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Alzheimer's Disease (AD) is a progressive neurological disease associated with behavioral abnormalities, memory loss, and cognitive impairment that cause major causes of dementia in the elderly. The pathogenetic processes cause complex effects on brain function and AD progression. The proper protein homeostasis, or proteostasis, is critical for cell health. AD causes the buildup of misfolded proteins, particularly tau and amyloid-beta, to break down proteostasis, such aggregates are toxic to neurons and play a critical role in AD pathogenesis. The rise of cellular senescence is accompanied by aging, marked by irreversible cell cycle arrest and the release of pro-inflammatory proteins. Senescent cell build-up in the brains of AD patients exacerbates neuroinflammation and neuronal degeneration. These cells senescence-associated secretory phenotype (SASP) also disturbs the brain environment. When proteostasis failure and cellular senescence coalesce, a cycle is generated that compounds each other. While senescent cells contribute to proteostasis breakdown through inflammatory and degradative processes, misfolded proteins induce cellular stress and senescence. The principal aspects of the neurodegenerative processes in AD are the interaction of cellular senescence and proteostasis failure. This review explores the interconnected roles of proteostasis disruption and cellular senescence in the pathways leading to neurodegeneration in AD.
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According to findings, long non-coding RNAs (lncRNAs) serves an integral part in growth and development of a variety of human malignancies, including Hepatoblastoma (HB). HB is a rare kind of carcinoma of the liver that mostly affects kids and babies under the age of three. Its manifestations include digestive swelling, abdominal discomfort, and losing weight. This thorough investigation digs into the many roles that lncRNAs serve in HB, giving views into their varied activities as well as possible therapeutic consequences. The function of lncRNAs in HB cell proliferation, apoptosis, migratory and penetrating capacities, epithelial-mesenchymal transition, and therapy tolerance is discussed. Various lncRNA regulatory roles are investigated in depth, yielding information on their effect on essential cell processes such as angiogenesis, apoptosis, immunity, and growth. Circulating lncRNAs are currently acknowledged as potential indications for the initial stages of identification of cancer, with the ability to diagnose as well as forecast. In addition to their diagnostic utility, lncRNAs provide curative opportunities as locations and actors, contributing to the expanding landscape of cancer research. Several HB-linked lncRNAs have been demonstrated to exhibit abnormal expression and are involved in tumor-like characteristics via DNA, RNA, or protein binding or encoding short peptides. As a result, a better knowledge of lncRNA instability might bring fresh perspectives into HB etiology as well as innovative strategies for HB early diagnosis and therapy. We describe the abnormalities of lncRNA expression in HB and their tumor-suppressive or carcinogenic activities during HB carcinogenesis in this study. Furthermore, we explore lncRNAs' diagnostic and therapeutic possibilities in HB.
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Hepatoblastoma , Neoplasias Hepáticas , RNA Longo não Codificante , Hepatoblastoma/genética , Hepatoblastoma/diagnóstico , Hepatoblastoma/patologia , Hepatoblastoma/terapia , Humanos , RNA Longo não Codificante/genética , Neoplasias Hepáticas/genética , Neoplasias Hepáticas/patologia , Neoplasias Hepáticas/diagnóstico , Biomarcadores Tumorais/genética , Regulação Neoplásica da Expressão GênicaRESUMO
Current trends in localized drug delivery are emphasizing the development of dual drug-loaded electrospun nanofibers (NFs) for an improved therapeutic effect on wounds, especially infected skin wounds. The objective of this study was to formulate a new healing therapy for an infected skin wound. To achieve this goal, this study involved the development and characterization of poly(vinyl alcohol) (PVA)/chitosan nanofibers loaded with ciprofloxacin and rutin hydrate. Polymers and drugs were used in different ratios. Nanofiber morphology was studied by scanning electron microscopy, thermal stability by thermogravimetric analysis, structural determination by the X-ray diffraction method, and integrity by Fourier transform infrared spectroscopy. Dissolution studies were performed to check the drug release behavior of the formulations. Antibacterial studies were performed against Staphylococcus aureus and Pseudomonas aeruginosa. The wound healing efficiency of dual drug-loaded nanofibers was measured by a full-thickness excisional wound model of rabbits. The fabricated nanofibers were smooth in morphology. According to FTIR findings, the drugs remained intact in the nanofibers. The results of swelling ratio and porosity revealed that the pore size was increased as the amount of chitosan was increased up to 30% but a further increase in chitosan concentration reduced the swelling ratio and porosity. Drug release studies of nanofibers depicted an initial burst effect and afterward controlled drug release behavior. Drug-loaded nanofibers showed better activity against S. aureus than P. aeruginosa. The antibacterial efficacy of rutin hydrate with ciprofloxacin was improved compared to that of the formulation having rutin hydrate only, likely due to the additive effect in activity. Based on wound healing studies, nanofibrous membranes acted as a promising wound dressing material as compared to the commercial wound healing formulation. Drug-loaded polymeric nanofibers were successfully fabricated by using an electrospinning method. These nanofibers showed an efficient ability to deliver drugs and treat infected wounds.
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Background: Skin wounds affect millions of individuals around the world, and their treatment is expensive. Objective: The purpose of this study was to make neomycin-loaded CG/PVA/PAN (NCPP) nanofibers to improve wound healing. Methods: The NCPP nanofibers were characterized by using thermogravimetric analysis (TGA), scanning electron microscopy (SEM), Fourier transform infrared spectroscopy, and X-ray diffraction. Drug solubility, dissolution, swelling ratio, erosion, and antibacterial studies were performed. The in vivo wound healing study of nanofibers was performed in a rabbit model and was supported by % age wound closure and histopathology. Results: The results of SEM showed some sort of agglomeration on the surface of fibers, while TGA showed 10% more stability for drug-loaded nanofibers. The drug permeation study indicated that the formulation with 15% PVA showed a controlled release profile of the drug. The NCPP nanofibers had an appreciable water retention capability. The NCPP nanofibers showed appreciable antibacterial activity against Enterococcus faecalis (Gram-positive bacteria) and Klebsiella pneumonia (Gram-negative bacteria). The wound healing study showed the better healing properties of NCPP nanofibers within 15 days. Conclusion: The findings helped us to conclude that the NCPP nanofibers were successfully fabricated and found to have a promising role in infected wound healing.
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The genesis of cancer is a precisely organized process in which normal cells undergo genetic alterations that cause the cells to multiply abnormally, colonize, and metastasize to other organs such as the liver, lungs, colon, and brain. Potential drugs that could modify these carcinogenic pathways are the ones that will be used in clinical trials as anti-cancer drugs. Resveratrol (RES) is a polyphenolic natural antitoxin that has been utilized for the treatment of several diseases, owing to its ability to scavenge free radicals, control the expression and activity of antioxidant enzymes, and have effects on inflammation, cancer, aging, diabetes, and cardioprotection. Although RES has a variety of pharmacological uses and shows promising applications in natural medicine, its unpredictable pharmacokinetics compromise its therapeutic efficacy and prevent its use in clinical settings. RES has been encapsulated into various nanocarriers, such as liposomes, polymeric nanoparticles, lipidic nanocarriers, and inorganic nanoparticles, to address these issues. These nanocarriers can modulate drug release, increase bioavailability, and reach therapeutically relevant plasma concentrations. Studies on resveratrol-rich nano-formulations in various cancer types are compiled in the current article. Studies relating to enhanced drug stability, increased therapeutic potential in terms of pharmacokinetics and pharmacodynamics, and reduced toxicity to cells and tissues are the main topics of this research. To keep the readers informed about the current state of resveratrol nano-formulations from an industrial perspective, some recent and significant patent literature has also been provided. Here, the prospects for nano-formulations are briefly discussed, along with machine learning and pharmacometrics methods for resolving resveratrol's pharmacokinetic concerns.
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Mangiferin (MGF), a xanthone derived from Mangifera indica L., initially employed as a nutraceutical, is now being explored extensively for its anticancer potential. Scientists across the globe have explored this bioactive for managing a variety of cancers using validated in vitro and in vivo models. The in vitro anticancer potential of this biomolecule on well-established breast cancer cell lines such as MDA-MB-23, BEAS-2B cells and MCF-7 is closer to many approved synthetic anticancer agents. However, the solubility and bioavailability of this xanthone are the main challenges, and its oral bioavailability is reported to be less than 2%, and its aqueous solubility is also 0.111 mg/mL. Nano-drug delivery systems have attempted to deliver the drugs at the desired site at a desired rate in desired amounts. Many researchers have explored various nanotechnology-based approaches to provide effective and safe delivery of mangiferin for cancer therapy. Nanoparticles were used as carriers to encapsulate mangiferin, protecting it from degradation and facilitating its delivery to cancer cells. They have attempted to enhance the bioavailability, safety and efficacy of this very bioactive using drug delivery approaches. The present review focuses on the origin and structure elucidation of mangiferin and its derivatives and the benefits of this bioactive. The review also offers insight into the delivery-related challenges of mangiferin and its applications in nanosized forms against cancer. The use of a relatively new deep-learning approach to solve the pharmacokinetic issues of this bioactive has also been discussed. The review also critically analyzes the future hope for mangiferin as a therapeutic agent for cancer management.
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The multidrug-resistant (MDR) human immunodeficiency virus 1 (HIV-1) infection is an unmet medical need. HIV-1 capsid plays an important role at different stages of the HIV-1 replication cycle and is an attractive drug target for developing therapies against MDR HIV-1 infection. Lenacapavir (LEN) is the first-in-class HIV-1 capsid inhibitor approved by the USFDA, EMA, and Health Canada for treating MDR HIV-1 infection. This article highlights the development, pharmaceutical aspects, clinical studies, patent literature, and future directions on LEN-based therapies. The literature for this review was collected from PubMed, authentic websites (USFDA, EMA, Health Canada, Gilead, and NIH), and the free patent database (Espacenet, USPTO, and Patent scope). LEN has been developed by Gilead and is marketed as Sunlenca (tablet and subcutaneous injection). The long-acting and patient-compliant LEN demonstrated a low level of drug-related mutations, is active against MDR HIV-1 infection, and does not reveal cross-resistance to other anti-HIV drugs. LEN is also an excellent drug for patients having difficult or limited access to healthcare facilities. The literature has established additive/synergistic effects of combining LEN with rilpivirine, cabotegravir, islatravir, bictegravir, and tenofovir. HIV-1 infection may be accompanied by opportunistic infections such as tuberculosis (TB). The associated diseases make HIV treatment complex and warrant drug interaction studies (drug-drug, drug-food, and drug-disease interaction). Many inventions on different aspects of LEN have been claimed in patent literature. However, there is a great scope for developing more inventions related to the drug combination of LEN with anti-HIV/anti-TB drugs in a single dosage form, new formulations, and methods of treating HIV and TB co-infection. Additional research may provide more LEN-based treatments with favorable pharmacokinetic parameters for MDR HIV-1 infections and associated opportunistic infections such as TB.
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Fármacos Anti-HIV , Infecções por HIV , HIV-1 , Infecções Oportunistas , Tuberculose Resistente a Múltiplos Medicamentos , Tuberculose , Humanos , Fármacos Anti-HIV/farmacologia , Fármacos Anti-HIV/uso terapêutico , Capsídeo , Antituberculosos/uso terapêutico , Infecções por HIV/tratamento farmacológico , Tuberculose Resistente a Múltiplos Medicamentos/tratamento farmacológicoRESUMO
Paroxetine is not suitable for oral administration due to its extensive first-pass metabolism, thus resulting in less bioavailability. This study aimed to prepare novel paroxetine-loaded solid lipid nanoparticles (SLNs) based sustained-release transdermal patches to overcome these problems by enhancing drug absorption and bioavailability. Nine formulations of paroxetine SLNs were prepared by the hot melt-homogenization method using different concentrations of glycerol monostearate (Kolliwax) and Tween 80. Then these prepared SLNs were incorporated in a matrix type transdermal patch having a matrix of ethyl cellulose and polyvinyl pyrrolidone in 3:2 with polyvinyl alcohol. The SLNs showed a particle size range of 113-230 nm and an entrapment efficiency of 85.14%. The SLNs showed sustained paroxetine release (77.86-95.63% release) up to 48 h. FTIR studies showed no interaction between drug and formulation components. Paroxetine is evenly distributed in an amorphous form in SLNs, as demonstrated by DSC as well as PXRD analysis. SLNs formulated patches showed higher drug permeation through the skin than drug-based transdermal patches., Draize patch test revealed no sign of erythema after applying paroxetine-loaded SLN patches (score 0) as observed with the marketed product. The developed SLNs based transdermal patches showed increased permeability and sustained release behaviour.
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Lipossomos , Paroxetina , Paroxetina/farmacologia , Administração Oral , Disponibilidade BiológicaRESUMO
Cyclooxygenase-2 (COX-2) is implicated in the development of chronic inflammatory diseases. Recently, pyridazine derivatives have emerged as a novel prototype to develop COX-2 inhibitors. Accordingly, some pyridazine-based COX-2 inhibitors are reported herein. The reaction of aldehyde 3 and different hydrazines yielded the corresponding hydrazones. The hydrazones were further derivatized to the title compounds, which were assessed for COX-1 and COX-2 inhibitory action, gastric ulcerogenic effects, and lipid peroxidation properties. Molecular docking studies and determination of the physicochemical parameters were also carried out. The allocated structures of the reported compounds were coherent with their spectroscopic data. The compounds 9a (IC50 = 15.50 nM, 114.77%), 9b (IC50 = 17.50 nM, 101.65%), 12 (IC50 = 17.10 nM, 104.03%), 16b (IC50 = 16.90 nM, 105.26%), and 17 (IC50 = 17.70 nM, 100.5%) displayed better COX-2 inhibition than celecoxib (IC50 = 17.79 nM, 100%). These outcomes were harmonious with the molecular docking studies of 9a, 9b, 12, 16b, and 17. These compounds also displayed comparable onset and the duration of action concerning celecoxib and indomethacin in the in vivo studies. No ulcerogenic effects were observed for 9a and 12, whereas 9b, 16b, and 17 showed an insignificant ulcerogenic effect compared to celecoxib. The compounds 9a, 9b, 12, 16b, and 17 displayed a better lipid peroxidation profile than celecoxib and indomethacin. The compounds 9a (%ABS = 84.09), 9b (%ABS = 84.09), 12 (%ABS = 66.87), 16b (%ABS = 75.02), and 17 (%ABS = 81.42) also displayed appreciable calculated absorption compared to celecoxib (%ABS = 82.09). The compounds 9a, 9b, 11, 16b, and 17 have been recognized and postulated as non-ulcerogenic COX-2 inhibitors with promising physicochemical parameters and gastric safety profile. These compounds may be useful candidates to combat diseases caused by higher levels of COX-2.
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Anti-Inflamatórios/farmacologia , Inibidores de Ciclo-Oxigenase 2/farmacologia , Descoberta de Drogas , Piridazinas/farmacologia , Anti-Inflamatórios/química , Antiulcerosos/química , Antiulcerosos/farmacologia , Fenômenos Químicos , Inibidores de Ciclo-Oxigenase 2/química , Relação Dose-Resposta a Droga , Descoberta de Drogas/métodos , Ligação de Hidrogênio , Peroxidação de Lipídeos/efeitos dos fármacos , Modelos Moleculares , Conformação Molecular , Estrutura Molecular , Análise Espectral , Relação Estrutura-AtividadeRESUMO
We have developed a new idea to synthesize a key intermediate molecule by utilizing deep eutectic solvent (DES) and ultrasound in a multistep reaction to ensure process cost-effectiveness. To confirm the stability of reagents with DES, electronic energies were calculated at the B3LYP/6-31+G(d,p) level of theory. DES stabilized the reagents mainly due to strong intermolecular hydrogen bonding. Key intermediate (3) and final compounds (4a-n) were synthesized in a higher yield of 95% and 80%-88%, respectively. Further, final compounds (4a-n) were assessed for their anti-inflammatory, analgesic, ulcerogenic, and lipid peroxidation. The compounds 4f, 4g, 4j, 4l, and 4m showed good anti-inflammatory activity, while 4f, 4i, and 4n exhibited very good analgesic activity as compared to the standard drug. The ulcerogenicity of selected compounds was far less than the indomethacin. The ligands had also shown a good docking score (4f = -6.859 kcal/mol and 4n = -7.077 kcal/mol) as compared to control indomethacin (-6.109 kcal/mol) against the target protein COX-2. These derivatives have the potential to block this enzyme and can be used as NSAID. The state-of-art DFT theory was used to validate the lipid peroxidation mechanism of the active compounds which was in good agreement with the variations of BDEs and IP of the tested compounds.
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Analgésicos , Anti-Inflamatórios não Esteroides , Inibidores de Ciclo-Oxigenase 2 , Ciclo-Oxigenase 2/metabolismo , Indóis , Simulação de Acoplamento Molecular , Analgésicos/síntese química , Analgésicos/química , Analgésicos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Inibidores de Ciclo-Oxigenase 2/síntese química , Inibidores de Ciclo-Oxigenase 2/química , Inibidores de Ciclo-Oxigenase 2/farmacologia , Feminino , Indóis/síntese química , Indóis/química , Indóis/farmacologia , Masculino , Camundongos , Relação Estrutura-Atividade , Ondas UltrassônicasRESUMO
Some novel non-ulcerogenic N-substitutedphenyl-6-oxo-3-phenylpyridazines as COX-2 inhibitors have been developed (Supplementary material Appendix 1). The novel aldehyde 3 was prepared by reacting 6-phenylpyridazin-3(2H)-one with 4-fluorobenzaldehyde. The aldehyde 3 was reacted with different hydrazines and thiazolidin-4-ones to obtain the novel N-substitutedphenyl-6-oxo-3-phenylpyridazine derivatives. These were assessed for their anti-inflammatory potential and gastric ulcerogenic effects. The molecular docking investigations were also undertaken. The spectroscopic data were coherent with the allocated structures of the compounds. The compounds 4a (IC50 = 17.45 nm; p < .05), 4b (IC50 = 17.40 nm; p < .05), 5a (IC50 = 16.76 nm; p < .05), and 10 (IC50 = 17.15 nm; p < .05) displayed better COX-2 inhibitory activity than celecoxib (IC50 = 17.79 nm; p < .05). These findings were consistent with the molecular docking investigations of 4a, 4b, 5a, and 10. The in vivo anti-inflammatory profile of 4a, 4b, 5a, and 10 was also superior to celecoxib and indomethacin. The compounds 4b, 5a, and 10 revealed no gastric ulcerogenic effects, wherein the compound 4a produced almost negligible gastric ulcerogenic effects than celecoxib and indomethacin. The compounds 4a, 4b, 5a, and 10 have been postulated as promising non-ulcerogenic COX-2 inhibitors.
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Inibidores de Ciclo-Oxigenase 2 , Piridazinas , Animais , Celecoxib/efeitos adversos , Celecoxib/uso terapêutico , Ciclo-Oxigenase 1/química , Ciclo-Oxigenase 1/metabolismo , Ciclo-Oxigenase 2/química , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/efeitos adversos , Inibidores de Ciclo-Oxigenase 2/síntese química , Inibidores de Ciclo-Oxigenase 2/química , Inibidores de Ciclo-Oxigenase 2/uso terapêutico , Edema/tratamento farmacológico , Feminino , Indometacina/efeitos adversos , Indometacina/uso terapêutico , Masculino , Simulação de Acoplamento Molecular , Estrutura Molecular , Piridazinas/efeitos adversos , Piridazinas/síntese química , Piridazinas/química , Piridazinas/uso terapêutico , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Relação Estrutura-AtividadeRESUMO
The purpose of this study was to fabricate a triple-component nanocomposite system consisting of chitosan, polyethylene glycol (PEG), and drug for assessing the application of chitosan-PEG nanocomposites in drug delivery and also to assess the effect of different molecular weights of PEG on nanocomposite characteristics. The casting/solvent evaporation method was used to prepare chitosan-PEG nanocomposite films incorporating piroxicam-ß-cyclodextrin. In order to characterize the morphology and structure of nanocomposites, X-ray diffraction technique, scanning electron microscopy, thermogravimetric analysis, and Fourier transmission infrared spectroscopy were used. Drug content uniformity test, swelling studies, water content, erosion studies, dissolution studies, and anti-inflammatory activity were also performed. The permeation studies across rat skin were also performed on nanocomposite films using Franz diffusion cell. The release behavior of films was found to be sensitive to pH and ionic strength of release medium. The maximum swelling ratio and water content was found in HCl buffer pH 1.2 as compared to acetate buffer of pH 4.5 and phosphate buffer pH 7.4. The release rate constants obtained from kinetic modeling and flux values of ex vivo permeation studies showed that release of piroxicam-ß-cyclodextrin increased with an increase in concentration of PEG. The formulation F10 containing 75% concentration of PEG showed the highest swelling ratio (3.42±0.02) in HCl buffer pH 1.2, water content (47.89±1.53%) in HCl buffer pH 1.2, maximum cumulative drug permeation through rat skin (2405.15±10.97 µg/cm2) in phosphate buffer pH 7.4, and in vitro drug release (35.51±0.26%) in sequential pH change mediums, and showed a significantly (p<0.0001) higher anti-inflammatory effect (0.4 cm). It can be concluded from the results that film composition had a particular impact on drug release properties. The different molecular weights of PEG have a strong influence on swelling, drug release, and permeation rate. The developed films can act as successful drug delivery approach for localized drug delivery through the skin.
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Sistemas de Liberação de Medicamentos/instrumentação , Nanocompostos/química , Administração Cutânea , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Masculino , Microscopia Eletrônica de Varredura , Piroxicam/administração & dosagem , Piroxicam/química , Polietilenoglicóis/química , Ratos , Ratos Sprague-Dawley , Difração de Raios X , beta-Ciclodextrinas/administração & dosagem , beta-Ciclodextrinas/químicaRESUMO
Several pathologies such as neurodegeneration and cancer are associated with aging, which is affected by many genetic and environmental factors. Healthy aging conceives human longevity, possibly due to carrying the defensive genes. For instance, FOXO (forkhead box O) genes determine human longevity. FOXO transcription factors are involved in the regulation of longevity phenomenon via insulin and insulin-like growth factor signaling. Only one FOXO gene (FOXO DAF-16) exists in invertebrates, while four FOXO genes, that is, FOXO1, FOXO3, FOXO4, and FOXO6 are found in mammals. These four transcription factors are involved in the multiple cellular pathways, which regulate growth, stress resistance, metabolism, cellular differentiation, and apoptosis in mammals. However, the accurate mode of longevity by FOXO factors is unclear until now. This article describes briefly the existing knowledge that is related to the role of FOXO factors in human longevity.
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Fatores de Transcrição Forkhead/metabolismo , Longevidade/genética , Humanos , Estresse Oxidativo , Fosforilação , Transdução de SinaisRESUMO
The objective of this study was to evaluate the anthelmintic, antimicrobial and antioxidant activities of Chenopodium album against gastrointestinal nematodes of sheep and some pathogenic microbes. A worm motility inhibition assay was used for in vitro study, and a faecal egg count reduction assay was used for an in vivo study. Various concentrations ranging from 100 to 500 µg/ml of the extract were subjected to antimicrobial screening by disc diffusion method against four selected bacterial (Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas multocida and Escherichia coli) and two fungal (Aspergillus flavus and Candida albicans) strains in order to estimate the medicinal potential of the herb. DPPH (1,1-diphenyl-2-picrylhydrazyl), riboflavin photo-oxidation, deoxyribose, lipid peroxidation assays were used for antioxidant activity. The extracts exhibited dose- and time-dependent anthelmintic effects on the Haemonchus contortus as compared to levamisole. The extract showed maximum inhibitory effect against S. aureus (28 ± 0.14 mm), while as mild inhibitory effect was observed against E. coli among the selected microbial strains. The effect produced by the different extract concentrations was comparable with the standard antibacterial agent streptomycin sulphate and antifungal agent nystatin, which were used as effective positive control in the study. The antioxidant activity showed that the extracts exhibited scavenging effect in concentration-dependent manner on superoxide anion radicals and hydroxyl radicals leading to the conclusion that the plant has broad spectrum anthelmintic, antimicrobial and antioxidant activities and could be a potential alternative for treating various diseases.
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Anti-Helmínticos/farmacologia , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Chenopodium album/química , Extratos Vegetais/farmacologia , Animais , Antioxidantes/química , Bactérias/efeitos dos fármacos , Compostos de Bifenilo , Fungos/efeitos dos fármacos , Haemonchus/efeitos dos fármacos , Levamisol/farmacologia , Picratos , Extratos Vegetais/químicaRESUMO
Over the past few years, considerable attention has been focused on carrageenan based bionanocomposites due to their multifaceted properties like biodegradability, biocompatibility, and nontoxicity. Moreover, these composites can be tailored according to the desired purpose by using different nanofillers. The role of ferromagnetic nanoparticles in drug delivery is also discussed here in detail. Moreover, this article also presents a short review of recent research on the different types of the carrageenan based bionanocomposites and applications.
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Carragenina/química , Sistemas de Liberação de Medicamentos/métodos , Imãs/química , Nanocompostos/química , Nanopartículas/química , Liberação Controlada de FármacosRESUMO
The present study is focused on the assessment of the medicinal therapeutic potential extracts of H. rosea to investigate their pharmacological implications based upon science proofs. The antioxidant activity of fraction of H. rosea, namely, n-hexane (HR-1), ethyl acetate (HR-2), chloroform (HR-3), and n-butanol (HR-4), was performed by using the DPPH radical scavenging method. The cytotoxicity and enzyme inhibition assessment were also performed. All the extracts showed significant antioxidant, antibacterial, and protein kinase inhibition but none of the extracts exhibited α-amylase inhibition activity. The chloroform extract HR-3 may block a kinase receptor from binding to ATP; the lead molecule will be isolated, which may stop cancerous cell growth and demotion of cell division. It is predicted that ethyl acetate, chloroform, and n-butanol extracts of H. rosea contain polyphenolics, flavonoids, and alkaloids that are biologically effective candidates exhibiting significant cytotoxicity, antioxidant, and antimicrobial activities. They may control oxidative damage in the body tissues and act as potential antidiabetic and anticancer agents. These studies will also be helpful for future drug designing and drug development research.
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Antibacterianos , Antioxidantes , Inibidores Enzimáticos , Oenothera/química , Extratos Vegetais , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Antibacterianos/toxicidade , Antioxidantes/química , Antioxidantes/farmacologia , Antioxidantes/toxicidade , Artemia/efeitos dos fármacos , Bactérias/efeitos dos fármacos , Compostos de Bifenilo , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/toxicidade , Testes de Sensibilidade Microbiana , Picratos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , alfa-Amilases/antagonistas & inibidoresRESUMO
The aim of present study was to enhance topical permeation of clotrimazole gel preparation by using various permeability enhancers such as coconut oil, pistachio oil and sodium lauryl sulphate (SLS). Clotrimazole gel preparations were prepared and optimized by using three factor, five level central composite design. A second-order polynomial equation was generated in order to estimate the effect of independent variables i.e. coconut oil (X1), pistachio oil (X2) and sodium lauryl sulphate (X3) at various dependent variables i.e. flux (Y1), lag time (Y2), diffusion coefficient (Y3), permeability coefficient (Y4), and input rate (Y5) of clotrimazole gel formulations. Ex vivo skin permeation study was performed through rat skin by using modified Franz diffusion cell system. Optimized formulation F8 exhibited highest flux 2.17 µg/cm2/min, permeability coefficient 0.0019 cm/min and input rate 1.543 µg/cm2/min, along with moderate lag time 77.27 min and diffusion coefficient 0.063 cm2/min, which is further supported by anti-fungal activity that exhibited more prominent zone of inhibition against Candida albicans, Aspergillus niger and Mucor. Thus, it can be concluded that permeation of clotrimazole gel was enhanced by various combination of coconut oil, pistachio oil and sodium lauryl sulphate but optimized formulation F8 containing 0.4 ml pistachio oil, 0.8 ml coconut oil and 0.04 g of SLS exhibited more pronounced and promising effect through rat skin.
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Acrilatos , Clotrimazol/síntese química , Administração Tópica , Animais , Clotrimazol/administração & dosagem , Clotrimazol/farmacocinética , Óleo de Coco/farmacologia , Composição de Medicamentos/métodos , Géis , Técnicas In Vitro , Pistacia/química , Óleos de Plantas/farmacologia , Ratos , Absorção Cutânea , Dodecilsulfato de Sódio/farmacologiaRESUMO
One year crossectional survey was carried out to determine and describe the prevalence and intensity of gastrointestinal parasite infections in hangul (Cervus elaphus hanglu) in Dachigam National Park of Kashmir through faecal examinations. Out of 153 faecal samples examined, 82 (53.59 %) were found infected with GIT helminthes. In present study seven helminth species were found, including five nematode [Haemonchus contortus (55.39 %), Trichuris ovis (39.75 %), Dictyocaulus viviparus (28.4.00 %), Oesophogostomum circumcincta (13.7 %) and Chabertia ovina (4.02 %)] one trematode [Fasciola hepatica (17.3 %)] and one cestode species [Moneizia expansa (6.05 %)]. Based on the severity of infection 81.7 % of hangul positive samples were severely infected (epg > 1,500), 8.3 % heavily infected (epg = 1,100-1,500), 3.8 % moderately infected (epg = 800-1,000) and 7.2 % mildly infected (epg = 500). Season, sex and age were the factors that influenced the epidemiological prevalence of GIT helminths in hangul in the present study. The maximum helminth infection was observed in summer season and lowest in winter (P = 0.003). Lower age groups were more infected than adult animals (P > 0.05). Prevalence was higher in males than females (P > 0.05). The present study will initially be of great significance to add to existing knowledge of the epidemiology of GIT helminth of hangul which is the pioneering study on this animal in the valley and the findings will be quite helpful to devise the appropriate control and prophylactic strategies for GIT helminthiasis of hangul in the Dachigam national park.
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Protocatechuic acid (3,4-dihydroxybenzoic acid, PCA) is a simple phenolic acid. It is found in a large variety of edible plants and possesses various pharmacological activities. This article aims to review the modern trends in phytochemical isolation and extraction of PCA from plants and other natural resources. Moreover, this article also encompasses pharmacological and biological activities of PCA. It is well known to have anti-inflammatory, antioxidant, anti-hyperglycemia, antibacterial, anticancer, anti-ageing, anti-athro- genic, anti-tumoral, anti-asthma, antiulcer, antispasmodic and neurological properties.
Assuntos
Hidroxibenzoatos/farmacologia , Envelhecimento/efeitos dos fármacos , Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Hidroxibenzoatos/isolamento & purificação , Fármacos Neuroprotetores/farmacologia , Cebolas/químicaRESUMO
The exposure to ultraviolet radiations (UVR) is the key source of skin sunburn; it may produce harmful entities, reactive oxygen species (ROS), leading to aging. The skin can be treated and protected from the injurious effects of ROS by using various pharmaceutical formulations, such as cream. Cream can be loaded with antioxidants to quench ROS leading to photo-protective effects. Moreover, modern medicines depend on ethnobotanicals for protection or treatment of human diseases. This review article summarizes various in vivo antioxidant studies on herbal creams loaded with phyto-extracts. These formulations may serve as cosmeceuticals to protect skin against injurious effects of UVR. The botanicals studied for dermatologic use in cream form include Acacia nilotica, Benincasa hispida, Calendula officinalis, Camellia sinensis, Camellia sinensis, Nelumbo nucifera, Capparis decidua, Castanea sativa, Coffea arabica, Crocus sativus, Emblica officinalis Gaertn, Foeniculum vulgare, Hippophae rhamnoides, Lithospermum erythrorhizon, Malus domestica, Matricaria chamomilla L., Moringa oleifera, Morus alba, Ocimum basilicum, Oryza sativa, Polygonum minus, Punica granatum, Silybum marianum, Tagetes erecta Linn., Terminalia chebula, Trigonella foenum-graecum, and Vitis vinifera. The observed anti-aging effects of cream formulations could be an outcome of a coordinating action of multiple constituents. Of numerous botanicals, the phenolic acids and flavonoids appear effective against UVR-induced damage; however the evidence-based studies for their anti-aging effects are still needed.