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1.
Braz. j. biol ; 83: e248083, 2023. tab, graf
Artículo en Inglés | LILACS-Express | MEDLINE, LILACSEXPRESS | ID: biblio-1278546

RESUMEN

Abstract Species of the genus Cordia have shown biological activities, such as anti-inflammatory, analgesic, antioxidant, antiviral, and antifungal activities. The species Cordia glabrata (MART) A.DC. Has no information concerning its phytochemical profile and possible biological activities. Thus, this study aimed to evaluate this profile in ethanolic extracts of young, adult and senescent leaves, as well as their antioxidant, photoprotective, antimicrobial, and virucidal potentials. Phytochemical analysis was performed by TLC (thin-layer chromatography) and showed the presence of flavonoids, tannins, and terpenes. The evaluation by UPLC-MS/MS (Ultra performance liquid chromatography - tandem mass spectrometer) evidenced the presence of caffeic (3.89 mgL-1), p-cumaric (6.13 mgL-1), and ferulic (0.58 mgL-1) acids, whilst, in GC/MS (Gas chromatography-mass spectrometry) analysis there was a greater amount of palmitic (51.17%), stearic (20.34%), linoleic (9.62%), and miristic (8.16%) fatty acids. The DPPH (2,2-Diphenyl-1-picrylhydrazyl) and ABTS+ (2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) radicals were used to verify the potential antioxidant activity, observing a better activity for the leaf extract in the adult phenological stage: 54.63 ± 1.06 µgmL-1 (DPPH) and 44.21 ± 1.69 mM (ABTS). The potential photoprotective activity of the extracts was determined by spectrophotometry and the in vitro values of SPF (Sun Protection Factor) in young and adult leaves (5.47 and 5.41, respectively) showed values close to the minimum SPF of 6.0 required by ANVISA (Brazilian Health Regulatory Agency). It was not observed an antimicrobial activity for Staphylococcus aureus with a minimum inhibitory concentration of 2000 μgmL-1, however the anti-herpetic assay against the Herpes simplex virus type 2 (HSV-2) showed a potent virucidal activity at the tested concentrations with CV50 value <0.195 μgmL-1 and a Selectivity Index (SI = CC50 / CV50) greater than 448. The results obtained in this study suggest that extracts of leaves of C. glabrata in their adult phenological stage have potential antioxidant, photoprotective and virucidal activity, considering in vitro test results.


Resumo Espécies do gênero Cordia apresentam atividades biológicas, como anti-inflamatória, analgésica, antioxidante, antiviral e antifúngica. Para a espécie Cordia glabrata (MART) A.DC., ainda não existem informações sobre seu perfil fitoquímico e possíveis atividades biológicas, deste modo, o presente estudo teve como objetivo avaliar este perfil em extratos etanólicos de folhas jovens, adultas e senescentes, bem como o potencial antioxidante, fotoprotetor, antimicrobiano e virucida. A análise fitoquímica foi realizada por CCD (Cromatografia em Camada Delgada), mostrando a presença de flavonóides, taninos e terpenos. Na avaliação por CLAE EM/EM (Cromatografia Líquida de Ultra Eficiência acoplada a Espectrometria de Massas) foi evidenciado a presença dos ácidos caféico (3,89 mgL-1), p-cumárico (6,13 mgL-1) e ferúlico (0,58 mgL-1), paralelamente, na CG/EM (Cromatografia Gasosa acoplada a Espectrometria de Massas) verificou-se maior quantidade dos ácidos graxos palmítico (51,17%), esteárico (20,34%), linoléico (9,62%) e mirístico (8,16%). Os radicais DPPH (2,2-Difenil-1-picrilhidrazil) e ABTS+ (2′-Azino-bis (ácido 3-etilbenzotiazolina-6-sulfônico)) foram utilizados para verificar o potencial antioxidante, observando-se uma atividade superior para o extrato da folha em sua fase fenológica adulta: 54,63 ± 1,06 µgmL-1 (DPPH) e 44,21 ± 1,69 mM (ABTS+). A potencial atividade fotoprotetora dos extratos foi determinada espectrofotometricamente e os valores in vitro de FPS (Fator de Proteção Solar) em folhas jovens e adultas (5,47 e 5,41 respectivamente) apresentaram valores próximos ao FPS mínimo de 6,0 exigido pela ANVISA (Agência Nacional de Vigilância Sanitária). Não foi observada atividade antimicrobiana para Staphylococcus aureus sendo a concentração inibitória mínima de 2000 μgmL-1, no entanto o ensaio anti-herpético contra o vírus Herpes simplex tipo 2 (HSV-2) mostrou uma potente atividade virucida nas concentrações testadas com um valor de CV50 <0,195 μgmL-1 e um Índice de Seletividade (IS = CC50 / CV50) maior que 448. Os resultados obtidos neste estudo sugerem que extratos de folhas de C. glabrata em seu estágio fenológico adulto apresentam potencial antioxidante, fotoprotetora e virucida, considerando os resultados de testes in vitro.

2.
Braz. j. biol ; 83: e244551, 2023. tab, graf
Artículo en Inglés | LILACS-Express | MEDLINE, LILACSEXPRESS | ID: biblio-1285626

RESUMEN

Abstract Origanum vulgare has been of great interest in academia and pharma industry due to its antioxidant, antifungal and antitumor properties. The present study aimed to find the anti-MRSA potential and in vivo toxicity assessments of O. vulgare. O. vulgare extract was used to monitor anti-MRSA activity in mice. Following MRSA established infection in mice (Mus musculus), treatment with O. vulgare was continued for 7 days. Autopsies were performed and re-isolation, gross lesion scoring and bacterial load in various organs were measured. Additionally, blood sample was analysed for hematological assays. Toxicity assessment of O. vulgare potential as medicine was done at 200 mg/kg and 400 mg/kg by evaluating liver and kidney functions. Bacterial load and gross lesion in lungs and heart were significantly low compared to positive control following O. vulgare treatment. Likewise, O. vulgare treated groups had hematological, neutrophil and TLC values similar to control groups. Increased AST, ALP and total bilirubin alongwith marked hepatocellular degeneration and distortion around the central vein, inflammatory cell infiltration, and cytoplasmic vacuolization of hepatic cells was observed at higher dose. It is concluded that crude extract of O. vulgare may contain beneficial secondary metabolites and in future may be explored for curing infectious diseases.


Resumo Origanum vulgare tem despertado grande interesse na academia e na indústria farmacêutica devido às suas propriedades antioxidantes, antifúngicas e antitumorais. O presente estudo teve como objetivo encontrar o potencial anti-MRSA e avaliações de toxicidade in vivo de O. vulgare. O extrato de O. vulgare foi usado para monitorar a atividade anti-MRSA em camundongos. Após infecção estabelecida por MRSA em camundongos (Mus musculus), o tratamento com O. vulgare foi continuado por 7 dias. As autópsias foram realizadas e o reisolamento, pontuação das lesões grosseiras e carga bacteriana em vários órgãos foram medidos. Além disso, a amostra de sangue foi analisada para ensaios hematológicos. A avaliação da toxicidade do potencial de O. vulgare como medicamento foi feita com 200 mg / kg e 400 mg / kg, avaliando as funções hepática e renal. A carga bacteriana e as lesões graves nos pulmões e no coração foram significativamente baixas em comparação com o controle positivo após o tratamento com O. vulgare. Da mesma forma, os grupos tratados com O. vulgare apresentaram valores hematológicos, de neutrófilos e de TLC semelhantes aos grupos de controle. Aumento de AST, ALP e bilirrubina total juntamente com degeneração hepatocelular marcada e distorção ao redor da veia central, infiltração de células inflamatórias e vacuolização citoplasmática de células hepáticas foram observados em doses mais altas. Conclui-se que o extrato bruto de O. vulgare pode conter metabólitos secundários benéficos e, no futuro, pode ser explorado para a cura de doenças infecciosas.

3.
Food Chem ; 367: 130696, 2022 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-34364145

RESUMEN

Oligosaccharides especially prebiotics take high attention in the development of foods because of their physiological properties in human health. They are generally synthetized enzymatically via transferases or hydrolases from mold or bacteria. The fact is that such oligosaccharides synthetized by probiotic bacteria, should be utilized by these microorganisms. This study focused on the production of oligosaccharides with prebiotic potential by crude enzyme preparation from bifidobacteria. Both monosubstrates and bisubstrates systems together with TLC and HPLC techniques, were applied. The crude enzyme preparation has different hydrolase activities such as α-glucosidase (2U/mL), ß-glucosidase (0.3 U/mL), α-galactosidase (1.2 U/mL), ß-galactosidase (0.4 U/mL), ß-fructosidase (11.5 U/mL). Additionally, it also has transglycosylation activities on lactose, lactulose, maltose and sucrose substrates. Two or three types of oligosaccharides were detected. The glycosyltransferase activity peaked at 45 °C, pH 6.6 and 30 g/100 mL substrate concentration. Significant high amount of oligosaccharides were formed in the case of lactose:sucrose combination than others. Both glucooligosaccharides and galactooligosaccharides are detected in the reaction mixtures of bisubstrate. When the lactose is present, the galactosyltransferation is predominated. One-one new types of oligosaccharides were detected in the reaction mixture of bioconversion. Among newly synthetized oligosaccharides, the fraction namely OS4 was utilized by probiotic bifidobacteria only. In conclusion, new types of galacto- and glucooligosaccharides with high prebiotic potentials were synthetized by the crude enzyme from probiotic Bifidobacterium strains.


Asunto(s)
Bifidobacterium , Prebióticos , Humanos , Lactulosa , Oligosacáridos , beta-Galactosidasa
4.
Methods Mol Biol ; 2387: 117-130, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-34643908

RESUMEN

Mycolactones are a family of polyketide synthase products made by the human pathogen Mycobacterium ulcerans that were recently identified as novel inhibitors of the host membrane translocation complex (Sec61). Here, we provide protocols for the purification of mycolactones from bacterial cultures, and for their quantitative assessment in biological samples.

5.
J Ethnopharmacol ; : 114697, 2021 Oct 06.
Artículo en Inglés | MEDLINE | ID: mdl-34626778

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Olax psittacorum (Lam.) Vahl. traditionally used by the tribal communities of 'INDIA' to heal conditions such as pain, psoriasis, mouthulcer, anemia, constipation as well as diabetes followed by scientific evidences like antipyretic, anti-inflammatory, antimicrobial, anti-viral, and anti-cancer property too. Aim of the experiment: Solvent fractionation process by using chloroform, distilled water and n-butanol has been developed to get the precipitate as a fraction (encrypted as FrAE-ISO) of leaf methanolic extract (LME) and established GC-MS and antiinflammatory evaluation. The aim was to enumerate the potency against inflammation of FrAE-ISO comparing with LME, SME (Stem methanolic extract) and Diclofenac. TLC of LME extract has been developed too for separation & evaluation of the compounds appeared as bands obtained by scraping process. The motive of the experiment was to acquire an isolate from LME that can able to show an emense anti-inflammatory action compared to LME and SME. MATERIALS AND METHODS: Priliminary phytochemical screening upon LME, SME and FrAE-ISO preformed by the standard methods of literatures. Scrapped portions of developed TLC plate (G-254 graded silica) of LME (n-Hexane:Ethylacetate; 7.5:2.5) were introduced to GC-MS evaluation. FrAE-ISO has introduced at a minute quantity (5 and 10 mg/kg/bw) within Wister albino rats (per os) against inflammation (model: carrageenan-induced paw edema) to evaluate its potency as compared to LME (25 mg/kg/bw), SME (25 mg/kg/bw) and Diclofenac (100 mg/kg). GC-MS evaluation has been conducted in both FrAE-ISO and scrapped sections to evaluate the presence of compounds qualitatively. RESULTS: LME and SME, qualitatively through different screening processes confirm the presence of glycosides, flavonoids, amino acids, tannins, and saponins respectively. According to the quantitative study of the extracts concerning total phenolic, flavonoid, tannin, and saponin content equivalent to gallic acid, quercetin, tannic acid, and diosgenin respectively have shown less amount of phenolic, flavonoid, and saponin content in SME (30.95, 205.33 and 30.82 mg/g extract respectively) as compared to LME (95.68, 713.33 and 66.41 mg/g extract respectively). Quantitative estimation has shown the presence of 825.27 mg of saponin equivalent to diosgenin per gram of FrAE-ISO. The GC-MS study has revealed that every section of the leaf extract has " Hexadecanoic acid, methyl ester " in common with other important compounds responsible for its potent contribution towards the anti-inflammatory property. The scrapped portions of the TLC plate having mixture of compounds but FrAE-ISO has shown a sharp peak in GC-MS (up to 34 min of run time) as well as few crystals like structures under the binocular microscope. Compact doses of FrAEISO (yield = 1.645%) i.e. 5 and 10 mg/kg body weight was able to compete with 100 mg/kg Diclofenac portraying 88%-95% inhibition respectively throughout all phases of inflammation with no-significant differences compared to standard evaluated by ANOVA (in SPSS). CONCLUSION: Olax psittacorum (Lam.) Vahl. could be a good choice to explore its importance within the pharmacognostic field of drug development and might be a better source of herbal-derived lead compounds which can help to treat other various activities like ulcer healing or anti-anemic property etc.

6.
BMC Complement Med Ther ; 21(1): 260, 2021 Oct 12.
Artículo en Inglés | MEDLINE | ID: mdl-34641875

RESUMEN

BACKGROUND: Current therapy of chronic hepatitis C virus (HCV) with direct-acting antivirals (DAAs) has dramatically improved the sustained virologic response (SVR) of affected patients; however, treatment with DAAs remains expensive, and drug-resistant HCV variants remain a threat. As a result, there is still a need to continue to develop affordable and effective drugs for the treatment of HCV. Previously, we have demonstrated that a crude extract from Artocarpus heterophyllus leaves is a potential anti-HCV candidate. In this study, we have further purified this crude extract, examined which sub-fraction possesses the highest antiviral activity, and then explored its efficacy at different HCV life cycle stages. We also assessed synergistic antiviral effects between the A. heterophyllus extract and commercially available anti-HCV drugs. METHODS: We used vacuum liquid chromatography (VLC) and high-performance liquid chromatography (HPLC) to fractionate a dichloromethane extract of A. heterophyllus leaves. We then examined the anti-HCV activity of the fractions using HCV genotype 2a, JFH1a; the antiviral mode of action was determined by exploring adding the treatments at different times. We examined the antiviral effects on the viral entry stage through a virucidal activity test, viral adsorption examination, and pretreatment of cells with the drug. The effects on the post-viral entry stage were determined by the levels of HCV protein expression and HCV RNA expression in infected cells. RESULTS: Through activity guided purification, we identified the sub-fraction FR3T3 as possessing the most robust anti-HCV activity with an IC50 value of 4.7 ± 1.0 µg/mL. Mode-of-action analysis revealed that FR3T3 inhibited post-viral entry stages such as HCV NS3 protein expression and HCV RNA replication with marginal effects on the viral entry stage. Thin-layer Chromatography (TLC) indicated that FR3T3 contained terpenoids and chlorophyll-related compounds. We also found a synergistic antiviral activity when the DCM extract of A. heterohyllus was used in combination therapy with commercial anti-HCV drugs; Ribavirin, Simeprevir, Cyclosporin A. CONCLUSIONS: The extract of A. heterophyllus and its sub-fraction, FR3T3, presented here have anti-HCV activities and could be candidate drugs for add-on-therapy for treatment of chronic HCV infections.

7.
Pulmonology ; 2021 Oct 08.
Artículo en Inglés | MEDLINE | ID: mdl-34629326

RESUMEN

INTRODUCTION: The diagnosis and severity assessment of COPD relies on spirometry, and in particular the FEV1. However, it has been proposed that hyperinflation and air-trapping are better predictors of exercise capacity and mortality than the FEV1. RESEARCH: QUESTION: Does static hyperinflation predict exercise capacity? METHODS: We conducted an observational prospective study. Patients with COPD referred to the lung function laboratory were consecutively recruited. Patients with hyperinflation (the experimental group) were compared to patients without hyperinflation (the control group). The sample sizes were determined assuming an effect size of 0.5 and a power of 0.80. RESULTS: We recruited 124 participants, of whom 87% were male, the mean age was 66.1 ± 8.8 years. 67% were symptomatic (GOLD B or D). Airflow limitation was moderate to severe in the majority of patients (median FEV1 47%, IQR 38-65%) and 43% of patients had static hyperinflation. The median 6MWD was 479 meters (404-510) and peak workload in CPET was 64 watts (46-88) with peak VO2 1.12 L/min, 0.89-1.31 L/min. Patients with lower FEV1, DLCO and IC/TLC and higher RV/TLC had reduced exercise capacity in both 6MWT and CPET, measured as lower distance, greater desaturation and ∆Borg dyspnoea, and reduced workload, peak VO2 and peak VE and higher desaturation and ventilatory limitation (VE/MVV). An IC/TLC < 0.33 predicted reduced exercise performance (peak O2 <60%). Dyspnoea assessed by mMRC and QoL measured by CAT and CCQ were also worse in the hyperinflation in COPD patients. CONCLUSION: In COPD patients, IC/TLC and RV/TLC are valuable predictors of exercise performance in both 6MWT and CPET and PRO.

8.
EJNMMI Radiopharm Chem ; 6(1): 35, 2021 Oct 11.
Artículo en Inglés | MEDLINE | ID: mdl-34633572

RESUMEN

BACKGROUND: Nanocolloidal human serum albumin radiolabelled with 99mTc provides a diagnostic radiopharmaceutical for sentinel node lymphoscintigraphy. NanoHSA (Nanotop), a commercially available kit, enables the simple preparation of this radiopharmaceutical via reconstitution with pertechnetate eluted from a generator. Thin-layer chromatography is widely used for determining radiochemical purity in clinical nuclear medicine. Quality control methods recommended by the manufacturer were sometimes reported to yield variable results. Therefore, we proposed and evaluated three alternative thin-layer chromatography methods for the quality control of [99mTc]Tc-NanoHSA from a commercially available kit. RESULTS: The radiochemical purity of [99mTc]Tc-NanoHSA determined with all methods was reproducible and met the requirements of the SPC and the European Pharmacopoeia (≥ 95%). Our quality control using iTLC-SG chromatographic paper in methyl ethyl ketone mobile phase identified only free pertechnetate as impurity, resulting in > 99% RCP. The quality control using iTLC-SG in 85% methanol or iTLC-SA in 0.9% NaCl identified an additional small fraction of a hydrophilic impurity, resulting in 95-97% RCP. Glucose was identified as a potential 99mTc-carrying hydrophilic species contributing to hydrophilic impurities. CONCLUSION: Our quality control of [99mTc]Tc-NanoHSA with non-polar mobile phase tended to underestimate the amount of hydrophilic impurities, although without compromising the final quality of the radiopharmaceutical. Alternative TLC methods using aqueous mobile phases enabled a more accurate determination of hydrophilic impurities.

9.
Sci Rep ; 11(1): 19624, 2021 Oct 04.
Artículo en Inglés | MEDLINE | ID: mdl-34608174

RESUMEN

The putative ferricrocin synthetase gene ferS in the fungal entomopathogen Beauveria bassiana BCC 2660 was identified and characterized. The 14,445-bp ferS encodes a multimodular nonribosomal siderophore synthetase tightly clustered with Fusarium graminearum ferricrocin synthetase. Functional analysis of this gene was performed by disruption with the bar cassette. ΔferS mutants were verified by Southern and PCR analyses. HPLC and TLC analyses of crude extracts indicated that biosynthesis of ferricrocin was abolished in ΔferS. Insect bioassays surprisingly indicated that ΔferS killed the Spodoptera exigua larvae faster (LT50 59 h) than wild type (66 h). Growth and developmental assays of the mutant and wild type demonstrated that ΔferS had a significant increase in germination under iron depletion and radial growth and a decrease in conidiation. Mitotracker staining showed that the mitochondrial activity was enriched in ΔferS under both iron excess and iron depletion. Comparative transcriptomes between wild type and ΔferS indicated that the mutant was increased in the expression of eight cytochrome P450 genes and those in iron homeostasis, ferroptosis, oxidative stress response, ergosterol biosynthesis, and TCA cycle, compared to wild type. Our data suggested that ΔferS sensed the iron excess and the oxidative stress and, in turn, was up-regulated in the antioxidant-related genes and those in ergosterol biosynthesis and TCA cycle. These increased biological pathways help ΔferS grow and germinate faster than the wild type and caused higher insect mortality than the wild type in the early phase of infection.

10.
AMB Express ; 11(1): 135, 2021 Oct 08.
Artículo en Inglés | MEDLINE | ID: mdl-34623537

RESUMEN

Incidence of various dreadful microbial infections and the development of antibiotic resistance by infection causative microbes are the main reasons for reducing aquaculture productivity. Hence, there is an immense need for the discovery of alternative and efficient treatment for quick recovery of diseased fishes. In the present study, Suaeda maritima leaf extracts (hexane, diethyl ether, ethanol, and water) were screened for in vitro and in vivo antibacterial and antioxidant activities. Out of all the four extracts, ethanolic extract showed highest antibacterial activity against S. aureus (4.9 ± 1.3 mm), B. subtilis (1.6 ± 0.3 mm), K. pneumoniae (4.2 ± 1.8 mm), and P. aeruginosa (4.1 ± 1.2 mm). Similarly, antioxidant activity was also higher for ethanolic extract (500 µg/mL) based on DPPH radical scavenging ability (71.6 ± 1.4%) and reducing potential (149 µg/mL) assays. Further, ethanolic extract was purified consecutively via column chromatography and preparative TLC where an active fraction was selected based on highest antibacterial (10.1 ± 1.4 mm) and antioxidant properties (82.3 ± 2.8%). Active fraction was loaded onto mass spectroscopy and identified the presence of four active constituents such as 1,2,9,10-tetramethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinolin-3-yl) methanol; 3',7-Dimethoxy-3-hydroxyflavone; Saponin and (19R)9acetyl19hydroxy10,14dimethyl20oxopentacyclo[11.8.0.0 < 2,10 > .0 < 4,9 > .0 < 14,19 >]henicos-17-yl-acetate. Besides, in vivo studies were conducted on Catla catla fingerlings infected with P. aeruginosa under laboratory conditions. The fingerlings were segregated into 5 groups, among which group 4 and 5 were treated with crude and purified extracts. Both the extracts were efficient in treating infected fingerlings and recorded 100% survival rate which is even better than group-3 treated with a synthetic antibiotic (77%). Hence, S. maritima leaf extract can be considered as a possible alternative medicine in aquaculture.

11.
Artículo en Inglés | MEDLINE | ID: mdl-34601693

RESUMEN

Monitoring aquatic health from environmental pollutants is critical, none more so than bisphenol-A (BPA), a ubiquitous endocrine-disrupting chemical (EDC). The present study brings out the responses of selected transcripts, hormone levels, and tissue histomorphology in a widely distributed fish species Cyprinus carpio (Linn.), following exposure to environmentally relevant (10, 100 ng/L) and higher (1000 ng/L) concentration of BPA. The response of cyp19a1a, cyp19a1b, and c3 significantly decreased, while that of vtg increased in their respective tissue domains. The hematological parameters TEC, Hb, and Hct decreased significantly in contrast to TLC (p < 0.05) at all exposure concentrations, whereas none of the erythrocytic indices (MCV, MCH, and MCHC) was perturbed. The steroidogenic hormone levels, such as estradiol and progesterone, increased significantly with increasing BPA concentrations. In contrast, the testosterone and all the thyroid hormones (T3, T4, and TSH) were suppressed significantly (p < 0.05). At the histological level, the BPA induced chondrocyte proliferation, which was accompanied by hemorrhage of the gill lamellae, increased melanomacrophagic centers (MMCs), and degeneration of tubules and fluid accumulation in the kidney. In parallel, binucleated hepatocytes and inflammations were prominent in the liver. Collectively, the histomorphology confirmed induction of degenerative effects in all the tissues investigated, while the cyclic responses of biochemical markers suggest an ability to regulate the impacts. However, a chronic exposure could result in overriding the endemic reproductive pathways with potential population-level effects. In conclusion, the study identified multiple molecular, cellular, and physiological markers that could be employed to detect early signs of BPA and more broadly EDC exposures. These markers in combination with a wide distribution of C. carpio should allow comparative studies of pollutants at environmental concentrations.

12.
Pak J Pharm Sci ; 34(3(Supplementary)): 1149-1156, 2021 May.
Artículo en Inglés | MEDLINE | ID: mdl-34602445

RESUMEN

As part of our continuous research to understand the interaction mechanism of drug and metallo-elements, heavy metal complexes of azithromycin (AZI) were synthesized with arsenic oxide, lead carbonate and silver chloride salts in molar ratio of 2: 1 (L: M). Synthesized heavy metal complexes have shown good percent yield and characterized through spectroscopic parameters including UV-Visible, TLC, FT-IR, NMR and elemental analysis (CHN). Spectroscopic characterization reveals the binding of ligand AZI with heavy metals in bi-dentate manner involving the hydroxide and 9a-NCH3 group of the aglycone ring of AZI. These newly synthesized heavy metal complexes were evaluated for their antimicrobial response against selected gram positive and gram negative organisms and antifungal species. It was noted that all newly synthesized complexes exhibits increased activity against B.subtilus whereas, AZI itself didn't show any activity, while synthesized complexes have low to moderate response against all the studied organisms. Complex A-M12 possess greater enzymatic response against both urease and alpha chymotrypsin among all the studied complexes. Results obtained were then statistically analyzed through one way ANOVA and Dunnett's test by using SPSS version 20.0 suggesting the significant response of complexes against selected organisms.

13.
Artículo en Inglés | MEDLINE | ID: mdl-34605186

RESUMEN

Plants of the Calea genus have been reported to contain lipophilic compounds, such as sesquiterpene lactones, with cytotoxic effect against different cancer cell lines. The aim of this manuscript was to investigate the chemical profile and cytotoxic activity of different fractions from C. phylolepis leaves on different human cancer cell lines. The fractions were prepared using solvent extraction of increasing polarity, yielding hexane, ethyl acetate, and methanolic fractions. All fractions were chemically analysed by thin layer chromatography (TLC) and their cytotoxic activity against HT-29 (colon adenocarcinoma), MCF-7 (breast cancer), U-251MG (malignant glioblastoma), and L929 (mouse fibroblast) cell lines was investigated. Among these, the hexane and ethyl acetate fractions showed higher cytotoxic effects, while the methanolic fraction did not show any cytotoxic effects. The major bioactive compound from the hexane fraction (12.15%) was isolated using chromatographic methods and was identified by nuclear magnetic resonance spectroscopy (NMR) and gas chromatography-mass spectrometry (GC-MS) analysis as 6-epi-ß-verbesinol coumarate. This compound showed activity against breast cancer cells (IC50 = 5.8 ± 1.0 µg/mL), similar to etoposide. Furthermore, 6-epi-ß-verbesinol coumarate showed low cytotoxicity to normal fibroblast cells, suggesting a high selectivity index (SI = 7.39) against breast cancer cells.

14.
Biol Futur ; 2021 Oct 04.
Artículo en Inglés | MEDLINE | ID: mdl-34606079

RESUMEN

Nowadays, the accumulation of non-degradable plastics and other disposed wastes leads to environmental pollution across the world. The production of eco-friendly and cost-effective poly-ß-hydroxybutyrate (PHB) could be a better alternative to conventional petroleum-based plastics and prevent environmental pollution. Besides, the area in and around Namakkal, Tamil Nadu, India is well known for poultries, currently facing the number of environmental issues due to the accumulation of chicken feather waste. This study focused on the production of eco-friendly PHB by recycling poultry (chicken feather) waste as the substrate. The native PHB producers were screened from the chicken waste disposal site in Namakkal by Sudan black B staining method. Further, the potent bacterial isolate was identified as Pseudomonas aeruginosa (NCBI accession MF18889) by phenotypic and genotypic characteristics. The PHB production media with chicken feather waste was statistically optimized by response surface methodology. The dry weight of PHB produced under optimized condition (15.96 g/L chicken feather waste, 37 °C temperature, 19.8 g/L glucose and 6.85 pH) was found to be 4.8 g/L. Besides, PHB was characterized and confirmed by thin-layer chromatography, Fourier-transform infrared spectroscopy and Gas chromatography-mass spectrometry analysis. Thus, this study concludes that poultry waste could be a complex nitrogen source for improving the growth of PHB producers and substantially increasing the yield of PHB, and it will be an eco-friendly and low-cost production in bioprocess technology.

15.
Acta Parasitol ; 2021 Oct 08.
Artículo en Inglés | MEDLINE | ID: mdl-34625859

RESUMEN

PURPOSE: Dogs are of immense social, psychological and economic importance in Nigeria and are severely affected by African trypanosomosis. However, the prevalence of canine African trypanosomosis (CAT) in Nigeria is underreported and the identification of the parasites relies mostly on basic morphological characteristics under the microscope, which could be misleading. The present study was carried out to determine the prevalence and characterize trypanosomes isolated from dogs in South east Nigeria. METHODS: A cross-sectional survey was carried out to determine the prevalence and molecular identification of trypanosomes in dogs in Enugu North Senatorial Zone (ENSZ), South east Nigeria. Dogs (n = 450) were randomly sampled, their blood collected and some characteristics such as sex, breed, sampling location, season and age duly noted. The blood samples were screened for trypanosomosis using standard trypanosome detection techniques. Trypanosome-positive blood samples were spotted on FTA® cards for molecular identification using nested Tubulin-PCR, ITS-PCR, TgsGP-PCR, and DNA sequencing. Some hematological parameters of the dogs such as packed cell volume (PCV), total leucocyte count (TLC), red blood cell count (RBC) were also determined. RESULTS: Of the 450 dogs sampled, 51 dogs were positive for trypanosomes with a prevalence rate of 11.3% (95% CI = 0.087-0.146). Trypanosoma brucei was the predominant trypanosome species infecting dogs in the study area. T. congolense, T. evansi, and T. vivax were also identified. The prevalence of canine trypanosomosis was significantly associated with season (χ2 = 13.821, df = 1, P = 0.0001) and the sampling location (χ2 = 6.900, df = 2, P = 0.032) while sex, breed, and age were not. The PCV and RBC of the infected dogs were significantly lower (p < 0.0001) than those of the uninfected dogs. CONCLUSIONS: CAT due to T. brucei is very prevalent in Enugu North Senatorial Zone, South east Nigeria and is associated with hematological changes. Our study also detected T. vivax in dogs in South east Nigeria which appears to be the first report of T. vivax in a dog in Nigeria.

16.
J AOAC Int ; 2021 Oct 09.
Artículo en Inglés | MEDLINE | ID: mdl-34626119

RESUMEN

BACKGROUND: Modafinil (MDF) is one of the drugs that used for the treatment of narcolepsy. OBJECTIVE: This manuscript involves the development and validation of two chromatographic stability indicating methods for MDF in the presence of its acid induced degradation. METHODS: Modafinil was degraded under different stress conditions and identification of the degradation product was performed using infrared and mass spectroscopy. The first method was thin layer chromatography where aluminum backed silica gel 60F254 plates were used and the developing system was dichloromethane- methanol (9:1, v/v). While the second method was an eco- friendly (HPLC) that utilized C-18 column and ethanol- H2O (30:70, v/v) as a mobile phase at flow rate 1 mL/min and UV detection at 220 nm. RESULTS: Good linear relationships were obtained within ranges of (1-10 µg/band) and (2-10 µg/mL) for TLC-densitometry and HPLC, respectively. The obtained results were statistically compared with those of the official HPLC method and showed no significant difference with respect to their accuracy and precision at p = 0.05. Greenness scores represent excellent green analysis in comparison with the reported studies. CONCLUSIONS: The proposed methods were validated according to ICH guidelines and were applied on bulk powder and pharmaceutical dosage form using eco-friendly mobile phases as the worldwide trend. HIGHLIGHTS: Chromatographic methods have been validated for estimation of MDF in the presence of its degradation product. Clarification of degradation pathway and the elucidation of the structure were stated for the first time. It's the first published method using greenness assessment metrics for the analysis of MDF.

17.
PLoS One ; 16(10): e0257807, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34613977

RESUMEN

Patients after lung transplantation are at risk for life-threatening infections. Recently, several publications on COVID-19 outcomes in this patient population appeared, but knowledge on optimal treatment, mortality, outcomes, and appropriate risk predictors is limited. A retrospective analysis was performed in a German high-volume lung transplant center between 19th March 2020 and 18th May 2021. Impact of COVID-19 on physical and psychological health, clinical outcomes, and mortality were analyzed including follow-up visits up to 12 weeks after infection in survivors. Predictive parameters on survival were assessed using univariate and multivariate proportional hazards regression models. Out of 1,046 patients in follow-up, 31 acquired COVID-19 during the pandemic. 12 of 31 (39%) died and 26 (84%) were hospitalized. In survivors a significant decline in exercise capacity (p = 0.034), TLC (p = 0.02), and DLCO (p = 0.007) was observed at follow-up after 3 months. Anxiety, depression, and self-assessed quality of life remained stable. Charlson comorbidity index predicted mortality (HR 1.5, 1.1-2.2; p = 0.023). In recipients with pre-existing CLAD, mortality and clinical outcomes were inferior. However, pre-existing CLAD did not predict mortality. COVID-19 remains a life-threatening disease for lung transplant recipients, particularly in case comorbidities. Further studies on long term outcomes and impact on pre-existing CLAD are needed.


Asunto(s)
COVID-19/epidemiología , Trasplante de Pulmón/estadística & datos numéricos , Receptores de Trasplantes/estadística & datos numéricos , Adulto , Femenino , Hospitalización , Humanos , Masculino , Persona de Mediana Edad , Calidad de Vida , Estudios Retrospectivos , Medición de Riesgo
18.
ACS Chem Biol ; 2021 Oct 14.
Artículo en Inglés | MEDLINE | ID: mdl-34647721

RESUMEN

Poly(ADP-ribose) polymerases, PARPs, transfer ADP-ribose onto target proteins from nicotinamide adenine dinucleotide (NAD+). Current mass spectrometric analytical methods require proteolysis of target proteins, limiting the study of dynamic ADP-ribosylation on contiguous proteins. Herein, we present a matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) method that facilitates multisite analysis of ADP-ribosylation. We observe divergent ADP-ribosylation dynamics for the catalytic domains of PARPs 14 and 15, with PARP15 modifying more sites on itself (+3-4 ADP-ribose) than the closely related PARP14 protein (+1-2 ADP-ribose)-despite similar numbers of potential modification sites. We identify, for the first time, a minimal peptide fragment (18 amino-acids) that is preferentially modified by PARP14. Finally, we demonstrate through mutagenesis and chemical treatment with hydroxylamine that PARPs 14/15 prefer acidic residues. Our results highlight the utility of MALDI-TOF in the analysis of PARP target modifications and in elucidating the biochemical mechanism governing PARP target selection.

19.
Artículo en Chino | MEDLINE | ID: mdl-34624946

RESUMEN

Objective: To investigate the clinical characteristics of acute exacerbation of acute lung disease (AECOPD) and to provide reference for clinical diagnosis and treatment. Methods: From January 2018 to December 2018, 127 patients with AECOPD were investigated retrospectively in March 2020, including 65 cases of pneumoconiosis with AECOPD group, 62 cases of AECOPD group, 127 cases of AECOPD group, the clinical characteristics, length of stay, cost difference and the correlation between pulmonary function and blood gas were analyzed in patients with AECOPD. Results: There was no significant difference in age, height, weight, BMI, ethnicity and smoking between the two groups (P>0.05) . The percentage of Neutrophil and hs-crp in pneumoconiosis combined with AECOPD group were significantly higher than those in AECOPD group (P<0.05) . The oxygen partial pressure in pneumoconiosis combined AECOPD group was lower than that in control group (P<0.05) . VC, FVC/Pred%, FEV(1)/Pred% in pneumoconiosis combined with AECOPD group were lower than those in AECOPD group, RV/Pred% and RV/TLC were higher than those in AECOPD group (P<0.05) . The hospitalization time and cost of the patients with AECOPD were significantly higher than that of the patients with AECOPD (P<0.05) . Conclusion: Compared with AECOPD group, the patients with pneumoconiosis combined AECOPD group had higher infection inflammation level, lower pulmonary function, longer hospitalization time and higher hospitalization cost.


Asunto(s)
Neumoconiosis , Enfermedad Pulmonar Obstructiva Crónica , Enfermedad Crónica , Carbón Mineral , Humanos , Neumoconiosis/complicaciones , Estudios Retrospectivos
20.
Beijing Da Xue Xue Bao Yi Xue Ban ; 53(5): 902-906, 2021 Oct 18.
Artículo en Chino | MEDLINE | ID: mdl-34650292

RESUMEN

OBJECTIVE: To analyze the preoperative pulmonary function in rotator cuff injury patients and the possible influencing factors. METHODS: All the rotator cuff surgery patients who underwent pre-operative pulmonary function examination in Peking University Third Hospital from Jan. 2020 to Jun. 2020 were retrospectively reviewed. Their perioperative medical records and main parameters of pulmonary function were collected from database management system, and their gender, age, body mass index (BMI), smoking history, time from injury, visual analogue scale (VAS) and other factors impacting on preoperative pulmonary function were studied. RESULTS: Twenty-nine patients with rotator cuff injury were included, among whom 1 patient was reported to have restrictive ventilation dysfunction and 2 patients to have obstructive ventilation dysfunction. All the three patients denied the history of respiratory diseases, and had no respiratory symptoms. In all enrolled patients, the mean forced expiratory volume in one second (FEV1)/ forced vital capacity (FVC) was 79.2%±5.9%, and the mean VAS pain score was 3.66±1.26. In addition, the dynamic pulmonary functions (FVC, FEV1) were reduced in more than half of the elderly, and the total lung capacity (TLC) was lower than the estimated value in 2/3 of the elderly. There were significant differences in three main indexes of pulmonary functions between genders, and the percentage of the estimated TLC between normal BMI group (18 kg/m2 < BMI < 24 kg/m2) and overweight/obesity group (BMI≥24 kg/m2) was significantly different. Based on the injury time longer than 1 year or not, the results indicated that FVC and TLC were significantly different between the two groups. CONCLUSION: In addition to gender and age, time from injury and severity of pain, as well as overweight/obesity, may influence pulmonary function outcomes in the elderly rotator cuff patients. Targeted intervention can be carried out on these factors before surgery. Preoperative lung function test can be used as one of the basic evaluation indexes for respiratory training and rehabilitation of patients.

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