• Journal of Microbiology and Biotechnology
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• 제20권6호
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• pp.988-994
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• 2010

The EtOAc fraction of Lespedeza cyrtobotrya showed mushroom tyrosinase inhibitory and radical scavenging activities. Four active compounds were isolated based on Sephadex LH-20 chromatography and HPLC, and the structures were elucidated, on the basis of their LC-MS and NMR spectral data, as 2-(2,4-dihydroxyphenyl)-6-hydroxybenzofuran (1), eriodictyol-7-O-glucopyranoside (2), haginin A (3), and dalbergioidin (4), respectively. Compound (1) showed mushroom tyrosinase inhibitory activity with an $IC_{50}$ value of $5.2\;{\mu}M$ and acted as a competitive inhibitor. Furthermore, $37.3\;{\mu}M$ of compound 1 reduced 50% of the melanin content on human melanoma (MNT-1) cells. The radical scavenging activities of compounds 1, 2, 3, and 4 were shown to have $IC_{50}$ values of 11.0, 24.5, 9.0, and $36.5\;{\mu}M$, respectively, in an ABTS system and $IC_{50}$ values of 42.7, 36.0, 37.7, and $61.7\;{\mu}M$, respectively, in a DPPH system. The mushroom tyrosinase inhibitory activity of the EtOAc fraction of Lespedeza cyrtobotrya was contributed by compounds 1, 3, and 4, and its radical scavenging activity was contributed by compounds 1-4.

• 한국식품과학회지
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• 제29권6호
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• pp.1269-1274
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• 1997

국내에서 재배된 Aloe vera에서 생리활성 물질인 acetylmannan을 분리 하고 그 제반의 특성을 규명하고 ACE저해효과 및 동력학적분석을 행한 결과 다음과 같은 결론을 얻었다. 알로에 베라 3.5 Kg으로 부터 에탄올에 불용성 다당체를 수득, 백색의 분말형태인 0.9 g의 acetylmannan을 얻었다. 분리한 acetylmannan은 탄수화물 67%를 함유하고 있으며 만노오즈는 60% 소량의 글루코오즈와 갈락토오즈로 이루어져 있고 아세틸기는 23%를 함유하고 있으며 acetyl group은 IR 스펙트럼에서 $1746\;cm^{-1}$, $1244\;cm^{-1}$ peak으로서 확인하였다. 과요오드 산화법에서 과요오드 음이온 소비량이 포름산 생성량에 비해 많고, 1, 4 글리코사이드 결합으로 이루어져 있음을 확인하였다. 또한 ACE에 대한 $IC_{-50}$ 값은 0.58 mM 이였으며, competitive 저해형식을 나타내었고. Ki 값은 0.068 mM 이였다.

• Bulletin of the Korean Chemical Society
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• 제32권12호
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• pp.4352-4360
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• 2011

A four dimensional quantitative structure activity relationship analysis was applied to a series of 50 flavonoid inhibitors of $p56^{lck}$ protein tyrosine kinase by the molecular comparative electron topological method. It was found that the -log (IC50) values of the compounds were highly dependent on the topology, size and electrostatic character of the substituents at seven positions of the flavonoid scaffold in this study. Depending on the negative or positive charge of the groups correctly embedded in these substituents, three-dimensional bio-structure to increase or decrease -log (IC50) values in the training set of 39 compounds was predicted. The test set of 11 compounds was used to evaluate the predictivity of the model. To generate 4D-QSAR model, the defined function groups and pharmacophore used as topological descriptors in the calculation of activity were of sufficient statistical quality ($R^2$ = 0.72 and $Q^2$ = 0.69). Ligand docking approach by using Dock 6.0. These compounds include many flavonoid analogs, They were docked onto human families of p56lck PTKs retrieved from the Protein Data Bank, 1lkl.pdb.

• ALGAE
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• 제21권3호
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• pp.343-348
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• 2006

This study was conducted to screen in vitro angiotensin - I converting enzyme (ACE) inhibitory activities of methanol (MeOH) and aqueous extracts at 20°C and 70°C, respectively, prepared from twenty-six red algae obtained from the coast of Jeju Island in Korea. Among aqueous extracts at 20°C (20AE) from red algae Lomentaria catenata showed the strongest ACE inhibitory activity and Lithophyllum okamurae recorded the second highest activity. From MeOH extract at 20°C (20ME) Ahnfeltiopsis flabelliformis possessed the strongest ACE inhibitory activity. Remarkable activities from MeOH extracts at 70°C (70ME) were observed in Grateloupia filicina, Sinkoraena lancifolia and Grateloupia lanceolata. However, no significant activity was found in aqueous extracts at 70°C (70AE). The IC50 values, which are concentrations required to inhibit 50% activity of ACE, for ACE inhibitory activities of 20AE from Lithophyllum okamurae and L. catenata were 13.78 and 12.21 μg mL–1, respectively. The IC50 values of 20ME from A. flabelliformis and Laurencia okamurae were 13.84 and 106.15 μg mL–1. Those of the 70ME from Bonnemaisonia hamifera, Grateloupia filicina, Sinkoraena lancifolia, G. lanceolata, Gracilaria vermiculophylla and L. okamurae ranged from 25.82 to 124.69 μg mL–1.

• 한국식생활문화학회지
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• 제25권6호
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• pp.832-838
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• 2010

In this study, the quality characteristics of jelly with black garlic (0, 10, 20, and 30%) were evaluated. The pH of jelly with black garlic decreased according to the amount of black garlic added. The sugar content of the jelly increased significantly with added black garlic. Lightness, redness, and yellowness decreased with increasing black garlic content. Moreover, the textural properties, which included hardness, springiness, cohesiveness, gumminess, and chewiness decreased in jelly that contained black garlic compared to the controls. Additionally, the antioxidant activity of jelly that contained black garlic increased in a concentration dependent manner. The $IC_{50}$ values of the DPPH radical scavenging activity for jelly that contained 10, 20 and 30% black garlic were 132.47, 50.97, 40.06, and 30.41 mg/mL, respectively. The $IC_{50}$ values of the hydroxyl radical scavenging activity of jelly decreased as the black garlic concentration increased. Finally, sensory results showed that the scores of over-all preference and buying intention for jelly with 20% black garlic were the highest.

• 한국자원식물학회지
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• 제28권3호
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• pp.312-320
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• 2015

Total phenol, flavonoid and antioxidant components of cabbage leaf samples derived from different cultivar were determined. Total phenol compound content showed the highest amount in methanol extracts from ‘YR Howol’ cultivar (11.72 ㎎/g), followed by ‘Harutame’ (10.66㎎/g), ‘Winstar’ (10.34 ㎎/g) and YR Hero (10.20 ㎎/g). The highest amount of total flavonoid content was observed from the methanol extracts of Harutame (5.39 ㎎/g), followed by Winstar (4.28 ㎎/g), Wialhowol (4.10 ㎎/g). The SOD enzyme activity showed a high activity of ‘YR Hogeo’ cultivar, and the cultivar of ‘YR Howol’ cultivar showed the lowest activity of SOD. The activity of CAT and APX showed higher values ‘Ogane’ and ‘YR Hogeol’ cultivars than the other cultivars. The POD activities showed relatively high values ‘Ogane’ and ‘YR Howol’ cultivars compared with other cultivars. The free radical (DPPH) scavenging activity showed lower IC₅₀ values of ‘Harutame’ (15.71) and ‘YR Howol’ cultivar (16.88), however methanol extract of ‘YR Hero’ cultivar (22.49) being the highest. The extracts of all cabbage cultivars in the reaction solution of pH 1.2 could be decomposed nitrite more than 50%. Especially, the cultivar ‘YR Hogeol’ and ‘Ogane’ showed a relatively high nitrite scavenging activity for each 60.13% and 57.20% respectively. The IC₅₀ values of antioxidant activity determined by ABTS were lower in ‘Harutame’ (17.04) and ‘YR Howol’ cultivar (17.97), and its results observed similar with values obtained from the same extracts by DPPH method. The result of this study suggests that the methanol extract of Brassica oleracea L. contains the high amount of phenolic and higher radical scavenging activities.

• 공업화학
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• 제31권6호
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• pp.612-623
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• 2020

본 연구는 Alcaligenes sp.와 Pseudomonas sp. 균주를 2종 혼합 배양 시, 혼합균주의 생장 및 인 제거에 5종의 중금속(Cd, Cu, Zn, Pb, Ni)이 미치는 저해효과를 정량적으로 평가하고자 수행되었다. 단일 중금속 처리 시 중금속별 Alcaligenes sp.와 Pseudomonas sp. 균주의 IC50는 Cd 0.75 mg/L, Cu 10.93 mg/L, Zn 7.08 mg/L, Pb 13.3 mg/L, Ni 15.78 mg/L 인 것으로 나타났다. 중금속 2종 처리 시 IC50는 Cd + Cu 처리구에서 가장 낮은 농도를 보였고, Ni + Pb 처리구에서 가장 높은 농도를 보였다. 단일 중금속 처리 시 중금속별 EC50 값은 Cd 0.54 mg/L, Cu 11.08 mg/L, Zn 6.14 mg/L, Pb 9.33 mg/L 및 Ni 13.81 mg/L이었다. 2종의 중금속 혼합 처리구별 EC50은 Cd + Zn 처리구에서 가장 낮은 농도, Zn + Ni 처리구에서 가장 높은 농도를 보였다. 2종 혼합 균주에 대한 2종 중금속 처리 결과 도출된 IC50 및 EC50 값을 기반 중금속 별 상호작용 평가 결과, 대부분 길항작용을 보이는 것으로 나타났으나, Cu + Ni 처리구에서는 상승작용을 보이는 것이 확인되었다. 따라서 본 연구 결과는 미생물을 이용한 오폐수 정화 처리 시 미생물의 성장 및 인 제거에 미치는 중금속의 독성으로 인한 저해효과에 대한 기초 자료를 제공할 수 있을 것으로 판단된다.

• 한국버섯학회지
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• 제12권4호
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• pp.304-310
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• 2014

본 실험에서는 꽃송이버섯 (Sparassis crispa, formerly S. crispa) 에탄올 추출물의 소수성 분획을 분리하고 각 분획의 DPPH 항산화 활성과 위암 (AGS), 폐암 (A529), 간암 (HepG2) 세포주를 이용한 항암 활성을 MTT assay를 통해 확인 하였다. SOCC를 사용하여 총 18개의 fraction으로 분획하였고 TLC와 세포주를 이용한 항암 활성 확인을 통하여 5개의 fraction으로 압축하였다. 항암활성이 높은 5개의 fraction은 HPLC-MS를 통해 각 분획물을 분석한 결과 항산화 활성을 보이지 않았으며 약 181.0의 분자량을 가진 물질이 지표물질로 확인되었으므로 이 물질의 화학식 동정을 위하여 추가실험이 필요하다. 세포주를 이용한 항암실험 결과 꽃송이버섯 추출물은 위암 (AGS), 폐암 (A529), 간암 (HepG2) 세포주 모두에서 양성대조군인 paclitaxel보다 낮은 세포 생존율을 보여 주었으며($IC_{50}$ value), 이것은 추후 꽃송이버섯 추출물에 포함된 항암 물질 분리 연구를 위한 기초연구 결과로서 무척 의미가 크다고 할 수 있다.

• Journal of Microbiology and Biotechnology
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• 제27권4호
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• pp.785-790
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• 2017

Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an $IC_{50}$ value of $1.21{\mu}M$; in addition, it was found to be highly effective against MAO-A, with an $IC_{50}$ value of $6.47{\mu}M$. Compound 1 was selective, but not extremely so, for MAO-B compared with MAO-A, with a selectivity index value of 5.35. Compound 1,8-dihydroxy-2-methyl-3-(4-methyl-1-oxopentyl)-9,10-phenanthrenedione (2) was moderately effective for the inhibition of MAO-B ($IC_{50}=14.50{\mu}M$) but not for MAO-A ($IC_{50}$ > $80{\mu}M$). There was no time-dependency in inhibition of MAO-A or -B by compound 1, and the MAO-A and -B activities were almost completely recovered in the dilution experiments with an excess amount of compound 1. Compound 1 showed competitive inhibition for MAO-A and -B, with $K_i$ values of 0.573 and $0.248{\mu}M$, respectively. These results suggest that piloquinones from a microbial source could be potent reversible MAO inhibitors and may be useful lead compounds for developing MAO enzyme inhibitors to treat related disorders, such as depression, Parkinson's disease, and Alzheimer's disease.

• 대한화학회지
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• 제64권2호
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• pp.79-83
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• 2020

A novel pharmacophore with epinastine (1) and NSAID moieties (2-5) was designed by molecular hybridization approach. The hybrid compounds 6-9 were synthesized by EDCI/HOBt or HATU-mediated coupling of 1 with salicylic acid (2), mefenamic acid (3), indomethacin (4) and naproxen (5), respectively, and were assessed for their inhibitory effect against NO production in LPS-induced RAW-264.7 macrophages in vitro. The Hybrids were found to exhibit significant NO production inhibitory effects with half-maximal inhibitory concentration (IC₅₀) values ranging in between 15.96 ± 1.32 and 36.68 ± 2.53 μM and were non-cytotoxic to macrophages. Comparing the inhibition concentration (IC₅₀), cytotoxicity concentration (CC₅₀) and in vitro efficacy index (iEI), 6 (IC₅₀ = 17.97 ± 1.92 μM; iEI = 11.13) and 9 (IC₅₀ = 15.96 ± 1.32 μM; iEI = 12.53) were better suited than other hybrids as well as their parent compound. Our findings signify that hybrids 6 and 9 may serve as platforms for continued investigations for the development of more efficient anti-inflammatory agents.