The inhibitory activities of 480156-S and its related compounds on prostaglandin synthetase.

1987 ◽  
Vol 90 (5) ◽  
pp. 295-302 ◽  
Author(s):  
Toshiro YAMAGUCHI ◽  
Katsumi HIROSE ◽  
Yutaka NAKAMURA ◽  
Koichi SUGENO
Keyword(s):  
Prostaglandin Synthetase ◽  
Inhibitory Activities ◽  
Related Compounds

scholarly journals Phytogrowth-Inhibitory Activities of .BETA.-Dolabrin and .GAMMA.-Thujaplicin, Hinokitiol-Related Compounds and Constituents of Thujopsis dolabrata Sieb. et Zucc. var hondai MAKINO.

2000 ◽  
Vol 23 (5) ◽  
pp. 645-648 ◽  
Author(s):  
Yoshikazu SAKAGAMI ◽  
Yoshihiko INAMORI ◽  
Nami ISOYAMA ◽  
Hiroshi TSUJIBO ◽  
Toshihiro OKABE ◽  
...  
Keyword(s):  
Inhibitory Activities ◽  
Related Compounds

scholarly journals Inhibitory activities and inhibition specificities of caffeic acid derivatives and related compounds toward 5-lipoxygenase.

1989 ◽  
Vol 37 (4) ◽  
pp. 1039-1043 ◽  
Author(s):  
Masanori SUGIURA ◽  
Youichiro NAITO ◽  
Yasunari YAMAURA ◽  
Chikara FUKAYA ◽  
Kazumasa YOKOYAMA
Keyword(s):  
Caffeic Acid ◽  
Caffeic Acid Derivatives ◽  
Inhibitory Activities ◽  
Related Compounds

Prostaglandin Activity in Sustained Inflammation of Human Skin before and after Aspirin

1977 ◽  
Vol 52 (6) ◽  
pp. 615-620 ◽  
Author(s):  
N. A. Plummer ◽  
C. N. Hensby ◽  
A. Kobza Black ◽  
M. W. Greaves
Keyword(s):  
Prostaglandin F2α ◽  
Activity Analysis ◽  
Prostaglandin Synthesis ◽  
Gas Liquid Chromatography ◽  
Prostaglandin Synthetase ◽  
Mediators Of Inflammation ◽  
Before And After ◽  
Pharmacologically Active ◽  
Related Compounds ◽  
Prior Administration

1. Pharmacologically active mediators of inflammation were obtained from suction bullae raised on normal and inflamed human abdominal skin. These contained a clear inflammatory exudate, which was analysed for known mediators of inflammation. 2. The exudates were examined for smooth muscle-contracting activity by a superfusion cascade bioassay, for prostaglandin F2α by radioimmunoassay and by Lipidex 5000 gel-partition chromatography for other prostaglandins and related compounds. 3. Tetrahydrofurfuryl nicotinate (Trafuril) was applied topically before and after systemic administration of aspirin. Trafuril alone caused a sustained inflammatory response within minutes of application, which was reduced by prior administration of aspirin (a known prostaglandin synthetase inhibitor). 4. Exudate from inflamed skin showed increased prostaglandin activity compared with exudate from contralateral non-inflamed skin. However, aspirin prevented this increase in prostaglandin activity. Analysis by thin-layer and gas—liquid chromatography further suggested that Trafuril-induced inflammation was mediated by certain prostaglandins and related compounds. 5. No evidence was obtained to suggest any change in histamine or bradykinin after Trafuril. We suggest that the response caused by Trafuril is mediated by increased synthesis of prostaglandins. Aspirin, by blocking prostaglandin synthesis, prevents or reduces the erythema.

Growth-inhibitory activities of some 1,4-naphthoquinones and related compounds on Staphylococcus aureus and Escherichia coli

1968 ◽  
Vol 14 (6) ◽  
pp. 661-666 ◽  
Author(s):  
G. J. Leahy ◽  
D. J Currie ◽  
H. L. Holmes ◽  
J. R. Maltman
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Electron Transport ◽  
Electron Transport Chain ◽  
Growth Inhibitory ◽  
Transport Chain ◽  
Half Wave ◽  
Inhibitory Activities ◽  
Related Compounds

Growth-inhibitory activities of some or all of 98 1,4-naphthoquinones and 16 related compounds on Escherichia coli and two strains of Staphylococcus aureus were determined alone or in combination. These values, when plotted against their polarographic half-wave potentials and those of their C2-n-butylthio analogs support the hypothesis that these compounds, or the products resulting from their reaction with a protein nucleophile, function by short-circuiting one or other of the quinones present in the electron-transport chain.

scholarly journals New inhibitors of methane production by rumen micro-organisms. Development and testing of inhibitors in vitro

1975 ◽  
Vol 34 (3) ◽  
pp. 429-446 ◽  
Author(s):  
J. W. Czerkawski ◽  
Grace Breckenridge
Keyword(s):  
Methane Production ◽  
Trichloroacetic Acid ◽  
Physical State ◽  
Pivalic Acid ◽  
Relative Activity ◽  
State Density ◽  
Inhibitory Activities ◽  
Micro Organisms ◽  
Related Compounds

1. A procedure is described for assaying in vitro the activity of various inhibitors of methane production by rumen micro-organisms.2. Methods of preparation of various inhibitors are described together with attempts to characterize these compounds by determining their physical properties (physical state, density, chromatographic behaviour), their hydrolysis by rumen contents and their relative potency as inhibitors.3. The results of preliminary studies with trichloroethanol and its ester with pivalic acid are given.4. The inhibitory activities of several groups of related compounds are reported. These include the polyhalogenated alcohols and their esters with pivalic acid, the esters of trihalogenated alcohols and monobasic fatty acids from C2to C16and the trihalogenated alcohol esters of dibasic acids. The results of experiments with esters of alcohols and polyhalogenated carboxylic and sulphonic acids are also given.5. It is concluded that the mechanism of action of the inhibitors might be similar to that of known polyhalogenated methane analogues (e.g. chloroform). The relative activity of various compounds might be partly governed by the ease of their absorption into the microbial cells and by the extent to which the esters can be hydrolysed by rumen contents.6. The results show that some substances are very poor inhibitors, unless they are esterified (e.g. trichloroacetic acid) but on the whole the esters in which the polyhalogen grouping is on the alcohol portion of the molecule are better inhibitors than those in which it is on the acid portion of the molecule.

scholarly journals Inhibition of staphylococcal α-toxin. The effect of aromatic polysulphonic acids on the lethal effect of α-toxin in mice

1968 ◽  
Vol 108 (1) ◽  
pp. 49-55 ◽  
Author(s):  
J. P. Arbuthnott ◽  
I. R. W. Lominski ◽  
Margaret Robson Wright
Keyword(s):  
Lethal Effect ◽  
Haemolytic Activity ◽  
Compound Viii ◽  
Test Compound ◽  
Inhibitory Activities ◽  
Related Compounds ◽  
Group 1

1. Certain aromatic polysulphonic acids, previously tested for inhibition of the haemolytic activity of staphylococcal α-toxin, together with some additional related compounds, were tested as possible inhibitors of α-toxin in mice. 2. Compounds that inhibited the haemolytic activity of α-toxin at concentrations of 0·16mm or less [compounds (I), (II), (IV), (V), (VII) and (VIII)] were found to inhibit the lethal effect of α-toxin. 3. With the exception of compound (VIII), amounts of 1mg. were required to inhibit 4 LD50 of toxin when the test compounds were premixed with α-toxin before injection; comparable inhibition with 0·3mg. of compound (VIII) was achieved without prolonged premixing. 4. Mixtures of α-toxin and compounds (I) and (II) containing an excess of test compound showed markedly diminished inhibitory activities. 5. The ‘half-molecule’ analogues of group 1 [compounds (III) and (XVIII)] were non-inhibitory. 6. Compounds (I)–(V), when administered separately from α-toxin by the same route (intraperitoneal), were active only when injected almost simultaneously with toxin, whereas compounds (VII) and (VIII) were strikingly inhibitory when injected 15min. before or after the toxin. 7. Compound (VIII) failed to inhibit the lethal effect of α-toxin when injected by a different route (intravenous).

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