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1.
Anticancer Agents Med Chem ; 24(5): 317-333, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-37936467

RESUMO

AIMS: The aim of this study is to isolate the Millettia pinnata (Karanj) leaf extract for pure compound with anticancer properties and to study the molecular target of the isolates in non-small cell lung cancer cell lines. BACKGROUND: In our earlier research Millettia pinnata leaf extract has demonstrated potential anticancer activities. Thus, in pursuit of the bioactive compounds, the most potential active extract from our previous study was purified. Furthermore, the anticancer properties of the isolated compound karanjin was studied and aimed for apoptosis and restraining growth. METHODS: A novel method was developed through column chromatography for isolation and purification of the compound karanjin from leaf chloroform extract. The purified component was then characterised using FTIR, mass spectrometry, and NMR. An MTT-based cytotoxicity assay was used to analyse cell cytotoxicity, whereas fluorescence staining was used for apoptosis and reactive oxygen species inhibition quantification. Furthermore, the real-time PCR assay was used to determine the molecular mechanism of action in cells causing cytotoxicity induced by karanjin dosing. RESULTS: The anticancer activity of karanjin in A549 cell line exhibited prominent activity revealing IC50 value of 4.85 µM. Conferring the predicted molecular pathway study, karanjin restrains the proliferation of cancer cells through apoptosis, which is controlled by extrinsic pathway proteins FAS/FADD/Caspases 8/3/9. Downregulation of KRAS and dependent gene expression also stopped cell proliferation. CONCLUSION: Karanjin has been identified as a compound with potential effect in non-small cell lung cancer cells. Molecular mechanism for apoptosis and inhibition of reactive oxygen species induced through H2O2 were observed, concluding karanjin have medicinal and antioxidant properties.


Assuntos
Benzopiranos , Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Humanos , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Espécies Reativas de Oxigênio/metabolismo , Peróxido de Hidrogênio/farmacologia , Neoplasias Pulmonares/tratamento farmacológico , Linhagem Celular Tumoral , Apoptose , Extratos Vegetais/farmacologia , Modelos Teóricos
2.
Bioorg Chem ; 140: 106805, 2023 11.
Artigo em Inglês | MEDLINE | ID: mdl-37634269

RESUMO

Enzymes are the biological macromolecules that have emerged as an important drug target as their upregulation/imbalance leads to various pathological conditions, such as inflammation, parasitic infection, Alzheimer's, cancer, and many others. Here, we designed and synthesized some morpholine tethered novel aurones and evaluated them as potential inhibitors for CTSB, α-amylase, lipase and activator for trypsin. All the newly synthesized compounds were fully characterized by various spectroscopic techniques (1H NMR, 13C NMR, HRMS) and the Z-configuration to them was assigned based on single crystal XRD data and 1H NMR chemical shift values. Further, the hybrids were evaluated for their intracellular (cathepsin B) and extracellular (trypsin, lipase, amylase) enzyme inhibition potencies. The in-vitro inhibition screening against cathepsin B revealed that most of the synthesized compounds are good competitive inhibitors (% inhibition = 22.91-75.04), with 6q (% inhibition = 75.04) and 6r (% inhibition = 71.13) as the eminent inhibitors of the series. At the same time, they exhibited weak to moderate inhibition towards amylase (% inhibition = 7.22-22.48) and lipase (% inhibition = 16.29-54.83). A significant trypsin activation (% activation = 107.42-196.47) was observed even at the micromolar concentration of the compounds. Furthermore, the drug-modeling studies showed a good correlation between the in-vitro experimental results and the calculated binding affinity of the screened compounds with all the tested enzymes. These findings are expected to provide a new lead in drug development for different pathological disorders wherever these enzymes are involved.


Assuntos
Catepsina B , Morfolinas , Simulação de Acoplamento Molecular , Tripsina , Morfolinas/farmacologia , Amilases , Lipase
3.
Int J Biol Macromol ; 222(Pt B): 2270-2308, 2022 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-36216101

RESUMO

The identification of x-ray crystal structure of cathepsin B (CTSB) in the early 90's enabled researchers to embark on a journey to understand and demystify its multiple catalytic mechanisms (endopeptidase/carboxypeptidase/peptidyl-dipeptidase) in diverse physiological processes and their switching into one another under different conditions. The engagement of CTSB in different pathological conditions due to its over-expression further highlighted the enhanced research interest around the domain. The occurrence of over-expressed CTSB in various diseases like Alzheimer's, cancer, arthritis, cardiovascular, etc., and the use of CTSB inhibitors for the treatment of these diseases have established its involvement in different pathological conditions. Such an understanding tempted researchers to design, synthesize, and screen diverse classes of compounds against CTSB. This in turn, helped in understanding their interactions with the active sites of the enzyme. Heterocyclic compounds comprise a very rich and broad class of medicinally important compounds that also hold great potential for CTSB inhibition. This review covers the CTSB inhibition potential of various natural and synthetic heterocyclic scaffolds. Researchers working in the fields of molecular modeling, drug design and development, and enzyme inhibitors can benefit significantly from this review.


Assuntos
Compostos Heterocíclicos , Neoplasias , Humanos , Catepsina B , Compostos Heterocíclicos/farmacologia , Inibidores Enzimáticos , Desenho de Fármacos
4.
Soft comput ; 26(22): 12115-12135, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36043118

RESUMO

In this paper, we presented a long short-term memory (LSTM) network and adaptive particle swarm optimization (PSO)-based hybrid deep learning model for forecasting the stock price of three major stock indices such as Sensex, S&P 500, and Nifty 50 for short term and long term. Although the LSTM can handle uncertain, sequential, and nonlinear data, the biggest challenge in it is optimizing its weights and bias. The back-propagation through time algorithm has a drawback to overfit the data and being stuck in local minima. Thus, we proposed PSO-based hybrid deep learning model for evolving the initial weights of LSTM and fully connected layer (FCL). Furthermore, we introduced an adaptive approach for improving the inertia coefficient of PSO using the velocity of particles. The proposed method is an aggregation of adaptive PSO and Adam optimizer for training the LSTM. The adaptive PSO attempts to evolve the initial weights in different layers of the LSTM network and FCL. This research also compares the forecasting efficacy of the proposed method to the genetic algorithm (GA)-based hybrid LSTM model, the Elman neural network (ENN), and standard LSTM. Experimental findings demonstrate that the suggested model is successful in achieving the optimum initial weights and bias of the LSTM and FC layers, as well as superior forecasting accuracy.

5.
Anticancer Agents Med Chem ; 22(12): 2292-2302, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34951582

RESUMO

BACKGROUND: The study aimed to investigate the augmented cytotoxic effects of polymer-coated (polylactic- co-glycolic acid-PLGA) gold nanoparticles (GNPs) carrying 5-fluorouracil (5-FU) in the management of lung cancer. METHODS: In this study, several formulations were prepared using a double emulsion (water-oil-water) method and evaluated for drug release behavior, compatibility, cell line toxicity (A549), and apoptosis assessment. RESULTS: Characterization results showed spherical polydispersed particles with size 29.11-178.21 nm, polydispersity index (PDI) 0.191-292, and zeta potential (ZP) 11.19-29.21 (-mV), respectively. Compared to others, the optimized polymer-coated 5-FU loaded gold nanoparticles (PFGNPs) illustrated a maximum drug loading (93.09±10.75%). The percent cumulative drug release of polymer-coated 5-FU loaded nanoparticles (PFNPs), 5-FU loaded gold nanoparticles (FGNPs), (PFGNPs) and 5-FU solution were 47.87±1.5, 41.09±1.8, 56.31±1.05, and 98.8±4.2%, respectively, over 10 h. following zero-order release kinetics (except 5-FU solution). From the MTT results, the cytotoxic effect of PFGNPs on the A549 cells was 82.89% compared to the 5-FU solution (74.91 %). EGFR and KRAS gene expression analysis under the influence of PFNPs, FGNPs, PFGNPs, and 5-FU was studied and observed maximum potency for PFNPs. CONCLUSION: PLGA coated biogenic gold nanoparticles have a combined effect to achieve high drug loading, sustained delivery, improved efficacy, and enhanced permeation. Conclusively, the approach may be promising to control lung cancer with reduced toxicity and improved efficacy.


Assuntos
Antineoplásicos , Neoplasias Pulmonares , Nanopartículas Metálicas , Nanopartículas , Antineoplásicos/farmacologia , Portadores de Fármacos , Fluoruracila/farmacologia , Ouro/farmacologia , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Tamanho da Partícula , Água
6.
Chem Biol Drug Des ; 100(6): 843-869, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-34592059

RESUMO

Over the past few decades, the dynamic progress in the synthesis and screening of heterocyclic compounds against various targets has made a significant contribution in the field of medicinal chemistry. Among the wide array of heterocyclic compounds, triazole moiety has attracted the attention of researchers owing to its vast therapeutic potential and easy preparation via copper and ruthenium-catalyzed azide-alkyne cycloaddition reactions. Triazole skeletons are found as major structural components in a different class of drugs possessing diverse pharmacological profiles including anti-cancer, anti-bacterial, anti-fungal, anti-viral, anti-oxidant, anti-inflammatory, anti-diabetic, anti-tubercular, and anti-depressant among various others. Furthermore, in the past few years, a significantly large number of triazole hybrids were synthesized with various heterocyclic moieties in order to gain the added advantage of the improved pharmacological profile, overcoming the multiple drug resistance and reduced toxicity from molecular hybridization. Among these synthesized triazole hybrids, many compounds are available commercially and used for treating different infections/disorders like tazobactam and cefatrizine as potent anti-bacterial agents while isavuconazole and ravuconazole as anti-fungal activities to name a few. In this review, we will summarize the biological activities of various 1,2,3-triazole hybrids with copious oxygen-containing heterocycles as lead compounds in medicinal chemistry. This review will be very helpful for researchers working in the field of molecular modeling, drug design and development, and medicinal chemistry.


Assuntos
Química Farmacêutica , Triazóis , Azidas , Reação de Cicloadição , Desenho de Fármacos , Estrutura Molecular , Relação Estrutura-Atividade , Triazóis/farmacologia , Triazóis/química
7.
J Med Phys ; 47(3): 262-269, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36684696

RESUMO

Purpose: To study the impact of different optimization methods in dealing with metallic hip implant using intensity-modulated radiotherapy (IMRT) and volumetric-modulated arc therapy (VMAT) techniques. Materials and Methods: A cohort of 16 patients having metallic implants was selected for the study. Three sets of IMRT and VMAT plans were generated. Set 1 IMRT (IM_Base), VMAT (VM_Base) without any restrictions on beam entry and exit, set 2 (IM_ENT and VM_ENT) optimizer restricts the beam entry and set 3 (IM_EXT+ENT), neither entry nor exit doses were allowed toward the metallic implant. Results: There was no significant difference in target (D95%) and organ-at-risk doses between IM_Base and IM_ENT. There were significant (P = 0.002) improvements in planning target volume (PTV) V95% and homogeneity from IM_EXT+ENT to IM_ENT. There was no significant difference in plan quality between VM_Base and VM_ENT. There were significant (P = 0.005) improvements in PTV, V95%, homogeneity from VM_EXT+ENT to VM_ENT. V40Gy, V30Gy for bladder, rectum, bowel, and bowel maximum dose decreases significantly (P < 0.005) in IM_ENT compared to IM_EXT+ENT, but not significant for VMAT plans. Similarly, there was a significant decrease in dose spill outside target (P < 0.05) comparing 40%, 50%, 60%, and 70% dose spills for IM_ENT compared to IM_EXT+ENT, but variations among VMAT plans are insignificant. VMAT plans were always superior to IMRT plans for the same optimization methods. Conclusion: The best approach is to plan hip prosthesis cases with blocked entry of radiation beam for IMRT and VMAT. The VMAT plans had more volumetric coverage, fewer hotspots, and lesser heterogeneity.

8.
Rep Pract Oncol Radiother ; 26(5): 688-711, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34760305

RESUMO

BACKGROUND: Routinely, patient's planning scans are acquired after administration of iodinized contrast media but they will be treated in the absence of that. Similarly, high energy photons have a better penetrating power, while low energy photons will result in tighter dose distribution and negligible neutron contamination. The aim of the study was to investigate a suitable photon beam energy in the presence of intravenous contrast medium. MATERIALS AND METHODS: An indigenously made original-contrast (OC) phantom was mentioned as virtual-contrast (VC) and virtual-without-contrast (VWC) phantom were generated by assigning the Hounsfield Units (HU) to different structures. Intensity-modulated (IMRT) and volumetric-modulated-arc (VMAT) plans were generated as per criteria of the TG-119 protocol. RESULTS: It was observed that the maximum dose to the spinal cord was better with 6 mega-voltage (MV) in IMRT. The coverage of Prostate PTV (PR PTV) was similar with all the photon energies and was comparable with TG-119, except for original-contrast (OC) phantom using the VMAT technique. Homogeneity-index (HI) was comparatively better for VMAT plans. CONCLUSION: The contrast CT images lower the dose to targets. IMRT or VMAT plans, generated on such CT images will be delivered with higher doses than evaluated. However, the overdose remains non-significant.

9.
Org Lett ; 23(17): 6709-6713, 2021 Sep 03.
Artigo em Inglês | MEDLINE | ID: mdl-34474577

RESUMO

A diverse reactivity of diazo compounds with nitrosoarene in an oxygen-transfer process and a formal [2 + 2] cycloaddition is reported. Nitosoarene has been exploited as a mild oxygen source to oxidize an in situ generated carbene intermediate under visible-light irradiation. UV-light-mediated in situ generated ketenes react with nitosoarenes to deliver oxazetidine derivatives. These operationally simple processes exemplify a transition-metal-free and catalyst-free protocol to give structurally diverse α-ketoesters or oxazetidines.

10.
Indian J Otolaryngol Head Neck Surg ; 72(4): 474-479, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33088777

RESUMO

Vertigo is the sensation of spinning or having one's surroundings spin about them. It represents about 25% of cases of occurrences of dizziness Yardley et al. (Br J Gen Pract 48(429):1131-1135, 1998). About 40% patients have peripheral vestibular dysfunction (Neuhauser in Curr Opin Neurol 20:40-46, 2007). Quality of life (QOL) is significantly impaired by vertigo (Patatas et al. in Braz J Otorhinolaryngol 75:387-394, 2009). To study the effect and compare vestibular exercises on QOL in patients with vestibular disorders. 120 individuals with vestibular disorders like acoustic neuroma, vestibular neuritis, labyrinthitis, Meniere's disease, vestibulopathy, ISSNHL and ototoxicity were included. Four groups adaptation exercises, habituation exercises, substitution exercises, and combined exercises were formed and 30 individuals were selected in each group randomly. Vestibular activities and participation (VAP) was administered before and after exercises to fulfill the aim. VAP Scale results revealed significant difference between pre and post treatment score in all groups, suggestive of positive effect on QOL in patients with vestibular disorders. Improvements in VAP Score between all groups were compared and significant difference was observed. Combined exercises group found to be best out of 4 exercises group.

11.
Oxid Med Cell Longev ; 2020: 6501294, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32774681

RESUMO

Pseudoalteromonas espejiana (P. espejiana) is a marine bacterium known for its high resistance to alkalinity. The ability of P. espejiana to reduce Au (III) and biosynthesize gold nanoparticles (AuNPs) is found positive and was confirmed using UV-VIS, EDS, SEM, and TEM studies. Previously, many studies have been reported regarding the crystalline nature of AuNPs; therefore, this research aims at studying the crystal growth behaviour of AuNPs through DLS and TEM studies. Spherically shaped and monodispersed, AuNPs ranging between 5 to 160 nm were obtained with an average particle size of 62 nm. Also, to achieve maximum production of AuNPs, the reaction kinetic study was performed using an ICP-OES method and the effect of various parameters including pH, temperature, rpm, and concentration of substrate was analyzed. During the biosynthesis process, an appropriate phase of nucleation, crystal growth, and saturation was observed and this helped to determine the rate constants and order of reaction. The parameters such as pH profile (pH 9), temperature (30°C), agitation speed (150 rpm), and enzyme substrate ratio (2 : 3) were found to be the best fits for maximum production of low size AuNPs. This demonstrates that in initial few hours, a quick conversion of the ionic gold precursor takes place into metallic gold nuclei, trailed by crystal growth via coalescence of small nuclei. Subsequently, it can be concluded that coalescence processes drive the crystal growth process of AuNPs over a time interval and finally leads to saturation and no newer particle formation in the solution.


Assuntos
Ouro/química , Nanopartículas Metálicas/química , Pseudoalteromonas
12.
Plants (Basel) ; 9(7)2020 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-32610670

RESUMO

Acmella oleracea is a promising cosmetic, nutraceutical, and pharmaceutical ingredient, and plants with high levels of active compounds are needed in the market. Cultivation can be valuable if sufficient levels of alkylamides are present in plant material. In this regard the application of biostimulants can be an innovative approach to increase yield of cultivation or bioactive compound levels. A. oleracea plants were cultivated in Northern Italy in an experimental site using three different types of biostimulants, triacontanol-based mixture (Tria), an extract from plant tissues (LL017), and seaweed extract (Swe). Plants were grown in the field in two different growing seasons (2018 and 2019). After treatments inflorescences were harvested and the quali-quantitative analysis of alkylamides and polyphenols was performed. Treated and control plants were compared for yields, morphometric measurements, quali-quantitative composition in secondary metabolites. Overall results show that both triacontanol-based mixture and the LL017 positively influenced plant growth (Tria >+ 22%; LL017 >+ 25%) and flower production (Tria >+ 34%; LL017 >+ 56%). The amount of alkylamides and polyphenols in flowers were between 2.0-5.2% and 0.03-0.50%, respectively. Biostimulant treatments ensure higher cultivation yields and allow maintenance of the alkylamide and polyphenol levels based on % (w/w), thus offering an advantage in the final quantity of extractable chemicals. Furthermore, data revealed that samples harvested in late season show a decrease of polyphenols.

13.
Asian Pac J Cancer Prev ; 21(6): 1731-1738, 2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-32592371

RESUMO

INTRODUCTION: Aim of study is to investigate the effect of hip prosthesis on 6 and 15 MV photon beam energies. MATERIALS AND METHODS: Prosthesis was kept at the level of tray position. The measurements were done on Varian Clinac-iX linac. Customized prosthesis, termed as Prosthetic Metal Implant (PMI) was made up of wrought austenitic stainless steel rod and covered with paraffin-wax. 'Standard prosthesis' was made up of wrought titanium alloy. The dose profiles were measured for three field sizes i.e. 5, 10 and 20 cm at 100 cm SSD for 6 and 15 MV energies. The perturbation index (PI) was also calculated. RESULTS: Perturbation caused by standard prosthesis was approximately 50% higher than that of PMI. This result may be due to difference in dimension and not because of material composition. Variation of central axis dose might be due to the dimensions of PMI used for experiment which gave intermediate response (e.g. 102.1%, 141.0% and 117.7% for Open, Standard and PMI respectively for 10x10 cm2 field size, 10 cm depth and 15MV photon beam setup )as compared to the 'open' and 'standard' prosthesis. Percentage dose at 10 cm for 6MV photon increased rapidly with field-size for PMI. But, for 15MV photon, difference was not significant. Surface dose (Ds) for PMI remains significantly higher for smaller field. CONCLUSION: The perturbation index varied from 0.05 to 0.22 for the measured energies and gave an idea to the planner to assess the behavior of the prosthesis. This range is applicable for both type of implants and for all clinical field-sizes. The attenuation caused by the prosthesis was significant and this effect should be considered in the treatment planning calculations.


Assuntos
Simulação por Computador , Prótese de Quadril , Aceleradores de Partículas/instrumentação , Imagens de Fantasmas , Fótons , Planejamento da Radioterapia Assistida por Computador/métodos , Humanos , Método de Monte Carlo , Dosagem Radioterapêutica , Titânio/química
14.
Rep Pract Oncol Radiother ; 25(4): 507-514, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32494224

RESUMO

AIM: To investigate the impact of Acuros XB (AXB) algorithm in the deep-inspiration breath-hold (DIBH) technique used for treatment of left sided breast cancer. BACKGROUND: AXB may estimate better lung toxicities and treatment outcome in DIBH. MATERIALS AND METHODS: Treatment plans were computed using the field-in-field technique for a 6 MV beam in two respiratory phases - free breathing (FB) and DIBH. The AXB-calculations were performed under identical beam setup and the same numbers of monitor units as used for AAA-calculation. RESULTS: Mean Hounsfield units (HU), mass density (g/cc) and relative electron density were -782.1 ±â€¯24.8 and -883.5 ±â€¯24.9; 0.196 ±â€¯0.025 and 0.083 ±â€¯0.032; 0.218 ±â€¯0.025 and 0.117 ±â€¯0.025 for the lung in the FB and DIBH respiratory phase, respectively. For a similar target coverage (p > 0.05) in the DIBH respiratory phase between the AXB and AAA algorithm, there was a slight increase in organ at risk (OAR) dose for AXB in comparison to AAA, except for mean dose to the ipsilateral lung. AAA predicts higher mean dose to the ipsilateral lung and lesser V20Gy for the ipsilateral and common lung in comparison to AXB. The differences in mean dose to the ipsilateral lung were 0.87 ±â€¯2.66 % (p > 0.05) in FB, and 1.01 ± 1.07% (p < 0.05) in DIBH, in V20Gy the differences were 1.76 ±â€¯0.83% and 1.71 ±â€¯0.82% in FB (p < 0.05), 3.34 ± 1.15 % and 3.24 ± 1.17 % in DIBH (p < 0.05), for the ipsilateral and common lung, respectively. CONCLUSION: For a similar target volume coverage, there were important differences between the AXB and AAA algorithm for low-density inhomogeneity medium present in the DIBH respiratory phase for left sided breast cancer patients. DIBH treatment in conjunction with AXB may result in better estimation of lung toxicities and treatment outcome.

15.
3 Biotech ; 9(11): 399, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31656737

RESUMO

The goal of this research was to explore the preliminary anticancer properties of five plants namely Calotropis procera, Moringa oleifera, Millettia pinnata, Basela alba and Euphorbia neriifolia available in Jharkhand which is used for the medicinal purpose by local tribes. In the present study, plant leaves from five species were collected, dried and extracted with solvents of increasing polarity, followed by assessment of their cytotoxicity in A549 non-small-cell lung cancer cells. In the antimicrobial assay, the methanol extract of the M. pinnata leaves exhibited comparatively higher zone of inhibition of 0.7 ± 0.20 cm against a Salmonella typhi culture than the other extracts. M. pinnata leaves extract also displayed the maximum percentage inhibition in the DPPH, 83.97 ± 0.01 FRAP, 193.14 ± 3.01 mM assays. Furthermore, the cytotoxicity of the chloroform (37.45 ± 1.04) and ethyl acetate extracts (34.20 ± 0.81) of M. pinnata against A549 cells was found relatively higher with respect to another extract. In contrast, a study with the L132 normal epithelial lung cell line revealed less toxicity from the chloroform extract (0.33 ± 0.19) compared to the ethyl acetate extract (6.65 ± 0.59). Based on these findings, phytochemical investigation on chloroform and ethyl acetate extract of M. pinnata was performed using UPLC-ESI-MS/MS analysis revealing the presence of ß-sitosterol, lanceolatin B, karanjin, and stigmasterol. Congruently, a complete phytochemical and cytotoxic investigation of the M. pinnata extract constituents might infer the potency of this extract/s as anticancer, antioxidant and antimicrobial agents.

16.
IET Nanobiotechnol ; 13(6): 626-633, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31432797

RESUMO

Green synthesis of gold nanoparticles (GNPs) has received substantial attention, because nanoparticles are produced in an eco-friendly way using biomolecules present in plant extracts in a single step reaction. This research article highlights GNPs obtained using shade-dried leaf extracts of Millettia pinnata (L.) with aqueous auric chloride (HAuCl4) at ambient temperature. In the present study, GNPs with average particle size 37 nm in size were fabricated. Furthermore, the synthesis method to obtain stable and monodispersed GNPs was advanced by optimising enzyme concentration 100 µg/ml, pH 5.4, substrate concentration 0.45 mM and 12 h time of reaction. The confirmation of GNPs formation and characterisation was followed by UV-vis-absorption spectroscopy, dynamic light scattering (DLS), and zeta potential (ZP) for the analysis of shape, size, and stability, respectively. TEM images and powder XRD revealed the GNPs synthesis of spherical-shaped nanoparticles in the face-centred cubic arrangement. Cytotoxicity of GNPs was studied against A549 lung cancer cells with IC50 14.76 µg/ml and found lower as compared to doxorubicin IC50 11.23 µg/ml but significant enough to be used as a vehicle GNPs produced using green source can be used as significant therapeutic agents and drug delivery carriers.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Carcinoma Pulmonar de Células não Pequenas/patologia , Ouro/química , Neoplasias Pulmonares/patologia , Nanopartículas Metálicas/química , Millettia/química , Células A549 , Antineoplásicos/química , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Ensaios de Seleção de Medicamentos Antitumorais , Química Verde/métodos , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Nanopartículas Metálicas/uso terapêutico , Extratos Vegetais/química , Folhas de Planta/química
17.
Indian J Otolaryngol Head Neck Surg ; 71(1): 99-103, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30906723

RESUMO

Benign Paroxysmal Positional Vertigo (BPPV) is the most common cause in patients with vertigo (Pereira et al. in Braz J Otorhinolaryngol (Impr) 76(6):704-708, 2010; Dix and Hallpike in Ann Otol Rhinol Laryngol 6:987-1016, 1952). Posterior Semicircular Canal BPPV (PSCBPPV) has more incidence and prevalence then Lateral, and Anterior Semicircular Canal BPPV (Alghwiri et al. in Arch Phys Med Rehabil 93:1822-1831, 2012). Quality of life (QoL) is significantly impaired by vertigo (Sargent et al. in Otol Neurotol 22:205-209, 2001; World Health Organization in International classification of functioning, disability and health, World Health Organization, Geneva, 2001). To study the effect and compare Epley, Semont maneuvers and Brandt-Daroff Exercise on QoL in patients with PSCBPPV. 90 individuals with unilateral PSCBPPV were selected based on positive Dix-Hallpike test. 3 groups Epley, Semont, and Brandt-Daroff were formed and 30 individuals were selected in each group randomly. Dix-Hallpike test and Vestibular Activities and Participation (VAP) Scale based on International Classification of Functioning were administered before and after Epley, Semont maneuvers, and Brandt-Daroff Exercise to fulfill the aim. VAP Scale results revealed significant difference between pre and post treatment score in all 3 groups, suggestive of positive effect on QoL in patients with PSCBPPV. Improvements in VAP Score between 3 groups were compared and significant difference was observed. Dix-Hallpike test results revealed that 90, 73.33, and 50% patients improved in Epely, Semont, and Brandt-Daroff group respectively. Epely maneuver found to be the best choice and then Semont and Brandt-Daroff should be least preferred in treatment of patients with PSCBPPV.

18.
J Gastrointest Cancer ; 50(3): 408-419, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29520733

RESUMO

PURPOSE: To evaluate the feasibility of flattening filter free beam (FFFB) for the treatment of gastric tumors and to review their benefits over 6MV flatten beam (6MV_FFB). METHODS: Fifteen patients with histologically proven gastric carcinoma were selected. CT scans with slice thickness of 0.3 cm were acquired and planning target volume (PTV) and organ at risk (OAR) were delineated. Plans were made retrospectively for each patient for the prescription dose of 45 Gy/25 fractions to the PTV. Four isocentric plans were compared in the present study on Varian TrueBeam linear accelerator (Varian Medical Systems, Palo Alto, CA, USA). RESULTS: PTV D98% was 44.41 ± 0.12, 44.38 ± 0.13, 44.59 ± 0.14, and 44.49 ± 0.19 Gy for IMRT 6MV_FFB, IMRT 6MV_FFFB, VMAT 6MV_FFB, and VMAT 6MV_FFFB respectively. 6MV_FFFB beam minimizes the mean heart dose Dmean (P = 0.001). VMAT dominates over IMRT when it came to kidney doses V12Gy (P = 0.02), V23Gy (P = 0.015), V28Gy (P = 0.011), and Dmax (P < 0.01). VMAT has significantly reduced the doses to kidneys. It was analyzed that 6MV_FFFB significantly reduces the dose to normal tissues (P = 0.006 and P = 0.018). VMAT significantly reduces the TMU, which is required to deliver the similar dose by IMRT (P < 0.01). CONCLUSIONS: Unflattened beam spares the organs at risk significantly to avoid the chances of secondary malignancies and reduces the intra-fraction motion during treatment due to provision of higher dose rate. Hence, we conclude that 6MV unflattened beam can be used to treat gastric carcinoma.


Assuntos
Órgãos em Risco/efeitos da radiação , Garantia da Qualidade dos Cuidados de Saúde/normas , Planejamento da Radioterapia Assistida por Computador/métodos , Radioterapia de Intensidade Modulada/instrumentação , Radioterapia de Intensidade Modulada/métodos , Neoplasias Gástricas/radioterapia , Tomografia Computadorizada por Raios X/métodos , Adolescente , Adulto , Idoso , Estudos Transversais , Estudos de Viabilidade , Feminino , Humanos , Processamento de Imagem Assistida por Computador/métodos , Masculino , Pessoa de Meia-Idade , Prognóstico , Dosagem Radioterapêutica , Radioterapia de Intensidade Modulada/classificação , Estudos Retrospectivos , Adulto Jovem
19.
J Genet Eng Biotechnol ; 16(2): 527-536, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30733770

RESUMO

Biogenic synthesis of silver nanoparticles using microorganisms has found interest recently since last decade because of their prospect to synthesize nanoparticles of various size, shape and morphology which are eco-friendly. Here, an eco-friendly method for production of silver nanoparticles from Bacillus clausii cultured from Enterogermina is explored. Along with the biosynthesis and conformity test, in silico studies was done on NADPH dependent nitrate reductase enzymes from the view point of designing a rational enzymatic strategy for the synthesis. The detailed characterization of the nanoparticles was carried out using UV-Vis spectroscopy, Dynamic Light Scattering (DLS) particle size analysis, Transmission Electron Microscopy (TEM), X-Ray Diffraction (XRD) analysis. Computational profiling and in silico characterization of NADH dependent enzymes was carried out based on literature and work done so far. Nitrate reductase sequence was retrieved from NCBI for characterization. Secondary structure was evaluated and verified by JPred as well as SOPMA Tool. Tertiary structure was also modeled by MODELLER and ITASSER parallel and the best structure was selected based on energy values. Structure validation was done by GROMACS and RMSD, RMSF, temperature variation plot were also plotted. Interactions graphs between nitrate reductase and ligand silver nitrate was done through molecular docking using Hex.

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