• Title/Summary/Keyword: active compound

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Chemical Stabilization Study for Sulfonylurea Herbicides (Sulfonylurea계(系) 제초제(除草劑)의 화학적(化學的) 안정성(安定性))

  • Chen, Chia-Chung
    • Korean Journal of Weed Science
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    • v.17 no.2
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    • pp.135-138
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    • 1997
  • Sulfonylureas are highly active herbicides which can be applied at very low rate(10-50g/ha) to control broadleaf weeds. The nature of this category of compound is, however, very unstable toward hydrolysis. Therefore, the preparation of these compounds as liquid formulation was not possible. Most of the current formulations of sulfonylurea are in dry forms such as water dispersible granule or wettable powder. Even in these dry forms, the active ingredients also encounter significant chemical decomposition. This study involves the preparation of the sulfonylurea salts by reacting the parent compound with base such as sodium hydroxide. The salt becomes stable toward hydrolysis and it turns soluble when diluted with water. This discovery makes the preparation for liquid formulation or soluble granule of sulfonylurea possible. The stoichiometry of base added to the neutral sulfonylurea is controlled quite precisely. The base has to be added enough to quench the acidic impurities in the technical material and to convert the active ingredient into salt. However, the base should not be overused to cause further saponification of the sulfonylurea salts. The chemical nature of these compounds is presented and the chemical reaction is described. New soluble liquid formulation and solid granule formulation of sulfonylurea are suggested.

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Induction of Apoptosis by (-)-epigallocatechin-3-gallate in HL-60 Cells (인체 혈액암세포주(HL-60)에서 (-)-epigallocatechin-3-gallate에 의한 Aapoptosis 유도)

  • 이해미;김연정;박태선
    • Journal of Nutrition and Health
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    • v.36 no.4
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    • pp.382-388
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    • 2003
  • (-)-Epigallocatechin-3-gallate (EGCG) is a polyphenolic compound found in peen tea leaves, and has been known to be one of the most potent catechin species which inhibits cell growth most possibly through an apoptotic cell death. We investigated the apoptotic activity of (-)-EGCG on the human myeloid leukemia cell line, HL-60. Our results of MTT test indicated that (-)-EGCG had a significant antiproliferation effect in HL-60 cells with $IC_{50}$/ (50% inhibition concentration) value of 65 $\mu$M. Giemsa statining of HL-60 cells treated with (-)-EGCG (100 $\mu$M) for 6hrs showed a typical apoptosis-specific morphological change including shrinkage of the cytoplasm, membrane blobbing and compaction of the nuclear chromatin. The DNA fragmentation was observed from the agarose gel electrophoresis of cells treated with (-)-EGCG for 3hrs or longer, and was progressed to a greater degree as treatment time increases. Treatment of the cells with (-)-EGCG (100 $\mu$M) resulted in a rapid release of mitochondrial cytochrome c into the cytosol, and a subsequent cleavage of caspase-3 to an active form in a treatment-time dependent manner. (-)-EGCG (100 $\mu$M) also stimulated proteolytic cleavage of poly-(ADP-ribose) polymerase (PARP) to an active form in HL-60 cells. Tlken together, (-)-EGCG appears to induce the apoptosis in human myeloid leukemia cells via a caspase-dependent pathway. These results suggest the possible application of (-)-EGCG, the major active compound in green tea, as an antiproliferative agent for cancer prevention.

Constituents of Antioxidative Activity and Free Radical Scavenging Effect from Galla Rhois (Rhus javanica Linne) (오배자의 항산화 활성성분 및 자유라디칼 소거효과)

  • Lee, Sung-Bae;Rhim, Tae-Jin;Lee, Kwang-Hoe;Cha, Bae-Cheon
    • Korean Journal of Pharmacognosy
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    • v.31 no.2
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    • pp.185-189
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    • 2000
  • This study was carried out to investigate the structure of antioxidative constituents and the free radical scavenging effect of the main ingredients from Galla Rhois(Rhus javanica Linne). Antioxidative activities of n-hexane, EtOAc and BuOH extracts of Galla Rhois were similar or even higher than that of natural (tocopherol) or synthetic antioxidant (BHA). It is suggested that major fractions for the antioxidative activity of Galla Rhois were the n-hexane, EtOAc and BuOH extract compartments. In the subsequently experiment, one active compound from n-hexane extract, three active compounds from EtOAc extract and one active compound from BuOH extract were isolated. Their chemical structures were identified as syringic acid, protocatechuic acid, gallic acid methylester, gallic acid and $1,2,3,4,6- penta-O-galloyl-{\beta}-D-glucose$ on the basis of the speculation of spectral data and chemical reaction. Among the compounds, protocatechuic acid, gallic acid methylester and $1,2,3,4,6- penta-O-galloyl-{\beta}-D-glucose$ showed most potent radical scavenging effect using DPPH method.

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A study on the Active Material FeS2 in Battery Fabricated by Mechanical Alloying

  • Jung Woo-Hyun;Ahn In-Shup;Ahn Hyo-Jun;Bae Sung-Yeal;Sung Tek-Kyoung;Kim Tae-Bum;Kim You-Young
    • Journal of Powder Materials
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    • v.12 no.3
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    • pp.179-185
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    • 2005
  • As the electrodes of secondary battery are made with sulfur compounds, excellent electrode system of environmental non-toxicity, high specific energy density and low material cost can be obtained. In this study, the $FeS_2$ fine compound powders for active material in the battery were synthesized by mechanical alloying. Fine Fe-53.5 wt.%S powders of 450 nm of mean size were fabricated by mechanical alloying for 60 hours at the horizontal attritor. As the mechanical alloying time increases, particle size of Fe-53.5 wt.%S was decreased and steady state of Fe-53.5 wt.%S compound powders was obtained at 30 hours. Fe-53.5 wt.%S cathode shows the excellent discharge capacity (1011 mAh/g).

Isolation of Dibromosceptrin with Antimalarial Activity from the Unidentified Sponge, Agelas sp. (Agelas속의 미동정 해면으로부터 항말라리아 활성을 갖는 Dibromosceptrin의 분리)

  • Park, Yeung-Beom;Lee, Jong-Soo;Lim, Chi-Won
    • Korean Journal of Pharmacognosy
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    • v.35 no.3 s.138
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    • pp.189-193
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    • 2004
  • In order to find some lead compounds for the treatment of opportunistic infections of malaria and pathogenic microbes, an undescribed Indonesian sponge Agelas sp. collected at Manado, Indonesian Waters, was suggested containing active compounds. Crude ethanolic extract of the sponge exhibited significant in vitro antimalarial and antimicrobial activity against Plasmodium falciparum (D6 colne) with $IC_{5O}$ values of $8\;{\mu}/ml$ and against pathogenic microbes such as Candida albicans $(150\;{\mu}/ml)$, Cryptococcus neoformans $(<20\;{\mu}/ml)$, Staphylococcus aureus $25\;{\mu}/ml$, methicillin-resistant Staphylococcus aureus $(<20\;{\mu}/ml)$, and Pseudomonas aeruginosa $(<20\;{\mu}/ml)$. Active compound (5.0 mg) was isolated from the ethanolic extracts of the sponge and purified by using silica gel and ODS column, successively. Active compound was elucidated as dibromosceptrin $(C_{22}H_{24}Br_2N_{10}O_2)$ by detailed analysis of FTESI-MS and comparison of $^1H,\;^{13}C$, DEPT and HMQC NMR spectral data with those reported.

Effect of Saururus chinensis (Lour.) Baill. Aquacupuncture on Anaphlylaxis in Mice (삼백초약침액(三白草藥鍼液)이 아나필락시스에 미치는 영향)

  • Choi, Kyu-Jung;Lee, So-Young;Kang, Kyung-Hwa;Lee, Yong-Tae;Song, Choon-Ho
    • Korean Journal of Acupuncture
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    • v.21 no.3
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    • pp.97-104
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    • 2004
  • Objective We investigated the effect of Saururus chinensis (Lour.) Baill. aquacupuncture (SCB) on anaphylaxis in mice. Methods : We conformed compound 48/80-induced mesenteric mast cell degranulation, active systemic anaphylatic shock and histamine release. Also observed acetic acid-induced vascular permeability and anti-dinitrophenyl (DNP) IgE-mediated passive cutaneous anaphylaxis. Results : SCB inhibited mesenteric mast cell degranulation and active systemic anaphylatic shock induced by compound 48/80 dose-dependently. When SCB was pretreated by intra-peritoneal injection, the serum histamine levels were reduced. SCB also significantly inhibited acetic acid-induced vascular permeability. In addition, SCB showed a significant inhibitory effect on anti-dinitrophenyl (DNP) IgE-mediated passive cutaneous anaphylaxis. Conclusion : These results indicated that SCB inhibits anaphylatic reaction.

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Safflower Seed Oil and Its Active Compound Acacetin Inhibit UVB-Induced Skin Photoaging

  • Jeong, Eun Hee;Yang, Hee;Kim, Jong-Eun;Lee, Ki Won
    • Journal of Microbiology and Biotechnology
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    • v.30 no.10
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    • pp.1567-1573
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    • 2020
  • Ultraviolet (UV) is one of the major factors harmful to skin health. Irradiation with ultraviolet accelerates the decline of skin function, causing the skin to have deep wrinkles, dryness, decreased procollagen production, and degradation of collagen. Novel materials are needed to prevent the aging of the skin by blocking the effects of UV. Safflower seed oil (Charthamus tinctorius L., SSO) contains significantly high levels of unsaturated fatty acids and phytochemicals. SSO has been traditionally used in China, Japan, and Korea to improve skin and hair. Our objective in this study was to determine the effect of SSO and its active compound acacetin on UVB-induced skin photoaging in HaCaT cells and human dermal fibroblasts (HDF). SSO inhibited UVB-induced matrix metalloproteinase-1 (MMP-1) at both protein and mRNA levels in HaCaT cells and HDF. MMP-1 is known to play important roles in collagen degradation and wrinkle formation. Acacetin, a type of flavonoid, is present in SSO. Similar to SSO, acacetin also inhibited UVB-induced MMP-1 protein and mRNA levels in HaCaT cells and HDF. MMP-1 mRNA is primarily regulated by the mitogen-activated kinase (MAPK) signaling pathway. Acacetin regulated the phosphorylation of JNK1/2 and c-jun, but did not inhibit the phosphorylation of ERK1/2, p38 and AKT. Taken together, these results indicate that SSO and its active compound acacetin can prevent UVB-induced MMP-1 expression, which leads to skin photoaging, and may therefore have therapeutic potential as an anti-wrinkle agent to improve skin health.

Neuroprotective effects of Paeonia lactiflora and its active compound paeoniflorin against Aβ25-35-induced neurotoxicity in SH-SY5Y cells

  • Nam, Mi Na;Kim, Ji-Hyun;Lee, Ah Young;Cho, Eun Ju
    • Journal of Applied Biological Chemistry
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    • v.64 no.2
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    • pp.105-112
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    • 2021
  • Excessive accumulation of the amyloid beta (Aβ) peptide has been implicated in the pathogenesis of Alzheimer's disease (AD). Paeonia lactiflora (PL) has been used in treatments of several conditions such as inflammation, arthritis, and cognitive impairment. The purpose of this study was to investigate the neuroprotective effect and mechanisms of PL and its active compound, paeoniflorin (PF), on Aβ25-35-induced neurotoxicity in SH-SY5Y cells. We evaluated cell viability, lactate dehydrogenase (LDH) release and reactive oxygen species (ROS) production. Furthermore, underlying mechanism of PL and PF on the regulation of amyloidogenic pathway was analyzed by Western blotting. In our results, Aβ25-35-induced neuronal cell loss was observed, whereas treatment with PL (10, 50, and 100 ㎍/mL) and PF (1, 5, and 10 ㎍/mL) significantly elevated the cell viability, and decreased LDH release and ROS production. In addition, exposure of SH-SY5Y cells to Aβ25-35 significantly increased the protein levels of amyloid precursor protein (APP)-C-terminal fragment β, β-site APP-cleaving enzyme, and presenilin-1 and -2. However, treatment with PL and PF inhibited the amyloidogenic pathway via the down-regulation of those protein expressions. Taken together, our results indicate that PL, and its active compound PF, could protect SH-SY5Y cells against Aβ25-35-induced cell neurotoxicity by attenuating LDH release and ROS production, and these effects may be attributed to regulation of amyloidogenic pathway-related protein expression. In conclusion, PL and PF could be a potential to prevent neurodegenerative disorders such as AD.

Inhibitory Effects of Flavonoids Isolated from the Leaves of Stewartia koreana on Nitric-oxide Production in LPS-stimulated RAW 264.7 Cells (노각나무 잎에서 분리된 플라보노이드에 의한 대식세포에서 산화질소 생성 억제효과)

  • Lee, Seung-Su;Bang, Myun-Ho;Park, Se-Ho;Chung, Dae-kyun;Yang, Seun-Ah
    • Journal of Life Science
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    • v.28 no.5
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    • pp.509-516
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    • 2018
  • Five phenolic compounds were isolated from the ethyl acetate fraction of leaves from Stewartia koreana, and their nitric-oxide (NO) inhibitory activities were measured to identify the major active constituents responsible for the efficacy of the extract against inflammatory reactions. These five compounds were quercetin (1), quercitrin (2), hyperin (3), quercetin-3-O-(6"-O-galloyl)-${\beta}$-D-galactopyranoside (4), and kaempferol 3-O-[2",6"-di-O-(trans-p-coumaroyl)]-${\beta}$-D-glucopyranoside (5). Among the separated compounds in the EtOAc fraction, compounds 4 and 5 were isolated for the first time, and no study has yet reported their anti-inflammatory effects. The compounds were identified by spectroscopic analysis, and the isolated compounds showed significant NO inhibitory effects in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Compound 5 showed the most potent inhibitory effect (63.35% inhibition) against LPS-induced NO production compared to that of compound 1 (17.17%), compound 2 (5.0%), compound 3 (3.92%), and compound 4 (6.32%) at $10{\mu}g/ml$ concentration. NO production was inhibited by suppressing the protein expression of inducible nitric-oxide synthase in LPS-stimulated RAW 264.7 macrophages. These results indicate that kaempferol 3-O-[2",6"-di-O-(trans-p-coumaroyl)]-${\beta}$-D-glucopyranoside might be the major active compound responsible for the anti-inflammatory effects of S. koreana.

Aroma Characterization of Roasted Bulgogi Reaction Flavor Manufactured by a High-temperature Reaction Apparatus (고온반응기로 제조한 구운 불고기 반응향의 향미특성)

  • Seo, Won-Ho;Kim, Young-Kwon;Jang, Seong-Ho;Baek, Hyung Hee
    • Korean Journal of Food Science and Technology
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    • v.47 no.2
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    • pp.176-183
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    • 2015
  • To characterize the aroma properties of roasted bulgogi reaction flavor obtained by using a high-temperature reaction apparatus, the volatile flavor and aroma-active compounds were analyzed using simultaneous steam distillation and solvent extraction (SDE)-gas chromatography-mass spectrometry-olfactometry (GC-MS-O). One hundred five volatile compounds were detected in roasted bulgogi reaction flavor using GC-MS. Out of these compounds, furfural was the most abundant volatile compound, followed in order of abundance by 5-methyl furfural, phenylacetaldehyde, and nonanal. Of the volatile compounds identified in roasted bulgogi reaction flavor, 33 aroma-active compounds were detected using GC-O. 2,3-Butanedione and furfural were the most intense aroma-active compounds detected. Other relatively intense odorants included hexanal, octanal, nonanal, undecanal, phenylacetaldehyde, 5-methyl furfural, 2,6-dimethyl pyrazine, and dimethyl trisulfide. These were important aroma-active compounds that contributed to the aroma of roasted bulgogi reaction flavor because of their potency and aroma properties. The concentrations of the aroma-active compounds increased as the reaction temperature increased, whereas those of the sulfide compounds decreased.