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1.
J Ethnopharmacol ; 324: 117763, 2024 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-38253274

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Sri Lankan traditional medicine uses Vernonia zeylanica and Mallotus repandus broadly for the treatment of a multitude of disease conditions, including wound healing. AIM OF THE STUDY: We aimed to scientifically validate the safety and efficacy of wound healing of an aqueous distillate of Vernonia zeylanica and Mallotus repandus (ADVM) mature leaves, tested on primary human dermal fibroblasts. MATERIALS AND METHODS: Human dermal fibroblasts isolated from clinical waste from circumcision surgery were characterized by flowcytometry and trilineage differentiation. The MTT dye reduction assay, and the ex vivo wound healing scratch assay established wound healing properties of ADVM using the primary human dermal fibroblast cell line. Upregulation of genes associated with wound healing (MMP3, COL3A1, TGFB1, FGF2) were confirmed by RT qPCR. GC-MS chromatography evaluated the phytochemical composition of ADVM. RESULTS: Compared to the synthetic stimulant, ß fibroblast growth factor, ADVM at 0.25% concentration on the primary dermal fibroblast cell line exhibited significant ex vivo, (i) 1.7-fold % cell viability (178.7% vs 304.3 %, p < 0.001), (ii) twofold greater % wound closure (%WC) potential (47.74% vs 80.11%, p < 0.001), and (iii) higher rate of % WC (3.251 vs 3.456 % WC/h, p < 0.05), sans cyto-genotoxicity. Up regulated expression of FGF2, TGFB1, COL3A1 and MMP3, genes associated with wound healing, confirmed effective stimulation of pathways of the three overlapping phases of wound healing (P < 0.05). GC-MS profile of ADVM characterized four methyl esters, which may be posited as wound healing phytochemicals. CONCLUSIONS: Exceeding traditional medicine claims, the exvivo demonstration of rapid skin regeneration, reiterated by upregulated expression of genes related to wound healing pathways, sans cytotoxicity, propounds ADVM, cued from traditional medicine, as a potential safe and effective natural stimulant for rapid wound-healing. Additionally, it may serve as an effective proliferative stimulant of dermal fibroblasts for cell therapy, with potential in reparative and regenerative therapy of skin disorders.


Assuntos
Mallotus (Planta) , Vernonia , Masculino , Humanos , Metaloproteinase 3 da Matriz/metabolismo , Fator 2 de Crescimento de Fibroblastos/metabolismo , Extratos Vegetais/química , Cicatrização , Pele , Medicina Tradicional , Fibroblastos
2.
Sci Rep ; 13(1): 12859, 2023 08 08.
Artigo em Inglês | MEDLINE | ID: mdl-37553373

RESUMO

Bats are described as the natural reservoir host for a wide range of viruses. Although an increasing number of bat-associated, potentially human pathogenic viruses were discovered in the past, the full picture of the bat viromes is not explored yet. In this study, the virome composition of Miniopterus phillipsi bats (formerly known as Miniopterus fuliginosus bats in Sri Lanka) inhabiting the Wavul Galge cave, Sri Lanka, was analyzed. To assess different possible excretion routes, oral swabs, feces and urine were collected and analyzed individually by using metagenomic NGS. The data obtained was further evaluated by using phylogenetic reconstructions, whereby a special focus was set on RNA viruses that are typically associated with bats. Two different alphacoronavirus strains were detected in feces and urine samples. Furthermore, a paramyxovirus was detected in urine samples. Sequences related to Picornaviridae, Iflaviridae, unclassified Riboviria and Astroviridae were identified in feces samples and further sequences related to Astroviridae in urine samples. No viruses were detected in oral swab samples. The comparative virome analysis in this study revealed a diversity in the virome composition between the collected sample types which also represent different potential shedding routes for the detected viruses. At the same time, several novel viruses represent first reports of these pathogens from bats in Sri Lanka. The detection of two different coronaviruses in the samples indicates the potential general persistence of this virus species in M. phillipsi bats. Based on phylogenetics, the identified viruses are closely related to bat-associated viruses with comparably low estimation of human pathogenic potential. In further studies, the seasonal variation of the virome will be analyzed to identify possible shedding patterns for particular viruses.


Assuntos
Quirópteros , Coronavirus , Animais , Humanos , Filogenia , Viroma , Sri Lanka , Coronavirus/genética
3.
Bioinorg Chem Appl ; 2022: 7821284, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36147773

RESUMO

Platinum-based compounds are actively used in clinical trials as anticancer agents. In this study, two novel platinum complexes, (C1 = [PtCl2(N(SO2quin)dpa)], C2 = [PtCl2(N(SO2azobenz)dpa)]) containing quinoline and azobenzene appended dipicolylamine sulfonamide ligands were synthesized in good yield. The singlet attributable to methylene CH2 protons of the ligands of C1 and C2 appears as two doublets in 1H NMR spectra, which confirms the presence of magnetically nonequivalent protons upon coordination to platinum. Structural data of N(SO2quin)dpa (L1), N(SO2azobenz)dpa (L2) and PtCl2(N(SO2quin)dpa) confirmed the formation of the desired compounds. Time-dependent density functional theory calculations suggested that the excitation of L1 show quin-unit-based π⟶π ∗ excitations (i.e., ligand-centered charge transfer, LC), while C1 shows the metal-ligand-to-ligand charge-transfer (MLLCT) character. L1 displays intense fluorescence from the 1LC excited state, while C1 gives phosphorescence from the 3LC state. Mammalian cell toxicity of ligands and complexes was assessed with NCI-H292 nonsmall-cell lung cancer cells. Further, C1 and C2 showed significantly low IC50 values compared with N(SO2azobenz)dpa and PtCl2(N(SO2quin)dpa). Fluorescence imaging data of both ligands and complexes revealed the potential fluorescence activity of these compounds for biological imaging. All four compounds are promising novel candidates that can be further investigated on their usage as potential anticancer agents and cancer cell imaging agents.

4.
Animals (Basel) ; 12(13)2022 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-35804573

RESUMO

This is the first report on the molecular identification and phylogeny of the Rousettus leschenaultii Desmarest, 1810, Rhinolophus rouxii Temminck, 1835, Hipposideros speoris Schneider, 1800, Hipposideros lankadiva Kelaart, 1850, and Miniopterus fuliginosus Kuhl, 1817, bat species in Sri Lanka, inferred from analyses by mitochondrially encoded cytochrome b gene sequences. Recent research has indicated that bats show enormous cryptic genetic diversity. Moreover, even within the same species, the acoustic properties of echolocation calls and morphological features such as fur color could vary in different populations. Therefore, we have used molecular taxonomy for the accurate identification of five bat species recorded in one of the largest cave populations in Sri Lanka. The bats were caught using a hand net, and saliva samples were collected non-invasively from each bat by using a sterile oral swab. Nucleic acids were extracted from the oral swab samples, and mitochondrial DNA was amplified by using primers targeting the mitochondrially encoded cytochrome b gene. This study reports the first molecular evidence for the identification of five bat species in Sri Lanka. Our findings will contribute to future conservation and systematic studies of bats in Sri Lanka. This study will also provide the basis for a genetic database of Sri Lankan bats which will contribute significantly to the investigation of potentially zoonotic bat viruses.

5.
Pathogens ; 11(4)2022 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-35456109

RESUMO

Bats are known as typical reservoirs for a number of viruses, including viruses of the family Paramyxoviridae. Representatives of the subfamily Orthoparamyxovirinae are distributed worldwide and can cause mild to fatal diseases when infecting humans. The research on Paramyxoviruses (PMVs) from different bat hosts all over the world aims to understand the diversity, evolution and distribution of these viruses and to assess their zoonotic potential. A high number of yet unclassified PMVs from bats are recorded. In our study, we investigated bat species from the families Rhinolophidae, Hipposiderae, Pteropodidae and Miniopteridae that are roosting sympatrically in the Wavul Galge cave (Koslanda, Sri Lanka). The sampling at three time points (March and July 2018; January 2019) and screening for PMVs with a generic PCR show the presence of different novel PMVs in 10 urine samples collected from Miniopterus fuliginosus. Sequence analysis revealed a high similarity of the novel strains among each other and to other unclassified PMVs collected from Miniopterus bats. In this study, we present the first detection of PMVs in Sri Lanka and the presence of PMVs in the bat species M. fuliginosus for the first time.

6.
Viruses ; 14(2)2022 02 07.
Artigo em Inglês | MEDLINE | ID: mdl-35215931

RESUMO

Coronaviruses (CoV) are divided into the genera α-CoVs, ß-CoVs, γ-CoVs and δ-CoVs. Of these, α-CoVs and ß-CoVs are solely capable of causing infections in humans, resulting in mild to severe respiratory symptoms. Bats have been identified as natural reservoir hosts for CoVs belonging to these two genera. Consequently, research on bat populations, CoV prevalence in bats and genetic characterization of bat CoVs is of special interest to investigate the potential transmission risks. We present the genome sequence of a novel α-CoV strain detected in rectal swab samples of Miniopterus fuliginosus bats from a colony in the Wavul Galge cave (Koslanda, Sri Lanka). The novel strain is highly similar to Miniopterus bat coronavirus 1, an α-CoV located in the subgenus of Minunacoviruses. Phylogenetic reconstruction revealed a high identity of the novel strain to other α-CoVs derived from Miniopterus bats, while human-pathogenic α-CoV strains like HCoV-229E and HCoV-NL63 were more distantly related. Comparison with selected bat-related and human-pathogenic strains of the ß-CoV genus showed low identities of ~40%. Analyses of the different genes on nucleotide and amino acid level revealed that the non-structural ORF1a/1b are more conserved among α-CoVs and ß-CoVs, while there are higher variations in the structural proteins known to be important for host specificity. The novel strain was named batCoV/MinFul/2018/SriLanka and had a prevalence of 50% (66/130) in rectal swab samples and 58% (61/104) in feces samples that were collected from Miniopterus bats in Wavul Galge cave. Based on the differences between strain batCoV/MinFul/2018/SriLanka and human-pathogenic α-CoVs and ß-CoVs, we conclude that there is a rather low transmission risk to humans. Further studies in the Wavul Galge cave and at other locations in Sri Lanka will give more detailed information about the prevalence of this virus.


Assuntos
Alphacoronavirus/genética , Alphacoronavirus/isolamento & purificação , Quirópteros/virologia , Infecções por Coronavirus/veterinária , Reservatórios de Doenças/veterinária , Reservatórios de Doenças/virologia , Genoma Viral , Alphacoronavirus/classificação , Animais , Cavernas/virologia , Infecções por Coronavirus/virologia , Evolução Molecular , Feminino , Masculino , Filogenia , Análise de Sequência de DNA , Sri Lanka
7.
Biodegradation ; 33(2): 117-133, 2022 04.
Artigo em Inglês | MEDLINE | ID: mdl-34989928

RESUMO

Application of genetically engineered bacterial strains for biodegradation of hydrocarbons is a sustainable solution for treating pollutants as well as in industrial applications. However, the process of bioengineering should be carefully carried out to optimize the output. Investigation of regulatory genes for bioengineering is essential for developing synthetic circuits for effective biocatalysts. Here we focus on LcaR, a putative transcriptional regulator affecting the expression of alkB2 and lcaR operon that has a high potential to become a tool in designing such pathways. Four LcaR dimers bind specifically to the upstream regulatory region where divergent promoters of alkB2 and lcaR genes are located with high affinity at a Kd of 0.94 ± 0.17 nM and a Hill coefficient is 1.7 ± 0.3 demonstrating cooperativity in the association. Ligand binding alters the conformation of LcaR, which releases the regulator from its cognate DNA. Tetradecanal and hexadecanal act as natural ligands of LcaR with an IC50 values of 3.96 ± 0.59 µg/ml and 0.68 ± 0.21 µg/ml, respectively. The structure and function of transcription factors homologous to LcaR have not been characterized to date. This study provides insight into regulatory mechanisms of alkane degradation with a direction towards potential applications in bioengineering for bioremediation and industrial applications.


Assuntos
Alcanos , Pseudomonas aeruginosa , Alcanos/metabolismo , Proteínas de Bactérias/metabolismo , Biodegradação Ambiental , Bioengenharia , Pseudomonas aeruginosa/metabolismo
8.
Biology (Basel) ; 10(12)2021 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-34943156

RESUMO

Mycobacterium tuberculosis is a well-known pathogen due to the emergence of drug resistance associated with it, where transcriptional regulators play a key role in infection, colonization and persistence. The genome of M. tuberculosis encodes many transcriptional regulators, and here we report an in-depth in silico characterization of a GntR regulator: MoyR, a possible monooxygenase regulator. Homology modelling provided a reliable structure for MoyR, showing homology with a HutC regulator DasR from Streptomyces coelicolor. In silico physicochemical analysis revealed that MoyR is a cytoplasmic protein with higher thermal stability and higher pI. Four highly probable binding pockets were determined in MoyR and the druggability was higher in the orthosteric binding site consisting of three conserved critical residues: TYR179, ARG223 and GLU234. Two highly conserved leucine residues were identified in the effector-binding region of MoyR and other HutC homologues, suggesting that these two residues can be crucial for structure stability and oligomerization. Virtual screening of drug leads resulted in four drug-like compounds with greater affinity to MoyR with potential inhibitory effects for MoyR. Our findings support that this regulator protein can be valuable as a therapeutic target that can be used for developing drug leads.

9.
Vaccines (Basel) ; 9(6)2021 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-34203592

RESUMO

Bats are known to be potential reservoirs of numerous human-pathogenic viruses. They have been identified as natural hosts for coronaviruses, causing Severe Acute Respiratory Syndrome (SARS) in humans. Since the emergence of SARS-CoV-2 in 2019 interest in the prevalence of coronaviruses in bats was newly raised. In this study we investigated different bat species living in a sympatric colony in the Wavul Galge cave (Koslanda, Sri Lanka). In three field sessions (in 2018 and 2019), 395 bats were captured (Miniopterus, Rousettus, Hipposideros and Rhinolophus spp.) and either rectal swabs or fecal samples were collected. From these overall 396 rectal swab and fecal samples, the screening for coronaviruses with nested PCR resulted in 33 positive samples, 31 of which originated from Miniopterus fuliginosus and two from Rousettus leschenaultii. Sanger sequencing and phylogenetic analysis of the obtained 384-nt fragment of the RNA-dependent RNA polymerase revealed that the examined M. fuliginosus bats excrete alphacoronaviruses and the examined R. leschenaultii bats excrete betacoronaviruses. Despite the sympatric roosting habitat, the coronaviruses showed host specificity and seemed to be limited to one species. Our results represent an important basis to better understand the prevalence of coronaviruses in Sri Lankan bats and may provide a basis for pursuing studies on particular bat species of interest.

10.
RSC Adv ; 11(29): 17658-17668, 2021 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-35480201

RESUMO

Three new Pt complexes, [PtCl2(N(SO2(2-nap))dpa)], [PtCl2(N(SO2(1-nap))dpa)] and [PtCl2(N(SO2pip)dpa)], containing a rare 8-membered ring were synthesized in good yield and high purity by utilizing the ligands N(SO2(2-nap))dpa, N(SO2(1-nap))dpa and N(SO2pip)dpa, which contain a dipicolylamine moiety. Structural studies of all three complexes confirmed that the ligands are bound in a bidentate mode via Pt-N(pyridyl) bonds forming a rare 8-membered ring. The intense fluorescence displayed by the ligands is quenched upon coordination to Pt. According to time dependent density functional theory (TDDFT) calculations, the key excitations of N(SO2(2-nap))dpa and [PtCl2(N(SO2(1-nap))dpa)] involve the 2-nap-ligand-centered π → π* excitations. While all six compounds have shown antiproliferative activity against human breast cancer cells (MCF-7), the N(SO2pip)dpa and N(SO2(2-nap))dpa ligands and [PtCl2((NSO2pip)dpa)] complex have shown significantly high cytotoxicity, directing them to be further investigated as potential anti-cancer drug leads.

11.
J Pharm Sci ; 109(2): 1130-1135, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-31568775

RESUMO

A sustained-release carrier system for the drug cephalexin (CEF) using functionalized graphene oxide is reported. PEGylation of GO (GO-PEG) and successful loading of CEF into PEGylated graphene oxide (GO-PEG-CEF) nanoconjugate are confirmed by Fourier transform infrared spectroscopy, Raman spectroscopy, and thermogravimetric analysis. Encapsulation efficiency of 69% and a loading capacity of 19% are obtained with the optimized formulation of GO-PEG-CEF. In vitro CEF release profiles show an initial burst release followed by a more sustained release over a 96 h period with cumulative release of 80%. The half maximal inhibitory concentration (IC50) values have both dose- and time-dependent antibacterial activity for GO-PEG-CEF against both gram-positive and gram-negative bacteria while pure CEF showed only dose-dependent antibacterial activity. The minimum inhibitory concentration values of GO-PEG-CEF are 7.8 and 3.9 µg/mL against S. aureus and B. cereus, respectively, while it is 10 µg/mL with pure CEF against both gram-positive bacteria. This confirms the enhanced antibacterial activity of GO-PEG-CEF over pure CEF against gram-positive bacteria. These findings therefore show GO-PEG-CEF is promising as a sustained-release nanoantibiotic system for effective treatment against S. aureus and B. cereus infections.


Assuntos
Grafite , Nanocompostos , Antibacterianos/farmacologia , Cefalexina , Preparações de Ação Retardada , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Staphylococcus aureus
12.
J Loss Prev Process Ind ; 61: 1-7, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31745379

RESUMO

Correctly applied rock dust can dilute, inert, and mitigate the explosive potential of float coal dust. Trickle dusters are one element of a comprehensive system to help prevent coal dust explosions in underground coal mines. Trickle dusters supply rock dust to inert fine float coal dust in areas where it is commonly deposited, such as the longwall tailgate returns, return airways, pillaring areas, and downwind of belt transfers. Dust deposition studies show that the effectiveness of trickle dusters depends on several key factors. Using multiple orifices, rock dust should be released near the mine roof in the direction of the airflow in order to spread the cloud cross the entry. The rock duster should have a mechanism to break up rock dust agglomerates as they leave the rock duster. The particle size distribution of the limestone rock dust and its airborne concentration should be proportional to the airborne size distribution and concentration of coal dust passing by the trickle duster. Specifically, rock dusts having a greater proportion of <74 µm material are more effective at minimizing downwind zones of explosible mixtures than mostly larger particles. In our testing, rock dusts having more than 95% of <74 µm sized particles were adequately dispersed by trickle dusters. Based on our results, the mass rate of rock dust discharge from the trickle duster should exceed the rate of float coal production by at least a factor of four in order to minimize accumulations of explosible dusts.

13.
Microbiologyopen ; 8(5): e00723, 2019 05.
Artigo em Inglês | MEDLINE | ID: mdl-30221843

RESUMO

The study aimed to determine the antibacterial/antibiofilm effect and mechanism of interaction of curcuminoids-intercalated Mg/Al layered double hydroxide (curcuminoids-LDH) against three different bacteria. Antimicrobial effect of curcuminoids-LDH nanohybrid was investigated against P. aeruginosa, S. aureus, and E. faecalis (for both standard strains and clinical isolates), using agar well diffusion method. Minimum inhibitory concentrations (MIC) of planktonic bacteria were determined using the broth microdilution method. MIC of biofilms (MBIC50 ) and killing time for 48 hr matured biofilms were determined by MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Scanning electron microscopy (SEM) was used to determine pre- and postexposure architecture of biofilms. The mechanism of the antibiofilm activity of curcuminoids-LDH was determined using UV-visible spectroscopy. All tested bacteria had given a zone of inhibition in the presence of curcuminoids-LDH. The MIC values were 0.200 g/ml for P. aeruginosa, 0.025 g/ml for S. aureus, and 0.100 g/ml for E. faecalis. The 48 hr matured biofilms were reduced by curcuminoids-LDH with an MBIC50 of 0.100 g/ml. The minimum time to achieve MBIC50 was 3 hr, and the reduction was constant until 48 hr. SEM images showed a significant reduction of biofilm cell density and exopolymer matrics for all biofilms in the presence of curcuminoids-LDH. UV-visible studies revealed the antibiofilm activity of curcuminoids-LDH as due to the auto-oxidation of curcuminoids. The oxidation products are more limited in both product concentration per unit time and the variety of products, compared to pure curcuminoids, resulting in sharper UV-visible peaks than in the case of the latter. Curcuminoids-LDH has a potential antibacterial activity against P. aeruginosa, S. aureus, and E. faecalis. An antibiofilm activity has been achieved within 3 hr of the treatment. Curcuminoids released from the LDH showed the antibacterial activity due to oxidation products interfering with bacterial cell functions, and also encapsulation in the LDH causes curcuminoids to exhibit the activity in a persistent manner compared to pure curcuminoids.


Assuntos
Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Diarileptanoides/farmacologia , Enterococcus faecalis/efeitos dos fármacos , Nanocompostos , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Hidróxido de Alumínio/farmacologia , Meios de Cultura , Hidróxido de Magnésio/farmacologia , Testes de Sensibilidade Microbiana , Viabilidade Microbiana/efeitos dos fármacos
14.
Bioinorg Chem Appl ; 2018: 2530851, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30245707

RESUMO

Metallotriazine complexes possess interesting biological and medicinal properties, and the present study focuses on the synthesis, characterization, and antimicrobial activity of four novel copper-triazine derivatives in search of potent antibacterial and antifungal drug leads. In this study, 3-(2-pyridyl)-5,6-diphenyl-1,2,4-triazine-4,4'-disulfonic acid monosodium salt (L1, ferrozine) and 3-(2-pyridyl)-5,6-di(2-furyl)-1,2,4-triazine-5,5'-disulfonic acid disodium salt (L2, ferene) have been used as ligands to study the complexation towards copper(II). The synthesized complexes, [CuCl2(ferrozine)]·7H2O·MeOH (1), [CuCl2(ferrozine)2]·5H2O·MeOH (2), [CuCl2(ferene)]·H2O·MeOH (3), and [CuCl2(ferene)2]·H2O·MeOH (4), have been characterized spectroscopically, and preliminary bioassays have been carried out. FTIR spectroscopic data have shown that N=N and C=N stretching frequencies of complexes have been shifted towards lower frequencies in comparison with that of the ligands, confirming new bond formation between Cu and N, which in turn lowers the strength of N=N and C=N bonds. In addition, a bathochromic shift has been observed for UV-visible spectra of complexes (1), (2), (3), and (4). Furthermore, elemental analysis data have been useful to obtain empirical formulas of these complexes and to establish the purity of each complex. Complexes (1) and (2) have shown antibacterial activity for both S. aureus (ATCC® 25923) and E. coli (ATCC® 25922) at 1 mg/disc concentration, and ferrozine has shown a larger inhibition zone against the clinical sample of C. albicans at 1 mg/disc concentration in comparison with the positive control, fluconazole.

15.
Bioinorg Chem Appl ; 2018: 7563820, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29670646

RESUMO

Four Zn(II) complexes containing a pyridyl triazine core (L1 = 3-(2-pyridyl)-5,6-di(2-furyl)-1,2,4-triazine-5',5″-disulfonic acid disodium salt and L2 = 3-(2-pyridyl)-5,6-diphenyl-1,2,4-triazine-4',4″-disulfonic acid sodium salt) were synthesized, and their chemical formulas were finalized as [Zn(L1)Cl2]·5H2O·ZnCl2 (1), [Zn(L1)2Cl2]·4H2O·2CH3OH (2), [Zn(L2)Cl2]·3H2O·CH3OH (3), and [Zn(L2)2Cl2] (4). The synthesized complexes are water soluble, making them good candidates for biological applications. All four complexes have been characterized by elemental analysis and 1H NMR, IR, and UV-Vis spectroscopy. The IR stretching frequency of N=N and C=N bonds of complexes 1-4 have shifted to lower frequencies in comparison with free ligands, and a bathochromic shift was observed in UV-Vis spectra of all four complexes. The binding studies of ligands and complexes 1-4 with bovine serum albumin (BSA) resulted binding constants (Kb) of 3.09 × 104 M-1, 12.30 × 104 M-1, and 16.84 × 104 M-1 for ferene, complex 1, and complex 2, respectively, indicating potent serum distribution via albumins.

16.
J Loss Prev Process Ind ; 54: 103-109, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29681689

RESUMO

The relationship between the explosion inerting effectiveness of rock dusts on coal dusts, as a function of the specific surface area (cm2/g) of each component is examined through the use of 20-L explosion chamber testing. More specifically, a linear relationship is demonstrated for the rock dust to coal dust (or incombustible to combustible) content of such inerted mixtures with the specific surface area of the coal and the inverse of that area of the rock dust. Hence, the inerting effectiveness, defined as above, is more generally linearly dependent on the ratio of the two surface areas. The focus on specific surface areas, particularly of the rock dust, provide supporting data for minimum surface area requirements in addition to the 70% less than 200 mesh requirement specified in 30 CFR 75.2.

17.
Fuel (Lond) ; 218: 306-315, 2018 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-29599565

RESUMO

When combustible materials ignite and burn, the potential for fire growth and flame spread represents an obvious hazard, but during these processes of ignition and flaming, other life hazards present themselves and should be included to ensure an effective overall analysis of the relevant fire hazards. In particular, the gases and smoke produced both during the smoldering stages of fires leading to ignition and during the advanced flaming stages of a developing fire serve to contaminate the surrounding atmosphere, potentially producing elevated levels of toxicity and high levels of smoke obscuration that render the environment untenable. In underground mines, these hazards may be exacerbated by the existing forced ventilation that can carry the gases and smoke to locations far-removed from the fire location. Clearly, materials that require high temperatures (above 1400 K) and that exhibit low mass loss during thermal decomposition, or that require high heat fluxes or heat transfer rates to ignite represent less of a hazard than materials that decompose at low temperatures or ignite at low levels of heat flux. In order to define and quantify some possible parameters that can be used to assess these hazards, small-scale laboratory experiments were conducted in a number of configurations to measure: 1) the toxic gases and smoke produced both during non-flaming and flaming combustion; 2) mass loss rates as a function of temperature to determine ease of thermal decomposition; and 3) mass loss rates and times to ignition as a function of incident heat flux. This paper describes the experiments that were conducted, their results, and the development of a set of parameters that could possibly be used to assess the overall fire hazard of combustible materials using small scale laboratory experiments.

18.
Chem Cent J ; 10: 71, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27942267

RESUMO

BACKGROUND: Re(I) tricarbonyl complexes exhibit immense potential as fluorescence imaging agents. However, only a handful of rhenium complexes have been utilized in biological imaging. The present study describes the synthesis of four novel rhenium complexes, their characterization and preliminary biological studies to assess their potential as biological imaging agents. RESULTS: Four facial rhenium tricarbonyl complexes containing a pyridyl triazine core, (L1 = 5,5'(3-(2-pyridyl)-1,2,4-triazine-5,6-diyl)-bis-2-furansulfonic acid disodium salt and L2 = (3-(2- pyridyl)-5,6-diphenyl-1,2,4-triazine-4',4''-disulfonic acid sodium salt) have been synthesized by utililzing two different Re metal precursors, Re(CO)5Br and [Re(CO)3(H2O)3]OTf in an organic solvent mixture and water, respectively. The rhenium complexes [Re(CO)3(H2O)L1]+ (1), Re(CO)3L1Br (2), [Re(CO)3(H2O)L2]+ (3), and Re(CO)3L2Br (4), were obtained in 70-85% yield and characterized by 1H NMR, IR, UV, and luminescence spectroscopy. In both H2O and acetonitrile, complexes display a weak absorption band in the visible region which can be assigned to a metal to ligand charge transfer excitation and fluorescent emission lying in the 650-710 nm range. Cytotoxicity assays of complexes 1, 3, and 4 were carried out for rat peritoneal cells. Both plant cells (Allium cepa bulb cells) and rat peritoneal cells were stained using the maximum non-toxic concentration levels of the compounds, 20.00 mg ml-1 for 1 and 3 and 5.00 mg ml-1 for 4 to observe under the epifluorescence microscope. In both cell lines, compound concentrated specifically in the nuclei region. Hence, nuclei showed red fluorescence upon excitation at 550 nm. CONCLUSIONS: Four novel rhenium complexes have been synthesized and characterized. Remarkable enhancement of fluorescence upon binding with cells and visible range excitability demonstrates the possibility of using the new complexes in biological applications.Graphical abstractMicrograph of rat peritoneal cells incubated with novel rhenium complex under epifluorescence microscope.

19.
Bioinorg Chem Appl ; 2016: 2675937, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27847444

RESUMO

A novel ligand bearing a central piperidinyl sulfonamide group, N(SO2pip)dpa, and its corresponding Re tricarbonyl complex, [Re(CO)3(N(SO2pip)dpa)]+, have been synthesized in good yield. The methylene CH2 signal seen as a singlet (4.54 ppm) in a 1H NMR spectrum of the ligand in DMSO-d6 appears as two doublets (5.39, 5.01 ppm) in a spectrum of the [Re(CO)3(N(SO2pip)dpa)]+ complex and confirms the presence of magnetically nonequivalent protons upon coordination to Re. Structural results revealed that the Re-N bond lengths fall within the normal range establishing coordination of ligand to metal. The presence of intraligand π → π⁎ and n → π⁎ transitions is indicated by the absorption peaks around 200-250 nm in UV-visible spectra. Absorption peaks in UV-visible spectra around 300 nm for metal complexes were identified as MLCT transitions. The S-N stretch observed as a strong peak at 923 cm-1 for N(SO2pip)dpa appeared at a shorter frequency, at 830 cm-1 in an FTIR spectrum of the [Re(CO)3(N(SO2pip)dpa)]+. The intense fluorescence displayed by the N(SO2pip)dpa ligand has quenched upon coordination to Re. Relatively low IC50 values given by human breast cancer cells, MCF-7, (N(SO2pip)dpa = 139 µM, [Re(CO)3(N(SO2pip)dpa)]+ = 360 µM) indicate that N(SO2pip)dpa and [Re(CO)3(N(SO2pip)dpa)]+ are promising novel compounds that can be further investigated on their usage as potential anticancer agents.

20.
Aquat Toxicol ; 177: 98-105, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-27262939

RESUMO

Chromium discharged in industrial effluents frequently occurs as an environmental pollutant, but the lethal and sub-lethal effects the heavy metal might cause in animals exposed to it have been insufficiently investigated. Selecting the amphibian Duttaphrynus melanostictus, we carried out laboratory tests to investigate the effects of short and long term exposure to hexavalent chromium (Cr(VI)) in both tadpoles and adult toads. The concentrations used were 0.002, 0.02, 0.2, 1.0 and 2.0mg/L, the first three corresponding to field levels. In vitro exposures were also carried out using toad erythrocytes and Cr(VI) concentrations of 0.0015, 0.003, 0.015, 0.03, 0.15mg/L. Mortality, growth retardation, developmental delays and structural aberrations were noted in the metal-treated tadpoles, with increasing incidence corresponding to increase in Cr(VI) level and duration of exposure. Many of the sub-lethal effects were evident with long term exposure to environmentally relevant levels of the toxicant. Changes in selected blood parameters and erythrocyte morphometry were also detected in Cr(VI) exposed toads, indicating anaemic and leucopenic conditions. In the genotoxicity study, DNA damage indicated by comet assay and increased micronuclei frequency, occurred at the low Cr(VI) concentrations tested. The multiple deleterious effects of exposure to chromium signal the need for monitoring and controlling the discharge of chromium to the environment. The dose-dependency and genotoxic effects observed in this widely distributed Asian toad indicates its suitability for monitoring heavy metal pollution in aquatic systems.


Assuntos
Bufonidae , Cromo/toxicidade , Poluentes Químicos da Água/toxicidade , Animais , Bufonidae/fisiologia , Relação Dose-Resposta a Droga , Eritrócitos/efeitos dos fármacos , Larva/efeitos dos fármacos , Testes de Toxicidade
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