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1.
J Infect Dev Ctries ; 18(1): 27-33, 2024 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-38377088

RESUMO

INTRODUCTION: Coronavirus disease 2019 (COVID-19) has infected millions of people globally. Many recent studies have suggested that the ABO blood type may contribute to COVID-19 infection immunopathogenesis. We aimed to determine the proportional distribution of COVID-19 infection among ABO blood types. METHODOLOGY: This retrospective research was conducted in the city of Jodhpur (Rajasthan), India. The research involved 1140 COVID-19 patients, whose medical records were available in blood banks. The data was evaluated statistically using IBM SPSS 26. RESULTS: The proportion of blood group B among infected patients was highest (37.36%). Among all the cases, blood group A had the highest odds ratio of 1.062 (CI 95%, 0.92-1.21, p = 0.412). All versus one blood group analysis also showed that blood group A (odds ratio = 1.062 [CI 95%, 0.92-1.22] p = 0.412) was more likely to be infected with COVID-19 than the remaining blood groups. In the year 2021, blood group B had the highest risk of COVID-19 infection (odds ratio = 1.138). CONCLUSIONS: Based on our findings, the blood groups A and B are more likely to be infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The overall average age for COVID-19 infection was lower, and the number of incidences in female patients was higher in 2021, relative to 2020. We found no evident relationship between COVID-19 vulnerabilities and blood group. A summary of the research is presented in Supplementary Figure 1.


Assuntos
COVID-19 , SARS-CoV-2 , Humanos , Feminino , COVID-19/epidemiologia , Estudos Retrospectivos , Sistema ABO de Grupos Sanguíneos , Índia/epidemiologia
2.
Future Microbiol ; 18: 323-334, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-37140267

RESUMO

Background: The present study evaluates the efficacy of bacteriophage therapy for urinary tract infection (UTI) in rats. Methods: UTI was established by inoculating Escherichia coli (100 µl) at a concentration of 1.5 × 108 CFU/ml per urethra via a cannula in different groups of rats. For treatment, phage cocktails (200 µl) were administered at varying concentrations of 1 × 108 PFU/ml, 1 × 107 PFU/ml and 1 × 106 PFU/ml. Results: The two doses of phage cocktail at the first two concentrations resulted in the cure of UTI. However, the lowest concentration of the phage cocktail warranted more doses to eradicate the causative bacteria. Conclusion: The quantity, frequency and safety of doses could be optimized in a rodent model using the urethral route.


Antimicrobial resistance is primarily caused by antibiotic overuse and misuse, which results in a decline in the ability of antibiotics to treat infections. Urinary tract infections (UTIs) are common but difficult to treat, as they are frequently caused by multidrug-resistant bacteria. Escherichia coli is a common cause of UTIs. Bacteriophages are a potentially viable alternative for the treatment of bacterial infections, and despite the numerous benefits of using phages as antibacterial therapeutics, there are surprisingly few original research articles based on clinical trials, specifically against UTIs. In this study, the efficiency of a customized bacteriophage cocktail for the treatment of UTIs, with varied doses administered directly into the urinary bladder of rats, was evaluated. At higher concentrations, UTIs were completely eradicated after two doses of the bacteriophage cocktail. However, at lower concentrations, additional doses were required to eradicate the infection. Phage therapy appears to have therapeutic potential, and this study indicates the potential frequency of dosages at appropriate concentrations. Phage therapy was both effective and safe.


Assuntos
Bacteriófagos , Infecções por Escherichia coli , Terapia por Fagos , Infecções Urinárias , Escherichia coli Uropatogênica , Ratos , Animais , Infecções por Escherichia coli/microbiologia , Infecções Urinárias/tratamento farmacológico , Antibacterianos/farmacologia
3.
Indian J Radiol Imaging ; 33(1): 98-100, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36855726

RESUMO

Aim To determine the effectiveness of the first trimester Samrakshan protocol for the identification of pregnant women at high risk for preterm pre-eclampsia (PE). Methods Samrakshan uses a protocol that integrates routine first-trimester ultrasound assessment at 11 to 14 gestation weeks with the measurement of mean arterial blood pressure and mean uterine artery pulsatility index assessment to determine a customized risk for preterm PE and fetal growth restriction. Based on the risk assessment, pregnant women are classified as high or low risk. Results The protocol had a high specificity (90.4%, 95% CI: 89.4%, 91.2%) and negative predictive value (98.1%, 95% CI: 97.6%, 99%) for preterm PE. The odds ratio and positive likelihood ratio for preterm PE were 16.7 (95% CI: 12.3, 22.6) and 6.64 (95% CI: 5.77, 7.63), respectively. Conclusions The positive likelihood ratio and odds ratios indicate that pregnant women identified as high risk for preterm PE using the first-trimester protocol of Samrakshan are significantly more likely to develop preterm PE than low-risk women.

4.
Appl Biochem Biotechnol ; 195(9): 5568-5582, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35666381

RESUMO

Urinary tract infections (UTIs) are among the most prevalent bacterial infections worldwide, with 11% of the global population getting infected every year. These infections are largely attributed to quorum sensing (QS)-dependent ability of pathogens to form biofilms in the urinary tract. Antimicrobial resistance is increasing, and the use of antimicrobial medicines in the future is yet uncertain. The desert medicinal plants have great potential to treat several diseases as per the available ethnobotanical database. Some of these plants have been used in folklore medicines to treat urinary tract infections also. There are many bioactive compounds derived from these desert medicinal plants that have been documented to possess antimicrobial as well as antibiofilm activity against uropathogens. The minimum biofilm inhibitory concentration (MBIC) of these plant extracts have been reported in the range of 31.5-250 µg/mL. The rising prevalence of drug-resistant diseases necessitates standardised modern analytical technologies to detect and isolate novel bioactive compounds from medicinal plants. This review seeks to combine the studies of desert plants with antimicrobial and anti-quorum sensing properties, supporting their sustainable use in treatment of urinary tract infections.


Assuntos
Anti-Infecciosos , Plantas Medicinais , Infecções Urinárias , Biofilmes , Percepção de Quorum , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Anti-Infecciosos/farmacologia , Infecções Urinárias/tratamento farmacológico , Antibacterianos/farmacologia
5.
J Med Case Rep ; 16(1): 482, 2022 Dec 28.
Artigo em Inglês | MEDLINE | ID: mdl-36575475

RESUMO

BACKGROUND: Fetal midgut volvulus is an uncommon yet potentially life-threatening condition. Prenatal diagnosis may pose a challenge, due to the paucity of specific signs and symptoms. Timely prenatal diagnosis of this condition is imperative to prevent fetal mortality and morbidity. CASE PRESENTATION: We present a rare case report of fetal midgut volvulus, malrotation, and intestinal obstruction at 32 weeks of gestation in a 31-year-old multigravida Indian patient who presented with decreased fetal movements. Fetal ultrasound revealed midgut volvulus with proximal bowel obstruction and polyhydramnios. The patient underwent emergency surgery, which revealed intestinal malrotation and confirmed the diagnosis of midgut volvulus. Untwisting of the volvulus was done followed by Ladd's procedure. Follow-up postoperative ultrasound was unremarkable. CONCLUSIONS: Delay in the diagnosis of fetal midgut volvulus leads to poor fetal and maternal outcomes. Hence, it is vital for radiologists, sonologists, and obstetricians to be aware of this condition while performing fetal sonography. Prompt diagnosis and surgical intervention are vital to reduce the morbidity and mortality associated with this condition.


Assuntos
Obstrução Intestinal , Volvo Intestinal , Gravidez , Feminino , Humanos , Adulto , Volvo Intestinal/diagnóstico por imagem , Volvo Intestinal/cirurgia , Volvo Intestinal/complicações , Diagnóstico Pré-Natal , Obstrução Intestinal/etiologia , Ultrassonografia Pré-Natal/efeitos adversos , Feto
6.
BMC Chem ; 16(1): 61, 2022 Aug 17.
Artigo em Inglês | MEDLINE | ID: mdl-35978438

RESUMO

INTRODUCTION: Aurora-A kinase is associated with the Aurora kinase family which has been considered a striking anticancer target for the treatment of human cancers. OBJECTIVE: To design, synthesize, anticancer evaluation, and docking studies of novel 2-(1-isonicotinoyl-3-phenyl-1H-pyrazol-4-yl)-3-phenylthiazolidin-4-one derivatives as Aurora-A Kinase inhibitors. METHOD: A total of 21 Pyrazole derivatives P (1-21) were synthesized by using the Vilsmeier Haack reagent which was characterized by FT-IR, 1H NMR, 13C NMR, and Mass spectroscopy. The synthesized derivatives were evaluated for their potential in vitro anticancer activity by MTT assay and Aurora-A kinase inhibition assay. RESULTS: The cytotoxicity assay (MTT assay) showed that compound P-6 exhibited potent cytotoxicity (IC50 = 0.37-0.44 µM) against two cancer (HCT 116 and MCF-7) cell lines, which were comparable to the standard compound, VX-680. Compound P-6 also showed inhibition of Aurora-A kinase with an IC50 value of 0.11 ± 0.03 µM. A Docking study was done to compound P-6 and P-20 into the active site of Aurora A kinase, in order to get the probable binding model for further study. CONCLUSION: A series of 21 novel pyrazole derivatives P(1-21) were designed, synthesized, in vitro anticancer evaluation, and docking studies for Aurora A kinase inhibition. The results established that P-6 is a prospective aspirant for the development of anticancer agents targeting Aurora-A kinase.

7.
Front Microbiol ; 13: 965053, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36016776

RESUMO

Urinary tract infection (UTI) is a common infectious disease that affects men and women. It is a significant health concern due to multidrug-resistant (MDR) organisms. Therefore, it is necessary to have a current understanding of the antibiotic susceptibility (AS) pattern of uropathogens to manage UTI effectively. Since the bacterial pathogen causing UTI and its AS vary with time and place, the prevailing AS pattern of the causative agents are essential for empirical antibiotic therapy. This study aims to determine the prevalence and AS of uropathogens isolated from UTI patients in the eastern part of Northern India. The study was carried out between November 2018 and December 2019. Clean catch midstream urine samples were collected and processed using standard guidelines for microbiological procedures. Positive microbiological cultures were found in 333 of the 427 patients, where 287 were gram-negative bacteria (GNB), and 46 were gram-positive bacteria (GPB). Females had a higher prevalence of UTI (60.7%) than males (39.3%) (p = 0.00024). The most susceptible age group in females was 18-50 years as compared to males, whereas at the age of 51-80 years and >80 years males were more susceptible than females (p = 0.053). The most prevalent pathogen identified were Escherichia coli (55.0%), followed by Proteus sp. (6.9%), Klebsiella pneumoniae (6.6%), Pseudomonas aeruginosa (6.3%), of which 96.0% were MDR bacteria. The susceptibility pattern of our study also revealed that amikacin, gentamycin and imipenem were the most effective drugs against GNB. In contrast, nitrofurantoin, vancomycin, and chloramphenicol were the most effective drugs against GPB. According tothe findings, MDR pathogens are very much prevalent. Since UTI is one of the most frequent bacterial diseases, proper management necessitates extensive investigation and implementation of antibiotic policy based on AS patterns for a particular region.

8.
Indian J Radiol Imaging ; 32(1): 30-37, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35722649

RESUMO

Aim The aim of the study is to determine improvements in perinatal mortality at the end of the first 2 years from the initiation of the Samrakshan program of the Indian Radiological and Imaging Association. Methods Samrakshan is a screening program of pregnant women that uses trimester-specific risk assessment protocols including maternal demographics, mean arterial pressure, and fetal Doppler studies to classify women as high risk or low risk for preterm preeclampsia (PE) and fetal growth restriction (FGR). Low dose aspirin 150 mg daily once at bedtime was started for pregnant women identified as high risk in the 11-13 6/7 weeks screening. The third-trimester screening focused on the staging of FGR and protocol-based management for childbirth and risk assessment for PE. Outcomes of childbirth including gestational age at delivery, development of PE, and perinatal mortality outcomes were collected. Results Radiologists from 38 districts of 16 states of India participated in the Samrakshan program that screened 2,816 first trimester, 3,267 second trimester, and 3,272 third trimester pregnant women, respectively. At 2 years, preterm PE was identified in 2.76%, preterm births in 19.28%, abnormal Doppler study in 25.76% of third trimester pregnancies, and 75.32% of stage 1 FGR delivered at term. The neonatal mortality rate was 9.86/1,000 live births, perinatal mortality rate was 18.97/1,000 childbirths, and maternal mortality was 58/100,000 live births compared with 29.5, 36, and 113, respectively in 2016. Conclusion Fetal Doppler integrated antenatal ultrasound studies in Samrakshan led to a significant reduction in preterm PE rates, preterm birth rates, and a significant improvement in mean birth weights. Perinatal, neonatal, and maternal mortality rates are significantly better than the targets for 2030 set by the Sustainable Development Goals-3.

9.
Plants (Basel) ; 11(2)2022 Jan 11.
Artigo em Inglês | MEDLINE | ID: mdl-35050071

RESUMO

Rice-wheat (RW) rotation is the largest agriculture production system in South Asia with a multifaceted role in maintaining the livelihood of people. The customary practices and indiscriminate use of synthetic fertilizers have culminated in the decline of its productivity and profitability during the past two decades, thus affecting the sustainability of wheat. Safe Rock® Minerals (SRM) is a multi-nutrient rich natural rock mineral with great potential to manage soil degradation, reducing the input of fertilizers, improving soil fertility, and plant health. Thus, a field trial was conducted at the research farm of ICAR-Indian Agricultural Research Institute, New Delhi from 2016 to 2018 to evaluate the impact of Safe Rock® Minerals (SRM) on biometric parameters, productivity, quality, and nutrient uptake by conventional wheat and System of Wheat Intensification (SWI) in the wheat-rice cropping system. The results indicate that SWI performed better in terms of growth, yield, and quality parameters than conventional wheat. Among nutrient management practices; the highest growth, yield, and yield attributes of wheat were achieved with the use of SRM application 250 kg ha-1 + 100% Recommended Dose of Fertilizer (RDF). SRM application also increased grain protein content significantly. In conclusion, the integrated use of SRM with organic manures can serve as an eco-friendly approach for sustainable wheat production.

10.
Appl Microbiol Biotechnol ; 105(24): 9047-9067, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34821965

RESUMO

The rise in multi-drug resistant bacteria and the inability to develop novel antibacterial agents limits our arsenal against infectious diseases. Antibiotic resistance is a global issue requiring an immediate solution, including the development of new antibiotic molecules and other alternative modes of therapy. This article highlights the mechanism of bacteriophage treatment that makes it a real solution for multidrug-resistant infectious diseases. Several case reports identified phage therapy as a potential solution to the emerging challenge of multi-drug resistance. Bacteriophages, unlike antibiotics, have special features, such as host specificity and do not impact other commensals. A new outlook has also arisen with recent advancements in the understanding of phage immunobiology, where phages are repurposed against both bacterial and viral infections. Thus, the potential possibility of phages in COVID-19 patients with secondary bacterial infections has been briefly elucidated. However, significant obstacles that need to be addressed are to design better clinical studies that may contribute to the widespread use of bacteriophage therapy against multi-drug resistant pathogens. In conclusion, antibacterial agents can be used with bacteriophages, i.e. bacteriophage-antibiotic combination therapy, or they can be administered alone in cases when antibiotics are ineffective.Key points• AMR, a consequence of antibiotic generated menace globally, has led to the resurgence of phage therapy as an effective and sustainable solution without any side effects and high specificity against refractory MDR bacterial infections.• Bacteriophages have fewer adverse reactions and can thus be used as monotherapy as well as in conjunction with antibiotics.• In the context of the COVID-19 pandemic, phage therapy may be a viable option.


Assuntos
Bacteriófagos , COVID-19 , Antibacterianos/uso terapêutico , Humanos , Pandemias , Estudos Prospectivos , SARS-CoV-2
11.
Biol Reprod ; 105(4): 808-821, 2021 10 11.
Artigo em Inglês | MEDLINE | ID: mdl-34159367

RESUMO

The outbreak of the coronavirus disease 2019 (COVID-19) has created havoc on the socio-economic aspect of the world. With billions of lives being affected by this wrecking pandemic, global fertility services were also not left untouched by its impact. The possibility of sexual transmission of SARS-CoV-2 virus, its impact on male and female fertility, pregnancy, its potential teratogenic effect, and handling of gametes in the clinical laboratories were major concerns among reproductive medicine specialists, which led down all the reproductive health services, including IUI, IVF/ICSI in most of the countries. Even the people did not intend to conceive during the pandemic crisis and were hesitant to avail such services. Discrete evidence regarding the pathophysiology of COVID-19 infection and its impact on the human reproductive system is not very clear. In this review article, we intend to incorporate all the evidence related to the COVID-19 infection and its impact on human reproduction available to date. It is our responsibility to provide rightful information and to keep our patients familiar with the existing lack of clear evidence. In this COVID-19 era, it is important that the fertility management be prioritized in sub-fertile couples with diminished fertility reserve and high-risk conditions, like malignancies, that may affect their long-term fertility prospects.


Assuntos
COVID-19/complicações , Genitália , Infertilidade/etiologia , Pandemias , Medicina Reprodutiva/tendências , Fenômenos Reprodutivos Fisiológicos , Técnicas de Reprodução Assistida/tendências , Animais , Feminino , Preservação da Fertilidade , Humanos , Infertilidade/terapia , Masculino , Gravidez
12.
Braz. arch. biol. technol ; 64: e21190749, 2021. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1278444

RESUMO

Abstract Bacteriocin has been identified as an excellent alternative to chemical preservatives due to its astonishing antimicrobial activity against food spoiling and food-borne pathogens. So there is a need to identify the newer and potent sources of bacteriocin producers. This study aims the isolation of potent bacteriocin producing microorganism from fresh fruits and vegetables, its production, purification, and characterization. Firstly, 43 isolates were analysed for its antimicrobial potential, out of which7 were found to inhibit the growth of various pathogens. Considering the results of antimicrobial activity; the microorganism isolated from mango was regarded as the most potent one; which was identified as Bacillus subtilis VS.70% ammonium sulphate precipitated and dialysed bacteriocin was purified using DEAE cellulose and sephadex G75 chromatography. Bacteriocin was purified by 24.64 fold with 8.65% recovery and its molecular weight was found to be 31.2kDa. The Purified bacteriocin was found to be stable at broad pH and temperature. It was found to be degraded by various proteases studied confirming its proteinaceous nature. Considering all these attributes; the purified bacteriocin isolated from Bacillus subtilis VS can be exploited by various food industries.


Assuntos
Peptídeo Hidrolases/análise , Bacteriocinas/análise , Anti-Infecciosos/análise , Bacillus subtilis , Cromatografia
13.
Drug Deliv ; 27(1): 888-899, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32551978

RESUMO

The present study was focused on investigating niosomal gels loaded with cholinergic drug; pilocarpine HCl, for prolonged precorneal residence time and improved bioavailability for glaucoma treatment. Pilocarpine HCl niosomes were prepared using various nonionic surfactants (span 20, span 60 and span 80), in the presence of cholesterol in different molar ratios by ether injection method. The selected formulations were incorporated into carbopol 934 and locust bean gum-based gels. TEM analysis confirmed that niosomes formed were spherical in shape and has a definite internal aqueous space with uniform particle size. Formulation F4 composed of span 60 and cholesterol (1:1) gave the highest entrapment (93.26 ± 1.75%) and slower release results after 8 hours (Q8h = 60.35 ± 1.87%) among other formulations. The in-vitro drug permeation studies showed that there was a prolonged release of drug from niosomal gels as compared to niosomes itself. Considering the in-vitro drug release, niosomal gel formulation G2 was the best among the studied formulations. The release data were fitted to an empirical equation, which indicated that the release follows non-Fickian diffusion mechanism. The stability study revealed that incorporation of niosomes in gel increased their stability than the niosome itself. No signs of redness, inflammation, swelling or increased tear production were observed over the study period for tested formulation by Draize's test. The intraocular pressure (IOP) lowering activity of G2 formulation showed relative bioavailability 2.64 times more than bioavailability of marketed Pilopine HS® gel. These results suggest that the niosomal gels containing pilocarpine HCl are promising ocular carriers for glaucoma treatment.


Assuntos
Sistemas de Liberação de Medicamentos/métodos , Pressão Intraocular/efeitos dos fármacos , Lipossomos/química , Pilocarpina/administração & dosagem , Pilocarpina/farmacologia , Administração Oftálmica , Animais , Química Farmacêutica/métodos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Glaucoma/tratamento farmacológico , Hexoses/química , Tamanho da Partícula , Pilocarpina/farmacocinética , Coelhos
14.
J Midlife Health ; 10(2): 70-74, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31391755

RESUMO

BACKGROUND: Sexual health is the most important aspect of person's well being, self-esteem and quality of life. Sexual pleasure leads to enhanced conjugal relationships and an overall healthy psychological state. There is paucity of data on sexual health of postmenopausal women. AIMS AND OBJECTIVES: To assess the prevalence and determinants of sexual health in postmenopausal women of North India. MATERIALS AND METHODS: The study was conducted over a period of 18 months, from January 2016 to June 2017. Standard FSFI-6 questionnaire and various socio-demographic factors were used to analyse the sexual health of 110 menopausal women. RESULTS: 80.9% postmenopausal women reported sexual dysfunction (SD). We found more sexual dysfunction in postmenopausal women with increasing age and increasing duration of menopause. Satisfied past sexual experience, joint family structure, low socioeconomic and education status were found to be important determinants of sexual health of postmenopausal females. Parity, substance use and past medical and gynaecological history of participants and various partner's factors like medical disorders, substance use and sexual disorders showed no association with sexual health in postmenopausal females. CONCLUSION: Sexuality varies with cultural and social differences across the globe. The prevalence of female sexual dysfunction in our study is much higher because Indian women are suppressed, self conscious, inhibited and hesistant to talk about their sexual problems with health care professionals. Also revalidation of the FSFI tool for Indian population is required. Further studies are needed to evaluate the sexual health in postmenopausal women.

15.
Artigo em Inglês | MEDLINE | ID: mdl-29697033

RESUMO

BACKGROUND: The benzimidazole ring is an important pharmacophore in modern drug discovery. Mannich reaction is one of the versatile reaction widely used in organic synthesis. Mannich base derivatives play an important role in medical field with diverse biological actions. OBJECTIVE: A series of N-(benzimidazol-1-ylmethyl)-4-chlorobenzamide derivatives (3a- 3m) were synthesized and evaluated for anti-inflammatory and antimicrobial potential. METHOD: Mannich reaction was used to synthesize N-(benzimidazol-1-ylmethyl)-4- chlorobenzamide analogues. The structures of novel target compounds were elucidated by spectral and analytical techniques and screened for in vivo anti-inflammatory activity and ulcerogenic activity. In addition, the prepared derivatives were also evaluated for in vitro antimicrobial activity against gram negative, gram positive and fungal strains. Further, in silico studies were carried out to define the interaction of the title compounds with COX-2 enzyme and microbial protein. RESULTS: The results revealed that out of thirteen molecules, compound 3a (containing chloromethyl substituent at 2-position of benzimidazole) showed significant antiinflammatory effect at a dose of 100 mg/kg p.o. and the experimental data was statistically significant at p≤0.05 level. Diclofenac sodium was taken as standard drug for antiinflammatory activity. Furthermore, derivative 3e (containing 2-chlorophenyl moiety at 2- position of benzimidazole scaffold) was found to be the most effective antimicrobial compound among the synthesized derivatives. Ciprofloxacin and clotrimazole were used as reference antimicrobial agents. Results from in vivo and in vitro studies of synthesized analogues were found to be in good correlation with in silico study. CONCLUSION: These results designate that N-(Benzimidazol-1-ylmethyl)-4-chlorobenzamide analogues, substituted with halogen functionality, could be used as potential lead for designing more potent anti-inflammatory and antimicrobial agents.


Assuntos
Anti-Infecciosos , Anti-Inflamatórios , Benzimidazóis , Edema/tratamento farmacológico , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/uso terapêutico , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Aspergillus niger/efeitos dos fármacos , Aspergillus niger/crescimento & desenvolvimento , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Benzimidazóis/química , Benzimidazóis/farmacologia , Benzimidazóis/uso terapêutico , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Carragenina , Edema/induzido quimicamente , Feminino , Masculino , Simulação de Acoplamento Molecular , Ratos Wistar , Testes de Toxicidade Aguda
16.
EXCLI J ; 15: 730-737, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-28337104

RESUMO

A series of 1-(4-methylquinolin-2-yl)-4,6-diaryl-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives was synthesized by the reaction of 3-cinnamoyl-4-hydroxy-6-methyl-2H-pyran-2-ones with 2-chloro-4,6-diphenylnicotinonitrile analogues in the presence of 2-hydrazino-4-methyl quinoline and ethanol. The newly synthesized compounds were characterized by IR, 1H NMR and mass spectral data. The synthetic series of novel quinoline-pyrazolopyridine hybrids were screened for in vitro schizont maturation assay against chloroquine sensitive 3D7 strain of Plasmodium falciparum, from which the most five active analogues were further evaluated for in vivo 4-day suppressive test in Swiss albino mice. Among the series, 5p (containing 4-Cl substituent attached to both aryl ring) portrayed considerable potent antimalarial activity during in vitro as well as in vivo study.

17.
Eur J Med Chem ; 70: 248-58, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24161702

RESUMO

Pyrazole has been the topic of interest for thousands of researchers across the world because of its wide spectrum pharmacological activities. Various structural modifications of the pyrazole nucleus have been made to explore its characteristics and biological potential. The present work aims to review the use of molecular modeling in the designing of novel pyrazole analogs that may target various receptors such as protein kinase inhibitor, tyrosine kinase, Aurora-A kinase, tumor growth factor (TGF), cyclin dependent kinase (CDK) and fibroblast growth factor (FGF), which are significant for the management of cancer. An insight has been given in this article for the importance of pyrazoles in the treatment of cancer and the perspectives that they hold for future research.


Assuntos
Antineoplásicos/farmacologia , Neoplasias/tratamento farmacológico , Pirazóis/farmacologia , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Humanos , Modelos Moleculares , Neoplasias/enzimologia , Neoplasias/metabolismo , Pirazóis/síntese química , Pirazóis/química
18.
EXCLI J ; 12: 1030-42, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-27298613

RESUMO

A series of 3-aryl-1-phenyl-1H-pyrazole derivatives was synthesized in good yield and assayed in vitro as inhibitors of the mice acetylcholinesterase (AChE) and two goat liver monoamine oxidase (MAO) isoforms, MAO-A and MAO-B. Most of the compounds demonstrated a good AChE and selective MAO-B inhibitory activities in the nanomolar or low micromolar range. N-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-yl) methylene) benzenamine (3e, pIC50 = 4.2) and N-((4-fluorophenyl)-1-phenyl-1H-pyrazole-4-yl) methylene) methanamine (3f, pIC50 = 3.47) were the most potent AChE and highly selective MAO-B inhibitors respectively. Structure activity relationships showed that chloro derivatives were more effective AChE inhibitors as compared to fluoro derivatives while reverse trend was observed in MAO-B inhibitory activity. With the aid of modeling studies, potential binding orientations as well as interactions of the compounds in the AChE and MAO-B active sites were examined.

19.
J Cancer Surviv ; 7(1): 104-14, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-23224753

RESUMO

PURPOSE: Childhood cancer survivors are at risk for late effects which may be managed pharmacologically. The purposes of this study were to estimate and compare the prevalence of psychoactive medication use of adult survivors of childhood cancer and sibling controls, identify predictors of medication use in survivors, and investigate associations between psychoactive medications and health-related quality of life (HRQOL). METHODS: Psychoactive medication use from 1994 to 2010 was evaluated in 10,378 adult survivors from the Childhood Cancer Survivor Study. A randomly selected subset of 3,206 siblings served as a comparison group. Multivariable logistic regression models were used to calculate odds ratios (OR) for baseline and new onset of self-reported psychoactive medication use and HRQOL. RESULTS: Survivors were significantly more likely to report baseline (22 vs. 15 %, p < 0.001) and new onset (31 vs. 25 %, p < 0.001) psychoactive medication use compared to siblings, as well as use of multiple medications (p < 0.001). In multivariable models, controlling for pain and psychological distress, female survivors were significantly more likely to report baseline and new onset use of antidepressants (OR = 2.66, 95 % CI = 2.01-3.52; OR = 2.02, 95 % CI = 1.72-2.38, respectively) and multiple medications (OR = 1.80, 95 % CI = 1.48-2.19; OR = 1.77, 95 % CI = 1.48-2.13, respectively). Non-cranial radiation and amputation predicted incident use of analgesics >15 years following diagnosis. Antidepressants were associated with impairment across all domains of HRQOL, with the exception of physical function. CONCLUSIONS: Prevalence of psychoactive medication use was higher among survivors for most medication classes, as was the use of multiple medications. Clinicians should be aware of the possible contribution of psychoactive medications to HRQOL. IMPLICATIONS FOR CANCER SURVIVORS: Survivors of childhood cancer are more likely to be prescribed psychoactive medication than their sibling counterparts, though use of such medication does not appear to normalize quality of life. Survivors are encouraged to consider additional interventions, including psychosocial support and physical exercise.


Assuntos
Prescrições de Medicamentos , Neoplasias/psicologia , Avaliação de Resultados em Cuidados de Saúde , Psicotrópicos/uso terapêutico , Qualidade de Vida , Estresse Psicológico/tratamento farmacológico , Sobreviventes/psicologia , Adolescente , Adulto , Feminino , Humanos , Masculino , Prevalência , Relatório de Pesquisa , Fatores de Risco , Estresse Psicológico/epidemiologia , Estresse Psicológico/etiologia , Estados Unidos/epidemiologia , Adulto Jovem
20.
Physiol Mol Biol Plants ; 18(2): 185-90, 2012 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-23573056

RESUMO

Standardization of biomass production in different vessels and bioreactor using explants and media for growth, total phenolic content and antioxidant capacity of shoot culture of Bacopa monnieri is described. Maximum number of shoots per explant, higher explants response irrespective of the type of explants, and higher shoot length was obtained on MS medium containing BAP (2.5 mg l(-1)) and IAA (0.01 mg l(-1)) with 3 % sucrose. This medium was selected by varying BAP concentration and recorded optimal for shoot culture on gelled medium. The condition of 0.5 cm explant size and 20 explant/40 ml (1 explant/2 ml) was optimal for high explant response, number of shoots per explant regenerated and shoots length. Among the different vessels used, maximum growth index was achieved in Growtek bioreactor (10.0) followed by magenta box (9.16), industrial glass jar (7.7) and conical flask (7.2). The cultures grown in conical flask (100 ml) were used as control. The total phenolic content and antioxidant capacity of in vitro grown plants was higher to that recorded for in vivo material. Among in vitro regenerated plants, the activity was maximal in the tissues grown in 250 ml conical flask. The most critical function for vessels is to support the optimum profusion (growing area for maximum growth) of shoots and for B. monnieri, Growtek bioreactor supported 1980 shoots l(-1) medium as compared to control (938 shoots l(-1)). Growtek bioreactor was considered effective system to produce B. monnieri biomass in culture without loss of antioxidant properties.

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