• 대한약리학회지
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• 제31권1호
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• pp.103-114
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• 1995

일부 malignant tumor에 Pt-complex의 일상 응용 과정에서 신장독성등의 심한 부작용이 문제점으로 지적되고 있다. 이 연구에서는 기존의 cisplatin보다 항암효과는 우수하면서, 부작용을 감소시킨 새로운 Pt-complex의 개발에 역점을 두었다. 본 연구에서 합성한 Pt(Ⅱ) complex는 carrier ligand로서 1,2-diaminocyclohexane(dach)을 사용하였고, leaving group으로는 diophosphine류인 1,2-bisdiphenylphosphinoethane(DPPE)을 도입하였으며, 물에 대한 용해도를 높이기 위해 dinitrate로 만들었다. 새로이 합성한 [Pt(Ⅱ)(trans-d-dach)(DPPE)]$(NO_3)_2$는 원소 분석, IR 및 $^{13}C-NMR$ 분석 data에 의하여 위의 물질임이 확인되었다. MTT assay method에 의한 항암활성 연구를 통하여 P-388, L-1210 lymphocytic leukemia cell과 SK-OV3 난소암세포에서 항암효과가 인정되었으며, 이 항암효과는 대조 약물로 사용된 cisplatin과 유사하였다. 토끼의 신세뇨관 세포와 인체의 신피질 세포를 이용한 cytotoxity 및 thymidine 섭취율과 인체 신피질 조직 배양을 이용한 glucose consumption 실험을 통하여 모두 cisplatin보다 신장독성이 현저히 감소되었다. 이상의 결과로 보아 Pt(Ⅱ)complexes는 carrier ligand와 leaving group의 선택에 따라 항암활성의 증가와 신독성의 감소를 일으키는 요인으로 보여지며, 이 연구에서 만들어진 Pt(Ⅱ)complex는 앞으로 다각적인 검토를 거쳐 새로운 항암화학요법제로 개발될 가능성이 있을 것으로 생각된다.

• Journal of Microbiology and Biotechnology
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• 제22권12호
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• pp.1665-1672
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• 2012

An 80% ethanol extract of Hizikia fusiforme was obtained and followed by successive fractionation using the organic solvents n-hexane, ethyl acetate, and n-butanol to identify the antioxidative substance. The aqueous part of the nbutanol fractionation step, showing high antioxidative activity, was subjected to reverse-phase liquid chromatography. As a result, a substance purified from a BB-2 fraction showed high antioxidative activity. The m/z 419 [M+H] molecular ion peak in the fraction was observed by the analysis of the ESI-LC/MS spectrum. By the analysis of 1H NMR (500 MHz, DMSO-$d_6$) and $^{13}C$ NMR (125 MHz, DMSO-$d_6$) spectra, a unique compound of the fraction was biochemically identified as a 5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone (5HHMF). We also investigated the effect of 5HHMF on human gastric AGS carcinoma cells. Western blot analysis suggested that the flavone substantially increased the levels of the death receptor-associated apoptosis mediators Fas, Fas L, FADD, TRADD, and DR4 in a concentration-dependent manner. The levels of Fas, Fas L, TRADD, and DR4 in the cells treated with 5HHMF ($5{\mu}g/ml$) were approximately 26.4-, 12.8-, 6.7-, and 9.8-times higher than those of non-treated cells, respectively. Of note, the level of FADD protein in the cells exposed to 5HHMF ($1{\mu}g/ml$) increased approximately 9.6-times. In addition, the cleavage of caspase-3, -8, and -9 in cultured AGS cells treated with 5HHMF was significantly confirmed. Therefore, our results suggest that 5HHMF from H. fusiforme is involved in the induction of death receptor-associated apoptosis mediators in human gastric AGS carcinoma cells.

• 한국작물학회:학술대회논문집
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• 한국작물학회 2022년도 추계학술대회
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• pp.312-312
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• 2022

Peanut hull as by-product has been discarded during peanut processing. However, peanut hull contains plenty of polyphenols that shows various physiological activities. The objectives of this study were to investigate anti-inflammatory and enzyme inhibitory activities of polyphenols from 'Sinpalkwang' peanut (Arachis hypogaea L.) hull. Compounds were isolated from methanol extracts of peanut hull by preparative-high performance liquid chromatography after identifying and quantifying polyphenols using Ultra performance liquid chromatography (UPLC) and UPLC-Quadrupole time-of-flight-mass spectrometry profiling. The structures of compounds were elucidated by one-dimensional [¹H, ¹³C] nuclear magnetic resonance (NMR) and two-dimensional NMR (correlated spectroscopy, heteronuclear single quantum coherence and heteronuclear multiple bond correlation). Three compounds were identified as 5,7-dihydroxy-4H-chromen-4-one (peak 2), luteolin (peak 4) and eriodictyol (peak 5). Significant differences in inflammatory mediator such as nitric oxide (NO), interleukin-6 (IL-6) and interleukin-1β (IL-lβ) in lipopolysaccharide stimulated Raw 264.7 macrophages and in enzyme (xanthine oxidase [XO] and α-glucosidase [AG]) inhibitory activities were observed between three compounds (p < 0.05). Peak 5 treated Raw 264.7 macrophages showed lower content of NO (16.4 uM), IL-6 (7.0 ng/mL), and IL-1β (60.6 pg/mL) than peak 2 (NO: 28.3 uM, IL-6: 11.3 ng/mL, IL-1β: 66.9 pg/mL) and peak 4 (NO: 24.7 uM, IL-6: 9.3 ng/mL, IL-1β: 62.6 pg/mL). Peak 5 showed higher XO inhibitory activity (84.7%) and higher AG inhibitory activity (52.4%) than peak 2 (XO inhibitory activity: 45.4%, AG inhibitory activity: 21.6%) and peak 4 (XO inhibitory activity: 37.9%, AG inhibitory activity: 37.5%) at concentration of 0.5mg/mL. This study suggests that peanut hull could be a potential source of anti-inflammatory and physiological materials while creating new use of discarded peanut hull as by-products concomitantly.

• 한국응용과학기술학회지
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• 제36권4호
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• pp.1259-1267
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• 2019

본 연구에서는 감국 꽃 추출물의 항산화 및 항염활성을 검색하고 유효성분을 분리하여 화학구조를 규명하였다. 감국 꽃 에탄올 추출물의 DPPH 및 ABTS⁺ 라디칼 소거 활성을 측정한 결과 우수한 라디칼 소거 활성이 있음을 확인하였다. 또한 LPS로 유도된 RAW264.7 대식세포에서 세포독성 없이 우수한 nitric oxide (NO) 저해 활성을 나타내었다. 감국 꽃 에탄올 추출물의 유효성분을 찾고자 medium pressure liquid chromatography (MPLC)를 실시하여 2개의 화합물을 분리하였으며 ¹H 및 ¹³C NMR 데이터 분석 및 문헌 비교를 통하여 화학구조를 동정하였다; Cynaroside (1), Apigetrin (2). 분리된 화합물을 HPLC를 통하여 정량분석을 수행하였으며 감국 꽃 추출물의 주요 성분으로 확인되었다. 화합물 1, 2의 항염활성을 확인한 결과 모두 농도의존적으로 우수한 NO 저해활성을 나타내었다. 이러한 연구 결과를 바탕으로 감국 꽃 추출물은 천연 항산화 및 항염 소재로써 활용 가능할 것으로 사료된다.

• 대한화학회지
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• 제59권3호
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• pp.215-224
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• 2015

Unsymmetrical tetradentate Schiff base N-(2-hydroxy-5-methylacetophenone)-N'-(2-hydroxy acetophenone) ethylene diamine (H₂L) and its complexes with Cr(III), Mn(II), Fe(III), Co(II), Ni(II) and Cu(II) have been synthesized and characterized by elemental analyses, magnetic susceptibility measurements, IR, electronic spectra and thermogravimetric analyses. ¹H, ¹³C-NMR and FAB Mass spectra of ligand clearly indicate the presence of OH and azomethine groups. Elemental analyses of the complexes indicate that the metal to ligand ratio is 1:1 in all complexes. Infrared spectra of complexes indicate a dibasic quadridentate nature of the ligand and its coordination to metal ions through phenolic oxygen and azomethine nitrogen atoms. The thermal behavior of these complexes showed the loss of lattice water in the first step followed by decomposition of the ligand in subsequent steps. The thermal data have also been analyzed for the kinetic parameters by using Horowitz-Metzger method. The dependence of the electrical conductivity on the temperature has been studied over the temperature range 313-403 K and the complexes are found to show semiconducting behavior. XRD and SEM images of some representative complexes have been recorded. The antimicrobial activity of the ligand and its complexes has been screened against various microorganisms and all of them were found to be active against the test organisms. The Fe(III) and Ni(II) complex have been tested for the catalytic oxidation of styrene.

• Journal of Microbiology and Biotechnology
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• 제23권2호
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• pp.161-166
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• 2013

At present, acetylcholinesterase (AChE) inhibitors are the first group of drugs to treat mild to moderate Alzheimer's disease (AD). Although beneficial in improving cognitive and behavioral symptoms, the effectiveness of AChE inhibitors has been questioned since they do not delay or prevent neurodegeneration in AD patients. Therefore, in the present study, in order to develop new and effective anti-AD agents from lichen products, both the AChE inhibitory and the neuroprotective effects were evaluated. The AChE inhibitory assay was performed based on Ellman's reaction, and the neuroprotective effect was evaluated by using the MTT method on injured PC12 cells. One AChE inhibitor ($IC_{50}$ = 27.1 ${\mu}g/ml$) was isolated by means of bioactivity-guided isolation from the extract of lichen-forming fungus Cladonia macilenta, which showed the most potent AChE inhibitory activity in previous screening experiment. It was then identified as biruloquinone by MS, and $^1H$- and $^{13}C$-NMR analyses. The inhibitory kinetic assay suggested that biruloquinone is a mixed-II inhibitor on AChE. Meanwhile, biruloquinone improved the viability of the $H_2O_2$- and ${\beta}$-amyloid-injured PC12 cells at 1 to 25 ${\mu}g/ml$. The protective effects are proposed to be related to the potent antioxidant activities of biruloquinone. These results imply that biruloquinone has the potential to be developed as a multifunctional anti- AD agent.

• Journal of Microbiology and Biotechnology
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• 제10권1호
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• pp.27-34
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• 2000

The chloroform and methanol (2;1, v/v) extract from an edible plant, Actinidia arguta Planchon, appeared to possess antitumor activity against human leukemias Jurkat T and U937 cells through inducing apoptosis. The substance in the solvent extract was purified by silica gel column chromatography, preparative TLC, and Sephadex LH-20 column chromatography. Characteristics of the substance analyzed by UV scanning analysis, $^1H$ and $^{13}C$ NMR spectra suggested that the substance belongs to the chlorophyll derivatives-like group. The $IC_{50}$ value of the chlorophyll derivative (Cp-D) determined by MTT assay was $15\mu\textrm{g}/ml$ for Jurkat, $10\mu\textrm{g}/ml$ for U937, and $11.4\mu\textrm{g}/ml$ for HL-60m and was more toxic to these leukemias than to solid tumors or normal fibroblast. In order to elucidate cellular mechanisms underlying the cytotoxicity, the effect of the Cp-D on Jurkat T cells was investigated. When cells were treated with the Cp-D at a concentration of $15\mu\textrm{g}/ml$, [3H]thymidine incorporation declined rapidly and wa undetectable in 1h. However, no significant changes were made in the cell cycle distribution of the cells by 24h. The sub-Gl peak representing apoptotic cells began to be detectable in 36h, at which time apoptotic DNA fragmentation was also detected on agarose gel electrophoresis, demonstrating that the cytotoxic effect of the Cp-D is attributable to the induced apoptosis. Under the same conditions, although the protein level of cyclin-dependent kinases such as cdc4, csk6, cdk2, and cdc2 was not significantly changed until 24h, the kinase activity of all c안 rapidly declined and reached a minimum level within 1-6h and then recovered to the initial level by 12h and sustained until 24h. These results suggest that inactivation of cdks at an inappropriate time during the cell cycle progression in jurkat T cells following a treatment with the Cp-D leads to induction of apoptotic cell death.

• 분석과학
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• 제13권2호
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• pp.173-178
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• 2000

두 개의 페놀기를 포함하는 열린 고리형태의 1, 14-Bis(2-hydroxybenzyl)-2, 6, 9, 12-tetraazatetradecane(bsated) 리간드를 염산염의 형태로 분리하여 원소 분석, 질량 스펙트럼 및 핵자기공명법으로 분석하였다. 합성된 리간드의 산 해리상수($logK^n{_H}$)와 $Cu^{2+}$, $Ni^{2+}$, $Co^{2+}$ 및 $Zn^{2+}$에 대한 안정도 상수($logK_{ML}$)를 전위차 적정법으로 결정하였다. 이때 온도는 $25^{\circ}C$ 및 이온강도는 0.10M($KNO_3$)로 고정시켰다. [Cu(bsated)] $(ClO_4)_2$ X-ray구조의 crystal data는 다음과 같다: Monoclinic space group $P2_1/n$, $a=17.856(4){\AA}$, $b=17.709(1){\AA}$, $c=8.539(2){\AA}$, $V=2700(2){\AA}$ with Z=4. tetrabutylammonium perchlorate 전해질의 dimethyl sulfoxide 용액속에서 [Cu(bsated)]$(ClO_4)_2$ 착물의 전기화학적 특성을 순환 전압-전류법 (CV)과 normal pulse voltammertry (NPV, 정상펄스전압전류법)으로 측정하였다.

• 한국작물학회지
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• 제56권3호
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• pp.244-249
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• 2011

본 연구는 콩 함유 사포닌의 함량을 쉽고 빠르게 정량할 수 있는 방법을 개발하기 위하여 시도하였다. 사포닌 표준 물질인 soyasaponin I은 대두에서 직접 분리하여 동정하였고, 분석은 HPLC/MS/MS를 이용하였으며 그 결과는 다음과 같다. 1. DAD 또는 ELSD를 이용하여 분석할 때보다 전처리 과정을 획기적으로 줄일 수 있어 신품종 육성의 선발과 같은 대량의 분석에 적합하였다. 2. Soyasaponin I의 함량은 나물콩과 같은 소립종에서 대립종에 비해 함량이 유의하게 높은 것으로 나타났다.

• 생약학회지
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• 제33권3호통권130호
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• pp.177-181
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• 2002

This study was carried out to investigate the antioxidative activities of Rosa davurica Pall for the purpose of development of novel antioxidant from natural products. Antioxidant activities of four different parts of Rosa davurica Pall such as fruit, leaf, stem and root were examined by measuring the radical scavenging effect on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. The methanol extract from the root of Rosa davurica Pall showed the highest antioxidative activity among 16 samples tested. And, we also tested radical scavenging effects of 5 different extract compartments(Hexane, $CHCl_3$, EtOAc, BuOH and $H_2O$ fraction). EtOAc and BuOH fractions from the root of Rosa davurica Pall exhibited antioxidative activities higher to those of natural, ${\alpha}-tocopherol$ or synthetic antioxidants, BHT. The antioxidative substance of EtOAc fraction from the root of Rosa davurica Pall was successively purified with silica gel adsorption column chromatography and Sephadex LH-20 column chromatography. The purified active substance was isolated as crystal and identified as (+)-catechin by $^{l}H-NMR$ and $^{13}C-NMR$. This compound exhibited DPPH radical scavenging activity with the $IC_50$ value of $1.7\;{\mu}g/ml$. In the analysis of catechin content, the leaf extracts contained the highest catechin, and fruit extracts contained the lowest catechin. Considering antioxidative activity on DPPH assay, the extracts of Rosa davurica Pall showed a possibility to be used as a new material for natural antioxidant and functional food.