• Food Science and Biotechnology
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• 제18권5호
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• pp.1173-1179
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• 2009

Trypsin inhibitors and lectins are defense proteins produced by many organisms. From Chinese 'Large Black Soybeans', a 60 kDa lectin and a 20 Da trypsin inhibitor (TI) were isolated using chromatography on Q-Sepharose, Mono Q, and Superdex 75. The TI inhibited trypsin and chymotrypsin with an $IC_{50}$ of 5.7 and $5{\mu}M$, respectively. Trypsin inhibitory activity of the TI was stable from pH 3 to 13 and from 0 to $65^{\circ}C$. Hemagglutinating activity of the lectin was stable from pH 2 to 13 and from 0 to $65^{\circ}C$. The TI was inhibited by dithiothreitol, signifying the importance of disulfide bond. The TI and the lectin inhibited HIV-1 reverse transcriptase ($IC_{50}$=44 and $26{\mu}M$), and proliferation of breast cancer cells ($IC_{50}$=42 and $13.5{\mu}M$) and hepatoma cells ($IC_{50}$=96 and $175{\mu}M$). The hemagglutinating activity of the lectin was inhibited most potently by L-arabinose. Neither the lectin nor the TI displayed antifungal activity.

• Food Science and Biotechnology
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• 제17권2호
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• pp.228-233
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• 2008

Considerable progress has been made in functionalization of the soy isoflavones through enzymatic modification of daidzin, genistin, and glycitin. After hydrolysis of $\beta$-glucosides into their corresponding aglycones, these compounds were structurally modified via biotransformations such as regioselective hydroxylation, enantioselective reduction, regioselective methylation, and polymerization. These reactions often resulted in an increase of the biological activities (e.g., anti oxidative activity, antiproliferative activity) and/or improvement of the physico-chemcial properties (e.g., water solubility, bioavailability). This review briefly summarizes on-going research activities on the biofunctionalization of the soy isoflavones.

• 생약학회지
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• 제31권1호
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• pp.77-81
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• 2000

The MeOH extract of Notopterygium incisum showed a strong cytotoxicity against B16 murine melanoma cell line. From this extract three furanocoumarins including bergamottin, isoimperatorin, notopterol and one polyacetylenic compound (falcarindiol) together with one phenylpropanoid (caffeic acid methyl ester) and one triterpenoid (pregnenolone) were isolated. The isolated compounds were evaluated for cytotoxic activity against four kinds of cancer cell lines, e.g. P388 (murine lymphocytic leukemia), B16 (murine melanoma), A549 (human lung carcinoma) and SK-OV-3 (human ovarian cancer). Among the isolates, falcarindiol and caffeic acid methyl ester expressed a significant antiproliferative activity against all tested cell lines.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2003년도 춘계학술대회 논문집
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• pp.68-69
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• 2003

Tributyltin (TBT) used world-wide in antifouling paints for ships is a widespread environmental pollutant and cause reproductive organs atrophy in rodents. At low doses, antiproliferative modes of action have been shown to be involved, whereas at higher doses apoptosis seems to be the mechanism of toxicity in reproductive organs by TBT. (omitted)

• 약학회지
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• 제45권2호
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• pp.161-168
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• 2001

The possible mechanism of the antiproliferative and apoptotic effects of Boswellia carterri water extract were studied in HL-60 human leukemia cells. The cytotoxicity of HL-60 cells after the treatment of Boswellia carterii water extract showed dose- and time-dependent manner. The apoptotic effect of 300 $\mu$g/ml Boswellia carterii water extract was demonstrated by DNA laddering. The activity of caspase 3-1ike protease was markedly increased in HL-60 cells treated with Boswellia carterii water extract. Furthermore, the level of Bcl-2 was time-dependently reduced, whereas Bax protein level was enhanced by Boswellia carterii water extract treatment. In conclusion, our results suggest that apoptotic effect of Boswellia carterii water extract may partly mediated through activations of caspase-3 activity and Bax expression, and inhibition of Bcl-2 expression.

• 한국식품영양과학회지
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• 제40권5호
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• pp.642-648
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• 2011

본 연구에서는 40여종의 육성계통 고추의 기능성 성분의 함량을 분석 및 활성 평가를 함으로써 우수 고추 품종 개발을 위한 database를 제공하고자 하였다. 연구 결과 capsaicinoid의 함량은 0.1에서 204.2 mg/100 g으로 나타났으며 ascorbic acid 함량은 279.1에서 1695.5 mg/100 g으로 넓은 분포 범위를 보였다. Polyphenol 함량은 2.6에서 10.2 mg/g 수준으로, flavonoid 함량은 1.4에서 5.7 mg/g 수준으로 나타났다. 항산화 활성 측정 결과는 육성계통 고추 breeding line No. 2500은 다른 계통에 비해 가장 높은 DPPH와 ABTS 라디칼 제거능을 나타내었으며 polyphenol과 flavonoid 함량 및 환원력이 다른 육성계통에 비해 높은 값을 나타내었다. 항암 효과는 breeding line No. 3201이 암세포 증식 저해율 84.5%로 가장 높은 효과를 나타내었으며 항염증 효과는 breeding line No. 3232가 75.2%로 가장 높은 nitric oxide 생성 억제율을 확인하였다. 본 연구에서는 육성계통에 따른 고추의 기능성 성분을 분석하고 다양한 생리활성을 평가하여 우수 품종 개량을 위한 성분 및 활성 database로 활용될 수 있을 것으로 생각된다.

• Natural Product Sciences
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• 제16권4호
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• pp.280-284
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• 2010

During liver fibrosis, hepatic stellate cells (HSCs) undergo a complex activation process characterized by increased proliferation and extracellular matrix deposition, which is the major pathological feature of hepatic cirrhosis. Therefore, suppression of HSCs activation has been proposed as therapeutic strategies for hepatic fibrosis. We tried to screen the antifibrotic activity of natural products employing HSC-T6, hepatic stellate cell lines as an in vitro assay system. In the present study, we investigated the antiproliferative activity of aerial parts and roots of Pulsatilla koreana Nakai (Ranunculaceae). Our present study shows that roots of P. koreana exerted more strong inhibitory activity compared to its aerial parts. In addition, among the fractions of the aqueous methanolic extract of P. koreana roots, both n-hexane and $CHCl_3$ fraction showed the strong inhibitory activity on HSC proliferation. Further study also demonstrated that the n-hexane and $CHCl_3$ fraction of P. koreana roots significantly inhibited the HSC proliferation in time- and concentration-related manners.

• 한국미생물·생명공학회지
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• 제30권4호
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• pp.420-424
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• 2002

고삼으로부터 항우식활성물질을 탐색하기 위하여 고삼의 에틸 아세테이트 추출물을 이용하여 치아우식의 주요한 원인 균인 Streptococcus mutans에 대한 항세균효과와 Glucosylransferase 활성억제효과를 파악하였다. S. mutans에 대한 항세균효과는 3차분획의 소분획에서 S. mutans에 대한 최소억제농도가 3.13 $\mu\textrm{g}$/ml으로 나타나 높은 항세균효과를 관찰할 수 있었다. 또한 고삼의 에틸 아세테이트추출물은 glucan의 형성을 저해하였으며 100$\mu\textrm{g}$/ml의 농도에서 77%의 저해율이 나타났고, 통계학적으로 유의성이 인정되었다(p<0.05). 항우식활성물질을 나타내는 성분을 찾기위하여 고삼의 에틸 아세테이트 추출물을 recycling prep-HPLC 방법과 TCL, LR, $^1$H-NMR, $^{13}$C-NMR의 분광화학적인 자료를 이용하여 (2S)-2'-methoxy kurarinone와(+)-kurarinone을 동정하였다.

• Biomolecules & Therapeutics
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• 제29권5호
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• pp.562-570
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• 2021

Topoisomerase IIα has been a representative anti-cancer target for decades thanks to its functional necessity in highly proliferative cancer cells. As type of topoisomerase IIα targeting drugs, topoisomerase II poisons are frequently in clinical usage. However, topoisomerase II poisons result in crucial consequences resulted from mechanistically induced DNA toxicity. For this reason, it is needed to develop catalytic inhibitors of topoisomerase IIα through the alternative mechanism of enzymatic regulation. As a catalytic inhibitor of topoisomerase IIα, AK-I-191 was previously reported for its enzyme inhibitory activity. In this study, we clarified the mechanism of AK-I-191 and conducted various types of spectroscopic and biological evaluations for deeper understanding of its mechanism of action. Conclusively, AK-I-191 represented potent topoisomerase IIα inhibitory activity through binding to minor groove of DNA double helix and showed synergistic effects with tamoxifen in antiproliferative activity.

• 대한한방내과학회지
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• 제28권3호
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• pp.473-491
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• 2007

Objectives : This study was designed to investigate the antiproliferative activity of the water extract of Samgibopae-tang (SGBPT) in NCI-H460 and A549 non-small-cell lung cancer cell lines Methods : In this study, we measured the subsistence, form of NCI-H460 and A549 non-small-cell lung cancer cell by hemocytometer and DAPI staining. In each cell, we analyzed DNA fragmentation. reverse transcription-polymerase chain reaction and measured activity of caspase-3, caspase-8 and caspase-9. Results and Conclusions : We found that exposure of A549 cells to SGBPT resulted in growth inhibition in a dose-dependent manner. butSGBPT did not affect the growth of NCI-H460 cells. The antiproliferative effect by SGBPT treatment in A549 cells was associated with morphological changes. SGBPT treatment partially induced the expression of DR5 cells and the expression of Faswas markedly increased in both transcriptional and translational levels in A549 cells. SGBPT treatment partially induced the expression of Bcl-2, Bcl-XL and the expression of Bid was markedly decreased in translational levels in A549 cells. However, SGBPT treatment did not affect the expression of IAP family in A549 orNCI-H460 cells. SGBPT treatment partially induced the expression of caspase-3, caspase-8, caspase-9 activity which markedly increased in a dose-dependent manners in A549 cells. The fragmental development of PARP and ${\beta}$-catenin protein was observed in A549 cells by SGBPT treatment. SGBPT treatment induced the expression of PLC-${\gamma}1$ protein which decreased in A549 cells. SGBPT treatment partially induced the expression of DFF45/ICAD which markedly increased in a dose-dependent manner in A549 cells. Taken together. these findings suggested that SGBPT-induced inhibition of human lung carcinoma did not affect NCI-H460 cell growth. However, SGBPT-induced inhibition of human lung carcinoma A549 cell growth was associated with the induction of death receptor and mitochondrial pathway. The results provided important new insights into the possible molecular mechanisms of the anti-cancer activity of SGBPT.