• Title/Summary/Keyword: active compound

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Synthesis of Several New Isoxazole, Imidazo[1, 2-a]pyridine, Imidazo[1, 2-a]pyrimidine, Benzoxadiazine and Benzothiazine Derivatives from Hydroximoyl Halides

  • Abdelhamid, Abdou O.;Abdou, Sadek E.;Mahgoub, Sayed A.
    • Archives of Pharmacal Research
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    • v.15 no.4
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    • pp.317-321
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    • 1992
  • Furoyldroximoyl chloride 3d reacted with 2-aminopyridine, 2-aminopyrimidine. O-aminophenol, O-phenylenediamine and aminothiophenol to afford imidazo [1, 2-a]pyridine 6. imidazo[1, 2-a]pyrimidine 8, benzoxadiazine 10, nitrosobenzopyrizine 13a and nitrosobenzothiazine 13b, respectively. Isoxazoline 18 and pyrrolidino[3, 4-d]isoxazolin-4, 6-dione derivatives 19a and 19b obtained by the reaction of 3 with acrylonitrile and N-arylmaleimide. Hydroximoyl chloride 3 reacted with thiophenol and sodium benzene-sulfinate to yield furylglyoxaloxime 16a and 16b, respectively. Hydroximoyl chloride 3 reacted also with some active methylene compound to give isoxazole derivatives 20-23, respectively.

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Hormonal Effect and Cytokinin Autonomy in callus Culture of Phaseolus vulgaris L. (식물 Hormone의 영향과 Cytokinin Autonomy)

  • 김상구
    • Journal of Plant Biology
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    • v.25 no.4
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    • pp.161-168
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    • 1982
  • The activities of auxins and cytokinins have been examined in the growth of callus tissue derived from Phaseolus vulgaris L. cv. Damyang. The synthetic auxin, picloram was the most effective in promoting callus growth and the range of effective concentrations (0.1$\mu{M}$ to 32$\mu{M}$) was broad. 2, 4-D also enhanced callus growth at the optimal concentration of 3.2$\mu{M}$. NAA promoted callus growth at relatively higher concentrations than other auxins tested. IAA was less effective in supporting callus growth. Cytokinin bearing saturated side chain ($N^6$-isopentyladenine) was approximately 30 times more active than the corresponding unsaturated compound, $N^6$-($\D^2$-isopentenyl) adenine. The abilities of cytokinin-autonomous growth were also examined. Callus tissues previously grown on concentrations lower and/or higher than optimal concentrations of cytokinins were better habituated in the subsequent passage. It was suggested that the development of cytokinin autonomy may be related to dosage-concentrations of cytokinin in the previous passage.

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Antitumor Agent from the Rhizome of Anemarrhena asphodeloides (지모(知母)의 항암활성성분에 관한 연구)

  • Lee, Seung-Ho;Ryu, Shi-Yong;Choi, Sang-Un;No, Zae-Sung;Kim, Sung-Ki;Lee, Chong-Ock;Ahn, Jong-Woong
    • Korean Journal of Pharmacognosy
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    • v.26 no.1
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    • pp.47-50
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    • 1995
  • EtOAc soluble part of MeOH extract of Anemarrhena asphodeloides rhizome was evaluated for the cytotoxicity against the five kinds of human tumor cell lines (A-549, SK-OV-3, SK-MEL-2, XF498 and HCT15) in vitro. Bioassay-guided fractionation of EtOAc soluble part led to the isolation of active compound which was identified as timosaponin A-III showed potent cytotoxic activity, but its genin, sarsasapogenin, did not show cell growth inhibition.

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Mollugin-mediated Inhibition of Proinflammatory Biomarkers in Lipopolysaccharide-stimulated RAW264.7 Cells

  • Kim, Jin-Kyung;Park, Geun-Mook;Jun, Jong-Gab
    • Biomedical Science Letters
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    • v.18 no.4
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    • pp.338-344
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    • 2012
  • Mollugin is the active compound of Rubia cordifolia, a well known herb widely used in alternative medicines for the treatment of various inflammatory diseases including arthritis and uteritis. In the present study, we investigated the anti-inflammatory effects of mollugin in lipopolysaccharide (LPS)-stimulated RAW264.7 murine macrophage cells. Treatment with mollugin significantly inhibited LPS-induced release of nitric oxide, prostaglandin $E_2$, and inflammatory cytokines, such as tumor necrosis factor-${\alpha}$ and interleukin-6. In addition, mollugin suppressed LPS-induced nuclear factor-kappa B (NF-${\kappa}B$) transcriptional activity. These results suggest that mollugin inhibits LPS-induced expression of inflammatory molecules via NF-${\kappa}B$, at least in part, and indicate the potential value of mollugin as a valuable new drug candidate for the treatment of various inflammatory diseases.

Study on Sol-Gel Prepared Phosphosilicate Glass-Ceramic For Low Temperature Phosphorus Diffusion into Silicon

  • Kim, Young-Sig
    • Transactions on Electrical and Electronic Materials
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    • v.2 no.2
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    • pp.32-36
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    • 2001
  • A new solid source for low temperature diffusion into silicon was developed. The source wafer consists of an “active” compound, which is sol-gel prepared phosphosilicate glass-ceramics containing 56% P$_2$O$\sub$5/, embedded in a skeletal foam-like, inert substrate. Phosphorus diffusion from the new solid sources at low temperatures (800-875$^{\circ}C$) produced reprodecible sheet resistances and shallow junctions. From a series of one hour doping runs, the life time of the phosphosilicate source was determined to be over 40 hours. The effective diffusion coefficient of phosphorus into silicon and the corresponding activation energy at 850$^{\circ}C$ were determined to be 7.5${\times}$10$\^$-15/ $\textrm{cm}^2$/sec and ∼3.9 eV, respectively.

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A New Triterpenoid Saponin from the Tropical Marine Sponge Lipastrotethya sp. (열대 해면동물 Lipastrotethya sp.에서 분리된 사포닌 화합물)

  • Eom, Tae-Yang;Lee, Yeon-Ju;Lee, Hyi-Seung
    • Ocean and Polar Research
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    • v.38 no.4
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    • pp.287-294
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    • 2016
  • Marine sponges have been a remarkably rich source of pharmacologically active and structurally diverse natural products. As a part of our continuing search for novel secondary metabolites of biomedical importance from marine invertebrate, we encountered the sponge Lipastrotethya sp. from Chuuk, Micronesia. The crude organic extract of this animal exhibited considerable cytotoxicity against the K562 cell line. Guided by the $^1H$ NMR analysis, flash chromatography of the crude extract followed by HPLC yielded a new triterpene glycoside, along with ten known saponins of the sarasinoside class. The structure of this new compound was determined by combined spectroscopic methods such as COSY, HSQC and HMBC experiment. Among these metabolites, six compounds exhibited moderate cytotoxicity against ACHN, MDA-MB-231, NCI-H23 and NUGC-3 cell lines.

Antifungal Activity of Streptomyces sp. Against Puccinia recondita Causing Wheat Leaf Rust

  • Yi, Yong-Sub;Kim, Seung-Hyun;Kim, Min-Woo;Choi, Gyung-Ja;Cho, Kwang-Yun;Song, Jae-Kyeong;Lim, Yoong-Ho
    • Journal of Microbiology and Biotechnology
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    • v.14 no.2
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    • pp.422-425
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    • 2004
  • To discover a potent strain against wheat leaf rust, soil samples collected from Ilgamho, Seoul, Korea were tested in vivo and a strain belonging to Streptomyces sp. was found to show good antifungal activity when fermented in a broth. The identification of the strain was carried out based on 16S rDNA analysis, and the active compound was separated from the fermented broth. Even though its structure was not determined completely, the authors report the results obtained so far indicate that the fermented broth of the strain showed activity against wheat leaf rust. Therefore, we propose that this may be a potential novel strain showing antifangal activity against Puccinia recondita.

A Study on the Matter of Using High Energetic Source with Environmental Pollution Reduce (환경오염을 줄이면서 고에너지원으로 이용되는 물질에 관한 연구)

  • 노기환;김준태
    • Journal of environmental and Sanitary engineering
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    • v.13 no.1
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    • pp.69-81
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    • 1998
  • The reactivity increase of unsunstituted energetic compound in cyclic ethers was found in order of three-membered cyclic form < five-membered cyclic form< four-membered cyclic form. The nucleophilicity and basicity of cyclic ethers can be explained by the negative charge on oxygen atom of cyclic ethers. The reactivity of propagation in the polymerization of cyclic ethers can be represented by positive charge on carbon atom and the LUMO energy of active species of cyclic ethers. The cationic polymerization of substituted cyclic ethers which have pendant energetic groups such as methoxy($-CH_{2}OCH_{3}$), azido($-CH_{2}N_{3}$), and nitrato($-CH_{2}ONO_{2}$) are investigated theoretically using the MNDO methods.

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Difference of Age-Related Sensitivity to Organophosphates (유기인계 농약의 연령에 따른 감수성 차이)

  • 성하정
    • Toxicological Research
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    • v.17 no.4
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    • pp.303-308
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    • 2001
  • The potential for a given anticholinesterase pesticide to exhibit age-related toxicity is essential information for an accurate and proper risk assessment of that compound. This investigation was designed to study the age-related toxicity of active metabolites of four organophosphates using in vitro detoxification measurement. The blood samples were collected from 1 month and 18 months old rats. The $IC_{50}$ values of mouse brain recombinant AChE of chlorpyrifos-oxon, diazoxon, malaoxon and paraoxon were 10.35, 112.84, 151.28 and 18.43 nM, respectively. When the plasma of young rats, and $CaCI_2$were added, the $IC_{50}$ values of mouse brain recombinant AChE of chlorpyrfos-oxon, diazoxon, malaoxon and paraoxon were 31.89, 164.25, 139.94 and 16.36 nM, respectively. The $IC_{50}$ values of mouse brain recombinant AChE of chlorpyrifos-oxon, diazoxon, malaoxon and paraoxon were changed to 136.840, 1244.45, 654.54 and 52.66 nM by A-esterases In adult rats. These results suggest that four organophosphates have a potential toxicity to exhibit age-related sensitivity.

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Utilization of Masking Techniques to Ameliorate Agricultural Odorants

  • Yoon, Young-Mo;Schilling, Mark W.;Bazemore, Russell
    • Food Science and Biotechnology
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    • v.14 no.5
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    • pp.689-693
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    • 2005
  • Different masking materials were evaluated for their ability to ameliorate odor of model poultry manure solution by assessing their effects on sensory pleasantness and odor intensity. Results indicated extracts from Eastern red cedar leaves, Loblolly pine needles', and commercial masking agents such as pine extract and odor neutralizer were effective (p<0.05) for masking odor of model poultry manure solution by increasing (p<0.05) pleasantness (82 and 86% increases in pleasantness using red cedar and pine needle extracts, respectively) and decreasing (p<0.05) odor intensity (odor intensity reduction by 66 and 76% using red cedar pine needle extract). The most odor-active compound in Loblolly pine needle extract was ${\alpha}$-terpineol (1,573.8 ug/g) which is responsible for aroma of pine trees (piney) and effective for ameliorating agricultural odors.