1,720,984 research outputs found
2D- and 3D-QSAR of tocainide and mexiletine analogues acting as Na(v)1.4 channel blockers
No full textEnantiomeric forms of Tocainide, Mexiletine, and structurally related local anaesthetic compounds, were
analyzed with respect to their potency in blocking Nav1.4 channel. Structure–activity relationships based
on in vitro pharmacological assays, suggested that an increase in terms of lipophilicity and/or molecular
surface as well as the presence of specific polar spacers might be determinant for receptor interactions.
QSAR and pharmacophore models were then used to support at 3D level this hypothesisEnantiomeric forms of Tocainide. Mexiletine, and structurally related local anaesthetic compounds, were analyzed with respect to their potency in blocking Na(v)1.4 channel. Structure-activity relationships based on in vitro pharmacological assays, suggested that an increase in terms of lipophilicity and/or molecular surface as well as the presence of specific polar spacers might be determinant for receptor interactions. QSAR and pharmacophore models were then used to support at 3D level this hypothesis. (C) 2008 Elsevier Masson SAS. All rights reserved
Fluorescent Light Energy (FLE) Generated through Red LED Light and a Natural Photoconverter Gel as a New, Non-Invasive Approach for Facial Age Control: A Pilot Study
Full text linkThis study, for the first time, evaluated the safety and efficacy of a new natural-based topical gel containing a spirulina extract. This photoconverter gel generates fluorescent light energy (FLE) via a red LED light device, which is proven to be effective for age control of facial skin. This was a one-centre, observational, uncontrolled pilot trial. Eight healthy female subjects aged 35 to 65 years old, with Fitzpatrick skin types II–V were recruited. The duration of the study was five treatment sessions of one treatment every seven days, with a final follow-up at one month after the last treatment session. The images and the related data were acquired with the SONY® Mod. DSCRX10M3, the Canfield VISIA Facial Imaging System®, and QUANTIFICARE 3D® analysis. Patient compliance was excellent (100%) and the treatment was described as warm and pleasant by the patients. After 30 days, VISIA parameters such as wrinkles, texture, red areas, and Trueskin Age® had improved. The safety and efficacy of the FLE treatment assessed in this trial were achieved for overall rejuvenation of facial skin, focusing on wrinkles evaluated via the specific VISIA algorithms
Overview of the Potential Beneficial Effects of Carotenoids on Consumer Health and Well-Being
Full text linkWell-known experimental research demonstrates that oxidative stress is the leading cause of the onset and progression of major human health disorders such as cardiovascular, neurological, metabolic, and cancer diseases. A high concentration of reactive oxygen species (ROS) and nitrogen species leads to damage of proteins, lipids, and DNA associated with susceptibility to chronic human degenerative disorders. Biological and pharmaceutical investigations have recently focused on exploring both oxidative stress and its defense mechanisms to manage health disorders. Therefore, in recent years there has been considerable interest in bioactive food plant compounds as naturally occurring antioxidant sources able to prevent, reverse, and/or reduce susceptibility to chronic disease. To contribute to this research aim, herein, we reviewed the beneficial effects of carotenoids on human health. Carotenoids are bioactive compounds widely existing in natural fruits and vegetables. Increasing research has confirmed that carotenoids have various biological activities, such as antioxidant, anti-tumor, anti-diabetic, anti-aging, and anti-inflammatory activities. This paper presents an overview of the latest research progress on the biochemistry and preventative and therapeutic benefits of carotenoids, particularly lycopene, in promoting human health. This review could be a starting point for improving the research and investigation of carotenoids as possible ingredients of functional health foods and nutraceuticals in the fields of healthy products, cosmetics, medicine, and the chemical industry
Synthesis and Biological Evaluation of Chiral α-Aminoanilides with Central Antinociceptive Activity
No full textTocainide and related optically active chiral alpha-aminoanilides were synthesized and tested in vivo via the hot plate test to evaluate their central analgesic action. The aims of the study were to verify if a) the increase in lipophilicity, obtained by the introduction of an alkyl group on the steric center (3f-i), and the replacement of the C=O group with the C=S (10) group as well as the introduction of a methyl or ethyl group on the amidic nitrogen atom (8a-c) would produce an increase in central analgesic efficacy with respect to Tocainide; b) the 2,6-xylidide moiety is crucial for high analgesic activity (3b-e); c) the hydrogen atom bonded to the amidic nitrogen moiety is an essential pharmacophoric element for analgesic activity. Among all the synthesized compounds, 3f showed antinociceptive properties with a good enantioselective index
1, 3‐Benzothiazoles as Antimicrobial Agents
No full textNovember 2015 1,3-Benzothiazoles as Antimicrobial Agents 1705Ivana Defrenza, Alessia Catalano,*Alessia Carocci,*Antonio Carrieri, Marilena Muraglia, Antonio Rosato,Filomena Corbo, and Carlo FranchiniDipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari ‘Aldo Moro’, via E. Orabona n. 4, 70125 Bari, Italy*E-mail: [email protected]; [email protected] November 5, 2013DOI 10.1002/jhet.2222Published online 24 October 2014 in Wiley Online Library (wileyonlinelibrary.com).Starting from 2-amino-1,3-mercaptobenzothiazoles recently reported (1a–h), a series of the corresponding2-mercapto-1,3-benzothiazole isosters (2a–h) were screened for their in vitro antibacterial and antifungalactivities. Results underline that the presence of the mercapto moiety at the 2-position of the heterocyclic nu-cleus is crucial for activity against bacteria. The biological screening against Candida spp. identified com-mercial 2f as the most promising compound as antifungal against Candida albicans and tropicalis.Molecular modeling studies supported these results. Then, to enlarge structure-activity relationship (SAR)studies on series 1, newly synthesized compounds (1k–p) were reported. All the compounds belonging to thisseries and bearing a bulky substituent at the 6-position of the aryl moiety showed high antifungal activity
Antimicrobial Synergistic Effects of Linezolid and Vancomycin with a Small Synthesized 2-Mercaptobenzothiazole Derivative: A Challenge for MRSA Solving
Full text linkMethicillin-resistant Staphylococcus aureus (MRSA) emerged as one of the leading causes of persistent human infections and makes it difficult to treat bacteremia, especially with biofilm formation. In this work, we investigated the in vitro synergism between Linezolid (LNZ) and Vancomycin (VAN) with a 2-mercaptobenzothiazole derivative, resulting in a new small-molecule antibacterial compound that we named BTZ2e, on several clinical MRSA, MRSE (methicillin-resistant Staphylococcus epidermidis) and control (ATCC Collection) strains in their planktonic and biofilms cultures. The broth microdilution method evaluated the susceptibility of planktonic cells to each investigated antibiotic combined with BTZ2e. The biofilm's metabolic activity was studied with the XTT reduction assay. As a result, in this study, biofilm formation was significantly suppressed by the BTZ2e treatment. In terms of minimal biofilm inhibitory concentration (MBIC), BTZ2e revealed an MBIC50 value of 32 mu g/mL against methicillin-susceptible S. aureus (MSSA) and 16 mu g/mL against methicillinresistant S. aureus ATCC 43300 biofilms. An inhibition range of 32 mu g/mL and 256 mu g/mL was registered for the clinical isolates. Interestingly, a synergistic effect (FICI <= 0.5) was encountered for the combination of BTZ2e with LNZ and VAN on several planktonic and sessile strains. In particular, the best result against planktonic cells emerged as a result of the synergistic association between LNZ and BTZ2e, while against sessile cells, the best synergistic association resulted from VAN and BTZ2e. The consistent results indicate BTZ2e as a promising adjuvant against multi-resistant strains such as MRSA and MRSE
Anticancer and Antibacterial Activity of Hyperforin and Its Derivatives
No full textllypcrtbrin ir a natural phloroglucinol tlraî hao baen knswn for îhe trc6lm{:!î of dsprer'niop. llyperforin clisplay* alro
antibacr€rial. antiprolifcranr and ontiangiogenic activity. Synrhetie dsrivatives ofhypcrlnrin have also recsfltly been reportsd lo porisc of hyperforin (nrirtoforin, tetrohydrohyperfbrin onil octalrydrohperlbrin) that
dcmonsrratcd promising antitunror uetivity. Anrong the{], octahyrJrohyper{orin alsn paset ofbact$ria
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
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