Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 97
Filtrar
1.
Environ Monit Assess ; 190(3): 148, 2018 Feb 17.
Artigo em Inglês | MEDLINE | ID: mdl-29455262

RESUMO

The present study attempts to understand the seasonal and spatial variations in the physico-chemical (temperature, pH, salinity, dissolved oxygen, and nutrients) and productivity characteristics of the northern Arabian Sea off the Indian coast. Samples were collected from four different sites off the Veraval coast. The values of the physical and chemical variables were higher during the summer season, whereas nutrient concentrations were high during the winter season due to the maturity of intake nutrients during post-monsoon and winter convective mixing during the northeast monsoon. The dissolved oxygen (DO) concentration was strongly and positively correlated with the net primary productivity (NPP) and chlorophyll a (Chl-a) content to support productivity along the region. Dissimilarity in study variables was observed between the inshore and offshore locations. Principal component analysis revealed a strong relationship between nutrients and productivity variables (Chl-a and NPP). Nutrient levels were high at inshore sites, which can be attributed to the heavy nutrient load from land-based anthropogenic activities and impact due to natural processes like water mixing, sedimentation, and wave activities. Nutrients were strongly and positively correlated with the productivity variables, i.e., Chl-a and NPP. Chl-a positively correlated with NPP (r = 0.90), which indicates that it is a principle productivity pigment in the marine ecosystem.


Assuntos
Clorofila/análise , Monitoramento Ambiental/métodos , Água do Mar/química , Clorofila A , Ecossistema , Índia , Oceanos e Mares , Oxigênio/análise , Fitoplâncton , Salinidade , Estações do Ano , Temperatura , Movimentos da Água
2.
J Contemp Dent Pract ; 19(3): 262-268, 2018 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-29603695

RESUMO

AIM: Silver colloidal nanoparticles have been incorporated into acrylic resins to induce antimicrobial properties. However, as additives, they can influence the mechanical properties of the final product. Mechanical properties are also dependent on different curing cycles. The aim of this study was to evaluate flexural strength of a denture base resin incorporated with different concentrations of silver colloidal nanoparticles subjected to two different curing cycles. MATERIALS AND METHODS: Lucitone 199 denture base resin was used into which silver colloidal nanoparticles were incorporated at 0.5 and 5% by polymer mass. Specimens devoid of nanoparticles were used as controls. A total of 60 specimens were fabricated and divided into two groups. Each group was divided into three subgroups consisting of 10 specimens each. The specimens were fabricated according to American Dental Association (ADA) specification No. 12 and tested for flexural strength using universal testing machine. RESULTS: Silver colloidal nanoparticle incorporation at 0.5% concentration increased the mean flexural strength in both curing cycles by 7.5 and 4.4%, respectively, when compared with the control group. CONCLUSION: The study suggested that the mean flexural strength value of 0.5% silver colloidal nanoparticles in denture base resin was above the value of the control group both in short and long curing cycles, which makes it clinically suitable as a denture base material. However, at 5% concentration, the statistically significant amount of decrease in flexural strength compared with the value of control group both in short and long curing cycles gives it a questionable prognosis. CLINICAL SIGNIFICANCE: The specimens incorporated with the antimicrobial agent 0.5% silver colloidal nanoparticles and processed by long curing cycles showed significant increase in its flexural strength compared with the control group, which makes it clinically suitable as a denture base material.


Assuntos
Bases de Dentadura , Nanopartículas Metálicas/química , Polimetil Metacrilato/química , Prata/química , Técnicas In Vitro , Resistência à Tração
3.
Indian J Plast Surg ; 50(3): 273-280, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29618862

RESUMO

BACKGROUND: Wounds have since long, contributed majorly to the health-care burden. Infected long-standing non-healing wounds place many demands on the treating surgeon and are devastating for the patients physically, nutritionally, vocationally, financially, psychologically and socially. Acetic acid has long been included among agents used in the treatment of infected wounds. In this study, we have evaluated the use of acetic acid for topical application in the treatment of infected wounds. MATERIALS AND METHODS: A total of 100 patients with infected wounds were treated with topical application of 1% acetic acid as dressing material after appropriate cleaning. A specimen of wound swab was collected before first application and further on days 3, 7, 10 and 14. Daily dressings of wounds were done similarly. Minimum inhibitory concentration (MIC) of acetic acid against various organisms isolated was determined. RESULTS: The patients treated ranged between 9 and 60 years, with the mean age 33 years. Nearly 70% of patients were male. Aetiologies of wounds: infective 35, diabetic 25, trauma 20, burns 10, venous ulcers 5 and infected graft donor site 5. Various microorganisms isolated include Pseudomonas aeruginosa (40%), Staphylococcus aureus (2%), Acinetobacter (12%), Escherichia Coli (5%), Proteus mirabilis (3%), Klebsiella (18%), methicillin-resistant S. aureus (10%), Streptococcus (2%) and Enterococcus (1%), Citrobacter (1%). Few wounds (6%) also isolated fungi. About 28%, 64% and 8% of patients isolated no growth on culture after 7, 14 and 21 days, respectively. MIC of all isolated organisms was ≤0.5%. CONCLUSION: pH of the wound environment plays a pivotal role in wound healing. Acetic acid with concentration of 1% has shown to be efficacious against wide range of bacteria as well as fungi, simultaneously accelerating wound healing. Acetic acid is non-toxic, inexpensive, easily available and efficient topical agent for effective elimination of wound infections caused due to multi-drug resistant, large variety of bacteria and fungus.

4.
Physiol Mol Biol Plants ; 21(3): 425-32, 2015 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-26261407

RESUMO

Boerhaavia diffusa L is a medicinal herb with immense pharmaceutical significance. The plant is used by many herbalist, Ayurvedic and pharmaceutical industries for production biopharmaceuticals. It is among the 46 medicinal plant species in high trade sourced mainly from wastelands and generally found in temperate regions of the world. However, the commercial bulk of this plant shows genetic variations which are the main constraint to use this plant as medicinal ingredient and to obtain high value products of pharmaceutical interest from this plant. In this study, we have regenerated the plant of Boerhaavia diffusa L through nodal explants and evaluated genetic fidelity of the micropropagated plants of Boerhaavia diffusa L with the help of random amplified polymorphic DNA (RAPD) markers. The results obtained using RAPD showed monomorphic banding pattern revealing genetic stability among the mother plant and in vitro regenerated plants of Boerhaavia diffusa L.

5.
Indian J Plast Surg ; 48(2): 123-8, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26424973

RESUMO

BACKGROUND: Indian noses are broader and lack projection as compared to other populations, hence very often need augmentation, that too by large volume. Costal cartilage remains the material of choice in large volume augmentations and repair of complex primary and secondary nasal deformities. One major disadvantage of costal cartilage grafts (CCG) which offsets all other advantages is the tendency to warp and become distorted over a period of time. We propose a simple technique to overcome this menace of warping. MATERIALS AND METHODS: We present the data of 51 patients of rhinoplasty done using CCG with counterbalancing technique over a period of 4 years. RESULTS: No evidence of warping was found in any patient up to a maximum follow-up period of 4 years. CONCLUSION: Counterbalancing is a useful technique to overcome the problem of warping. It gives liberty to utilize even unbalanced cartilage safely to provide desired shape and use the cartilage without any wastage.

6.
Indian J Plast Surg ; 48(2): 172-7, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26424982

RESUMO

UNLABELLED: Augmentation rhinoplasty can be carried out using a wide range of materials including autologous bone and/or cartilage as well as alloplasts. Use of biologic bone and cartilage grafts results in lower infection rates, but they are associated with long-term resorption and donor-site morbidity. Alloplastic materials, in particular silicone, have been associated in literature with extrusion, necrosis of the tip, mobility and deviation or displacement of the implant, immobile nasal tip and infection. However, they have the advantages of being readily available and easy to reshape with no requirement for harvesting autografts. AIM: To overcome these problems associated with silicone implants for which the authors have devised a novel technique, the "rideon technique". MATERIALS AND METHODS: The present study was carried out on 11 patients over a period of 4 years. The authors have devised a simple technique to fix the silicone implant and retain it in place. Restricting the implant to only dorsum avoided common complications related to the silicone implant. RESULTS: The authors have used this technique in 11 patients with encouraging results. Follow-up ranged from 12 months to 36 months during which patients were assessed for implant mobility, implant extrusion and tip necrosis. There was no incidence of above mentioned complications in these patients. CONCLUSION: The "rideon technique" provides excellent stability to silicone implants and restricting the implant only to dorsum not only eliminates chances of tip necrosis and thus implant extrusion but also maintains natural shape, feel and mobility of the tip.

7.
PLoS One ; 19(9): e0310648, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39302919

RESUMO

Ruminant livestock are major contributors to anthropogenic methane emissions in the United States and worldwide. Enteric methane is generated by methanogenic archaea residing in ruminant digestive tracts. Information on when methanogens colonize the gut and when they begin to interact with bacteria during the early phases of the ruminant life cycle is less explored. The objectives of this study were (i) to investigate the composition of the methanogenic archaeal community at birth and through the weaning transition and (ii) to determine if and when the methanogenic archaea begin to interact with bacteria in the lower gut of neonatal dairy calves. Ten female Holstein calves (approximately 45kg birth weight) were enrolled in the study. Fecal samples were collected every two weeks (Wk 2, 4, 6, 8, 10, and 12) between birth and weaning and analyzed for methanogenic archaeal diversity via 16S rRNA amplicon sequencing and quantitative real-time PCR (RT-qPCR). Estimates of alpha diversity (Observed species, and Shannon diversity index) and beta diversity (weighted and unweighted UniFrac distances) showed significant differences (P < 0.05) between archaeal communities across timepoints. Both 16S rRNA amplicon sequencing and RT-qPCR analyses revealed Methanobrevibacter was the most prevalent genus at Wk2, Wk4, and Wk6, whereas Methanosphaera gradually increased with time and was most abundant at Wk10 and Wk12. Correlation analysis revealed that Methanobrevibacter and Methanosphaera were inversely correlated with each other and formed distinct cohorts with specific bacterial lineages similar to those reported in the mature rumen, thus revealing that these associations are established during the preweaning period. Therefore, the preweaning period presents a window of opportunity to interfere with early-life methanogenic colonization with the ultimate goal of reducing enteric methane emissions without perturbing ruminal function later in the life of dairy cattle.


Assuntos
Metano , RNA Ribossômico 16S , Desmame , Animais , Bovinos/microbiologia , Feminino , Metano/metabolismo , RNA Ribossômico 16S/genética , Bactérias/classificação , Bactérias/genética , Bactérias/isolamento & purificação , Microbioma Gastrointestinal , Fezes/microbiologia , Archaea/genética , Archaea/classificação , Animais Recém-Nascidos/microbiologia
8.
Cureus ; 16(6): e62943, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-39044890

RESUMO

BACKGROUND: Mental health issues are a major cause of poor life outcomes. Heartfulness (HFN) meditation is recommended for stress management and daily awareness. Although studies have shown that HFN can improve burnout and well-being, the biological mechanism underlying oxidative stress markers in a healthy human is unclear. OBJECTIVE: The purpose of this study was to determine whether HFN meditation benefits mindfulness responses and also to examine the impact of HFN meditation on oxidative stress in healthy individuals. METHODS: This prospective study involved 60 healthy individuals aged 18-24, divided into experimental and control groups, and implemented an HFN meditation intervention over 12 weeks. Both groups' serum malondialdehyde and serum nitrate levels were examined before and after the intervention. Additionally, psychometric evaluations concerning mindfulness and experiential avoidance were conducted utilizing scales such as the Mindful Attention Awareness Scale (MAAS), Five-Facet Mindfulness Questionnaire (FFMQ), Self-Compassion Scale (SCS), and Experiential Avoidance (EA). RESULTS: Following a three-month intervention period, serum malondialdehyde (MDA) levels in the experimental group did not show a significant increase, whereas in the control group, there was a significant increase (p < 0.000). Conversely, serum nitrate levels in the experimental group exhibited a significant increase (p < 0.05). Additionally, psychological stress decreased, as indicated by various questionnaire tools such as MAAS, FFMQ, SCS, and EA, with mindfulness showing an increase. However, a decrease in EA was seen. CONCLUSION: Heartfulness meditation has a positive impact on both mindfulness and oxidative stress. This suggests that consistent, long-term participation in HFN meditation could enhance mental health and foster overall well-being.

9.
Heliyon ; 10(10): e31217, 2024 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-38813177

RESUMO

We developed a novel chromogenic reagent and sensor by selective approach, for the detection and identification of dichlorvos, which we tested with the thin layer chromatography method. For the first time, we reported in situ-generated glyoxal as a hydrolysis product, which then interacts with isoniazid to produce a yellow-colored cyclic compound. We used well-known spectroscopic techniques to confirm the chemical identity of the final product. We initially investigated the reaction using a variety of approaches, followed by attempts to establish the reaction mechanism using Density Functional Theory by Gaussian software.

10.
Anat Sci Educ ; 16(3): 384-390, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36683409

RESUMO

Historically, adverse events have reflected poorly on both the practice of dissection and the perception of the discipline of anatomy. The recent public dissection of a body donor is a regression to an unethical historical practice and was strongly denounced by anatomists around the world. The individual whose donated body was sourced from a 'for-profit" company in the United States had not given consent for a public dissection. This violates the ethics surrounding consent and body donation and potentially places the future of body donor programs in jeopardy as it compromises community frameworks around epistemic trust. Recent guiding frameworks by international anatomical associations on the ethical use of bodies have cemented the way in which body donor programs should operate. This viewpoint reflects on past and current events pertaining to public dissections and questions how these indignities may influence the public's interaction with human bodies. The authors argue that public dissection should be prohibited as it is against social mores. Social pressure should be applied to individuals or companies who wish to profit from unethical anatomical practice and legislation prohibiting public dissection should be introduced in those countries where it does not yet exist.


Assuntos
Anatomistas , Anatomia , Humanos , Anatomia/educação , Cadáver , Dissecação , Doadores de Tecidos
11.
Chempluschem ; 86(8): 1167-1176, 2021 08.
Artigo em Inglês | MEDLINE | ID: mdl-34409757

RESUMO

A solvent-assisted grinding method has been used to prepare co-crystals in substituted dihydropyrimidines (DHPM) that constitutes pharmacologically active compounds. These were characterized using FT-IR, PXRD, and single-crystal X-ray diffraction. In order to explore the possibility of formation of halogen (XB) and hydrogen bonding (HB) synthons in the solid state, co-crystallization attempts of differently substituted DHPM molecules, containing nitro, hydoxy, and chloro substituents, with different co-formers, such as 1,4-diiodo tetrafluorobenzene (1,4 DITFB) and 3-nitrobenzoic acid (3 NBA) were performed. The XB co-crystals (C2aXB, C2bXB, and C2cXB) prefer the formation of C-I⋅⋅⋅O/C-I⋅⋅⋅S XB synthon, whereas the HB co-crystal (C2dHB) is stabilized by N-H⋅⋅⋅O H-bond formation. Hirshfeld surface analysis revealed that the percentage contribution of intermolecular interactions for XB co-crystals prefer equal contribution of XB synthon along with HB synthon. Furthermore, the interaction energy was analyzed using energy frameworks, which suggests that their stability, a combination of electrostatics and dispersion, is enhanced through XB/HB in comparison to the parent DHPMs.


Assuntos
Halogênios , Cristalização , Cristalografia por Raios X , Ligação de Hidrogênio , Espectroscopia de Infravermelho com Transformada de Fourier
13.
Trans Indian Natl Acad Eng ; 5(2): 373-378, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-38624411

RESUMO

Influenza like pandemics are a severe threat to any established health care system as many thousands of patients would need emergency ventilator support during the acute respiratory failure stage, and this quickly overloads the existing facilities. The present article addresses the design and development of a human breathing assist machine (ventilator) prototype for use by qualified medical professionals in the emergency room, as well as in other locations, where a regular ventilator machine cannot be made available. The ventilator has been designed using readily available locally sourced materials, which can be assembled in a short time. This ensures the minimum required features to ventilate a patient in emergency conditions. The popular crank-rocker mechanism has been used to meet some of the vital design requirements of the emergency ventilator. The size of the links has been chosen to maintain a fixed inspiratory-to-expiratory (I:E) time ratio of 1:2. The kinematic linkage design has been kept modular by introducing a feature to adjust the location of the rocker tip to control the tidal volume from 100 ml to 600 ml of oxygenated air per breath. A virtual CAD model, based on the above-mentioned linkage design, has been designed to assess the variation of the position and velocity with time. Finally, a working prototype has been made, and it was observed that the I:E time ratio of 1:2 was achieved satisfactorily.

14.
J Orthop ; 19: 128-131, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32025119

RESUMO

The bicipital groove (BG) forms an indentation between the greater and lesser humeral tubercles and lodges the long head of biceps brachii tendon (LHBBT) along with the ascending branch of the circumflex humeral artery. This study aimed to determine the dimensions (length, width, depth) of the BG in a select South African population. The dimensions of the BG in one hundred and sixty (n = 160; Right: 80; Left: 80, Male: 100; Female: 60) unpaired dry bone humerii were measured with a digital caliper (Linear Tools 2012, 0-150 mm, LIN 86500963) and was analyzed using SPSS (V25). Results: Bicipital groove dimensions: (a) Length (mm): Right 66.64 ± 9.06, Left 68.31 ± 11.52; Male 67.44 ± 9.12, Female 67.53 ± 12.25; (b) Width (mm): Right 8.98 ± 1.49, Left 9.27 ± 1.30; Male 9.18 ± 1.45, Female 9.05 ± 1.31; (c) Depth (mm): Right 7.73 ± 1.31, Left 7.20 ± 1.18; Male 7.43 ± 1.29, Female 7.53 ± 1.24. The mean BG length observed in this study disagreed with previous studies where smaller lengths were reported. In addition, the comparison of the mean BG depth in this study also revealed a statistically significant difference which may suggest that increased depth in the BG is a common finding in right side of BG specimens. This finding was unique as BG depth is associated with biceps tendon pathology and augments South African shoulder-related literature. Since biceps tendon pathology is associated with decreased biceps activity and pain, investigation of the BG may provide useful data to evaluate individuals with potential abnormality of the bicep tendon. It may also be used as a landmark for humeral head replacement in the treatment of proximal humerus fractures.

15.
Anat Sci Educ ; 13(6): 721-731, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32077216

RESUMO

Cultural practices in the African continent have been thought to impact negatively on body donation. Thus, most African countries continue to rely on unclaimed bodies for dissection programs, or bequests from the white population. The latter situation is dominant in South African medical schools. Since South Africa is multi-cultural with nine main ethnic groups of the Black African population, it is important to seek the reasons behind lack of participation in body donation. This report represents a move in this direction with its qualitative study of the cultural practices of the Zulu ethnic group in the province of KwaZulu-Natal from the perspective of a variety of participants, with emphasis on their treatment of the human body after death. Four themes emerged from interviews: (1) Death is not the end; (2) Effect of belief in ancestors; (3) Significance of rituals and customs carried out on human tissue; and (4) Burial as the only method of body disposal. Each of these themes is discussed in relation to the likelihood of body donation being seen by Zulus as an acceptable practice. It is concluded that this is unlikely, on account of the need to preserve the linkage between the physical human body and the spirit of the deceased person, and the perceived ongoing relationship between the spirit of the dead and the living. In view of these conclusions, a number of options are canvassed about the manner in which anatomists in KwaZulu-Natal might obtain bodies for dissection. These possibilities have implications for anatomists working in comparable cultural contexts.


Assuntos
População Negra/etnologia , Sepultamento , Etnicidade , Doadores de Tecidos/psicologia , Obtenção de Tecidos e Órgãos , Adulto , Anatomistas , Anatomia/educação , Atitude Frente a Morte/etnologia , Cadáver , Dissecação , Feminino , Grupos Focais , Humanos , Masculino , Pessoa de Meia-Idade , Pesquisa Qualitativa , Faculdades de Medicina/provisão & distribuição , África do Sul
16.
J Crit Care Med (Targu Mures) ; 6(4): 217-223, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33200092

RESUMO

The novel coronavirus disease, 2019 (COVID - 19) evolved as an unprecedented pandemic. The severe acute respiratory syndrome-corona virus-2 (SARS-CoV-2) infection has been associated with significantly deranged coagulation parameters and increased incidence of thrombotic events. Deranged coagulation parameters, such as D-dimers and fibrin degradation products, can indicate a poor prognosis, and their measurement will help stratify the patients according to the disease severity, need of intensive care unit admission, and prediction of the clinical course. Gaps in understanding the natural history of the disease cause difficulties in tailoring therapies and optimizing the management of patients. Lack of specific treatment further complicates this situation. While thrombotic events can cause significant morbidity and mortality in patients, a focused approach to the prevention and treatment of venous thromboembolism (VTE) can, to a great extent, decrease the disease burden caused by thrombotic diseases. Pharmacological prophylactic anticoagulants and mechanical therapies such as pneumatic compression devices can help prevent venous thromboembolism and other thrombotic events. Thrombotic events due to COVID-19, their prevention and management, are the focus of this paper, with the prospect of providing insights into this relatively unexplored area.

17.
Cytokine X ; 2(4): 100035, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32895645

RESUMO

The SARS-CoV-2 virus responsible for the COVID-19 pandemic can result in severe or fatal disease in a subset of infected patients. While the pathogenesis of severe COVID-19 disease has yet to be fully elucidated, an overexuberant and harmful immune response to the SARS-CoV-2 virus may be a pivotal aspect of critical illness in this patient population. The inflammatory cytokine, IL-6, has been found to be consistently elevated in severely ill COVID-19 patients, prompting speculation that IL-6 is an important driver of the pathologic process. The inappropriately elevated levels of inflammatory cytokines in COVID-19 patients is similar to cytokine release syndrome (CRS) observed in cell therapy patients. We sought to describe outcomes in a series of severely ill patients with COVID-19 CRS following treatment with anti-IL-6/IL-6-Receptor (anti-IL-6/IL-6-R) therapy, including tocilizumab or siltuximab. At our academic community medical center, we formed a multi-disciplinary committee for selecting severely ill COVID-19 patients for therapy with anti-IL-6 or IL-6-R agents. Key selection criteria included evidence of hyperinflammation, most notably elevated levels of C-reactive protein (CRP) and ferritin, and an increasing oxygen requirement. By the data cutoff point, we treated 31 patients with anti-IL-6/IL-6-R agents including 12 who had already been intubated. Overall, 27 (87%) patients are alive and 24 (77%) have been discharged from the hospital. Clinical responses to anti-IL-6/IL-6-R therapy were accompanied by significant decreases in temperature, oxygen requirement, CRP, IL-6, and IL-10 levels. Based on these data, we believe anti-IL-6/IL-6-R therapy can be effective in managing early CRS related to COVID-19 disease. Further study of anti-IL-6/IL-6-R therapy alone and in combination with other classes of therapeutics is warranted and trials are underway.

18.
SAR QSAR Environ Res ; 30(12): 919-933, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31702401

RESUMO

Folates are essential biomolecules required to carry out many crucial processes in leishmania parasite. Dihydrofolate reductase-thymidylate synthase (DHFR-TS) and pteridine reductase 1 (PTR1) involved in folate biosynthesis in leishmania have been established as suitable targets for development of chemotherapy against leishmaniasis. In the present study, various computational tools such as homology modelling, pharmacophore modelling, docking, molecular dynamics and molecular mechanics have been employed to design dual DHFR-TS and PTR1 inhibitors. Two designed molecules, i.e. 2-(4-((4-nitrobenzyl)oxy)phenyl)-1H-benzo[d]imidazole and 2-(4-((2,4-dichlorobenzyl)oxy)phenyl)-1H-benzo[d]oxazolemolecules were synthesized. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay was performed to evaluate in vitro activity of molecules against promastigote form of Leishmania donovani using Miltefosine as standard. 2-(4-((4-nitrobenzyl)oxy)phenyl)-1H-benzo[d]imidazole and 2-(4-((2,4-dichlorobenzyl)oxy)phenyl)-1H-benzo[d]oxazolemolecules were found to be moderately active with showed IC50 = 68 ± 2.8 µM and 57 ± 4.2 µM, respectively.


Assuntos
Antiprotozoários/farmacologia , Leishmania donovani/efeitos dos fármacos , Complexos Multienzimáticos/química , Oxirredutases/química , Proteínas de Protozoários/química , Tetra-Hidrofolato Desidrogenase/química , Timidilato Sintase/química , Antiprotozoários/síntese química , Antiprotozoários/química , Benzimidazóis/síntese química , Benzimidazóis/química , Benzimidazóis/farmacologia , Benzoxazóis/síntese química , Benzoxazóis/química , Benzoxazóis/farmacologia , Descoberta de Drogas , Concentração Inibidora 50 , Leishmania donovani/metabolismo , Modelos Moleculares , Fosforilcolina/análogos & derivados , Fosforilcolina/farmacologia , Relação Estrutura-Atividade
19.
Int J Pharm ; 560: 205-218, 2019 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-30742985

RESUMO

There is an increasing demand for new lipidic biocompatible and safe materials for self-microemulsifying drug delivery system (SMEDDS). The present work reports the synthesis, characterization, oral mucosal irritation study, and application of novel erucic acid ester of G0-PETIM dendron based bicephalous heterolipid (BHL) as an oil phase in SMEDDS using Efavirenz (EFA), a BCS class II drug with poor water solubility and poor bioavailability. Studies were conducted to optimize EFA SMEDDS using different ratios of the BHL as oil phase and surfactant: co-surfactant weight ratios (Km). At Km (1.5), the microemulsion was spontaneously formed in water with mean globule size of 22.78 ±â€¯0.25 nm and polydispersity index (PDI) of 0.23 ±â€¯0.031 with high drug loading efficiency of 80.35 ±â€¯3.1%. Standard stability tests were performed on EFA SMEDDS and the results indicated it to be highly stable. The in vitro dissolution profile of EFA SMEDDS showed >95% of the drug release within an hour and expectedly substantial enhancement in in vivo bioavailability was observed; almost 6-fold increase in bioavailability with parameters Cmax 5.2 µg/mL, Tmax 3 h, and AUC(0-∞) 23.48 µg/h/mL respectively as compared the plain suspension of the drug. In conclusion, the BHL can be used effectively as an oil phase in SMEDDS to enhance solubility and bioavailability of BCS Class II drugs. Further, it holds, in general, a great promise as a new excipient for solubility and bioavailability enhancements.


Assuntos
Benzoxazinas/administração & dosagem , Sistemas de Liberação de Medicamentos , Excipientes/química , Lipídeos/química , Alcinos , Animais , Área Sob a Curva , Benzoxazinas/química , Benzoxazinas/farmacocinética , Disponibilidade Biológica , Química Farmacêutica/métodos , Ciclopropanos , Dendrímeros/química , Liberação Controlada de Fármacos , Emulsões , Ácidos Erúcicos/química , Masculino , Tamanho da Partícula , Ratos , Ratos Wistar , Inibidores da Transcriptase Reversa/administração & dosagem , Inibidores da Transcriptase Reversa/química , Inibidores da Transcriptase Reversa/farmacocinética , Solubilidade , Tensoativos/química
20.
Inorg Chem ; 47(23): 11191-6, 2008 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-19228026

RESUMO

Treating the bis(imido) W(NAr)(2)Cl(2)(DME) with 2 equiv of cyclooctyne in pentane results in precipitation of a yellow complex containing a 6-membered metallacycle, W(C(8)H(12)C(8)H(12)NAr)(NAr)Cl(2) (1). This easily accessible compound was tested for its ability to effect carbonyl olefination/ring-closing metathesis (CO/RCM) with two substrates. One ketone was tested, 1-acetyl-1-(3-butenyl)cyclopentane, which generates 1-methylspiro[4.4]non-1-ene on CO/RCM. An ester, 4-benzoyloxybut-1-ene, was also test with 1 for CO/RCM. The dichloride 1 was found to be inactive; consequently, several derivatives were prepared, fully characterized including X-ray diffraction, and tested: W(C(8)H(12)C(8)H(12)NAr)(NAr)(OEt)(2) (2), W(C(8)H(12)C(8)H(12)NAr)(NAr)(OC(6)H(4)-p-OMe)(2) (3), W(C(8)H(12)C(8)H(12)NAr)(NAr)(OC(6)F(5))(2) (4), and W(C(8)H(12)C(8)H(12)NAr)(NAr)(Cl)(OTf) (5). In addition, synthesis of cationic complexes was attempted using 1 with Na[B(Ar(F))(4)] or AlCl(3). We were unsuccessful in fully characterizing the cations; however, these cations generated in situ show very high activity for CO/RCM with these substrates.

SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA