• BMB Reports
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• v.43 no.4
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• pp.268-272
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• 2010

Aldo-keto reductase family 1 B10 (AKR1B10) is a member of the NADPH-dependent aldo-keto reductase (AKR) superfamily, and has been considered to be a potential cancer therapeutic target. Total extract from the bark of Rhus verniciflua (Toxicodendron vernicifluum (Stokes)) showed AKR1B10 inhibitory activity. To identify the active compounds from R. verniciflua responsible for AKR1B10 inhibition, nine compounds were isolated via bioactivity-guided isolation and tested for their effects against recombinant human AKR1B10 (rhAKR1B10). Results showed that butein, isolated from the ethyl acetate fraction, was most able to inhibit rhAKR1B10. The inhibitory rate of butein against rhAKR1B10 was 42.86% at $1\;{\mu}M$ with an IC50 value of $1.47\;{\mu}M$, and enzyme kinetic analysis revealed its inhibition mode to be uncompetitive.

• Korean Journal of Pharmacognosy
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• v.40 no.3
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• pp.238-243
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• 2009

We examined ethanol extracts prepared from 23 Korean local plants obtained in Pyeongchang, Gangwon-do for their inhibitory effects on recombinant human AKR 1 B10 (rhAKR1B10) in vitro. To do this, rhAKR1B10 was first expressed in E. coli as a biological active form and purified by using Ni-affinity chromatography followed by gel permeation chromatography. Then, rhAKR1B10 was used for screening out 23 Korean local plant extracts having an inhibitory activity against itself. Among them, six extracts showed more than 50% inhibition of rhAKR1B10 activity at the concentration of $10{\mu}g$/ml. Especially, the extracts of Ligularia fischeri var. spiciformis Nakai and Rhus trichocarpa Miq. were the most potent because their $IC_{50}$ values were 2.94 and $2.00{\mu}g$/ml, respectively.

• Journal of Applied Biological Chemistry
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• v.52 no.4
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• pp.216-220
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• 2009

Aldo-keto reductase family 1 B10 (AKR1B10) has been considered as a potential cancer therapeutic target. Ethanol extracts prepared from 82 Korean local plants were examined for their antioxidant activity and inhibitory effects on recombinant human AKR1B10 (rhAKR1B10) in vitro. 21 extracts showed more than 80% of ABTS radical scavenging activity at $100\;{\mu}g/mL$ and 11 extracts inhibited more than 50% of rhAKR1B10 activity at $10\;{\mu}g/mL$. Especially, 9 extracts showed potent inhibition on rhAKR1B10 activity compared with positive control tetramethylene glutaric acid.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.1
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• pp.111-116
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• 2013

Background: Cigarette smoking is the major risk factor for development of lung cancer. Identification of effects of tobacco on airway gene expression may provide insight into the causes. This research aimed to compare gene expression of large airway epithelium cells in normal smokers (n=13) and non-smokers (n=9) in order to find genes which discriminate the two groups and assess cigarette smoking effects on large airway epithelium cells.Materials and Methods: Genes discriminating smokers from non-smokers were identified by applying a neural network clustering method, growing self-organizing maps (GSOM), to microarray data according to class discrimination scores. An index was computed based on differentiation between each mean of gene expression in the two groups. This clustering approach provided the possibility of comparing thousands of genes simultaneously. Results: The applied approach compared the mean of 7,129 genes in smokers and non-smokers simultaneously and classified the genes of large airway epithelium cells which had differently expressed in smokers comparing with non-smokers. Seven genes were identified which had the highest different expression in smokers compared with the non-smokers group: NQO1, H19, ALDH3A1, AKR1C1, ABHD2, GPX2 and ADH7. Most (NQO1, ALDH3A1, AKR1C1, H19 and GPX2) are known to be clinically notable in lung cancer studies. Furthermore, statistical discriminate analysis showed that these genes could classify samples in smokers and non-smokers correctly with 100% accuracy. With the performed GSOM map, other nodes with high average discriminate scores included genes with alterations strongly related to the lung cancer such as AKR1C3, CYP1B1, UCHL1 and AKR1B10. Conclusions: This clustering by comparing expression of thousands of genes at the same time revealed alteration in normal smokers. Most of the identified genes were strongly relevant to lung cancer in the existing literature. The genes may be utilized to identify smokers with increased risk for lung cancer. A large sample study is now recommended to determine relations between the genes ABHD2 and ADH7 and smoking.

• BMB Reports
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• v.38 no.2
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• pp.151-160
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• 2005

By a cDNA array representing 2308 signal transduction related genes, we studied the expression profiles of HeLa cells stably transfected by Hepatitis C virus nonstructural protein 4B (HCV-NS4B). The alterations of the expression of four genes were confirmed by real-time quantitative RT-PCR; and the aldo-keto reductase family 1, member C1 (AKR1C1) enzyme activity was detected in HCV-NS4B transiently transfected HeLa cells and Huh-7, a human hepatoma cell line. Of the 2,308 genes we examined, 34 were up-regulated and 56 were down-regulated. These 90 genes involved oncogenes, tumor suppressors, cell receptors, complements, adhesions, transcription and translation, cytoskeletion and cellular stress. The expression profiling suggested that multiple regulatory pathways were affected by HCV-NS4B directly or indirectly. And since these genes are related to carcinogenesis, host defense system and cell homeostatic mechanism, we can conclude that HCV-NS4B could play some important roles in the pathogenesis mechanism of HCV.