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1.
Mol Biotechnol ; 2024 Apr 23.
Article in English | MEDLINE | ID: mdl-38652428

ABSTRACT

Melanin is the major pigment responsible for the coloring of mammalian skin, hair, and eyes to defend against ultraviolet radiation. However, excessive melanin production has resulted in numerous types of hyperpigmentation disorders. Tyrosinase-related protein 1 (TYRP1) is a transmembrane glycoprotein enzyme found in many organisms, including humans, that plays an important role in melanogenesis. Thus, controlling the enzyme activity of TYRP1 with tyrosinase inhibitors is a vital step in the treatment of hyperpigmentation problems in humans. In the present investigation, virtual screening, pharmacokinetics, drug docking, and molecular dynamics (MD) simulation were used to find the most potent drug as an inhibitor of TYRP1 to effectively treat hyperpigmentation disorder. The 3D structure of TYRP1 was retrieved from the Protein Data Bank (PDB) database (PDB ID: 5M8M) and validated by the Ramachandran plot. Pharmacokinetics and drug-likeness showed that mycosporine 2 glycine (M2G) and shinorine (SHI) were the best compounds over other ligands in the same (P-1) structural pose. However, MD simulations of the M2G showed the highest CDOCKER interaction energy (-45.182 kcal/mol) and binding affinity (-65.0529 kcal/mol) as compared to SHI and reference drugs. The molecular binding modes RMSD and RMSF plots have exhibited more relevance to the M2G ligand in comparison to other drug ligands. The bioactivity and ligand efficiency profiles revealed that M2G is the most effective compound as a TYRP1 inhibitor. Thus, M2G could be used as a most effective drug for developing valuable sunscreen products to cure hyperpigmentation-related diseases.

2.
Viruses ; 15(6)2023 05 24.
Article in English | MEDLINE | ID: mdl-37376534

ABSTRACT

Since the onset of the coronavirus disease 2019 (COVID-19) pandemic, the virus kept developing and mutating into different variants over time, which also gained increased transmissibility and spread in populations at a higher pace, culminating in successive waves of COVID-19 cases. The scientific community has developed vaccines and antiviral agents against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) disease. Realizing that growing SARS-CoV-2 variations significantly impact the efficacy of antiviral therapies and vaccines, we summarize the appearance and attributes of SARS-CoV-2 variants for future perspectives in drug design, providing up-to-date insights for developing therapeutic agents targeting the variants. The Omicron variant is among the most mutated form; its strong transmissibility and immune resistance capacity have prompted international worry. Most mutation sites currently being studied are in the BCOV_S1_CTD of the S protein. Despite this, several hurdles remain, such as developing vaccination and pharmacological treatment efficacies for emerging mutants of SARS-CoV-2 strains. In this review, we present an updated viewpoint on the current issues faced by the emergence of various SARS-CoV-2 variants. Furthermore, we discuss the clinical studies conducted to assist the development and dissemination of vaccines, small molecule therapeutics, and therapeutic antibodies having broad-spectrum action against SARS-CoV-2 strains.


Subject(s)
COVID-19 , Vaccines , Humans , SARS-CoV-2/genetics , RNA, Viral , COVID-19/prevention & control
3.
Waste Manag ; 154: 175-186, 2022 Dec.
Article in English | MEDLINE | ID: mdl-36244206

ABSTRACT

This study presents a novel recycling scheme for spent Li-ion batteries that involves the leaching of lithium in hot water followed by the dissolution of all transition metals in HCl solution and their separation using the ionic liquid Cyphos IL104. The parametric studies revealed that >84 % Li was dissolved while the cathode material was leached at 90 °C for 2 h. Approximately 98 % Li from the non-acidic solution was directly precipitated as Li2CO3 at a Li+:CO32- ratio of 1:1.5. The transition metals from the Li-depleted cathode mass were efficiently (>98 %) dissolved in 3.0 mol·L-1 HCl at 90 °C for a 3 h leaching process. Manganese from the chloride leach liquor was selectively precipitated by adding KMnO4 at a 1.25-fold higher quantity than the stoichiometric ratio, pH value 2.0, and temperature 80 °C. The remaining co-existing metals (Ni and Co) were separated from the chloride solution by contacting it with a phosphonium-based ionic liquid at an equilibrium pH value of 5.4 and an organic-to-aqueous phase ratio of 2/3. The loaded ionic liquid was quantitatively stripped in 2.0 mol·L-1 H2SO4 solution, which yielded high-purity CoSO4·xH2O crystals after evaporation of the stripped liquor. Subsequently, ∼99 % nickel was recovered as nickel carbonate [NiCO3·2Ni(OH)2] from the Co-depleted raffinate by the precipitation performed at Ni2+:CO32- ratio of 1:2.5, pH value of 10.8, and temperature of 50 °C. Finally, a process flow with mass and energy balances yielding a high recovery rate of all metals in the exhausted cathode powder of spent LiBs was proposed.

4.
3 Biotech ; 12(10): 261, 2022 Oct.
Article in English | MEDLINE | ID: mdl-36082361

ABSTRACT

Pectin lyase (PNL) is an important enzyme of the pectinases group which degrades pectin polymer to 4,5-unsaturated oligogalacturonides by a unique ß-elimination mechanism and is used in several industries. The existence of multigene families of pectin lyases has been investigated by mining microbial genomes. In the present study, 52 pectin lyase genes were predicted from sequenced six species of Fusarium, namely F. fujikuroi, F. graminearum, F. proliferatum, F. oxysporum, F. verticillioides and F. virguliforme. These sequences were in silico characterized for several physico-chemical, structural and functional attributes. The translated PNL proteins showed variability with 344-1142 amino acid residues, 35.44-127.41 kDa molecular weight, and pI ranging from 4.63 to 9.28. The aliphatic index ranged from 75.33 to 84.75. Multiple sequence alignment analysis showed several conserved amino acid residues and five distinct groups marked as I, II, III, IV, and V were observed in the phylogenetic tree. The Three-dimensional Structure of five of these PNLs, each representing a distinct group of phylogenetic trees was predicted using I-TASSER Server and validated. The pectin lyase proteins of Fusarium species revealed close similarity with pectin lyase of Aspergillus niger PelA(1IDJ) and PelB(1QCX). Diversity in the structural motifs was observed among Fusarium species with 2 ß-sheets, 1 ß-hairpin, 7-12 ß bulges, 18-25 strands, 6 -11 helices, 1 helix-helix interaction, 32-49 ß turns, 2-6 γ turns and 2- 3 disulfide bonds. The unique Pec_lyase domain was uniformly observed among all PNL proteins confirming its identity. The genome-wide mining of Fusarium species was attempted to provide the diversity of PNL genes, which could be explored for diverse applications after performing cloning and expression studies. Supplementary Information: The online version contains supplementary material available at 10.1007/s13205-022-03333-w.

5.
Waste Manag ; 121: 175-185, 2021 Feb 15.
Article in English | MEDLINE | ID: mdl-33360816

ABSTRACT

This study has attempted to ascertain the linkages between circular bio-economy (CirBioeco) and recycling of electronic (e-)waste by applying microbial activities instead of the smelter and chemical technologies. To build the research hypothesis, the advances on biotechnology-driven recycling processes for metals extraction from e-waste has been analyzed briefly. Thereafter, based on the potential of microbial techniques and research hypothesis, the structural model has been tested for a significance level of 99%, which is supported by the corresponding standardization co-efficient values. A prediction model applied to determine the recycling impact on CirBioeco indicates to re-circulate 51,833 tons of copper and 58 tons of gold by 2030 for the production of virgin metals/raw-materials, while recycling rate of the accumulated e-waste remains to be 20%. This restoration volume of copper and gold through the microbial activities corresponds to mitigate 174 million kg CO2 emissions and 24 million m3 water consumption if compared with the primary production activities. The study potentially opens a new window for environmentally-friendly biotechnological recycling of e-waste under the umbrella concept of CirBioeco.


Subject(s)
Electronic Waste , Copper , Electronic Waste/analysis , Electronics , Gold , Recycling
6.
Mini Rev Med Chem ; 2020 08 07.
Article in English | MEDLINE | ID: mdl-32767940

ABSTRACT

The article has been withdrawn at the request of the authors and editor of the journal Mini-Reviews in Medicinal Chemistry due to incoherent content. Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused. The Bentham Editorial Policy on Article Withdrawal can be found at https://benthamscience.com/editorialpolicies-main.php Bentham Science Disclaimer: It is a condition of publication that manuscripts submitted to this journal have not been published and will not be simultaneously submitted or published elsewhere. Furthermore, any data, illustration, structure or table that has been published elsewhere must be reported, and copyright permission for reproduction must be obtained. Plagiarism is strictly forbidden, and by submitting the article for publication the authors agree that the publishers have the legal right to take appropriate action against the authors, if plagiarism or fabricated information is discovered. By submitting a manuscript, the authors agree that the copyright of their article is transferred to the publishers if and when the article is accepted for publication.

7.
Plant Physiol Biochem ; 151: 689-704, 2020 Jun.
Article in English | MEDLINE | ID: mdl-32353675

ABSTRACT

The maintenance of ROS homeostasis, membrane biogenesis and recycling of molecules are common stress responses involving specific and complex regulatory network. Ubiquitination is an important and common mechanism which facilitates environmental adaptation in eukaryotes. In the present study we have cloned the AlRabring7, an E3-Ub-ligase, previously identified as AlRab7 interacting partner. The role of AlRabring7 for ubiquitinating AlRab7 and facilitating stress tolerance is analysed. The AlRabring7, with an open-reading frame of 702 bp encodes a protein of 233 amino acids, with RING-HC domain of 40 amino acids. In silico analysis shows that AlRabring7 is a C3HC4-type RING E3 Ub ligase. The protein - protein docking show interaction dynamics between AlRab7-AlRabring7-Ubiquitin proteins. The AlRab7 and AlRabring7 transcript showed up-regulation in response to different salts i.e: NaCl, KCl, CaCl2, NaCl + KCl, NaCl + CaCl2, imposing ionic as well as hyperosmotic stress, and also with oxidative stress by H2O2 treatment. Interestingly, the AlRabring7 showed early transcript expression with maximum expression in shoots on combinatorial stresses. The AlRab7 showed delayed and maximum expression with NaCl + CaCl2 stress treatment. The AlRab7 complements yeast ypt7Δ mutants and restored the fragmented vacuole. The in vitro ubiquitination assay revealed that AlRabring7 function as E3 ubiquitin ligase and mediates AlRab7 ubiquitination. Overexpression of AlRab7 and AlRabring7 independently and when co-transformed enhanced the growth of yeast cells during stress conditions. Further, the bimolecular fluorescence complementation assay shows the in planta interaction of the two proteins. Our results suggest that AlRab7 and AlRabring7 confers enhanced stress tolerance in yeast.


Subject(s)
Oxidative Stress , Saccharomyces cerevisiae , Ubiquitin-Protein Ligases , Ubiquitination , Hydrogen Peroxide , Oxidative Stress/genetics , Saccharomyces cerevisiae/genetics , Saccharomyces cerevisiae/metabolism , Ubiquitin-Protein Ligases/metabolism , Ubiquitination/genetics
8.
Curr Genomics ; 20(7): 469-482, 2019 Nov.
Article in English | MEDLINE | ID: mdl-32655286

ABSTRACT

BACKGROUND: Low Birth Weight (LBW) (birth weight <2.5 Kg) newborns are associated with a high risk of infection, morbidity and mortality during their perinatal period. Compromised innate immune responses and inefficient hematopoietic differentiation in term LBW newborns led us to evaluate the gene expression status of hematopoiesis. MATERIALS AND METHODS: In this study, we compared our microarray datasets of LBW-Normal Birth Weight (NBW) newborns with two reference datasets to identify hematopoietic stem cells genes, and their differential expression in the LBW newborns, by hierarchical clustering algorithm using gplots and RcolorBrewer package in R. RESULTS: Comparative analysis revealed 108 differentially expressed hematopoiesis genes (DEHGs), of which 79 genes were up-regulated, and 29 genes were down-regulated in LBW newborns compared to their NBW counterparts. Moreover, protein-protein interactions, functional annotation and pathway analysis demonstrated that the up-regulated genes were mainly involved in cell proliferation and differentiation, MAPK signaling and Rho GTPases signaling, and the down-regulated genes were engaged in cell proliferation and regulation, immune system regulation, hematopoietic cell lineage and JAK-STAT pathway. The binding of down-regulated genes (LYZ and GBP1) with growth factor GM-CSF using docking and MD simulation techniques, indicated that GM-CSF has the potential to alleviate the repressed hematopoiesis in the term LBW newborns. CONCLUSION: Our study revealed that DEHGs belonged to erythroid and myeloid-specific lineages and may serve as potential targets for improving hematopoiesis in term LBW newborns to help build up their weak immune defense against life-threatening infections.

9.
Curr Drug Metab ; 20(6): 416-429, 2019.
Article in English | MEDLINE | ID: mdl-30227814

ABSTRACT

BACKGROUND: Nanotechnology is gaining significant attention worldwide for cancer treatment. Nanobiotechnology encourages the combination of diagnostics with therapeutics, which is a vital component of a customized way to deal with the malignancy. Nanoparticles are being used as Nanomedicine which participates in diagnosis and treatment of various diseases including cancer. The unique characteristic of Nanomedicine i.e. their high surface to volume ratio enables them to tie, absorb, and convey small biomolecule like DNA, RNA, drugs, proteins, and other molecules to targeted site and thus enhances the efficacy of therapeutic agents. OBJECTIVE: The objective of the present article is to provide an insight of several aspect of nanotechnology in cancer therapeutics such as various nanomaterials as drug vehicle, drug release strategies and role of nanotechnology in cancer therapy. METHODS: We performed an extensive search on bibliographic database for research article on nanotechnology and cancer therapeutics and further compiled the necessary information from various articles into the present article. RESULTS: Cancer nanotechnology confers a unique technology against cancer through early diagnosis, prevention, personalized therapy by utilizing nanoparticles and quantum dots.Nano-biotechnology plays an important role in the discovery of cancer biomarkers. Quantum dots, gold nanoparticles, magnetic nanoparticles, carbon nanotubes, gold nanowires etc. have been developed as a carrier of biomolecules that can detect cancer biomarkers. Nanoparticle assisted cancer detection and monitoring involves biomolecules like proteins, antibody fragments, DNA fragments, and RNA fragments as the base of cancer biomarkers. CONCLUSION: This review highlights various approaches of cancer nanotechnology in the advancement of cancer therapy.


Subject(s)
Nanomedicine/methods , Nanotechnology/methods , Neoplasms/diagnosis , Neoplasms/drug therapy , Dendrimers , Diagnostic Imaging , Genetic Therapy , Humans , Micelles , Nanoshells , Nanotubes , Phototherapy , Quantum Dots
10.
J Mech Behav Biomed Mater ; 75: 538-548, 2017 11.
Article in English | MEDLINE | ID: mdl-28850924

ABSTRACT

The study reports the synthesis and characterization of gelatin-tamarind gum (TG) based filled hydrogels for drug delivery applications. In this study, three different types of carbon nanotubes (CNTs) were incorporated within the dispersed TG phase of the filled hydrogels. The prepared hydrogels were thoroughly characterised using bright field microscope, FESEM, FTIR spectroscopy, differential scanning calorimeter, and mechanical tester. The swelling and the drug (salicylic acid) release properties of the filled hydrogels were also evaluated. The micrographs revealed the formation of biphasic systems. The internal phase appeared as agglomerates, and the CNTs were confined within the dispersed TG phase. FTIR and XRD studies revealed that CNTs promoted associative interactions among the components of the hydrogel, which promoted the formation of large crystallite size. The mechanical study indicated better resistance to the breakdown of the architecture of the CNT-containing filled hydrogels. Drug release studies, both passive and iontophoretic, suggested that the non-Fickian diffusion of the drug was prevalent during its release from hydrogel matrices. The prepared hydrogels were cytocompatible with human keratinocytes. The results suggested the probable use of such hydrogels in wound healing, tissue engineering and drug delivery applications.


Subject(s)
Drug Carriers/chemistry , Drug Liberation , Gelatin/chemistry , Hydrogels/chemistry , Keratinocytes/drug effects , Tamarindus/chemistry , Humans , Nanotubes, Carbon/chemistry
11.
Front Plant Sci ; 8: 819, 2017.
Article in English | MEDLINE | ID: mdl-28611792

ABSTRACT

The WRKY transcription factors (TFs), play crucial role in plant defense response against various abiotic and biotic stresses. The role of WRKY3 and WRKY4 genes in plant defense response against necrotrophic pathogens is well-reported. However, their functional annotation in tomato is largely unknown. In the present work, we have characterized the structural and functional attributes of the two identified tomato WRKY transcription factors, WRKY3 (SlWRKY3), and WRKY4 (SlWRKY4) using computational approaches. Arabidopsis WRKY3 (AtWRKY3: NP_178433) and WRKY4 (AtWRKY4: NP_172849) protein sequences were retrieved from TAIR database and protein BLAST was done for finding their sequential homologs in tomato. Sequence alignment, phylogenetic classification, and motif composition analysis revealed the remarkable sequential variation between, these two WRKYs. The tomato WRKY3 and WRKY4 clusters with Solanum pennellii showing the monophyletic origin and evolution from their wild homolog. The functional domain region responsible for sequence specific DNA-binding occupied in both proteins were modeled [using AtWRKY4 (PDB ID:1WJ2) and AtWRKY1 (PDBID:2AYD) as template protein structures] through homology modeling using Discovery Studio 3.0. The generated models were further evaluated for their accuracy and reliability based on qualitative and quantitative parameters. The modeled proteins were found to satisfy all the crucial energy parameters and showed acceptable Ramachandran statistics when compared to the experimentally resolved NMR solution structures and/or X-Ray diffracted crystal structures (templates). The superimposition of the functional WRKY domains from SlWRKY3 and SlWRKY4 revealed remarkable structural similarity. The sequence specific DNA binding for two WRKYs was explored through DNA-protein interaction using Hex Docking server. The interaction studies found that SlWRKY4 binds with the W-box DNA through WRKYGQK with Tyr408, Arg409, and Lys419 with the initial flanking sequences also get involved in binding. In contrast, the SlWRKY3 made interaction with RKYGQK along with the residues from zinc finger motifs. Protein-protein interactions studies were done using STRING version 10.0 to explore all the possible protein partners involved in associative functional interaction networks. The Gene ontology enrichment analysis revealed the functional dimension and characterized the identified WRKYs based on their functional annotation.

12.
Front Microbiol ; 7: 1899, 2016.
Article in English | MEDLINE | ID: mdl-27965634

ABSTRACT

Cyanobacteria are rich source of array of bioactive compounds. The present study reports a novel antibacterial bioactive compound purified from cyanobacterium Nostoc sp. MGL001 using various chromatographic techniques viz. thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Further characterization was done using electrospray ionization mass spectroscopy (ESIMS) and nuclear magnetic resonance (NMR) and predicted structure of bioactive compound was 9-Ethyliminomethyl-12-(morpholin - 4 - ylmethoxy) -5, 8, 13, 16-tetraaza-hexacene - 2, 3 dicarboxylic acid (EMTAHDCA). Structure of EMTAHDCA clearly indicated that it is a novel compound that was not reported in literature or natural product database. The compound exhibited growth inhibiting effects mainly against the gram negative bacterial strains and produced maximum zone of inhibition at 150 µg/mL concentration. The compound was evaluated through in silico studies for its ability to bind 30S ribosomal fragment (PDB ID: 1YRJ, 1MWL, 1J7T, and 1LC4) and OmpF porin protein (4GCP, 4GCQ, and 4GCS) which are the common targets of various antibiotic drugs. Comparative molecular docking study revealed that EMTAHDCA has strong binding affinity for these selected targets in comparison to a number of most commonly used antibiotics. The ability of EMTAHDCA to bind the active sites on the proteins and 30S ribosomal fragments where the antibiotic drugs generally bind indicated that it is functionally similar to the commercially available drugs.

13.
J Surg Case Rep ; 2016(5)2016 May 10.
Article in English | MEDLINE | ID: mdl-27165749

ABSTRACT

Patellar tendon rupture is an uncommon clinical presentation, which generally affects the under 40s who are active in sport. Bilateral rupture of both tendons is much rarer. It occurs most frequently in patients with predisposing factors such as corticosteroid use or systemic diseases. The authors present the case of a 56-year-old male on long-term statin therapy who sustained this injury following a fall on ice. He had no known risk factors for tendon rupture. Surgical treatment involved tendon repair using Krakow suture via bony tunnels in the patella. Statins have previously been associated with tendon ruptures at other sites but there have been no published cases of bilateral patellar tendon rupture linked to statin use. We review the literature regarding the association between statins and tendon rupture.

14.
Dalton Trans ; 45(4): 1443-54, 2016 Jan 28.
Article in English | MEDLINE | ID: mdl-26674056

ABSTRACT

Potassium salts of phenolate based polydentate xanthate ligands 4,4'-bis(2-dithiocarbonatobenzylideneamino)diphenyl ether () and 4,4'-bis(2-dithiocarbonatonaphthylmethylideneamino)diphenyl ether () have been synthesized and characterized, prior to use. The reaction of or with M(OAc)2 in Et3N affords access to a rare series of binuclear metallomacrocyclic xanthate complexes of the type [M2-µ(2)-bis-(κ(2)S,S-xan(1)/xan(2))] () which quickly forms [2 : 2] binuclear N,O-bidentate Schiff base macrocyclic complexes of the type [M2-µ(2)-bis-(κ(2)N,O-L(1)/L(2))] ( = 4,4'-bis(2-hydroxybenzylideneamino)diphenyl ether, = 4,4'-bis(2-hydroxynaphthylmethylidene-amino)diphenyl ether) via evolution of CS2 in solution. The compounds were characterized by microanalysis, relevant spectroscopy (FT-IR, UV-visible), mass spectrometry (ESI-MS), and powder and single crystal XRD techniques. In vitro anticancer activity of all the compounds was evaluated against HEP 3B (hepatoma) and IMR 32 (neuroblastoma) by the MTT assay. Remarkably, the binuclear copper(ii) xanthate complexes were found to be extremely active against both the cell lines (IC50: 8.1 ± 0.8 µM (), 8.8 ± 1.7 µM () against HEP 3B and 1.9 ± 0.3 µM () and 7.3 ± 0.6 µM () against IMR 32) and this projects them as good candidates for potent antitumor agents and the IC50 values confirm their better potency than the reference drug cisplatin. The flow-cytometric density plot illustrates the induction of apoptosis in HEP 3B and IMR 32 cells after treatment with , , , and .


Subject(s)
Antineoplastic Agents/pharmacology , Cobalt/pharmacology , Copper/pharmacology , Macrocyclic Compounds/pharmacology , Organometallic Compounds/pharmacology , Phenols/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Apoptosis/drug effects , Cell Proliferation/drug effects , Cell Survival/drug effects , Cobalt/chemistry , Copper/chemistry , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Macrocyclic Compounds/chemical synthesis , Macrocyclic Compounds/chemistry , Molecular Structure , Organometallic Compounds/chemical synthesis , Organometallic Compounds/chemistry , Phenols/chemistry , Schiff Bases/chemistry , Schiff Bases/pharmacology , Structure-Activity Relationship , Tumor Cells, Cultured
15.
J Mech Behav Biomed Mater ; 55: 250-263, 2015 Mar.
Article in English | MEDLINE | ID: mdl-26594784

ABSTRACT

The current study reports the development and characterization of soy lecithin based novel self-assembled emulsion hydrogels. Sesame oil was used as the representative oil phase. Emulsion gels were formed when the concentration of soy lecithin was >40% w/w. Metronidazole was used as the model drug for the drug release and the antimicrobial tests. Microscopic study showed the apolar dispersed phase in an aqueous continuum phase, suggesting the formation of emulsion hydrogels. FTIR study indicated the formation of intermolecular hydrogen bonding, whereas, the XRD study indicated predominantly amorphous nature of the emulsion gels. Composition dependent mechanical and drug release properties of the emulsion gels were observed. In-depth analyses of the mechanical studies were done using Ostwald-de Waele power-law, Kohlrausch and Weichert models, whereas, the drug release profiles were modeled using Korsmeyer-Peppas and Peppas-Sahlin models. The mechanical analyses indicated viscoelastic nature of the emulsion gels. The release of the drug from the emulsion gels was diffusion mediated. The drug loaded emulsion gels showed good antimicrobial activity. The biocompatibility test using HaCaT cells (human keratinocytes) suggested biocompatibility of the emulsion gels.


Subject(s)
Anti-Bacterial Agents/chemistry , Biocompatible Materials/chemistry , Drug Carriers/chemistry , Glycine max/chemistry , Hydrogels/chemistry , Lecithins/chemistry , Anti-Bacterial Agents/pharmacology , Bacillus subtilis/drug effects , Biocompatible Materials/pharmacology , Cell Line , Cell Survival/drug effects , Drug Carriers/pharmacology , Drug Liberation , Emulsions , Escherichia coli/drug effects , Humans , Lecithins/pharmacology , Mechanical Phenomena , Metronidazole/chemistry
16.
AAPS PharmSciTech ; 16(6): 1254-62, 2015 Dec.
Article in English | MEDLINE | ID: mdl-25771735

ABSTRACT

The present study discusses about the preparation and characterization (thermal, mechanical, and electrical) of the genipin-crosslinked gelatin emulgels. Emulgels have gained importance in recent years due to their improved stability than emulsions and ability to control the drug release. Mustard oil was used as the representative oil. A decrease in the enthalpy and entropy of the formulations was observed with the increase in the oil fraction. The mechanical studies suggested formation of softer emulgels as the oil fraction was increased. As the proportion of the oil fraction was increased in the emulgels, there was a corresponding increase in the impedance. The drug release properties from the emulgels were also studied. Ciprofloxacin was used as the model antimicrobial drug. The drug release was higher from the emulgels whose electrical conductivity was higher.


Subject(s)
Emulsions/chemistry , Gelatin/chemistry , Gels/chemistry , Iridoids/chemistry , Anti-Infective Agents/administration & dosage , Anti-Infective Agents/chemistry , Chemistry, Pharmaceutical/methods , Ciprofloxacin/administration & dosage , Ciprofloxacin/chemistry , Drug Liberation , Electricity , Emulsions/administration & dosage , Gelatin/administration & dosage , Gels/administration & dosage , Iridoids/administration & dosage
17.
PLoS One ; 10(2): e0117823, 2015.
Article in English | MEDLINE | ID: mdl-25658941

ABSTRACT

YhdE, a Maf-like protein in Escherichia coli, exhibits nucleotide pyrophosphatase (PPase) activity, yet its cellular function remains unknown. Here, we characterized the PPase activity of YhdE on dTTP, UTP and TTP and determined two crystal structures of YhdE, revealing 'closed' and 'open' conformations of an adaptive active site. Our functional studies demonstrated that YhdE retards cell growth by prolonging the lag and log phases, particularly under stress conditions. Morphology studies showed that yhdE-knockout cells transformed the normal rod shape of wild-type cells to a more spherical form, and the cell wall appeared to become more flexible. In contrast, YhdE overexpression resulted in filamentous cells. This study reveals the previously unknown involvement of YhdE in cell growth inhibition under stress conditions, cell-division arrest and cell-shape maintenance, highlighting YhdE's important role in E. coli cell-cycle checkpoints.


Subject(s)
Cell Cycle Checkpoints/physiology , Escherichia coli Proteins/metabolism , Escherichia coli/enzymology , Pyrophosphatases/metabolism , Escherichia coli/genetics , Escherichia coli Proteins/genetics , Gene Knockdown Techniques , Pyrophosphatases/genetics
18.
J Mater Sci Mater Med ; 26(2): 118, 2015 Feb.
Article in English | MEDLINE | ID: mdl-25672596

ABSTRACT

The current study describes the in-depth characterization of agar-gelatin based co-hydrogels, emulgels and bigels to have an insight about the differences in the properties of the formulations. Hydrogels have been extensively studied as vehicle for controlled drug release, whereas, the concept of emulgels and bigels is relatively new. The formulations were characterized by scanning electron microscopy, FTIR spectroscopy, XRD and mechanical properties. The biocompatibility and the ability of the formulations to be used as drug delivery vehicle were also studied. The scanning electron micrographs suggested the presence of internal phases within the agar-gelatin composite matrices of co-hydrogel, emulgel and bigel. FTIR and XRD studies suggested higher crystallinity of emulgels and bigels. Electrical impedance and mechanical stability of the emulgel and the bigel was higher than the hydrogel. The prepared formulations were found to be biocompatible and suitable for drug delivery applications.


Subject(s)
Agar/chemistry , Delayed-Action Preparations/chemical synthesis , Gelatin/chemistry , Hydrogels/chemistry , Metronidazole/chemistry , Anti-Infective Agents/administration & dosage , Anti-Infective Agents/chemistry , Compressive Strength , Diffusion , Elastic Modulus , Hardness , Materials Testing , Metronidazole/administration & dosage , Phase Transition
19.
Mater Sci Eng C Mater Biol Appl ; 48: 688-99, 2015 Mar.
Article in English | MEDLINE | ID: mdl-25579972

ABSTRACT

Stearic acid and its derivatives have been used as gelators in food and pharmaceutical gel formulations. However, the mechanism pertaining to the stearic acid based gelation has not been deciphered yet. Keeping that in mind, we investigated the role of stearic acid on physic-chemical properties of oleogel. For this purpose, two different oil (sesame oil and soy bean oil) formulations/oleogels were prepared. In depth analysis of gel kinetics, gel microstructure, molecular interactions, thermal and mechanical behaviors of the oleogels were done. The properties of the oleogels were dependent on the type of the vegetable oil used and the concentration of the stearic acid. Avrami analysis of DSC thermograms indicated that heterogeneous nucleation was coupled with the one-dimensional growth of gelator fibers as the key phenomenon in the formation of oleogels. Viscoelastic and pseudoplastic nature of the oleogels was analyzed in-depth by fitting the stress relaxation data in modified Peleg's model and rheological studies, respectively. Textural studies have revealed that the coexistence of hydrogen bond dissipation and formation of new bonds is possible under stress conditions in the physical oleogels.


Subject(s)
Sesame Oil/chemistry , Soybean Oil/chemistry , Stearic Acids/chemistry , Elasticity , Hot Temperature , Organic Chemicals/chemistry , Viscosity
20.
J Mech Behav Biomed Mater ; 43: 1-17, 2015 Mar.
Article in English | MEDLINE | ID: mdl-25549573

ABSTRACT

Over the past decade, researchers have been trying to develop alternative gel based formulations in comparison to the traditional hydrogels and emulgels. In this perspective, bigels were synthesized by mixing gelatin hydrogel and stearic acid based organogel by hot emulsification method. Two types of bigels were synthesized using sesame oil and soy bean oil based stearate organogels. Gelatin based emulgels prepared using sesame oil and soy bean oil were used as the controls. Microscopic studies revealed that the bigels contained aggregates of droplets, whereas, emulgels showed dispersed droplets within the continuum phase. The emulgels showed higher amount of leaching of oils, whereas, the leaching of the internal phase was negligible from the bigels. Presence of organogel matrix within the bigels was confirmed by XRD, FTIR and DSC methods. Bigels showed higher mucoadhesive and mechanical properties compared to emulgels. Cyclic creep-recovery and stress relaxation studies confirmed the viscoelastic nature of the formulations. Four elemental Burger's model was employed to analyze the cyclic creep-recovery data. Cyclic creep-recovery studies suggested that the deformation of the bigels were lower due to the presence of the organogels within its structure. The formulations showed almost 100% recovery after the creep stage and can be explained by the higher elastic nature of the formulations. Stress relaxation study showed that the relaxation time was higher in the emulgels as compared to the bigels. Also, the % relaxation was higher in emulgels suggesting its fluid dominant nature. The in vitro biocompatibility of the bigels was checked using human epidermal keratinocyte cell line (HaCaT). Both emulgels and bigels were biocompatible in nature. The in vitro drug (ciprofloxacin) release behavior indicated non-Fickian diffusion of the drug from the matrices. The drug release showed good antimicrobial effect against Escherichia coli. Based on the results, it was concluded that the developed bigels may have huge potential to be used as alternatives to emulgels.


Subject(s)
Chemical Phenomena , Drug Carriers/chemistry , Gelatin/chemistry , Hydrogels/chemistry , Mechanical Phenomena , Stearates/chemistry , Temperature , Ciprofloxacin/chemistry , Ciprofloxacin/pharmacology , Drug Carriers/pharmacology , Drug Liberation , Escherichia coli/drug effects , Humans , Keratinocytes/cytology , Keratinocytes/drug effects , Materials Testing , Stearates/pharmacology
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