• The Korean Journal of Pesticide Science
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• v.12 no.1
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• pp.1-8
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• 2008

The widespread and diverse sulfonylurea (SU) resistance problem has found in Korea, where one-shot-treatment herbicides such as pylazosulfuron/molinate and bensulfuron/molinate have been used continuously since 1989. The SU-resistant weeds of 7 annual weeds and 3 perennial weeds as of 2008 have confirmed in paddy fields in Korea. An effective management to SU-resistant weeds requires an integrated approach toward the weed control system, in particular, as to the drastic changes of herbicides development. Recent trend of new paddy herbicides in Japan has been developing to maximize the management of SU-resistant weeds. In the future, it is expected that the development of paddy herbicides in Korea is likely to be shifted toward the new "one-shot-treatment" included with herbicides of over 3-ways to maximize the control of resistant weeds. Bromobutide and carfentrazone are effective against sedges and broad-leaved weeds, respectively, and benzobicyclone and pyrimisulfam are effective against sedges and broad-leaved weeds.

• 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.

• Korean Journal of Weed Science
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• v.18 no.3
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• pp.268-279
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• 1998

• The Korean Journal of Pesticide Science
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• v.13 no.4
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• pp.290-297
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• 2009

This research aims to contribute the characterization of acetolactate synthase (Ec 4.1.3.18; ALS) and the resistance mechanism by sequence analysis of ALS gene of the sulfonylurea-resistant and -susceptible Monochoria vaginalis. The ALS gene was obtained from susceptible (S) and resistant (R) M. vaginalis to sulfonylurea herbicides (SUs). The 815 bp the fragment and the genomic DNA sequence coding for acetolactate synthase (ALS) of S and R biotypes of M. vaginalis were cloned and sequenced. Nineteen clones were divided greatly into 4 groups as result of sequencing. The first group was not difference to S type, the second group was amino acid of P197S which found point mutations causing substitution of serine for proline at amino acid 197, the third group was observed greatly other part of 6 places than group 1, and the fourth group appeared the intergrade of group 1 and 3. Therefore, it could be assumed what ALS gene of various types can be one plant. The peptide of the 13 amino acid Domain A region for ALS genes from R biotype of M. vaginalis differed from that of the S biotype by one base substitution at proline codon of Domain A. It could also be confirmed that point mutation of serine for proline at amino acid 197.

• Bulletin of the Korean Chemical Society
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• v.28 no.6
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• pp.947-952
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• 2007

Mycobacterium tuberculosis is a pathogen responsible for 2-3 million deaths every year worldwide. The emergence of drug-resistant and multidrug-resistant tuberculosis has increased the need to identify new antituberculosis targets. Acetohydroxy acid synthase, (AHAS, EC 2.2.1.6), an enzyme involved in branched-chain amino acid synthesis, has recently been identified as a potential anti-tuberculosis target. To assist in the search for new inhibitors and “receptor-based” design of effective inhibitors of tubercular AHAS (TbAHAS), we constructed four different structural models of TbAHAS and used one of the models as a target for virtual screening of potential inhibitors. The quality of each model was assessed stereochemically by PROCHECK and found to be reliable. Up to 89% of the amino acid residues in the structural models were located in the most favored regions of the Ramachandran plot, which indicates that the conformation of each residue in the models is good. In the models, residues at the herbicide-binding site were highly conserved across 39 AHAS sequences. The binding mode of TbAHAS with a sulfonylurea herbicide was characterized by 32 hydrophobic interactions, the majority of which were contributed by residue Trp516. The model based on the highest resolution X-ray structure of yeast AHAS was used as the target for virtual screening of a chemical database containing 8300 molecules with a heterocyclic ring. We developed a short list of molecules that were predicted to bind with high scores to TbAHAS in a conformation similar to that of sulfonylurea derivatives. Five sulfonylurea herbicides that were calculated to efficiently bind TbAHAS were experimentally verified and found to inhibit enzyme activity at micromolar concentrations. The data suggest that this time-saving and costeffective computational approach can be used to discover new TbAHAS inhibitors. The list of chemicals studied in this work is supplied to facilitate independent experimental verification of the computational approach.

• 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.

• The Korean Journal of Pesticide Science
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• v.8 no.4
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• pp.332-337
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• 2004

A suspected biotype of Scirpus planiculmis to be resistant to sulfonylurea(SU) herbicides was identified in Seosan reclaimed paddy fields in Korea, in 2004. The fields have been cultivated for monocultural rice production with wet-direct seeding method and continuously treated with SU-based herbicide mixtures for thirteen years since 1990. In greenhouse studies, 6 different SU herbicides, such as azimsulfuron, bensulfuron-methyl, cinosulfuron, ethoxysulfuron imazosulfuron and pyrazosulfuron-ethyl, completely controlled the Musan assession of Scirpus planiculmis at the recommended dose of each herbicide, however, the Seosan accession of S. planiculmis biotype was survived 20 to 45% even treated with 5 times higher dose of each recommended rate of all herbicides treated. The $GR_{50}$ values of 6 SU herbicides for Seosan accession of S. planiculmis were 47 to 100 times higher than those for Musan accession of S. planiculmis. The $I_{50}$ values pyrazosulfuron-ethyl to acetolactate synthase(ALS) extracted from Sesan and Muan accession of S. planiculmis were 409 nM and 0.8 nM, respectively. The $I_{50}$ value of Seosan was 511 times higher than that of Muan accession. These results suggested that the Seosan accession of S. planiculmis have strong resistant characteristics to 6 SU herbicides, respectively, indicating that resistance might be due to the alteration in the target site of ALS.

• Korean Journal of Weed Science
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• v.32 no.1
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• pp.57-69
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• 2012

This study was conducted to find the effective management of main weeds including herbicide-resistant Echinochloa oryzicola, Scirpus juncoides and Monochoria vaginalis in direct seeded rice on puddled paddy surface. The dominant dominances in direct seeded rice on puddled paddy surface were increased for three years between 2009-2011. In weed distribution in 2011, the occurrence density of S. juncoides decreased greatly, but it of E. oryzicola increased especially as compared with it of 2009. Benzobicyclon, mesotrione and pyrimisulfan were effective to sulfonylurea(SU)-resistant S. juncoides and M. vaginalis at 5 and 12 days after seeding, however, the efficacy of bromobutide to sulfonylurea-resistant M. vaginalis was decreased slightly at 12 days after seeding. And carfentrazon and pyrazolate were ineffective to S. juncoides. In direct seeded rice on puddled paddy surface which ACCase and ALS inhibitor-resistant E. oryzicola was not occurred, benzobicyclon+penoxsulam+pyrazosulfuron-ethyl ET, bromobutide+imazosulfuron+metamifop GR, and flucetosulfuron+mesotrione+pretilachlor GR showed the control effect over 94% to main weeds included sulfonylurea-resistant S. juncoides and M. vaginalis. The E. oryzicola dominating in direct seeded rice on puddled paddy surface were not any affected to the survival by treatment with recommended doses of cyhalofop-butyl and penoxsulam tested. The ACCase and ALS inhibitor-resistant E. oryzicola was effectively controlled by mefenacet and fentrazamide up to the 2nd leaf stage. In direct seeded rice on puddled paddy surface domiating coincidentally by herbicide-resistant E. oryzicola, S. juncoides and M. vaginalis, "one-shot herbicide" included with mefenacet, fentrazamide, penoxsulam and metamifop could't be used because of low control effect or rice injury. The sequential treatment of benzobicyclon+thiobencarb SE and bensulfuron+mefenacet+thiobencarb GR controlled effectively the herbicide-resistant E. oryzicola, S. juncoides and M. vaginalis in direct seeded rice on puddled paddy surface. The days required by the 3rd leaf stage of herbicide-resistant E. oryzicola, S. juncoides and M. vaginalis in direct seeded rice on puddled paddy surface seeded in May 20 shortened by 4 days as compared with it of June 10.

• Korean Journal of Weed Science
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• v.31 no.2
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• pp.119-133
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• 2011

Sulfonylurea (SU)-resistant weeds include seven annual weeds such as Monochoria vaginalis, Scirpus juncoides and Cyperus difformis, etc., and three perennial weeds of Scirpus planiculmis, Sagittaria pigmaea and Eleocharis acicularis as of 2010 since identification Monochoria korsakowii in the reclaimed rice field in 1998. The Echinochloa oryzoides resistant to acetyl CoA carboxylase (ACCase) and acetolactate synthase (ALS) inhibitors has been confirmed in wet-direct seeding rice field of the southern province, Korea in 2009. In the beginning of occurrence of SU-resistant weeds the M. vaginalis, S. juncoides and C. difformis were rapidly and individually spreaded in different fields, however, theses resistant weeds have been occurring simultaneously in the same filed as time goes by. The resistant biotype by weed species demonstrated about 10- to 1,000-fold resistance, base on $GR_{50}$ (50% growth reduction) values of the SU herbicides tested. And the resistant biotype of E. oryzoides to cyhalofop-butyl, pyriminobac-methyl, and penoxsulam was about 14, 8, and 11 times more resistant than the susceptible biotype base on $GR_{50}$ values. In history of paddy herbicides in Korea, the introduction of SU herbicides including besulfuron-metyl and pyrazosulfuron-ethyl that control many troublesome weeds at low use rates and provide excellent crop safety gave farmers and many workers for herbicide business refreshing jolt. The products and applied area of SU-included herbicides have been rapidly increased, and have accounted for about 69% and 96%, respectively, in Korea. The top ten herbicides by applied area were composed of all SU-included herbicides by 2003. The concentrated and successive treatment of ACCase and ALS inhibitors for control of barnyardgrass in direct-seeded rice led up to the resistance of E. oryzoides. Also, SU-herbicides like pyrazosulfuron-ethyl and imazosulfuron which are effective to barnyardgrass can be bound up with the resistance of E. oryzoides. The ALS activity isolated from the resistant biotype of M. korsakowii to SU-herbicides tested was less sensitive than that of susceptible biotype. The concentration of herbicide required for 50% inhibition of ALS activity ($I_{50}$) of the SU-resistant M. korsakowii was 14- to 76-fold higher as compared to the susceptible biotype. No differences were observed in the rates of [$^{14}C$]bensulfuron uptake and translocation. ALS genes from M. vaginalis resistant and susceptible biotypes against SU-herbicides revealed a single amino acid substitution of proline (CCT), at 197th position based on the M. korsakowii ALS sequence numbering, to serin (TCT) in conserved domain A of the gene. Carfentrazone-ethyl and pyrazolate were used mainly to control SU-resistant M. vaginalis by 2006, the early period, in Korea. However, the alternative herbicides such as benzobicyclone, to be possible to control simultaneously the several resistant weeds, have been developing and using broadly because the several resistant weeds have been occurring simultaneously in the same filed. The top ten herbicides by applied area in Korea have been occupied by products of 3-way mixture type including herbicides with alternative mode of action for the herbicide resistant weeds. Mefenacet, fentrazamide and cafenstrole had excellent controlling effects on the ACCase and ALS inhibitors resistant when they were applied within 2 leaf stage.

• Korean Journal of Agricultural Science
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• v.41 no.2
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• pp.85-99
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• 2014

Sulfonylurea (SU)-resistant weeds of eight annual weeds, Monochoria vaginalis, Scirpus juncoides and Cyperus difformis, etc., and four perennial weeds, Scirpus planiculmis, Sagittaria pigmaea, Eleocharis acicularis and Sagittaria trifolia as of 2013 since identification Monochoria korsakowii in the reclaimed rice field in 1998. And the resistant Echinochloa oryzoides to ACCase and ALS inhibitors has been confirmed in rice fields of the southern province, Korea in 2009. In the beginning, the M. vaginalis, S. juncoides and C. difformis of these SU-resistant weeds were rapidly and individually spreaded in different fields, however, these resistant weeds have been occurring simultaneously in the same filed recently. The resistant biotype by weed species demonstrated about 10-to 1,000-fold resistance, based on $GR_{50}$ values of the SU herbicides tested. And the resistant biotype of E. oryzoides to cyhalofop-butyl, pyriminobac-methyl, and penoxsulam was about 14, 8, and 11 times more resistant than the susceptible biotype base on $GR_{50}$ values. The products and applied area of SU-included herbicides have been increased rapidly, and have accounted for about 69% and 96% in Korea, respectively. In Korea, the main cause of SU-resistant weed is extensive use of these herbicides. The top ten herbicides by applied area were composed of all SU-included herbicides by 2003. The concentrated and successive treatment of ACCase and ALS inhibitors for control of barnyardgrass in rice led up to the resistance of E. oryzoides. Also, SU-herbicides like pyrazosulfuron-ethyl and imazosulfuron which effective to barnyardgrass can be bound up with the resistance of E. oryzoides. The ALS activity isolated from the resistant biotype of M. korsakowii to SU-herbicides tested was less sensitive than that of susceptible biotype. The concentration of herbicide required for 50% inhibition of ALS activity ($I_{50}$) of the SU-resistant M. korsakowii was 14-to 76-fold higher as compared to the susceptible biotype. No differences were observed in the rates of [$^{14}C$]bensulfuron uptake and translocation. Acetolactate synthase (ALS) genes from M. vaginalis resistant and susceptible biotypes against SU-herbicides revealed a single amino acid substitution of proline (CCT), at 197th position based on the M. korsakowii ALS sequence numbering, to serin (TCT) in conserved domain A of the gene. Carfentrazone-ethyl and pyrazolate were used mainly to control SU-resistant M. vaginalis by 2006 in Korea. However, the alternative herbicides such as benzobicyclone, to be possible to control simultaneously the several resistant weeds, have been developing and using broadly, because the several resistant weeds have been occurring simultaneously in the same fieled. The top ten herbicides by applied area in Korea have been occupied by products of 3-way mixture type including herbicides with alternative mode of action for the herbicide resistant weeds. Mefenacet, fentrazamide and cafenstrole had excellent controlling effects on the ACCase and ALS inhibitors resistant when they were applied within 2nd leaf stage.