxystilbene compounds were reported to inhibit P450 1 enzymes and were rated as candidate chemopreventive agents. In this study, we investigated the inhibitory effect of 2-[2-(3,5-dimethoxyphenyl)vinyl]-thiophene (DMPVT), produced from the chemical modification of oxyresveratrol, on the activities of P450 1 enzymes. The inhibitory potential by DMPVT on the P450 1 enzyme activity was evaluated with the Escherichia coli membranes of the recombinant human cytochrome P450 1A1, 1A2, or 1B1 coexpressed with human NADPH-P450 reductase. DMPVT significantly inhibited ethoxyresorufin O-deethylation (EROD) activities with $IC_{50}$ values of 61, 11, and 2 nM for 1A1, 1A2, and 1B1, respectively. The EROO activity in OMBA-treated rat lung microsomes was also significantly inhibited by OMPVT in a dose-dependent manner. The modes of inhibition by DMPVT were non-competitive for all three P450 enzymes. The inhibition of P450 1B1-mediated EROD activity by OMPVT did not show the irreversible mechanism-based effect. The loss of EROD activity in P450 1B1 with OMPVT incubation was not blocked by treatment with the trapping agents such as glutathione, N-acetylcysteine, or dithiothreitol. Taken together, the results suggested DMPVT to be a strong noncompetitive inhibitor of human P450 1 enzymes that should be considered as a good candidate for a cancer chemopreventive agent in humans.

• Fisheries and Aquatic Sciences
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• 제3권3_4호
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• pp.195-199
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• 2000

Tyrosinase inhibitory activities of 14 kinds of seaweed, Ecklonia stolonifera, Ecklonia cava, Undaria pinnatiflda, Laminaria japonica, Sargassum fulvellum, Sargassum miyabei, Sargassum thunbergii, Porphyra yezoensis, Gracilaria verrucosa, Carpopeltis affinis, Pachymeniopsis elliptica, Gelidium amansii, Codium fragile and Ulva pertusa were determined using commercially available mushroom tyrosinase in an in vitro assay system. The $1\%$ (w/v) methanol extract from E. stolonifera showed the highest tyrosinase inhibitory activity of $79.0\%$, electron donating activity of $79.0\%$ and total phenol content of 3.75 mg/100g. Ethyl acetate-methanol-water (7 : 2 : 0.2, v/v) fraction $(0.5\%,\;w/v)$ isolated from the methanol extract showed tyrosinase inhibitory activity of $75.9 \%$, electron donating activity of $88.1 \%$ and total phenol content of 4.38 mg/100g. Tyrosinase inhibitory activity was closely associated with total phenol content (R = 0.99) and electron donating activity (R=0.99). Maximum absorption wavelength of the fraction was 218nm and that of phenolic compounds showed about a range from 210 to 220nm. The inhibition mode of the fraction was noncompetitive inhibition.

• Biomolecules & Therapeutics
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• 제1권1호
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• pp.93-97
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• 1993

We have previously reported that an NADPH-dependent succinic semialdehyde reductase was purified homogeneously from bovine brain by several chromatographic procedures, and was found to be a monomeric protein with a molecular mass of 28 kDa (Cho et al., Eur. J. Biochem. 1993). Since succinic semialdehyde is an important intermediate in the ${\gamma}$-aminobutyrate(GABA) shunt and GABA level is associated with various forms of human neurological disorders, we have investigated the effects of anticonvulsant drugs on the succinic semialdehrde reductase. Among the drugs tested, sodium valproate and diphenylhydantoin inhibited the enzyme activity, while some other drugs, barbiturate and chlorpromazine, had no inhibitory effects on the enzyme activity. The purified enzyme was also injected as an immunogen into Balb/c mice to obtain monoclonal antibodies (mob) and several mobs to the protein were produced from the fusion experiments.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.226.3-227
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• 2003

Lactic acid bacteria have been considered as the most beneficial probiotic organisms contributing to inhibition of harmful and putrefactive intestinal bacteria. Among them, Bifidobacterium spp. has been considered as one of the most beneficial probiotic organism that can improve the health of humans, since it is one of the major bacteria flora in human intestine. However, the harmful enzyme-inhibitory activity of lactic acid bacteria of Kimchi, which is a representative Korean fermented food has not been evaluated. (omitted)

• Journal of Microbiology and Biotechnology
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• 제12권1호
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• pp.59-64
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• 2002

An angiotensin I-converting enzyme (EC 3.4.15.1) (ACE), which can convert inactive angiotensin I into angiotensin II, a vasoconstrictor, is one of the key enzymes in controlling hypertension. It is suggested that the inhibition of ACE prevents hypertension, and many inhibitory peptides have already been reported. In the current study, oligonucleotides encoding ACE inhibitory peptides (IY, VKY) were chemically synthesized and designed to be multimerised due to isoschizomer sites (BamHI, BglII). The cloned gene named AP3 was multimerised up to 6 times in pBluescript and expressed in BL2l containing pGEX-KG. The fusion protein (GST-AP3) was easily purified with a high recovery by an affinity resin, yielding 38 mg of synthetic AP3 from a 1-1 culture. The digestion of AP3 by chymotrypsin exhibited an $IC_50$ value of $18.53{\mu}M$. In conclusion, the present experiment indicated that AP3 could be used as a dietary antihypertensive drug, since the potent ACE inhibitory activity of AP3 could be activated by chymotrypsin in human intestine.