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The objective of the research was to identify significant variables that impact the porosity-related properties of CaCO3 particles. The Placket-Burman design was employed to screen multiple variables, including pH, molar concentrations of calcium chloride and sodium carbonate, temperature, concentration of Gelucire 44/14, Cremophor RH40, Solutol HS15, Labrasol, mixing rate, reaction time, and order of addition. The response variables were surface area, pore radius, and pore volume. Influential methodologies such as XRD, FTIR, Raman spectroscopy, and TGA were utilized to validate the precipitate type. The BET surface area ranged from 1.5 to 16.14 m2/g, while the pore radius varied from 2.62 to 6.68 nm, and the pore volume exhibited a range of 2.43 to 37.97 cc/gm. Vaterite structures with spherical mesoporous characteristics were observed at high pH, whereas calcite formations occurred at low pH. The order of addition impacted the surface area but did not affect the pore volume. To maximize the surface area, a lower reaction time and molar concentrations of sodium carbonate were found to be advantageous. The pore radius was influenced by the pH, surfactants, and reaction conditions. The sediments were categorized based on the percentage of vaterite formation. The instrumental techniques effectively characterized the precipitates and provided a valuable complementary analysis.
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The master molecular regulators and mechanisms determining longevity and health span include nitric oxide (NO) and superoxide anion radicals (SOR). L-arginine, the NO synthase (NOS) substrate, can restore a healthy ratio between the dangerous SOR and the protective NO radical to promote healthy aging. Antioxidant supplementation orchestrates protection against oxidative stress and damage-L-arginine and antioxidants such as vitamin C increase NO production and bioavailability. Uncoupling of NO generation with the appearance of SOR can be induced by asymmetric dimethylarginine (ADMA). L-arginine can displace ADMA from the site of NO formation if sufficient amounts of the amino acid are available. Antioxidants such as ascorbic acids can scavenge SOR and increase the bioavailability of NO. The topics of this review are the complex interactions of antioxidant agents with L-arginine, which determine NO bioactivity and protection against age-related degeneration.
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Antioxidantes , Óxido Nítrico , Humanos , Óxido Nítrico/metabolismo , Antioxidantes/farmacología , Longevidad , Óxido Nítrico Sintasa/metabolismo , Arginina/metabolismoRESUMEN
Metabolic syndrome is a multifaceted pathophysiologic condition that is largely caused by an imbalance between caloric intake and energy expenditure. The pathogenesis of metabolic syndrome is determined by an individual's genetic/epigenetics and acquired factors. Natural compounds, notably plant extracts, have antioxidant, anti-inflammatory, and insulin-sensitizing properties and are considered to be a viable option for metabolic disorder treatment due to their low risk of side effects. However, the limited solubility, low bioavailability, and instability of these botanicals hinder their performance. These specific limitations have prompted the need for an efficient system that reduces drug degradation and loss, eliminates unwanted side effects, and boosts drug bioavailability, as well as the percentage of the drug deposited in the target areas. The quest for an enhanced (effective) drug delivery system has led to the formation of green-engineered nanoparticles, which has increased the bioavailability, biodistribution, solubility, and stability of plant-based products. The unification of plant extracts and metallic nanoparticles has helped in the development of new therapeutics against metabolic disorders such as obesity, diabetes mellitus, neurodegenerative disorders, non-alcoholic fatty liver, and cancer. The present review outlines the pathophysiology of metabolic diseases and their cures with plant-based nanomedicine.
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Efectos Colaterales y Reacciones Adversas Relacionados con Medicamentos , Enfermedades Metabólicas , Síndrome Metabólico , Nanopartículas del Metal , Nanopartículas , Humanos , Distribución Tisular , Nanopartículas/uso terapéutico , Enfermedades Metabólicas/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéuticoRESUMEN
Cannabidiol (CBD), one of the most promising constituents isolated from Cannabis sativa, exhibits diverse pharmacological actions. However, the applications of CBD are restricted mainly due to its poor oral bioavailability. Therefore, researchers are focusing on the development of novel strategies for the effective delivery of CBD with improved oral bioavailability. In this context, researchers have designed nanocarriers to overcome limitations associated with CBD. The CBD-loaded nanocarriers assist in improving the therapeutic efficacy, targetability, and controlled biodistribution of CBD with negligible toxicity for treating various disease conditions. In this review, we have summarized and discussed various molecular targets, targeting mechanisms and types of nanocarrier-based delivery systems associated with CBD for the effective management of various disease conditions. This strategic information will help researchers in the establishment of novel nanotechnology interventions for targeting CBD.
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Plant fractions have a diversity of biomolecules that can be used to make complicated reactions for the bioactive fabrication of metal nanoparticles (NPs), in addition to being beneficial as antioxidant medications or dietary supplements. The current study shows that Urtica dioica (UD) and biologically synthesized silver nanoparticles (AgNPs) of UD have antibacterial and antioxidant properties against bacteria (Escherichia coli and Pseudomonas putida) and Drosophila melanogaster (Oregon R+). According to their ability to scavenge free radicals, DPPH, ABTS, TFC, and TPC initially estimated the antioxidant potential of UD and UD AgNPs. The fabricated AgNPs were analyzed (UV−Vis, FTIR, EDS, and SEM) to determine the functional groups (alcohol, carboxylic acids, phenol, proteins, and aldehydes) and to observe the shape (agglomerated crystalline and rod-shaped structure). The disc diffusion method was used to test the antimicrobial properties of synthesized Ag-NPs against E. coli and P. putida. For 24 to 120 h, newly enclosed flies and third instar larvae of Drosophila were treated with UD and UD AgNPs. After exposure, tests for biochemical effects (acetylcholinesterase inhibition and protein estimation assays), cytotoxicity (dye exclusion), and behavioral effects (jumping and climbing assays) were conducted. The results showed that nanoparticles were found to have potent antimicrobial activity against all microbial strains tested at various concentrations. In this regard, ethno-medicinal characteristics exhibit a similar impact in D. melanogaster, showing (p < 0.05) significantly decreased cellular toxicity (trypan blue dye), enhanced biochemical markers (AChE efficacy and proteotoxicity), and improved behavioral patterns in the organism treated with UD AgNPs, especially in comparison to UD extract. The results of this study may help in the utilization of specific plants as reliable sources of natural antioxidants that may have been beneficial in the synthesis of metallic NPs, which aids in the production of nanomedicine and other therapeutic applications.
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Visceral leishmaniasis (VL) is one of the most fatal and neglected tropical diseases caused by Leishmania donovani (L. donovani). The applications of currently available chemotherapy (amphotericin B, miltefosine, and others) in VL treatment have been limited due to their poor bioavailability, unfavorable toxicity profile, and prolonged parenteral dosing. Quercetin (QT), a potent natural antioxidant, is a prominent target when conducting investigations on alternative therapies against L. donovani infections. However, the therapeutic applications of QT have been restricted due to its low solubility and bioavailability. In the present study, we developed and evaluated the antileishmanial activity (ALA) of quercetin-loaded nanoemulsion (QTNE) against L. donovani clinical strains. In vitro anti-promastigote assay results demonstrated that QTNE (IC50 6.6 µM, 48 h) significantly inhibited the growth of parasites more efficiently than the pure QT suspension in a dose- and time-dependent manner. Results of the anti-amastigote assay revealed that the infected macrophages (%) of QTNE were significantly more than those of the pure QT suspension at all concentrations (6.6, 26.4, and 52.8 µM; p < 0.05, p < 0.01 compared to the control). Moreover, the results of in vitro and ex vivo studies assisted in determining the mechanistic insights associated with the ALA of QTNE. The overall findings suggested that QTNE exhibited potential ALA by enhancing the intracellular ROS and nitric oxide levels, inducing distortion of membrane integrity and phosphatidylserine release (AV/PI), rupturing the parasite DNA (late apoptosis/necrosis process), and upregulating the immunomodulatory effects (IFN-γ and IL-10 levels). Additionally, QTNE showed superior biocompatibility against all of the treated healthy cells (PBMCs, PECs, and BMCs) as compared to the control. In conclusion, QTNE acts as a potential antileishmanial agent targeting both promastigote and intracellular amastigote forms of L. donovani, which thus opens a new avenue for the use of QTNE in VL therapy.
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Antiprotozoarios , Leishmania donovani , Leishmaniasis Visceral , Animales , Antiprotozoarios/farmacología , Antiprotozoarios/uso terapéutico , Humanos , Leishmaniasis Visceral/tratamiento farmacológico , Leishmaniasis Visceral/parasitología , Ratones , Ratones Endogámicos BALB C , Quercetina/farmacología , Quercetina/uso terapéuticoRESUMEN
Natural antioxidants derived from plants have been proven to have significant inhibitory effects on the free radicals of living organisms during actively metabolization. Excessive production of free radicals increases the risk of neurodegenerative diseases, such as Alzheimer's disease, Parkinson's disease, and motor sclerosis. This study aimed to compare the ethnopharmacological effects of Urtica dioica (UD), Matricaria chamomilla (MC), and Murraya koenigii (MK) on the amelioration of rotenone-induced toxicity in wild-type Drosophila melanogaster (Oregon R+) at biochemical, cellular, and behavioral levels. Phytoextracts were prepared from all three plants, i.e., UD, MC, and MK (aqueous and ethanolic fractions), and their bioactive compounds were evaluated using in vitro biochemical parameters (DPPH, ABTS, TPC, and TFC), UV-Vis, followed by FT-IR and HPLC. Third instar larvae and freshly eclosed flies were treated with 500 µM rotenone alone or in combination with UD, MC, and MK for 24 to 120 h. Following exposure, cytotoxicity (dye exclusion test), biochemical (protein estimation and acetylcholinesterase inhibition assays), and behavioral assays (climbing and jumping assays) were performed. Among all three plant extracts, MK exhibited the highest antioxidant properties due to the highest TPC, TFC, DPPH, and ABTS, followed by UD, then MC. The overall trend was MK > UD > MC. In this context, ethnopharmacological properties mimic the same effect in Drosophila, exhibiting significantly (p < 0.05) reduced cytotoxicity (trypan blue), improved biochemical parameters (proteotoxicity and AChE activity), and better behavioral parameters in the organisms cotreated with phyto extracts compared with rotenone. Conclusively, UV-Vis, FTIR, and HPLC analyses differentiated the plant extracts. The findings of this research may be beneficial in the use of select herbs as viable sources of phyto-ingredients that could be of interest in nutraceutical development and various clinical applications.
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The link between bio-metals, Alzheimer's disease (AD), and its associated protein, amyloid-ß (Aß), is very complex and one of the most studied aspects currently. Alzheimer's disease, a progressive neurodegenerative disease, is proposed to occurs due to the misfolding and aggregation of Aß. Dyshomeostasis of metal ions and their interaction with Aß has largely been implicated in AD. Copper plays a crucial role in amyloid-ß toxicity, and AD development potentially occurs through direct interaction with the copper-binding motif of APP and different amino acid residues of Aß. Previous reports suggest that high levels of copper accumulation in the AD brain result in modulation of toxic Aß peptide levels, implicating the role of copper in the pathophysiology of AD. In this review, we explore the possible mode of copper ion interaction with Aß, which accelerates the kinetics of fibril formation and promote amyloid-ß mediated cell toxicity in Alzheimer's disease and the potential use of various copper chelators in the prevention of copper-mediated Aß toxicity. KEYWORDS: Short Twitter Statement: Authors explore copper ion interaction w/ Aß and kinetics of fibril formation in promoting amyloid-ß mediated cell toxicity in Alzheimer's disease and the potential use of copper chelators in the prevention of copper-mediated Aß toxicity. SHORT TWITTER STATEMENT: Authors explore copper ion interaction w/Aß and kinetics of fibril formation in promoting amyloid-ß mediated cell toxicity in Alzheimer's disease and the potential use of copper chelators in the prevention of copper-mediated Aß toxicity.
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Enfermedad de Alzheimer , Enfermedades Neurodegenerativas , Enfermedad de Alzheimer/tratamiento farmacológico , Enfermedad de Alzheimer/metabolismo , Péptidos beta-Amiloides/metabolismo , Quelantes/química , Quelantes/farmacología , Quelantes/uso terapéutico , Terapia por Quelación , Cobre/metabolismo , Humanos , Metales/químicaRESUMEN
Complementary alternative medicine approaches are growing treatments of diseases to standard medicine practice. Many of these concepts are being adopted into standard practice and orthomolecular medicine. Age-related diseases, in particular neurodegenerative disorders, are particularly difficult to treat and a cure is likely a distant expectation for many of them. Shifting attention from pharmaceuticals to phytoceuticals and "bugs as drugs" represents a paradigm shift and novel approaches to intervention and management of age-related diseases and downstream effects of aging. Although they have their own unique pathologies, a growing body of evidence suggests Alzheimer's disease (AD) and vascular dementia (VaD) share common pathology and features. Moreover, normal metabolic processes contribute to detrimental aging and age-related diseases such as AD. Recognizing the role that the cerebral and cardiovascular pathways play in AD and age-related diseases represents a common denominator in their pathobiology. Understanding how prosaic foods and medications are co-metabolized with the gut microbiota (GMB) would advance personalized medicine and represents a paradigm shift in our view of human physiology and biochemistry. Extending that advance to include a new physiology for the advanced age-related diseases would provide new treatment targets for mild cognitive impairment, dementia, and neurodegeneration and may speed up medical advancements for these particularly devastating and debilitating diseases. Here, we explore selected foods and their derivatives and suggest new dementia treatment approaches for age-related diseases that focus on reexamining the role of the GMB.
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Neurodegeneration is the destruction of neurons, and once the neurons degenerate they can't revive. This is one of the most concerned health conditions among aged population, more than â¼70% of the elderly people are suffering from neurodegeneration. Among all of the neurodegenerative diseases, Alzheimer's disease (AD), Parkinson's disease (PD) and Poly-glutamine disease (Poly-Q) are the major one and affecting most of the people around the world and posing excessive burden on the society. In order to understand this disease in non-human animal models it is pertinent to examine in model organism and various animal model are being used for such diseases like rat, mice and non-vertebrate model like Drosophila. Drosophila melanogaster is one of the best animal proven by several eminent scientist and had received several Nobel prizes for uncovering mechanism of human related genes and highly efficient model for studying neurodegenerative diseases due to its great affinity with human disease-related genes. Another factor is also employed to act as therapeutic or preventive method that is nutraceuticals. Nutraceuticals are functional natural compounds with antioxidant properties and had extensively showed the neuroprotective effect in different organisms. These nutraceuticals having antioxidant properties act through scavenging free radicals or by increasing endogenous cellular antioxidant defense molecules. For the best benefit, we are trying to utilize these nutraceuticals, which will have no or negligible side effects. In this review, we are dealing with various types of such nutraceuticals which have potent value in the prevention and curing of the diseases related to neurodegeneration.HighlightsNeurodegeneration is the silently progressing disease which shows its symptoms when it is well rooted.Many chemical drugs (almost all) have only symptomatic relief with side effects.Potent mechanism of neurodegeneration and improvement effect by nutraceuticals is proposed.Based on the Indian Cuisine scientists are trying to find the medicine from the food or food components having antioxidant properties.The best model to study the neurodegenerative diseases is Drosophila melanogaster.Many nutraceuticals having antioxidant properties have been studied and attenuated various diseases are discussed.
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Enfermedades Neurodegenerativas , Anciano , Animales , Antioxidantes/uso terapéutico , Suplementos Dietéticos , Modelos Animales de Enfermedad , Drosophila , Drosophila melanogaster , Humanos , Ratones , Enfermedades Neurodegenerativas/tratamiento farmacológico , RatasRESUMEN
Tuberculosis (TB) is a recurrent and progressive disease, with high mortality rates worldwide. The drug-resistance phenomenon of Mycobacterium tuberculosis is a major obstruction of allelopathy treatment. An adverse side effect of allelopathic treatment is that it causes serious health complications. The search for suitable alternatives of conventional regimens is needed, i.e., by considering medicinal plant secondary metabolites to explore anti-TB drugs, targeting the action site of M. tuberculosis. Nowadays, plant-derived secondary metabolites are widely known for their beneficial uses, i.e., as antioxidants, antimicrobial agents, and in the treatment of a wide range of chronic human diseases (e.g., tuberculosis), and are known to "thwart" disease virulence. In this regard, in silico studies can reveal the inhibitory potential of plant-derived secondary metabolites against Mycobacterium at the very early stage of infection. Computational approaches based on different algorithms could play a significant role in screening plant metabolites against disease virulence of tuberculosis for drug designing.
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AIMS: Isoformononetin (IFN), a methoxyl isoflavone present in most of human dietary supplements. However, being a highly potent antioxidant and anti-inflammatory molecule, its activity against neuronal oxidative stress and neuroinflammation has not been explored till now. The present study was inquested to assess the antioxidant, anti-apoptotic and anti-inflammatory activity of IFN against streptozotocin induced neuroinflammation in different brain regions of rat. MAIN METHODS: Four groups of animals were subjected to treatment as control, toxic control (STZ; single intracerebrovascular injection), third group (STZ + IFN; 20 mg/kg p.o.), fourth group (IFN) for 14 days. The different brain regions of rats were evaluated for inflammatory, apoptotic and biochemical antioxidant markers. The brain tissues were further assessed for gene expression, immunohistochemical and western blotting examination for localization of inflammasome cascade expression that plays a pivotal role in neuroinflammation. KEY FINDINGS: The modulation in oxidant/antioxidant status after exposure of STZ was significantly balanced after administration of IFN to rats. Further, IFN was also found to be an apoptotic agent as it modulates the apoptotic gene (Bax) and anti-apoptotic gene (BcL2) expression. IFN significantly curtailed the augmented protein expression of NLRP3, NLRP2, ASC, NFκBP65, IL-1ß and caspase-1 due to STZ administration in cortex and hippocampus rat brain regions. SIGNIFICANCE: The aforementioned results proclaim the neuroprotective functioning of IFN against STZ induced inflammation. IFN significantly prevents the neuroinflammation by decreasing the generation of ROS that reduces the activation of NLRP3/ASC/IL-1 axis thereby exerting neuroprotection as evidenced in rat model of STZ induced neuroninflammation.
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Antioxidantes/farmacología , Proteínas Adaptadoras de Señalización CARD/metabolismo , Encefalitis/prevención & control , Interleucina-1/metabolismo , Isoflavonas/farmacología , Proteína con Dominio Pirina 3 de la Familia NLR/metabolismo , Estreptozocina/toxicidad , Animales , Modelos Animales de Enfermedad , Encefalitis/inducido químicamente , Encefalitis/metabolismo , Encefalitis/patología , Expresión Génica/fisiología , Interferones/fisiología , Peroxidación de Lípido/efectos de los fármacos , Óxido Nítrico/biosíntesis , Estrés Oxidativo/efectos de los fármacos , Conejos , Ratas , Ratas Sprague-Dawley , Especies Reactivas de Oxígeno/metabolismo , Transducción de Señal , Factor de Necrosis Tumoral alfa/metabolismoRESUMEN
Oxidative stress, the imbalance of the antioxidant system, results in an accumulation of neurotoxic proteins in Alzheimer's disease (AD). The antioxidant system is composed of exogenous and endogenous antioxidants to maintain homeostasis. Superoxide dismutase (SOD) is an endogenous enzymatic antioxidant that converts superoxide ions to hydrogen peroxide in cells. SOD supplementation in mice prevented cognitive decline in stress-induced cells by reducing lipid peroxidation and maintaining neurogenesis in the hippocampus. Furthermore, SOD decreased expression of BACE1 while reducing plaque burden in the brain. Additionally, Astaxanthin (AST), a potent exogenous carotenoid, scavenges superoxide anion radicals. Mice treated with AST showed slower memory decline and decreased depositions of amyloid-beta (Aß) and tau protein. Currently, the neuroprotective potential of these supplements has only been examined separately in studies. However, a single antioxidant cannot sufficiently resist oxidative damage to the brain, therefore, a combinatory approach is proposed as a relevant therapy for ameliorating pathological changes in AD.
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Enfermedad de Alzheimer/tratamiento farmacológico , Enfermedad de Alzheimer/etiología , Superóxido Dismutasa/farmacología , Enfermedad de Alzheimer/metabolismo , Animales , Antioxidantes/metabolismo , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Biomarcadores , Estudios Clínicos como Asunto , Suplementos Dietéticos , Manejo de la Enfermedad , Susceptibilidad a Enfermedades , Evaluación Preclínica de Medicamentos , Humanos , Neuronas/efectos de los fármacos , Neuronas/metabolismo , Estrés Oxidativo/efectos de los fármacos , Especies Reactivas de Oxígeno/metabolismo , Superóxido Dismutasa/metabolismo , Superóxido Dismutasa/uso terapéutico , Resultado del Tratamiento , Xantófilas/metabolismo , Xantófilas/farmacología , Xantófilas/uso terapéuticoRESUMEN
One of the major challenges of medical sciences has been finding a reliable compound for the pharmacological treatment of Alzheimer's disease (AD). As most of the drugs directed to a variety of targets have failed in finding a medical solution, natural products from Ayurvedic medicine or nutraceutical compounds emerge as a viable preventive therapeutics' pathway. Considering that AD is a multifactorial disease, nutraceutical compounds offer the advantage of a multitarget approach, tagging different molecular sites in the human brain, as compared with the single-target activity of most of the drugs used for AD treatment. We review in-depth important medicinal plants that have been already investigated for therapeutic uses against AD, focusing on a diversity of pharmacological actions. These targets include inhibition of acetylcholinesterase, ß-amyloid senile plaques, oxidation products, inflammatory pathways, specific brain receptors, etc., and pharmacological actions so diverse as anti-inflammatory, memory enhancement, nootropic effects, glutamate excitotoxicity, anti-depressants, and antioxidants. In addition, we also discuss the activity of nutraceutical compounds and phytopharmaceuticals formulae, mainly directed to tau protein aggregates mechanisms of action. These include compounds such as curcumin, resveratrol, epigallocatechin-3-gallate, morin, delphinidins, quercetin, luteolin, oleocanthal, and meganatural-az and other phytochemicals such as huperzine A, limonoids, azaphilones, and aged garlic extract. Finally, we revise the nutraceutical formulae BrainUp-10 composed of Andean shilajit and B-complex vitamins, with memory enhancement activity and the control of neuropsychiatric distress in AD patients. This integrated view on nutraceutical opens a new pathway for future investigations and clinical trials that are likely to render some results based on medical evidence.
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Enfermedad de Alzheimer/dietoterapia , Enfermedad de Alzheimer/prevención & control , Suplementos Dietéticos , Fitoquímicos/uso terapéutico , Enfermedad de Alzheimer/metabolismo , Animales , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Humanos , Ovillos Neurofibrilares/efectos de los fármacos , Ovillos Neurofibrilares/metabolismo , Fitoquímicos/farmacología , Resultado del TratamientoRESUMEN
The joint attack on the body by metabolic acidosis and oxidative stress suggests that treatment in degenerative diseases, including Alzheimer's disease (AD), may require a normalizing of extracellular and intracellular pH with simultaneous supplementation of an antioxidant combination cocktail at a sufficiently high dose. Evidence is also accumulating that combinations of antioxidants may be more effective, taking advantage of synergistic effects of appropriate antioxidants as well as a nutrient-rich diet to prevent and reverse AD. This review focuses on nutritional, nutraceutical and antioxidant treatments of AD, although they can also be used in other chronic degenerative and neurodegenerative diseases.
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Enfermedad de Alzheimer/tratamiento farmacológico , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Dieta , Suplementos Dietéticos , Sinergismo Farmacológico , Humanos , Estrés Oxidativo/efectos de los fármacosRESUMEN
Alzheimer's disease (AD) is the most common progressive human neurodegenerative disorder affecting elderly population worldwide. Hence, prevention of AD has been a priority of AD research worldwide. Based on understanding of disease mechanism, different therapeutic strategies involving synthetic and herbal approaches are being used against AD. Among the herbal extract, Ginkgo biloba extract (GBE) is one of the most investigated herbal remedy for cognitive disorders and Alzheimer's disease (AD). Standardized extract of Ginkgo biloba is a popular dietary supplement taken by the elderly population to improve memory and age-related loss of cognitive function. Nevertheless, its efficacy in the prevention and treatment of dementia remains controversial. Specifically, the added effects of GBE in subjects already receiving "conventional" anti-dementia treatments have been to date very scarcely investigated. This review summarizes recent advancements in our understanding of the potential use of Ginkgo biloba extract in the prevention of AD including its antioxidant property. A better understanding of the mechanisms of action of GBE against AD will be important for designing therapeutic strategies, for basic understanding of the underlying neurodegenerative processes, and for a better understanding of the effectiveness and complexity of this herbal medicine.
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Enfermedad de Alzheimer/tratamiento farmacológico , Antioxidantes/uso terapéutico , Enfermedades del Sistema Nervioso/tratamiento farmacológico , Fármacos Neuroprotectores/uso terapéutico , Extractos Vegetales/uso terapéutico , Anciano , Animales , Ginkgo biloba , Humanos , Resultado del TratamientoRESUMEN
Ulcer is one of the most common diseases affecting throughout the world population. The allopathic treatment of ulcer adversely affects the health by causing harmful side effects. Currently, many herbal plants and secondary metabolites have been used for the ulcer treatment. In the present review, many herbal plants and their parts (root, rhizome, bark, leaves and fruits) have been listed in the table are currently being used for ulcer treatment. These metabolites are responsible for ulcer-neutralization or anti-inflammatory properties. In silico study, plant metabolites showed interaction between protodioscin (secondary metabolites of Asparagus racemosus) and interferon-γ (virulent factor of gastric ulcer) during molecular docking. All the residues of interferon-γ exhibited hydrophobic interactions with plant metabolites. These interactions helps in understanding the plant secondary metabolites vis a vis will open a new door in the research field of new drug discovery and designing for the ulcer treatment.
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The present study aimed for in vitro-in vivo-in silico simulation studies of experimentally designed (32-factorial) Capmul PG-8-cored, Eudragit RSPO-Lutrol F 127 nanocapsules to ferry felodipine using GastroPlus™. The in silico parameter sensitivity analysis for pharmacokinetic parameters was initially assessed to justify the preparation of felodipine-loaded nanocapsules (FLNs) with enhanced solubility to overcome the bioavailability issues of felodipine. The overall integrated desirability ranged between 0.8187 and 0.9488 for three optimized FLNs when analyzed for mean particle size, zeta potential, encapsulation efficiency, and in vitro dissolution parameters. The morphological evaluation (SEM, TEM, and AFM) demonstrated spherical nanoparticles (200-300 nm). Validated LC-MS/MS analysis demonstrated enhanced relative bioavailability (13.37-fold) of optimized FLN as compared to suspension. The simulated regional absorption of the FLN presented significant absorption from the cecum (26.3%) and ascending colon (20.1%) with overall absorption of 67.4% from the GIT tract. Furthermore, in vitro-in vivo correlation demonstrated the Wagner-Nelson method as the preferred model as compared to mechanistic and numerical deconvolution on the basis of least mean absolute prediction error, least standard error of prediction, least mean absolute error, and maximum correlation coefficient (r 2 = 0.920). The study demonstrated enhanced oral absorption of felodipine-loaded nanocapsules, and GastroPlus™ was found to be an efficient simulation tool for in vitro-in vivo-in silico simulations.
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Felodipino/sangre , Felodipino/química , Nanocápsulas/química , Administración Oral , Animales , Antiarrítmicos/sangre , Antiarrítmicos/química , Disponibilidad Biológica , Evaluación Preclínica de Medicamentos/métodos , Tamaño de la Partícula , Ácidos Polimetacrílicos/química , Ácidos Polimetacrílicos/metabolismo , Ratas , Ratas Sprague-Dawley , Espectrometría de Masas en Tándem/métodosRESUMEN
BACKGROUND: Mental disorders are the most common health problems in the worldwide population. Current medicines against these conditions have undesired side effects or limited effectiveness. These disadvantageous pharmacological and therapeutic characteristics provoke a low adherence to treatment in an important percentage of patients with mental disorders. Since ancient times, ethnically different groups have been using plants extracts as medicines for the treatment of mental conditions including dementia, depression and anxiety disorders. Among them are extracts of Ginkgo biloba, a tree in the division Gingophyta, that has been used by millions of people worldwide. OBJECTIVE: This review aims to discuss current scientific evidence of efficacy, neuroprotective and antioxidant effects as mechanism of action, side effects and potential interaction with other commonly prescribed anxiolytic drugs. METHODS: A PubMed search of preclinical studies as well as individual clinical trials and meta-analysis were scrutinized. RESULTS: Various preclinical and clinical studies have shown a positive effect of Ginkgo biloba to improve cognitive abilities in impaired individuals and reducing anxiety under pathological conditions. CONCLUSION: A more advanced clinical research is needed to confirm the efficacy of Gingko biloba for the treatment of anxiety in different health conditions.