• 제목/요약/키워드: inhibitory compound

검색결과 1,014건 처리시간 0.027초

Nitric Oxide and PGE$_2$ production Inhibitory Activities of Phenolic Compounds from Sophora japonica Linne

  • Kim, Hyun-Jung;Sim, Jae-Geul;Yeom, Seung-Hwan;Kim, Min-Kee;Lee, Jae-Hee;Lee, Min-Won
    • 대한약학회:학술대회논문집
    • /
    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
    • /
    • pp.193.2-193.2
    • /
    • 2003
  • Phytochemical examination of Sophorae Fructus yielded six phenolic compounds. The structures were elucidated as genistein(1), genistin(2) and genistein 7-O-${\alpha}$- L-rhamnopyranoside(3) by phytochemical and spectral evidences. The other compounds(4, 5, 6) are understudied by 2D-NMR. Nitric Oxide and PGE$_2$ production inhibitory activities in INF-${\gamma}$, LPS stimulated RAW 264.7 cell were examined. Compound 2 and 4 showed significant nitrogen monoxide(NO) production inhibitory activity in IFN-${\gamma}$, LPS stimulated RAW 264.7 cell. (omitted)

  • PDF

Inhibitory Effect of Spirodela Polyrhiza on the Mast Cell-Mediated Immediate Hypersensitivity

  • Kim Young Hee;Ko Woo Shin
    • 동의생리병리학회지
    • /
    • 제18권3호
    • /
    • pp.919-923
    • /
    • 2004
  • Spirodela polyrhiza(L.) Schleid (Lemnaceae) have been used as a traditional drug in treating urticaria and itching. However, the exact role of Spirodela polyrhiza in allergic reaction has not been clarified yet. Type 1 hypersensitivity (immediate hypersensitivity), popularly known as allergy, is a major clinical problem in humans. It has been found that the histamine release from mast cells is an essential step in the pathological process of immediate hypersensitivity. In the present study, the effect of aqueous extract of Spirodela polyrhiza (AESP) on immediate hypersensitivity was investigated. AESP inhibited the antigen-induced passive cutaneous anaphylaxis (PCA). AESP in vitro exhibited a dose-dependent inhibition of degranulation in RPMC stimulated by compound 48/80. AESP also suppressed the morphological changes and the increase of intracellular free calcium level induced by compound 48/80. These results suggest that inhibitory effect of AESP on immediate hypersensitivity may be mediated through the decrease of intracellular free calcium levels, and AESP importantly contributes to the treatment of anaphylaxis and may be useful for other allergic disease.

Isolation of Intestinal Glucose Uptake Inhibitor from Punica granatum L.

  • Kim, Hye-Kyung;Baek, Soon-Sun;Cho, Hong-Yon
    • Preventive Nutrition and Food Science
    • /
    • 제16권2호
    • /
    • pp.135-141
    • /
    • 2011
  • Inhibition of intestinal glucose uptake is beneficial in reducing the blood glucose level for diabetes. To search for an effective intestinal glucose uptake inhibitor from natural sources, 70 native edible plants, fruits and vegetables were screened using Caco-2 cells and fluorescent D-glucose analog 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl) amino]-2-deoxy-D-glucose (2-NBDG). A compound that was able to inhibit glucose uptake was isolated from methanol extract of Punica granatum L. and called PG-1a. PG-1a appears to be a phthalic acid-diisononyl ester- like compound (PDE) with molecular weight of 418. The inhibitory effect of PG-1a on intestinal glucose uptake was dose-dependent with 89% inhibition at $100\;{\mu}g$/mL. Furthermore, the intestinal glucose uptake inhibitory effect of PG-1a was 1.2-fold higher than phlorizin, a well known glucose uptake inhibitor. This study suggests that PG-1a could play a role in controlling the dietary glucose absorption, and that PG-1a can effectively improve the diabetic condition, and may be used as an optional therapeutic and preventive agent.

肛腸療法에 의한 辛蒲湯의 抗아나필락시 效果 (Antianaphylactic Effect of Sinpo-tang by Anal Therapy)

  • 이종범;문석재;문구;원진희;김태균;배남규
    • 한방안이비인후피부과학회지
    • /
    • 제14권1호
    • /
    • pp.240-249
    • /
    • 2001
  • Objective : Anal Therapy is another way of taking medicine and applies to each field of clinical treatment extensively. Sinpo-tang(SPT) has been used for the treatment of a allergic rhinitis. In this study, the auther investigated the anti anaphylactic action of Sinpo-tang by anal therapy was investigated on cutaneous allergic reaction models. Methods : Results : 1. Sinpo-tang (0,001-0.1 g/kg) dose-dependently inhibited the compound 48/80-induced ear swelling response in mice. Inhibitory effect of Sinpo-tang was significant (P < 0.05) at the doses of 0.01, 0.1 g/kg. 2. Sinpo-tang (0.001-0.1 g/kg) inhibited the cutaneous allergic reaction activated by anti-dinitrophenyl IgE in rats. Of special note, Sinpo-tang (0.1 g/kg) inhibited the cutaneous allergic reaction by $68\%$. 3. This inhibitory effect of Sinpo-tang was confirmed by observation of alcian blue/nuclear fast red stained-mast cells in the cutaneous tissue. 4. Sinpo-tang (0.01-1 g/L) dose-dependently inhibited the compound 48/80-induced histamine release from the peritoneal mast cells. Conclusions :These results indicate that anal therapy of Sinpo-tang may be beneficial in the treatment of mast cell-mediated anaphylaxis by inhibition of histamine release from mast cells in vivo and in vitro.

  • PDF

Cytotoxic and Antimicrobial Activities of Bioactive Monoterpenophenols

  • Oh In Kio;Lee Hyun Ok;Ahn Jong Woong;Kim Hyung Min;Shin Ji Hee;Lim Jin A;Chun Hyun Ja;Baek Seung Hwa
    • 동의생리병리학회지
    • /
    • 제16권6호
    • /
    • pp.1270-1276
    • /
    • 2002
  • Compounds 1 - 12 were tested for their growth inhibitory effects against tumor cell lines using two different 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) and sulforhodamine B protein (SRB) assays and antimicrobial activity. The cytotoxic activity of methyl-4-[{(2E)-3,7-dimethyl-2,6-octadienyl}oxy]-3-methoxy benzoate (1) exhibit more active than that of 5-fluorouracil (11) on human oral epithelioid carcinoma (KB, ATCC No. OCL 17) cell lines. But this compound (1) on human skin melanoma (SK-MEL-3, HBT 69) cell lines shows less active than that of adriamycin (12). However, compound 9 showed the antimicrobial activity against S. epidermidis (MIC, 15.625 ㎍/㎖), S. aureus, C. albicans (MIC, 31.25 ㎍/㎖), S. mutans, S. typhimurium, P. putida (MIC. 125 ㎍/㎖) and P. aeruginosa (MIC, 500 ㎍/㎖).

Salmonella 실험계에서 케일즙액의 항돌연변이의 효과와 활성획분 (Antimutagenic Effect and Active Compound Analysis of Kale Juice in Salmonella Assay System)

  • 이선미;박건영;이숙희
    • 한국식품영양과학회지
    • /
    • 제26권5호
    • /
    • pp.965-971
    • /
    • 1997
  • Antimutagenic effects of kale juice on the mutagenicity induced by $B_{1}(AFB_{1})$ N-methyl-N'-N-nitrosoguanidine(MNNG) in Salmonella assay system were studied. The freeze dried kale juice significantly reduced the mutagenicity induced by $AFB_{1}$ in Salmonella typhimurium TA100 and TA98. However, the kale juice exhibited less inhigbitory effect on the mutagenicity induced by MNNG as the concentrations of the juice sample increased. Also, kale juice after dialysis (>12,000, Mw) appeared to have 42.3∼89.5% of inhibitory effects against $AFB_{1}$, however, the dialyzate did not show any inhibitory effect against MNNG. To separate and identify the antimutagenic compounds from the kale juice, the dialyzates were further fractioned by using Sepharose CL-6B-200 gel filtration. Fraction number 13 showed the strong antimutagenic activity against $AFB_{1}$, and the fraction exhibited positive results of a characterized colour reactions of protein, carbohydrate and phenolic compound. Therefore, one of the possible active compounds from the kale juice was supposed to a glycoprotein(Mw. 270,000) which seemed unstable with heating.

  • PDF

Quercitrin Gallate Down-regulates Interleukin-6 Expression by Inhibiting Nuclear Factor-kB Activation in Lipopolysaccharide-stimulated Macrophages

  • Min, Kyung-Rak;Kim, Byung-Hak;Chang, Yoon-Sook;Kim, Young-Soo
    • Natural Product Sciences
    • /
    • 제12권2호
    • /
    • pp.113-117
    • /
    • 2006
  • Quercitrin gallate was previously isolated from Persicaria lapathifolia (Polygonaceae) as an inhibitor of superoxide production. In the present study, quercitrin gallate was found to inhibit interleukin (IL)-6 production in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 with an $IC_{50}$ value of $63\;{\mu}M$. Furthermore, quercitrin gallate attenuated LPS-induced synthesis of IL-6 transcript but also inhibited LPS-induced IL-6 promoter activity, indicating that the compound could down-regulate IL-6 expression at the transcription level. Since nuclear factor (NF)-kB has been shown to play a key role in LPS-inducible IL-6 expression, an effect of quercitrin gallate on LPS-induced NF-kB activation was further analyzed. Quercitrin gallate exhibited a dosedependent inhibitory effect on LPS-induced nuclear translocation of NF-kB without affecting inhibitory kB (IkB) degradation, and subsequently inhibited LPS-induced NF-kB transcriptional activity in macrophages RAW 264.7. Taken together, quercitrin gallate down-regulated LPS-induced IL-6 expression by inhibiting NF-kB activation, which could provide a pharmacological potential of the compound in IL-6-related immune and inflammatory diseases.

Amentoflavone의 아라키돈산 유리효소인 phopholipase $A_2$에 대한 저해활성 및 비만세포에서 histamine 유리 억제효과 (Inhibitory Activity of Amentoflavone on Arachidonic Acid Releasing Enzyme, Phopholipase $A_2$ and Inhibition of Histamine Release from Mast Cells)

  • 문태철;이은경;이승호;손건호;김현표;강삼식;장현욱
    • 생약학회지
    • /
    • 제33권1호통권128호
    • /
    • pp.49-52
    • /
    • 2002
  • Amentoflavone, naturally occurring biflavonoid, isolated from the leaves of Ginko biloba, selectively inhibited human seceretory phospholipase $A_2$. This compound potently and irreversibly inhibited human group IIA in a dose dependent manner with an $IC_50$ about $3\;{\mu}M$. Amentoflavone inhibited phospholipase $A_2$ by a noncompetitive manner with the apparent Ki value of $1{\times}10^{-5}M$. In addition, the inhibitory activity of amentoflavone is rather specific against group IIA phospholipase $A_2$ than group IB phospholipase $A_2$. Furthermore, this compound strong inhibit histamine release from $A_{23187}$ treated rat peritoneal mast cells. These results indicate naturally occurring biflavonoid represents a novel anti-inflammatory agent.

Topoisomerase I and II Inhibitory Activities and Cytotoxic Constituents from the Barks of Tilia amurnesis

  • Piao, Dong Gen;Lee, You-Jeong;Seo, Chang-Seob;Lee, Chong-Soon;Kim, Jae-Ryong;Chang, Hyun-Wook;Son, Jong-Keun
    • Natural Product Sciences
    • /
    • 제17권3호
    • /
    • pp.245-249
    • /
    • 2011
  • Eight compounds, squalene (1), friedelin (2), ${\beta}$-sitosterol (3), ${\beta}$-sitosterol-3-O-glucoside (4), ${\alpha}$-tocopherol (5), betulinic acid (6), trilinolein (7) and 1-O-(9Z,12Z-Octadecadienoyl)-3-nonadecanoyl glycerol (8), were isolated from the barks of Tilia amurensis. Their chemical structures were identified by comparing their physicochemical and spectral data with those published in the literature. These isolated compounds were examined for their inhibitory activities against topoisomerase I and II. Compound 7 showed significant inhibition of DNA topoisomerase I and II activities, with percent decreases in activity of 87 and 95%, respectively at a concentration of $100\;{\mu}M$. Compound 6 exhibited cytotoxicity against the human colon adenocarcinoma cell line (HT-29), the human breast adenocarcinoma cell line (MCF-7) and the human liver hepatoblastoma cell line (HepG-2), with $IC_{50}$ values of 20, 59 and $16\;{\mu}M$, respectively.

2-클로로메틸-5-(2-Phenylthiazol-4-yl)-1,3,4-옥사디아졸의 새로운 4급 암모늄염의 합성과 계면활성도 (Synthesis and Surface Activity of New Quaternary Ammonium Salts Prepared from 2-Chloromethyl-5-(2-Phenylthiazol-4-yl)-1,3,4-Oxadiazole)

  • 배선건;연영흠
    • 공업화학
    • /
    • 제17권3호
    • /
    • pp.286-290
    • /
    • 2006
  • 새로운 4급 염화 암모늄염, {alkyldimethyl-[5-(2-phenylthiazol-4-yl]-1,3,4-oxadiazol-2-ylmethyl]quaternary ammonium chlorides (ADOQACs): 6}을 화합물 5와 몇 가지 N,N-dimethylalkyl amine을 반응시켜 합성하였다. 합성한 화합물들의 구조와 물리적 특성을 조사하였고 계면활성을 측정하였다. 화합물 6의 표면장력($\gamma_{cmc}$)과 최소저해농도(MIC)는 알킬기의 영향을 받은 것으로 나타났으며, 특히 화합물 6c와 6d가 좋은 항균력과 계면활성을 보였다.