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BACKGROUND: Mefenamic acid (MFA), a common analgesic, causes central nervous system (CNS) toxicity at high doses with a proposed activity on the Gamma-aminobutyric acid (GABA) system. However, it remains unknown whether flumazenil (FMZ), a GABA type A receptor (GABAAR) antagonist, can reverse MFA toxicity. METHODS: The behavioral and neurophysiological effects of MFA were investigated in mice with and without FMZ pre-treatment. The elevated zero maze (EZM) and marble burying tests were used to assess anxiety-like behaviors and burying activities, respectively. The standard bar test was used to evaluate catalepsy, while the actophotometer test was used to measure locomotor activity. Seizure intensity was scored, and fatalities were counted. RESULTS: Without FMZ pre-treatment, MFA induced behavioral and neurophysiological effects in a dose-dependent manner as follows: At a dose of 20 mg/kg, i.p, MFA-treated mice exhibited anxiety-like behaviors, which was determined by a significant increase in the time spent in the closed areas and a significant decrease in the number of entries to the open areas of the EZM apparatus. These mice also showed a significant decrease in the burying activity, manifested as a significant decrease in the number of buried marbles. At 40 mg/kg, i.p., MFA-treated mice showed catalepsy that was associated with a significant decrease in locomotor activity. At a dose of 80 mg/kg, i.p., mice developed fatal tonic-clonic seizures (seizure score = 4). Pre-treatment with FMZ (5 mg/kg, i.p.) significantly reversed the anxiety-like behaviors and restored marble-burying activity. Additionally, FMZ prevented catalepsy, significantly restored locomotor activity, reduced seizure intensity (seizure score = 0.3) and significantly reduced mortalities. CONCLUSIONS: The present study's findings indicate that activation of the GABAAR is involved in the CNS toxicity of MFA, and FMZ reverses MFA toxicity by interfering with this receptor.
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Flumazenil , Ácido Mefenámico , Ratones , Animales , Flumazenil/efectos adversos , Ácido Mefenámico/efectos adversos , Receptores de GABA-A , Catalepsia , Sistema Nervioso Central , Convulsiones/inducido químicamente , Convulsiones/tratamiento farmacológico , Ácido gamma-Aminobutírico/efectos adversos , Conducta AnimalRESUMEN
Although people with human leukocyte antigens (HLA) DQ2 and/or DQ8 are more likely to develop celiac disease (CD), the condition cannot be fully explained by this genetic predisposition alone. Multiple, as yet unidentified, factors contribute to the genesis of CD, including genetics, the environment, and the immune system. In order to provide insight into a prospective possibility and an expanded screening technique, we aim to undertake a comprehensive and meta-analytical study of the assessment and distribution of HLA class II (HLA-DQ2/DQ8) in adult CD patients. A systematic review was conducted using an electronic search of databases (PubMed, Google Scholar, Embase, and Direct Science) from January 2004 to February 2022. DQ2/DQ2 homozygotes have the highest risk of developing CD. DQ2/DQ8 typing is an effective test to exclude CD from the differential diagnosis of a patient with CD symptoms. Although other non-HLA genes have been associated with CD, they are rarely considered at diagnosis because they account for only a small proportion of the heritability of CD. This finding, together with the information gathered previously, may be useful in considering widely available and economically feasible screening options for celiac disease in young people.
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Enfermedad Celíaca , Humanos , Adulto , Adolescente , Enfermedad Celíaca/diagnóstico , Estudios Prospectivos , Predisposición Genética a la EnfermedadRESUMEN
Mentha longifolia is a valuable medicinal and aromatic plant that belongs to Lamiaceae family. This study looked at the antibacterial effects of M. longifolia essential oil and pulegone in edible coatings made of chitosan and alginate on the growth of Staphylococcus aureus, Listeria monocytogenes, and Escherichia coli in cheese. For this purpose, first fresh mint plant was collected from the cold region of Jiroft in Kerman province. Plant samples were dried in the shade at ambient temperature, and essential oil was prepared using Clevenger. The essential oil was analyzed by gas chromatography using mass spectrometric (GC/MS) detection. The major composition of M. longifolia oil was pulegone (26.07%), piperitone oxide (19.72%), and piperitone (11.88%). The results showed that adding M. longifolia essential oils and pulegone to edible coatings significantly reduced the growth of bacteria during storage. The bacterial population decreased by increasing the concentration of chitosan, M. longifolia, and pulegone in edible coatings. When the effects of pulegone and M. longifolia essential oils on bacteria were compared, it was found that pulegone had a stronger effect on bacterial population reduction. Coating treatments showed more antibacterial activity on E. coli than other bacteria. In general, the results of this research showed that alginate and chitosan coatings along with M. longifolia essential oil and its active ingredient pulegone had antibacterial effects against S. aureus, L. monocytogenes, and E. coli in cheese.
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Queso , Quitosano , Películas Comestibles , Mentha , Aceites Volátiles , Aceites Volátiles/química , Mentha/química , Quitosano/farmacología , Monoterpenos/química , Alginatos/farmacología , Staphylococcus aureus , Escherichia coli , Queso/análisis , Bacterias , Antibacterianos/farmacología , Antibacterianos/análisisRESUMEN
Retama monosperma L. (Boiss.) or Genista monosperma L. (Lam.), known locally as "R'tam", is a spontaneous and annual herb that belongs to the Fabaceae family. It is native to the Mediterranean regions, specifically in the desert areas and across the Middle Atlas in Morocco. This plant has been extensively used in folk medicine and it is rich in bioactive compounds, including polyphenols, flavonoids, and alkaloids. Current research efforts are focusing on the development of novel natural drugs as alternatives to various organic and non-organic chemical products from Retama monosperma. In addition, extract, and isolated compounds obtained from different parts of the chosen plant have been described to exhibit multiple biological and pharmacological properties such as antioxidant, anti-aging, anti-inflammatory, antihypertensive, anti-helminthic, disinfectant, diuretic, and hypoglycemic effects. The plant-derived extract also acts as an antimicrobial agent, which is highly efficient in the treatment of bacterial, viral, and fungal infections. Its antiproliferative effects are associated with some mechanisms, such as the inhibition of cell cycle arrest and apoptosis. In light of these assessments, we critically highlight the beneficial effects of the flowers, stems, seeds extracts, and isolated compounds from R. monosperma (L.) Boiss in human health care, industrial, and other applications, as well as the possible ways to be employed as a potential natural source for future drug discovery.
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Fabaceae , Genista , Humanos , Fabaceae/química , Extractos Vegetales/química , Apoptosis , Polifenoles/farmacologíaRESUMEN
Exposure to water-pipe smoking, whether flavored or unflavored, has been shown to instigate inflammation and oxidative stress in BALB/c mice. This consequently results in alterations in the expression of inflammatory markers and antioxidant genes. This study aimed to scrutinize the impact of Epigallocatechin gallate (EGCG)-a key active component of green tea-on inflammation and oxidative stress in BALB/c mice exposed to water-pipe smoke. The experimental setup included a control group, a flavored water-pipe smoke (FWP) group, an unflavored water-pipe smoke (UFWP) group, and EGCG-treated flavored and unflavored groups (FWP + EGCG and UFWP + EGCG). Expression levels of IL-6, IL1B, TNF-α, CAT, GPXI, MT-I, MT-II, SOD-I, SOD-II, and SOD-III were evaluated in lung, liver, and kidney tissues. Histopathological changes were also assessed. The findings revealed that the EGCG-treated groups manifested a significant decline in the expression of inflammatory markers and antioxidant genes compared to the FWP and UFWP groups. This insinuates that EGCG holds the capacity to alleviate the damaging effects of water-pipe smoke-induced inflammation and oxidative stress. Moreover, enhancements in histopathological features were observed in the EGCG-treated groups, signifying a protective effect against tissue damage induced by water-pipe smoking. These results underscore the potential of EGCG as a protective agent against the adverse effects of water-pipe smoking. By curbing inflammation and oxidative stress, EGCG may aid in the prevention or mitigation of smoking-associated diseases.
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Catequina , Fumar en Pipa de Agua , Ratones , Animales , Antioxidantes/farmacología , Antioxidantes/metabolismo , Estrés Oxidativo , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Catequina/farmacología , Expresión Génica , Superóxido Dismutasa/metabolismoRESUMEN
Cedrus atlantica (Endl.) Manetti ex Carriere is an endemic tree possessing valuable health benefits which has been widely used since time immemorial in international traditional pharmacopoeia. The aim of this exploratory investigation is to determine the volatile compounds of C. atlantica essential oils (CAEOs) and to examine their in vitro antimicrobial, antioxidant, anti-inflammatory, and dermatoprotective properties. In silico simulations, including molecular docking and pharmacokinetics absorption, distribution, metabolism, excretion, and toxicity (ADMET), and drug-likeness prediction were used to reveal the processes underlying in vitro biological properties. Gas chromatography-mass spectrophotometry (GC-MS) was used for the chemical screening of CAEO. The antioxidant activity of CAEO was investigated using four in vitro complementary techniques, including ABTS and DPPH radicals scavenging activity, ferric reductive power, and inhibition of lipid peroxidation (ß-carotene test). Lipoxygenase (5-LOX) inhibition and tyrosinase inhibitory assays were used for testing the anti-inflammatory and dermatoprotective properties. GC-MS analysis indicated that the main components of CAEO are ß-himachalene (28.99%), α-himachalene (14.43%), and longifolene (12.2%). An in vitro antimicrobial activity of CAEO was examined against eleven strains of Gram-positive bacteria (three strains), Gram-negative bacteria (four strains), and fungi (four strains). The results demonstrated high antibacterial and antifungal activity against ten of them (>15 mm zone of inhibition) using the disc-diffusion assay. The microdilution test showed that the lowest values of MIC and MBC were recorded with the Gram-positive bacteria in particular, which ranged from 0.0625 to 0.25 % v/v for MIC and from 0.5 to 0.125 % v/v for MBC. The MIC and MFC of the fungal strains ranged from 0.5 to 4.0% (MIC) and 0.5 to 8.0% v/v (MFC). According to the MBC/MIC and MFC/MIC ratios, CAEO has bactericidal and fungicidal activity. The results of the in vitro antioxidant assays revealed that CAEO possesses remarkable antioxidant activity. The inhibitory effects on 5-LOX and tyrosinase enzymes was also significant (p < 0.05). ADMET investigation suggests that the main compounds of CAEO possess favorable pharmacokinetic properties. These findings provide scientific validation of the traditional uses of this plant and suggest its potential application as natural drugs.
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Antiinfecciosos , Aceites Volátiles , Aceites Volátiles/química , Antioxidantes/química , Cedrus , Monofenol Monooxigenasa/farmacología , Simulación del Acoplamiento Molecular , Pruebas de Sensibilidad Microbiana , Antiinfecciosos/farmacología , Antibacterianos/farmacología , Hongos , Bacterias Grampositivas , Antiinflamatorios/farmacologíaRESUMEN
This study aimed to determine the chemical composition of the essential oils (EOs) of Ocimum basilicum L., as well as to evaluate the antibacterial, antidiabetic, dermatoprotective, and anti-inflammatory properties, and the EOs and aqueous extracts of O. basilicum. The antibacterial activity was evaluated against bacterial strains, Gram-positive and Gram-negative, using the well diffusion and microdilution methods, whereas the antidiabetic activity was assessed in vitro using two enzymes involved in carbohydrate digestion, α-amylase and α-glucosidase. On the other hand, the dermatoprotective and anti-inflammatory activities were studied by testing tyrosinase and lipoxygenase inhibition activity, respectively. The results showed that the chemical composition of O. basilicum EO (OBEO) is dominated by methyl chavicol (86%) and trans-anethol (8%). OBEO exhibited significant antibacterial effects against Gram-negative and Gram-positive strains, demonstrated by considerable diameters of the inhibition zones and lower MIC and MBC values. In addition, OBEO exhibited significant inhibition of α-amylase (IC50 = 50.51 ± 0.32 µg/mL) and α-glucosidase (IC50 = 39.84 ± 1.2 µg/mL). Concerning the anti-inflammatory activity, OBEO significantly inhibited lipoxygenase activity (IC50 = 18.28 ± 0.03 µg/mL) compared to the aqueous extract (IC50 = 24.8 ± 0.01 µg/mL). Moreover, tyrosinase was considerably inhibited by OBEO (IC50 = 68.58 ± 0.03 µg/mL) compared to the aqueous extract (IC50 = 118.37 ± 0.05 µg/mL). The toxicological investigations revealed the safety of O. basilicum in acute and chronic toxicity. The finding of in silico analysis showed that methyl chavicol and trans-anethole (main compounds of OBEO) validate the pharmacokinetics of these compounds and decipher some antibacterial targets.
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Ocimum basilicum , Aceites Volátiles , Ocimum basilicum/química , Monofenol Monooxigenasa , alfa-Glucosidasas , Aceites Volátiles/farmacología , Aceites Volátiles/química , Antibacterianos/farmacología , Antiinflamatorios/farmacología , LipooxigenasasRESUMEN
INTRODUCTION: There is a paramount need for moral development for pharmacists and pharmacy students to practice the patient-centered profession. We aimed to explore the current situational judgment utilizing ethical reasoning among undergraduate pharmacy students. METHODS: A set of ten ethical dilemmas, representing potential real-life situations that the students come across in the university and may face in the future as a pharmacist were developed by a team of students, academic staff, and stakeholders. These ethical dilemmas were validated, checked for accuracy, and piloted. An online questionnaire was created consisting of these ten scenarios as open-ended questions and administered to fourth year and fifth year PharmD students in a public university located at the city of Mecca, Saudi Arabia, asking them how they would react in that situation. Responses of the participants were analyzed using thematic analysis independently by four researchers and inter-rater agreement were achieved through consensus. RESULTS: Out of 205, 186 students completed the questionnaire with a response rate of 90.7%. Analysis and resulted in the generation of 32 codes, which were then categorized into seven overarching themes: student engagement, social and professional responsibility, academic integrity, legal obligation, moral obligation, signposting, and moral engagement and patient safety. CONCLUSIONS: Undergraduate pharmacy students experience complex state of mind in connection with ethical reasoning. The participants' situational judgment were driven by cultural norm, authority, and responsibility. Student engagement is also affected by the state of mind and feelings of mutual trust, perceived cultural influence and peer pressure. The students were prone to seek help from university administrators or teachers when faced with situations in which they were helpless.
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Estudiantes de Farmacia , Humanos , Juicio , Farmacéuticos , Solución de Problemas , Arabia SauditaRESUMEN
Atherosclerosis is one of the main underlying causes of cardiovascular diseases (CVD). It is associated with chronic inflammation and intimal thickening as well as the involvement of multiple cell types including immune cells. The engagement of innate or adaptive immune response has either athero-protective or atherogenic properties in exacerbating or alleviating atherosclerosis. In atherosclerosis, the mechanism of action of immune cells, particularly monocytes, macrophages, dendritic cells, and B- and T-lymphocytes have been discussed. Immuno-senescence is associated with aging, viral infections, genetic predispositions, and hyperlipidemia, which contribute to atherosclerosis. Immune senescent cells secrete SASP that delays or accelerates atherosclerosis plaque growth and associated pathologies such as aneurysms and coronary artery disease. Senescent cells undergo cell cycle arrest, morphological changes, and phenotypic changes in terms of their abundances and secretome profile including cytokines, chemokines, matrix metalloproteases (MMPs) and Toll-like receptors (TLRs) expressions. The senescence markers are used in therapeutics and currently, senolytics represent one of the emerging treatments where specific targets and clearance of senescent cells are being considered as therapy targets for the prevention or treatment of atherosclerosis.
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Aterosclerosis , Senescencia Celular , Humanos , Senescencia Celular/genética , Envejecimiento/metabolismo , Citocinas/metabolismo , Inflamación/patologíaRESUMEN
2-(4-Chlorophenyl)-5-benzoxazoleacetic acid (CBA) and its ester, methyl-2-(4-chloro-phenyl)-5-benzoxazoleacetate (MCBA), were synthesized, and their structures were confirmed by 1HNMR, IR, and mass spectrophotometry. The anti-psoriatic activities of CBA and MCBA were tested using an imiquimod (IMQ)-induced psoriatic mouse model, in which mice were treated both topically (1% w/w) and orally (125 mg/kg) for 14 days. The erythema intensity, thickness, and desquamation of psoriasis were scored by calculating the psoriasis area severity index (PASI). The study also included the determination of histopathological alterations in the skin tissues of treated mice. Topical and oral administration of CBA and MCBA led to a reduction in erythema intensity, thickness, and desquamation, which was demonstrated by a significant decrease in the PASI value. In addition, skin tissues of mice treated with CBA and MCBA showed less evidence of psoriatic alterations, such as hyperkeratosis, parakeratosis, scale crust, edema, psoriasiform, and hyperplasia. After administration of either topical or oral dosing, the anti-psoriatic effects were found to be stronger in MCBA-treated than in CBA-treated mice. These effects were comparable to those produced by Clobetasol propionate, the reference drug. This drug discovery could be translated into a potential new drug for future clinical use in psoriasis treatment.
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Benzoxazoles , Psoriasis , Animales , Benzoxazoles/farmacología , Benzoxazoles/uso terapéutico , Modelos Animales de Enfermedad , Imiquimod/efectos adversos , Ratones , Ratones Endogámicos CBA , Preparaciones Farmacéuticas , Psoriasis/inducido químicamente , PielRESUMEN
The present study investigated and compared the quality and chemical composition of Moroccan walnut (Juglans regia L.) oil. This study used three extraction techniques: cold pressing (CP), soxhlet extraction (SE), and ultrasonic extraction (UE). The findings showed that soxhlet extraction gave a significantly higher oil yield compared to the other techniques used in this work (65.10% with p < 0.05), while cold pressing and ultrasonic extraction gave similar yields: 54.51% and 56.66%, respectively (p > 0.05). Chemical composition analysis was carried out by GC−MS and allowed 11 compounds to be identified, of which the major compound was linoleic acid (C18:2), with a similar percentage (between 57.08% and 57.84%) for the three extractions (p > 0.05). Regarding the carotenoid pigment, the extraction technique significantly affected its content (p < 0.05) with values between 10.11 mg/kg and 14.83 mg/kg. The chlorophyll pigment presented a similar content in both oils extracted by SE and UE (p > 0.05), 0.20 mg/kg and 0.16 mg/kg, respectively, while the lowest content was recorded in the cold-pressed oil with 0.13 mg/kg. Moreover, the analysis of phytosterols in walnut oil revealed significantly different contents (p < 0.05) for the three extraction techniques (between 1168.55 mg/kg and 1306.03 mg/kg). In addition, the analyses of tocopherol composition revealed that γ-tocopherol represented the main tocopherol isomer in all studied oils and the CP technique provided the highest content of total tocopherol with 857.65 mg/kg, followed by SE and UE with contents of 454.97 mg/kg and 146.31 mg/kg, respectively, which were significantly different (p < 0.05). This study presents essential information for producers of nutritional oils and, in particular, walnut oil; this information helps to select the appropriate method to produce walnut oil with the targeted quality properties and chemical compositions for the desired purpose. It also helps to form a scientific basis for further research on this plant in order to provide a vision for the possibility of exploiting these oils in the pharmaceutical, cosmetic, and food fields.
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Juglans , Juglans/química , Aceites de Plantas/química , Ácidos Grasos/análisis , Nueces/química , Tocoferoles/análisisRESUMEN
Walnut oil, like all vegetable oils, is chemically unstable because of the sensitivity of its unsaturated fatty acids to the oxidation phenomenon. This phenomenon is based on a succession of chemical reactions, under the influence of temperature or storage conditions, that always lead to a considerable change in the quality of the oil by promoting the oxidation of unsaturated fatty acids through the degradation of their C-C double bonds, leading to the formation of secondary oxidation products that reduce the nutritional values of the oil. This research examines the oxidative stability of roasted and unroasted cold-pressed walnut oils under accelerated storage conditions. The oxidative stability of both oils was evaluated using physicochemical parameters: chemical composition (fatty acids, phytosterols, and tocopherols), pigment content (chlorophyll and carotenoids), specific extinction coefficients (K232 and K270), and quality indicators (acid and peroxide value) as well as the evaluation of radical scavenging activity by the DPPH method. The changes in these parameters were evaluated within 60 days at 60 ± 2 °C. The results showed that the levels of total phytosterols, the parameters of the acid and peroxide value, K232 and K270, increased slightly for both oils as well as the total tocopherol content and the antioxidant activity affected by the roasting process. In contrast, the fatty acid profiles did not change considerably during the 60 days of our study. After two months of oil treatment at 60 °C, the studied oils still showed an excellent physicochemical profile, which allows us to conclude that these oils are stable and can withstand such conditions. This may be due to the considerable content of tocopherols (vitamin E), which acts as an antioxidant.
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Juglans , Fitosteroles , Juglans/química , Antioxidantes/química , Tocoferoles , Aceites de Plantas/química , Ácidos Grasos/química , Vitamina E , Ácidos Grasos Insaturados , Peróxidos , Estrés OxidativoRESUMEN
This study aimed to evaluate the effects of peanut varieties cultivated in Morocco (Virginia and Valencia) and extraction methods (cold press, CP; Soxhlet, Sox and maceration, and Mac) on the fatty acid profile, phytosterol, and tocopherol contents, quality characteristics, and antioxidant potential of peanut seed oil. The DPPH method was used to determine the antioxidant activity of the oils. The results revealed that fatty acid content was slightly affected by the extraction technique. However, the CP method was shown to be an excellent approach for extracting oil with desirable quality features compared to the Sox and Mac methods. Furthermore, the peanut oil extracted via CP carried a higher amount of bioactive compounds and exhibited remarkable antioxidant activities. The findings also revealed higher oleic acid levels from the Virginia oil, ranging from 56.46% to 56.99%. Besides, a higher total phytosterol and tocopherol content and DPPH scavenging capacity were obtained from the Valencia oil. Analyzing the study, it can be inferred that extraction method and variety both affect the composition of the peanut oil's bioactive compounds and antioxidant activity. This information is relevant for extracting peanut oil with a greater level of compounds of industrial interest.
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Antioxidantes , Fitosteroles , Aceite de Cacahuete/química , Antioxidantes/farmacología , Antioxidantes/análisis , Aceites de Plantas/química , Virginia , Tocoferoles/análisis , Ácidos Grasos/química , Vitamina E/análisis , Valor Nutritivo , Fitosteroles/análisis , ArachisRESUMEN
In this work, ZnO, CrZnO, RuZnO, and BaZnO nanomaterials were synthesized and characterized in order to study their antibacterial activity. The agar well diffusion, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) assays were used to determine the antibacterial activity of the fabricated nanomaterials against Staphylococcus aureus ATCC 29213, Escherichia coli ATCC35218, Klebsiella pneumoniae ATCC 7000603, and Pseudomonas aeruginosa ATCC 278533. The well-diffusion test revealed significant antibacterial activity against all investigated bacteria when compared to vancomycin at a concentration of 1 mg/mL. The most susceptible bacteria to BaZnO, RuZnO, and CrZnO were Staphylococcus aureus (15.5 ± 0.5 mm), Pseudomonas aeruginosa (19.2 ± 0.5 mm), and Pseudomonas aeruginosa (19.7 ± 0.5), respectively. The MIC values indicated that they were in the range of 0.02 to 0.2 mg/mL. The MBC values showed that the tested bacteria's growth could be inhibited at concentrations ranging from 0.2 to 2.0 mg/mL. According to the MBC/MIC ratio, BaZnO, RuZnO, and CrZnO exhibit bacteriostatic effects and may target bacterial protein synthesis based on the results of the tolerance test. This study shows the efficacy of the above-mentioned nanoparticles on bacterial growth. Further biotechnological and toxicological studies on the nanoparticles fabricated here are recommended to benefit from these findings.
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Infecciones Estafilocócicas , Staphylococcus aureus , Humanos , Pruebas de Sensibilidad Microbiana , Pseudomonas aeruginosa , Klebsiella pneumoniae , Antibacterianos/farmacología , Escherichia coli , BacteriasRESUMEN
Chalcones have been well examined in the extant literature and demonstrated antibacterial, antifungal, anti-inflammatory, and anticancer properties. A detailed evaluation of the purported health benefits of chalcone and its derivatives, including molecular mechanisms of pharmacological activities, can be further explored. Therefore, this review aimed to describe the main characteristics of chalcone and its derivatives, including their method synthesis and pharmacotherapeutics applications with molecular mechanisms. The presence of the reactive α,ß-unsaturated system in the chalcone's rings showed different potential pharmacological properties, including inhibitory activity on enzymes, anticancer, anti-inflammatory, antibacterial, antifungal, antimalarial, antiprotozoal, and anti-filarial activity. Changing the structure by adding substituent groups to the aromatic ring can increase potency, reduce toxicity, and broaden pharmacological action. This report also summarized the potential health benefits of chalcone derivatives, particularly antimicrobial activity. We found that several chalcone compounds can inhibit diverse targets of antibiotic-resistance development pathways; therefore, they overcome resistance, and bacteria become susceptible to antibacterial compounds. A few chalcone compounds were more active than conventional antibiotics, like vancomycin and tetracycline. On another note, a series of pyran-fused chalcones and trichalcones can block the NF-B signaling complement system implicated in inflammation, and several compounds demonstrated more potent lipoxygenase inhibition than NSAIDs, such as indomethacin. This report integrated discussion from the domains of medicinal chemistry, organic synthesis, and diverse pharmacological applications, particularly for the development of new anti-infective agents that could be a useful reference for pharmaceutical scientists.
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Antiinfecciosos , Antimaláricos , Chalcona , Chalconas , Chalcona/farmacología , Chalconas/farmacología , Chalconas/química , Antifúngicos/farmacología , Vancomicina , Antimaláricos/farmacología , Antiinfecciosos/farmacología , Antiinfecciosos/química , Antibacterianos/farmacología , Antibacterianos/química , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios no Esteroideos/farmacología , Indometacina , Preparaciones Farmacéuticas , Lipooxigenasas , Tetraciclinas , Relación Estructura-ActividadRESUMEN
Traditional medicine is critical in disease treatment and management. Herbs are gaining popularity for disease management and treatment. Therefore, they can be utilised as complementary and alternative treatment (CAT) ingredients. Atopic dermatitis (AD) is one of the common non-communicable diseases. It is characterised by chronic inflammatory skin disease with intense pruritus and eczematous lesions. AD is associated with oxidative stress, microbial infection, and upregulation of inflammatory cytokines. Both children and adults could be affected by this skin disorder. The prevalence of AD is increasing along with the country's level of development. This review revisited the literature on four medicinal herbs widely used as complementary medicine to manage AD. These therapeutic herbs are commonly eaten as food and used as spices in Asian cuisine. The four food herbs reviewed are Cassia alata, Coriandrum sativum, Curcuma longa Linn, and Azadirachta indica. Their traditional uses and phytochemical content will be covered. Four relevant pharmacological and biological activities of the plants crucial in AD management have been reviewed and discussed, including anti-inflammatory, anti-microbial, antioxidant, and wound recovery.
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Azadirachta , Cassia , Terapias Complementarias , Coriandrum , Dermatitis Atópica , Ingredientes Alimentarios , Senna , Curcuma , Dermatitis Atópica/tratamiento farmacológicoRESUMEN
Mirtazapine is a tetracyclic anti-depressant with poor water solubility. The aim of this study was to improve the dissolution rate of mirtazapine by delivering the drug as a liquisolid compact. Central composite design (CCD) was employed for the preparation of mirtazapine liquisolid compacts. In this, the impacts of two independent factors, i.e., excipient ratio (carrier:coating) and different drug concentration on the response of liquisolid system were optimized. Liquisolid compacts were prepared using propylene glycol as a solvent, microcrystalline cellulose as a carrier, and silicon dioxide (Aerosil) as the coating material. The crystallinity of the formulated drug and the interactions between the excipients were examined using X-ray powder diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR), respectively. The dissolution study for the liquisolid compact was carried out as per FDA guidelines. The results showed loss of crystallinity of the mirtazapine in the formulation and was completely solubilized in non-volatile solvent and equally dispersed throughout the powder system. Moreover, drug dissolution was found to be higher in liquisolid compacts than the direct compressed conventional tablets (of mirtazapine). The liquisolid technique appears to be a promising approach for improving the dissolution of poorly soluble drugs like mirtazapine.
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Excipientes , Dióxido de Silicio , Excipientes/química , Mirtazapina , Polvos , Dióxido de Silicio/química , Solubilidad , Solventes/química , Comprimidos/químicaRESUMEN
Leaves, husk, kernels, and bark methanolic extracts of Juglans regia L. were tested for their in vitro antidiabetic, anti-inflammatory, and antioxidant activities. For these purposes, α-amylase and α-glucosidase were used as the main enzymes to evaluate antidiabetic activities. Moreover, lipoxidase and tyrosinase activities were tested to estimate anti-inflammatory properties. Antioxidant properties of Juglans regia L., extracts were determined using three different assays. Leaves extract has an important radical scavenging activity and a-amylase inhibition. Similarly, husk extracts showed high total phenolic content (306.36 ± 4.74 mg gallic acid equivalent/g dry extract) with an important α-amylase inhibition (IC50 = 75.42 ± 0.99 µg/mL). Kernels exhibit significant tyrosinase (IC50 = 51.38 ± 0.81 µg/mL) correlated with antioxidant activities (p < 0.05). Husk and bark extracts also showed strong anti-lipoxidase activities with IC50 equal to 29.48 ± 0.28 and 28.58 ± 0.35 µg/mL, respectively. HPLC-DAD-ESI-MS/MS analysis highlights the phenolic profile of methanolic extracts of Juglans regia L. plant parts. The identified polyphenols were known for their antioxidant, antidiabetic (dicaffeoyl-quinic acid glycoside in kernels), and anti-inflammatory (3,4-dihydroxybenzoic acid in leaves) activities. Further investigations are needed to determine molecular mechanisms involved in these effects as well as to study the properties of the main identified compounds.
Asunto(s)
Antioxidantes , Juglans , Antioxidantes/química , Juglans/química , Hipoglucemiantes/química , Espectrometría de Masas en Tándem , Monofenol Monooxigenasa , Cromatografía Líquida de Alta Presión , Corteza de la Planta/química , Extractos Vegetales/química , Antiinflamatorios/farmacología , Antiinflamatorios/análisis , Fenoles/farmacología , Fenoles/análisis , Hojas de la Planta/química , alfa-AmilasasRESUMEN
Background and Objectives: The Coronavirus disease 2019 (COVID-19) pandemic caused significant disruption to established medical care systems globally. Thus, this study was aimed to compare the admission and outcome variables such as number of patient and its severity, acute recanalisation therapy given pre-post COVID-19 at a primary stroke centre located in Malaysia. Methods: This cross-sectional hospital-based study included adult ischaemic stroke patients. Variables of the study included the number of ischaemic stroke patients, the proportions of recanalisation therapies, stroke severity during admission based on the National Institutes of Health Stroke Scale, functional outcome at discharge based on the modified Rankin Scale, and relevant workflow metrics. We compared the outcome between two six-month periods, namely the pre-COVID-19 period (March 2019 to September 2019) and the COVID-19 period (March 2020 to September 2020). Results: There were 131 and 156 patients, respectively, from the pre-COVID-19 period and the COVID-19 period. The median door-to-scan time and the median door-to-reperfusion time were both significantly shorter in the COVID-19 period (24.5 min versus 12.0 min, p = 0.047) and (93.5 min versus 60.0 min, p = 0.015), respectively. There were also significantly more patients who received intravenous thrombolysis (7.6% versus 17.3%, p = 0.015) and mechanical thrombectomy (0.8% versus 6.4%, p = 0.013) in the COVID-19 period, respectively. Conclusions: The COVID-19 pandemic may not have caused disruptions of acute stroke care in our primary stroke centre. Our data indicated that the number of ischaemic stroke events remained stable, with a significant increase of recanalisation therapies and better in-hospital workflow metrics during the COVID-19 pandemic period. However, we would like to highlight that the burden of COVID-19 cases in the study area was very low. Therefore, the study may not have captured the true burden (and relevant delays in stroke patient management) during the COVID-19 pandemic. The effect of the pandemic crisis is ongoing and both pre-hospital and in-hospital care systems must continue to provide optimal, highly time-dependent stroke care services.
Asunto(s)
Isquemia Encefálica , COVID-19 , Accidente Cerebrovascular , Adulto , Estudios Transversales , Humanos , Malasia/epidemiología , Pandemias , SARS-CoV-2 , Accidente Cerebrovascular/epidemiología , Accidente Cerebrovascular/terapia , Trombectomía , Terapia Trombolítica , Tiempo de Tratamiento , Resultado del TratamientoRESUMEN
BACKGROUND: Artificial Intelligence (AI) plays an important role in many fields, including medical education, practice, and research. Many medical educators started using ChatGPT at the end of 2022 for many purposes. OBJECTIVE: The aim of this study was to explore the potential uses, benefits, and risks of using ChatGPT in education modules on integrated pharmacotherapy of infectious disease. METHODS: A content analysis was conducted to investigate the applications of ChatGPT in education modules on integrated pharmacotherapy of infectious disease. Questions pertaining to curriculum development, syllabus design, lecture note preparation, and examination construction were posed during data collection. Three experienced professors rated the appropriateness and precision of the answers provided by ChatGPT. The consensus rating was considered. The professors also discussed the prospective applications, benefits, and risks of ChatGPT in this educational setting. RESULTS: ChatGPT demonstrated the ability to contribute to various aspects of curriculum design, with ratings ranging from 50% to 92% for appropriateness and accuracy. However, there were limitations and risks associated with its use, including incomplete syllabi, the absence of essential learning objectives, and the inability to design valid questionnaires and qualitative studies. It was suggested that educators use ChatGPT as a resource rather than relying primarily on its output. There are recommendations for effectively incorporating ChatGPT into the curriculum of the education modules on integrated pharmacotherapy of infectious disease. CONCLUSIONS: Medical and health sciences educators can use ChatGPT as a guide in many aspects related to the development of the curriculum of the education modules on integrated pharmacotherapy of infectious disease, syllabus design, lecture notes preparation, and examination preparation with caution.