Phenylalanine Butyramide Is a New Cosmetic Ingredient with Soothing and Anti-Reddening Potential

Human skin is colonized by diverse commensal microbes, making up the skin microbiota (SM), contributing to skin integrity and homeostasis. Many of the beneficial effects aroused by the SM are exerted by microbial metabolites such as short-chain fatty acids (SCFAs), including butyric acid. The SCFAs can be used in cosmetic formulations against skin diseases to protect SM by preserving and/or restoring their natural balance. Unpleasant sensorial properties and unfavorable physico-chemical properties of butyrate strongly limit its cosmetic use. In contrast, some butyrate derivatives, including phenylalanine butyramide (C13H18N2O2, FBA), a solid form of butyric acid, are odorless while retaining the pharmacokinetic properties and safety profile of butyric acid. This study assessed the FBA’s permeation across the skin and its soothing and anti-reddening potential to estimate its cosmetic application. The dosage method used to estimate FBA’s levels was validated to be sure of analytical results. The FBA diffusion tests were estimated in vitro using a Franz-type vertical diffusion cell. The soothing action was evaluated in vivo by Colorimeter CL400, measuring the erythema index. The results suggest that the FBA represents an innovative way to exploit the benefits of butyric acid in the cosmetic fields since it cannot reach the bloodstream, is odorless, and has a significative soothing action (decrease the erythema index −15.7% after 30′, and −17.8% after 60′).

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Mining a Nanoparticle Dataset, Compiled Within the MODENA-COST Action

Research Anthology on Synthesis, Characterization, and Applications of Nanomaterials ◽

10.4018/978-1-7998-8591-7.ch071 ◽

2021 ◽

pp. 1706-1724

Author(s):

Sabine Van Miert ◽

Jan Creylman ◽

Geert R. Verheyen

Keyword(s):

Chemical Properties ◽

In Vitro Testing ◽

Cost Action ◽

Robust Model ◽

Physico Chemical ◽

Classification And Regression ◽

Toxic Potential ◽

Sheer Number

Engineered nanomaterials (ENM) have new or enhanced physico-chemical properties compared to their micron-sized counterparts, but may also have an increased toxic potential. Animal and in vitro testing are typically employed to investigate the toxic effects of (nano)materials. The sheer number of ENMs and their physico-chemical parameters make it impossible to only use in vivo and in vitro testing, and modelling technologies are also deployed to find relationships between ENM parameters and toxicity. A heterogenous dataset containing information on 192 nanoparticle endpoints was compiled within the MODENA COST-Action consortium. Here, the available data was mined to identify relationships between nanoparticle properties and cell-death as measured with four cytotoxicity assays. ANOVA, collinearity analyses and classification and regression trees gave indications on potential relations between the NP-properties and toxicity, but could not deliver a robust model. More information and datapoints are necessary to build well-validated models.

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In Vitro Physico-Chemical Characterization and Standardized In Vivo Evaluation of Biocompatibility of a New Synthetic Membrane for Guided Bone Regeneration

Materials ◽

10.3390/ma12071186 ◽

2019 ◽

Vol 12 (7) ◽

pp. 1186

Author(s):

Lívia da Costa Pereira ◽

Carlos Fernando de Almeida Barros Mourão ◽

Adriana Terezinha Neves Novellino Alves ◽

Rodrigo Figueiredo de Brito Resende ◽

Marcelo José Pinheiro Guedes de Uzeda ◽

...

Keyword(s):

Bone Regeneration ◽

Chemical Properties ◽

Chemical Characterization ◽

Guided Bone Regeneration ◽

Tissue Reaction ◽

In Vivo Evaluation ◽

Physico Chemical ◽

Tissue Reactions

This study’s aim was to evaluate the biocompatibility and bioabsorption of a new membrane for guided bone regeneration (polylactic-co-glycolic acid associated with hydroxyapatite and β-tricalcium phosphate) with three thicknesses (200, 500, and 700 µm) implanted in mice subcutaneously. Scanning electron microscopy, X-ray diffraction, Fourier transform infrared spectroscopy, and the quantification of carbon, hydrogen and nitrogen were used to characterize the physico-chemical properties. One hundred Balb-C mice were divided into 5 experimental groups: Group 1—Sham (without implantation); Group 2—200 μm; Group 3—500 μm; Group 4—700 μm; and Group 5—Pratix®. Each group was subdivided into four experimental periods (7, 30, 60 and 90 days). Samples were collected and processed for histological and histomorphometrical evaluation. The membranes showed no moderate or severe tissue reactions during the experimental periods studied. The 500-μm membrane showed no tissue reaction during any experimental period. The 200-μm membrane began to exhibit fragmentation after 30 days, while the 500-μm and 700-µm membranes began fragmentation at 90 days. All membranes studied were biocompatible and the 500 µm membrane showed the best results for absorption and tissue reaction, indicating its potential for clinical guided bone regeneration.

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Optimization of Innovative Three-Dimensionally-Structured Hybrid Vesicles to Improve the Cutaneous Delivery of Clotrimazole for the Treatment of Topical Candidiasis

Pharmaceutics ◽

10.3390/pharmaceutics11060263 ◽

2019 ◽

Vol 11 (6) ◽

pp. 263 ◽

Cited By ~ 4

Author(s):

Maria Letizia Manca ◽

Iris Usach ◽

José Esteban Peris ◽

Antonella Ibba ◽

Germano Orrù ◽

...

Keyword(s):

Electron Microscopy ◽

Transmission Electron Microscopy ◽

Chemical Properties ◽

Chemical Characterization ◽

Yeast Cells ◽

Unilamellar Vesicles ◽

Transmission Electron ◽

Physico Chemical

New three-dimensionally-structured hybrid phospholipid vesicles, able to load clotrimazole in a high amount (10 mg/mL), were obtained for the first time in this work by significantly reducing the amount of water (≤10%), which was replaced with a mixture of glycerol and ethanol (≈90%). A pre-formulation study was carried out to evaluate the effect of both the composition of the hydrating medium and the concentration of the phospholipid on the physico-chemical properties of hybrid vesicles. Four different three-dimensionally-structured hybrid vesicles were selected as ideal systems for the topical application of clotrimazole. An extensive physico-chemical characterization performed using transmission electron microscopy (TEM), cryogenic transmission electron microscopy (cryo-TEM), 31P-NMR, and small-angle X-ray scattering (SAXS) displayed the formation of small, multi-, and unilamellar vesicles very close to each other, and was capable of forming a three-dimensional network, which stabilized the dispersion. Additionally, the dilution of the dispersion with water reduced the interactions between vesicles, leading to the formation of single unilamellar vesicles. The evaluation of the in vitro percutaneous delivery of clotrimazole showed an improved drug deposition in the skin strata provided by the three-dimensionally-structured vesicles with respect to the commercial cream (Canesten®) used as a reference. Hybrid vesicles were highly biocompatible and showed a significant antifungal activity in vitro, greater than the commercial cream Canesten®. The antimycotic efficacy of formulations was confirmed by the reduced proliferation of the yeast cells at the site of infection in vivo. In light of these results, clotrimazole-loaded, three-dimensionally-structured hybrid vesicles appear to be one of the most innovative and promising formulations for the treatment of candidiasis infections.

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The fermentation of polydextrose in the large intestine and its beneficial effects

Beneficial Microbes ◽

10.3920/bm2013.0065 ◽

2014 ◽

Vol 5 (3) ◽

pp. 305-313 ◽

Cited By ~ 19

Author(s):

H. Röytiö ◽

A.C. Ouwehand

Keyword(s):

Large Intestine ◽

Complex Structure ◽

Short Chain Fatty Acids ◽

Short Review ◽

Fermentation Products ◽

Beneficial Effects ◽

Glucose Polymer ◽

Upper Gastrointestinal

Polydextrose is a randomly bonded glucose polymer with a highly branched and complex structure. It resists digestion in the upper gastrointestinal tract and is partially fermented in the large intestine by the colonic microbes. Due to its complex structure, a plethora of microbes is required for the catabolism of polydextrose and this process occurs slowly. This gradual fermentation of polydextrose gives rise to moderate amounts of fermentation products, such as short chain fatty acids and gas. The production of these metabolites continues in the distal part of the colon, which is usually considered to be depleted of saccharolytic fermentation substrates. The fermentation of polydextrose modifies the composition of the microbiota in the colon, and has been shown to impact appetite and satiety in humans and improve the gastrointestinal function. The purpose of this short review is to summarise the in vitro, in vivo and human studies investigating the fermentation properties of polydextrose in the large intestine.

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Potential Applications of Biphosphonates in Dental Surgical Implants

International Journal of Immunopathology and Pharmacology ◽

10.1177/039463200702000304 ◽

2007 ◽

Vol 20 (3) ◽

pp. 455-465 ◽

Cited By ~ 6

Author(s):

D. Berardi ◽

T. Carlesi ◽

F. Rossi ◽

M. Calderini ◽

R. Volpi ◽

...

Keyword(s):

Alveolar Bone ◽

Chemical Properties ◽

Osteonecrosis Of The Jaw ◽

In Vivo Experiments ◽

Surgical Implants ◽

Physico Chemical ◽

Potential Applications ◽

Collateral Effect

Biphosphonates are largely used for their unquestionable properties of inhibiting bone resorption by osteoclast in the treatment of various osteometabolic illnesses such as osteoporosis, multiple myeloma, tumors which metastasize to the bone and malignant hypercalcemia. In this literature review the physico-chemical properties, biologic activities and the mechanisms of action of biphosphonates are described. The use of these drugs is discussed, analyzing the quantity of results which have emerged through in vitro and in vivo experiments on animal models. In this study the efficiency of these drugs is demonstrated in contrasting the osteolitic processes of the alveolar bone, in promoting the neoformation and in bettering the quality of bone implants. However, it is important to draw attention to a worrying correlation which has emerged during the last 3–4 years, between osteonecrosis of the jaw (ONJ) and the systemic administration of aminobiphosphonates. This collateral effect did not emerge following the use of non-aminobiphosphonates. The aim of this revie w is to identify the guidelines for the use of biphosphonates in oral implant surgery.

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Design, Synthesis, Pharmacological Evaluation and Vascular Effects of Delphinidin Analogues

Current Pharmaceutical Design ◽

10.2174/1381612825666190206144913 ◽

2019 ◽

Vol 24 (46) ◽

pp. 5580-5589 ◽

Cited By ~ 3

Author(s):

Samuel Legeay ◽

Kien Trân ◽

Yannick Abatuci ◽

Hélène Justiniano ◽

Claire Lugnier ◽

...

Keyword(s):

Chemical Properties ◽

Estrogen Receptor Α ◽

Polyphenolic Compounds ◽

Strong Increase ◽

No Production ◽

Vascular Effects ◽

Oh Groups ◽

Beneficial Effects

Background: Among polyphenolic compounds suggested to prevent cardiovascular diseases (CVDs) and to explain the “French paradox”, the anthocyanidin delphinidin (Dp) has been reported to support at least partly the vascular beneficial effects of dietary polyphenolic compounds including those from fruits and related products as red wine. It has also been highlighted that Dp interacts directly with the active site of estrogen receptor α (ERα), leading to activation of endothelial NO synthase (eNOS) pathway thus contributing to the prevention of endothelial dysfunction in mice aorta. However, anthocyanidins have very low bioavailability and despite a well described in vitro efficacy, the very high hydrophilicity and physicochemical instability of Dp might explain the lack of in vivo reported effects. Objective: The aim of this study was to identify new Dp analogues with increased lipophilicity and vasorelaxation potential by a chemical modulation of its structure and to characterize the signaling pathway notably in relation with ERα signaling and nitric oxide (NO) production. Method: OCH3-substituted delphinidin analogues were obtained through the coupling of the corresponding acetophenones with substituted benzaldehydes. Prediction of resorption of the flavylium derivatives was performed with the calculated logP and induction of vasorelaxation was performed by myography on WT and ERαKO mice thoracic aorta rings and compared to Dp. NO production was evaluated in vitro on human primary endothelial cells. Results: Eight Dp analogues were synthesized including four new flavylium derivatives. Two compounds (9 and 11) showed a strong increase of vasorelaxation potential and a theoretically increased bioavailability compared to Dp. Interestingly, 9 and 11 induced increased O2 - or NO endothelial production respectively and revealed a novel NO-dependent ERα-independent relaxation compared to Dp. We suggested that this mechanism may be at least in part supported by the inhibition of vascular cyclic nucleotide phosphodiesterase (PDEs). Conclusion: The current study demonstrated that pharmacomodulation of the Dp backbone by replacement of OH groups by OCH3 groups of the A and B rings led to the identification and characterization of two compounds (9 and 11) with enhanced physio-chemical properties that could be associated to higher permeability capability and pharmacological activity for the prevention of CVDs compared to Dp.

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The Puzzling Potential of Carbon Nanomaterials: General Properties, Application, and Toxicity

Nanomaterials ◽

10.3390/nano10081508 ◽

2020 ◽

Vol 10 (8) ◽

pp. 1508

Author(s):

Danica Jović ◽

Vesna Jaćević ◽

Kamil Kuča ◽

Ivana Borišev ◽

Jasminka Mrdjanovic ◽

...

Keyword(s):

Carbon Nanomaterials ◽

Wide Spectrum ◽

Chemical Properties ◽

Carbon Nanomaterial ◽

In Vivo Models ◽

Physico Chemical ◽

The Impact ◽

Cell Signaling Pathways

Being a member of the nanofamily, carbon nanomaterials exhibit specific properties that mostly arise from their small size. They have proved to be very promising for application in the technical and biomedical field. A wide spectrum of use implies the inevitable presence of carbon nanomaterials in the environment, thus potentially endangering their whole nature. Although scientists worldwide have conducted research investigating the impact of these materials, it is evident that there are still significant gaps concerning the knowledge of their mechanisms, as well as the prolonged and chronic exposure and effects. This manuscript summarizes the most prominent representatives of carbon nanomaterial groups, giving a brief review of their general physico-chemical properties, the most common use, and toxicity profiles. Toxicity was presented through genotoxicity and the activation of the cell signaling pathways, both including in vitro and in vivo models, mechanisms, and the consequential outcomes. Moreover, the acute toxicity of fullerenol, as one of the most commonly investigated members, was briefly presented in the final part of this review. Thinking small can greatly help us improve our lives, but also obliges us to deeply and comprehensively investigate all the possible consequences that could arise from our pure-hearted scientific ambitions and work.

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Physico-chemical properties of oral streptococcal cell surfaces and their relation with adhesion to solid substrata in vitro and in vivo

Colloids and Surfaces ◽

10.1016/0166-6622(89)80350-6 ◽

1989 ◽

Vol 42 (3-4) ◽

pp. 345-353 ◽

Cited By ~ 9

Author(s):

H.J. Busscher ◽

A.H. Weerkamp ◽

H.C. van der Mei ◽

D. van Steenberghe ◽

M. Quirynen ◽

...

Keyword(s):

Chemical Properties ◽

Cell Surfaces ◽

Physico Chemical

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Health Concerns of Various Nanoparticles: A Review of Their in Vitro and in Vivo Toxicity

Nanomaterials ◽

10.3390/nano8090634 ◽

2018 ◽

Vol 8 (9) ◽

pp. 634 ◽

Cited By ~ 57

Author(s):

Marziyeh Ajdary ◽

Mohammad Moosavi ◽

Marveh Rahmati ◽

Mojtaba Falahati ◽

Mohammad Mahboubi ◽

...

Keyword(s):

Chemical Properties ◽

Protein Corona ◽

In Vitro Models ◽

The Body ◽

Limiting Factor ◽

Key Factors ◽

Cytotoxic Effects ◽

Physico Chemical

Nanoparticles (NPs) are currently used in diagnosis and treatment of many human diseases, including autoimmune diseases and cancer. However, cytotoxic effects of NPs on normal cells and living organs is a severe limiting factor that hinders their use in clinic. In addition, diversity of NPs and their physico-chemical properties, including particle size, shape, surface area, dispersity and protein corona effects are considered as key factors that have a crucial impact on their safe or toxicological behaviors. Current studies on toxic effects of NPs are aimed to identify the targets and mechanisms of their side effects, with a focus on elucidating the patterns of NP transport, accumulation, degradation, and elimination, in both in vitro and in vitro models. NPs can enter the body through inhalation, skin and digestive routes. Consequently, there is a need for reliable information about effects of NPs on various organs in order to reveal their efficacy and impact on health. This review covers the existing knowledge base on the subject that hopefully prepares us better to address these challenges.

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