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1.
Environ Res ; 252(Pt 3): 118979, 2024 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-38685303

RESUMO

Shark is a seafood commodity that is a good source of minerals and accumulates heavy metals and trace elements through biomagnification, which can pose health risk if taken above the permissible limit. A study was conducted on commonly landed eleven shark species (Scoliodon laticaudus, Rhizopriodon oligolinx, Sphyrna lewini (CR), Carcharhinus macloti, Carcharinus limbatus, Carcharhinus amblyrhynchoides, Carcharhinus sorrah, Carcharinus falciformes(VU), Glaucostegus granulatus, Chiloscyllium arabicum, Loxodon macrorhinus) and analyzed for their heavy metal content, Hazard Index, Total Hazard Quotient, Metal Pollution Index, and also calculated the health risk associated with the consumption. Most of the heavy metals and trace minerals were found to be within the acceptable limit. The Targeted Hazard Quotient (THQ) and the Hazard Index (HI) of all the species except two were less than 1 (HI ≤ 1.0). The Metal Pollution Index (MPI) is showing either no impact or very low contamination. An overall study on hazard identification and health risk characterization in terms of heavy metals shows contamination of some heavy metals in sharks, but there is no potential human health risk associated with consumption.

3.
Cureus ; 15(7): e42216, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37605713

RESUMO

India is native to many tribal communities: Bharia (Madhya Pradesh), Bihl (Rajasthan), Santhal (Bihar, Jharkhand), Bodo (Assam, West Bengal), and many more. They reside in isolated geographical regions, which poses challenges in reaching out to them. In addition, they still have firm beliefs and taboos regarding menstruation. Knowledge about menstrual health and hygiene is one of the most important aspects of tribal health. Therefore, it is important to synthesize the results of menstrual hygiene data from the Indian tribal population. We have calculated the pooled prevalence of sanitary pad use, dustbin disposal, and hygienic reuse of menstrual materials. Online databases, namely PubMed, Cochrane Central, CINAHL, Pan African Journals, EBSCO, and Google Scholar, were searched. After the removal of duplicates, a quality check, and screening of cross-references, 19 articles were selected for final review. Statistical analysis was done by Revman 5.4 and STATA 17.0. A p-value of <0.05 was considered statistically significant. PRISMA guidelines were followed. The protocol registration number was CRD42022331376. This is a non-funded article. The pooled prevalence of sanitary pad use in Indian tribal females was 2% (95% CI 1 to 3). The pooled prevalence of dustbin disposal of menstrual material was 1% (95% CI: 0.00 to 0.02). The pooled prevalence of hygienic reuse of menstrual materials was 1%. Sanitary menstrual hygiene practices are very less prevalent in Indian tribal females. Awareness programs and tribal health policies need to be accelerated for the promotion of menstrual hygiene. Also, literature on the use, disposal, and storage of menstrual adsorbents is scarce in Indian tribes. Health research in this area needs to be emphasized.

4.
Cureus ; 15(3): e36851, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-37123757

RESUMO

Cerebral palsy (CP) is a neurological disorder that affects muscle tone, movement, and motor skills in children. One of the most common symptoms of cerebral palsy is spasticity, which is characterised by involuntary muscle contractions and stiffness. Both botulinum toxin and casting have been used as standalone treatments for spasticity in cerebral palsy, but which is better is still unclear. The aim of the present meta-analysis was to compare the effects on spasticity of serial casting and/or botulinum toxin type A (BoNT-A) in conjunction with or as independent therapies. Studies up to February 2022 were identified in four separate databases. The inclusion criteria were randomised controlled trials (RCTs) that compared different therapies (Botulinum toxin A, or BoNT-A, and casting) and assessed spasticity improvement in children with spastic cerebral palsy who were younger than 18 years old and were published in English. With a 95% confidence interval (CI), the standardised mean difference (SMD) was utilised to calculate treatment effects. The Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) 2020 checklist was followed to undertake the current study. The search for relevant literature in four databases generated 147 results. After the abstract and full-text screening, five publications with a total of 190 cerebral palsy patients were included in this systematic review and meta-analysis. In patients with cerebral palsy, both methods - botulinum toxin and casting- apply globally; our systematic review tries to find out the most effective treatment between the two but does not show any significant difference in these methods. As we know, botulinum toxin is expensive, and the casting method is time-consuming and poorly accepted by patients. There is a need for an excellent study to examine the impact of casting and botulinum toxin type A.

5.
Am J Blood Res ; 13(2): 71-76, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37214645

RESUMO

BACKGROUND: Limited literature was available on the pattern and determinants of mortality among inborn neonates in comparison to the out born ones. The study's goal was to investigate the patterns and risk factors for mortality among hospitalised, on-ventilator inborn and out born neonates. MATERIALS AND METHODS: It was an unmatched, case-control, pilot study conducted between January and December 2020 using information retrieved from the medical records of patients attending the neonatal intensive care unit (NICU) of a tertiary healthcare facility, namely Narayan Medical College & Hospital, situated in eastern India. RESULTS: Congenital pneumonia was the leading cause of death in inborn neonates, with an overall mortality rate of 33.4%. Meanwhile, the overall fatality rate for out born neonates was found to be 43.3%, with birth hypoxia being the most common cause. The only significant attribute affecting mortality in inborn neonates was low arterial blood gas (ABG) pH, whereas in out born neonates they were prematurity, thrombocytopenia, low ABG pO2, and high pCO2. Overall, new-borns with thrombocytopenia, low ABG pO2, and high pCO2 were observed to be at higher risk for mortality compared to others. CONCLUSION: The mortality rate of out born neonates was higher than inborn ones. The attributes affecting mortality were observed to be prematurity, thrombocytopenia, low ABG pH, pO2, and high pCO2.

6.
Sci Rep ; 13(1): 267, 2023 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-36609579

RESUMO

Microwave absorbing materials for high-temperature harsh environments are highly desirable for aerodynamically heated parts and engine combustion induced hot spots of aircrafts. This study reports ceramic composites with excellent and stable high-temperature microwave absorption in air, which are made of polymer-derived SiOC reinforced with core-shell nanophase structure of ZrB2/ZrO2. The fabricated ceramic composites have a crystallized t-ZrO2 interface between ZrB2 and SiOC domains. The ceramic composites exhibit stable dielectric properties, which are relatively insensitive to temperature change from room temperature to 900 °C. The return loss exceeds - 10 dB, especially between 28 and 40 GHz, at the elevated temperatures. The stable high-temperature electromagnetic (EM) absorption properties are attributed to the stable dielectric and electrical properties induced by the core-shell nanophase structure of ZrB2/ZrO2. Crystallized t-ZrO2 serve as nanoscale dielectric interfaces between ZrB2 and SiOC, which are favorable for EM wave introduction for enhancing polarization loss and absorption. Existence of t-ZrO2 interface also changes the temperature-dependent DC conductivity of ZrB2/SiOC ceramic composites when compared to that of ZrB2 and SiOC alone. Experimental results from thermomechanical, jet flow, thermal shock, and water vapor tests demonstrate that the developed ceramic composites have high stability in harsh environments, and can be used as high-temperature wide-band microwave absorbing structural materials.

7.
Curr Neuropharmacol ; 21(7): 1558-1574, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-35950245

RESUMO

Quercetin (Qu), a dietary flavonoid, is obtained from many fruits and vegetables such as coriander, broccoli, capers, asparagus, onion, figs, radish leaves, cranberry, walnuts, and citrus fruits. It has proven its role as a nutraceutical owing to numerous pharmacological effects against various diseases in preclinical studies. Despite these facts, Qu and its nanoparticles are less explored in clinical research as a nutraceutical. The present review covers various neuroprotective actions of Qu against various neurodegenerative diseases (NDs) such as Alzheimer's, Parkinson's, Huntington's, and Amyotrophic lateral sclerosis. A literature search was conducted to systematically review the various mechanistic pathways through which Qu elicits its neuroprotective actions and the challenges associated with raw Qu that compromise therapeutic efficacy. The nanoformulations developed to enhance Qu's therapeutic efficacy are also covered. Various ongoing/completed clinical trials related to Qu in treating various diseases, including NDs, are also tabulated. Despite these many successes, the exploration of research on Qu-loaded nanoformulations is limited mostly to preclinical studies, probably due to poor drug loading and stability of the formulation, time-consuming steps involved in the formulation, and their poor scale-up capacity. Hence, future efforts are required in this area to reach Qu nanoformulations to the clinical level.


Assuntos
Nanopartículas , Doenças Neurodegenerativas , Humanos , Quercetina/uso terapêutico , Quercetina/farmacologia , Doenças Neurodegenerativas/tratamento farmacológico
8.
J Family Med Prim Care ; 12(12): 3409-3411, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38361863

RESUMO

Acute hemorrhagic edema of infancy (AHEI) is a benign and rare presentation of leukocytoclastic vasculitis that usually affects children between 4 months and 24 months of age. It is characterized by purpuric and ecchymotic lesions that mainly involve the distal extremities, the face, and the ears. It usually follows some viral or bacterial infection. Here, we report a case of a 25-month-old male child who presented with mild grade fever and upper respiratory tract infection symptoms. Subsequently, he developed progressive purpuric and ecchymotic lesions over his body, mainly on his lower limbs and face. Laboratory tests were done, showing elevated C-reactive protein and erythrocyte sedimentation rate with rest of normal results. In view of patients having respiratory symptoms, reverse-transcriptase polymerase chain reaction of a nasopharyngeal swab for coronavirus disease 2019 (COVID-19) was done, which came out to be positive. The baby received supportive care only. He gradually improved and was discharged successfully. AHEI may be a possible after effect of COVID-19 infection.

9.
Genes (Basel) ; 13(12)2022 11 24.
Artigo em Inglês | MEDLINE | ID: mdl-36553473

RESUMO

Bipolaris sorokiniana is a fungal pathogen that infects wheat, barley, and other crops, causing spot blotch disease. The disease is most common in humid, warm, wheat-growing regions, with South Asia's Eastern Gangetic Plains serving as a hotspot. There is very little information known about its genetic variability, demography, and divergence period. The current work is the first to study the phylogeographic patterns of B. sorokiniana isolates obtained from various wheat and barley-growing regions throughout the world, with the goal of elucidating the demographic history and estimating divergence times. In this study, 162 ITS sequences, 18 GAPDH sequences, and 74 TEF-1α sequences from B. sorokiniana obtained from the GenBank, including 21 ITS sequences produced in this study, were used to analyse the phylogeographic pattern of distribution and evolution of B. sorokiniana infecting wheat and barley. The degrees of differentiation among B. sorokiniana sequences from eighteen countries imply the presence of a broad and geographically undifferentiated global population. The study provided forty haplotypes. The H_1 haplotype was identified to be the ancestral haplotype, followed by H_29 and H_27, with H_1 occupying a central position in the median-joining network and being shared by several populations from different continents. The phylogeographic patterns of species based on multi-gene analysis, as well as the predominance of a single haplotype, suggested that human-mediated dispersal may have played a significant role in shaping this pathogen's population. According to divergence time analysis, haplogroups began at the Plio/Pleistocene boundary.


Assuntos
Bipolaris , Hordeum , Triticum , Bipolaris/genética , Hordeum/microbiologia , Triticum/microbiologia
10.
Pharmaceutics ; 14(11)2022 Nov 05.
Artigo em Inglês | MEDLINE | ID: mdl-36365203

RESUMO

Present study deciphers development of oral polysaccharide-based colon targeted solid self-nanoemulsifying drug delivery system (S-SNEDDS) of xanthohumol (XH). Several studies have shown that XH has anti-inflammatory and antioxidant properties, suggesting that it could be a good candidate for the treatment of colorectal diseases (CRD). Despite its potential, XH has a low aqueous solubility. As a result, its bioavailability is constrained by the dissolution rate. The liquid (L)-SNEDDS was constituted using Labrafac PG as oil, Tween 80 as surfactant and Transcutol P as co-surfactant. The L-SNEDDS was then adsorbed onto the surface of guar gum and pectin and developed into S-SNEDDS powder. Ternary phase diagram was used to optimize the process of developing L-SNEDDS. The formulation showed mean droplet size of 118.96 ± 5.94 nm and zeta potential of -19.08 ± 0.95 mV and drug loading of 94.20 ± 4.71%. Dissolution studies carried out in medium containing rat caecal contents (RCC) represented the targeted release of S-SNEDDS powder. It was observed that S-SNEDDS showed less than 10% release XH in initial 5 h and rapid release occurred between the 5th and 10th hour. Results of cytotoxicity studies revealed good cytotoxicity of XH loaded S-SNEDDS for Caco2 cells as compared to raw-XH.

11.
Eur J Pharmacol ; 931: 175173, 2022 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-35940236

RESUMO

Advances in biotechnology have led to improving human health with number of novel approaches to mitigate life-threatening diseases such as human immunodeficiency virus (HIV) infection, cancer, and neurodegenerative diseases. In the case of HIV, the damage caused by the retrovirus to the immune system leads to opportunistic infection as well as an elevated risk of autoimmune disease and cancer. Furthermore, clinical symptoms associated with the virus itself may arise. Antiretroviral drug therapy using reverse transcriptase inhibitors, protease inhibitors, fusion inhibitor, chemokine receptor 5 antagonist and integrase strand transfer inhibitors have shown promising results in treating HIV infection and available in market in the form of various dosage forms. However, they are unable to completely cure the disease because of complexity in pathogenesis of HIV. In addition, these drugs have some limitations of poor solubility, permeability or, poor receptor binding capacity. To overcome these drawbacks, many novel drug delivery systems for the drugs belonging to above mentioned categories have been developed. The possibility of treating HIV infection using CRISPR-Cas9 gene editing has been found in 2015. This provided a new area of research to the scientists who are working towards alternative treatment strategies for HIV infections. The present article describes about various treatment strategies used to treat HIV infections with special emphasis on the role of CRISPR/Cas9 gene-based technology. The potential benefits of specific epigenetic modification in the c-c chemokine receptor 5 gene (CCR5) via various delivery methods are also highlighted.


Assuntos
Infecções por HIV , Sistemas CRISPR-Cas/genética , Edição de Genes/métodos , Terapia Genética/métodos , Infecções por HIV/tratamento farmacológico , Infecções por HIV/genética , Humanos , Receptores de Quimiocinas/genética
12.
Biomed Res Int ; 2022: 1659338, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35832856

RESUMO

Diabetic wound (DW) is a secondary application of uncontrolled diabetes and affects about 42.2% of diabetics. If the disease is left untreated/uncontrolled, then it may further lead to amputation of organs. In recent years, huge research has been done in the area of wound dressing to have a better maintenance of DW. These include gauze, films, foams or, hydrocolloid-based dressings as well as polysaccharide- and polymer-based dressings. In recent years, scaffolds have played major role as biomaterial for wound dressing due to its tissue regeneration properties as well as fluid absorption capacity. These are three-dimensional polymeric structures formed from polymers that help in tissue rejuvenation. These offer a large surface area to volume ratio to allow cell adhesion and exudate absorbing capacity and antibacterial properties. They also offer a better retention as well as sustained release of drugs that are directly impregnated to the scaffolds or the ones that are loaded in nanocarriers that are impregnated onto scaffolds. The present review comprehensively describes the pathogenesis of DW, various dressings that are used so far for DW, the limitation of currently used wound dressings, role of scaffolds in topical delivery of drugs, materials used for scaffold fabrication, and application of various polymer-based scaffolds for treating DW.


Assuntos
Diabetes Mellitus , Pé Diabético , Amputação Cirúrgica , Curativos Hidrocoloides , Diabetes Mellitus/terapia , Pé Diabético/terapia , Humanos , Polímeros/uso terapêutico , Cicatrização
13.
Urol Ann ; 14(2): 167-171, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35711480

RESUMO

Objective: The objective was to study the symptomatology of testicular torsion of patients operated in our hospital and their operative results in relation to the duration of symptoms. Materials and Methods: Data of all patients operated for acute scrotum at all ages over a 14 months' time were collected from hospital records. Symptomatology and operative results were studied. Results: Out of 101 consecutive scrotal explorations done in this time, 63.4% of all scrotal explorations were testicular torsion (n = 64). 22.8% were appendage torsion (n = 23) and 13.9% were epididymo-orchitis (n = 14). The peak age of testicular torsion was in the 11-15 years range and the left side is more common (65.6%). Symptoms of scrotal pain (92.2%), abdominal pain (18.8%), nausea/vomiting (18.8%), fever (9.4%), and urinary symptoms (3.1%) were seen in decreasing order of frequency. Among acute scrotum patients who had symptoms of nausea/vomiting or abdominal pain, testicular torsion was found to be significantly higher compared to those who did not have these symptoms (χ2 = 0.044, P < 0.05). In all cases presented within 6 h of symptom onset, testicles were saved and salvage rates reduced with delay in presentation. The testicular salvage rates were 28.1% (18 out of 64 torsions). Patients below 18 years had more chance of going for orchiectomy than others (75% vs 66.7%). Patients who presented after 24 h had a statistically significantly lower salvage rate of 7.7% compared to those who presented within 24 h duration, 52.2%(χ2 = 0.001, P < 0.05). Those with orchiopexy had a median duration of symptom of 6.5 h and the same for orchiectomy patients were 72 h. Our median symptom duration for testicular torsion was 36 h and it is higher than many other countries. Conclusions: Delay in presentation to the health-care facility is the major cause of poor salvage rates in the state and its improvement requires public health interventions and health education.

14.
Environ Sci Pollut Res Int ; 29(33): 50488-50499, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35230633

RESUMO

Fisetin is a polyphenolic flavonoid reported to have antioxidant, anti-inflammatory, and anti-cancer activities. However, it loses its importance as an effective phytochemical due to its poor water solubility and lower bioavailability. In the present study, the self-nanoemulsifying drug delivery system (SNEDDS) of fisetin was developed in order to improve its pharmacological activity. The developed SNEDDS of fisetin was evaluated for improving the rotenone-induced behavioral changes in the rats, and its efficacy was compared with naïve fisetin. It was noticed that fisetin loaded in the SNEDDS formulation significantly (p < 0.001) ameliorated the rotenone-induced alteration in the body weight, grip strength, beam walk, postural instability, etc., in rats when compared to the effect of naïve fisetin. Naïve fisetin significantly (p < 0.05) ameliorated the effect of rotenone on the level of dopamine only at a higher dose. Whereas, SNEDDS of fisetin produced a significant (p < 0.05) effect at both dose levels when compared with the diseased group as well as also produced a significant (p < 0.05) effect when compared with the naïve fisetin group. The results of histopathological examination revealed about the neuroprotective effect of SNEDDS loaded with fisetin as observed through the protection of neuronal damage. From this study, it was concluded that SNEDDS improved the anti-Parkinsonian activity of fisetin by improving the behavioral alteration produced by rotenone due to enhancement in its solubility and bioavailability.


Assuntos
Nanopartículas , Rotenona , Administração Oral , Animais , Disponibilidade Biológica , Emulsões , Flavonóis , Tamanho da Partícula , Ratos , Solubilidade
15.
Chem Biol Interact ; 356: 109869, 2022 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-35231453

RESUMO

Fisetin (FS) is a bioactive flavonoid obtained mostly from apple and strawberry and classified under the category of food supplements due to numerous pharmacological effects against various diseases through multiple mechanistic pathways. It acts as excellent neuroprotective, cardioprotective, anti-invasive, anti-tumorigenic, anti-angiogenic, anticancer, antidiabetics, antioxidant, anti-inflammatory agent. Despite having excellent safety and efficacy profile, FS is very less explored to clinical research either as food supplement or, as therapeutic agent due to its poor aqueous solubility, low bioavailability and reduced blood brain barrier permeability. Multiple mechanistic pathways through which FS elicits its pharmacological actions and the challenges associated with FS that compromises therapeutic efficacy are described in this article. The nanoformulations developed to enhance the bioavailability and therapeutic efficacy of FS are also covered with detailed description of research works carried by various researchers. These include nanoemulsions, liposomes, ethosomes, glycerosomes, polymeric micelles, self-nanoemulsifying drug delivery system and polymeric nanoparticles. Various patents pertaining to extraction/isolation, formula composition and therapeutic uses of FS as well as some clinical studies conducted using FS as active moiety are also enlisted.


Assuntos
Flavonóis , Nanopartículas , Disponibilidade Biológica , Sistemas de Liberação de Medicamentos
16.
Neurotoxicology ; 90: 19-34, 2022 05.
Artigo em Inglês | MEDLINE | ID: mdl-35219781

RESUMO

The current study elucidates pharmacological evaluation of bromelain as a bioactive compound obtain from pineapple stem belongs to family Bromeliaceae in AlCl3 and D - galactose induced mice. In mice, co-administration of AlCl3 at dose 5 mg/kg b.w., via the oral route, and D - galactose at dose 60 mg/kg b.w., via intraperitoneal route for 90 days resulted in cognitive impairment, spatial learning, and memory deficits, as well as neurotoxicity. However, 30 consecutive days, treatments via an intraperitoneal route with bromelain low dose (Brm L) at dose 10 mg/kg b.w., bromelain high dose (Brm H) at dose 20 mg/kg b.w., donepezil (Dnpz) at dose 2 mg/kg b.w., and Brm L + Dnpz at doses 10, 2 mg/kg b.w. were considerably reversed the effect of AlCl3 and D - galactose induced AD mice. Consequences of behavioral parameters (Morris water maze, elevated plus maze and locomotor), biochemical estimation (MDA, GSH, SOD, CAT, Nitrite and AChE), and ELISA tests (mouse BACE, Aß1 - 42, TNF-α, IL-6, and BDNF) confirmed significant (p < 0.05) neuroprotective effect of treatments in AlCl3 and D - galactose induced mice. Additionally, hematoxylin and eosin staining of the cerebral cortex and the hippocampus exposed eosinophilic lesions and hyperchromatic nuclei in AD mice, but these neurodegenerative effects were eliminated by Brm L, Brm H, Dnpz, and Brm L + Dnpz treatments. Thus, bromelain alone and in combination with donepezil prevent AlCl3 and D - galactose induced spatial learning and memory deficits, as well as cognitive impairment, by increasing cholinergic activity and synaptic plasticity, as well as reducing oxidative damage, neuroinflammation, Aß 1-42 aggregations, and histopathological damage, according to our findings. The present study consequences indicate that bromelain alone and in combination with donepezil appears to have neuroprotective properties. Henceforward, this may be a promising treatment option for Alzheimer's disease.


Assuntos
Doença de Alzheimer , Fármacos Neuroprotetores , Cloreto de Alumínio/farmacologia , Cloreto de Alumínio/uso terapêutico , Doença de Alzheimer/induzido quimicamente , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/psicologia , Animais , Bromelaínas/farmacologia , Bromelaínas/uso terapêutico , Modelos Animais de Doenças , Donepezila/farmacologia , Donepezila/uso terapêutico , Galactose/toxicidade , Hipocampo , Aprendizagem em Labirinto , Transtornos da Memória/tratamento farmacológico , Camundongos , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Estresse Oxidativo
17.
Bioorg Med Chem ; 56: 116612, 2022 02 15.
Artigo em Inglês | MEDLINE | ID: mdl-35026631

RESUMO

Continuing on our antiviral drug discovery research, we intended to diversify our lead anti-HIV-1 inhibitor by non-classical isosteric replacement of amide to 1,2,4-oxadiazoles. The resulting molecules isoxazole-1,2,4-oxadiazole analogs were synthesized using mild bases in ethanol under microwave irradiation. The anti-HIV potential was checked in human CD4+ reporter cell lines, TZM-bl and CEM-GFP, at the highest non-cytotoxic concentration (HNC), demonstrating that 3-((3-(p-tolyl)isoxazol-5-yl)methyl)-1,2,4-oxadiazole and 3-((3-(4-chlorophenyl)isoxazol-5-yl)methyl)-1,2,4-oxadiazole inhibit HIV-1 replication significantly and could be considered as a new lead candidate against HIV-1.


Assuntos
Fármacos Anti-HIV/farmacologia , HIV-1/efeitos dos fármacos , Isoxazóis/farmacologia , Oxidiazóis/farmacologia , Fármacos Anti-HIV/síntese química , Fármacos Anti-HIV/química , Linhagem Celular , Relação Dose-Resposta a Droga , Humanos , Isoxazóis/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Oxidiazóis/síntese química , Oxidiazóis/química , Relação Estrutura-Atividade , Replicação Viral/efeitos dos fármacos
18.
Int J Pharm ; 612: 121306, 2022 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-34813906

RESUMO

Liquid self-nanoemulsifying drug delivery system (L-SNEDDS) of curcumin and quercetin were prepared by dissolving them in isotropic mixture of Labrafil M1944CS®, Capmul MCM®, Tween-80® and Transcutol P®. The prepared L-SNEDDS were solidified using Ganoderma lucidum extract, probiotics and Aerosil-200® using spray drying. These were further converted into pellets using extrusion-spheronization. The mean droplet size and zeta potential of L-SNEDDS were found to be 63.46 ± 2.12 nm and - 14.8 ± 3.11 mV while for solid SNEDDS pellets, these were 72.46 ± 2.16 nm and -38.7 ± 1.34 mV, respectively. The dissolution rate for curcumin and quercetin each was enhanced by 4.5 folds while permeability was enhanced by 5.28 folds (curcumin) and 3.35 folds (quercetin) when loaded into SNEDDS pellets. The Cmax for curcumin and quercetin containing SNEDDS pellets was found 532.34 ± 5.64 ng/mL and 4280 ± 65.67 ng/mL, respectively. This was 17.55 and 3.48 folds higher as compared to their naïve forms. About 50.23- and 5.57-folds increase in bioavailability was observed for curcumin and quercetin respectively, upon loading into SNEDDS pellets. SNEDDS pellets were found stable at accelerated storage conditions. The developed formulation was able to normalize the levels of blood glucose, lipids, antioxidant biomarkers, and tissue architecture of pancreas and liver in streptozotocin induced diabetic rats as compared to their naïve forms.


Assuntos
Curcumina , Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Nanopartículas , Probióticos , Reishi , Administração Oral , Animais , Disponibilidade Biológica , Diabetes Mellitus Experimental/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Emulsões , Tamanho da Partícula , Pós/uso terapêutico , Quercetina/uso terapêutico , Ratos , Solubilidade , Estreptozocina
19.
ACS Mater Au ; 2(2): 117-123, 2022 Mar 09.
Artigo em Inglês | MEDLINE | ID: mdl-36855766

RESUMO

Unlike metal-ornamented hybrid material and linear polymers, we invoked the growth of a biodegradable superstructured cross-linked polyamide-ester material. The material is thermally stable. The thiol-alkene photoclicked material acted as an efficient water remediator. The material efficiently monitored amphiphilic dyes like rhodamine B (RHB), methylene blue (MB), and chronic mercuric ions in water. The adsorption kinetics revealed the material could adsorb >95% dyes within 24 h. The RHB-functionalized polymer could sense mercuric ions too. The Density functional theory (DFT) calculation shows a chelated mercury complex with thioether in the polymer, Poly-Am-RhAll, to form a comparatively more stable complex.

20.
Eur J Pharmacol ; 911: 174529, 2021 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-34592305

RESUMO

Myrcene (Myr) has been reported to show neuroprotective effects in cerebral ischemia. In this research work, we investigated the Myr effect on neurobehavioural, and neuropathological alteration in mice induced by Aluminium trichloride (AlCl3) and D - galactose. The administration of AlCl3 (5 mg/kg; p. o.), and D - galactose (60 mg/kg; i. p.) for 90 days in mice resulted in spatial learning and memory deficits, cognitive decline, as well as neurotoxicity. The treatments with Myr low dose (100 mg/kg), Myr high dose (200 mg/kg), donepezil (2 mg/kg), and Myr low dose + donepezil (100 + 2 mg/kg) were administered via intraperitoneal route for 30 days significantly reversed the neurobehavioral, and neuropathological effects of AlCl3 and D - galactose in mice. The results of behavioural tests such as Morris water maze, elevated plus maze, and locomotor; biochemical analysis such as malondialdehyde (MDA), glutathione (GSH), superoxide dismutase (SOD), catalase (CAT), nitrite, and acetylcholinesterase (AChE); and ELISA tests such as mouse ß - secretase (BACE), amyloid-beta peptide1-42 (Aß1 - 42), tumor necrosis factor - α (TNF-α), interleukin - 6 (IL-6), and brain-derived neurotrophic factor (BDNF) demonstrated a significant (p < 0.05) neuroprotective effect of the Myr and donepezil co-treatments. In addition, hematoxylin and eosin staining of the cerebral cortex and hippocampus revealed eosinophilic lesions and hyperchromatic nuclei in Alzheimer's disease mice, but treatments with Myr low dose, Myr high dose, donepezil, and Myr low dose + donepezil reversed these neurodegenerative effects. Myr showed these activities by enhancing synaptic plasticity and cholinergic activity, as well as reducing oxidative damage, neuroinflammation, Aß1-42 aggregations, and histopathological damage. Myr alone and in combination with donepezil may serve as a potential candidate for the treatment of Alzheimer's disease.


Assuntos
Doença de Alzheimer
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