• Journal of Applied Biological Chemistry
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• 제49권1호
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• pp.24-27
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• 2006

Four ursane-type triterpenoids, 2${\alpha}$,3${\alpha}$,19${\alpha}$-trihydroxy-24-norurs-4(23),12-dien-28-oic acid (1), 4(R),23-epoxy-2${\alpha}$,3${\alpha}$,19${\alpha}$-trihydroxy-24-norurs-12-en-28-oic acid (2), myrianthic acid (3), and tormentic acid (4), and a phenolic compound, ethyl gallate (5), from an EtOAc-soluble extract of the stems of Rumex japonicus, were subjected to in vitro bioassays to evaluate advanced glycation end products (AGEs) and rat lens aldose reductase (RLAR) inhibitory activity. Compounds 1 and 5 exhibited a significant inhibitory activity on AGEs formation with $IC_{50}$ value of 87 ${\mu}M$ and on RLAR with $IC_{50}$ value of 14.3 ${\mu}M$, respectively. Ethyl gallate (5) was isolated for the first time from this plant.

• Natural Product Sciences
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• 제13권2호
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• pp.160-163
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• 2007

Four glycosides, rosamultin (1), tetracentronside B (2), 4-O-methylellagic acid 3-O-${\alpha}$-$_L$-rhamnopyranoside (3), and vanillic acid 4-O-${\beta}$-$_L$-glucopyranoside (4), isolated from the roots extract of Potentilla discolor, were subjected to in vitro bioassays to evaluate the inhibitory activity on advanced glycation end products (AGEs) formation and rat lens aldose reductase (RLAR). Compound 3 exhibited a significant inhibitory activity against both AGEs formation and RLAR with IC$_{50}$ values of 79.5 and 8.03 ${\mu}$M, respectively. All the compounds (1-4) were isolated for the first time from this plant.

• Archives of Pharmacal Research
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• 제28권12호
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• pp.1365-1375
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• 2005

The antiestrogenic effects of marijuana smoke condensate (MSC) and three major cannabinoids, i.e., $\bigtriangleup^{9}$-tetrahydrocannabinol (THC), cannabidiol (CBD), and cannabinol (CBN), were evaluated using in vitro bioassays, viz., the human breast cancer cell proliferation assay, the recombinant human estrogen receptor (ER) competitive binding assay, and the reporter gene assay. The inhibitory effects on estrogen were also examined using the ethoxyresorufin-O­deethylase (EROD) assay, the aromatase assay, and the 17$\beta$-estradiol ($E_{2}$) metabolism assay. The results showed that MSC induced the antiestrogenic effect via the ER-mediated pathway, while THC, CBD, and CBN did not have any antiestrogenic activity. This suggests that the combined effects of the marijuana smoke components are responsible for the antiestrogenicity of marijuana use. In addition, MSC induced the CYP1A activity and the $E_{2}$ metabolism, but inhibited the aromatase activity, suggesting that the antiestrogenic activity of MSC is also related to the indirect ER-dependent pathway, as a result of the depletion of the in situ $E_{2}$ level available to bind to the ER. In conclusion, pyrogenic products including polycyclic aromatic hydrocarbons (PAHs) in the non-polar fraction, which is the most biologically active fraction among the seven fractions of MSC, might be responsible for the antiestrogenic effect.

• Journal of the Korean Wood Science and Technology
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• 제52권1호
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• pp.31-46
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• 2024

Subterranean termite attacks on cajuput (Melaleuca cajuputi) seedling roots were widespread in several of Java's Perum Perhutani Forest Management Units. This attack was suspected to be related to the chemical components of the cajunput seedling roots. This study was conducted to determine the bioactivity of cajuput seedling root extract as an attractant for the subterranean termite Coptotermes curvignathus Holmgren (Isoptera: Rhinotermitidae). The extraction process was performed according to ASTM D1108-96, and the extract was characterized using gas chromatography-mass spectrometry (GC-MS). Bioactivity testing of the extracts was carried out using attractiveness and no-choice feeding bioassays. The results showed that the average root extraction yield from cajunput seedlings was 4.94%. The attractiveness of the extract solutions at concentrations of 0.50%, 0.75%, and 1.00% were 45.33%, 62.00%, and 74.67%, respectively. The mortality rate of C. curvignathus termites ranged from 9.63% to 24.44%. Cajuput seedling root extract's lethal concentration 50 was 2.45% (non-toxic). GC-MS analysis showed that the extract contained linoleic acid, which has the potential to attract insects.

• Molecules and Cells
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• 제20권1호
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• pp.142-150
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• 2005

Members of the multifunctional Cyp family have been isolated from a wide range of organisms. However, few functional studies have been performed on the role of these proteins as chaperones in red alga. For studying the function of cDNA GjCyp-1 isolated from the red alga (Griffithsia japonica), we expressed and purified a recombinant GjCyp-1 containing a hexahistidine tag at the amino-terminus in Escherichia coli. An expressed fusion protein, $H_6GjCyp-1$ maintained the stability of E. coli proteins up to $50^{\circ}C$. For a functional bioassay for recombinant $H_6GjCyp-1$, the viability of E. coli cells overexpressing $H_6GjCyp-1$ was compared with that of cells not expressing $H_6GjCyp-1$ at $50^{\circ}C$. After high temperature treatment for 1 h, E. coli overexpressing $H_6GjCyp-1$ survived about three times longer than E. coli lacking $H_6GjCyp-1$. Measurement of the light scattering of luciferase (luc) showed that GjCyp-1 prevents the aggregation of luc during mild heat stress and that the thermoprotective activity of GjCyp-1 is blocked by cyclosporin A (CsA), an inhibitor of Cyps. Furthermore, the Cyp-CsA complex inhibited the growth of E. coli under normal conditions. The results of the GjCyp-1 bioassays as well as in vitro studies strongly suggest that Cyp confers thermotolerance to E. coli.

• 한국환경성돌연변이발암원학회지
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• 제23권2호
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• pp.45-50
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• 2003

Biological activities of PAHs are not known although PAHs are considered as carcinogens. Recent industrial society has human widely exposed to PAHs (polynuclear aromatic hydrocarbons) that are comming from the incomplete combustion of organic material as wider spread environmental contaminants. Our laboratory have been studied the effect of PAHs in the human breast cancer MCF-7 cells. In this study, we examined the human breast cancer MCF-7 cells as a new system to evaluate bioactivity of PAHs. We have selected 13 PAHs to examine bioassay using CYP1A1-luciferase reporter gene expression system where CYP1A1 1.6 Kb 5flanking region DNA was cloned in front of luciferase reporter gene and this plasmid was transfected into MCF-7 cells transiently. This cells then used for the study to observe the effect of PAHs. We demonstrated that PAHs induced the CYP1A1 promoter, CYP1A1 mRNA and 7-ethoxyresolufin O-deethylase (EROD) activities in a concentration-dependant manner. None of PAHs that we have tested showed stronger stimulatory effect on CYP1 gene expression than TCDD. Benz(a)anthracene and benzo(b)fluoranthene were weak responders to CYP1A1 promoter activity stimulation, CYP1A1 mRNA and EROD induction in MCF-7 cells and these chemicals seemed to respond less either CYP1A1 mRNA or EROD than CYP1A1 promoter activity. Benzo(k)fluoranthene, chrysene, and dibenzo(a, h)anthracene showed strong response to CYP1A1 promoter activity stimulation, CYP1A1 mRNA increase and also EROD induction in MCF-7 cells. Results of dose response study suggested that two strong responding PAHs, such as benzo(k)fluoranthene and dibenzo(a, h)anthracene might be mediated through Aryl hydrocarbon receptors system in MCF-7 cells.

• 한국식물병리학회:학술대회논문집
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• 한국식물병리학회 2003년도 정기총회 및 추계학술발표회
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• pp.95.2-96
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• 2003

In order to develop a new microbial fungicide for the control of vegetable diseases using endophytic bacteria, a total of 260 bacterial strains were isolated from fresh tissues of 5 plant species. After they were cultured in broth media, their antifungal activities were screened by in vivo bioassays against Botrytis cinerea(tomato gray mold), Pythium ultimum(cucumber damping-off), Phytopkhora infestans(tomato late blight), Colletotrichum orbiculare(cucumber anthracnose), and Blumeria graminis f. sp. hordei(barley powdery mildew). As the results of screening, 38 bacterial strains showed potent antifungal activities against at least one of 5 plant pathogens. A bacterial strain EB072 displayed potent disease control activities against 3 plant diseases. Among the bacterial strains with a potent antifungal activity against cucunlber anthracnose, three bacterial strains, EB054, EB151 and EB215, also displayed a potent in vitro antifungal activity against C. acutatum, a fungal agent causing pepper anthracnose. A bacterial strain EB215 obtained from roots of cucumber was identified as Burkholderia cepacia based on its physiological and biochemical characteristics and 165 rRNA gene sequence. An antifungal substance was isolated from the liquid cultures of B. cepacia EB215 strain by ethyl acetate partitioning, repeated silica gel column chromatography, and invitro bioassay, Its structural determination is in progress by various instrumental analyses.

• BMB Reports
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• 제40권2호
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• pp.163-171
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• 2007

Functional elements of the conserved helix 7 in the poreforming domain of the Bacillus thuringiensis Cry $\delta$- endotoxins have not yet been clearly identified. Here, we initially performed alanine substitutions of four highly conserved aromatic residues, $Trp^{243}$, $Phe^{246}$, $Tyr^{249}$ and $Phe^{264}$, in helix 7 of the Cry4Ba mosquito-larvicidal protein. All mutant toxins were overexpressed in Escherichia coli as 130-kDa protoxins at levels comparable to the wild-type. Bioassays against Stegomyia aegypti mosquito larvae revealed that only W243A, Y249A or F264A mutant toxins displayed a dramatic decrease in toxicity. Further mutagenic analysis showed that replacements with an aromatic residue particularly at $Tyr^{249}$ and $Phe^{264}$ still retained the high-level toxin activity. In addition, a nearly complete loss in larvicidal activity was found for Y249L/F264L or F264A/ Y249A double mutants, confirming the involvement in toxicity of both aromatic residues which face towards the same direction. Furthermore, the Y249L/F264L mutant was found to be structurally stable upon toxin solubilisation and trypsin digestion, albeit a small change in the circular dichroism spectrum. Altogether, the present study provides for the first time an insight into the highly conserved aromaticity of $Tyr^{249}$ and $Phe^{264}$ within helix 7 playing an important role in larvicidal activity of the Cry4Ba toxin.

• 한국유기농업학회지
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• 제24권4호
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• pp.881-891
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• 2016

포식성 천적 사막이리응애의 멀구슬, 후추 정향의 추출물과 이들의 혼합물에 대한 감수성을 검정하였다. 사막이리응애 암컷성충은 실험 식물추출물들의 처리 7일 후에 76-86%의 생존율을 나타냈으며, 무처리 암컷성충에 비해 62.6-93.4%의 산란 수를 보였고, 산란된 난들의 부화에 영향이 없었다. 실험 식물추출물들의 처리는 사막이리응애 난에 대해 전혀 영향이 없어 100% 부화하였다. 또한 이들 식물추출물의 처리는 약충의 생존율에 큰 영향이 없었다. 사막이리응애의 발육태들은 실험 식물추출물들이 처리된 잎 절편에서 생존율에 큰 영향을 받지 않아, 78-90%의 개체들이 성충태에 도달하였다. 이상의 결과로 보아, 실험 식물추출물들은 식식성응애류의 종합관리 체계에서 사막이리응애와 함께 활용할 수 있을 것으로 생각된다.

• 식물병연구
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• 제10권4호
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• pp.349-352
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• 2004

4품종(남도마늘, 고흥마늘, 단양마늘, 중국산 수입마늘)의 마늘추출액의 식물병원세균과 진균에 대한 항균효과를 조사하였다. 실내실험에서 마늘추출액은 그람양성세균, 그람음성세균, 진균 모두에 좋은 항균효과를 나타내었다. 본 연구에 사용된 4품종의 마늘추출액 중 남도마늘과 중국산 수입마늘이 보다 좋은 항균효과를 나타내었다. 그람양성세균인 Clavibacter michiganensis가 마늘추출액에 가장 민감하였으며, Burkholderia cepacia가 가장 저항성이 컸다. 마늘추출액을 이용한 오이 흰가루병에 대한 항균효과 포장실험에서는 59.7${\sim}$61.9%의 방제가를 보여주었다.