Search results for "Mace"
showing 10 items of 4713 documents
Synthesis and Evaluation of a Novel Series of Pyrrolizine Derivatives as Dual Cyclooxygenase-1 and 5-Lipoxygenase Inhibitors
1997
The aim of our study was to investigate structure activity relationship following the replacement of the 6-phenyl substituent at the 6,7-diaryl-2,3-dihydropyrrolizine template by various heteroaromatic residues. In this context we developed a new, efficient, and highly sensitive test method for the screening of dual cyclooxygenase-1 (COX-1) and 5-lipoxygenase (5-LOX) inhibitors. We used human platelets as a source of COX-1 and human PMNLs as a source of 5-LOX. Both cell types were isolated from the same volume of blood. PGE2 and LTB4 respectively were determined by highly selective and sensitive ELISA kits, using monoclonal antibodies. For a single determination at most 0.5 mL whole blood i…
In-vitro and Ex-vivo Inhibition of Blood Platelet Aggregation by Naftazone
1996
Abstract Because of the considerable interest in the role of platelets and antiplatelet therapy in cardiovascular disease, including the aggregation of platelets to each other during arterial thrombosis and atherogenesis, we have studied the effect of naftazone (Etioven), an original vasculotropic drug on platelet aggregation. Rat and human platelets were prepared and incubated in-vitro with different concentrations of naftazone. We found that naftazone inhibited both platelet secretion and aggregation in platelet-rich plasma (PRP) and washed platelets after stimulation with thrombin or ADP. Rats were also treated intraperitoneally for five days with various naftazone doses (0.125-10 mg kg−…
Non-steroidal Anti-inflammatory Agents, Part 19:E-2-Pyrrolizin-5-yl Acrylic Acids as Potent Dual or Selective Inhibitors of Bovine Cyclooxygenase and…
1995
The pyrrolizinyl substituted acrylic acid derivatives represent another class of dual and selective inhibitors of cyclooxygenase and 5-lipoxygenase. By modifying their substitution pattern at the phenyl moiety of C-6 the balance between the activity against cyclooxygenase and against 5-lipoxygenase can be shifted. Structure-activity relationships are discussed. Compound 6k is the most potent and well-balanced dual inhibitor of both enzymes, while the highest selectivity of lipoxygenase inhibition was found for 6j. The activity and selectivity of compounds with an additional sulfur moiety depend on the oxidation status of this atom, giving an indication of the discussed coupling between pero…
Inhibition of inflammatory responses by epitaondiol and other marine natural products
1995
The marine metabolites pacifenol, stypotriol triacetate and epitaondiol were tested for their effects on a number of inflammatory responses. Epitaondiol exhibited a potent topical anti-inflammatory activity related to inhibition of leukocyte accumulation. The other compounds showed a lower potency, similar to that of indomethacin. None of the compounds affected superoxide generation by human neutrophils but pacifenol effectively inhibited the degranulation response. This compound and epitaondiol decreased the release of eicosanoids with a higher potency on the cyclo-oxygenase pathway. Only epitaondiol inhibited human recombinant synovial phospholipase A2 activity in a concentration-dependen…
Influence of traditional Chinese anti-inflammatory medicinal plants on leukocyte and platelet functions.
2003
Abstract The enzymes 5-lipoxygenase and elastase are therapeutic targets in dermatological disorders such as psoriasis. Fifteen extracts from traditional Chinese medicinal plants used to treat topical inflammations were screened for their inhibitory effect on lipoxygenase, cyclooxygenase and elastase activity in intact leukocytes and platelets. Astragalus membranaceus, Forsythia suspensa and Poria cocos inhibited 5-lipoxygenase, with IC50 values of 141, 80 and 141 μg mL−1, respectively. The latter two species, along with Angelica dahurica and Angelica pubescens, also inhibited elastase (IC50 values of 80, 123, 68 and 93 μg mL−1, respectively), while A. pubescens, Atractylodes macrocephala, …
Spectrofluorimetric Quantification of Malondialdehyde for Evaluation of Cyclooxygenase-1/Thromboxane Synthase Inhibition
1999
The in vitro assay developed by Hartmann and Ledergerber (1995) utilizing the spectrofluorimetric quantification of malondialdehyde after reaction with thiobarbituric acid was modified and used for further investigations. The human whole blood was replaced by a platelet suspension of pig blood, and calcium ionophore A23187 was used instead of collagen for inducing the arachidonic acid cascade. The modified assay represents a simple, time and cost saving method for the evaluation of cyclooxygenase-1/thromboxane synthase inhibition. The reproducibility and comparability of results is given. Additional experiments allow classification of selective phospholipase A2, cyclooxygenase-1, and thromb…
Griffonianone D, an isoflavone with anti-inflammatory activity from the root bark of Millettia griffoniana.
2003
A new isoflavone, griffonianone D (1), and the previously known compounds durmillone and odorantin were isolated from a chloroform extract of the root bark of Millettia griffoniana. The structure of 1 was established as (7E)-(6",7"-dihydroxy-3",7"-dimethyloct-2"-enyl)oxy-4'-methoxyisoflavone on the basis of its spectral data. The chloroform extract of the root bark of M. griffoniana and compound 1 showed anti-inflammatory effects in different experimental models of inflammation.
A Method to Evaluate Chewing Efficiency in Infants Through Food Bolus Characterization: A Preliminary Study
2015
Chewing skills develop greatly during the two first years of life, but the evolution of masticatory efficiency has never been directly measured so far. A bottleneck for such study is the difficulty in using the chew-and-spit method with infants and very young children. Herein, we propose a new method based on a model gel enclosed in a food feeder, which has been assessed with adult subjects. Subjects chewed and compressed the gel either alone or enclosed in two different feeders. Analysis of the number of particles and particle area distribution revealed that one feeder,made from silicone teat, interfered with bolus breakdown. However, similar results were observed between experiments in a …
Chemical Composition of the Essential Oils of Three Species of the Apiaceae Family Growing Wild in Sicily: Bonannia graeca, Eryngium maritimum and Op…
2013
n the present study the chemical composition of the essential oils from aerial parts of Bonannia graeca (L.) Halácsy and Opopanax chironium (L.) Kock, and from aerial parts and roots of Eryngium maritimum L. was evaluated by GC and GC-MS. α-Pinene (15.2%) and β-pinene were recognized as the main constituents of B. graeca, whereas the aerial parts of O. chironium contained mainly the diterpene cembrene and the coumarin angelicin. In both aerial parts and roots of E. maritimum germacrene D (10.4% and 15.9%, respectively) and 2,4,5-trimethylbenzaldehyde (8.3% and 6.7%) were the most abundant components
SPECTRAL COMPOSITION OF EATING SOUNDS GENERATED BY CRISPY, CRUNCHY AND CRACKLY FOODS
1995
Separate air and bone conducted food sounds generated by six subjects biting into eight foods were recorded and analysed by a fast Fourier transform (FFT) signal analyser. A panel of 60 subjects classified the 8 foods according to their texture: crispy, crunchy and crackly and these textural characteristics were described by spectral characteristics of biting sounds. Crispy foods (such as extruded flat breads) were found to generate high pitched sounds that show a high level of frequencies higher than 5 kHz, especially for air conduction. Crunchy foods (such as raw carrot) generate low pitched sounds with a characteristic peak on frequency range 1.25 to 2 kHz for air conduction. And crackly…