1,720,977 research outputs found
Pharmacological characterization of new compounds and herbal derivatives for pain and inflammation treatment
Full text linkIntroduction: Despite the availability of several analgesic and anti-inflammatory options, the effective treatment of pain and inflammation is still a challenge for clinicians, and the balance between efficacy and safety aspects remains both crucial and difficult. Thus, the identification of new potential targets which may affect pain and inflammatory processes is becoming an urgent clinical and therapeutic need. This scientific project derives from a close collaboration with various national and foreign research groups, in order to establish an efficient and highly multidisciplinary approach to investigate the pharmacological profile of new compounds and herbal derivatives with significant antinociceptive and antinflammatory effects to be used for the treatment of pain and inflammation.
Materials and Methods: The research approach involves the in vivo studies of natural (ammonium glycyrrhizinate; rubiscolin-6 and soymorphin-6) and non-natural compounds (C-terminal amides derivatives of rubiscolin-6 and soymorphin-6; six analogues of endomorphin-2 and DAPEA; two compounds obtained in silico studies; a series of lonidamine with high CB1 receptor affinity and new pH-sensitive formulation of niosomes containing Polysorbate 20 derivatized by Glycine and loaded with ibuprofen) using murine models of pain and inflammation. All experiments were carried out using male CD-1 mice weighing 25 g.
Results: The results suggest the potential use of ammonium glycyrrhizinate for clinical treatment of pain and/or inflammatory-related diseases, included diabetic peripheral neuropathy. The results obtained by in vivo studies testing two natural compounds, rubiscolin-6 and soymorphin-6, and their C-terminal amides derivatives, show that rubiscolin-6 was able to increase the nociceptive threshold to thermal stimuli after supraspinal administration, but was ineffective after subcutaneous administration, in an experimental paradigm of chemical-induced nociception as the formalin test. On the other hand, instead, its derivatives (rubiscolin-6 C-amide) centrally administered demonstrates a strong antinociceptive effect higher than rubiscolin-6, and it is effective after subcutaneous administration. Both soymorphin-6 and its derivative soymorphin-6 C-amide induced a robust antinociceptive effect after central administration in tail flick test but both peptides have not been able to change the behavioral response to chemical-induced nociception in the formalin test. The in vivo antinociceptive profile of new six tetrapeptide models containing α-amino-γ-lactam of Freidinger in position 2 and 3, as analogues of endomorphin-2 (EM-2) and DAPEA, revealed that one of them (peptide A2D) exhibited a strong antinociceptive effect in vivo after intracerebroventricular administration, performing better than the parent compounds EM-2 and DAPEA. Peptide A3D is also able to produce antinociceptive effect both in the acute and in the inflammatory phase of the formalin test. The in vivo results obtained from two compounds (tripeptides 6 and 11) derived from previous in silico studies revealed their ability to induce an antinociceptive effect after intracerebroventricular and subcutaneous administrations in the tail flick and formalin tests, respectively. Subsequently, it was analyzed the in vivo orexant/anorexant and antinociceptive profile of a series of lonidamine joined Leu-, tert/Leu- and Val-amino acids with different C-terminal functional groups (LONI 1-4,11) as novel compounds with high CB1 receptor affinity and selectivity with different biological activity depending on the C-terminal substitution and amino acid residues and endowed with activities. The results demonstrated that LONI2 and LONI4 were able to inhibit food intake (anorexant effect) consistent with an inverse agonism at CB1 receptors. On the other hand, LONI11, an agonist towards cannabinoid receptors CB1 and CB2, proved to carry out a significant orexant an antinociceptive effect at the central and periphery levels. Finally, a new pH-sensitive formulation of niosomes containing Polysorbate 20 derivatized by Glycine and loaded with ibuprofen (NioIbu) was in vivo tested, using models of pain and inflammation. The results demonstrated that NioIbu, administered 2h before testing, reduced nociception, whereas the free form of ibuprofen was ineffective.
Conclusion: In conclusion, these findings create prospects for conducting clinical studies with the compounds presented, which show in fact their effectiveness for chronic pain and inflammation control
A novel identification system for potentially counterfeit medical devices based on the visual analysis through evaluation sheet .
No full textBackground. The counterfeiting of medical devices has been a growing problem for several years, especially since the extension of the internet. Regulatory authorities are responsible, in collaboration with relevant national and international stakeholders, for establishing mechanisms to detect falsified products circulating in their territories and for removing them from the market. Thus it might be useful develop a simple and affordable preliminary screening methods to be used by inspectors to decide in the field whether to collect a sample for further laboratory analysis or not. We here report a new method to compare the physical appearances of suspected samples with those of known genuine products based on the new regulation 2017/745 on medical devices.
Methods. According to the new Regulation (EU) 2017/745 on medical devices, we have collected all the requirements regarding the information supplied with the device, including: qualitative composition of the device and quantitative information on the main constituent or constituents responsible for achieving the principal intended action, the labeling and packaging and the CE marking of conformity. Thanks to these pieces of information, along with those concerning the physical characteristics of the product, permit us to compare the potentially counterfeit medical devices with the known genuine products.
Results. We developed a new and quick method to provide evidence that the sample comes from a falsified product. We have designed a table (Table 1) containing a list of questions to ask yourself to compare potentially counterfeit medical device with the known genuine products. The questions include the visual analysis of packaging and the information reported on the package (Does it reflect the appearance of the original form and colour? Is the packaging size the same as the original? Is this system homologous to the original? Do the information on the packaging reflect the appearance of the original colour and form?...), including qualitative and quantitative information (Since it is a substance-based medical device, is the overall qualitative composition of the device reported? Does this match that of its original counterpart?...), the presence and the conformity of CE marking (Is there an EC marking? Is the marking clear, legible and indelible?...) and the physical analysis of the characteristics of the product (Do they all have the same shape if they are tablets/capsules? Do all tablets/capsules have the same size among them and compared to the original? Do all the tablets have the same type of surface coating?...).The questions provide a simple yes or no answer.
Conclusions. Visual analysis is an important part of the inspection process in the pharmaceutical industry. Falsified medical devices may be identified from this simple and quick method
Ammonium glycyrrhizinate prevents apoptosis and mitochondrial dysfunction induced by high glucose in SH-SY5Y cell line and counteracts neuropathic pain in streptozotocin-induced diabetic mice
No full textGlycyrrhiza glabra, commonly known as liquorice, contains several bioactive compounds
such as flavonoids, sterols, triterpene, and saponins; among which, glycyrrhizic acid, an oleananetype saponin, is the most abundant component in liquorice root. Diabetic peripheral neuropathy
is one of the major complications of diabetes mellitus, leading to painful condition as neuropathic
pain. The pathogenetic mechanism of diabetic peripheral neuropathy is very complex, and its
understanding could lead to a more suitable therapeutic strategy. In this work, we analyzed the
effects of ammonium glycyrrhizinate, a derivate salt of glycyrrhizic acid, on an in vitro system,
neuroblastoma cells line SH-SY5Y, and we observed that ammonium glycyrrhizinate was able to
prevent cytotoxic effect and mitochondrial fragmentation after high-glucose administration. In an
in vivo experiment, we found that a short-repeated treatment with ammonium glycyrrhizinate was
able to attenuate neuropathic hyperalgesia in streptozotocin-induced diabetic mice. In conclusion,
our results showed that ammonium glycyrrhizinate could ameliorate diabetic peripheral neuropathy,
counteracting both in vitro and in vivo effects induced by high glucose, and might represent a
complementary medicine for the clinical management of diabetic peripheral neuropathy
Polypharmacy and Nutraceuticals in veterans: 1 partners in crime?
No full textMulti-morbidity and resulting polypharmacy are very common in veterans and represent a clinical patient safety issue. In fact, if on one hand a suitable polypharmacy can extend life expectancy and maintain the quality of life, on the other hand it can be associated with a high probability of prescribing a potentially detrimental drug. The most worrisome consequence of polypharmacy is the occurrence of therapeutic failures, adverse drug withdrawal events and drug-drug interactions. Despite the efficacy of herbal preparations and nutraceuticals remains controversial, users who are in favor of personal health control often have strong beliefs that herbal preparations and dietary supplements are natural and with fewer side effects. Actually, US data indicate that potential interactions can occur in case of co-administration of drugs and herbal/nutritional supplements or mineral-fortified foods and fruit juices. Veterans who receive primary care in the Veterans Affairs health system have a high burden of chronic disease, with a high prevalence of cardiovascular diseases and clinical risk factors, such as obesity. Facilitating healthy diets, physical activity and weight management in the veteran population is an important public health challenge. Although the Mediterranean Pyramid could be the basis for integrative medicine for veterans with disabilities, patient-centred and interprofessional approaches (including physical medicine and rehabilitation clinicians, pharmacologists and nutritionists) and interventions are needed in order to prevent malnutrition, self-prescription of CAM and food-drug and/or nutraceutical-drug interactions and to achieve optional rehabilitation
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Variations on the Author
Full text link“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
Appropriate Similarity Measures for Author Cocitation Analysis
Full text linkWe provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
Dispelling the Myths Behind First-author Citation Counts
Full text linkWe conducted a full-scale evaluative citation analysis study of scholars in the XML research field to explore just how different from each other author rankings resulting from different citation counting methods actually are, and to demonstrate the capability of emerging data and tools on the Web in supporting more realistic citation counting methods. Our results contest some common arguments for the continued
use of first-author citation counts in the evaluation of scholars, such as high correlations between author rankings by first-author citation counts and other citation
counting methods, and high costs of using more realistic citation counting methods that are not well-supported by the ISI databases. It is argued that increasingly available digital full text research papers make it possible for citation analysis studies to go beyond what the ISI databases have directly supported and to employ more
sophisticated methods
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