• Title/Summary/Keyword: 7-dihydro-3

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Inhibition of the Formation of Adducts Between Metabolites of Benzo(a)pyrene and DNA by Panaxydol in vivo and in vitro (Benzo(a)pyrene 대사물질들의 DNA에 대한 Adduct 형성 억제에 미치는 Parlalrydol의 효과)

  • 박진규;김신일
    • Journal of Ginseng Research
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    • v.13 no.1
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    • pp.42-48
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    • 1989
  • The binding of bay region diol-epoxides of polycyclic aromatic hydrocarbons (PAHs) to target tissue DNA is thought to be essential for the initiation of cancer by these compounds. In this study we investigated the effect of polyacetylenes such as panaxynol and panaxydol on the formation of benzo(a)pyreno (BP)-metabolite-DNA adduct in the liver of ICR mice. Treatment of mice by i.p. administration of polyacetylenes produced a marked reduction in BP metabolite binding to DNA in vitro. Following i.v. administration of (3H)BP(300, ${\mu}$Ci/21 nmoles/0.1 nt DMSO) to mice, radioactivity was detected in the DNA of the liver in vivo. The result of tentative identification of the 4 peaks between the two standard markers for high pressure liquid chromatography showed that the peaks. I, II, III, and IV were BP-phenol oxide-DNA adduct (or BP-diol-epoxide-dCyt. adduct), (-) BP$.$diolepoxide I:dGuO adduct, (+) BP-diol-epoxide I: dGuo adduct, and BP-diol-epoxide II:dGuO adduct, respectively. The minor adduct, (-) BP-diol epoxide I: dGuo was reduced to 6971 of the amount of the control, while the major adduct, (+) BP-diolepoxide I: dGuO(peak II) which was produced from (-) BP-7, 8-diol was reduced to 78% of that of the control. The amount of the minor adduct, BP-diol-epoxide II:dGuo adduct(peak IV) which formed from (+) BP-7, 8-diol was 58% of the control. These results show that the panaxydol is more related to inhibition of the formation of the minor ad- ducts than of the major adducts, which were generally produced from ($\pm$) BP-7, 8-dihydro-dials.

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Micronucleus Test of DW-116, a Novel Antibacterial Quinolone (신규 퀴놀론 항균제 DW-116의 소핵시험)

  • Moon, Eun-Yi;Lee, Jin;Choi, Chung-Ha;Lee, Chi-Woo;Chung, Yong-Ho;Yoon, Sung-June;Lee, Dog-Keun
    • Biomolecules & Therapeutics
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    • v.4 no.3
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    • pp.239-243
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    • 1996
  • DW-116 {(1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hydrochloride) is a new quinolone antibiotic with a broad antibacterial spectrum against G(+) and G(-) bacteria. DW-116 was evaluated for the appearance of micronucleus in polychromatic erythrocytes (PCEs) of mouse bone marrow cells after intraperitoneal and oral single administration. We prepared the bone marrow cells at 30hr after drug administration and they were used for measuring PCE with micronucleus. The results showed there was no statistically significant increase in the numbers of PCEs with micronucleus in all DW-116 administered groups compared with a negative control group. The results also showed that the ratio of normochromatic erythrocytes(NCEs) to PCEs of all DW-116 administered groups was not significantly different from that of a negative control group. These results suggested that DW-116 may not cause any chromosomal damage and it has no in vivo mutagenic potential under these experimental conditions.

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Evaluation of Lethality by Chemical Marker (Chemical Marker를 이용한 살균도 예측)

  • Choi, Yang-Mun;Kim, Hie-Joon
    • Korean Journal of Food Science and Technology
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    • v.29 no.1
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    • pp.32-37
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    • 1997
  • The rate constants and activation energies for formation of two chemical markers, M-1 and M-2 at sterilization temperatures were determined in a meatball system. Destruction rates for bacterial spores were also determined. The rate constants for M-1 and M-2 formation at $121^{\circ}C$ were 0.03 and 0.28 Abs/min, respectively. The activation energies for M-1 and M-2 were 27.9 and 24.6 Cal/mol. M-2 was formed faster than M-1 and reached a maximum and decreased. M-1 formation continued up to 30 min at $121^{\circ}C$ and 10 min at $131^{\circ}C$, which makes M-1 a more useful chemical marker for high $F_0$ values. The D-values for spores (B. stearothermophilus ATCC 12980) at 111, 114.4, 117.7 and $121^{\circ}C$ were 7.5, 4.5, 1.9 and 0.58 respectively. At temperatures between 111 and $121^{\circ}C$, there was a liner correlation between destruction of the spores and the M-1 formation. It was difficult to get accurate D-value at $126^{\circ}C\;and\;131^{\circ}C$, because almost all spores were dead before temperature at the center of the meatball reached $126^{\circ}C$. These data suggest that the chemical marker should be used to evaluate overprocessing as well as microbial lethality in aseptic processing.

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The Effects of Ginseng Saponin Fraction on Growth and Siderophore Formation in Eseherichia coli K-12 (인삼사포닌 분획이 Escherichia coli K-12의 성장과 Siderophore 생성에 미치는 영향)

  • 조영동;이용범
    • Journal of Ginseng Research
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    • v.7 no.2
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    • pp.102-107
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    • 1983
  • The effects of saponin, one of major components (Panax ginseng C.A. Meyer), on the growth of E. coli K-12 and the formation of siderphore was observed The following results were obtained. 1. When E. coli was grown on medium containing 1${\times}$10-5%-11${\times}$10-1% of the saponin, the rate of growth was stimulated at 10-1% of the saponin significantly compared to that of control. 2. When E. coli K-12 was grown on medium containing 1${\times}$10-1% of the saponin, the amount of siderphore was two times as much as the control. 3. The growth of E. coli was observed to be dependent on the concentration of siderophore when siderophore was added to medium. 4. The effect of saponin on the formation of siderophore in vitro was observed to reach maximum at 1${\times}$10-3% of the saponin. Such results suggest that the growth rate of E. coli K-12 could be enhanced by ginseng saponin fraction through stimulation of siderphore formation. We have described the fast growth of E. coli, K-12 and B. subtilis, rapid uptake of 14C-glucose, and high level of other metabolites such as lipids and proteins of E. coli, and B. subtilis in medium containing saponing fraction compared to that of microorganisms without saponin fraction.1∼3Such differences were claimed to be due to rapid uptake of 14C-glucose by widened periplasmic region throught unknown mechanism in the prescence of saponin fraction in medium3 and have raised a question whether there is another possible factor, siderophore4(Greek for iron bears), since microorganisms must secure a sufficient amount of iron for normal growth. These are known to be synthesized by the cells under iron-deficient condition and in most case, excreted into the medium5, where they can complex and solubilize any iron present there. It is generally believed that these complexes are then taken into the cells presumably by specific transport systems, thus providing iron for cell metabolism. Within the group of enteric bacteria, only three species (E. coli, S. typhimurium, and A. aerogense) have, so far, been studied in a ny detail. The main iron-binding compound produced by these species is enterochelin, and its role in iron transport is now well established. And biosynthesis of enterochelin from 2, 3- dihydroxybenzoate and serine in the prescence of magnesium ions and ATP was reported6. 2, 3-dihydroxybenzoate was also shown to involve isochorismate and 2, 3-dihydro-2, 3-dihydroxybenzoate as intermediate.7∼11 The present paper deals with the effect of ginseng saponin fraction on growth, the level of enterochelin formation in vivo and the conversion of 2, 3-dihydroxybenzoate and serine into entrochelin in vitro, and entrochelin obtained on the growth in relation to possible explanation of ginseng saponin fraction on the rapid growth of E. coli, K-12.

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Studies on the Residue of Carbofuran (Carbofuran의 잔류(殘溜)에 관(關)한 연구(硏究))

  • Park, Y.D.;Keum, S.S.;Lee, K.S.;Hong, Y.C.
    • Applied Biological Chemistry
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    • v.20 no.2
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    • pp.236-241
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    • 1977
  • Analytical method of carbofuran (2,3-dihydro-2, 2-dimethyl-7-benzofuranyl methyl carbamate) residues and its persistence in rice seeds, rice seedlings, rice plants and soils were studied by gas-liquid chromatographic analysis using electron capture detector. 1. The effective column material for clean-up is Florisil (5% $H_2O$)+Alumina (4% $H_2O$)+absorbent mixture with rinsing the first 300l of eluants to remove impurities in the column materials. 2. The method of applying an gelatin encapsulated carbofuran to the root zone of rice plant is the longest persistence in its residues. 3. By seed treatment, no carbofuran residues were detected in rice seeds and seedlings. 4. The amounts of carbofuran residues in rice seedlings is in proportion to the soaking time of rice seedlings in carbofuran solution rather than the concentration of the chemical. 5. Applying carbofuran by root zone has the higher and the loger residual effect than broadcast. 6. Persistence of carbofuran in the high clay content soil is longer than in the low clay content soil. 7. No carbofuran residue was detected in rough rice at havesting time.

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Invitro and Virtual Screening of Bioactive Molecule from Mycelium of Trichoderma atroviride Inhibit the UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine Deacetylases (LpxC) for Treatment of Bacterial Infection

  • Saravanakumar, Kandasamy;Park, Cheol-Ho;Wang, Myeong-Hyeon
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2018.04a
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    • pp.67-67
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    • 2018
  • Trichoderma species are a rich source of metabolites, but less known for biomedical potential. This work deals with antibacterial and antioxidant potentials of intracellular non-cytotoxic metabolites, extracted from Trichoderma atroviride (KNUP001). A total of 53 fractions was collected by column chromatography and tested for cytotoxicity by MTT assay. Only one fraction (F41) was found to be non-toxic to Vero cells with $95.4{\pm}0.61%$ of survival. The F41 was then subjected to chemical analysis, antibacterial and antioxidant assays. The F41 at $500{\mu}g.ml^{-1}$ showed the total antioxidant of $48.70{\pm}2.90%$, DPPH radical scavenging activity of $37.25{\pm}2.25$, nitric oxide (NO) radical scavenging activity of $54.55{\pm}1.95$ and $H_2O_2$ radical scavenging activity of $43.75{\pm}3.21$. The F41 at $25{\mu}g.ml^{-1}$ displayed antibacterial activity against E. coli ($14.25{\pm}0.2mm$), P. mirabilis ($10.4{\pm}0.6mm$), S. dysenteriae ($18.6{\pm}03mm$), S. paratyphi A ($14.1{\pm}1.1mm$), E. aerogenes ($5.6{\pm}0.4mm$) and S. marcescens ($14.25{\pm}0.2mm$). GC-MS analysis revealed the dominant presence of oleic acid C 18.1 (63.18%), n-hexadecanoic acid (6.17%), and ethyl oleate (4.93%) and potent molecules such as 8-[(2E)-2-(3-hydroxybenzylidene)hydrazinyl]-1,3,7-trimethyl-3,7-dihydro-1H-purine-2,6-dione, 2-(Dimethylamino)ethyl (1Z)-N-hydroxy-2-(4-morpholinyl)-2-oxoethanimidothioate, Fluorene in the F41, and virtual study revealed that these molecules are likely responsible for the antibacterial activities of F41. Hence, further investigation deserves on purification and characterization of the active metabolites from T. atroviride strain KNUP001 towards developing molecular leads to effective antibacterial drugs, and non-toxic to host cells.

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Comparison of Volatile Aroma Compounds between Synurus deltoides and Aster scaber Leaves (수리취와 참취 엽의 휘발성 향기성분 비교)

  • Lee, Kyeong-Cheol;Sa, Jou-Young;Wang, Myeong-Hyeon;Han, Sang-Sup
    • Korean Journal of Medicinal Crop Science
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    • v.20 no.1
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    • pp.54-62
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    • 2012
  • This study was investigated to compare the volatile aroma compounds of Synurus deltoides and Aster scaber. The volatile aroma compounds from Synurus deltoides and Aster scaber were extracted by soild-phase microextraction (SPME) methods. S. deltoides had 97 volatile aroma compounds such as including 5-acetyl-1,2-dihydro acenaphtylene (14.63%), ${\beta}$-cubebene (9.31%), caryophyllene (8.97%), ${\beta}$-chamigrene (7.14%), ${\beta}$-selinene (2.71), ${\alpha}$-farnesene (2.47%), ${\alpha}$-bergamotene (2.26%), ${\beta}$-elemene (1.94%), etc. A. scaber had 84 volatile aroma compounds such as (+)-epi-bicyclosesquiphellandrene (10.38%), terpinolen (10.09%), caryophyllene (6.04%), 8-isopropenyl-1,5-dimethyl-1,5-cyclodeca diene (5.42%), ${\alpha}$-himachalene (5.04%), ${\beta}$-thujene (4.37%), ${\beta}$-pinene (4.28%), ${\beta}$-cubebene (3.99%), etc. Conclusively, the main common volatile aroma compounds in S. deltoides and A. scaber leaves were 19 volatile aroma compounds such as caryophyllene, terpinolen, ${\beta}$-cubebene. But the composition and amount of volatile aroma compounds were very different between the two species.

Anthelmintic Natural Products against Clonorchis sinensis and the Analogues (간디스토마에 작용하는 천연물 및 그 유사체)

  • 안병준;이재구
    • YAKHAK HOEJI
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    • v.30 no.5
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    • pp.253-265
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    • 1986
  • Among 230 species of herbal drugs screened, thirty one show the anthelmintic activities in vitro against Clonorchis sinensis, the chinese liver fluke. The active substances have been isolated and their structures identified. Some of the active substances and their derivatives have been synthesized, followed by anthelmintic activity tests. The extracts from the active drugs cause damages in organs of the adult worm in the hepatic duct of rabbit. Some fresh water fish, which function as bad hosts for the fluke, excrete defense substances against the cercaria of the fluke. The defense substances have been isolated from Cyprinus carpio and Cyprinus carpio nudus, followed by structural identification. The results are summarized as follows: l) The bark of Machilus thunbergii as well as the seed of Schizandra chinensis contain meso-dihydro-guaiaretic acid as the anthelmintic component. Among derivatives synthesized, 4-phenyl-1-((3, 4-dihydroxyphenyl)-, 4-phenyl-1-(3-hydroxy-4-methoxy phenyl)-and 4-phenyl-1-(4-hydroxy-3-methoxy phenyl)-2, 3-dimethyl butanes show considerable activities. Administration of the bark extract mainly damages the bladder of the adult worm. 2) The active substance from the roasted fruit of Prunus mume is 2-hydroxymethylfurfural. This substance is produced during the roasting process. Administration of the fruitextract causes a damage of the bladder of the adult worm. 3) The active substance from the root of Scutellaria baicalensis is 5.2'-dihydroxy-6, 7, 8, 6'-tetramethoxyflavone. 4) Beside alantolactone, a very strong anthelmintic component is contained in the root of Inula helenium. Administration of the root extract causes irreversible damage on the worm, affecting mainly the reproductive organs. 5) The cercaricidal substances from the epidermis of C. carpio and C. carpio nudus are ethyl linoleate and linoleic acid, respertively. 6) The cercaricidal substances from various kinds of fresh water fish have different $R_f$ values, implying that the defense substances are species-specific. Unexpectedly, the fish with good host function, for example Pseudorasbora parva, excrete the defense substances, too. The defense substances are possibly organ-specific in individual species; the organs essenstial for the existence of the species excrete the defense substances, allowing other parts to be invaded by the cercaria. 7) The cercaricidal fraction of Carassius carassius is detected only in the fish which have been collected during the summer time from May to September, Its secretion is not dependent on water temperature. Thus, it seems to be possible that the secretion of the defense substance would be stimulated through a contact between the fish and cercaria.

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Effect of Carbofuran on Rice Growth (식물생장조절제(植物生長調節劑) Carbofuran이 벼 생육(生育)에 미치는 영향(影響))

  • Kim, Soon-Chul
    • Korean Journal of Weed Science
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    • v.7 no.1
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    • pp.98-106
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    • 1987
  • The effect of carbofuran (2, 3-Dihydro-2,2-dimethyl-benzofuran-7-ylmethyl carbamate) on rice growth was evaluated as a direct growth stimulant of rice. For this, several laboratory and field trials conducted from 1981 to 1986 at the Yeongnam Crop Experiment Station. Carbofuran solution affected the germination of rice seed. The growth of seminal roots was adversely affected by the increase of carbofuran concentrations while the length of single root became longer with the concentration increment up to 50 ppm. Carbofuran application (0.18g ai/$m^2$) at the rice nurserybed significantly enhanced the rice growth and recovered from the Low temperature damage. The enhancement effect was more pronounced at the plot that applied carbofuran before rice seeding as soil incorporation than top-dressing. The effect of growth enhancement further extended to transplanted lowland rice. This effect was greater at double cropping area (late of June transplanting) compared to single cropping area (May transplanting). Among important agronomic traits, the increment of panicle number was the most important direct effect for increasing rice grain yield by carbofuran application. Carbofuran application also exhibited the reducing effect against low temperature damage at reductive division stage and at rice heading stage and against submergence damage at booting stage through enhancement of fertile grain ratio, ripening ratio or photosynthetic activity.

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3,9-Diferuloyl-6-oxopterocarpen (Tensolin-F$^\circledR$): a Novel Anti-wrinkle Agent for Cosmeceuticals (새로운 주름개선 소재: 3,9-diferuloyl-6-oxopterocarpen (Tensolin-F$^\circledR$)의 개발과 화장품 응용)

  • 이범천;이정재;박성민;김철배;심관섭;김진화;이근수;이천일;표형배
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.1
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    • pp.7-13
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    • 2004
  • As a novel anti-wrinkle agent, 3,9-diferuloyl-6-oxopterocarpen (Tensolin-F$^{(R)}$) has been synthesized and its anti-aging effects have been investigated. In the present study, to investigate the relationship between aging and Tensolin-F$^{(R)}$, we examined its effect on scavenging activities of radicals and reactive oxygen species (ROS), in vitro inhibition activity of matrix-metalloproteinase (MMP) and expression of UVA-induced MMPs in human dermal fibroblasts (HDF). Tensolin-F$^{(R)}$ was found to show activities of scavenging radicals and ROS with the $IC_{50}$/ values of 0.2 mM and 0.95 mM against 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and superoxide radicals, respectively, in the xanthine/xanthine oxidase system. Fluorometric assays for the proteolytic activities of MMP-l (collagenase) were performed using fluorescent collagen substrates. Tensolin-F$^{(R)}$ inhibited the activities of MMP-l in a dose-dependent manner and the $IC_{50}$/ values calculated from semi-log plots were 0.025 mM. Also, UVA induced MMP-1 expression was reduced 85% by treatment with Tensolin-F$^{(R)}$ at 0.8 uM, which was reduced dose-dependent manner. The results of clinical study showed that 4.8 mM Tensolin-F$^{(R)}$ treated group reduced wrinkle significantly compared with placebo treated group (P 〈 0.05). Taken together, these result suggest that Tensolin-F$^{(R)}$ act as an anti-wrinkle agent by taking effects to antioxidation and reducing UVA-induced MMP-l production.-l production.