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Given the future demand for food crops, increasing crop productivity in drought-prone rainfed areas has become essential. Drought-tolerant varieties are warranted to solve this problem in major crops, with drought tolerance as a high-priority trait for future research. Maize is one such crop affected by drought stress, which limits production, resulting in substantial economic losses. It became a more serious issue due to global climate change. The most drought sensitive among all stages of maize is the reproductive stages and the most important for overall maize production. The exact molecular basis of reproductive drought sensitivity remains unclear due to genes' complex regulation of drought stress. Understanding the molecular biology and signaling of the unexplored area of reproductive drought tolerance will provide an opportunity to develop climate-smart drought-tolerant next-generation maize cultivars. In recent decades, significant progress has been made in maize to understand the drought tolerance mechanism. However, improving maize drought tolerance through breeding is ineffective due to the complex nature and multigenic control of drought traits. With the help of advanced breeding techniques, molecular genetics, and a precision genome editing approach like CRISPR-Cas, candidate genes for drought-tolerant maize can be identified and targeted. This review summarizes the effects of drought stress on each growth stage of maize, potential genes, and transcription factors that determine drought tolerance. In addition, we discussed drought stress sensing, its molecular mechanisms, different approaches to developing drought-resistant maize varieties, and how molecular breeding and genome editing will help with the current unpredictable climate change.
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Secas , Zea mays , Zea mays/genética , Melhoramento Vegetal , Resistência à Seca , Produtos Agrícolas/genética , PercepçãoRESUMO
Stripe rust (Sr), caused by Puccinia striiformis f. sp. tritici (Pst), is the most devastating disease that poses serious threat to the wheat-growing nations across the globe. Developing resistant cultivars is the most challenging aspect in wheat breeding. The function of resistance genes (R genes) and the mechanisms by which they influence plant-host interactions are poorly understood. In the present investigation, comparative transcriptome analysis was carried out by involving two near-isogenic lines (NILs) PBW343 and FLW29. The seedlings of both the genotypes were inoculated with Pst pathotype 46S119. In total, 1106 differentially expressed genes (DEGs) were identified at early stage of infection (12 hpi), whereas expressions of 877 and 1737 DEGs were observed at later stages (48 and 72 hpi) in FLW29. The identified DEGs were comprised of defense-related genes including putative R genes, 7 WRKY transcriptional factors, calcium, and hormonal signaling associated genes. Moreover, pathways involved in signaling of receptor kinases, G protein, and light showed higher expression in resistant cultivar and were common across different time points. Quantitative real-time PCR was used to further confirm the transcriptional expression of eight critical genes involved in plant defense mechanism against stripe rust. The information about genes are likely to improve our knowledge of the genetic mechanism that controls the stripe rust resistance in wheat, and data on resistance response-linked genes and pathways will be a significant resource for future research.
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Basidiomycota , Triticum , Triticum/genética , Melhoramento Vegetal , Basidiomycota/genética , Genótipo , Perfilação da Expressão Gênica , Doenças das Plantas/genética , Resistência à Doença/genéticaRESUMO
Tetracycline (TC) antibiotic that is effective against wide-range micro-organisms, thereby used to control bacterial infection. The partial metabolism of TC antibiotics in humans and animals leads to the contamination of TC in the environments like water bodies. Thus, requirements to treat/remove/degrade TC antibiotics from the water bodies to control environmental pollution. In this context, this study focuses on fabricating PVP-MXene-PET (PMP) based photo-responsive materials to degrade TC antibiotics from the water. Initially, MXene (Ti2CTx) was synthesized using a simple etching process from the MAX phase (Ti3AlC2). The synthesized MXene was encapsulated using PVP and cast onto the surface of PET to fabricate PMP-based photo-responsive materials. The rough surface and micron/nano-sized pores within the PMP-based photo-responsive materials might be improved the photo-degradation of TC antibiotics. The synthesized PMP-based photo-responsive materials were tested against the photo-degradation of TC antibiotics. The band gap value of the MXene and PMP-based photo-responsive materials was calculated to be â¼1.23 and 1.67 eV. Incorporating PVP within the MXene increased the band gap value, which might be beneficial for the photo-degradation of TC, as the minimum band gap value should be â¼1.23 eV or more for photocatalytic application. The highest photo-degradation of â¼83% was achieved using PMP-based photo-degradation at 0.1 mg/L of TC. Furthermore, â¼99.71% of photo-degradation of TC antibiotics was accomplished at pH â¼10. Therefore, the fabricated PMP-based photo-responsive materials might be next-generation devices/materials that efficiently degrade TC antibiotics from the water.
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Antibacterianos , Tetraciclina , Humanos , Catálise , Tetraciclina/química , Antibacterianos/química , Água , Tomografia por Emissão de PósitronsRESUMO
Fats contribute majorly to food flavour, mouthfeel, palatability, texture, and aroma. Though solid fats are used for food formulation due to the processing benefits over oils, their negative health effects should not be overlooked. Oleogelation is thus used to transform liquid oil into a gel which function like fats and provide the nutritional benefits of oils. Additionally, only food-grade gelators convert the oils into solid-like, self-standing, three-dimensional gel networks. Rice bran wax, candelilla wax, carnauba wax, and sunflower wax are mainly used plant waxes for formulating oleogels as a result of their low cost, availability, and excellent gelling ability. A comprehensive information about the wax based oleogels, their characteristics and applications is needed. The present review discusses the effect of different plant-based waxes on the properties of the oleogel formed. The article provides information on how the physical and chemical properties of waxes impact the oleogel properties such as oil binding capacity, critical concentration, rheological, thermal, textural, morphological, and oxidative stability. Moreover, the current and potential applications of oleogels in the food sector have also been covered this article.
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OBJECTIVES: To evaluate the long-term outcomes of intrascleral haptic fixation of posterior chamber intraocular lens (PCIOL) with fibrin glue in children. METHODS: This is a retrospective case study conducted in a tertiary eye institute in North India. A total of 118 eyes of 82 children who underwent glued intrascleral haptic fixation of PCIOLs were retrospectively analyzed. Detailed analysis of the indication for surgery and ocular and systemic associations was performed. The outcome measures included intraoperative complications, final visual and refractive outcomes, and postoperative complications. RESULTS: The mean age of the patients was 10.16±3.94 years. Fifty-one patients (62.2%) were male and 31 (37.8%) were female. The mean follow-up period was 31.28±13.22 months. The mean preoperative corrected distance visual acuity was 1.18±0.63 Logarithm of Mean angle of resolution (logMAR) which improved to 0.60±0.58 logMAR postoperatively at 6 weeks (P<0.001). The mean preoperative and 6 weeks postoperative endothelial cell density were 3,176.08±318.6 and 2,936±289.9 cells/mm2, respectively (P=0.23). In the immediate postoperative period, corneal edema (19 eyes; 16.1%), decentered IOL/tilt (3 eyes; 2.54%), vitreous hemorrhage (3 eyes; 2.54%), optic capture (4 eyes; 3.38%), and hypotony (2 eyes; 1.69%) were seen. In the late postoperative period (>6 weeks), retinal detachment was observed in two eyes that had associated Marfan syndrome. Cystoid macular edema was seen in four eyes (3.38%), and glaucoma was seen in five eyes (4.23%). CONCLUSIONS: Fibrin glue-assisted intrascleral haptic fixation of a PCIOL is a safe and effective method to manage aphakia with inadequate capsular support in children.
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Adesivo Tecidual de Fibrina , Lentes Intraoculares , Adolescente , Criança , Feminino , Adesivo Tecidual de Fibrina/uso terapêutico , Tecnologia Háptica , Humanos , Índia , Masculino , Estudos RetrospectivosRESUMO
BACKGROUND: The COVID-19 public health emergency (PHE) has significantly changed medical practice in the United States, including an increase in the utilization of telemedicine. Here, we characterize change in neuro-ophthalmic care delivery during the early COVID-19 PHE, including a comparison of care delivered via telemedicine and in office. METHODS: Neuro-ophthalmology outpatient encounters from 3 practices in the United States (4 providers) were studied during the early COVID-19 PHE (March 15, 2020-June 15, 2020) and during the same dates 1 year prior. For unique patient visits, patient demographics, visit types, visit format, and diagnosis were compared between years and between synchronous telehealth and in-office formats for 2020. RESULTS: There were 1,276 encounters for 1,167 patients. There were 30% fewer unique patient visits in 2020 vs 2019 (477 vs 670) and 55% fewer in-office visits (299 vs 670). Compared with 2019, encounters in 2020 were more likely to be established, to occur via telemedicine and to relate to an efferent diagnosis. In 2020, synchronous telehealth visits were more likely to be established compared with in-office encounters. CONCLUSIONS: In the practices studied, a lower volume of neuro-ophthalmic care was delivered during the early COVID-19 public health emergency than in the same period in 2019. The type of care shifted toward established patients with efferent diagnoses and the modality of care shifted toward telemedicine.
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COVID-19/epidemiologia , Oftalmopatias/epidemiologia , Neurologia/organização & administração , Visita a Consultório Médico/tendências , Oftalmologia/organização & administração , Pandemias , Telemedicina/métodos , Comorbidade , Feminino , Humanos , Masculino , Estudos Retrospectivos , SARS-CoV-2 , Estados Unidos/epidemiologiaRESUMO
A series of rhodanine-3-acetic acid derivatives were synthesized via Knoevenagel condensation of rhodanine-3-acetic acid with various substituted aromatic aldehydes. The synthesized derivatives were screened in vitro for understanding the inhibitory potential towards pancreatic lipase (PL), a key enzyme responsible for the digestion of dietary fats. Derivative 8f exhibited a potential inhibitory activity towards PL (IC50 = 5.16 µM), comparable to that of the standard drug, orlistat (0.99 µM). An increase in the density of the aromatic ring resulted in potential PL inhibition. The enzyme kinetics of 8f exhibited a reversible competitive-type inhibition, similar to that of orlistat. Derivative 8f exhibited a MolDock score of -125.19 kcal/mol in docking studies, and the results were in accordance with their PL inhibitory potential. Furthermore, the reactive carbonyl group of 8f existed at a distance adjacent to Ser152 (≈3 Å) similar to that of orlistat. Molecular dynamics simulation (10 ns) of the 8f-PL complex revealed a stable binding conformation of 8f in the active site of PL (maximum root mean square displacement of ≈2.25 Å). The present study identified novel rhodanine-3-acetic acid derivatives with promising PL inhibitory potential, and further lead optimization might result in potent PL inhibitors.
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Desenho de Fármacos , Inibidores Enzimáticos/síntese química , Lipase/antagonistas & inibidores , Pâncreas/enzimologia , Rodanina/análogos & derivados , Rodanina/síntese química , Animais , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/toxicidade , Humanos , Dose Letal Mediana , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , Ligação Proteica , Rodanina/química , Rodanina/farmacologia , Relação Estrutura-AtividadeRESUMO
OBJECTIVES: To study the epidemiology, clinical profile, and the role of rapid tests in the diagnosis of acute bacterial meningitis (ABM) in children (1-59 months). MATERIALS AND METHODS: A total of 250 cerebrospinal fluid (CSF) and 187 blood samples received from clinically suspected cases of ABM were processed based on standard microbiological protocols. CSF samples were also subjected to antigen and nucleic acid detection. Antibiotic susceptibility testing was done according to the Clinical Laboratory Standards Institute guidelines. Children were also evaluated for outcomes and were followed up until 6 months after discharge. RESULTS: Eighty one cases were reported to be having clinically confirmed ABM, out of which group B Streptococcus was the most common pathogen detected in 49.3% (40) patients followed by Streptococcus pneumoniae, Staphylococcus aureus, Hemophilus influenzae type b, Escherichia coli, Klebsiella pneumoniae, and Neisseria meningitidis ACYW135 in 23.4% (19), 7.4% (6), 6.1% (5), 6.1% (5), 6.1% (5), and in 1.2% (1) patients, respectively. Complications were observed in 54.3% of the children. A follow-up of 6 months after discharge was possible in 39.5% (32) patients among whom sequelae were recorded in 93.7% (30) patients. CONCLUSION: ABM remains a major cause of neurological sequelae worldwide. Although culture is the gold standard test for its detection, the investigation takes a longer time and the results are influenced by prior antimicrobial therapy. In such cases, rapid tests aid in the early diagnosis of ABM for instituting appropriate management.
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Testes de Fixação do Látex/métodos , Meningites Bacterianas/diagnóstico , Meningites Bacterianas/epidemiologia , Pré-Escolar , Feminino , Humanos , Lactente , MasculinoRESUMO
Aim & objective: Levormeloxifene (L-ORM) and raloxifene (RAL) are selective estrogen receptor modulators used in the treatment of postmenopausal osteoporosis and breast cancer. Here, we developed and validated a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the simultaneous estimation of both drugs. Materials & methods: A quality-by-design (QbD) approach was used for the optimization of the nanoemulsion, and US FDA guidelines were followed for method validation. Results: Multiple reaction monitoring transitions were used for L-ORM (459.05â98.50), RAL (475.00â112.02) and internal standard (180.10â110.2). Analytes were resolved in a C18 column with 80:20 v/v% acetonitrile (ACN), 0.1% formic acid in triple-distilled water as a mobile phase. The developed method was linear over a concentration range of 1-600 ng/ml. Pharmacokinetic results of free L-ORM-RAL and the L-ORM-RAL nanoemulsion showed Cmax of free L-ORM - 70.65 ± 16.64, free RAL 13.53 ± 2.72, L-ORM nanoemulsion 65.07 ± 14.0 and RAL-nanoemulsion 59.27 ± 17.44 ng/ml. Conclusion: Future findings will contribute to the treatment of postmenopausal osteoporosis and breast cancer using L-ORM and RAL.
[Box: see text].
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Disponibilidade Biológica , Emulsões , Cloridrato de Raloxifeno , Moduladores Seletivos de Receptor Estrogênico , Espectrometria de Massas em Tandem , Espectrometria de Massas em Tandem/métodos , Cloridrato de Raloxifeno/farmacocinética , Cloridrato de Raloxifeno/administração & dosagem , Emulsões/química , Humanos , Cromatografia Líquida/métodos , Moduladores Seletivos de Receptor Estrogênico/farmacocinética , Moduladores Seletivos de Receptor Estrogênico/administração & dosagem , Animais , Administração Oral , Nanopartículas/química , Feminino , Osteoporose Pós-Menopausa/tratamento farmacológicoRESUMO
Phytosomes (phytophospholipid complex) are dosage forms that have recently been introduced to increase the stability and therapeutic effect of herbal medicine. Currently, bioactive herbs and the phytochemicals they contain are considered to be the best remedies for chronic diseases. One promising approach to increase the efficacy of plant-based therapies is to improve the stability and bioavailability of their bio-active ingredients. Phytosomes employ phospholipids as their active ingredients, and use their amphiphilic properties to solubilize and protect herbal extracts. The unique properties of phospholipids in drug delivery and their use in herbal medicines to improve bioavailability results in significantly enhanced health benefits. The introduction of phytosome nanotechnology can alter and revolutionize the current state of drug delivery. The goal of this review is to explain the application of phytosomes, their future prospects in drug delivery, and their advantages over conventional formulations. Please cite this article as: Chauhan D, Yadav PK, Sultana N, Agarwal A, Verma S, Chourasia MK, Gayen JR. Advancements in nanotechnology for the delivery of phytochemicals. J Integr Med. 2024; 22(4): 385-398.
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Sistemas de Liberação de Medicamentos , Nanotecnologia , Compostos Fitoquímicos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/administração & dosagem , Compostos Fitoquímicos/farmacocinética , Humanos , Fosfolipídeos/química , Disponibilidade Biológica , Fitoterapia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Extratos Vegetais/farmacocinéticaRESUMO
Aim: A newer LC-MS/MS method was developed and validated for the simultaneous quantification of raloxifene (RL) and cladrin (CL). Methodology: Both drugs were resolved in RP-18 (4.6 × 50 mm, 5 µ) Xbridge Shield column using acetonitrile and 0.1% aqueous solution of formic acid (FA) (70:30% v/v) as mobile phase by using biological matrices in female Sprague-Dawley rats using-MS/MS. Results: The developed method was found to be linear over the concentration ranges of 1-600 ng/ml, and lower limit of quantification was 1 ng/ml for RL and CL, respectively. Pharmacokinetic results of RL+CL showed Cmax = 4.23 ± 0.61, 26.97 ± 1.14 ng/ml, at Tmax(h) 5.5 ± 1.00 and 3.5 ± 1.00, respectively. Conclusion: Pharmacokinetic study results will be useful in the future for the combined delivery of RL and CL for osteoporosis treatment.
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Isoflavonas , Espectrometria de Massa com Cromatografia Líquida , Espectrometria de Massas em Tandem , Ratos , Feminino , Animais , Ratos Sprague-Dawley , Cromatografia Líquida/métodos , Espectrometria de Massas em Tandem/métodos , Cloridrato de Raloxifeno , Reprodutibilidade dos Testes , Cromatografia Líquida de Alta Pressão/métodosRESUMO
Sesame (Sesamum indicum L.) is a globally cultivated oilseed crop renowned for its historical significance and widespread growth in tropical and subtropical regions. With notable nutritional and medicinal attributes, sesame has shown promising effects in combating malnutrition cancer, diabetes, and other diseases like cardiovascular problems. However, sesame production faces significant challenges from environmental threats such as charcoal rot, drought, salinity, and waterlogging stress, resulting in economic losses for farmers. The scarcity of information on stress-resistance genes and pathways exacerbates these challenges. Despite its immense importance, there is currently no platform available to provide comprehensive information on sesame, which significantly hinders the mining of various stress-associated genes and the molecular breeding of sesame. To address this gap, here a free, web-accessible, and user-friendly genomic web resource (SesameGWR, http://backlin.cabgrid.res.in/sesameGWR/) has been developed This platform provides key insights into differentially expressed genes, transcription factors, miRNAs, and molecular markers like simple sequence repeats, single nucleotide polymorphisms, and insertions and deletions associated with both biotic and abiotic stresses.. The functional genomics information and annotations embedded in this web resource were predicted through RNA-seq data analysis. Considering the impact of climate change and the nutritional and medicinal importance of sesame, this study is of utmost importance in understanding stress responses. SesameGWR will serve as a valuable tool for developing climate-resilient sesame varieties, thereby enhancing the productivity of this ancient oilseed crop.
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INTRODUCTION: Novel injectables possess applications in both local and systemic therapeutics delivery. The advancement in utilized materials for the construction of complex injectables has tremendously upgraded their safety and efficacy. AREAS COVERED: This review focuses on various strategies to produce novel injectables, including oily dispersions, in situ forming implants, injectable suspensions, microspheres, liposomes, and antibody-drug conjugates. We herein present a detailed description of complex injectable technologies and their related drug formulations permitted for clinical use by the United States Food and Drug Administration (USFDA). The excipients used, their purpose and the challenges faced during manufacturing such formulations have been critically discussed. EXPERT OPINION: Novel injectables can deliver therapeutic agents in a controlled way at the desired site. However, several challenges persist with respect to their genericization. Astronomical costs incurred by innovator companies during product development, complexity of the product itself, supply limitations with respect to raw materials, intricate manufacturing processes, patent evergreening, product life-cycle extensions, relatively few and protracted generic approvals contribute to the exorbitant prices and access crunch. Moreover, regulatory guidance are grossly underdeveloped and significant efforts have to be directed toward development of effective characterization techniques.
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Aprovação de Drogas , Sistemas de Liberação de Medicamentos , Injeções , United States Food and Drug Administration , Humanos , Estados Unidos , Desenvolvimento de Medicamentos , Composição de Medicamentos , Excipientes/química , Preparações Farmacêuticas/administração & dosagem , Animais , Química FarmacêuticaRESUMO
Aim & Objective: This study evaluates the potential of combining paclitaxel (PTX) and bortezomib (BTZ) for breast cancer therapy. Materials & Methods: The nanoformulation was optimized via Box-Behnken Design (BBD), with method validation adhering to US-FDA guidelines. Results: Multiple reaction monitoring transitions for PTX, BTZ and internal standard were m/z 855.80â286.60, 366.80â226.00 and 179.80â110.00, respectively. Elution done on C18 Luna column with 0.1% FA in MeOH:10 mM ammonium acetate. The size of nanoformulation was 133.9 ± 1.97 nm, PDI 0.19 ± 0.01 and zeta potential -19.20 ± 1.36 mV. Pharmacokinetics showed higher Cmax for PTX-BTZ-NE (313.75 ± 10.71 ng/ml PTX, 11.92 ± 0.53 ng/ml BTZ) versus free PTX-BTZ (104 ± 13.06 ng/ml PTX, 1.9 ± 0.08 ng/ml BTZ). Conclusion: Future findings will contribute to the treatment of breast cancer using PTX and BTZ.
[Box: see text].
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Nitroimidazoles comprise a class of broad-spectrum anti-microbial drugs with efficacy against parasites, mycobacteria, and anaerobic Gram-positive and Gram-negative bacteria. Among these drugs, metronidazole (MTZ) is commonly used with other antibiotics to prevent infection in open fractures. However, the effect of MTZ on bone remains understudied. In this paper, we evaluated six nitroimidazole drugs for their impact on osteoblast differentiation and identified MTZ as having the highest osteogenic effect. MTZ enhanced bone regeneration at the femur osteotomy site in osteopenic ovariectomized (OVX) rats at the human equivalent dose. Moreover, in OVX rats, MTZ significantly improved bone mass and strength and improved microarchitecture compared to the vehicle-treated rats, which was likely achieved by an osteogenic mechanism attributed to the stimulation of the Wnt pathway in osteoblasts. To mitigate the reported neurological and genotoxic effects of MTZ, we designed an injectable sustained-release in situ gel formulation of the drug that improved fracture healing efficacy by 3.5-fold compared to oral administration. This enhanced potency was achieved through a significant increase in the circulating half-life and bioavailability of MTZ. We conclude that MTZ exhibits osteogenic effects, further accentuated by our sustained-release delivery system, which holds promise for enhancing bone regeneration in open fractures.
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Chronic kidney disease-induced secondary hyperparathyroidism (CKD-SHPT) heightens fracture risk through impaired mineral homeostasis and elevated levels of uremic toxins (UTs), which in turn enhance bone remodeling. Etelcalcetide (Etel), a calcium-sensing receptor (CaSR) agonist, suppresses parathyroid hormone (PTH) in hyperparathyroidism to reduce excessive bone resorption, leading to increased bone mass. However, Etel's effect on bone quality, chemical composition, and strength is not well understood. To address these gaps, we established a CKD-SHPT rat model and administered Etel at a human-equivalent dose concurrently with disease induction. The effects on bone and mineral homeostasis were compared with a CKD-SHPT (vehicle-treated group) and a control group (rats without SHPT). Compared with vehicle-treated CKD-SHPT rats, Etel treatment improved renal function, reduced circulating UT levels, improved mineral homeostasis parameters, decreased PTH levels, and prevented mineralization defects. The upregulation of mineralization-promoting genes by Etel in CKD-SHPT rats might explain its ability to prevent mineralization defects. Etel preserved both trabecular and cortical bones with attendant suppression of osteoclast function, besides increasing mineralization. Etel maintained the number of viable osteocytes to the control level, which could also contribute to its beneficial effects on bone. CKD-SHPT rats displayed increased carbonate substitution of matrix and mineral, decreased crystallinity, mineral-to-matrix ratio, and collagen maturity, and these changes were mitigated by Etel. Further, Etel treatment prevented CKD-SHPT-induced deterioration in bone strength and mechanical behavior. Based on these findings, we conclude that in CKD-SHPT rats, Etel has multiscale beneficial effects on bone that involve remodeling suppression, mineralization gene upregulation, and preservation of osteocytes.
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Osso e Ossos , Calcimiméticos , Hiperparatireoidismo Secundário , Peptídeos , Ratos Sprague-Dawley , Insuficiência Renal Crônica , Animais , Hiperparatireoidismo Secundário/tratamento farmacológico , Hiperparatireoidismo Secundário/patologia , Insuficiência Renal Crônica/tratamento farmacológico , Insuficiência Renal Crônica/complicações , Insuficiência Renal Crônica/patologia , Insuficiência Renal Crônica/metabolismo , Osso e Ossos/efeitos dos fármacos , Osso e Ossos/metabolismo , Osso e Ossos/patologia , Peptídeos/farmacologia , Calcimiméticos/farmacologia , Calcimiméticos/uso terapêutico , Ratos , Hormônio Paratireóideo/farmacologia , Masculino , Calcificação Fisiológica/efeitos dos fármacos , Densidade Óssea/efeitos dos fármacosRESUMO
Bacterial contamination in water bodies is a severe scourge that affects human health and causes mortality and morbidity. Researchers continue to develop next-generation materials for controlling bacterial infections from water. Photo-antibacterial activity continues to gain the interest of researchers due to its adequate, rapid, and antibiotic-free process. Photo-antibacterial materials do not have any side effects and have a minimal chance of developing bacterial resistance due to their rapid efficacy. Photocatalytic two-dimensional nanomaterials (2D-NMs) have great potential for the control of bacterial infection due to their exceptional properties, such as high surface area, tunable band gap, specific structure, and tunable surface functional groups. Moreover, the optical and electric properties of 2D-NMs might be tuned by creating heterojunctions or by the doping of metals/carbon/polymers, subsequently enhancing their photo-antibacterial ability. This review article focuses on the synthesis of 2D-NM-based hybrid materials, the effect of dopants in 2D-NMs, and their photo-antibacterial application. We also discuss how we could improve photo-antibacterials by using different strategies and the role of artificial intelligence (AI) in the photocatalyst and in the degradation of pollutants. Finally, we discuss was of improving the photo-antibacterial activity of 2D-NMs, the toxicity mechanism, and their challenges.
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BACKGROUND: Several studies have been conducted on 4-H chromene compounds because of their intriguing pharmacological and biological properties. Various new natural compounds having a chromene foundation have been reported over the past 20 years. OBJECTIVE: In the present study, we reported the acute oral toxicity, antioxidant activity, and molecular docking study of the most active 4H-chromene derivative2-(4-Bromo-phenoxy)-N-[6-chloro-4-(4-chlorophenyl)-3-cyano-4H-chromen-2-yl]-acetamide (A9). METHOD: The acute oral toxicity was carried out as per OECD 423 guidelines. For investigating the antioxidant activity, various biochemical parameters in colon tissue like SOD, CAT, MDA, PC and GSH and also enzyme levels, such as ALT, AST, ALP, and LDH, were measured in this experiment. RESULTS: Acute oral toxicity study indicated that the A9 ligand was found to be safer in animals. Additionally, the A9 ligand had significant antioxidant properties at various doses and was not found to be harmful to the liver. Due to its stronger binding energy and the appropriate interactions that induce inhibition, the A9 ligand's antioxidant function was also validated by additional molecular docking research. CONCLUSION: This compound can be exploited as a lead molecule in further research.
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BACKGROUND: Hydrated strontium perchlorate [Sr(ClO4)2.3H2O] acts as a very strong oxidizing and dehydrating agent. Until now, it could not be reported as a catalyst in dehydration mechanism-based organic synthetic reactions. Therefore, it is important to find whether it could be an effective catalyst for one-pot multicomponent reactions (MCRs). OBJECTIVE: The main objective of the present work is the development of a novel process for the synthesis of 1,4-dihydropyrimidinones through the one-pot multicomponent strategy using hydrated Sr(ClO4)2 as a catalyst. Furthermore, it includes process optimization, stereoselectivity, and spectroscopic characterization of the synthesized compounds. METHODS: Conventional and microwave-supported synthesis of 1,4-dihydropyrimidinones using 20 mol % of hydrated Sr(ClO4)2 catalyst via the one-pot solvent-free reaction was discovered as a new catalytic MCR methodology. The box-Behnken design approach and advanced analytical techniques were used for process optimization and reaction analysis. RESULTS: The results confirmed that hydrated Sr(ClO4)2; works as an efficient catalyst for one-pot multicomponent organic synthesis under both conventional and microwave heating. It is an effective catalyst for laboratory synthesis of 1,4-dihydropyrimidinones stereoselectively with moderate to excellent yield without any undesirable effect. Microwave heating provided the desired product within 1-4 minutes. Moreover, this method provides easy isolation of the pure products simply by recrystallization, and without the use of a chromatographic purification method. CONCLUSION: The simplicity and neutrality of reaction conditions, easy post-reaction workup, higher satisfactory to excellent yield, effectiveness, the diversity of substrates, etc. render the hydrated Sr(ClO4)2 catalyst-based protocol for the stereoselective synthesis of 1,4-dihydropyrimidinones as a highly efficient method. Furthermore, it has been found to be safe un-der laboratory reaction conditions and no undesirable issues have been faced during the process.