A New Bi-Functional Derivative of Polyethylene Glycol as Molecular Carrier for Eugenol and Ibuprofen

Eugenol (EU) and ibuprofene (IBU) were covalently bound to a bi-functionalized PEG, used as molecular carrier of drugs and the release kinetics of the two bioactive molecules was studied in vitro in buffer solution at pH 7.4, in simulated gastric fluid and in mouse plasma. The hydrolysis studies showed a specific cleavage dependent on the pH of the medium and by the presence of proteolytic enzymes in mouse plasma. Studies in vitro on the release of the parent drug from this double prodrug in various media, indicate that the adduct may be sufficiently stable to pass intact the gastrointestinal tract and release into the circulation EU and IBU. Many advantages may be achieved by the synthesis of the prodrug EU-PEG-IBU related to synergistic analgesic and anti-inflammatory effects, to the reduction of the adverse reactions and the improvement of the chemical-physical properties of the parent drugs

New Triterpenes from the Fungus Gloeophyllum odoratum

Two new triterpene acids (1, 2), together with a complex mixture of lecithins (3), were isolated from the fungus Gloeophyllum odoratum. Their structures were elucidated on the basis of extensive spectroscopic analyses. The extract of Gloeophyllum odoratum considerably inhibited thrombin (72% at a concentration of 120 g/mL); the less polar fraction of the methanolic extract from the mushroom exhibited interesting activity (47% at a concentration of 120 g/mL) against thrombin. Compounds 1 and 2 were responsible for this activity

Opis svojstava ekstra djevičanskog maslinovog ulja dobivenog iz raznih kultivara

The determination of some minor components of extra virgin olive oil, and in particular of the polyphenolic fraction of pigments and fragrances, can contribute to the characterization of the monovarietal productions: the quali-quantitative assessment of these substances can in fact contribute to the valorisation of typicalities and, at the same time, consent to the optimisation of the operational techniques during the processing and the eventual blending. The analytical techniques, applied here for the characterisation of extra virgin olive oil of Abruzzo and Istria, have highlighted that chemical composition can enhance the valorisation of these typical products. Nevertheless, further sampling program is needed to evidence typical composition profile that might be used as “origin markers”.Određivarije nekih manjih komponenata ekstra djevičanskog maslinovog ulja, naročito polifenolne frakcije pigmemta i mirisa, može doprinijeti svojstvima monovarijetetnih proizvoda: kvalitativna i kvalitativna procjena tih supstancija može zapravo doprinijeti valorizaciji tipičnosti te, istodobno omogućiti optimizaciju operativnih tehnika za vrijeme prerade i miješanja. Analitičke tehnike, ovdje primijenjene za opis svojstava ekstra djevičanskog maslinovog ulja iz Abruzza i Istre pokazuju da kemijski sastav može popraviti vrijednost ovih tipičnih proizvoda. Ipak, potreban je dodatni program uzorkovanja da se dokaže tipični profil sas¬tava, što se može upotrijebiti kao "oznaka podrijetla"

Opis svojstava ekstra djevičanskog maslinovog ulja dobivenog iz raznih kultivara

The determination of some minor components of extra virgin olive oil, and in particular of the polyphenolic fraction of pigments and fragrances, can contribute to the characterization of the monovarietal productions: the quali-quantitative assessment of these substances can in fact contribute to the valorisation of typicalities and, at the same time, consent to the optimisation of the operational techniques during the processing and the eventual blending. The analytical techniques, applied here for the characterisation of extra virgin olive oil of Abruzzo and Istria, have highlighted that chemical composition can enhance the valorisation of these typical products. Nevertheless, further sampling program is needed to evidence typical composition profile that might be used as “origin markers”.Određivarije nekih manjih komponenata ekstra djevičanskog maslinovog ulja, naročito polifenolne frakcije pigmemta i mirisa, može doprinijeti svojstvima monovarijetetnih proizvoda: kvalitativna i kvalitativna procjena tih supstancija može zapravo doprinijeti valorizaciji tipičnosti te, istodobno omogućiti optimizaciju operativnih tehnika za vrijeme prerade i miješanja. Analitičke tehnike, ovdje primijenjene za opis svojstava ekstra djevičanskog maslinovog ulja iz Abruzza i Istre pokazuju da kemijski sastav može popraviti vrijednost ovih tipičnih proizvoda. Ipak, potreban je dodatni program uzorkovanja da se dokaže tipični profil sas¬tava, što se može upotrijebiti kao "oznaka podrijetla"

CHOLANE AND LANOSTANE DERIVATIVES: ANTIMICROBIAL EVALUATION

Steroids are natural compounds with several important applications in many fields of research, such as medicinal chemistry, pharmacology, supramolecular chemistry and nanotechnology.In particular, bile acids such as lithocholic acid (LCA) and ursodeoxycholic acid (UDCA) have been considered quite useful as starting points for a rich and different set of medicinal chemistry activities. Besides, the discovery of bioactive ingredients from plants and fungi is always the main target in medicinal chemistry. The lanostane-type triterpenoid 3b-hydroxylanosta-8,24-diene-21-oic acid (Trametenolic acid, TMA) was the main bioactive component of Gloeophyllum odoratum, which was reported to possess widely bioactivities, including tumor cell anti-proliferation effects (for example, human HL-60 leukemia, human KB epidermoid carcinoma, murine L1210 leukemia cells, Caski, HT-3, T-24, etc.), inhibition of enzyme activity (human thrombin, bovine trypsin and so on).Nevertheless, trametenolic acid was scarcely investigated as antimicrobial agent. Structurally, bile acids (LCA and UDCA) and trametenolic acid are similar since they may be regarded as consisting of two components, a rigid steroid nucleus and an aliphatic side chain possessing a carboxyl group. On the basis of these considerations, six new compounds bearing a guanidine moiety in their side chain were synthesized using LCA, UDCA and TMA as starting materials. The parent bile acids, TMA and their resulting derivatives were evaluated for antimicrobial activity against S. aureus, B. subtilis and M. smegmatis. The derivative 3a-hydroxy-23-guanidino-5b-cholane showed the best activity, with MIC values of 12.5 \u3bcM against S. aureus, 5 \u3bcM against B. subtilis and 50 \u3bcM against M. smegmatis. The cytotoxic activity of bile acids, trametenolic acid and derivatives was also evaluated against HT-29 cell lin

JAZF1, A Novel p400/TIP60/NuA4 Complex Member, Regulates H2A.Z Acetylation at Regulatory Regions

Histone variants differ in amino acid sequence, expression timing and genomic localization sites from canonical histones and convey unique functions to eukaryotic cells. Their tightly controlled spatial and temporal deposition into specific chromatin regions is accomplished by dedicated chaperone and/or remodeling complexes. While quantitatively identifying the chaperone complexes of many human H2A variants by using mass spectrometry, we also found additional members of the known H2A.Z chaperone complexes p400/TIP60/NuA4 and SRCAP. We discovered JAZF1, a nuclear/nucleolar protein, as a member of a p400 sub-complex containing MBTD1 but excluding ANP32E. Depletion of JAZF1 results in transcriptome changes that affect, among other pathways, ribosome biogenesis. To identify the underlying molecular mechanism contributing to JAZF1's function in gene regulation, we performed genome-wide ChIP-seq analyses. Interestingly, depletion of JAZF1 leads to reduced H2A.Z acetylation levels at > 1000 regulatory sites without affecting H2A.Z nucleosome positioning. Since JAZF1 associates with the histone acetyltransferase TIP60, whose depletion causes a correlated H2A.Z deacetylation of several JAZF1-targeted enhancer regions, we speculate that JAZF1 acts as chromatin modulator by recruiting TIP60's enzymatic activity. Altogether, this study uncovers JAZF1 as a member of a TIP60-containing p400 chaperone complex orchestrating H2A.Z acetylation at regulatory regions controlling the expression of genes, many of which are involved in ribosome biogenesis

An intimate and imperial feminism: Meliscent Shephard and the regulation of prostitution in colonial India

This paper seeks to construct an antinostalgic portrait of an imperial feminist. As the representative of the Association for Moral and Social Hygiene (AMSH) in India between 1928 and 1947, Meliscent Shephard was an embodiment not only of the feminist urge to challenge patriarchal gender relations, but also of the imperialist urge to classify and fathom the world through a series of racist typologies. Despite an earlier belief that blame for the exploitation of prostitutes lay with the colonial state and economy, she later fell back on explanations based on notions of Indian society and religion. Operating in a period of heightened anticolonial nationalism, these latter views thwarted any hope of her forging successful connections with emergent Indian social reform groups. This failure to cultivate intimate relations with Indian colleagues marks a failure at the level of national and racial politics. Shephard did, however, cultivate an intimate relationship with correspondents at the AMSH in London, while her experiences of the sexual geographies of Indian cities provided a form of intimate interaction that would inspire her mission to close down tolerated brothels. As such, this paper marks an empirical engagement with the intimate frontiers at which the affective grid of colonial politics was marked out

Fluorescence-Based Methods for Detecting Caries Lesions: Systematic Review, Meta-Analysis and Sources of Heterogeneity

Background Fluorescence-based methods have been proposed to aid caries lesion detection. Summarizing and analysing findings of studies about fluorescence-based methods could clarify their real benefits. Objective We aimed to perform a comprehensive systematic review and meta-analysis to evaluate the accuracy of fluorescence-based methods in detecting caries lesions. Data Source Two independent reviewers searched PubMed, Embase and Scopus through June 2012 to identify papers/articles published. Other sources were checked to identify non-published literature. Study Eligibility Criteria, Participants and Diagnostic Methods The eligibility criteria were studies that: (1) have assessed the accuracy of fluorescence-based methods of detecting caries lesions on occlusal, approximal or smooth surfaces, in both primary or permanent human teeth, in the laboratory or clinical setting; (2) have used a reference standard; and (3) have reported sufficient data relating to the sample size and the accuracy of methods. Study Appraisal and Synthesis Methods A diagnostic 2×2 table was extracted from included studies to calculate the pooled sensitivity, specificity and overall accuracy parameters (Diagnostic Odds Ratio and Summary Receiver-Operating curve). The analyses were performed separately for each method and different characteristics of the studies. The quality of the studies and heterogeneity were also evaluated. Results Seventy five studies met the inclusion criteria from the 434 articles initially identified. The search of the grey or non-published literature did not identify any further studies. In general, the analysis demonstrated that the fluorescence-based method tend to have similar accuracy for all types of teeth, dental surfaces or settings. There was a trend of better performance of fluorescence methods in detecting more advanced caries lesions. We also observed moderate to high heterogeneity and evidenced publication bias. Conclusions Fluorescence-based devices have similar overall performance; however, better accuracy in detecting more advanced caries lesions has been observed

The COVID-19 pandemic and its global effects on dental practice. An international survey

Objectives: A multicentre survey was designed to evaluate the impact of COVID-19 outbreak on dental practice worldwide, estimate the COVID-19 related symptoms/signs, work attitudes and behaviour and the routine use of protective measures and Personal Protective Equipment (PPE). Methods: A global survey using a standardized questionnaire with research groups from 36 countries was designed. The questionnaire was developed and pretested during April 2020 and contained three domains: 1) Personal data; 2) COVID-19 positive rate and symptoms/signs presumably related to the coronavirus; 3) Working conditions and PPE adopted after the outbreak. Countries’ data were grouped by the Country Positive Rate (CPR) during the survey period and by Gross-National-Income per capita. An ordinal multinomial logistic regression model was carried out with COVID-19 self-reported rate referred by dental professionals as dependent variable to assess the association with questionnaire items. Results: A total of 52,491 questionnaires were returned with a male/female ratio of 0.63. Out of the total respondents, 7,859 dental professionals (15%) reported symptoms/signs compatible with COVID-19. More than half of the sample (n = 27,818; 53%) stated to use FFP2/N95 masks, while 21,558 (41.07%) used eye protection. In the bivariate analysis, CPR and N95/FFP2 were significantly associated (OR = 1.80 95%CI = 1.60/2.82 and OR = 5.20 95%CI = 1.44/18.80, respectively), while Gross-National-Income was not statistically associated with CPR (OR = 1.09 95%CI = 0.97/1.60). The same significant associations were observed in the multivariate analysis. Conclusions: Oral health service provision has not been significantly affected by COVID-19, although access to routine dental care was reduced due to country-specific temporary lockdown periods. While the dental profession has been identified at high-risk, the reported rates of COVID-19 for dental professionals were not significantly different to those reported for the general population in each country. These findings may help to better plan oral health care for future pandemic events