scholarly journals Salicylic Acid as Ionic Liquid Formulation May Have Enhanced Potency to Treat Some Chronic Skin Diseases

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 216
Author(s):  
Joanna Klebeko ◽  
Paula Ossowicz-Rupniewska ◽  
Ewelina Świątek ◽  
Joanna Szachnowska ◽  
Ewa Janus ◽  
...  

In recent years, numerous studies have shown that conversion of conventional drugs in ionic liquid (IL) formulation could be a successful strategy to improve their physicochemical properties or suggest a new route of administration. We report the synthesis and detailed characterization of eight salicylic acid-based ILs (SA-ILs) containing cation non-polar or aromatic amino acid esters. Using in vitro assays, we preliminary evaluated the therapeutic potency of the novel SA-ILs. We observed that conversion of the SA into ionic liquids led to a decrease in its cytotoxicity toward NIH/3T3 murine embryo fibroblasts and human HaCaT keratinocytes. It should be mentioned is that all amino acid alkyl ester salicylates [AAOR][SA] inhibit the production of the proinflammatory cytokine IL-6 in LPS-stimulated keratinocytes. Moreover, keratinocytes, pretreated with [PheOMe][SA] and [PheOPr][SA] seem to be protected from LPS-induced inflammation. Finally, the novel compounds exhibit a similar binding affinity to bovine serum albumin (BSA) as the parent SA, suggesting a similar pharmacokinetic profile. These preliminary results indicate that SA-ILs, especially those with [PheOMe], [PheOPr], and [ValOiPr] cation, have the potential to be further investigated as novel topical agents for chronic skin diseases such as psoriasis and acne vulgaris.

1998 ◽  
Vol 14 (3) ◽  
pp. 226-233 ◽  
Author(s):  
Jürgen Hoyer ◽  
Mechthild Averbeck ◽  
Thomas Heidenreich ◽  
Ulrich Stangier ◽  
Karin Pöhlmann ◽  
...  

Epstein's “Constructive Thinking Inventory” (CTI) was developed to measure the construct of experiential intelligence, which is based on his cognitive-experiential self-theory. Inventory items were generated by sampling naturally occurring automatic cognitions. Using principal component analysis, the findings showed a global factor of coping ability as well as six main factors: Emotional Coping, Behavioral Coping, Categorical Thinking, Personal Superstitious Thinking, Esoteric Thinking, and Naive Optimism. We tested the replicability of this factor structure and the amount of statistical independence (nonredundancy) between these factors in an initial study of German students (Study 1, N = 439) and in a second study of patients with chronic skin disorders (Study 2, N = 187). Factor congruence with the original (American) data was determined using a formula proposed by Schneewind and Cattell (1970) . Our findings show satisfactory factor congruence and statistical independence for Emotional Coping and Esoteric Thinking in both studies, while full replicability or independence could not be found in both for the other factors. Implications for the use and further development of the CTI are discussed.


2021 ◽  
Vol 22 (5) ◽  
pp. 2731
Author(s):  
Piotr Garnuszek ◽  
Urszula Karczmarczyk ◽  
Michał Maurin ◽  
Arkadiusz Sikora ◽  
Jolanta Zaborniak ◽  
...  

A new PSMA ligand (PSMA-D4) containing the Glu-CO-Lys pharmacophore connected with a new linker system (L-Trp-4-Amc) and chelator DOTA was developed for radiolabeling with therapeutic radionuclides. Herein we describe the synthesis, radiolabeling, and preliminary biological evaluation of the novel PSMA-D4 ligand. Synthesized PSMA-D4 was characterized using TOF-ESI-MS, NMR, and HPLC methods. The novel compound was subject to molecular modeling with GCP-II to compare its binding mode to analogous reference compounds. The radiolabeling efficiency of PSMA-D4 with 177Lu, 90Y, 47Sc, and 225Ac was chromatographically tested. In vitro studies were carried out in PSMA-positive LNCaP tumor cells membranes. The ex vivo tissue distribution profile of the radioligands and Cerenkov luminescence imaging (CLI) was studied in LNCaP tumor-bearing mice. PSMA-D4 was synthesized in 24% yield and purity >97%. The radio complexes were obtained with high yields (>97%) and molar activity ranging from 0.11 to 17.2 GBq mcmol−1, depending on the radionuclide. In vitro assays confirmed high specific binding and affinity for all radiocomplexes. Biodistribution and imaging studies revealed high accumulation in LNCaP tumor xenografts and rapid clearance of radiocomplexes from blood and non-target tissues. These render PSMA-D4 a promising ligand for targeted therapy of prostate cancer (PCa) metastases.


2017 ◽  
Vol 14 (2) ◽  
pp. e69
Author(s):  
H. Abdel Hafez ◽  
A.A. Abdel-Motaleb ◽  
H.D. Gaber ◽  
G.S.T. Al-Attar

Vaccines ◽  
2020 ◽  
Vol 9 (1) ◽  
pp. 13
Author(s):  
Lydia Riepler ◽  
Annika Rössler ◽  
Albert Falch ◽  
André Volland ◽  
Wegene Borena ◽  
...  

Neutralizing antibodies are a major correlate of protection for many viruses including the novel coronavirus SARS-CoV-2. Thus, vaccine candidates should potently induce neutralizing antibodies to render effective protection from infection. A variety of in vitro assays for the detection of SARS-CoV-2 neutralizing antibodies has been described. However, validation of the different assays against each other is important to allow comparison of different studies. Here, we compared four different SARS-CoV-2 neutralization assays using the same set of patient samples. Two assays used replication competent SARS-CoV-2, a focus forming assay and a TCID50-based assay, while the other two assays used replication defective lentiviral or vesicular stomatitis virus (VSV)-based particles pseudotyped with SARS-CoV-2 spike. All assays were robust and produced highly reproducible neutralization titers. Titers of neutralizing antibodies correlated well between the different assays and with the titers of SARS-CoV-2 S-protein binding antibodies detected in an ELISA. Our study showed that commonly used SARS-CoV-2 neutralization assays are robust and that results obtained with different assays are comparable.


2018 ◽  
Vol 19 (11) ◽  
pp. 3519 ◽  
Author(s):  
Agustina Bernal-Vicente ◽  
Daniel Cantabella ◽  
Cesar Petri ◽  
José Hernández ◽  
Pedro Diaz-Vivancos

Salinity is considered as one of the most important abiotic challenges that affect crop productivity. Plant hormones, including salicylic acid (SA), are key factors in the defence signalling output triggered during plant responses against environmental stresses. We have previously reported in peach a new SA biosynthetic pathway from mandelonitrile (MD), the molecule at the hub of the cyanogenic glucoside turnover in Prunus sp. In this work, we have studied whether this new SA biosynthetic pathway is also present in plum and the possible role this pathway plays in plant plasticity under salinity, focusing on the transgenic plum line J8-1, which displays stress tolerance via an enhanced antioxidant capacity. The SA biosynthesis from MD in non-transgenic and J8-1 micropropagated plum shoots was studied by metabolomics. Then the response of J8-1 to salt stress in presence of MD or Phe (MD precursor) was assayed by measuring: chlorophyll content and fluorescence parameters, stress related hormones, levels of non-enzymatic antioxidants, the expression of two genes coding redox-related proteins, and the content of soluble nutrients. The results from in vitro assays suggest that the SA synthesis from the MD pathway demonstrated in peach is not clearly present in plum, at least under the tested conditions. Nevertheless, in J8-1 NaCl-stressed seedlings, an increase in SA was recorded as a result of the MD treatment, suggesting that MD could be involved in the SA biosynthesis under NaCl stress conditions in plum plants. We have also shown that the plum line J8-1 was tolerant to NaCl under greenhouse conditions, and this response was quite similar in MD-treated plants. Nevertheless, the MD treatment produced an increase in SA, jasmonic acid (JA) and reduced ascorbate (ASC) contents, as well as in the coefficient of non-photochemical quenching (qN) and the gene expression of Non-Expressor of Pathogenesis-Related 1 (NPR1) and thioredoxin H (TrxH) under salinity conditions. This response suggested a crosstalk between different signalling pathways (NPR1/Trx and SA/JA) leading to salinity tolerance in the transgenic plum line J8-1.


2019 ◽  
Vol 13 (46) ◽  
pp. 584-608
Author(s):  
Manuela Sobral Bentes de Melo ◽  
Nara Freire Leão Rocha ◽  
Stéfany Silva Magalhães ◽  
Lais Landim Sousa

Diversos estudos têm revelado a existência de uma relação entre aspectos psicossociais e o desenvolvimento ou agravamento de dermatoses crônicas, dentre as quais se encontra a psoríase. Fatores psicológicos, stress e outros eventos da vida são capazes de agravar de 40 e 80% dos casos. O estudo objetivou analisar a forma como esses aspectos podem ensejar o surgimento, a reincidência ou a acentuação do quadro clínico. Metodologia: Estudo de casos concretos com pacientes portadores da psoríase, além de uma vasta literatura bibliográfica acerca da temática. Conclusão: Ficou demonstrada a importância do tratamento psíquico e fisiológico, bem como a necessidade do desenvolvimento de estratégias de coping para enfretamento das situações sociais envolvidas.   


Dermatology ◽  
2020 ◽  
Vol 236 (4) ◽  
pp. 324-328 ◽  
Author(s):  
Lynda Grine ◽  
Giulia Tochtermann ◽  
Hilde Lapeere ◽  
Nele Maes ◽  
Günther F.L. Hofbauer ◽  
...  

Background: Psoriasis and atopic dermatitis are chronic skin diseases that greatly affect the quality of life. Both diseases can be triggered or exacerbated by stress. Objective: We aimed to differentiate personality traits between patients with chronic skin conditions and people treated for stress in a pilot study. Methods: Patients participating voluntarily in educational programs in Belgium and Switzerland were recruited to complete personality trait questionnaires, including the Temperament and Character Inventory (TCI) and the Tridimensional Personality Questionnaire (TPQ). A comparison was made with patients treated for work-related stress. Results: A total of 48 and 91 patients suffering from skin diseases and work-related stress, respectively, were included in the study. Based on the questionnaires, we found that dermatology patients were less persistent and impulsive than those with work-related stress. Dermatology patients also exhibited more rigidness and less focus on performance. Finally, patients with work-related stress seem more likely to change in response to health-promoting programs than patients with chronic dermatoses. Conclusion: Patients with chronic skin diseases may perceive and cope with stress differently in comparison to patients with work-related stress due to inherent personality traits. Therefore, stress coping mechanisms may differ among different diseases. More research is needed into the design of educational interventions and the impact of personality traits in disease-specific groups.


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