• Weed & Turfgrass Science
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• v.6 no.1
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• pp.28-31
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• 2017

The mutation rate of proline in the position 197 (Pro197) in acetohydroxy acid synthase (AHAS) is highest among sulfonylurea (SU) herbicide-resistance mutants. Therefore, it is significant to investigate the resistance mechanism for the mutation and to develop the herbicides specific to the mutants. SU herbicide resistance mechanism of the mutants, 197Ser, 197Thr and 197Ala, in AHAS were targeted for designing new SU-herbicide. We did molecular dynamics (MD) simulation for understanding SU herbicide-resistance mechanisms of AHAS mutants and designed new herbicides with docking and MD evaluations. We have found that mutation to 197Ala and 197Ser enlarged the entrance of the active site, while 197Thr contracted. Map of the root mean square derivation (RMSD) and radius gyrations (Rg) revealed the domain indicating the conformations for herbicide resistant. Based on the enlarging-contracting mechanism of active site entrance, we designed new herbicides with substitution at the heterocyclic moiety of a SU herbicide for the complementary binding to the changed active site entrances of mutants, and designed new herbicides. We confirmed that our screened new herbicides bonded to both AHAS wild type and mutants with higher affinity, showing more stable binding conformation than the existing herbicides.

• Korean Journal of Agricultural Science
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• v.41 no.1
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• pp.17-22
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• 2014

This study was conducted to evaluate the efficacy of formulations and application timings of imazosulfuron+fentrazamide in rice field. Weeding efficacy of imazosulfuron+fentrazamide SC (75+300 g a.i./ha) was more than 95% except Bidens tripartita. The efficacy of this formulation was not related to its formulations but was highly related to application timing. Herbicide application before 5 days after transplanting was best timing to get a maximum weed control. Systemic application before and after transplanting was much higher than single application for weed control. Second leaf stage of Echinochloa spp. and sulfonylurea resistant Monochoria vaginalis was controled over 90% in the imazosulfuron+fentrazamide SC (75+300 g a.i./ha). Based on these data, imazosulfuron+fentrazamide can be applied to provide effective weed control especially in the field infested with herbicide resistant M. vaginalis.

• Korean Journal of Weed Science
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• v.32 no.2
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• pp.133-138
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• 2012

This study was conducted to investigate the herbicidal activity against resistant biotype on sulfonylurea (SU) herbicides such as Scirpus juncoides and Monochoria vaginalis at the glasshouse and paddy rice cultivation area. In order to investigate resistance breakability against SU-resistanted annual weeds, new rice herbicides containing tefuryltrione [p-hydrophenyl pyruvate dioxygenase (HPPD) inhibitor] were tested. In both lab test and field experiment, tefuryltrione mixture, 4-HPPD inhibitor had shown excellent efficacy with a bleaching on the leaves of resistant annual weeds at early time after treatment and showed excellent persistance. Especially, tefuryltrione mixture had shown excellent controlling effect on annual and perennial SU-resistant S. juncoides in the regional field experiment. In phytotoxicity test, this tefuryltrione mixture had shown good selectivity to common rice species.

• Journal of The Korean Society of Inherited Metabolic disease
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• v.6 no.1
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• pp.52-57
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• 2006

Permanent neonatal diabetes(PND) is a rare form of diabetes characterized by insulin-requiring hyperglycemia that is diagnosed within the first 3 months of life. In most cases, the causes are not known. Recently, mutations in the gene KCNJ11 encoding the Kir6.2 subunit of the ATP-sensitive K+ charmel have been described in patients with PND. We report a child with PND due to a lysine-to-arginine substitution at position 170(K170R) of gene encoding Kir6.2 Our patient was diagnosed at 7 weeks of age and had been treated with subcutaneous insulin for 6.5 years. Recently, our patient has been changed from subcutaneous insulin to oral glibenclamide therapy at a daily dose of 7.5 mg 3 times a day(0.9 mg/kg/day) at the age of 6.5 years. Before glibenclamide therapy, c-peptide level was 0.1 ng/ml(normal 1.0-3.5 ng/ml) and hemoglobin HbA1c level was 7.8%(normal <6%). After 6 days of treatment, her c-peptide and insulin levels were 2.3 ng/ml and $9.6{\mu}U/ml$(normal $5-25{\mu}U/ml$), respectively. After 1 month later, the insulin and c-peptide levels were in the nonnal range without any episodes of hyper- or hypoglycemia. This case demonstrated that oral sulfonylurea may be the treatment of choice in PND patients with KCNJ11 mutation even at a young age.

• The Korean Journal of Physiology and Pharmacology
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• v.19 no.3
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• pp.197-202
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• 2015

Sulfonylureas are widely used as an antidiabetic drug. In the present study, the effects of sulfonylurea administered supraspinally on immobilization stress-induced blood glucose level were studied in ICR mice. Mice were once enforced into immobilization stress for 30 min and returned to the cage. The blood glucose level was measured 30, 60, and 120 min after immobilization stress initiation. We found that intracerebroventricular (i.c.v.) injection with $30{\mu}g$ of glyburide, glipizide, glimepiride or tolazamide attenuated the increased blood glucose level induced by immobilization stress. Immobilization stress causes an elevation of the blood corticosterone and insulin levels. Sulfonylureas pretreated i.c.v. caused a further elevation of the blood corticosterone level when mice were forced into the stress. In addition, sulfonylureas pretreated i.c.v. alone caused an elevation of the plasma insulin level. Furthermore, immobilization stress-induced insulin level was reduced by i.c.v. pretreated sulfonylureas. Our results suggest that lowering effect of sulfonylureas administered supraspinally against immobilization stress-induced increase of the blood glucose level appears to be primarily mediated via elevation of the plasma insulin level.

• The Korean Journal of Pesticide Science
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• v.17 no.4
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• pp.314-334
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• 2013

This study explored an efficient modified Quick, Easy, Cheap, Effective, Rugged and safe (QuEChERS) method combined with liquid chromatography-electrospray ionization with tandem mass spectrometric detection for the analysis of residues of 76 pesticides in brown rice, barley and corn including acidic sulfonylurea herbicides. Formic acid (1%) acid in acetonitrile and dispersive solid phase extractions used for extraction of pesticides and clean-up of the extract respectively. Two fortified spikes at 50 and 200 ng $g^{-1}$ levels were performed for recovery test. Mean recoveries of majority of pesticides at two spike levels ranged from 73.2 to 132.2, 80.9 to 136.8, 66.6 to 143.5 for brown rice, barley and corn respectively with standard error (CV) less than 10%. Good linearity of calibration curves were achieved with $R^2$ > 0.9907 within the observed concentration ranged. The modified method also provided satisfactory results for sulfonylurea herbicides. The method was applied to the determination of residues of target pesticides in real samples. A total of 26 pesticides in 36 out of 98 tasted samples were observed. The highest concentration was observed for tricyclazole at 1.17 mg $kg^{-1}$ in brown rice. This pesticide in two brown rice samples exceeded their MRLs regulated for rice in republic of Korea. Except tricyclazole none of the observed pesticides' concentration was higher than their MRLs. The results reveal that the method is effectively applicable to routine analysis of residues of target pesticides in brown rice, barley and corn.

• The Korean Journal of Pesticide Science
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• v.9 no.3
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• pp.250-261
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• 2005

This study was conducted to investigate the herbicidal response and effective control strategy of sulfonylurea(SU)-resistant Scirpus juncoides Roxb. occurred in the paddy fields of Korea. A biotype of Scirpus juncoides Roxb. resistant to SU was identified in the paddy fields treated with SU herbicide-based mixtures for seven consecutive years. The apparent SU resistance observed in Scirpus juncoides Roxb. was completely confirmed in greenhouse tests. The susceptible biotype was almost controlled at the recommended dose of all the tested, but the resistant biotype was survived 20 to 30% even at 10 times higher dose of each the recommended dose of SU herbicides. The $GR_{50}$ values of 4 SU herbicides for the resistant biotype were 53 to 88 times higher than those for the susceptible biotype. The acetolactate synthase(ALS) isolated from the resistant biotype against bensulfuron-methyl and pyrazosulfuron-ethyl was less sensitive than that of the susceptible biotype. The $I_{50}$ values of the resistant biotype against bensulfuron-methyl and pyrazosulfuron-ethyl were 498 and 126 times higher than those for the susceptible biotype. A rapid diagnosis for identifying resistance of Scirpus juncoides Roxb. was possible within at least 3 days after SU herbicides. Three herbicides having different mode of action from SU herbicide, carfentrazone-ethyl, pyrazolate and simetryne exhibited excellent controlling effects on the resistant biotype of Scirpus juncoides Roxb. till 3.5 leaf stage. Among the SU-based herbicides, pyriminobac-methyl+pyrazosulfuroil-ethyl+carfentrazone-ethyl GR and azimsulfuron+carfentrazone-ethyl+pyriminobac-methyl GR were very effective to control resistant biotype of Scirpus juncoides Roxb. without rice injury. The resistant biotype which were not controlled with SU herbicise-based herbicides survived from the fields were effectively controlled by bentazone SL.

• BMB Reports
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• v.30 no.1
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• pp.13-17
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• 1997

The inhibitory effect of herbicides such as sulfonylurea derivatives, imidazolinones and pyrimidylsalicylate has been examined on the purified valine sensitive acetolactate synthase (ALS) from Serratia marcescens. The concentration of sulfometuron methyl which inhibits 50% of the ALS activity was 2.5 mM. The required concentrations of triasulfuron, primisulfuron methyl and imazaquin for the 50% inhibition of the ALS activity were 1 mM. The resistance of Serratia ALS to sulfometuron methyl, imazapyr and imazaquin is similar to that of E. coli ALS 1. However, pyrimidylsalicylate showed a potent inhibitory effect on the Serratia ALS almost 13 times more potent than on E. coli ALS II, which is known as herbicide-sensitive isozyme. The inhibitory mode was competitive against pyruvate. 150 value was determined to be $17{\mu}M$ in an assay mixture containing 20 mM pyruvate, and the $K_1$, value was calculated to be $0.4{\mu}m$ from the modified double reciprocal plot of 1/V versus $1/S^2$.

• The Korean Journal of Physiology and Pharmacology
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• v.5 no.2
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• pp.157-163
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• 2001

The effects of dimethyl sulfoxide (DMSO) were studied in two groups of Xenopus oocytes, one expressing ATP sensitive $K^+\;(K_{ATP})$ channel comprised of sulfonylurea receptor SUR1 and inwardly rectifying $K^+$ channel subunit Kir6.2, and the other expressing renal $K_{ATP}$ channel ROMK2. At concentrations of $0.3{\sim}10%$ (vol/vol) DMSO inhibited whole cell Kir6.2/SUR1 currents elicited by bath application of sodium azide (3 mM) in a concentration-dependent manner. The inhibition constant and Hill coefficient were 2.93% and 1.62, respectively. ROMK2 currents, however, was not affected significantly by DMSO. The results support the idea that DMSO inhibits $K_{ATP}$ channel expressed in Xenopus oocyte through a protein-specific mechanism(s) that remains to be further elucidated.

• Proceedings of the Korean Society of Potoscience Conference
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• 2002.06a
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• pp.69-69
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• 2002