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1.
Biotechnol Appl Biochem ; 71(2): 402-413, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38287712

RESUMO

Malonyl-CoA serves as the main building block for the biosynthesis of many important polyketides, as well as fatty acid-derived compounds, such as biofuel. Escherichia coli, Corynebacterium gultamicum, and Saccharomyces cerevisiae have recently been engineered for the biosynthesis of such compounds. However, the developed processes and strains often have insufficient productivity. In the current study, we used enzyme-engineering approach to improve the binding of acetyl-CoA with ACC. We generated different mutations, and the impact was calculated, which reported that three mutations, that is, S343A, T347W, and S350W, significantly improve the substrate binding. Molecular docking investigation revealed an altered binding network compared to the wild type. In mutants, additional interactions stabilize the binding of the inner tail of acetyl-CoA. Using molecular simulation, the stability, compactness, hydrogen bonding, and protein motions were estimated, revealing different dynamic properties owned by the mutants only but not by the wild type. The findings were further validated by using the binding-free energy (BFE) method, which revealed these mutations as favorable substitutions. The total BFE was reported to be -52.66 ± 0.11 kcal/mol for the wild type, -55.87 ± 0.16 kcal/mol for the S343A mutant, -60.52 ± 0.25 kcal/mol for T347W mutant, and -59.64 ± 0.25 kcal/mol for the S350W mutant. This shows that the binding of the substrate is increased due to the induced mutations and strongly corroborates with the docking results. In sum, this study provides information regarding the essential hotspot residues for the substrate binding and can be used for application in industrial processes.


Assuntos
Acetil-CoA Carboxilase , Streptomyces antibioticus , Acetil-CoA Carboxilase/genética , Acetil-CoA Carboxilase/metabolismo , Streptomyces antibioticus/metabolismo , Acetilcoenzima A/genética , Simulação de Acoplamento Molecular , Mutação , Saccharomyces cerevisiae/metabolismo , Escherichia coli/metabolismo
2.
Biomed Chromatogr ; 38(10): e5968, 2024 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-39039695

RESUMO

Withania somnifera belongs to the family Solanaceae, commonly called ashwagandha, and is traditionally used as an astringent, hepatoprotective and antioxidant, and as a treatment for rheumatism. Therefore the current study aimed to explore the dichloromethane fraction of W. somnifera whole plant (DCFWS) and ethyl acetate fraction of W. somnifera (EAFWS) using gas chromatoghraphy-mass spectrometry (GC-MS) analysis and to find the acetylcholinesterase inhibition potential along with spasmolytic activity. The GC-MS-detected phytochemicals were 2,4-bis(1,1-dimethylethyl), hexadecanoic acid, 1-nonadecene and 11-octadecenoic acid. The DCFWS and EAFWS exhibited acetylcholinesterase inhibitory potential with significant inhibitory concentration values. The acute toxicity results of both fractions showed high toxicity, causing emesis at 0.5 g and both emesis and diarrhea at 1 g/kg. Both fractions exhibited significant (p ≤ 0.01) laxative activity against metronidazole (7 mg/kg) and loperamide hydrochloride (4 mg/kg) induced constipation. Both DCFWS (66.8 ± 3.85%) and EAFWS (58.58 ± 3.28%) significantly (p ≤ 0.05) increased charcoal movement compared with distal water (43.93 ± 4.34%). Similarly the effect of DCFWS on KCl-induced (80 mm) contraction was more significant as compared with EAFWS. It was concluded that the plant can be used in the treatment of gastrointestinal tract diseases such as constipation. Furthermore, additional work is required in the future to determine the bioactive compounds that act as therapeutic agents in W. somnifera.


Assuntos
Cromatografia Gasosa-Espectrometria de Massas , Compostos Fitoquímicos , Extratos Vegetais , Withania , Withania/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Cromatografia Gasosa-Espectrometria de Massas/métodos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/química , Animais , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/análise , Masculino , Constipação Intestinal/tratamento farmacológico , Camundongos , Ratos
3.
J Cardiovasc Electrophysiol ; 34(6): 1370-1376, 2023 06.
Artigo em Inglês | MEDLINE | ID: mdl-37232420

RESUMO

INTRODUCTION: Radiofrequency ablation (RFA) for atrial fibrillation (AF) has been associated with variable incidence (0.88%-10%) of pericarditis manifested as chest pain, possibly more prevalent with the advent of high-power short-duration (HPSD) ablation. This has led to the widespread use of colchicine in preventative protocols for postablation pericarditis. However, the efficacy of preventative colchicine has not been validated yet. OBJECTIVE: To evaluate the efficacy of a routine postoperative colchicine regimen (0.6 mg twice a day for 14 days post-AF ablation) for prevention of postablation pericarditis in patients undergoing HPSD ablation. METHOD: We retrospectively evaluated consecutive single-operator HPSD AF ablation procedures at our institution from June 2019 to July 2022. A colchicine protocol was introduced in June 2021 for the prevention of postablation pericarditis. All ablations were performed with 50 watts. Patients were divided into colchicine and noncolchicine groups. We recorded incidence of postablation chest pain, emergency room (ER) visit for chest pain, pericardial effusion, pericardiocentesis, any ER visit, hospitalization, AF recurrence, and cardioversion for AF within the first 30 days following ablation. We also recorded colchicine-related side effects and medication compliance. RESULTS: Two hundred and ninety-four consecutive HPSD AF ablation patients were screened for the study. After implementing the prespecified exclusion criteria, a total of 205 patients were included in the final analysis, yielding 101 patients in the colchicine group and 104 patients in the noncolchicine group. Both groups were well-matched for demographic and procedural parameters. There was no significant difference in postablation chest pain (9.9% vs. 8.6%, p = .7), pericardial effusion (2.9% vs. 0.9%, p = .1), ER visits (11.9% vs. 12.5%, p = .2), 30-day hospitalization for AF recurrence (0.9% vs. 0.96%, p = .3), and 30-day need for cardioversion for AF (3.9% vs. 5.7%, p = .2). Fifteen (15) patients had severe colchicine-related diarrhea, out of which 12 discontinued it prematurely. There were no major procedural complications in either group. CONCLUSION: In this single-operator retrospective analysis, prophylactic colchicine was not associated with significant reduction in the incidence of postablation chest pain, pericarditis, 30 day hospitalization, ER visits, or AF recurrence or need of cardioversion within first 30 days after HPSD ablation for AF. However, its usage was associated with significant diarrhea. This study concludes no additional advantage of prophylactic use of colchicine after HPSD AF ablation.


Assuntos
Fibrilação Atrial , Ablação por Cateter , Derrame Pericárdico , Pericardite , Veias Pulmonares , Humanos , Fibrilação Atrial/diagnóstico , Fibrilação Atrial/cirurgia , Fibrilação Atrial/tratamento farmacológico , Colchicina/efeitos adversos , Estudos Retrospectivos , Derrame Pericárdico/diagnóstico , Derrame Pericárdico/epidemiologia , Derrame Pericárdico/etiologia , Resultado do Tratamento , Pericardite/diagnóstico , Pericardite/prevenção & controle , Pericardite/epidemiologia , Diarreia/tratamento farmacológico , Diarreia/etiologia , Diarreia/cirurgia , Dor no Peito/cirurgia , Ablação por Cateter/efeitos adversos , Ablação por Cateter/métodos , Recidiva , Veias Pulmonares/cirurgia
4.
Pacing Clin Electrophysiol ; 46(11): 1387-1392, 2023 11.
Artigo em Inglês | MEDLINE | ID: mdl-37713192

RESUMO

BACKGROUND: Radiofrequency catheter ablation (RFA) for atrial fibrillation (AF) is being increasingly performed without fluoroscopy. This study aims to determine the safety of fluoroless RFA for patients with pre-existing cardiac implantable electronic devices (CIED). METHODS: This is a single-center, single-operator, retrospective, observational study of 225 consecutive fluoroless RFA procedures for AF from June 1, 2019 to June 1, 2022. All procedures were performed with intracardiac echocardiography (ICE) support. Patients with pre-existing CIED were extracted from the database. Each CIED was interrogated at the start and end of each procedure and at 30-day follow-up. Pre- and post-procedure CIED interrogations were compared for any change in device or lead parameters. Patients were tracked for any subsequent device malfunction. RESULTS: Out of 225 fluoroless AF ablations, 25 (10.2%) had pre-existing CIED (14 dual-chamber pacemakers, three dual-chamber defibrillators, three single-chamber defibrillators, one single chamber pacemaker, and four biventricular devices). Mean patient age was 71 ± 6 years. The mean duration of indwelling CIED was 1804 ± 1645 days (range: 78-6267 days). One (4%) patient had lead-related fibrin on ICE imaging. There was no significant difference in lead(s) threshold, impedance, or sensing post procedure or at 30-day follow-up compared to pre procedure. None of the patients required lead revision. There were no intra- or post-op thromboembolic events or subsequent device infection. One patient underwent CIED extraction after 11 months for an unrelated secondary device infection. CONCLUSIONS: Radiofrequency catheter ablation for AF can be safely performed without fluoroscopy in patients with pre-existing CIED.


Assuntos
Fibrilação Atrial , Ablação por Cateter , Desfibriladores Implantáveis , Humanos , Idoso , Fibrilação Atrial/cirurgia , Estudos Retrospectivos , Resultado do Tratamento , Ablação por Cateter/métodos
5.
Mar Drugs ; 21(5)2023 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-37233467

RESUMO

Seaweed has been known to possess beneficial effects forhuman health due to the presence of functional bioactive components. The n-butanol and ethyl acetate extracts of Dictyota dichotoma showed ash (31.78%), crude fat (18.93%), crude protein (14.5%), and carbohydrate (12.35%) contents. About 19 compounds were identified in the n-butanol extract, primarily undecane, cetylic acid, hexadecenoic acid, Z-11-, lageracetal, dodecane, and tridecane, whereas 25 compounds were identified in the ethyl acetate extract, mainly tetradecanoic, hexadecenoic acid, Z-11-, undecane, and myristic acid. FT-IR spectroscopy confirmed the presence of carboxylic acid, phenols, aromatics, ethers, amides, sulfonates, and ketones. Moreover, total phenolic contents (TPC) and total flavonoid contents (TFC) in ethyl acetate extract were 2.56 and 2.51 mg GAE/g and in n-butanol extract were 2.11 and 2.25 mg QE/g, respectively. Ethyl acetate and n-butanol extracts at a high concentration of 100 mg mL-1 showed 66.64 and 56.56 % inhibition of DPPH, respectively. Antimicrobial activity revealed that Candida albicans was the most susceptible microorganism, followed by Bacillus subtilis, Staphylococcus aureus, and Escherichia coli, whereas Pseudomonas aeruginosa showed the least inhibition at all concentrations. The in vivo hypoglycemic study revealed that both extracts exhibited concentration-dependent hypoglycemic activities. In conclusion, this macroalgae exhibited antioxidant, antimicrobial, and hypoglycemic potentials.


Assuntos
Anti-Infecciosos , Phaeophyceae , Alga Marinha , Antioxidantes/farmacologia , Antioxidantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Hipoglicemiantes/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , 1-Butanol , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química
6.
World J Microbiol Biotechnol ; 39(12): 345, 2023 Oct 16.
Artigo em Inglês | MEDLINE | ID: mdl-37843704

RESUMO

Macroalgae has the potential to be a precious resource in food, pharmaceutical, and nutraceutical industries. Therefore, the present study was carried out to identify and quantify the phyco-chemicals and to assess the nutritional profile, antimicrobial, antioxidant, and anti-diabetic properties of Nitella hyalina extracts. Nutritional composition revealed0.05 ± 2.40% ash content, followed by crude protein (24.66 ± 0.95%), crude fat (17.66 ± 1.42%), crude fiber (2.17 ± 0.91%), moisture content (15.46 ± 0.48%) and calculated energy value (173.50 ± 2.90 Kcal/100 g). 23 compounds were identified through GC-MS analysis in ethyl acetate extract, with primary compounds being Palmitic acid, methyl ester, (Z)-9-Hexadecenoic acid, methyl ester, and Methyl tetra decanoate. Whereas 15 compounds were identified in n-butanol extract, with the major compounds being Tetra decanoic acid, 9-hexadecanoic acid, Methyl pentopyranoside, and undecane. FT-IR spectroscopy confirmed the presence of alcoholic phenol, saturated aliphatic compounds, lipids, carboxylic acid, carbonyl, aromatic components, amine, alkyl halides, alkene, and halogen compounds. Moreover, n-butanol contains 1.663 ± 0.768 mg GAE/g, of total phenolic contents (TPC,) and 2.050 ± 0.143 QE/g of total flavonoid contents (TFC), followed by ethyl acetate extract, i.e. 1.043 ± 0.961 mg GAE/g and 1.730 ± 0.311 mg QE/g respectively. Anti-radical scavenging effect in a range of 34.55-46.35% and 35.39-41.79% was measured for n-butanol and ethyl acetate extracts, respectively. Antimicrobial results declared that n-butanol extract had the highest growth inhibitory effect, followed by ethyl acetate extract. Pseudomonas aeruginosa was reported to be the most susceptible strain, followed by Staphylococcus aureus and Escherichia coli, while Candida albicans showed the least inhibition at all concentrations. In-vivo hypoglycemic study revealed that both extracts exhibited dose-dependent activity. Significant hypoglycemic activity was observed at a dose of 300 mg/kg- 1 after 6 h i.e. 241.50 ± 2.88, followed by doses of 200 and 100 mg/kg- 1 (245.17 ± 3.43 and 250.67 ± 7.45, respectively) for n-butanol extract. In conclusion, the macroalgae demonstrated potency concerning antioxidant, antimicrobial, and hypoglycemic properties.


Assuntos
Anti-Infecciosos , Nitella , Antioxidantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Hipoglicemiantes/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , 1-Butanol , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química , Ésteres
7.
Ann Noninvasive Electrocardiol ; 27(5): e12948, 2022 09.
Artigo em Inglês | MEDLINE | ID: mdl-35305546

RESUMO

Cross stimulation is defined as stimulation of one cardiac chamber when the stimulation of the other chamber is expected. We present a case of an eighty three year old patient with history of dual chamber pacemaker implantation with recent generator change which showed interesting ECG findings.


Assuntos
Eletrocardiografia , Marca-Passo Artificial , Idoso de 80 Anos ou mais , Estimulação Cardíaca Artificial , Ventrículos do Coração/diagnóstico por imagem , Humanos
8.
Int J Mol Sci ; 23(17)2022 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-36077425

RESUMO

Malate dehydrogenase, which facilitates the reversible conversion of malate to oxaloacetate, is essential for energy balance, plant growth, and cold and salt tolerance. However, the genome-wide study of the MDH family has not yet been carried out in tomato (Solanum lycopersicum L.). In this study, 12 MDH genes were identified from the S. lycopersicum genome and renamed according to their chromosomal location. The tomato MDH genes were split into five groups based on phylogenetic analysis and the genes that clustered together showed similar lengths, and structures, and conserved motifs in the encoded proteins. From the 12 tomato MDH genes on the chromosomes, three pairs of segmental duplication events involving four genes were found. Each pair of genes had a Ka/Ks ratio < 1, indicating that the MDH gene family of tomato was purified during evolution. Gene expression analysis exhibited that tomato MDHs were differentially expressed in different tissues, at various stages of fruit development, and differentially regulated in response to abiotic stresses. Molecular docking of four highly expressed MDHs revealed their substrate and co-factor specificity in the reversible conversion process of malate to oxaloacetate. Further, co-localization of tomato MDH genes with quantitative trait loci (QTL) of salt stress-related phenotypes revealed their broader functions in salt stress tolerance. This study lays the foundation for functional analysis of MDH genes and genetic improvement in tomato.


Assuntos
Solanum lycopersicum , Regulação da Expressão Gênica de Plantas , Estudo de Associação Genômica Ampla , Solanum lycopersicum/metabolismo , Malato Desidrogenase/genética , Malato Desidrogenase/metabolismo , Malatos/metabolismo , Simulação de Acoplamento Molecular , Família Multigênica , Filogenia , Proteínas de Plantas/metabolismo , Estresse Fisiológico/genética
9.
Molecules ; 27(13)2022 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-35807565

RESUMO

Chrozophora tinctoria is an annual plant of the family Euphorbiaceae, traditionally used as a laxative, a cathartic and an emetic. A methanolic extract of Chrozophora tinctoria (MEC) whole plant and an n-butanol fraction of Chrozophora tinctoria (NBFC) were analyzed by gas chromatography-mass spectrometry (GC-MS) to detect the phytochemicals. MEC and NBFC were tested for in vitro anti acetylcholinesterase (AChE) potential. The effect of both samples on intestinal propulsive movement and spasmolytic activity in the gastrointestinal tract (GIT) was also studied. About twelve compounds in MEC and three compounds in NBFC were tentatively identified through GC-MS. Some of them are compounds with known therapeutic activity, such as toluene; imipramine; undecane; 14-methyl-pentadecanoic acid methyl ester; and hexadecanoic acid. Both NBFC and MEC samples were checked for acute toxicity and were found to be highly toxic in a dose-dependent manner, causing diarrhea and emesis at 1 g/kg concentration in pigeons, with the highest lethargy and mortality above 3 g/kg. Both the samples of Chrozophora tinctoria revealed significant (p ≤ 0.01) laxative activity against metronidazole (7 mg/kg) and loperamide hydrochloride (4 mg/kg)-induced constipation. NBFC (81.18 ± 2.5%) and MEC (68.28 ± 2.4%) significantly increased charcoal meal intestinal transit compared to distal water (41.15 ± 4.3%). NBFC exhibited a significant relaxant effect (EC50 = 3.40 ± 0.20 mg/mL) in spontaneous rabbit jejunum as compared to MEC (EC50 = 4.34 ± 0.68 mg/kg). Similarly, the impact of NBFC on KCl-induced contraction was more significant than that of MEC (EC50 values of 7.22 ± 0.06 mg/mL and 7.47 ± 0.57 mg/mL, respectively). The present study scientifically validates the folk use of Chrozophora tinctoria in the management of gastrointestinal diseases such as constipation. Further work is needed to isolate the phytochemicals that act as diarrheal agents in Chrozophora tinctoria.


Assuntos
Euphorbiaceae , Laxantes , Animais , Constipação Intestinal/induzido quimicamente , Constipação Intestinal/tratamento farmacológico , Diarreia/induzido quimicamente , Diarreia/tratamento farmacológico , Euphorbiaceae/química , Laxantes/farmacologia , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/química , Coelhos
10.
Molecules ; 27(7)2022 Mar 26.
Artigo em Inglês | MEDLINE | ID: mdl-35408541

RESUMO

Chrozophora tinctoria (Euphorbiaceae) has been used as an emetic, anthelminthic, and cathartic agent in traditional medicine. We used gas chromatography-mass spectrometry (GC-MS) to characterize the composition of ethyl acetate (EAC) and dichloromethane (DCMC) fractions from the whole Chrozophora tinctoria plant. EAC and DCMC fractions were evaluated for acetylcholinesterase (AChE) inhibitory activity and acute toxicity. Their effects on intestinal propulsive movement and spasmogenic activity of the gastrointestinal tract (GIT) muscle were also assessed. The compounds detected in both fractions were mostly fatty acids, with about seven compounds in EAC and 10 in DCMC. These included pharmacologically active compounds such as imipramine, used to treat depression, or hexadecanoic acid methyl ester, an antioxidant. Both EAC and DCMC fractions inhibited acetylcholinesterase (AChE) activity with IC50 values of 10 µg and 130 µg, respectively. Both the fractions were found to be toxic in a dose-dependent manner, inducing emesis at 0.5 g or higher and lethargy and mortality from 3-5 g upwards. Similarly, both of the fractions showed laxative activity in metronidazole- and loperamide-induced constipation models. EAC relaxed the intestinal muscle at a lower dose (1 mg/mL) than DCMC. Similarly, the EAC extract showed a significant relaxation effect (EC50 = 0.67 ± 0.15 mg/mL) on KCL-induced contraction in rabbit jejunum as compared to DCMC (EC50 = 5.04 ± 0.05 mg/kg). The present study strongly supports the folklore that this valuable plant is a cathartic agent. Further work is required to isolate and validate the bioactive compounds that act as diarrheal agents in Chrozophora tinctoria.


Assuntos
Euphorbiaceae , Extratos Vegetais , Acetilcolinesterase , Animais , Catárticos , Euphorbiaceae/química , Laxantes/farmacologia , Extratos Vegetais/química , Coelhos
11.
Pak J Pharm Sci ; 35(3): 835-840, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35791484

RESUMO

The present paper presents results of analgesic, antipyretic activity and anti-inflammatory potential of extract obtained from Acacia cyanophylla when tested at different doses. Analgesic potential of the crude methanolic extract tested by acetic acid assay was dose dependent and maximum activity of 61.60% was measured at 400 mg/kg. Analgesic activity by hot plate method revealed that maximum activity of 36.98% was noted when the mice were exposed to 90 minutes at higher dose of 400 mg/kg. Similar pattern for antipyretic activity was observed as noted for analgesic activity. Anti-inflammatory activity was dose and time dependent when evaluated by Carrageenan-induced paw edema and Xylene-induced ear edema model. Maximum anti-inflammatory activity (43.32%) was shown by crude methanolic extract of Acacia cyanophylla at 400mg/kg-1 after 5 hours on Carrageenan-induced paw edema model. Similarly, maximum (68.80%) anti-inflammatory activity was noted when accessed by Xylene-induced ear edema model at the dose of 200mg/kg after 60 minutes. No in vivo toxicity of the extracts up to the dose of 2000mg/kg was observed using albino mice.


Assuntos
Acacia , Analgésicos , Anti-Inflamatórios , Antipiréticos , Acacia/química , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Antipiréticos/farmacologia , Carragenina , Edema/induzido quimicamente , Edema/tratamento farmacológico , Febre/tratamento farmacológico , Camundongos , Extratos Vegetais/farmacologia , Xilenos
12.
Pak J Pharm Sci ; 33(1): 27-32, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32122827

RESUMO

The current research describes the antimicrobial potential of methanol, n-hexane, n-butanol, ethyl acetate and aqueous extracted samples from the leaves and fruits tissues of Capsicum annuum. Different solvent extracted samples were screened against six pathogenic microorganisms including five bacterial and one fungal specie by disc diffusion susceptibility assay using 1, 2 and 3 mg disc-1 concentrations. When analyzed statistically the data showed that different solvent extracted samples from both leaves and fruits of Capsicum annuum revealed varying degrees of antibacterial and antifungal activities. n-butanol and ethyl acetate extracted fractions from both leaves and fruits showed significant inhibition of growth against all the tested microorganisms at 1, 2 and 3 mg disc-1 concentrations. Escherichia coli were completely resistant to aqueous extracts obtained from the leaves at all the three concentrations. Klebsiella pneumonia was resistant to n-hexane extracted fraction from leaves at 1mg disc-1 concentration, however, was susceptible at 2 and 3 mg disc-1 concentrations. The growth of Pseudomonas aeruginosa and Staphylococcus aureus were effectively inhibited by all the solvent extracted fractions from the fruits while aqueous fraction was not able to inhibit the growth of Bacillus subtilis. The growth of Candida albicans was effectively inhibited by ethyl acetate extracted fraction from leaves at 3 mg disc-1 concentration.


Assuntos
Anti-Infecciosos/farmacologia , Capsicum/química , Extratos Vegetais/farmacologia , Solventes/química , Anti-Infecciosos/química , Frutas/química , Testes de Sensibilidade Microbiana/métodos , Testes de Sensibilidade Microbiana/estatística & dados numéricos , Extratos Vegetais/química , Folhas de Planta/química
13.
Inorg Chem ; 58(13): 8763-8774, 2019 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-31247847

RESUMO

Four new organic-inorganic hybrids, [N(C4H9)4]5H[{HNC2O(CH2O)3P2V3W15O59}C44N4H29O3] (TPPOH-1POM), [N(C4H9)4]10H2[{HNC2O(CH2O)3P2V3W15O59}2C44N4H28O2] (TPPOH-2POM trans), [N(C4H9)4]10H2[{HNC2O(CH2O)3P2V3W15O59}2C44N4H28O2] (TPPOH-2POM cis), and [N(C4H9)4]15H3[{HNC2O(CH2O)3P2W15V3O59}3C44N4H27O] (TPPOH-3POM), have been synthesized by covalently grafting the Dawson-type polyoxometalate (POM) [N(C4H9)4]5[H4P2W15V3O62] onto new porphyrins N-[1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl]-4-[10,15,20-tris(4-hydroxyphenyl)porphyrin-5-yl]benzamide (TPPOH-1Tris), 4,4'-[5,15-bis(4-hydroxyphenyl)porphyrin-10,20-diyl]bis[ N-[1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl]benzamide] (TPPOH-2Tris trans), 4,4'-[10,15-bis(4-hydroxyphenyl)porphyrin-5,20-diyl]bis[ N-[1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl]benzamide] (TPPOH-2Tris cis). and 4,4',4″-[20-(4-hydroxyphenyl)porphyrin-5,10,15-triyl]tris[ N-[1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl]benzamide] (TPPOH-3Tris), respectively, in N, N-dimethylacetamide under nitrogen. The hybrid compounds were thoroughly characterized by elemental analysis, FT-IR, NMR (1H, 2D NOESY, 31P, and 51V), ESI-MS, MALDI-TOF-MS, UV-vis, and fluorescence spectroscopy. All porphyrins and their corresponding hybrids exhibited remarkable third-order nonlinear-optical responses under laser irradiation, with the intensity of light at focus E0 being 4.2 µJ at wavelength 532 nm, pulse duration τ = 6 ns, and repetition rate 10 Hz. The molecular second hyperpolarizability (γ) values of the hybrids (TPPOH-1POM, TPPOH-2POM trans, TPPOH-2POM cis, TPPOH-3POM) were calculated to be 8.48 × 10-28 esu, 8.94 × 10-28 esu, 10.16 × 10-28 esu, and 8.93 × 10-28 esu, while the molecular second hyperpolarizability (γ) of their corresponding porphyrin precursors (TPPOH-1Tris, TPPOH-2Tris trans, TPPOH-2Tris cis, and TPPOH-3Tris) were 7.19 × 10-28 esu, 8.09 × 10-28 esu, 9.07 × 10-28 esu, and 7.24 × 10-28 esu, respectively. The γ values of the cis forms were found to be superior to those of all other compounds, indicating the significant role of the greater dipole moment and low symmetry of the cis form compared to other compounds. It was also found that the fluorescence intensity was decreased by 81.52%, 90.37%, 93.93%, and 84.62% for the hybrids TPPOH-1POM, TPPOH-2POM trans, TPPOH-2POM cis, and TPPOH-3POM with respect to their corresponding precursors, respectively, which reveals the Dawson-type POM as a strong quencher. This quenching phenomenon not only indicates again unequivocally the formation of hybrid compounds but also may imply a photoinduced electron/energy-transfer process favored from a porphyrin moiety to a Dawson-type POM moiety.

14.
Pak J Pharm Sci ; 32(2): 515-519, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31081760

RESUMO

The present research work investigate the antimicrobial activities of crude methanolic extracted samples from the leaves of Litsea glutinosa against different microorganisms through disc diffusion assay applied in two different concentrations of 1 and 2mg disc1. The tested microbial species included B. subtilis, E. coli, P. aeruginosa, K. pneumoniae and C. albicans. The crude methanolic extract was applied in two different concentrations of 1 and 2mg disc1. Analysis of the data revealed that crude methanolic extracted samples showed different ranges of antimicrobial activities against all the tested microbes at both concentrations. Maximum growth inhibition was measured against gram negative Pseudomonas aeruginosa followed by the fungal specie Candida albicans. In case of Petroleum extracted fractions maximum growth reduction was measured in Candida albicans at higher concentration. Similarly, growth inhibition was more in Pseudomonas aeruginosa at higher concentration of aqueous extracted samples. Different solvent extracted samples showed the presence of alkaloids, flavonoids, proteins, fats, oils, tannins, carbohydrates, sterols and saponins.


Assuntos
Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Litsea/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Alcaloides/análise , Fracionamento Químico/métodos , Avaliação Pré-Clínica de Medicamentos , Flavonoides/análise , Metanol/química , Testes de Sensibilidade Microbiana , Extratos Vegetais/análise , Plantas Medicinais/química , Solventes/química , Taninos/análise
15.
Pak J Pharm Sci ; 32(1): 177-184, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30772807

RESUMO

Different solvent extracted samples from the leaves and fruits tissues of D. stramonium were tested against five pathogenic microorganisms by disc diffusion susceptibility method using 1, 2 and 3mg disc-1 concentrations. Methanol and chloroform extracted fractions from both leaves and fruits measured good growth inhibition of all the tested microorganisms at all concentrations. Bacillus subtilis was very resistant to n-butanol and aqueous extracted fractions of fruits tissues at all the tested three concentrations. The growths of Pseudomonas aeruginosa and Klebsiella pnuemonia were efficiently reduced by all the solvent extracted fractions from the fruits while aqueous fraction was unable to restrain the growth of Bacillus subtilis. The growth of Candida albicans was effectively reduced by aqueous extracted fraction from the leaves tissue at the highest concentration. Maximum growth reduction of (77%) was shown by chloroform extracted fractions from the leaves against Klebsiella pneumonia at 3mg disc-1 concentration. Minimum zone of inhibition (35.4%) was measured by n-butanol extracted fractions from the leaves against Pseudomonas aeruginosa at the lowest concentrations of 1mg disc-1. In case of leaves the most vulnerable bacteria was Bacillus subtilis while in case of fruits Klebsiella pneumonia was the most susceptible while Bacillus subtilis was the most resistant one.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Datura stramonium , Frutas , Fungos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta , Solventes/química , Antibacterianos/isolamento & purificação , Antifúngicos/isolamento & purificação , Bactérias/crescimento & desenvolvimento , Datura stramonium/química , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Farmacorresistência Bacteriana , Frutas/química , Fungos/crescimento & desenvolvimento , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química
16.
Pak J Pharm Sci ; 32(5): 2083-2089, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31813874

RESUMO

Medicinal and aromatic plants contribute to major portion of the flora. The plant materials obtained from these plants are used in the pharmaceuticals, cosmetics, and drug industries. Tamarix dioica is locally used in the management of splenic and hepatic inflammation as well as diuretic and carminative. It also possesses cytotoxic, antimicrobial, antifungal and anti-inflammatory activity. The present study investigates the anti-inflammatory, anti-pyretic and analgesic activities of the crude methanolic extract from Tamarix dioica. Anti-inflammatory activity was measured by Carrageenan Induced Paw Edema and Xylene Induced Ear Edema methods. Pyrexia induction with Brewer's yeast assay was used to determine antipyretic activity and analgesic activity was estimated by acetic acid induced writhing and hot plate methods. The data indicated that anti-inflammatory, anti-pyretic and analgesic activities of the crude methanolic extract from Tamarix dioica was dose and time dependent when measured by different assays. Exposure of model animal to increasing concentrations of the plant extract for longer period increased their anti-inflammatory, anti-pyretic and analgesic activities. Significantly highest anti-inflammatory, anti-pyretic and analgesic activities were noted at highest doses of the crude methanolic extract for longer exposure compared with their respective controls.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Antipiréticos/farmacologia , Tamaricaceae/química , Ácido Acético/farmacologia , Analgésicos/química , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Antifúngicos/química , Antifúngicos/farmacologia , Antipiréticos/química , Modelos Animais de Doenças , Edema/tratamento farmacológico , Edema/microbiologia , Feminino , Inflamação/tratamento farmacológico , Fígado/efeitos dos fármacos , Masculino , Metanol/química , Fitoterapia/métodos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Baço/efeitos dos fármacos
17.
Microb Pathog ; 114: 116-123, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29174698

RESUMO

This study describes the first ever utilization of cell free aqueous extract of cyanobacterium Leptolyngbya JSC-1 as a source of strong reducing and stabilizing agents for the optimal biofabrication of gold nanoparticles (AuNPs) through an eco-friendly synthetic route. Well dispersed crystalline AuNPs of spherical morphology with a particle size of 100-200 nm were prepared. FTIR spectral analysis was then performed to characterize the possible functionalities of JSC-1 extract, mainly involved in stabilizing and formation of AuNPs. Based on the redox potential of JSC-1 extract, it was further confirmed that the extract provide a strong reducing environment in the reaction medium and causes reduction of gold ions. The resultant AuNPs were then explored to find out their photo-catalytic activity for methylene blue and antibacterial activities against E. coli (18 ± 2 mm) and S. aureus (14 ± 2 mm). It has been mechanistically identified that AuNPs caused bacterial membrane damage and cell disruption by inducing the production of intracellular reactive oxygen species (ROS). Together, these finding reveals that biochemically capped AuNPs are the promising antibacterial agents that induce oxidative stress in the two bacterial species evaluated and cause their membrane disruption leading to cell leakage and death.


Assuntos
Antibacterianos/farmacologia , Cianobactérias/metabolismo , Excipientes/farmacologia , Ouro/química , Nanopartículas Metálicas/química , Antibacterianos/química , Bactérias/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Excipientes/química , Ouro/farmacologia , Química Verde , Testes de Sensibilidade Microbiana , Nanotecnologia/métodos , Oxirredução , Estresse Oxidativo/efeitos dos fármacos , Tamanho da Partícula , Espécies Reativas de Oxigênio/metabolismo , Staphylococcus aureus/efeitos dos fármacos
18.
Pak J Pharm Sci ; 31(5): 1845-1852, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30150179

RESUMO

The present research investigates the antimicrobial activities of the samples extracted from the leaves and fruits of Eucalyptus globulus through disc diffusion susceptibility assay using 1, 2 and 3mg disc-1 concentrations. Different extracted samples from the leaves and fruits of Eucalyptus globulus exhibited different degrees of antimicrobial. The data indicated that n-butanol and ethyl acetate extracted fraction of both the leaves and fruits inhibited the growth of all microorganisms at all the tested concentrations. Aqueous extracted sample of the leaves inhibited the growth of Candida albicans while the same fraction from the fruits showed no activity against Bacillus subtilis at any concentration. N-hexane extracted samples of the leaves inhibited the growth of Bacillus subtilis, E. coli and Pseudomonas aeruginosa at the tested concentrations while no activity was recorded against Klebsiella pneumonia, Candida albicans and Stephylococcus aureus. N-butanol extracted samples from the leaves and fruits showed activity against Pseudomonas aeruginosa at the tested concentrations. In case of leaves, the most susceptible bacteria was Bacillus subtilis (gram positive) and Stephylococcus aureus (gram positive) was the most resistant one. In case of fruits the most susceptible bacteria was Stephylococcus aureus (gram positive) and E. coli (Gram negative) was the most resistant one.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Eucalyptus , Frutas , Extratos Vegetais/farmacologia , Folhas de Planta , Antibacterianos/isolamento & purificação , Antifúngicos/isolamento & purificação , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Humanos , Klebsiella pneumoniae/efeitos dos fármacos , Klebsiella pneumoniae/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana/métodos , Extratos Vegetais/isolamento & purificação , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/crescimento & desenvolvimento , Solventes/farmacologia
19.
Pak J Pharm Sci ; 31(3): 947-952, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29716878

RESUMO

The present study was conducted to investigate the phytochemical screening and antimicrobial activities of stem bark of Bombax ceiba L. The methanol extract was subjected to qualitative phytochemical screening using standard procedures. The results indicated the presence of alkaloids, tannins, glycosides, reducing sugar, saponins, phlobatanins and terpenoids. The antimicrobial activity was measured by disc diffusion method. Data revealed that Pseudomonas aeruginosa was inhibited by both methanol and ethanol extracts at the concentration of 2mg disc-1 {21.8mm (68.12%) and 21.3mm (66.56%)}. Similarly, methanol extract reduced the growth of Bacillus subtilis by 17.1mm (74.34%) at the concentration of 1 mg disc-1. However, ethanol extract showed a good activity of 18mm (121.6%) and 20.6mm (112.5%) against Xanthomonas maltophilia at concentrations of 1 and 2 mg disc-1, respectively. Aqueous extract showed 16 mm (53.33% Z.I) against Escherichia coli at 2 mg disc-1. Klebsiella pneumoniae was found resistant to all of the three extracts, while the growth of Candida albicans was inhibited by methanol through 16.5 mm (58.92% Z.I) at 1 mg disc-1. The above study concluded the medicinal potential of B. ceiba.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Bombax , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antifúngicos/química , Antifúngicos/isolamento & purificação , Avaliação Pré-Clínica de Medicamentos/métodos , Humanos , Testes de Sensibilidade Microbiana/métodos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Casca de Planta , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Árvores
20.
Inorg Chem ; 56(16): 9436-9447, 2017 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-28795802

RESUMO

Two new porphyrin-polyoxometalate hybrids, namely, [(C4H9)4N]10H2[{COHNC(CH2O)3P2V3W15O59}2C44N4H28]·CH3CN 1, bearing two covalent-bonded Wells-Dawson-type polyoxometalates (POMs), and [(C4H9)4N)]5H[COHNC(CH2O)3P2V3W15O59{C44H29N4}]·CH3CN 2, bearing one covalent-bonded POM, have been synthesized and thoroughly characterized by means of elemental analysis, powder XRD, FT-IR, 1H (31P, 51V) NMR, MALDI-TOF-MS, UV-vis spectra, and cyclic voltammetry measurement. Experimental results demonstrate that while all the compounds show remarkable third-order optical nonlinearities, the hybrids 1 and 2 are superior to their corresponding porphyrin precursors (molecular second hyperpolarizability γ = 8.0 × 10-28 esu for 54-N-N'(1,3-tetrahydroxy-2-(dihydroxymethyl)propan-4-diyl)benz-diamide,10,15,20-triphenyl porphyrin that is the precursor for the hybrid 1, γ = 2.6 × 10-28 esu for 54-N-(1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)benz-amide,10,15,20-triphenyl porphyrin that is the precursor for the hybrid 2), and the hybrid 1 (γ = 12.9 × 10-28 esu) is superior to the hybrid 2 (γ = 12.2 × 10-28 esu) reflecting more POM moieties covalently bonded to the porphyrin moiety exerting more significant influence on the third-order optical nonlinearities. Meanwhile, attachment of POMs on the porphyrin results in significant fluorescence quenching (fluorescence intensity is decreased 97% for the hybrid 1 and 80% for the hybrid 2 with respect to that of their corresponding porphyrin precursors) indicating strong electron transfer from porphyrin moiety to the polyoxometalate moiety. Lower transition energy, small energy difference between singlet and triplet excited states, and faster intersystem crossing (ISC) process of the hybrids are favorable to enhance the NLO responses of hybrids 1 and 2 resulting from the facile electron transfer from the porphyrin moiety to the Dawson POM moiety when the hybrids are subjected to laser irradiation, which is thought to be responsible to the superior of the hybrid 1 to hybrid 2 and the superior of the hybrids to their corresponding porphyrin precursors as well.

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