• Title/Summary/Keyword: active ingredient(A.I.)

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Development of an Alternative Analytical Method without Related Substance Reference Standards for Fenofibrate in Korean Pharmacopoeia (페노피브레이트 유연물질 표준품 대체시험법 개발)

  • Kim, Jung Hyun;Kim, Min Young;Kwon, Eun Kyung;Lee, Kwang Moon;Choi, Don Woong
    • YAKHAK HOEJI
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    • v.59 no.3
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    • pp.98-106
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    • 2015
  • Analytical method for related substances can be categorized into two methods depending on the necessity of reference standard (RS). The analytical method of related substances with RS is fast and accurate, but it's very expensive and technically difficult to synthesize RS due to their complicated structure. Another method is using relative retention time (RRT) and relative response factor (RRF) which are already validated with RS. Validation of this method is not easy and time consuming, but once it has been developed, it can save cost and time. In this study, we developed the analytical method for related substances of fenofibrate using RRT and RRF. We validated the method by evaluating specificity, linearity, accuracy and precision according to the "Manual for Guideline Application for Validation of Analytical Procedures" of MFDS. Also, we calculated RRT and RRF between fenofibrate and fenofibrate related substances. The results of this study showed high specificity for fenofibrate and fenofibrate related substances. Correlation coefficient(r) of all substances were more than 0.99, and the recovery of fenofibrate, fenofibrate related substance I, II and III were 99.44%, 100.84%, 99.14% and 101.58%, respectively. Precision of fenofibrate and its related substances were ranged between RSD 0.29% and 0.93%. Quantification limits of fenofibrate, fenofibrate related substance I, II and III were determined to be $0.03{\mu}g/ml$, $0.05{\mu}g/ml$, $0.04{\mu}g/ml$ and $0.02{\mu}g/ml$, respectively by confirming signal to noise ratio of each chromatogram. The RRT for fenofibrate related substance I, II and III were determined to be 0.35, 0.41 and 1.34, respectively. Also, the RRF for fenofibrate related substance I, II and III were determined to be 1.28, 0.98 and 0.79, respectively. The developed method was applied to determine contents for fenofibrate related substances in commercial fenofibrate (active pharmaceutical ingredient). As a result, developed analytical methods of related substances will be used for revising the monograph of fenofibrate in Korean Pharmacopoeia revision and contribute quality control of drugs by improving cost and time consuming problem of RS.

Studies on the Pasture Improvement with Herbicides III. Effect of different cutting intervals of shrubs after glyphosate application on establishment and teild of surface-sown pasture species (제초제에 의한 초지개량시험 III. Glyphsate 살포후의 관목제거간격이 겉뿌림 목초의 정착과 수량에 미치는 영향)

  • Kim, D.A.;Kwon, C.H.;Seo, S.;Lee, M.Y.
    • Journal of The Korean Society of Grassland and Forage Science
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    • v.6 no.1
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    • pp.1-5
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    • 1986
  • In series of pasture improvement studies with herbicides on nonarable hilly area, the effects of different cutting intervals (10, 20, 30 and 40 days) after glyphosate (2.9 kg/ha active ingredient) application on establishment and development of surface-sown orchardgrass(Dactylis glomerata L.) and ladino clover (Trifolium repens L.) was measured during 1983-1984. The cutting intervals of the existing shrubs after glyphosate application had no differential effect on establishment, seedling vigor, dry matter yield of surface-sown pasture species and botanical composition of improved pasture. Results showed that good control of the existing shrubs for surface-sown pasture species can be achieved by cutting the shrubs from 10 to 40 days after glyphosate application.

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Chemical Constituents of Brassica campestris ssp pekinensis (배추(Brassica campestris ssp pekinensis) 지상부의 화학성분)

  • Choi, Yeon-Hee;Kim, Jung-Sook;Seo, Jee-Hee;Lee, Jung-Won;Kim, Young-Sup;Ryu, Shi-Yong;Lee, Kang-Ro;Kim, Young-Kyoon;Kim, Sung-Hoon
    • Korean Journal of Pharmacognosy
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    • v.35 no.3 s.138
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    • pp.255-258
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    • 2004
  • Chinese cabbage (Brassica campestris ssp pekinensis) is one of the most popular green vegetables in Cruciferae family, which consisted in many Korean food. All kinds of Chinese cabbage are used both fresh and cooked with certain varieties being more suitable than others for some uses. A unique dish, Kimchi, has been developed in Korea and elsewhere by fermenting Chinese cabbage and pickling it in salt solution. Though lots of beneficial effect of Kimchi on human health has been published before, it is still debatable and in vague on the active origin of the Kimchi or of the Chinese cabbage responsible for the corresponding biological activities. We have recently conducted photochemical investigation of the Chinese cabbage, which is the main ingredient of the Korean traditional food, Kimchi. The MeOH extract of Chinese cabbage was partitioned with ethylacetate and BuOH, successively. The ethyl acetate soluble part was subjected to column chromatography with silica gel and RP-18, which gave finally five minor components, i.e., ${\beta}-sitosterol$ (1), indole-3-acetonitrile (2), 4-methoxyindole-3-acetonitrile (3), methyl ferulate (4), glycerol 1-(9,12,15-octadecatrienoate) (5). The structures of them were established on the basis of spectral $(^1H-NMR,\;^{13}C-NMR)$ evidences.

Effect of Tetramethylpyrazine on Pro-Inflammatory Cytokine Expressions in Mouse Brain Tissue following Intracerebroventricular Lipopolysaccharide Treatment (Tetramethylpyrazine이 LPS의 뇌실주입에 따른 생쥐 뇌조직의 Pro-Inflammatory Cytokines 발현에 미치는 영향)

  • Choi, Yong-Seok;Won, Jong-Woo;Yoo, Inwoo;Shin, Jung-Won;Kim, Seong-Joon;Sohn, Nak-Won
    • The Korea Journal of Herbology
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    • v.28 no.1
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    • pp.83-90
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    • 2013
  • Objectives : Tetramethylpyrazine (TMP) is an active ingredient in Ligusticum wallichii and has a wide range of neuroprotection effects. This study investigated anti-neuroinflammatory effect of TMP on brain regions in intracerebroventricular (i.c.v.) lipopolysaccharide (LPS)-treated C57BL/6 mice. Methods : TMP was administered intraperitoneally at doses of 10, 20, and 30 mg/kg at 1 h prior to LPS (3 mg/kg) i.c.v. injection. mRNA level of pro-inflammatory cytokines, including tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin (IL)-$1{\beta}$ and IL-6, was measured in the cerebral cortex, hippocampus, and hypothalamus tissue using real-time polymerase chain reaction at 24 h after the LPS injection. Cyclooxygenase-2 (COX-2) positive cells in the hypothalamus was also observed using immunohistochemistry at 24 h after the LPS injection. Results : At a dose of 30 mg/kg TMP significantly attenuated up-regulation of TNF-${\alpha}$ and IL-$1{\beta}$ mRNA in the cerebral cortex and IL-$1{\beta}$ mRNA in the hippocampus. In the hypothalamus, doses of 20 mg/kg and 30 mg/kg TMP significantly attenuated up-regulation of TNF-${\alpha}$, IL-$1{\beta}$, and IL-6 mRNA induced by the LPS injection. In addition, TMP (30 mg/kg) significantly reduced the number of COX-2 positive cells in the hypothalamus. Conclusion : These results indicate that TMP has an anti-inflammatory effect on neuroinflammation, especially in the hypothalamus, induced by LPS i.c.v. injection and suggest that TMP-containing Ligusticum wallichii may play a modulatory role on the systemic responses following hypothalamic inflammation.

A novel protocol for batch-separating gintonin-enriched, polysaccharide-enriched, and crude ginsenoside-containing fractions from Panax ginseng

  • Rami Lee;Han-Sung Cho;Ji-Hun Kim;Hee-Jung Cho;Sun-Hye Choi;Sung-Hee Hwang;Hyewon Rhim;Ik-Hyun Cho;Man-Hee Rhee;Do-Geun Kim;Hyoung-Chun Kim;Seung-Yeol Nah
    • Journal of Ginseng Research
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    • v.47 no.3
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    • pp.366-375
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    • 2023
  • Background: Ginseng contains three active components: ginsenosides, gintonin, and polysaccharides. After the separation of 1 of the 3 ingredient fractions, other fractions are usually discarded as waste. In this study, we developed a simple and effective method, called the ginpolin protocol, to separate gintonin-enriched fraction (GEF), ginseng polysaccharide fraction (GPF), and crude ginseng saponin fraction (cGSF). Methods: Dried ginseng (1 kg) was extracted using 70% ethanol (EtOH). The extract was water fractionated to obtain a water-insoluble precipitate (GEF). The upper layer after GEF separation was precipitated with 80% EtOH for GPF preparation, and the remaining upper layer was vacuum dried to obtain cGSF. Results: The yields of GEF, GPF, and cGSF were 14.8, 54.2, and 185.3 g, respectively, from 333 g EtOH extract. We quantified the active ingredients of 3 fractions: L-arginine, galacturonic acid, ginsenosides, glucuronic acid, lysophosphatidic acid (LPA), phosphatidic acid (PA), and polyphenols. The order of the LPA, PA, and polyphenol content was GEF > cGSF > GPF. The order of L-arginine and galacturonic acid was GPF >> GEF = cGSF. Interestingly, GEF contained a high amount of ginsenoside Rb1, whereas cGSF contained more ginsenoside Rg1. GEF and cGSF, but not GPF, induced intracellular [Ca2+]i transient with antiplatelet activity. The order of antioxidant activity was GPF > GEF = cGSF. Immunological activities (related to nitric oxide production, phagocytosis, and IL-6 and TNF-α release) were, in order, GPF > GEF = cGSF. The neuroprotective ability (against reactive oxygen species) order was GEF > cGSP > GPF. Conclusion: We developed a novel ginpolin protocol to isolate 3 fractions in batches and determined that each fraction has distinct biological effects.

Antioxidant and Antiaging Effect of Ginseng Berry Extract Fermented by Lactic Acid Bacteria (유산균 발효에 의한 인삼열매 추출물의 항산화 및 항노화 효과)

  • Jeon, Ji-Min;Choi, Sung-Kyu;Kim, Yun-Jeong;Jang, Su-Jin;Cheon, Jong-Woo;Lee, Hyun-Sang
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.37 no.1
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    • pp.75-81
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    • 2011
  • The effect of lactic acid bacteria.fermented ginseng berry extract (FGBE) on physiological activities was evaluated. The contents of ginsenosides Re, Rc, and Rb1 in ginseng berry extract (GBE) were increased after fermentation by lactic acid bacteria when analyzed by high performance liquid chromatography. Antioxidant activity of GBE and FGBE was also analyzed by DPPH radical scavenging activity assay and SOD.like activity assay. FGBE showed a 86.34 % inhibition of DPPH radical and a 76.82 % inhibition by SOD.like activity at a concentration of 1.00 %. GBE showed a 49.78 % inhibition of DPPH radical and a 40.80 % inhibition by SOD.like activity at the same concentration. Furthermore, procollagen type I (COL1A1) gene expression increased by 823.13 % and matrix metal-loproteinase(MMP)-1 and tumor necrosis factor (TNF)-${\alpha}$ gene expression decreased by 87.88 % and 99.92 %, respectively, in human fibroblast cultured with FGBE at a concentration of 0.50 %. These results suggest that FGBE could be used as an active ingredient for functional cosmetics.

Assessment of the Residues of Benfuresate and Oxolinic Acid in Crops (Benfuresate와 Oxolinic Acid의 작물체중 잔류량 평가)

  • Park, Dong-Sik;Yang, Jae-E.;Han, Dae-Sung
    • Korean Journal of Environmental Agriculture
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    • v.14 no.3
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    • pp.312-318
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    • 1995
  • Residues of benfuresate in rice and oxolinic acid in Chinese cabbage were determined through the field experiments in order to establish the safe use and the maximum residue limit(MRL) of these pesticides in Korea. The herbicide benfuresate powder was sprayed into the paddy field with a level of 0.6kg(active ingredient)/ha and rice (Oryza sativa L.) was grown. At harvest, residues of benfuresate in brown rice and stem were analyzed using gas chromatograph. The residue of oxolinic acid in Chinese cabbage (Brassica campestris subsp. napus var pekinesis MAKINO) was analyzed using HPLC after foliar-spraying this fungicide into the cabbages at a level of 15kg/ha. The recovery efficiencies of benfuresate and oxolinic acid were 87-89% and 90-95%, respectively. The respective residues of benfuresate in rice and oxolinic acid in Chinese cabbage were in the range of 0.27-0.46 mg/kg and 0.23-1.53kg/kg. Residual concentrations of these pesticides in crops increased with the increased application frequencies, followed the first-order kinetics and linearly decreased with time. The highest residue of 1.53 mg/kg of oxolinic acid was observed when this fungicide was sprayed six times until three days prior to harvest, but this level was far lower t㏊n 5 mg/kg, which is the maximum residue limit(MRL) set by FAO/WHO.

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Intermacromolecular Complex Formation between Helix Strilctilral Polypeptides through Hydrogen Bonding (수소 결합을 통한 Helix 폴리 펩타이드사이의 복합체 형성)

  • 조병기;김창규
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.18 no.1
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    • pp.99-132
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    • 1992
  • Polypeptide has been used broadly as an active ingredient in cosmetics We thought it is very important to investigate the adsorption behavior of polypeptide in order to pre-estimate the effect of these polypeptides. For the study of polypeptide adsorption, we have investigated complex formation of basic homopolypeptides, poly(L-proline) Form I [PLP(I)], Form II [PLP(II)] and poly(4-hydroxy-L-proline) (PHLP) with acidic homopolypeptides, poly(L-glutamic acid) (PLGA), poly(D-glutamic acid) (PDGA) and poly(L-aspartic acid) (PLAA) through hydrogen bonding in a hydroalcoholic medium with viscometer, 1ight scatter, pH meter and circular dicroism (CD). The polypeptides used in this study have helical structure in some conditions. The result exhibited that al 1 the complexes were formed as the composition of basic/acidic homopolypeptide : L:2 irrespective of the complex systems used. A more favorable complex is formed in the PLP(II)-PLGA system than PHLP-PLGA because PLP(II) has a more flexible helical conformation, whereas PHLP has a more rigid helical conformation. The right-handed helix PLGA formed the complex favorably and quickly with the left-handed helix PLP(II), whereas the left-handed helix PDGA formed the complex favorably with the right-handed helix PLP(I). The effect of side chain of the acidic homopolypeptides on the complexation was also studied. The result showed that more favorable condition for the complexation was PLGA-PLP(II) system which has longer side chain at acidic homopolypeptide than PLAA - PLP(II). All the above facts were well supported by CD measurement for the complex systems. By the CD spectra for the complexes we could deduce the conformational change of each homopolypeptide in the complexes On the basis of the above results, we performed the adsorption test of PLP(I, II) and PHLP on the hair having a left-handed helix. The adsorption amount of each polypeptide was analyzed by HPLC. The result showed that PLP(I) was adsorbed more than PLP(II), PLP(II) was adsorbed more than PHLP on the hair. On adsorbing polypeptides having a helical structure on the hair through hydrogen bonding, it could be concluded that the helical polypeptides having the opposite directional structure to the hair are adsorbed more than those having the same directional structure with the hair and also the polypeptides having a flexible conformation are adsorbed more than those having a rigid conformation.

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Antioxidant and Anti-inflammatory Effects of Fermented Blackcurrant Fruit Extracts with Saccharomycopsis fibuligera (Saccharomycopsis fibuligera로 발효된 블랙커런트추출물의 항산화 및 항염증 효과)

  • Jang, Jun-Hwan;Lee, Hyung-Kyu;Bae, Jun-Tae;Lee, Jae-Seob;Hwang, Bang-Yeon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.46 no.4
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    • pp.403-413
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    • 2020
  • While searching for useful microorganisms, Saccharomycopsis fibuligera which can be used as cosmetic materials were divided from Jeju island's traditional fermented foods. In this study, blackcurrant extract which contains a large amount of anthocyanin glycosides was fermented with S. fibuligera. HPLC analysis was performed to analyze the components of blackcurrant extract (BE) and fermented blackcurrant fruit extract (FBE). As a result, bio-conversion of delphinidin and cyanidin were able to be identified. In order to verify the anti-oxidant effect of BE and FBE, we investigated radical scavenging ability with DPPH and ABTS. In addition, to confirm anti-inflammatory effect, we investigated inhibition effect of nitric oxide (NO) production on lipopolysaccharide (LPS) - stimulated RAW264.7 macrophages, and inhibition effect of the expression of inflammatory-related proteins (iNOS, COX-2) by western blot analysis. As a result, as FBE has anti-oxidant and anti-inflammatory effects, we suggest that it might be used as an active ingredient for cosmetics.

Evaluation of Fungicides, Nozzle Type, and Spray Volume on Control of Typhula Blight on Cool Season Turfgrass (한지형잔디에 설부병 방제에 대한 살균제, 노즐타입 및 살포약량의 평가)

  • Chang, Tae-Hyun;Chang, Seog-Won;Jung, Geun-Hwa
    • Asian Journal of Turfgrass Science
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    • v.25 no.2
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    • pp.160-170
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    • 2011
  • Commercial formulation of fungicides was studied in vitro for sensitivity against Typhula species causal agents of Typhula blight. Efficacies of fungicides application, spray volume, nozzle types and fungicides applied time (early fall and late fall) were evaluated for their influence on the chemical control of Typhula blight of turfgrass during the winter season in Wisconsin. All fungicides effectively reduced the mycelial growth of eight isolates of Typhula spp. in vitro on potato dextrose agar (PDA) media. For inhibitory effects on mycelial growth of eight isolates, propiconazole was the most effective at $1.0{\mu}g$ active ingredient (a.i) / ml of PDA. Typhula incarnata two isolates were significantly more sensitive to all fungicides of PDA than six isolates of three varieties of T. ishikariensis. For 2 years in field experiment, unsprayed control has significantly more disease severity than seven fungicides were applied to field plots at two locations. Propiconazole was the most effective for controlling Typhula blight, at two locations in both years. The level of disease control was not dependent on fungicides spray volume or nozzle types at two locations. The disease damage treated with triadimefon applied time (early fall and late fall) was not significantly different at two location for two years.