• The Korean Journal of Pesticide Science
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• v.7 no.4
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• pp.239-247
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• 2003

This experiment was carried out to study the resistant mechanism of sulfonylurea(SU) herbicides to Monochoria korsakowii occurring in the rice fields of Korea. The activity of acetolactate synthase(ALS), absorption and translocation of $[^{14C}]$bensulfuron-methyl, and DNA sequence of ALS genes were studied. The apparent SU resiatance to Monochoria korsakowii was confirmed in greenhouse testes. Fresh weight accumulation$(GR_{50})$ in the resistant biotype was about 5- to 64-fold higher in the presence of six SU herbicides compared to the susceptible biotype. The ALS activity isolated from the resistant biotype to herbicides tested was less sensitive than that of susceptible biotype. The concentration of herbicide required for 50% inhibition of ALS activity$(I_{50})$ was 14- to 76-fold higher as compared to the susceptible biotype. No differences were observed in the rates of $[^{14C}]$bensulfuron uptake and translocation. However, the DNA sequence from the resistant biotype differed from that of the susceptible biotype by single nucleotide substitution at three amino acid each in the middle region excluding the ends of ALS genes. We found three point mutations causing substitution of serine for threonine at amino acid 168, arginine for histidine at amino acid 189, and a aspartic acid for phenylalanine at amino acid 247, respectively, in the resistant biotype.

• Korean Journal of Weed Science
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• v.18 no.4
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• pp.333-340
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• 1998

The combined effects of primisulfuron and imazethapyr treated with piperonyl butoxide(PBO) on growth inhibition and acetolactate synthase(ALS) activity in corn were studied to identify the tolerance mechanism among corn cultivars. Pioneer 3751 IR showed resistance to primisulfuron and imazethapyr, but Pioneer 3751 and Chalok 2 were susceptible to them. Pioneer 3751 IR was tolerant to primisulfuron regardless of PBO treatment, but Pioneer 3751, Suwon 118 and Chalok 2 were more greatly inhibited by combined treatment of primisulfuron with PBO. Synergistic effect on growth inhibition in Pioneer 3751 IR, Pioneer 3751, Suwon 118 and Chalok 2 was not occurred when imazethapyr was treated with PBO, but Pioneer 3751, Suwon 118 and Chalok 2 tended to inhibit by combined treatment of imazethapyr with PBO. Pioneer 3751 IR showed higher ALS activity than Pioneer 3751 when primisulfuron or imazethapyr was treated. ALS activity was inhibited by primisulfuron at $0.01{\mu}M$ or above and imazethapyr at $1{\mu}M$ or above, and inhibitory effect on ALS activity was observed by primisufuron and imazethapyr treatments with PBO.

• Applied Biological Chemistry
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• v.41 no.1
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• pp.99-103
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• 1998

Triazolopyrimidine sulfonanilide (TP) derivative is one of excellent herbicide compounds. We have synthesized three classes of a new sulfonamide derivative (TPP) as Acetolactate synthase (ALS) inhibitors, in which the benzene ring in TP skeleton was converted to substituted pyrimidyl ring and examined their inhibitory activities on barley for ALS. $I_{50}$ values of the inhibitors ranged from 0.005 to 2 mM. Comparing the $I_{50}$ value of each class of TPP derivatives, the substituents in pyrimidine and triazolopyrimidine ring were found to affect the degree of ALS inhibition. TPP with substituted methyl group in pyrimidine ring showed higher inhibitory activity than that with methoxy group, while the substitution of the cyclopentano group in triazolopyrimidine ring gave very large inhibitory activity than that of methyl group. The present study established that variation of the electron density by substitution at heterocyclic ring is a very important factor for ALS inhibition, but showed no dependence on steric effect by substituents.

• Korean Journal of Weed Science
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• v.18 no.2
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• pp.171-178
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• 1998

Growth response and acetolactate synthase(ALS) activity were examined to determine the resistance of corn cultivars to primisulfuron when primisulfuron and/ or insecticide Terbufos were applied. Pioneer 3571 IR showed resistance to primisulfuron regardless of Terbufos treatment, but Pioneer 3571 was greatly injured with primisulfuron plus Terbufos treatment. Suwon 118 was relatively tolerant to primisulfuron compared to Chalok 2, but crop injury was occurred at both cultivars by primisulfuron plus Terbufos treatment. ALS activity at Pioneer 3751 IR was very high in primisulfuron and/ or Terbufos treatment. Suwon 118 also showed higher ALS activity compared to Pioneer 3751 and Chalok 2, but ALS activities were greatly decreased by primisulfuron plus Terbufos treatment at Suwon 118 and Chalok 2. The $I_{50}$ concentration for 50% inhibition of the ALS enzyme was 10.0, 0.06, 7.75, and 0.04${\mu}M$ for Pioneer 3751 IR, Pioneer 3751, Suwon 118, and Chalok 2, respectively. Consequently, resistance of corn cultivars to primisulfuron was significantly related to ALS activity. Crop injury and lower ALS activity were recognized in susceptible corn cultivars by primisulfuron plus Terbufos treatment.

• BMB Reports
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• v.55 no.12
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• pp.621-626
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• 2022

Amyotrophic lateral sclerosis (ALS) is an incurable neurodegenerative disease characterized by the degeneration of motor neurons in the spinal cord. Main symptoms are manifested as weakness, muscle loss, and muscle atrophy. Some studies have reported that alterations in sphingolipid metabolism may be intimately related to neurodegenerative diseases, including ALS. Acid sphingomyelinase (ASM), a sphingolipid-metabolizing enzyme, is considered an important mediator of neurodegenerative diseases. Herein, we show that ASM activity increases in samples from patients with ALS and in a mouse model. Moreover, genetic inhibition of ASM improves motor function impairment and spinal neuronal loss in an ALS mouse model. Therefore, these results suggest the role of ASM as a potentially effective target and ASM inhibition may be a possible therapeutic approach for ALS.

• Korean Journal of Pharmacognosy
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• v.44 no.1
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• pp.75-82
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• 2013

Previous studies have shown that Aloe QDM complex, which is consisted of chromium (Cr), aloesin (ALS) and processed Aloe vera gel (PAG), exert antidiabetic activity in a high fat diet-induced mouse model of type 2 diabetes. In this study we examined the mechanism of the antidiabetic activity of the Aloe QDM complex. Rat myoblast cell line L6 cells were cultured in the presence of Cr, ALS, and PAG alone and in combinations, and then the capability of the cells to uptake glucose was examined using radiolabeled glucose. All of the 3 agents, Cr, ALS and PAG, exerted glucose uptake-enhancing activity in L6 cells. The most potent capability to uptake glucose was observed when L6 cells were cultured with the Aloe QDM complex. The activity of the Aloe QDM complex to enhance glucose uptake was prominent in conditions where existing insulin concentrations are low. We also examined the effects of the Aloe QDM complex on the plasma membrane expression of GLUT4 in L6 cells. The Aloe QDM complex increased the content of GLUT4 in the plasma membrane, while decreasing the content of GLUT4 in the light microsome. Taken together, these results show that the antidiabetic activity of the Aloe QDM complex is at least in part due to the stimulation of glucose uptake into the muscle cells, and this activity of the Aloe QDM complex is mediated through the enhancement of the translocation of GLUT4 into the plasma membrane.

• Korean Journal of Weed Science
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• v.18 no.3
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• pp.197-204
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• 1998

This study was conducted to determine the activity of ALS, content of endogenous free amino acids and fatty acids affected by herbicide mixture of cyhalofop-butyl, pyribenzoxim and pyrazosulfuron-ethyl. $I_{50}$ values (concentration required for 50% inhibition of ALS activity) of pyribenzoxim herbicide on the activity of ALS in Echinochloa crus-galli and Cyperus serotinus in vitro were recorded at 4${\times}$100 nM and 5${\times}$10 nM, respectively, while $I_{50}$ values of pyrazosulfuron against E crus-galli and C. serotinus were 4.5${\times}$10 nM and 4${\times}$10 nM, respectively, and the mixture of two herbicides showed additive effect on ALS activity at the low application rate, and independent effect at the high application rates of two herbicides. The inhibition rates of the three herbicides mixture treatment on the three branch-chain amino acids such as valine, leucine and isoleucine were 74.6%, 66.6% and 57.9% in C. serotinus and 36.6% 51.1% and 48.1% in E. crus-galli, respectively. A little bit higher inhibitory effect on the three branch-chain amino acids in C. serotinus and E. crus-galli seedlings was observed in two herbicide mixture of pyribenzoxim with pyrazosulfuron than three herbicide mixture of cyhalofop with pyribenzoxim and pyrazosulfuron. The interaction among three herbicides showed non-antagonism on the amounts of endogenous free amino acids.

• Applied Biological Chemistry
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• v.40 no.4
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• pp.277-282
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• 1997

Acetolactate synthase (ALS) was partially purified from Escherichia coli MF2000/pTATX containing Arabidopsis thaliana ALS gene. The partially purified ALS was examined for its sensitivity toward various modifying reagents such as iodoacetic acid, iodoacetamide, N-ethylmaleimide (NEM), 5,5'-dithiobis(2-nitrobenzoic acid) (DTNB), p-chloromercuribenzoic acid (PCMB), and phenylglyoxal. It was found that PCMB inhibited the enzyme activity most strongly followed by DTNB and NEM. Since iodoacetic acid did not compete with substrate pyruvate, it appeared that cysteine is not involved in the substrate binding site. On the other hand, the substrate protected the enzyme partly from inactivation by phenylglyoxal, which might indicate interaction of arginine residue with the substrate. The partially purified enzyme was inhibited by end products, valine and isoleucine, but not by leucine. However, the ALS modified with PCMB led to potentiate the feedback inhibition of all end products. Additionally, derivatives of pyrimidyl sulfur benzoate, a candidate for a new herbicide for ALS, were examined for their inhibitory effects.

• KOREAN JOURNAL OF CROP SCIENCE
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• v.47 no.4
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• pp.328-334
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• 2002

A Lindernia dubia (L.) Pennell var. dubia accession from Jeonnam province, Korea was tested for resistance to sulfonylurea (SU) herbicides, imazosulfuron and pyrazosulfuron-ethyl in whole-plant response bioassay. The accession was confirmed resistant to both herbicides. The $GR_{50}$ (herbicide concentration that reduced shoot dry weight by 50%) values of resistant accession were 264 and 19 times higher to imazosulfuron and pyrazosulfuronethyl, respectively, than that of the standard susceptible accession. The surviving resistant L. dubia after pyrazosulfuron-ethyl + molinate application can be controlled by sequential applications of soil-applied herbicides, butachlor, dithiopyr, pyrazolate, and thiobencarb and foliar herbicides, bentazon. Sulfonylurea-based mixtures such as mixtures of azimsulfuron + anilofos, bensulfuron-methyl + oxadiazon, pyrazosulfuron-ethyl + fentrazamide, and pyrazosulfuron-ethyl + anilofos + carfentrazon can also be used to control the surviving resistant L. dubia. However, use of these mixtures should be restricted to a special need basis. Thus, we suggest that sequential applications of non-SU-based mixtures such as butachlor + pyrazolate and MCPB + molinate + simetryne be used to control the surviving resistant L. dubia after SU herbicide applications. Rice yield was reduced 24 % by resistant L. dubia that survived after the pyrazosulfuron-ethyl + molinate application compared with pyrazolate + butachlor in transplanted rice culture. In vitro ALS activity of the resistant biotype was 40 and 30 times more resistant to imazosulfuron and pyrazosulfuron-ethyl, respectively, than the susceptible biotype. Result of in vitro ALS assay that the resistance mechanism of L. dubia to SU herbicides may be due, in part, to an alteration in the target enzyme, ALS.

• Korean Journal of Weed Science
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• v.16 no.1
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• pp.64-71
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• 1996

This study was conducted to determine the physiological responses of corn plants to chlorsulfuron, CHL, (2-chloro-N-(((4-methoxy-6-methyl-1,3,5- triazin-2-yl)amino)carboxyl) benzenesulfonamide) and/or imazaquin, IMA, (2-(4,5-dihydro-4-methyl-4-(1-methyl)-5-oxo-1H-imidazol-2y1)-3-quinoline carboxylic acid). CHL inhibited the plant growth within 6h after treatment, whereas IMA inhibited the growth more slowly(i.e., 36h). CHL inhibited the cell division of the root tips rapidly, however, little effect was found with IMA treatment. Neither CHL nor IMA had effect on the cell elongation of the shoots. CHL inhibited acetolactate synthase(ALS) activity of the roots within 1h after treatment. Interaction between CHL and IMA in growth inhibition was found to be additive or synergistic with simultaneous or sequential treatment of the two herbicides, respectively. In addition, interaction between CHL and IMA in ALS inhibition was found to be additive when the two herbicides were treated simultaneously.