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https://www.readbyqxmd.com/read/29138987/optimized-ciclopirox-based-eudragit-rlpo-nail-lacquer-effect-of-endopeptidase-enzyme-as-permeation-enhancer-on-transungual-drug-delivery-and-efficiency-against-onychomycosis
#1
Abeer Khattab, Samia Shalaby
The aims of our investigation were to develop and optimize ciclopirox (CPX) nail lacquer using nonbiodegradable Eudragit RLPO (E-RLPO) as a film former and to assess its penetration efficiency across the human nail plate. Preliminary trials such as hydration enhancement factor (HEF), a retained drug in the nail plate, and SEM were studied to select the optimized permeation enhancer to be incorporated in the optimized lacquer formulation. A 3(3) full factorial design was built up to study the effect of three different factors, concentration of E-RLPO (10, 20, and 30%), Tween 80 (0...
November 14, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29131581/template-assisted-enzymatic-synthesis-of-oligopeptides-from-a-polylactide-chain
#2
Jenny Fagerland, Daniela Pappalardo, Björn Schmidt, Per-Olof Syrén, Anna Finne Wistrand
Peptides are often attached to polymer materials, as bioactive components, for the control of interactions between the material and its surrounding proteins and cells. However, synthesizing peptides and attaching them to polymers can be challenging and laborious. Herein, we describe the grafting of oligopeptides to an aliphatic polyester, using a one-step chemo-enzymatic synthesis with papain as the biocatalyst. To enable enzyme-mediated functionalization of the polyester, ethyl hept-6-enoylalaninate (grafter) was synthesized and attached to polylactide chains using thiol-ene click reactions...
November 13, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/29128390/nsp3-of-coronaviruses-structures-and-functions-of-a-large-multi-domain-protein
#3
REVIEW
Jian Lei, Yuri Kusov, Rolf Hilgenfeld
The multi-domain non-structural protein 3 (Nsp3) is the largest protein encoded by the coronavirus (CoV) genome, with an average molecular mass of about 200 kD. Nsp3 is an essential component of the replication/transcription complex. It comprises various domains, the organization of which differs between CoV genera, due to duplication or absence of some domains. However, eight domains of Nsp3 exist in all known CoVs: the ubiquitin-like domain 1 (Ubl1), the Glu-rich acidic domain (also called "hypervariable region"), a macrodomain (also named "X domain"), the ubiquitin-like domain 2 (Ubl2), the papain-like protease 2 (PL2(pro)), the Nsp3 ectodomain (3Ecto, also called "zinc finger domain"), as well as the domains Y1 and CoV-Y of unknown functions...
November 8, 2017: Antiviral Research
https://www.readbyqxmd.com/read/29128226/camel-milk-protein-hydrolysates-with-improved-technofunctional-properties-and-enhanced-antioxidant-potential-in-in-vitro-and-in-food-model-systems
#4
Kholoud Awad Al-Shamsi, Priti Mudgil, Hassan Mohamed Hassan, Sajid Maqsood
Camel milk protein hydrolysates (CMPH) were generated using proteolytic enzymes, such as alcalase, bromelain, and papain, to explore the effect on the technofunctional properties and antioxidant potential under in vitro and in real food model systems. Characterization of the CMPH via degree of hydrolysis, sodium dodecyl sulfate-PAGE, and HPLC revealed that different proteins in camel milk underwent degradation at different degrees after enzymatic hydrolysis using 3 different enzymes for 2, 4, and 6 h, with papain displaying the highest degradation...
November 8, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/29127014/structural-insights-and-binding-of-a-natural-ligand-succinic-acid-with-serine-and-cysteine-proteases
#5
R Manohar, N H V Kutumbarao, Raghavendra Sashi Krishna Nagampalli, D Velmurugan, K Gunasekaran
In the age of growing infectious diseases, there is a great demand for new inhibitors which can exhibit minimum side effects. Owing to the importance of proteases in life cycle and invasion, they have been projected as attractive targets for structure based drug designing against microbes including viruses. Here we report the inhibitory activity of a well known natural compound succinic acid against both serine and cysteine proteases. The ligand is found co-crystallized with Bovine pancreatic trypsin in one of our crystallization trials and the diffraction data up to1...
November 7, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29122948/microrna-regulation-of-type-2-innate-lymphoid-cell-homeostasis-and-function-in-allergic-inflammation
#6
Priti B Singh, Heather H Pua, Hannah C Happ, Christoph Schneider, Jakob von Moltke, Richard M Locksley, Dirk Baumjohann, K Mark Ansel
MicroRNAs (miRNAs) exert powerful effects on immunity through coordinate regulation of multiple target genes in a wide variety of cells. Type 2 innate lymphoid cells (ILC2s) are tissue sentinel mediators of allergic inflammation. We established the physiological requirements for miRNAs in ILC2 homeostasis and immune function and compared the global miRNA repertoire of resting and activated ILC2s and T helper type 2 (TH2) cells. After exposure to the natural allergen papain, mice selectively lacking the miR-17∼92 cluster in ILC2s displayed reduced lung inflammation...
November 9, 2017: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/29108648/cyclosporin-a-indirectly-attenuates-activation-of-group-2-innate-lymphoid-cells-in-papain-induced-lung-inflammation
#7
Fujimi Kudo, Masashi Ikutani, Masanori Iseki, Satoshi Takaki
Cyclosporin A (CsA) is a well-known immunosuppressant that is used against steroid-resistant asthma. Group 2 innate lymphoid cells (ILC2s) and type 2 helper T (Th2) cells produce Th2 cytokines including IL-5 and play important roles in asthma pathogenesis. Here, we studied the effects of CsA in allergen-induced lung inflammation in mice and found that CsA decreased the number of lung ILC2s and attenuated papain-induced activation of ILC2s accompanied with IL-5 expression. The ILC2 suppression mediated by CsA was not observed in culture or in lymphocyte-deficient Rag2(-/-) mice...
October 27, 2017: Cellular Immunology
https://www.readbyqxmd.com/read/29102407/physical-and-kinematic-properties-of-cryopreserved-camel-sperm-after-elimination-of-semen-viscosity-by-different-techniques
#8
Khalid El-Bahrawy, Sherif Rateb, Marwa Khalifa, Davide Monaco, Giovanni Lacalandra
This investigation aimed to determine the influence of using different techniques for liquefaction of semen on post-thaw physical and dynamic characteristics of camel spermatozoa. A total of 144 ejaculates were collected from 3 adult camels, Camelus dromedarius, twice-weekly over 3 consecutive breeding seasons. A raw aliquot of each ejaculate was evaluated for physical and morphological properties, whereas the remaining portion was diluted (1:3) with glycerolated Tris lactose egg yolk extender, and was further subjected to one of the following liquefaction treatments: control (untreated), 5μl/ml α-amylase, 0...
October 31, 2017: Animal Reproduction Science
https://www.readbyqxmd.com/read/29080507/mucus-permeating-self-emulsifying-drug-delivery-systems-sedds-about-the-impact-of-mucolytic-enzymes
#9
Nuri Ari Efiana, Thi Nhu Quynh Phan, Arko Jatmiko Wicaksono, Andreas Bernkop-Schnürch
This study aimed to improve the mucus permeating properties of self-emulsifying drug delivery systems (SEDDS) by anchoring lipidized bromelain, papain and trypsin using palmitoyl chloride. SEDDS containing enzyme-palmitate conjugates were characterized regarding droplet size and zeta potential. Their mucus permeating properties were evaluated by Transwell diffusion and rotating tube method using fluorescein diacetate (FDA) as marker. Degree of substitution of modified enzymes was 35.3%, 47.8% and 38.5% for bromelain-palmitate, papain-palmitate and trypsin-palmitate, respectively...
October 23, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29079537/enzyme-decorated-drug-carriers-targeted-swords-to-cleave-and-overcome-the-mucus-barrier
#10
Claudia Menzel, Andreas Bernkop-Schnürch
The use of mucus permeating drug carrier systems being able to overcome the mucus barrier can lead to a remarkable enhancement in bioavailability. One promising approach is the design of mucolytic enzyme decorated carrier systems (MECS). These systems include micro- and nanoparticles as well as self-emulsifying drug delivery systems (SEDDS) decorated with mucin cleaving enzymes such as papain (PAP) or bromelain (BRO). MECS are able to cross the mucus barrier in a comparatively efficient manner by cleaving mucus substructures in front of them on their way to the epithelium...
October 24, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/29069895/hydrodabcyl-a-superior-hydrophilic-alternative-to-the-dark-fluorescence-quencher-dabcyl
#11
Oxana Kempf, Karl Kempf, Rainer Schobert, Elisa Bombarda
Dark fluorescence quenchers are nonfluorescent dyes that can modulate the fluorescence signal of an appropriate fluorophore donor in a distance-dependent manner. Dark quenchers are extensively used in many biomolecular analytical applications, such as studies with fluorogenic protease substrates or nucleic acids probes. A very popular dark fluorescence quencher is dabcyl, which is a hydrophobic azobenzene derivative. However, its insolubility in water may constitute a major drawback, especially during the investigation of biochemical systems whose natural solvent is water...
November 7, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/29068239/a-phytophthora-palmivora-extracellular-cystatin-like-protease-inhibitor-targets-papain-to-contribute-to-virulence-on-papaya
#12
Rebecca Gumtow, Dongliang Wu, Janice Uchida, Miaoying Tian
Papaya fruits, stems and leaves are rich in papain, a cysteine protease that has been shown to mediate plant defense against pathogens and insects. Yet the oomycete Phytophthora palmivora is a destructive pathogen that infects all parts of papaya plants, suggesting that it has evolved cysteine protease inhibitors to inhibit papain to enable successful infection. Out of five putative cystatin-like extracellular protease inhibitors (PpalEPICs) from P. palmivora transcriptomic sequence data, PpalEPIC8 appeared to be unique to P...
October 25, 2017: Molecular Plant-microbe Interactions: MPMI
https://www.readbyqxmd.com/read/29068048/possibilities-for-developing-texture-modified-beef-steaks-suitable-for-older-consumers-using-fruit-derived-proteolytic-enzymes
#13
Cristina Botinestean, Carolina Gomez, Yingqun Nian, Mark A E Auty, Joseph P Kerry, Ruth M Hamill
Meat intakes in the older population are commonly reduced because the relatively tough texture of meat can impair mastication. Fruit-derived proteolytic enzymes have been reported to have beneficial effects on tenderness, by causing significant degradation of myofibrillar proteins and collagen. Three treatments including: papain, bromelain and a 50:50 mixture of papain/bromelain, alongside one control were applied to beef M. semitendinosus steaks. Effects on Warner - Bratzler shear force, texture parameters, color, and cook loss were determined...
October 25, 2017: Journal of Texture Studies
https://www.readbyqxmd.com/read/29064679/mutation-of-asn-475-in-the-venezuelan-equine-encephalitis-virus-nsp2-cysteine-protease-leads-to-a-self-inhibited-state
#14
Jaimee R Compton, Matthew J Mickey, Xin Hu, Juan J Marugan, Patricia M Legler
The alphaviral nsP2 cysteine protease of the Venezuelan equine encephalitis virus (VEEV) is a validated antiviral drug target. Clan CN proteases contain a cysteine protease domain that is intimately packed with an S-adenosyl-l-methionine-dependent RNA methyltransferase (SAM MTase) domain. Within a cleft formed at the interface of these two domains, the peptide substrate is thought to bind. The nucleophilic cysteine can be found within a conserved motif, (475)NVCWAK(480), which differs from that of papain ((22)CGSCWAFS(29))...
November 9, 2017: Biochemistry
https://www.readbyqxmd.com/read/29043497/characterization-of-actinidia-virus-1-a-new-member-of-the-family-closteroviridae-encoding-a-thaumatin-like-protein
#15
A G Blouin, R Biccheri, M E Khalifa, M N Pearson, C Poggi Pollini, C Hamiaux, D Cohen, C Ratti
A new member of the family Closteroviridae was detected in Actinidia chinensis grown in Italy, using next generation sequencing of double-stranded RNA. The virus isolate, named Actinidia virus 1 (AcV-1) has a genome of 18,848 nts in length, a structure similar to the unclassified persimmon virus B (PeVB) and contains 12 open reading frames (ORFs) greater than 6 KDa, one carrying two papain-like leader proteases, a methyltransferase, a helicase and an RNA-dependent RNA polymerase domain. Additional ORFs code for homologs of heat shock protein 70, heat shock protein 90 and a coat protein...
October 17, 2017: Archives of Virology
https://www.readbyqxmd.com/read/29042963/warm-sparse-dense-wave-inhibits-cartilage-degradation-in-papain-induced-osteoarthritis-through-the-mitogen-activated-protein-kinase-signaling-pathway
#16
Munan Lin, Yanhong Lin, Xihai Li, Wenna Liang, Shuiliang Wang, Jiansheng Liu, Xianxiang Liu, Lidian Chen, Yin Qin
Cartilage degradation is an important in the pathogenesis of osteoarthritis (OA). Abnormal activation of the mitogen-activated protein kinase (MAPK) signaling pathway in chondrocytes promotes an inflammatory response, resulting in the release of chondral matrix-degrading enzymes that accelerate the degradation of cartilage. As a non-pharmaceutical and non-invasive physical therapy regimen, warm sparse-dense wave (WSDW) has been successfully used for the treatment of OA. However, it remains unclear whether WSDW inhibits cartilage degradation in OA through the MAPK signaling pathway...
October 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29039273/in-vitro-selection-of-phytomonas-serpens-cells-resistant-to-the-calpain-inhibitor-mdl28170-alterations-in-fitness-and-expression-of-the-major-peptidases-and-efflux-pumps
#17
Simone S C Oliveira, Inês C Gonçalves, Vitor Ennes-Vidal, Angela H C S Lopes, Rubem F S Menna-Barreto, Claudia M D'Ávila-Levy, André L S Santos, Marta H Branquinha
The species Phytomonas serpens is known to express some molecules displaying similarity to those described in trypanosomatids pathogenic to humans, such as peptidases from Trypanosoma cruzi (cruzipain) and Leishmania spp. (gp63). In this work, a population of P. serpens resistant to the calpain inhibitor MDL28170 at 70 µ m (MDLR population) was selected by culturing promastigotes in increasing concentrations of the drug. The only relevant ultrastructural difference between wild-type (WT) and MDLR promastigotes was the presence of microvesicles within the flagellar pocket of the latter...
October 17, 2017: Parasitology
https://www.readbyqxmd.com/read/29036575/peptides-of-the-variable-igg-domain-as-potential-biomarker-candidates-in-primary-open-angle-glaucoma-poag
#18
Carsten Schmelter, Natarajan Perumal, Sebastian Funke, Katharina Bell, Norbert Pfeiffer, Franz H Grus
Autoantibody profiling has gained increasing interest in the research field of glaucoma promising the detection of highly specific and sensitive marker candidates for future diagnostic purposes. Recent studies demonstrated that immune responses are characterized by the expression of congruent or similar complementarity determining regions (CDR) in different individuals and could be used as molecular targets in biomarker discovery. Main objective of this study was to characterize glaucoma-specific peptides from the variable region of sera-derived immunoglobulins using liquid chromatography--mass spectrometry (LC-MS)-based quantitative proteomics...
November 15, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/29031995/comparison-of-deproteinization-agents-on-bonding-to-developmentally-hypomineralized-enamel
#19
Manikandan Ekambaram, Robert P Anthonappa, Sharaschandra R Govindool, Cynthia Ky Yiu
OBJECTIVE: To compare bonding of dental adhesive to hypomineralized enamel (HE) after pre-treatment with either 5% sodium hypochlorite (NaOCl) solution or papain-based papacarie gel. METHODS: Normal enamel (NE) and HE obtained from hypomineralized first permanent molars were acid-etched with 32% phosphoric acid and randomly allocated into no deproteinization, deproteinization using 5% NaOCl, or deproteinization usping papacarie gel groups. Subsequently, the specimens were bonded, packed with composite resins and subjected to micro-shear bond strength (MSBS) testing and the data analysed using 2-way ANOVA and Tukey tests...
October 11, 2017: Journal of Dentistry
https://www.readbyqxmd.com/read/29023186/photodynamic-therapy-associated-with-a-blue-dye-papain-based-gel-and-evaluation-of-its-degradation-of-type-i-collagen-fibers
#20
Sergio Brossi Botta, Patricia Aparecida Ana, Marcela Leticia Leal Gonçalves, Kristianne Porta Santos Fernandes, Raquel Agnelli Mesquita-Ferrari, Renato de Araújo Prates, Aldo Brugnera Junior, Sandra Kalil Bussadori
OBJECTIVE: The aim of this in vitro study was to evaluate the degradation of type I collagen fibers after treatment with a papain-based gel associated with a blue dye (PapaMBlue™) for use in antimicrobial photodynamic therapy. MATERIALS AND METHODS: For such, 60 bioabsorbable membrane sponge discs were used. Group 1 was the negative control group. In groups 2, 3, and 4, the papain-based gel PapaMBlue gel was applied all over the samples for 4 min and irradiated using red laser (660 ± 10 nm) with 15, 30, and 40 J/cm(2), respectively...
October 12, 2017: Photomedicine and Laser Surgery
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