THE INHIBITORY EFFECT OF PROPOLIS AND CAFFEIC ACID PHENETHYLESTER ON CYCLOOXYGENASE ACTIVITY IN J774 MACROPHAGES.

The effect of an ethanolic extract of propolis, with and without CAPE, and some of its components on cyclooxygenase (COX-1 and COX-2) activity in J774 macrophages has been investigated. COX-1 and COX-2 activity, measaured as prostaglandin E-2 (PGE(2)) production, were concentration-dependently inhibited by propolis (C x 10(-3)-3 x 10(2) mugml(-1)) with an IC50 of 2.7 mugml(-1) and 4.8 x 10(-2) mugml(-1), respectively. Among the compounds tested pinocembrin and caffeic, ferulic, cinnamic and chlorogenic acids did not affect the activity of COX isoforms. Conversely, CAPE (2.8 x 10(-4)-28 mugml(-1); 10(-9)-10(-4) M) and galangin (2.7 x 10(-4)-27 mugml(-1); 10(-9)-10(-4) M) were effective, the last being about ten-twenty times less potent. In fact the IC50 of CAPE for COX-1 and COX-2 were 4.4 x 10(-1) mugml(-1) (1.5 x 10(-6) M) and 2 x 10(-3) mugml(-1) (6.3 x 10(-9) M), respectively. The IC50 of galangin were 3.7 mugml(-1) (15 x 10(-6) M) and 3 x 10(-2) mugml(-1) (120 x 10(-1) M), for COX-1 and COX-2 respectively. To better investigate the role of CAPE, we tested the action of the ethanolic extract of propolis deprived of CAPE, which resulted about ten times less potent than the extract with CAPE in the inhibition of both COX-1 and COX-2, with an IC50 of 30 mugml(-1) and 5.3 x 10(-1) mugml(-1), respectively. Moreover the comparison of the inhibition curves showed a significant difference (p < 0.001). These results suggest that both CAPE and galangin contribute to the overall activity of propolis, CAPE being more effective

Drones Classification by the Use of a Multifunctional Radar and Micro-Doppler Analysis

The classification of targets by the use of radars has received great interest in recent years, in particular in defence and military applications, in which the development of sensor systems that are able to identify and classify threatening targets is a mandatory requirement. In the specific case of drones, several classification techniques have already been proposed and, up to now, the most effective technique was considered to be micro-Doppler analysis used in conjunction with machine learning tools. The micro-Doppler signatures of targets are usually represented in the form of the spectrogram, that is a time–frequency diagram that is obtained by performing a short-time Fourier transform (STFT) on the radar return signal. Moreover, frequently it is possible to extract useful information that can also be used in the classification task from the spectrogram of a target. The main aim of the paper is comparing different ways to exploit the drone’s micro-Doppler analysis on different stages of a multifunctional radar. Three different classification approaches are compared: classic spectrogram-based classification; spectrum-based classification in which the received signal from the target is picked up after the moving target detector (MTD); and features-based classification, in which the received signal from the target undergoes the detection step after the MTD, after which discriminating features are extracted and used as input to the classifier. To compare the three approaches, a theoretical model for the radar return signal of different types of drone and aerial target is developed, validated by comparison with real recorded data, and used to simulate the targets. Results show that the third approach (features-based) not only has better performance than the others but also is the one that requires less modification and less processing power in a modern multifunctional radar because it reuses most of the processing facility already present

From Phytocannabinoids to Cannabinoid Receptors and Endocannabinoids: Pleiotropic Physiological and Pathological Roles Through Complex Pharmacology

Apart from having been used and misused for at least four millennia for, among others, recreational and medicinal purposes, the cannabis plant and its most peculiar chemical components, the plant cannabinoids (phytocannabinoids), have the merit to have led humanity to discover one of the most intriguing and pleiotropic endogenous signaling systems, the endocannabinoid system (ECS). This review article aims to describe and critically discuss, in the most comprehensive possible manner, the multifaceted aspects of 1) the pharmacology and potential impact on mammalian physiology of all major phytocannabinoids, and not only of the most famous one Δ9-tetrahydrocannabinol, and 2) the adaptive pro-homeostatic physiological, or maladaptive pathological, roles of the ECS in mammalian cells, tissues, and organs. In doing so, we have respected the chronological order of the milestones of the millennial route from medicinal/recreational cannabis to the ECS and beyond, as it is now clear that some of the early steps in this long path, which were originally neglected, are becoming important again. The emerging picture is rather complex, but still supports the belief that more important discoveries on human physiology, and new therapies, might come in the future from new knowledge in this field

A new tissue acquisition technique in pancreatic cystic neoplasm: endoscopic ultrasound-guided through-the-needle forceps biopsy

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Antinociceptive effects of tetrazole inhibitors of endocannabinoid inactivation: Cannabinoid and non-cannabinoid receptor-mediated mechanisms

Background and purpose: Tetrazoles were recently developed as inhibitors of the cellular uptake of the endocannabinoid anandamide or of its hydrolysis by fatty acid amide hydrolase (FAAH), but were proposed to act also on non-endocannabinoid-related serine hydrolases. Experimental approach: We tested, in a model of inflammatory pain induced in mice by formalin, five chemically similar inhibitors: (i) OMDM119 and OMDM122, two potent carbamoyl tetrazole FAAH inhibitors with no effect on anandamide uptake; (ii) LY2183240, a carbamoyl tetrazole with activity as both FAAH and uptake inhibitor; (iii) OMDM132, a non-carbamoyl tetrazole with activity only as uptake inhibitor and iv) OMDM133, a non-carbamoyl tetrazole with no activity at either FAAH or uptake. Results: All compounds (2.5-10 mg kg -1, i.p.) inhibited the second phase of the nocifensive response induced by intraplantar injection of formalin. The effects of OMDM119, OMDM122 and OMDM133 were not antagonized by pretreatment with cannabinoid CB 1 receptor antagonists, such as rimonabant or AM251 (1-3 mg kg -1, i.p.). The effects of LY2183240 and OMDM132 were fully or partially antagonized by rimonabant, respectively, and the latter compound was also partly antagonized by the CB 2 receptor antagonist, AM630. Conclusions and implications: (i) non-FAAH hydrolases might be entirely responsible for the antinociceptive activity of some, but not all, tetrazole FAAH inhibitors, (ii) the presence of a carbamoylating group is neither necessary nor sufficient for such compounds to act through targets other than FAAH and (iii) inhibition of anandamide uptake is responsible for part of this antinociceptive activity, independently of effects on FAAH. © 2008 Macmillan Publishers Limited All rights reserved