• Title/Summary/Keyword: New and known compounds

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Alteration of Panax ginseng saponin composition by overexpression and RNA interference of the protopanaxadiol 6-hydroxylase gene (CYP716A53v2)

  • Park, Seong-Bum;Chun, Ju-Hyeon;Ban, Yong-Wook;Han, Jung Yeon;Choi, Yong Eui
    • Journal of Ginseng Research
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    • v.40 no.1
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    • pp.47-54
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    • 2016
  • Background: The roots of Panax ginseng contain noble tetracyclic triterpenoid saponins derived from dammarenediol-II. Dammarene-type ginsenosides are classified into the protopanaxadiol (PPD) and protopanaxatriol (PPT) groups based on their triterpene aglycone structures. Two cytochrome P450 (CYP) genes (CYP716A47 and CYP716A53v2) are critical for the production of PPD and PPT aglycones, respectively. CYP716A53v2 is a protopanaxadiol 6-hydroxylase that catalyzes PPT production from PPD in P. ginseng. Methods: We constructed transgenic P. ginseng lines overexpressing or silencing (via RNA interference) the CYP716A53v2 gene and analyzed changes in their ginsenoside profiles. Result: Overexpression of CYP716A53v2 led to increased accumulation of CYP716A53v2 mRNA in all transgenic roots compared to nontransgenic roots. Conversely, silencing of CYP716A53v2 mRNA in RNAi transgenic roots resulted in reduced CYP716A53v2 transcription. HPLC analysis revealed that transgenic roots overexpressing CYP716A53v2 contained higher levels of PPT-group ginsenosides ($Rg_1$, Re, and Rf) but lower levels of PPD-group ginsenosides (Rb1, Rc, $Rb_2$, and Rd). By contrast, RNAi transgenic roots contained lower levels of PPT-group compounds and higher levels of PPD-group compounds. Conclusion: The production of PPD- and PPT-group ginsenosides can be altered by changing the expression of CYP716A53v2 in transgenic P. ginseng. The biological activities of PPD-group ginsenosides are known to differ from those of the PPT group. Thus, increasing or decreasing the levels of PPT-group ginsenosides in transgenic P. ginseng may yield new medicinal uses for transgenic P. ginseng.

Integrative applications of network pharmacology and molecular docking: An herbal formula ameliorates H9c2 cells injury through pyroptosis

  • Zhongwen Qi;Zhipeng Yan;Yueyao Wang;Nan Ji;Xiaoya Yang;Ao Zhang;Meng Li;Fengqin Xu;Junping Zhang
    • Journal of Ginseng Research
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    • v.47 no.2
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    • pp.228-236
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    • 2023
  • Background: QiShen YiQi pills (QSYQ) is a Traditional Chinese Medicine (TCM) formula, which has a significant effect on the treatment of patients with myocardial infarction (MI) in clinical practice. However, the molecular mechanism of QSYQ regulation pyroptosis after MI is still not fully known. Hence, this study was designed to reveal the mechanism of the active ingredient in QSYQ. Methods: Integrated approach of network pharmacology and molecular docking, were conducted to screen active components and corresponding common target genes of QSYQ in intervening pyroptosis after MI. Subsequently, STRING and Cytoscape were applied to construct a PPI network, and obtain candidate active compounds. Molecular docking was performed to verify the binding ability of candidate components to pyroptosis proteins and oxygen-glucose deprivation (OGD) induced cardiomyocytes injuries were applied to explore the protective effect and mechanism of the candidate drug. Results: Two drug-likeness compounds were preliminarily selected, and the binding capacity between Ginsenoside Rh2 (Rh2) and key target High Mobility Group Box 1 (HMGB1)was validated in the form of hydrogen bonding. 2 μM Rh2 prevented OGD-induced H9c2 death and reduced IL-18 and IL-1β levels, possibly by decreasing the activation of the NLRP3 inflammasome, inhibiting the expression of p12-caspase1, and attenuating the level of pyroptosis executive protein GSDMD-N. Conclusions: We propose that Rh2 of QSYQ can protect myocardial cells partially by ameliorating pyroptosis, which seems to have a new insight regarding the therapeutic potential for MI.

Evaluation of Carcinogenic Metals in Particulate Using New ISO Standard Method (국제표준규격에 의한 입자상 물질 중 발암성 금속의 평가)

  • Park, Ji Young;Yoon, Chung Sik;Ha, Kwon Chul
    • Journal of Korean Society of Occupational and Environmental Hygiene
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    • v.18 no.2
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    • pp.99-107
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    • 2008
  • We quantified the human carcinogenic metals (chromium, nickel) in fumes from flux cored arc welding using stainless steel (FCAW/SS) wires. Zinc and calcium were also quantified because of their possibility of zinc chromate and calcium chromate, respectively. Welding was performed in an American Welding Society standard fume collection chamber. Insoluble and soluble forms of metals were analyzed by ISO 15202 method. Total chromium (insoluble+soluble) content and total nickel content were lower in FCAW/SS fumes (4.65%, 1.05%, respectively)than in stainless steel content (ca. 18%, 8%,respectively). Insoluble fraction in total chromium was 79.8 (range 64.5~95.1)% and 94.4(range 90.1~98.1)% in total nickel. Atomic emission spectroscopy used in this study does not differentiate the chromium valence status while ACGIH defines its carcinogenicity according to the valence status. From this study and previous study, we estimated the hexavalent chromium content in FCAW/SS was 0.2~1.1% and about 85% of them was soluble. The content of zinc and calcium, which can be existed as chromate forms, was low (0.02 %, 0.04% respectively) in FCAW/SS. Exposure assessment for zinc chromate and calcium chromate is possible because chromium in both compounds is used as a surrogate even though it is not well known that what compounds of zinc and calcium are formed in welding fume.

Glycosyl flavones from Humulus japonicus suppress MMP-1 production via decreasing oxidative stress in UVB irradiated human dermal fibroblasts

  • Nam, Eui Jeong;Yoo, Gyhye;Lee, Joo Young;Kim, Myungsuk;Jhin, Changho;Son, Yang-Ju;Kim, Sun Young;Jung, Sang Hoon;Nho, Chu Won
    • BMB Reports
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    • v.53 no.7
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    • pp.379-384
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    • 2020
  • Exposure to Ultraviolet (UV) light induces photoaging of skin, leading to wrinkles and sunburn. The perennial herb Humulus japonicus, widely distributed in Asia, is known to have anti-inflammatory, antimicrobial, and antioxidant effects. However, the physiological activities of isolated compounds from H. japonicus have rarely been investigated. This study focused on the isolation of active compounds from H. japonicus and the evaluation of their effects on photoaging in UVB-irradiated human fibroblast (Hs68) cells. When the extract and four fractions of H. japonicus were treated respectively in UVB-irradiated Hs68 cells to investigate anti-photoaging effects, the ethyl acetate (EtOAc) fraction showed the strongest inhibitory effect on MMP1 secretion. From EtOAc fraction, we isolated luteolin-8-C-glucoside (1), apigenin-8-C-glucoside (2), and luteolin-7-O-glucoside (3). These compounds suppressed UVB-induced MMP-1 production by inhibiting the phosphorylation of the mitogen-activated protein kinases (MAPKs) and activator protein-1 (AP-1). When the antioxidant activity of the compounds were estimated by conducting western blot, calculating the bond dissociation energies of the O-H bond (BDE) at different grade, and measuring radical scavenging activity, we found luteolin-8-C-glucoside (1) showed the strongest activity on the suppression of UVB-induced photoaging. These results demonstrate the inhibitory effect of three flavone glycosides derived from H. japonicus on MMP-1 production, MAPK and AP-1 signaling, and oxidative stress; this could prove useful in suppressing UVB induced photoaging.

Present Status and Problems of Chemical Seed Treatment of Seedborne Diseases (종자소독의 현황과 문제점)

  • Lee Du Hyung
    • Korean journal of applied entomology
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    • v.22 no.2 s.55
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    • pp.130-137
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    • 1983
  • A wide variety of pathogens are known io be seedborne, carried either as infectious mycelium internally or as contaminants on the seed coat. When seed is infected with a pathogen, the seed nay be rendered nonviable or it may remain viable but produce weak seedling. In some cases, the Infected seedling nay not be severely weakened, but nay serve as a source of primary inoculum within a community of plants. A recent problem nay be the dissemination of seedborne pathogens occurring as a result of the massive movements of seed, as a part of the 'Green revolution' Disease of great danger to agriculture may be introduced with seed from other parts of world. Seed treatment with organic mercury compounds in liquid form had become popular since about 1955. Organic mercury compounds contributed considerably to the increase in production of many crops and vegetables. In 1975, however, the use of organic mercury compound was forbidden because of doubts regarding their residual mammalian toxicity in agricultural products. Benomyl-thiram mixture, thiophanate methyl-;hiram mixture and TCMB have now been registered as seed disinfectants for the use of rice blast, brown spot and Bakanae disease. Oxathiinsthiram mixture has been registered as seed disinfectant for barley and wheat loose smut and leaf stripe of barley. Agricultural techniques have made such rapid progress that the nursery methods changed from the use of paddy nursery to box nursery designed for machine-transplanting. The spread of rice transplanting machines has caused increase of seedborne diseases. Among seedborne diseases, Bakanae disease has remarkably increased and causes much damage recently. In order to counter this trend, seed disinfectants must also be diversified. First, effective non-selective disinfectants need to be developed, and second, appropriate control methods always need to be prepared in parallel with the development of new techniques for cultivation.

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Assessment of Sensitivity of Photo-Chromosomal Assay in the Prediction of Photo-carcinogenicity (광염색체이상시험의 광발암성 예측능력에 대한 평가)

  • Hong Mi-Young;Kim Ji-Young;Lee Young Mi;Lee Michael
    • Toxicological Research
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    • v.21 no.2
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    • pp.99-105
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    • 2005
  • Photo-mutagenic compounds have been known to alter skin cancer rates by acting as initiators or by affecting subsequent steps in carcinogenesis. The objectives of this study are to investigate the utility of photo-chromosomal aberration (photo-CA) assay for detecting photo-clastogens, and to evaluate its ability to predict rodent photocarcinogenicity. Photo-CA assay was performed with five test substances that demonstrated positive results in photo-carcinogenicity tests: 8-Methoxypsoralen (photoactive substance that forms DNA adducts in the presence of ultraviolet A irradiation), chlorpromazine (an aliphatic phenothiazine an alpha-adrenergic blocking agent), lomefloxacin (an antibiotic in a class of drugs called fluoroquinolones), anthracene (a tricyclic aromatic hydrocarbon a basic substance for production of anthraquinone, dyes, pigments, insecticides, wood preservatives and coating materials) and Retinoic acid (a retinoid compound closely related to vitamin A). For the best discrimination between the test substance-mediated genotoxicity and the undesirable genotoxicity caused by direct DNA absorption, a UV dose-response of the cells in the absence of the test substances was firstly analyzed. All 5 test substances showed a positive outcome in photo-CA assay, indicating that the photo-CA test is very sensitive to the photo-genotoxic effect of UV irradiation. With this limited data-set, an investigation into the predictive value of this photo-CA test for determining the photo-carcinogenicity showed that photo-CA assay has the high ability of a test to predict carcinogenicity. Therefore, the photo-CA test using mammalian cells seems to be a sensitive method to evaluate the photo-carcinogenic potential of new compounds.

A useful material isolation from the Bombycis corpus (Beauveria bassiana) growing of the silkworm, Bombyx mori L. (백강잠(Bombysis corpus)으로부터 유용물질 분리)

  • 정이연;남성희;홍인표;유승헌;권학철;이강노
    • Journal of Sericultural and Entomological Science
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    • v.45 no.1
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    • pp.25-30
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    • 2003
  • This study was carried out to investigate active constituents of Bombysis corpus on the neurite outgrowth from PC 12 cells led to isolate three new and a known sphingolipids from the n-hexane soluble portion and five amines from the butanol soluble portion of its methanol extract. On the basis of spectroscopic data, their structures have been elucidated as (4E,6E,2S,3R)-2-N-eicosanoyl-4,6-tetradecasphingadienine, (4E,2S,3R)-2-N-eicosanoyl-4-tetradecasphingenine,(4E,6E,2S,3R)-2-N-docosanoyl-4,6-tetradecasphingadienine,(4E,6E,2S,3R)-2-N-docosanoyl-4,6-tetradecasphingadienine,(4E,2S,3R)-2-N-octadecanoyl-4-tetradecasphingenine, 1,7-dimethyl-xanthine, uracil, urea, betaine and tyrosine, respectively. The neurite outgrowth activities of these compounds were examined in PC12 cells by measuring the length of neurites. These compounds promoted neurite outgrowth in PC12 cells significantly.

Ginsenosides analysis of New Zealand-grown forest Panax ginseng by LC-QTOF-MS/MS

  • Chen, Wei;Balan, Prabhu;Popovich, David G.
    • Journal of Ginseng Research
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    • v.44 no.4
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    • pp.552-562
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    • 2020
  • Background: Ginsenosides are the unique and bioactive components in ginseng. Ginsenosides are affected by the growing environment and conditions. In New Zealand (NZ), Panax ginseng Meyer (P. ginseng) is grown as a secondary crop under a pine tree canopy with an open-field forest environment. There is no thorough analysis reported about NZ-grown ginseng. Methods: Ginsenosides from NZ-grown P. ginseng in different parts (main root, fine root, rhizome, stem, and leaf) with different ages (6, 12, 13, and 14 years) were extracted by ultrasonic extraction and characterized by Liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry. Twenty-one ginsenosides in these samples were accurately quantified and relatively quantified with 13 ginsenoside standards. Results: All compounds were separated in 40 min, and a total of 102 ginsenosides were identified by matching MS spectra data with 23 standard references or published known ginsenosides from P. ginseng. The quantitative results showed that the total content of ginsenosides in various parts of P. ginseng varied, which was not obviously dependent on age. In the underground parts, the 13-year-old ginseng root contained more abundant ginsenosides among tested ginseng samples, whereas in the aboveground parts, the greatest amount of ginsenosides was from the 14-year-old sample. In addition, the amount of ginsenosides is higher in the leaf and fine root and much lower in the stem than in the other parts of P. ginseng. Conclusion: This study provides the first-ever comprehensive report on NZ-grown wild simulated P. ginseng.

Butyrolactones Derivatives from the Fermentation Products of an Endophytic Fungus Aspergillus versicolor

  • Ye, Yan-Qing;Xia, Cong-Fang;Yang, Juan-Xia;Yang, Yu-Chun;Qin, Ying;Gao, Xue-Mei;Du, Gang;Li, Xue-Mei;Hu, Qiu-Fen
    • Bulletin of the Korean Chemical Society
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    • v.35 no.10
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    • pp.3059-3062
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    • 2014
  • Two new butyrolactones, asperphenol A (1) and B (2), together with four known butyrolactones (3-6) were isolated from the fermentation products of an endophytic fungus Aspergillus versicolor. Their structures were elucidated by spectroscopic methods including extensive 1D- and 2D-NMR techniques. Compounds 1-6 were also tested for their anti-tobacco mosaic virus (anti-TMV) activities. The results showed that compound 2 exhibited high anti-TMV activity with inhibition rate of 46.7%. The other compounds also exhibited potential anti-TMV activities with inhibition rates in the range of 21.8-28.4%.

Current status of natural product industry and its commercial application to health functional foods

  • Park, Jong Dae
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2018.10a
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    • pp.21-21
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    • 2018
  • Natural product substances have historically served as the most significant also be prepared by source of new leads for pharmaceutical development. They can chemical synthesis(both semisynthesis and total synthesis) and have played a important role in the field of organic chemistry by providing synthetic targets. Rcently, they have also been extended for commercial purpose to refer to medicinal products, health functional foods, dietary supplements and cosmetics from natural sources. A large number of currently prescribed drugs have been either directly derived from or inspired by natural products. However, with the advent of robotics, bioinformatics, high throughput screening(HTS), molecular biology-biotechnology, combinatorial chemistry, in silico(molecular modeling) and other methodologies, the pharmaceutical industry has largely moved away from plant derived natural products as a source for leads and prospective drug candidates. The strategy for natural prduct industry is now changing from drug approaches to health foods by identifying effective natural products as preparations. In Korea, a lot of development of natural product based drugs have been done, but very few on health functional foods. The concept of natural product based health foods is not active components as lead compounds but standardized extracts or preparation mixed with other medicinal plants. The representative material has been recently known to be a standardized ginseng extract "Ginsana G 115" developed by Swiss Pharmaton company. The purpose of this presentation is to underline how natural products research continues to make significant contributions in the domain of discovery and development of new health functional foods. It is proposed to present the development of high value added health food or health functional foods through scientific investigation on efficacy and standardization of new materials form natural products.

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